bluuebunny/crossref_metadata_2025 huggingface dataset:
СИНТЕТИЧНІ ШКІРИ НА ОСНОВІ ВОДНОГО РОЗЧИНИ ПОЛІУРЕТАНУ ТА ЇХ ФІЗИКО-МЕХАНІЧНІ ВЛАСТИВОСТІ
Authors: ШЕГИНСЬКИЙ О.В. , ДЗЮБИНСЬКИЙ А.В. , ДЗЮБИНСЬКА О.В.
Published: August 2020

Мета. Метою нашого дослідження є оцінка властивостей синтетичних шкір, виготовлених шляхом застосування поліефірного каркасного матеріалу і використання водного розчину поліуретану.
Помітні результати досягнуті в ґалузі виробництва м’яких синтетичних і синтетичних шкір. Синтетичні шкіри добре імітують натуральну шкіру, достатньо м’які, еластичні, мають хороші властивості. До основних недоліків синтетичних шкір слід віднести відсутність належних фізико-механічних властивостей. Дефіцит натуральних шкір, що постійно зростає, призводить до необхідності прискорення розроблення і виробництва синтетичних матеріалів з поліпшеними  властивостями.
Одним із шляхів вирішення цих проблем є застосування нових, екологічно чистих синтетичних шкір з покращеними властивостями. Можливість виробництва таких синтетичних шкір дозволить розширити сучасний асортимент.
Результати. Фізико-механічні властивості синтетичної шкіри визначають її структура та раціональний рецептурний склад є якісними показниками синтетичної шкіри і вказують на підходи щодо регулювання їх властивостей. Результати досліджень синтетичних шкір, одержаних з використанням різних основ, показали наявність необхідних споживних властивостей, що створює умови виробництва широкого асортименту синтетичних шкір з новими наперед заданими споживними властивостями. За результатами експертизи встановлено,   що синтетична шкіра, виготовлена на основі водного розчину поліуретану, відповідає санітарно-гігієнічним вимогам і може використовуватися як у взуттєвій, так і в інших галузях легкої промисловості.
Наукова новизна. Застосування водного розчину поліуретану робить процес виготовлення синтетичних шкір менш трудомісткім та більш економічним (виключаються процеси промивання основи і напівфабрикату від залишків диметилформаміду, а головне процес регенерації водно-диметилформамідної суміші і біологічне очищення стічних вод (який до того ж потребує вартісного обладнання).
Практична значимість. Показники властивостей синтетичної шкіри залежать від обраної основи, лицьового покриття тощо. Одержані результати свідчать про можливість регулювання фізико-механічних  властивостей синтетичної шкіри шляхом зміни співвідношення компонентів.
Effect of Tablet Surface Area and Surface Area/Volume on Drug Release from Lamivudine Extended Release Matrix Tablets
Authors: P Narayana Raju , K Prakash , T Rama Rao , Reddy B.C.S. , V Sreenivasulu , M Lakshmi Narasu
Published: August 2020

The purpose of this study was to investigate the influence of tablet surface area/ volume (SA/Vol) on drug release from extended-release matrix tablets of lamivudine prepared with hydroxy propyl methylcellulose (HPMC). Highly soluble drug such as lamivudine was utilized in this study to give predominantly diffusion-controlled release. Drug release from HPMC matrix tablets with similar values of SA/Vol was comparable within the same tablet shaped tablet. Tablets having the same surface area but different SA/Vol values did not result in similar drug release, tablets with larger SA/Vol values had faster release profiles. Utility of SA/Vol to affect drug release was demonstrated by changing drug doses, and altering tablet shape to adjust SA/Vol. When SA/Vol was held constant, similar release profiles were obtained. Thus, surface area/volume is one of the key variables in controlling drug release from HPMC matrix tablets. Proper use of this variable has practical application by formulators who may need to duplicate drug release profiles from tablets of different sizes and different shapes.
Development of Fast Dissolving Carbamazepine Tablets: Effect of Functionality of Superdisintegrants
Authors: Rao N. G. Raghavendra , Patel Tarun , Kumar Rathan
Published: August 2020

Carbamazepine, a dibenzapine derivative with structure resembling that of tricyclic antidepressants, is used in the treatment of epilepsy. The major problem of this drug is very low solubility in biological fluids and poor bioavailability after oral administration. Carbamazepine fast dissolving tablets (FDT) have been prepared by direct compression method. Effects of superdisintegrants (such as croscarmellose sodium, crospovidone and sodium starch glycolate) on wetting time, disintegrating time, drug content, in vitro release, and stability parameters have been studied. The prepared tablets were characterized by DSC and FTIR Studies. No chemical interaction between drug and excipients was confirmed by DSC and FTIR studies. Disintegration time and dissolution parameters (t50% and t90%) decreased with increase in the level of croscarmellose sodium and crosspovidone, whereas disintegration time and dissolution parameters increased with increase in the level of the sodium starch glycolate in tablets. Among all formulations f8 was considered best. The results concluded that fast dissolving tablets of poorly soluble drug carbamazepine, showing enhanced dissolution, will lead to improved bioavailability, improved effectiveness and hence better patient compliance.
Formulation and In vitro Evaluation of Mucoadhesive Buccal Patches of Ondansetron Hydrochloride
Authors: Shayeda  , Dharani Sathish
Published: August 2020

The goal of the present investigation was to design and evaluate mucoadhesive buccal patches of Ondansetron Hydrochloride (OND) which is used for nausea and vomiting associated with cancer chemotherapy and radiotherapy. Permeation of OND was calculated ex vivo using porcine buccal membrane. Buccal films were developed by solvent-casting technique using Hydroxy Propyl Methyl Cellulose(HPMC E15) as mucoadhesive polymer. The patches were evaluated for weight variation, thickness variation, surface pH, moisture absorption, in vitro residence time, mechanical properties, in vitro release, ex vivo permeation studies and drug content uniformity. The formulation F3 was found to give the better results and obeys first order kinetics.
Rapid Synthesis and Biological/Pharmacological Evaluation of Mannich Bases from Dihydropyrimidinones
Authors: Reddy V M , G Somasekher , B Durgaprasad , T Madhukar Reddy , Dubey P K
Published: August 2020

Twenty new Mannich bases from four different, dihydropyrimidinones using 5 different secondary amines along with either 37% formaldehyde or paraformaldehyde under two different experimental conditions, conventional and micro-wave irradiation were prepared and characterized with the help of their analytical and spectral (IR, 1H NMR and mass) data. Based on the 1H NMR data (disappearance of protons signals at δ 7.24-7.41 characteristic of N3-H) specifically characterized as N3- substituted product and not the alternative N1- substituted. Dihydropyrimidinones on the other hand were prepared by the Biginelli reaction using sulfamic acid as the catalyst, again under two experimental conditions: conventional and MW-irradiation. Sulfamic acid was found to be quite facile for the reaction. The use of paraformaldehyde in place of 37% formaldehyde was also convenient for the Mannich reaction. Assay of compounds for analgesic and anti-bacterial activities revealed their inferior potency when compared to the standard employed.
Formulation and Evaluation of Mucoadhesive Tablet: Influence of Some Hydrophilic Polymers on the Release Rate and In Vitro Evaluation
Authors: Singh S K , Bothara S B , Singh S , Patel R , Dodia R
Published: August 2020

Extending the residence time of a dosage form at a particular site and controlling the release of drug from the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability. The objective of this study was to extend the GI residence time of the dosage form and control the release of Tramadol HCl using mucoadhesive tablet to achieve controlled plasma level of the drug which is especially useful for 12 hrs. Matrix tablets of Tramadol HCl were formulated using different mucoadhesive polymers namely guar gum, xanthan gum and Methocel (HPMC K15M and HPMC K100M). Formulations were evaluated for preformulation parameters, in vitro drug release profile and release kinetics. The formulations were found to have good preformulation characteristics. FTIR spectroscopy indicated the absence of any significant chemical interaction within dug and excipients. The release mechanism of Tramadol HCl from matrix tablets indicated anomalous (non-Fickian) transport mechanism and followed zero order kinetics. The retention time of the mucoadhesive tablet on the mucous membrane were investigated to develop a bioadhesive polymer-based controlled release delivery system and to evaluate the performance of such a delivery devices. The combination of HPMC K15: HPMC K100: Xanthan gum (1:2:1) and HPMC K 100: Xanthan gum (2:2) showed a greater bioadhesive strength as compared to single gum and other hydrophilic polymer combination tablet. The stability studies were performed on optimized formulation as per ICH guideline, result showed that there was no significant change in physical characteristic, adhesive strength and In vitro release.
Synthesis and Biological Evaluation of Novel 4-Ethyl-3-methyl-N-phenyl-3,4- dihydroquinoxalin-2-amine Derivatives"
Authors: Patidar Ashutosh Kumar , C H S Venkataramana , V Madhavan
Published: August 2020

Substituted anilines were reacted with ethyl-2-bromopropionate to give different substituted 2-bromo-N-phenylpropionamides, which were further condensed with o-phenylenediamines to give corresponding 3-methyl-N-phenyl-3,4-dihydroquinoxalin-2-amines. 4-ethyl-3-methyl-N-phenyl-3,4-dihydroquinoxalin-2-amines were synthesized by the N-alkylation of 3-methyl-N-phenyl-3,4

2-bromo-N-phenylpropionamides; 

-dihydroquinoxalin-2-amines using ethyl iodide.
Butea Monosperma (LAM.) Kuntze – A Comprehensive Review
Authors: Mazumder P M , Das M K , Das S
Published: August 2020

The traditional systems of medicine together with folklore medicine continue to play a significant role in our health care system for the betterment of mankind. Butea monosperma (Lam.) kuntze is a commonly used herb in Ayurvedic medicine. Butea monosperma (Palas) belongs to the family Fabaceae, grown wildly in many parts of India. The plant is used highly by the rural and tribal people in curing various disorders. Butea monosperma has an effective natural origin that has a  tremendous future for research. The novelty and applicability of Butea monosperma are hidden. Such things can be overcome through modern scientific research. The present article describes various traditional and medicinal utility of the plant and an attempt was made to gather information about the chemical composition and pharmacological activity of the plant and/ or its constituents.
Pharmacological Activities of Flavonoids: A Review
Authors: Agrawal A D
Published: August 2020

Flavonoids belong to a group of polyphenolic compounds,  Ca+2-ATPase, xanthine oxidase, phosphodiesterase, and which are classified as flavones, flavanones, catechins and lipoxygenase. They also have a regulatory role on different anthocyanins. Flavonoids of different classes have several  hormones like androgens, estrogens and thyroids. In the view pharmacological activities. Flavonoids possess of their wide pharmacological and biological actions, they pharmacological and biochemical effects, which inhibit a seem to have great therapeutic potential. number of enzymes such as aldose reductase, cycloxygenase,
Post–market In vitro Equivalency Evaluation of Paracetamol Tablets in Kedah, Malaysia
Authors: A R Chandrasekaran , Han Chen Yi , Chung Alex Chin Yang , Cheang Lim Wei , Ping Low Sing
Published: August 2020

Six brands of paracetamol (acetaminophen) 500 mg tablets have been evaluated using specific quality control tests for uniformity of weight, hardness, friability, content, disintegration and dissolution with the aim to assess its bioequivalence. The results obtained have been discussed in details using monographs in United States Pharmacopeia and British Pharmacopoeia. In conclusion, despite some apparent minor differences in tablet hardness and disintegration time profiles, the dissolution characteristics of various paracetamol tablets appears to be similar and not significantly different from various manufacturers.
Valsartan Loaded Solid Lipid Nanoparticles: Development, Characterization, and In vitro and Ex vivo Evaluation
Authors: Sahoo Subhashree , Chakraborti C K , Naik S
Published: August 2020

Qualitative analysis of a mucoadhesive polymeric (hydroxypropyl methylcellulose, HPMC) suspension of norfloxacin was carried out with the aim of developing an oral controlled release gastro-retentive dosage form. The characterization of ultrasonicated formulation was performed by Fourier Transform Infrared Spectroscopy (FTIR), Raman spectroscopy, X-ray powder diffraction (XRD) and Scanning electron microscopy (SEM) analyses. For interpretation, FTIR (400-4000 cm-1 region) and Raman (140-2400 cm-1 region) spectra were used. XRD data of pure drug, polymer and the mucoadhesive polymeric suspension were obtained using a powder diffractometer, scanned from a Bragg’s angle (2θ) of 10˚ to 70˚. In addition, dispersion of particle was studied using SEM techniques. The results from FTIR and Raman spectroscopic analyses of the mucoadhesive suspension suggested that carboxylic groups of norfloxacin and hydroxyl groups of HPMC undergo chemical interaction leading to esterification and hydrogen bonding. The XRD data indicated the retention of crystalline nature of norfloxacin in the mucoadhesive suspension. Moreover, the SEM image analysis suggested that in the formulation, maximum particles exhibited network like structure to produce pseudoplastic flow. From our analysis, it may be concluded that it is feasible to prepare a homogeneous, uniformly dispersed, pharmaceutically stable controlled release norfloxacin suspension that has better bioavailability and penetration capacity.
Pharmaceutical Development and Clinical Pharmacokinetic Evaluation of Gastroretentive Floating Matrix Tablets of Levofloxacin
Authors: Rao Y. Madhusudan , Doodipala N , Palem C R , Reddy S
Published: August 2020

The most common approach for achieving sustained drug release is by the use of hydrophilic polymeric excipients directly compressed with active ingredients into tablets. Hydrophilic polymers swell in the presence of water to form hydrogel structures from which drugs are released by slow diffusion. The purpose of this study was to prepare a floating drug delivery system of levofloxacin, a fluoroquinolone antibiotic.  Levofloxacin is highly soluble in acidic media and precipitates in alkaline media, thereby losing its solubility. We designed a gastroretentive system of levofloxacin to enhance bioavailability by retaining them in the acidic environment of the stomach. Tablets were prepared by the direct compression technique using polymers such as hydroxypropyl- methylcellulose (HPMC K4M, HPMC K15M, and HPMC K100M). Sodium bicarbonate was utilized as a gas-generating agent. Tables were evaluated for their physical characteristics such as hardness, thickness, friability, weight variation, drug content, swelling studies, and floating properties. Tablet formulations were evaluated by in vitro dissolution studies. Formulations showed a floating lag time of 30 seconds and a floating time above 12 hours. Among these formulations F3, F7 and F11 exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. The best formulation (F3) was selected based on in vitro characteristics and further tested in healthy volunteers by radiographic studies of tablets by incorporating BaSO4. These clinical studies revealed that the tablets remained in the stomach for 240 ± 30 minutes in fasting human volunteers, indicating gastric retention of the system.
Development and Evaluation of Novel Floating Drug Delivery Systems of Metoclopramide Hydrochloride
Authors: Wamorkar Vinay , Samar A , Reddy A , Ch Anusha , Saikrishna C V , N Santoshkumar
Published: August 2020

Several distinct novel drug delivery systems are being employed for effective delivery of medications to patients. Oral delivery is by far the most preferable route of drug delivery and oral sustained-release gastroretentive drug delivery systems offer several advantages. These drug delivery systems are beneficial for drugs with absorption from the upper parts of the gastrointestinal tract and for those acting locally in the stomach, improving the bioavailability of these drugs. Floating drug delivery systems (FDDS) are one of the gastroretentive drug delivery systems used to achieve prolonged gastric residence time. Multiple unit FDDS avoid the “all-or-none” gastric emptying nature of single unit systems. In the present research study, floating formulation as solid (capsule) or liquid (in situ gel) drug delivery systems were developed for improving the gastric residence time of the anti-emetic agent metoclopramide hydrochloride. Floating capsules were prepared using combinations of various natural and synthetic polymers. Simultaneously, in situ gel was prepared using completely bio-degradable natural polymers. Both systems were able to sustain drug release for up to 8 hours. These formulations were compared with marketed forms and found to be more convenient from a patient as well as a biopharmaceutical standpoint. To assess the stability of these formulations, accelerated stability testing was conducted as per ICH guidelines. Both formulations were found to be stable upon completion of the accelerated stability period.
"A New RP-HPLC Method for the Simultaneous Determination of Drotaverine Hydrochloride and Paracetamol in a Tablet Dosage Form"
Authors: Vyas A J , Patel J K , Chavda J V , A Bhandari
Published: August 2020

A simple, precise, and accurate isocratic RP-HPLC method was developed and validated for determination of Drotaverine hydrochloride (DROT) and paracetamol (PCM) in bulk drug and tablet formulations. Isocratic RP-HPLC separation was achieved on a Varian Microsorb mv C18 column (250 4.6 mm id, 5 mm particle size) using the mobile phase acetonitrile: water: triethylamine (TEA) (55:45:0.3%) with the pH adjusted to 3.5 and orthophosphoric acid at a flow rate of 1.6 ml/min. The retention time of DROT and PCM were 3.2713 and 1.5735 minutes, respectively. The detection was performed at 230 nm and samples of 20 µl were manually injected. The method was validated for linearity, precision, accuracy, robustness, and specificity. The method was found to be linear in the concentration range of 2-16 µg/ml with a correlation coefficient of 0.9997 for DROT and 12.5-100 µg/ml with a correlation coefficient of 0.9992 for PCM. The Calculated Limit of detection (LOD) and Limit of Quantitation (LOQ) for DROT were 0.0872 and 0.2644 µg/ml, respectively, and for PCM 0.2965 and 0.8984 µg/ml, respectively. The accuracy (recovery) was found to be in the range of 99.13%-101.52% with RSD of 1.194% for DROT and 99.09%-100.33% for PCM with RSD of 1.096%.
Cytotoxic, Antioxidant and Antimicrobial Activity of Polygonum Chinensis Linn
Authors: A.R. Srividya , Shalom A , R Chandrasekhar , P Vijayan , Vishnuvarthtan V.J
Published: August 2020

Polygonum chinensis linn belongs to the family Polygonaceae. The plant used in this study was shade dried and extracted with methanol by a cold maceration process. Qualitiave phytochemicals estimation showed the presence of the majority of compounds including terpinoids, flavonoids, tannins, saponins and glycosides. All the extracts showed moderate inhibition ranged from 12- 14 mm against both Gram-positive and Gram-negative strains and 00-21 mm against fungal trains.  In the two-fold serial dilution method, the minimum inhibitory concentration of the extract ranges between 250 – >1000 µg/ml.  The leaf extract of polygonum chinensis showed the potent activity with an IC50 value of 18.59 ± 0.356 µg/ml. In DPPH, the lipid peroxidation and hydrogen peroxide method, the leaf extract showed potent antioxidant activity. Root and stem extract showed moderate antioxidant activity. All the extracts showed moderate cytotoxicity to all the five cell lines Vero, A-549, L6, BRL, 3A and L-929 with CTC50 value ranging from 400-125 µg/ml. Short-term cytotoxicity studies were conducted for all the extracts against (Dalton Lymphocytes ascites) cells.  The CTC50 value was found to be 435 µg/ml. Thus, the extracts of P. Chinensis may possess cytotoxic, antioxidant and antimicrobial activity.
Separation and Purification of Proanthocyanidins Extracted from Pomegranate’s Peels (Punica Granatum)
Authors: Zam Wissam , G Bashour , W Abdelwahed , W Khayata
Published: August 2020

This study was designed to find the best method to separate proanthocyanidins from other phenolic compounds extracted from pomegranate’s peel and to investigate their radical scavenging capacity. Water is used as an effective solvent for extracting antioxidant compounds from pomegranate’s peel (Punica granatum). The final extract contained closely related compounds not readily separable. Proanthocyanidins are the most potent antioxidant found in this extract and the purification and separation from other phenolic compounds is an important challenge. A comparison of two SPE cartridges, including silica-based C18 and aminopropyl for the isolation and purification of proanthocyanidins extracted from pomegranate’s peel, showed that the proposed SPE method with aminopropyl cartridge using alkalized aqueous acetone as eluent was more effective for the purification and the separation of extractable proanthocyanidins.
Formulation and Evaluation of a Pulsatile Delivery System of Losartan Potassium by Factorial Design
Authors: Shivhare Umesh D , Kakade V N
Published: August 2020

The present study was aimed to prepare a time-dependent pulsed release system for the programmed release of losartan potassium for the treatment of hypertension. The core tablets of losartan potassium were prepared using wet granulation containing a superdisintegrant. The design was based on 32 full factorial design containing 2 factors evaluated at 3 levels and the experimental trials were performed on coating of the core tablets. Eudragit S100 and Eudragit L100 were used as pH dependent polymers for coating of the tablets. Factors influenced the lag time and In-vitro drug release of formulations, called as dependent factors. Dissolution studies of coated tablets in media with pH (1.2 and 6.8) showed that drug release could be modulated by optimizing the concentration of Eudragit L100: Eudragit S100. Polynomial mathematical model generated for various response variable using multiple linear regression analysis, were found to be statistically significant. Contour plots and response surface plots were drawn and optimum formulation were selected by feasibility and desirability function. The experimental values obtained from the optimized formulation highly agreed with the predicted values. The results of in vitro dissolution studies indicated that formulation P5 is the most successful formulation of the study and exhibited lag time 5.5 h and drug release 95.23 % in 12 h. The total release pattern was very close to the theoretical release profile of pulsed release system. The study showed that lag time prior to drug release was highly affected by the coating level. The dissolution data revealed that the level of coating and the ratio of polymers are very important to achieve an optimum formulation. Stability study of the optimized formulation indicates no significant difference in release profile after a period of one month.
Formulation Optimization and Evaluation of Nanostructured Lipid Carriers Containing Valsartan
Authors: Patel Ravish J , Patel Zil P
Published: August 2020

Nanostructured lipid carriers (NLCs), a lipid based colloidal carrier system, offer many advantages such as increase the solubility, improves the bioavailability and therapeutic efficacy. Incorporation of liquid lipid can improve the drug loading capacity in the NLCs. Valsartan is an antihypertensive drug with low oral bioavailability ranging from 10-35% because of poor solubility and extensive first pass hepatic metabolism. The purpose of present study was to develop and characterize the valsartan loaded nanostructured lipid carriers (Val-NLCs) to enhance the solubility, bypass the hepatic first-pass metabolism, and enhance the lymphatic absorption leading to greater oral bioavailability. Valsartan loaded NLCs were prepared by melt emulsification method and optimized using a two level full factorial design. Effect of content of Capmul MCM EP on crystallinity of tristearin was studied by differential scanning calorimetry (DSC) method. The particle size, entrapment efficiency, drug loading and zeta potential values of optimized batch were 62±0.494 nm, 86.59±0.671, 8.65±0.06 % and -17.4 mV, respectively. TEM images showed spherical particles with diameter of around 50 nm. In vitro drug release of 70% was observed at the end of 12 hrs. Ex-vivo drug release of 90% was observed in 2 hrs. Stability study indicated that the prepared Val-NLCs suspension was stable at refrigerator conditions for one month. Lyophilization produced free flowing Val-NLCs powder from suspension and was easy to reconstitute. Based on these results, it is concluded that NLCs are promising drug delivery for improving the oral bioavailability of valsartan.
Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor
Authors: Chandrethiya G D , Shelat P K , Zaveri M N
Published: August 2020

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.
Carbon Nanotubes, Quantum Dots and Dendrimers as Potential Nanodevices for Nanotechnology Drug Delivery Systems
Authors: Malik Prashant , Gulati Neha , Malik Raj Kaur , Nagaich Upendra
Published: August 2020

Nanotechnology deal with the particle size in nanometers. Nanotechnology is ranging from extensions of conventional device physics to completely new approaches based upon molecular self assembly, from developing new materials with dimensions on the nanoscale to direct control of matter on the atomic scale. In nanotechnology mainly three types of nanodevices are described: carbon nanotubes, quantum dots and dendrimers. It is a recent technique used as small size particles to treat many diseases like cancer, gene therapy and used as diagnostics. Nanotechnology used to formulate targeted, controlled and sustained drug delivery systems. Pharmaceutical nanotechnology embraces applications of nanoscience to pharmacy as nanomaterials and as devices like drug delivery, diagnostic, imaging and biosensor materials. Pharmaceutical nanotechnology has provided more fine tuned diagnosis and focused treatment of disease at a molecular level.
Formulation Development of Aceclofenac Nanosuspension as an Alternative Approach for Improving Drug Delivery of Poorly Soluble Drugs
Authors: Prabu S. Lakshmana , Sharavanan S P , Govindaraju S , Suriyaprakash T N K
Published: August 2020

Poor water solubility of active pharmaceutical ingredients is a major problem in drug discovery and formulation development. Nanoparticle engineering process has been seen as a promising approach for the enhancement of drug solubility. In this study, we present an approach of nanosizing a drug/polymeric complex to increase both solubility and dissolution rate of poorly-water soluble drug aceclofenac, which is widely used as anti-inflammatory drug. Polymeric nanosuspensions were prepared by nanoprecipitation method by using biodegradable polymer loaded with aceclofenac, with the aim to improve anti-inflammatory therapy. The prepared formulation was evaluated for drug excipients compatibility study, polydispersity index, particle size analysis, surface morphology, zeta potential, drug release features and stability. These study results indicate the suitability of formulation procedure for preparation of nanosized poorly-water soluble drug formulation with significantly improved in vitro dissolution rate and fast onset of therapeutic drug effect.
Formulation Development of Oral Mucoadhesive Tablets of Losartan Potassium using Mucilage Isolated from Diospyros melonoxylon Roxb Seeds
Authors: Singh Sudarshan , Bothara Sunil B
Published: August 2020

Diospyros melonoxylon Roxb is a small tree with rather slender stem and smooth grey bark belonging to family Ebenaceae found widely in Chhattisgarh. The present investigation reports the isolation of mucilage from Diospyros melonoxylon seeds as per AOAC guideline and evaluating it as mucoadhesive agent. Physiochemical characteristics of mucilage, such as appearance, solubility, swelling index, microbial count, loss on drying, viscosity, hydration capacity, flow property, hausner ratio and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, using Losartan Potassium as model drug. Granules were prepared by wet granulation process using polyvinylpirroli-done as binding agent. Mucilage was used in four different concentrations i.e. 20, 40 and 60 % w/w. The prepared granules were evaluated for micrometrics property. The tablet were prepared and evaluated for weight variation, thickness diameter, hardness, percent friability, in vitro dissolution and degree of swelling. The property of bioadhesive strength of isolated mucilage was compared with Guar Gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. The tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.2063N, 0.3837N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study of effect of intensity of agitation at different rpm (50 and 150) and electrolyte (NaCl and CaCl2), and formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months all formulation showed stability with respect to release pattern.
Optimization of Diclofenac Sodium Orodispersible Tablets with Natural Disintegrants using Response Surface Methodology
Authors: Panda Bibhu Prasad , Patro C.S , Kesharwani D , Rao M.E.B
Published: August 2020

Traditionally experimental methods in the pharmaceutical formulation development involve significant amount of time and efforts to get an optimized dosage form. It is very much desirable as per industrial perspective to obtain suitable, optimized and stable formulation with minimum amount of time and effort. The purpose of this study was to study the synergic effect of natural disintegrants and central composite design in optimization of diclofenac sodium orodispersible tablets. In this study, central composite design was applied to study the effect of natural disintegrant as independent variables i.e. seed mucilage of Plantago ovata, and seed mucilage of Ocimum basilicum. Diclofenac sodium orodispersible tablets were prepared by direct compression method on Cadmech single punch machine using flat 8-mm punches and characterized for the dependent variables like disintegration time and cumulative percent drug released after 25 minutes. Optimization study by multiple regression analysis revealed that, 6% of Plantago ovata and 5% Ocimum   basilicum was found to be optimum which has disintegrated in 36 secs and cumulative percent drug released was 99.2% at               25 minutes. A checkpoint formulation was prepared to prove the validity of the evolved mathematical model. These findings suggest that synergic effect of natural disintegrants of Plantago ovata and Ocimum   basilicum employed with systematic experimental design approach have greater influence in optimization of diclofenac sodium orodispersible tablets. It is likely that this formulation technology can be exploited for commercial production of dispersible tablets.
Development of RP-HPLC Method for Estimation of Valsartan and Hydrochlorothiazide in Tablets
Authors: Menezes Cylma , M Vishal , B Shyamkumar , N Reema
Published: August 2020

A simple, efficient and reproducible reversed phase high performance liquid chromatographic (RP-HPLC) method was developed and validated for the simultaneous estimation of valsartan and hydrochlorothiazide in bulk and in tablets. A column having 250 x 4.6 mm i.d. (Kromasil C18) in isocratic mode with mobile phase containing 50 mM potassium dihydrogen o-phosphate buffer (triethylamine 0.2%), (pH 3.7 adjusted with o-phosphoric acid): acetonitrile (56:44 v/v) was used. The flow rate was 1.0 ml/min and effluent was monitored at 232 nm.  The retention time of valsartan and hydrochlorothiazide was 10.15 and 3.78 min respectively. All calibration curves showed good linear correlation coefficients within the tested limits (r2 > 0.9995). The linearity dynamic range was found to be 20-150 µg/ml and 5-45 µg/ml for valsartan and hydrochlorothiazide respectively. Percentage recoveries for valsartan and Hydrochlorothiazide were 100.45 % and 98.75 % respectively. All the analytical validation parameters were determined and found in the limit as per the International Conference on Harmonization (ICH) guidelines which indicates the validity of the method. The developed method was found to be accurate, precise and robust for the simultaneous estimation of valsartan and hydrochlorothiazide in bulk and in tablets.
Green Synthesis of Silver Nanoparticles by Allamanda cathartica L. Leaf Extract and Evaluation for Antimicrobial Activity
Authors: Rao M. Linga , G Bhumi , N Savithramma
Published: August 2020

Silver nanoparticles (SNPs) exhibit tremendous applications in medicine as antimicrobial agent.  The use of different parts of plants for the synthesis of nanoparticles is considered as a green technology as it does not involve any harmful chemicals.  In the present study, we report a rapid biosynthesis of silver nanoparticles from aqueous leaf extract of medicinal plant Allamanda cathartica.  The active phytochemicals present in the plant were responsible for the quick reduction of silver ion to metallic silver nanoparticles. The reduced silver nanoparticles were characterized by using UV-Vis spectrophotometry, Scanning Electron Microscope (SEM), Energy Dispersive Analysis of X-ray (EDAX) and Atomic Force Microscopy (AFM).  The spherical shaped silver nanoparticles were observed and it was found to 19-40 nm range of size.  These phytosynthesized SNPs were tested for their antimicrobial activity and it analyzed by measuring the inhibitory zone. A. cathartica aqueous leaf extract of SNPs showed highest toxicity to Pseudomonas followed by Klebsiella, Bacillus and E. coli and lowest toxicity towards Proteus. In fungal species, highest inhibition zone was noted against Rhizopus followed by Curvularia, Aspergillus flavus and Aspergillus niger and minimum inhibition zone was observed against Fusarium species.  These results suggest a promising potential of Indian plant-based green chemistry for production of SNPs for biomedical and nanotechnology applications.
Formulation and Evaluation of Fast Dissolving Gliclazide Tablets by Complexation with Hydroxypropyl-β-Cyclodextrin
Authors: Aly Adel M , Al-Akhali Khaled M. , Alrefaey Hesham , Shaker Mahmoud A.
Published: August 2020

Gliclazide (GZ) is practically insoluble in water and its bioavailability is limited by dissolution rate. The aim of the present study was to enhance the dissolution rate and bioavailability of GZ by complexation with hydroxypropyl (HP)-β-cyclodextrin (CD) applying three different methods; physical mixing, kneading technique and spray drying technique.  Also, to evaluate the dissolution rate and the hypoglycemic effect of the prepared complexes, in comparison with the GZ market product (Glizide tablets) in Saudi market. The produced complexes were characterized and evaluated using Differential Scanning Calorimetry (DSC), X-ray Diffractometry (XRD), Scanning Electron Microscope (SEM) and the in vitro release studies. All the methods of preparation of complexes were found to be effective in improving the solubility of gliclazide in comparison with the commercial product (Glizide tablets). The formation of inclusion complexes was evident in these formulations as shown by DSC and XRD studies. The inclusion complexes prepared by spray drying method in 1:1 molar ratios were the most effective method for improving the solubility of GZ. The in-vivo hypoglycemic effect of the complexed GZ-HP-β-CD prepared by spray drying significantly improved the biological performance and therapeutic efficacy of the drug compared to Glizide market product.
Innovative Eco-friendly Approaches for Green Synthesis of Silver Nanoparticles
Authors: Bhosale Rohit Rajendra , Kulkarni A S , Gilda S S , Aloorkar N H , Osmani R A , Harkare B R
Published: August 2020

Nanotechnology is an escalating field that has made its contribution to all spheres of human life. The green synthesis of nanoparticles has paved for better methodologies and approaches in the medicinal field. Nowadays silver, gold and other metallic nanoparticles are used as an efficient carrier for drug molecules for developing novel drug delivery systems. In course of synthesizing these nanoparticles various chemicals, solvents and reagents are used which harms our eco system directly or indirectly. Silver nanoparticles (Ag NPs) have been widely used as a novel therapeutic agent extending its use as antibacterial, antifungal, anti-viral and anti-inflammatory agent. Silver nanoparticles (Ag NPs) prepared by green synthesis have many advantages over conventional methods involving chemical agents associated with environmental toxicity. Green synthetic methods include polysaccharide method, irradiation method, biological method, polyoxometallates method and tollens method. Green synthesis of nanoparticles is found to be an emerging branch of nanotechnology. The use of environmentally benign materials like plant leaf extract for the synthesis of nanoparticles offers numerous benefits of eco-friendliness and compatibility for pharmaceutical and biomedical applications as they do not use toxic chemicals in the synthesis protocols. Rapid and green synthetic methods using various plant extracts have shown a great potential in silver nanoparticles (Ag NPs) synthesis. This review article describes the bio-inspired synthesis of nanoparticles that provides advancement over chemical and physical methods as it is cost effective, eco-friendly and more effective in a variety of applications.
RP-HPLC Assay for Estimation of Pitavastatin in Bulk and Pharmaceutical Dosage Forms
Authors: Tirumala K , Gautam CH.V.S , Gangadhar J , Jayajeevitha M , K Vanitha Prakash
Published: August 2020

Reverse phase high performance liquid chromatographic (RP-HPLC) method was developed and validated for the estimation of pitavastatin in tablet dosage form. A Phenomenex Luna C18, 150×4.6 mm i.d, 5 µm particle size with mobile phase consisting of buffer 0.01M potassium dihydrogen ortho phosphate pH (3.75) adjusted with dilute orthophosphoric and acetonitrile in the ratio of 20:80 v/v was used. The flow rate was 1.2 mL/min and eluents were monitored at 248 nm. The retention time was 4.1min. The detector response was linear in the concentration of 25-150 µg/mL, with the regression coefficient of 0.9998. Quantification was done by calculating area of the peak and the limit of detection and limit of quantification were 1.9 µg/mL and 5.7 µg/mL respectively. The percentage assay of pitavastatin was 101.1%. The results of study showed that the proposed RP-HPLC method is simple, rapid, precise and accurate which is useful for the routine determination of pitavastatin in bulk drug and in its pharmaceutical dosage forms.
Antihyperglycemic Effects of Tragia plukenetii Ethanolic Extract
Authors: Sama Venkatesh , T Rajini , Afrooz Humera , P Balaraju , Reddy B. Madhava , Mullangi Ramesh
Published: August 2020

Plants represent a major potential source of drugs for treating diabetes. The study of plants having antidiabetic activity may give a new approach in the treatment of diabetes mellitus. Tragia plukenetii is traditionally claimed to be useful in the treatment of diabetes. The present study was intended to evaluate the antihyperglycemic activity of aqueous ethanolic extract on normal fasted, glucose loaded and alloxan induced diabetic rats, at an oral dose of 75, 150 and 300 mg/kg in male Wistar rats. The alcoholic extract has not produced any hypoglycemia in normal fasted rats. The ethanolic extract has displayed a significant dose dependent antihyperglycemic activity in oral glucose tolerance test and in alloxan induced diabetic rats at an oral dose of 150 and 300 mg/kg. The ethanolic extract has effectively scavenged the stable free DPPH radical in-vitro. It is concluded that Tragia plukenetii aerial parts alcoholic extract is effective in controlling blood glucose levels in diabetic rats.
Self Microemulsifying Nutraceutical and Drug Delivery Systems
Authors: Wankhade Vikrant P , Kale Nivedita S , Tapar K.K
Published: August 2020

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.
Formulation and Characterization of Nateglinide Nanosuspension by Precipitation Method
Authors: Papdiwal Amruta , Sagar Kishor , Pande Vishal
Published: August 2020

Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.
Selective Enumeration of Lactobacillus acidophilus for Probiotic Formulations
Authors: Bhattacharyya Barun K , Chowdhury S , Das S , Saha P K , Mukherjee S , Manna A , Bhattacharjee D
Published: August 2020

Probiotic microorganisms have been utilized for many years in food processing, preservations and for nutraceutical health benefits.  There are a large number of pharmaceutical formulations containing probiotic microorganisms available in the market worldwide. Majority of these organisms are the members specifically from genera Lactobacillus, Lactococcus and Bifidobacterium. A number of media have been proposed for selective or differential enumeration of lactobacilli and bifidobacteria in mixed populations. The development of selective medium using different types of ingredients and antibiotic are well practiced. In the present study we have developed a selective medium for the enumeration of Lactobacillus acidophilus by utilizing the antibiotic ofloxacin resistance of the organism in Lactobacilli MRS-agar. Samples were analyzed by determining viable counts in reference Lactobacilli MRS agar and selective Lactobacilli MRS-ofloxacin agar media. The results were statistically analyzed to evaluate the precision, accuracy, reproducibility and selectivity of the method developed.  Thus MRS containing ofloxacin medium can be used for selective enumeration of Lactobacillus acidophilus strains available in commercial formulations containing Bifidobacterium species.
Development and Evaluation of Novel Fast Disintegrating Acetaminophen Tablets
Authors: Pethe Anil M , Patil A.T. , Telange D R , Tatode A A
Published: August 2020

In this study, attempts were made to design and developed disintegrating drug delivery system, Acetaminophen fast disintegrating tablet (AFDT) by combining super disintegrants and direct compression method. Acetaminophen is widely used as “over the counter” and “common household drug” as analgesic and antipyretic along with poor absorption due to first pass metabolism. So we aimed to use our novel delivery system to achieve rapid absorption in patients like mentally ill, bed ridden and those who do not have easy access to water. The (AFDT) were produced by combining three super disintegrants viz. Croscarmellose, Crospovidone and Sodium starch glycolate in 4% w/w as ratio of (1:1, 1:2, 2:1) using direct compression method. The optimized batch (A3) of tablet were evaluated for post – compression parameters like hardness (4.5 ± 0.75 kg.cm2), friability ((0.76 %), wetting time (42 ± 0.92 sec), water absorption ratio (98.6 %), disintegration time (24.00 ± 0.83 sec.) were found to be acceptable according to standard limits. The in vitro release rate of acetaminophen from (AFDT) was found to be more than that simple formulation in pH (5.8) using USP dissolution test apparatus type-II. These results indicated that, the new (AFDT) formulation system combined advantage of faster release of acetaminophen, which had better effects of rapid oral absorption. Therefore, the AFDT may be used as fast disintegrating delivery system for OTC drug with poor absorption due to first pass metabolism.