bluuebunny/crossref_metadata_2025 huggingface dataset:
Formulation and in vitro Evaluation of Gastroretentive Drug Delivery System for Ranitidine Hydrochloride
Authors: Janardhan Dumpeti , Lingam Meka , Krishna Mohan Chinnala , Venkateswarlu Vobalaboina
Published: August 2020

The purpose of this investigation was to prepare a gastroretentive drug delivery system of ranitidine hydrochloride. Currently, floating tablets are one of the important categories of drug delivery systems with gastric retentive behavior. Ranitidine is a H2 blocker and absorbed from the upper part of GIT and hence there is need to develop a dosage form that releases the drug in stomach so that it can be absorbed from upper part of GIT leading to improved bioavailability. Six different gastroretentive tablets of ranitidine HCl were prepared by direct compression using different concentrations of Hydroxy propyl methyl cellulose (HPMC K4M), Carbopol, Sodium carboxy methyl cellulose, sodium bicarbonate and citric acid. The formulations were coded as HE1, HE2, HC1, HC2, HEC1 and HEC2. The formulations were evaluated for pharmacopoeial quality control tests and all the physical parameters evaluated for quality control were within the acceptable limits of Pharmacopoeia. All the formulations were subjected to in vitro drug release study and compared with that of marketed formulation. The floating lag time of the prepared formulations is good except for one formulation (HC1) and the floating time for all the formulations was >12 hours except HC1 which does not float at all. In conclusion, effervescent is essential for the formulation to have good floating property and carbopol retards the drug release in floating formulations. The statistical analysis of the parameters dissolution efficiency of dissolution data, floating behavior and drug content after storage at 40°C and 75% RH for three months showed no significant change by Student’s t-test indicating that formulation (HEC1) could provide a minimum shelf life of 2 years.
Preparation of Rapidly Disintegrating Glipizide Tablets by Surface Solid Dispersion through Superdisintegrants
Authors: M. Aly Adel
Published: August 2020

The objective of this investigation was to enhance the dissolution of glipizide using solid dispersions containing different superdisintegrants and to prepare rapidly disintegrating glipizide tablets with rapid absorption through the oral cavity by direct compression of the prepared solid dispersion. Primojel, Ac-Di-Sol and Kollidon CL were used as superdisintegrants. These excipients were used in different ratios and by using solvent evaporation method, rapidly disintegrating glipizide tablets were prepared by direct compression of the prepared solid dispersion, as well as, by camphor sublimation method aiming for more enhancing of tablet disintegration. Glipizide loaded with Kollidon CL showed the best dissolution properties compared to the other tested excipients. The physical properties of all the prepared GZ tablet formulations were found to be acceptable according to USP/NF2002. Kollidon CL containing formulations showed the most rapid disintegration time values reaching one second in tablets prepared by camphor sublimation method. The most effective formula in decreasing the blood glucose level was that containing glipizide loaded with Kollidon CL, with significant difference from the physically mixed ingredients or the pure GZ powder depending on Student’s T-test for area above the blood glucose level.
Design and Charecterization of Anticancer Engineered Resealed Erythrocytes
Authors: Doijad R. C. , Deshmukh N. V. , Bhambere D. S. , Joseph Rony , Manvi F. V.
Published: August 2020

A number of investigators have been focusing their attention on the encapsulation of antineoplastic drugs within erythrocytes to diminish their side effects. In this study, human erythrocytes have been loaded by methotrexate (MTX) as a model drug using hypotonic hemolysis method for targeted delivery of this drug. A series of in vitro tests have been carried out to characterize the carrier cells in vitro, including loading parameters, hemoglobin release kinetics, particle size distribution, SEM analysis, osmotic and turbulence fragilities. Carrier erythrocytes having acceptable loading parameters, released their drug content according to zero-order kinetics. Mean corpuscular hemoglobin content values of the cells decreased, the apparent cell sizes measured using dynamic laser scattering, were not significantly different from normal erythrocytes, but the real sizes, measured using SEM, and surface topologies were quite different between loaded and unloaded cells. The MTX-loaded cells were remarkably more fragile compared to the normal cells. Drug loaded erythrocytes showed preferential drug targeting to liver followed by lungs, kidney and spleen. Totally, MTX-loaded erythrocytes seem to be a promising delivery system for targeting the drug to reticuloendothelial system (RES).
Lamivudine Liposomes for Transdermal Delivery - Formulation, Characterization, Stability and In vitro Evaluation
Authors: Pai S. Roopa , Devi V. Kusum
Published: August 2020

: Lamivudine, an antiretroviral is commonly used in the treatment of HIV infections. Upon oral administration, it exhibits dose dependent toxic effects such as hepatotoxicity, hyperglycemia, hyperlipidemia, lactic acidosis, lipodystropy, osteonecrosis. These side effects often require dosage reduction or even cessation of treatment. Thus, the problems associated with oral administration led us to explore the possibilities of designing novel drug delivery system for lamivudine with an alternative route of administration. In the present study, liposomes of lamivudine were prepared by thin film hydration and their potential for transdermal drug delivery has been evaluated in vitro. In the preparation of liposomes, process and formulation parameters were standardized. Liposomes were evaluated for their physicochemical properties such as appearance, particle size, particle size distribution and drug entrapment. Liposomes stored at lower temperature conditions, retained 96 % of the incorporated drug. Residual solvents in the formulation were determined by Gas Chromatography and content of lipids was estimated by Stewart assay. Permeation studies of liposomal formulations were carried out across rat abdominal skin using modified Franz diffusion cells. The lamivudine liposomes with good stability and appreciably controlled skin permeation with minimal retention of drug in the skin were successfully prepared
Formulation and Evaluation of Orally Disintegrating Tablets of Buspirone
Authors: K Rajitha , Y Shravan Kumar , D Adukondalu , Gannu Ramesh , Y Madhusudan rao
Published: August 2020

Buspirone is a classical anxiolytic agent. The present investigation deals with formulation of orodispersible tablets (ODT) of buspirone that disintegrate in the oral cavity upon contact with saliva and thereby should improve therapeutic efficacy.
Development of New Delivery Strategies to Increase Bioavailability of Curcumin
Authors: Viswanath Guduri , Jithan Aukunuru , Reddy VM
Published: August 2020

Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, Cm) is a natural product which possesses antioxidant, anti-inflammatory and anti-tumor activities. Here, intravenous liposomes or transdermal ointment containing curcumin were formulated for stable systemic delivery of the drug. Intravenous small unilamellar vesicles were prepared using thin film-hydration technique followed by sonication while the ointment was prepared using a fusion technique. Transport across the mice skin was performed so as to select the optimum ointment formulation intended for systemic delivery. Both Pharmacokinetics and Pharmacodynamic (anti-inflammatory effect) studies were performed in rats with the selected ointment and liposomal formulations. The results indicated that both liposomal formulation and transdermal ointment after local administration were effective in achieving positive pharmacodynamic effects although drug levels are not be seen with the currently employed assay methods. The results suggest that both these delivery systems lead to very low systemic levels of the drugs. The present formulations provide improved systemic delivery of curcumin, which has therapeutic potential as an antioxidant and anti-inflammatory.
Synthesis and Pharmacological Activity of Some Substituted Menthone Semicarbazone and Thiosemicarbazone Derivatives
Authors: Verma Krishan , Pandeya S N , Singh U K , Gupta S , Prashant P , Anurag  , Bhardwaj Gautam
Published: August 2020

A series of Menthone semicarbazone and thiosemicarbazone derivatives (3a-h) were synthesized and characterized by their spectral data and screened for anticonvulsant and analgesic activity. Compounds investigated showed significant anticonvulsant and analgesic activity
Evaluation of Glycine max Merill. Seeds for Antiarthritic Activity in Male Wistar Rats
Authors: J Shankaranarayanan , AJM Christina , Betanabhatla Kalyan S , Athimoolam Jagan , K Sundara Saravanan , Mahalingam Balakumar
Published: August 2020

The present study was carried out to evaluate the antiarthritic activity of Glycine max seeds in adjuvant induced arthritis in rats. Antiarthritic activity was assessed based on the paw volume, biochemical parameters, haematological parameters and histological parameters. The changes in the above said parameters were reversed by the G.max seed extract administered at the dose of 60 mg/kg orally. Hence further detailed investigation is required to isolate the compound responsible for the antiarthritic activity
Effect of Polymeric Compositions on Pharmacotechnical Properties of Carvedilol Transdermal Film
Authors: D. Shivhare Umesh , P. Dorlikar Vikrant , P. Bhusari Kishore , B. Mathur Vijay , N. Mirani Bhiku
Published: August 2020

Transdermal films of carvedilol were prepared by using Eudragit RL100  (ERL100) either alone or in combination with Eudragit RS100 (ERS100), hydroxypropyl methylcellulose K 15 LV (HPMC), and ethyl cellulose (EC). The drug release was extended over a period of 24 h from all formulations. The formulation A5 showed 98.33 cumulative % drug releases in 24 h and followed zero order kinetics. The drug transport mechanism was observed to be Fickian. The cumulative % drug diffused through artificial permeation membrane (cellophane A 393) from same formulation was 100.52 % over a 12 h. The mechanism of dug release was governed by Peppas model and the drug diffusion rate followed zero order kinetics. The formulation A5 comprising of polymers ERL 100, ERS 100, EC and   HPMC in 7:1:1:1 ratio fulfills the requirement of good TDDS.
"Aphrodisiac Activity of Roots of Mimosa pudica Linn. Ethanolic Extract in Mice"
Authors: Pande Milind , Pathak Anupam
Published: August 2020

The present study was aimed to investigate the effect ethanolic extract of roots of Mimusa pudica Linn. (Mimosae) on libido of sexually normal Swiss Albino male mice. The suspension of the extract was administered orally at the dose of 100, 250, and 500 mg / kg, to different groups of male mice (n = 6) once a day for seven days. The female albino mice involved in mating were made receptive by hormonal treatment. The general libido and potency were determined and compared with the standard reference drug sildenafil citrate. A change in hormonal parameter like testosterone was evaluated. Oral administration of the extract significantly increased the libido and hormonal levels of testosterone. The most appreciable effect of the extract was observed at the dose of 500 mg/kg. The results indicated that the ethanolic extract of roots of Mimusa pudica Linn. (Mimosae) produced a significant and sustained increase in the aphrodisiac activity of normal male mice, without any adverse effects.
Synthesis of Some New Imidazo[1,2-b] Pyridazines
Authors: M. Sumakanth , Reddy V. Malla , Krishnan V.S.H. , Sastry B.S.
Published: August 2020

Several 2,6-diaryl-imidazo[1,2-b]pyridazines (5 & 7) were prepared from 3-amino-6-aryl-pyridazines (3) which in turn were obtained from the corresponding 6-aryl-pyridazine-3(2H)-ones(1) via., 6-aryl-pyridazin-3(2H)-thiones (2) as intermediates, by a reaction with an appropriate a-halocarbonyl compounds (4) or a-haloacyl carbamates (6) in a suitable solvent at reflux temperature. The resulted products were characterized by their physical, analytical and spectral data.
Dendrimers: The Novel Pharmaceutical Drug Carriers
Authors: Shishu  , Maheshwari Manjul
Published: August 2020

Dendrimers represent a novel class of structurally controlled macromolecules derived from a branches-upon-branches structural motif. These consist of well defined, highly branched moieties that radiate from a central core and are synthesized through a stepwise, repetitive reaction sequence that guarantees complete shells for each generation, leading to formation of monodisperse polymers. The synthetic procedures developed for dendrimer preparation permit nearly complete control over the critical molecular design parameters, such as size, shape, surface/interior chemistry, flexibility, and topology by virtue of which these macromolecules offer diverse applications in drug delivery, solubility enhancement, gene therapy and diagnostic field. This article provides an insight into the structure, synthesis, properties, types and the applications of dendrimers in the bio-medical field.
3D QSAR Studies on Benzoxazoles and Oxazolo-(4, 5-b)pyridines as Anti-fungal agents
Authors: Begum Shaheen , K Satya Parameshwar , G K Ravindra , G Achaiah
Published: August 2020

Benzoxazoles and Oxazolo-[4,5-b]pyridines  have been reported as potent anti-fungal agents. 3D QSAR tools including CoMFA and CoMSIA have been known to be a promising approaches is to correlate structures and activity which further enable the medicinal chemists to design more potent molecules thus curtailing the cost and time in drug research. CoMFA and CoMSIA studies have been carried out on 31 molecules of benzoxazole and oxazolopyridines in order to determine the structural properties required for effective antifungal activity. 26 compounds were evaluated for establishing QSAR model, which was then validated by predicting the activities of five test set molecules. All the molecules were aligned by SYBYL database alignment which led to a best model with q2 value of 0.835, r2=0.976 and r2pred=0.773. This model was further employed to derive CoMSIA models, a best model with steric, electrostatic, hydrophobic and hydrogen bond acceptor indices exhibited q2 = 0.812, r2=0.971 and r2pred=0.81. The models thus obtained from this study can be useful for the design and development of new potential anti-fungal agents.
Development of Stability Indicating Reverse Phase HPLC Method for Aripiprazole from Solid Dosage form
Authors: Nerkar Pankaj , Gide Parag , Chitnis Abhishek , Mahajan Hitendra , Gattani Surendra
Published: August 2020

Aripiprazole is a novel antipsychotic drug, generally used in schizophrenia and known to act as a partial agonist at D2 and 5 –HT2A receptors. Since stability indicating method is required to discriminate between the intact analyte and degradation products, the present work is aimed at performing purposeful degradation of aripiprazole by exposing it to various pH conditions, oxidative conditions, dry heat and sunlight. Also it describes the final method of analysis of aripiprazole from the tablets. The chromatographic analysis was carried out on HiQSil C8 column (250 X 4.6 mm, 5 µm), mobile phase was Acetonitrile: Potassium Phosphate buffer (pH =3, 100 mM), (40:60 V/V); injection volume 100 µL, detection was carried out at λmax 225nm. Flow rate was 1.0 ml/min. The developed stability indicating method for aripiprazole was validated as per International Conference on Harmonization (ICH) guidelines.
Biodegradable Nanoparticles - A Novel Approach for Oral Administration of Biological Products
Authors: Prusty Amiya Kumar , Sahu Susanta Kumar
Published: August 2020

Recent developments in science and technology lead towards miniaturization, touching all the spheres of life starting from automobile industry to pharmaceutical industry. The advances in nanotechnology, helps in preparing nanoparticles containing biologically active proteins, that have all the benefits of nanoparticulate system as well as maintain the stability and activity of the biological preparations against low pH of gastric fluid and action of proteolytic enzymes. The nanoparticle preparation method discussed is ionic gelation between a polycationic and a polyanionic polymer under magnetic stirring. The polymers used for preparation of nanoparticles are biodegradable and hydrophilic. Nanoparticles due to their small size can penetrate through smaller capillaries and are easily taken up by cells that allow efficient drug accumulation at the target sites. Nanoparticles maintained sustained drug release over a period of days or even weeks decreasing the frequency of injection in case of parenteral preparations. By preparing nanoparticles using polycations like chitosan, the tight junctions between epithelial cells are opened making paracellular diffusion feasible. Therefore, the nanosized biological products are much more efficient in reaching the target site than the original proteins or peptides.
Solid Lipid Nanoparticles: A Promising Drug Delivery Technology
Authors: S. Pragati  , S. Kuldeep  , S. Ashok  , M. Satheesh
Published: August 2020

One of the situations in the treatment of disease is the delivery of efficacious medication of appropriate concentration to the site of action in a controlled and continual manner. Nanoparticle represents an important particulate carrier system, developed accordingly. Nanoparticles are solid colloidal particles ranging in size from 1 to 1000 nm and composed of macromolecular material. Nanoparticles could be polymeric or lipidic (SLNs). Industry estimates suggest that approximately 40% of lipophilic drug candidates fail due to solubility and formulation stability issues, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles (SLNs) are important advancement in this area. The bioacceptable and biodegradable nature of SLNs makes them less toxic as compared to polymeric nanoparticles. Supplemented with small size which prolongs the circulation time in blood, feasible scale up for large scale production and absence of burst effect makes them interesting candidates for study. In this present review this new approach is discussed in terms of their preparation, advantages, characterization and special features.
Chitosan Based Nanoparticles in Drug Delivery
Authors: Patel J. K. , N. P. Jivani
Published: August 2020

Nanoparticles have gained considerable attention in recent years as one of the most promising drug delivery systems owing to their unique potentials via combining the different characteristics of hydrophilicity and hydrophobicity with a nanoparticle (e.g., very small size). Several polymeric nanoparticulate systems have been prepared and characterized in recent years, based on both natural and synthetic polymers, each with its own advantages and drawbacks. Among the natural polymers, chitosan has been studied extensively for preparation of nanoparticles.  Chitosan nanoparticles have been reported with different characteristics with respect to drug delivery. This review presents various types of chitosan based nanoparticles in drug delivery.
Stavudine Loaded Microcapsules using various Cellulose Polymers: Preparation and In-Vitro Evaluation
Authors: Padala Narayana R. , Prakash K.  , Bonepally C. S. Reddy , Krishnaveni B.  , Shantakumari K.  , Lakshmi N. M.
Published: August 2020

The objective of the present study was to prepare and characterize the microcapsules for the controlled release of Stavudine using cellulose acetate butyrate (CAB), ethyl cellulose (EC), hydroxy propyl methyl cellulose phthalate (HPMCP). The microcapsules were prepared by solvent evaporation method using acetone and liquid paraffin as a drug dispersion and liquid manufacturing phase, respectively. The prepared microcapsules were characterized for particle size distribution (PSD), percent drug content, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared microcapsules were filled in hard gelatin capsules and kept for accelerated stability study as per ICH guidelines for about 3 months. The prepared microcapsules were spherical and free flowing. The entrapment efficiency was found to be 25-45%. The release of drug from the microcapsules was extended upto 12 hours and more. FTIR and DSC thermo graphs showed stable character of stavudine. Scanning electron microscopic study revealed that then microcapsules were spherical and porous in nature. The release kinetics study revealed that the prepared microcapsules were best fitted to the Higuchi model, first order and followed by Zero order and indicating that the drug release was diffusion controlled. The release was mainly influenced by the type of polymer and its viscosity. The DSC study revealed that there is no drug to polymer interaction and showed the stable character of the drug which was further confirmed by the assay of accelerated stability of microcapsules.
Factors Influencing the Design and Performance of Oral Sustained/Controlled Release Dosage Forms
Authors: Mamidala Ranjith Kumar , Ramana Vamshi , G Sandeep , Lingam Meka , Gannu Ramesh , Yamsani Madhusudan Rao
Published: August 2020

Of all drug delivery systems, oral drug delivery remains the most preferred option for administration for various drugs. Availability of wide variety of polymers and frequent dosing intervals helps the formulation scientist to develop sustained/controlled release products. Oral Sustained release (S.R) / Controlled release (C.R) products provide an advantage over conventional dosage forms by optimizing bio-pharmaceutic, pharmacokinetic and pharmacodynamic properties of drugs in such a way that it reduces dosing frequency to an extent that once daily dose is  sufficient for therapeutic management through uniform plasma concentration providing maximum utility of drug  with reduction in local and systemic side effects and cure or control condition in shortest possible time by smallest quantity of drug to assure greater patient compliance. This review describes the various factors influencing the design and performance of sustained/controlled release products along with suitable illustrations.
Quantification of Intramolecular Hydrogen Bond in Neurotransmitter Dopamine
Authors: Garipelli Nagaraju , RB Sunoj  , Reddy B Madhava , AV Jithan , Runja Chinnalaliah
Published: August 2020

Dopamine is a catecholamine chemically, 3, 4-dihydroxyphenyethylamine. It has intramolecular H-bond (IHB) between the two hydroxyl groups. The energy of intramolecular H-bond might contribute energy in binding of the neurotransmitter with the receptors. Here the IHB in Dopamine is calculated in different levels of theories. The energetics of intramolecular hydrogen bonds is of fundamental importance in biochemistry. In contrast with intermolecular H-bonds, whose enthalpy can be determined by a supermolecular approach, there is no general accepted procedure to determine the enthalpy of an intramolecular H-bond. In this work, different ways for assessing the energetics of intramolecular H-bonds of selected aromatic systems were applied and compared. They include the widely used conformational analysis approach (cis-trans method), a recently proposed isodesmic reaction method, and a new procedure that is designated as the ortho-para method.
Floating Drug Delivery Systems
Authors: Nadigoti Jagadeesh , Shayeda
Published: August 2020

Management of illness through medication is entering a new era in which growing number of novel drug delivery systems are being employed and are available for therapeutic use. Oral sustained release gastro-retentive dosage forms (GRDFs) offer many advantages for drugs with absorption from upper parts of gastrointestinal tract and for those acting locally in the stomach, improving the bioavailability of the medication. Floating Drug Delivery Systems (FDDS) is one amongst the GRDFs used to achieve prolonged gastric residence time. Multiple unit FDDS avoid “all-or-nothing” gastric emptying nature of single unit systems. Apart from the background, formulation aspects and evaluation of FDDS, recent developments are also covered in this review.
Pulsatile Drug Delivery Systems: An Overview
Authors: Parmar Ramesh D. , Parikh Rajesh K. , G. Vidyasagar  , Patel Dhaval V. , Patel Chirag J. , Patel Biraju D.
Published: August 2020

Pulsatile  Drug  Delivery  Systems  are  gaining  a  lot  of  interest  as  they  deliver  the  drug  at  the  right  place  at  the  right  time  and  in  the  right  amount,  thus  providing  spatial  and  temporal  delivery  and  increasing  patient  compliance.  These  systems  are  designed  according  to  the  circadian  rhythm  of  the  body.  The  principle  rationale  for  the  use  of  pulsatile  release  of  the  drugs is where  a  constant  drug  release  is  not  desired.  A  pulse  has  to  be  designed  in  such  a  way  that  a  complete  and  rapid  drug  release  is  achieved  after  the  lag  time.  Various  systems  like  capsular  systems,  osmotic  systems,  single-  and  multiple-unit  systems  based  on  the  use  of  soluble  or  erodible  polymer  coating  and  use  of  rupturable  membranes  have  been  dealt  with  in  the  article.  It  summarizes  the  latest  technological  developments,  formulation  parameters,  and  release  profiles  of  these  systems.  These  systems  are  beneficial  for  the  drugs  having  chronopharmacological  behavior  where  night  time  dosing  is  required,  such  as  anti-arhythmic  and  anti-asthmatic.
Piperine- Review of Advances in Pharmacology
Authors: Singh Amritpal , Duggal Sanjiv
Published: August 2020

Piperine, an alkaloid, is found in Piper longum L. and Piper nigrum L. The plants containing piperine are widely used in Alternative and Complementary Therapies for curing an array of disorders. Piperine obtained from botanical sources is about 98% pure. It is produced in the laboratory for chemical and medical purposes. Piperine is helpful in reducing inflammation, improving digestion, and relieving pain and asthma. It is reported to improve the production of serotonin, it may relieve stomach ulcerations. It improves the bioavailability of other nutritive substances including beta carotene, curcumin, selenium, pyroxidine, glucose, and amino acids. Extensive data has been complied in favour of piperine in a wide range of pharmacological studies. The review analyses recent advances in pharmacology research on piperine.
Design and Development of Metformin HCl Floating Microcapsules using Two Polymers of Different Permeability Characteristics
Authors: Nath Bipul , Nath Lila Kanta , Mazumdar Bhaskar , Sharma Niraj , Sarkar Mrinal
Published: August 2020

The objective of the present investigation was to design a sustained release floating microcapsules of Metformin HCl using two polymers of different permeability characteristics Cellulose acetate butyrate (MW of 16,000) and Eudragit RL100 (MW of 150,000) using the oil-in-oil emulsion solvent evaporation method. Polymers were used separately and in combination (1:1) to prepare different microcapsules using acetone as organic phase. In all batches of microcapsules, the total polymer concentration was kept constant (10%w/w). No significant differences in drug loading in microcapsules made from different polymer were noted. Drug loaded microcapsules were found to float on 0.1M HCl for more than 8 hour. FT-IR study showed no drug polymer interaction. SEM study clearly revealed the smoothness of the spherically shaped particles. All the prepared microcapsules showed higher amount of drug release in phosphate buffer (pH 6.8) as compared to the release in 0.1M HCl (pH 1.2). Evaluation of the release data reveals that microcapsules prepared from RL100, Cellulose acetate butyrate and combination of both the polymers exhibit Higuchi spherical matrix release, followed by first order and zero-order release kinetics. Finally, the drug loaded floating microcapsules were found to be safe, economical and will overcome the drawbacks associated with the drug in conventional tablet form, by reducing plasma drug fluctuations.
Synthesis and Pharmacological Evaluation of New 2-aryl-3, 4-dihydro-4-oxo Quinazolin [2,3-b]-2,3-dihydro-4-phenyl [1,3,4] Thiadiazepines
Authors: Shiva kumar B. , Kalyane Navnath V. , Krishna B. Shivaram , Shireesha B. , Reddy V. M.
Published: August 2020

Three different 3-amino-2-mercaptoquinazolin-4(3H)-ones were prepared from the substituted anthranilic acids. Likewise four different chalcones were also prepared by mixed aldol condensation of four aromatic aldehydes with acetophenone. Each of the 3-amino, 2-mercapto quinazolinones was subjected to a cycloaddition reaction with chalcones, separately by heating under reflux in acetic anhydride. The product obtained in each case has been purified and characterized as the respective 2-aryl-3,4-dihydro-4-oxoquinazolin-[2,3-b]-2,3-dihydro-4-phenyl –1,3,4-thiadiazepine on the basis of  their analytical and spectral data.

            These new fused thiadiazepines were evaluated for their locomotor, anti psychotic and muscle relaxant activities by standard methods using animal models and compared with that of standard employed
In Vitro and In Vivo Evaluation of Hepatoprotective Activity of Gymnema Sylvestre
Authors: Srividya A.R. , Varma Sameer Kumar , Dhanapal S.P , Vadivelan R. , Vijayan P.
Published: August 2020

Leaves of Gymnema sylvestre were extracted by hot and cold maceration.  Qualitative phytochemical analysis of the plant extract showed the presence of majority of compounds like alkaloids, carbohydrates, flavonoids, terpienoids, glycosides, proteins, amino acids, phenolic compounds and tannins..  Among the two extracts, the            hydro- alcoholic extract prepared by the hot maceration has shown high phenol content 6.51 ± 0.231 mg/g, high total favonolid content 89.51 ± 0.100 mg/g. By DPPH method, total antioxidant capacity, reducing power ability of the               hydro-alcoholic extract prepared by hot maceration process was evaluated. The freshly prepared rat hepatocytes were treated with different concentration of hydro-alcoholic extract prepared by the hot maceration process. The antihepatotoxicity produced by the extract at the concentration of 200, 400,600 µg/ml was found effective against the          D – galactosamine-induced hepatotoxicity, where as at the concentration of 800 µg/ml was found to be cytotoxic. A significant increase in the levels of ASAT, ALAT,ALP, total bilirubin, direct bilirubin ( P< 0.001) were observed. The cells were treated with  the hydro-alcoholic extract different extracts of Gymnema sylvestre showed a significant restoration of the altered biochemical parameters towards the normal (P<0.001) when compared to D- galactosamine treated groups and were found to be  dose  dependent.  A similar result was obtained when D- galactosamine intoxicated hepatocytes were treated with silymarin.
Assessment of Bioactivity and Membrane Stabilizing Potential of Cissus multistriata Fruit Extracts
Authors: James Omale , Nnacheta Okafor Polycarp , Irene Ijeh Ifeoma
Published: August 2020

In this study, comparative evaluation of cytotoxicity and membrane stabilizing capacity of the ripe and unripe fruit extracts of Cissus multistriata was carried out. Medicinal plants constitute an important component of flora and are diverse in Nigeria. The pharmacological evaluation of substances from plants is an established method for the identification of lead compounds which lead to the development of novel and safe medicinal agents. Alcoholic extract of Cissus multistriata fruit was screened for cytotoxicity using brine shrimp lethality test. The ripe fruit extract was far less toxic (LC50 =2845.125µg/ml) when both fruits were compared to the reference standard, potassium dichromate­ (LC50=180.147µg/ml) used. The membrane stabilizing activity of the extracts compare favorably with that of Indomethacin, a standard anti-inflammatory drug used with the unripe fruit extract being the highest. This study has demonstrated Cissus multistriata fruit extract is relatively safe for the ethno medicinal and other uses to which it is put.
Xenotransplantation from Transgenic Animals: A Critical Analysis
Authors: JB Omajali
Published: August 2020

The current shortage in human organs has made xenotransplantation a potential source of organ transplant in humans. The use of primates could not provide the needed results in humans as many attempted organ transplants involving primate-to-humans were not so successful. Coupled with this, is their limited number and the fact that they are endangered species. Consequent upon this, transgenic pigs became the candidate of choice with the potential of solving this issue of organ shortage. Apart from having organ identical with humans, they have high reproductive rate and can be efficiently manipulated genetically to obtain desired results in humans. However, there are potential problems which exist with xenotransplantation using transgenic pigs as an alternative source. Currently, most of these problems are being overcome. This will not only reduce the problems of organ shortage but will open a new chapter in xenotransplantation from transgenic animals in the near future. This article discusses the potential benefits of using transgenic animals as a practical solution to human organ transplant. It further points out some of the potential problems of using these animals and how these problems are currently being overcome
An Insight into Herb - Drug Interactions
Authors: Rodda Harish Chandra , Molmoori Raj Kumar , Samala Sujatha , Banala Nagaraj , Ciddi Veeresham
Published: August 2020

Alternative medicine is becoming popular worldwide and this is clearly evident from the rapidly escalating sales figures. The time tested and clinically proven  herbal medicines like St. John’s wort, Ginkgo biloba, Garlic, Ephedra, Echinacea etc., make up most of the world’s market as for as alternative medicine is concerned. In spite of its increasing popularity, global criticism regarding the safety of herbal medicines is gaining importance. The surfacing of the adverse effects/adverse events due to concomitant use of herbs and prescription medicines undermine the safety of herbal medicines. The safety of herbal medicines still remains a daunting task. The herbs like St. John’s wort, Ginkgo biloba, Garlic, Ephedra, Echinacea etc., have been reported to interact pharmacokinetically and pharmacodynamically with several prescription medicines. The available literature also bolsters that concomitant use of herbs and drugs can lead to several adverse effects/adverse events. This article presents most of the significant herb – drug interactions reported till date along with a note on the predicted interactions which may/may not occur. There are certain herb – drug combinations which can produce therapeutic benefit and these beneficial herb – drug combinations are also detailed in this article. This review gives an insight into herb – drug interactions, stressing the need to carryout studies on herb – drug interactions at a faster pace, which can strengthen the concept of herbal medicine
Pharmacokinetics of Moxifloxacin in A 5/6th Nephrectomized Rat Model
Authors: Kothandam Hariprasath , Palaniyappan Venkatesh , Idpuganti Sudheer Babu , Muthusamy Umamaheswari
Published: August 2020

Moxifloxacin (MFLX) is a new 8-methoxyfluoroquinolone derivative with a broad spectrum of antibacterial activity. MFLX at doses of 200 and 400 mg was selected to conduct the pharmacokinetic study and the drug was given orally to control and nephrectomized rats. A 5/6th nephrectomized rat model was used in this study. The drug levels in the plasma were determined using a spectrofluorimetric assay. The pharmacokinetic parameters viz. peak plasma concentration (Cmax) and area under the curve (AUC0-8) of the nephrectomized and control rats were compared. The Cmax for both 200 and 400 mg dose of MFLX in nephrectomized rats showed significant difference(P<0.001) from the control group, which reveals the changes in the Cmax of MFLX in renal failure. The AUC0-8 for both 200 and 400 mg dose of MFLX in nephrectomized rats differ significantly (P<0.001) from sham operated control group, which implies the variation in MFLX availability in altered renal function. The AUC0-8 for 400 mg dose of MFLX in nephrectomized rats differ significantly from 200 mg dose of MFLX in nephrectomized group, which reveals that in higher dose, MFLX shows an abrupt increase in the drug availability in renal failure. It is conclude that preclinical drug monitoring of moxifloxacin in laboratory animals can be performed by using 5/6th nephrectomized rat models for determining the dose of MFLX for kidney failured patients. Various pharmacokinetic parameters determined differed in nephrectomised rats when compared to the control.
Expressions Used In O. Hashimov’s Story “Love”
Authors: Rakhimova Sulur
Published: August 2020

This article discusses the phrases used in O.Hoshimov’s story “Love”. The study of phraseological units in Uzbek linguistics is connected with the name of the doctor of philological sciences, professor, linguist Sh.Rakhmatullayev. A scholar describes phraseological units as follows: A phrase consisting of more than one lexical base is called a phrase (phraseological unit). As the meaning of a phrase develops the amount of phraseological meaning changes.
“Head” Related Phrases In Chinese Language And Their Semantics
Authors: Akimov Tair
Published: August 2020

Everyone knows that phraseological units are the most popular genre of oral folk art, which was formed as a result of life observations of the ancestors. Learning and analyzing Chinese phraseology allow us to better understand the inner world of the Chinese nation. This article reveals and semantically analyzes aspects of the word “head” that are closely related to Chinese culture. The worldview, deep logical thoughts, feelings, superstitions, lifestyle and environment of the Chinese people are described in phraseological expressions in a concise and clear form.

This article discusses the semantics and features of Chinese-language phraseological phrases associated with the word “head”. Chinese-language phrases associated with “head” express meanings such as wisdom and ignorance, process of thinking, cunning,sagacity, and planning. Phraseological units in Chinese linguistics are closely related to practical life and determine such features as philosophical and ideological thinking, logical observation. Taking into account the above, the article provides a comparative analysis of phraseological units related to “head” in Chinese and Uzbek languages. The figurative meanings of the word “head” are being revealed, semantic connections and semantic structure of phrases in the sentence are in the process of learning. Chinese phraseological expressions are poorly studied in Uzbek-Chinese studies. We hope that this work will provide practical assistance to our young people who are learning Chinese.
Results Of A Study Of Special Training Of 16-17 Year Old Players
Authors: Shermukhamedov Aziz Toxirovich
Published: August 2020

In football, the effectiveness of competitive activities depends on a number of factors, among which the special training of the athlete is of great importance. The article explores questions related to the special training of athletes in a football sport. The structure of competition activities of 16-17 year old players has been studied and analyzed through pedagogical methods. Indicators reflecting the specific game endurance and speed-endurance of the teams were studied.
Semantic And Structural Properties Of The Banking And Financial Terminology Of The Uzbek Language
Authors: Shirinova Ekaterina Turakulovna
Published: August 2020

This article discusses information on the study of terminology in Uzbek and world linguistics. Thematic grouping of banking and financial terms, which play an important role in Uzbek language vocabulary, is considered. The author gives the criteria for the distribution of terms into thematic groups, their peculiar properties examples to substantiate the hypothesis. The paradigmatic relations between the terms of this sphere are indicated. A structural analysis of the banking and financial terms of the Uzbek language is carried out.  On the basis of the anthropocentric approach, the role of the human factor in the banking and financial terminology of the Uzbek language is studied. Cognitive metaphors that exist in the terminology are considered.
PENGARUH KEBIJAKAN PROMOSI JABATAN DAN ROTASI PEKERJAAN TERHADAP KINERJA KARYAWAN PEMKOT BANDUNG
Authors: Suparno Asep
Published: August 2020

Tujuan dari penelitian ini adalah untuk mengetahui Pengaruh Kebijakan Promosi Jabatan Dan Rotasi Pekerjaan Terhadap Kinerja Karyawan Pada Pemkot BandungPenelitian ini menggunakan kuisioner dengan skala pengukuran menggunakan skala Likert yang dianalisis menggunakan uji validitas, reabilitas dan analisis jalur menggunakan SPSS 13. Sampel dalam penelitian ini adalah 30 orang pegawai Pemkot Bandung. Hasil penelitian ini menunjukkan variabel kebijakan Promosi jabatan dan rotasi kerja secara positif dan signifikan berpengaruh terhadap kinerja karyawan Pemkot Bandung. Nilai R menunjukkan sebesar 75.3% kebijakan Promosi jabatan dan rotasi kerja berpengaruh terhadap kinerja karyawan. Dengan mengetahui hubungan antara variabel-variabel ini, kebijakan Promosi jabatan dan rotasi kerja dapat digunakan untuk meningkatkan kinerja karyawan pada Pemkot Bandung.
PERAN AUDIT INTERNAL TERHADAP PENGENDALIAN INTERN PENERIMAAN KAS PADA PT INTI (PERSERO) BANDUNG
Authors: Karmana Dedi
Published: August 2020

Penelitian ini bertujuan untuk mengetahui dan mengkajiPenerapan Audit Internal Pada PT INTI (Persero),Pelaksanaan Pengendalian Intern Penerimaan Kas dan Besarnya Pengaruh Audit Internal Terhadap Pengendalian Intern Penerimaan Kas pada PT INTI (Persero).Metode penelitian yang digunakan pada penelitian ini adalah metode kuantitatif. Hasil penelitian, diperoleh nilai rata-rata variabel X (Audit Internal) sebesar 3,40 berada pada kriteria "cukup baik" dan variabel Y (Pengendalian Intern Penerimaan Kas)" sebesar 3,34 berada pada kriteria "cukup balk". Koefisien korelasi diperoleh hubungan yang positif dan signifikan sebesar 0,828 dan termasuk dalam kategori sangat kuat. Artinya terdapat hubungan yang sangat kuat antara Audit Internal terhadap Pengendalian Intern Penerimaan Kas pads PT INTI (Persero). Koefisien determinasi sebesar 0,686 atau 68,6%. Artinya Audit Internal mempengaruhi Pengendalian Intern Penerimaan Kas Sebesar 68,4% sedangkan sisanya 31,4% dipengaruhi oleh faktor lain. Dengan demikian dapat disimpulkan bahwa hipotesi penelitian diterima yaitu "Audit Internal Berpengaruh terhadap Pengendalian Intern Penerimaan Kas".
PENGARUH CAPITAL ADEQUACY RATIO, NON PERFORMING LOAN, LOAN TO DEPOSIT RATIO DAN BIAYA OPERASIONAL PENDAPATAN OPERASIONAL TERHADAP RETURN ON ASSET PADA PT BANK MANDIRI PERIODE 2010-2017
Authors: Djalil Ardinal
Published: August 2020

Masalah keuangan merupakan salah satu masalah yang sangat vital bagi bank dalam perkembangan bisnis suatu perusahaan. Salah satu tujuan utama didirikannya perusahaan adalah untuk memperoleh keuntungan (Profit) yang maksimal, sehingga kinerja keuangan merupakan hal yang penting bagi setiap perusahaan didalam persaingan bisnis untuk mempertahankan perusahaannya dalam memperoleh keuntungan. Penelitian ini bertujuan untuk mengetahui Pengaruh Capital Adequacy Ratio (CAR), Non Performing Loan (NPL), Loan to Deposit Ratio (LDR) dan Biaya Operasional Pendapatan Operasional (BOPO) Terhadap Profitabilitas Return on Asset (ROA) Pada PT Bank Mandiri Periode 2010-2017. Jenis penelitian yang akan digunakan dalam penelitian ini adalah metode penelitian deskriptif dan verifikatif. Hasil penelitian ini menunjukan bahwa (1) Nilai rata-rata CAR sebesar 16,38% (2) Nilai rata-rata NPL sebesar 2,28% (3) Nilai rata-rata LDR sebesar 76,47% (4) Nilai rata-rata BOPO sebesar 68,28% (5) Nilai ROA sebesar 3,23% (6) CAR (X1) berpengaruh tidak signifikan terhadap ROA (Y) sebesar 4,2% (7) NPL (X2) berpengaruh tidak signifikan terhadap ROA (Y) sebesar 1,4% (8) LDR (X3) berpengaruh tidak signifikan terhadap ROA (Y) sebesar 2,91% (9) BOPO (X4) berpengaruh tidak signifikan terhadap ROA (Y) sebesar 9,3% (10) antara CAR (X1), NPL (X2), LDR (X3), BOPO (X4) secara bersama-sama (simultan) memberikan pengaruh signifikan terhadap ROA (Y) PT Bank Mandri periode 2010-2017.
Pengaruh Laba Bersih, Arus Kas Bebas, Dan Arus Kas Operasi Terhadap Dividen Tunai Pada 12 Perusahan Makanan Dan Minuman Yang Terdaftar Di Bursa Efek Indonesia (Periode 2012-2018)
Authors: Djalil Ardinal
Published: August 2020

Abstract : Cash Dividends are the most common type distributed by companies to shareholders. Because cash dividends help reduce the risk of uncertainty in shareholder investment activities. And for companies dividend payments can be used to strengthen the company's position in finding additional funds in the capital market. In determining the amount of dividends to be distributed by management is often faced with a difficult decision. This difficulty is caused by management having to consider paying dividends that are smaller, larger, permanent or stable, because any decision on dividend payments will result in investors acting on the company's shares.

This study aims to analyze the effect of net income, free cash flow and operating cash flow on cash dividends. Data was obtained from companies listed on the Indonesian stock exchange in the period 2010-2016. This research uses descriptive verification research method. The independent variables in this study are Net Income (X1), Free Cash Flow (X2), and Operating Cash Flow (X3) and the dependent variable in this study is Cash Dividend (Y).

The results of the study and discussion show that in partial testing (t-test), obtained from the tcount for Net Profit of 2.727 and tcount for Free Cash Flow of 2.086 is greater than the table of 1.989. For Operating Cash Flow variable has no influence on Cash Dividends. The assessment can be seen from the tcount for Operating Cash Flow of -1.201 smaller than t table 1.989.

Whereas in simultaneous testing (F test), Net Profit (X1), Free Cash Flow (X2) and Operating Cash Flow (X3) simultaneously affect Cash Dividends. The coefficient of determination obtained by 16%, while the remaining 84% is influenced by other factors ignored by the writer in this study.
Konsep tata ruang permukiman Baluwarti Keraton Kasunanan Surakarta
Authors: Hartanto Tri , Yuuwono Abito Bamban
Published: August 2020

Penelitian terkait permukiman sudah banyak dilakukan oleh para ahli baik di dalam negeri maupun di luar negeri. Permukiman sebagai obyek penelitian telah lama dilakukan karena terkait dengan sosial budaya yang berkembang di masyarakat. Penelitian ini memilih lokus permukiman Baluwarti, dan fokus penelitian adalah tata ruang permukimannyaÂ  yang memiliki kekhasan tersendiri. Kekhasan tata ruang permukiman Baluwarti yang dimaksud adalah bahwa permukiman ini berbeda dengan permukiman tradisional lainya karena permukiman ini berada di dalam kawasan keraton Surakarta. Dimana keraton Surakarta dikenal sebagai pusat kebudayaan Jawa. Sehingga permukiman tradisional lainya yang berada di Jawa, tentunya bersumber dari budaya keraton Surakarta. Paradaigma penelitian adalah Kualitatif dangan metode historical reading dan observasi, sedangkan analisis menggunakan induktif. Kebaharuan dari penelitian ini adalah akan ditemukan konsep tata ruang permukiman Baluwarti yang memiliki kekhasan, dari nilai-nilai tradisi dan budaya Keraton Surakarta Hadiningrat yang kaya akan tradisi dan budaya (budaya Jawa), karena berada di dalam kawasan keraton. Berbeda dengan penelitian-penelitian permukiman yang telah dilakukan sebelumnya dengan lokus penelitian berada di luar keraton. Berdasarkan penelitian yang telah dilakukan bahwa konsep tata ruang Baluwarti merupakan konsep yang dipertahankan dari permukiman ini dibangun, yaitu pada masa Paku Buwana III (1745-1788M) adalahÂ  menjaga keharmonisan manusia dengan Tuhan, keharmonisan manusia dengan manusia (masyarakat), dan keharmonisan manusia dengan alam.