bluuebunny/crossref_metadata_2025 huggingface dataset:
SGLT2 Inhibitors: A New Generation of Antidiabetic Drugs
Authors: Kulkarni S.K , Kuchana Madhavi , Reddy D Samba
Published: August 2020

The incidence of type 2 diabetes is markedly increasing worldwide. Despite a plethora of therapeutic options available for the treatment of type 2 diabetes, the ability to effectively normalize blood glucose levels and prevent    long-term complications of diabetes remains elusive. There is intense search for new drugs for diabetes.  One novel therapeutic class of antidiabetic drugs is sodium-glucose cotransporter 2 (SGLT2) inhibitors. SGLT2 is renal membrane transporter that plays an important role in glucose reabsorption within kidneys. Hence, inhibition of SGLT2 enhances renal glucose excretion, consequently lowers blood glucose levels in an insulin- independent manner. This article describes various SGLT2 inhibitors currently available in the market and also agents that are undergoing clinical trials for the treatment of type 2 diabetes. Currently three SGLT2 inhibitors are approved for clinical use and several others are still in development. The emerging data suggest that SGLT2 inhibitors hold great promise for the clinical management of type 2 diabetes. It remains to be seen whether this class of drugs offers additional advantages over the existing oral hypoglycemic agents.
Cationic Diclofenac Lipid Nanoemulsion for Improved Oral Bioavailability: Preparation, Characterization and In Vivo Evaluation
Authors: Veerabrahma Kishan , Madishetty Swapna , Syed Muzammil Afzal , Kandadi Prabhakar
Published: August 2020

Cationic nanoemulsions were reported to have increased bioavailability. The aim of present study was to prepare a cationic lipid nanoemulsion of diclofenac acid (LNEs) for improved oral bioavailability to treat arthritic conditions. The LNEs of diclofenac acid were prepared by using soya bean oil, egg lecithin, cholesterol and stearylamine. Stearylamine was used as positive charge inducer. The LNEs were processed by homogenization and ultrasonication. The formulation composition was selected based on earlier reports. The LNEs were characterized for size and zeta potential. The physical stability of LNEs was studied using autoclaving, centrifugal, desorption (dilution effect) stresses and on storage. The total drug content and entrapment efficiency were determined using HPLC. During in vivo studies in Wistar rats, the pharmacokinetic parameters of LNEs were compared with a prepared diclofenac suspension in sodium CMC mucilage. The selected formulations, F1, F2 and F3, were relatively stable during centrifugal stress, dilution stress and on storage. The drug content was found to be 2.38 ± 1.70 mg/ml for F1, 2.30 ± 0.82 mg/ml for F2, and 2.45 ± 0.66 mg/ml for F3. The entrapment efficiencies were 97.83 ± 0.53%, 97.87 ± 1.22% and 98.25 ± 0.21% for F1, F2 and F3 respectively. The cumulative percentage drug release from F1, F2 and F3 showed more release in pH 6.8 phosphate buffer than in pH 1.2 HCl. During oral bioavailability studies, the LNEs showed higher serum concentrations than a suspension. The relative bioavailability of the LNE formulations F1, F2 and F3 were found to be 2.35, 2.94 and 6.28 times that of F4 suspension and were statistically significant. Of all, the cationic lipid nanoemulsion (F3) was superior in improving bioavailability, when compared with plain emulsion (F1) and cholesterol containing LNE (F2). The study helps in designing the cationic oral nanoemulsions to improve the oral bioavailability of diclofenac.
The Novel Drugs of 2014 –Record Approvals for Niche Markets
Authors: Reddy D Samba
Published: August 2020

In 2014, 41 new drugs were approved by the FDA, the highest approval in two decades. This number was 52% higher than the 27 approvals in 2013, indicating another year of excellent innovation and productivity. Seventeen drugs (41%) were First-in-Class with a new or unique mechanism of action for treating a disease. Moreover, 17 of 41 (41%) of these novel drugs were for the treatment of rare diseases, a testament to continued focus or shift to niche diseases. The U.S. FDA is the leading authority for drug approvals worldwide. Many schemes and tracks at the FDA have led to accelerated approval of novel drugs. Such reviews as fasttrack or breakthrough designation are established for meeting demand more quickly. Despite such historic drug approvals, there is continued productivity crisis in R & D due to steady cost escalation for drug discovery and development. The U.S. pharmaceutical market is forecasted to increase from an estimated value of $395 billion in 2014 to reach $548 billion by 2020. The prices appear to be increasing faster for branded prescription drugs. Overall, the current drug approvals and trends clearly reveal the pharma industry shift to niche diseases for pricing power and return on investment.
Development and Evaluation of Optimized Gastroretentive Mucoadhesive Tablets of Famotidine for Gastro-Esophageal Reflux Disease
Authors: Vishal Suryavanshi , Nazim Sayyed , Khan Imran
Published: August 2020

The aim of the present investigation was to increase the gastric residence time of Famotidine by designing and optimization of gastroretentive mucoadhesive tablet, thereby improving bioavailability of Famotidine. Famotidine conventional tablets have been reported by many Scientists to exhibit poor oral bioavailability and fluctuations in plasma drug concentration. This results, either in precipitation of side effects or reduction in drug concentration at the target site. Famotidine is a histamine H2-receptor antagonist. It is widely prescribed in active duodenal ulcers, gastric ulcers, Zollinger-Ellison syndrome and gastro esophageal reflux disease. The effective treatment requires administration of 20 mg of Famotidine 4 times a day. A conventional dose of 20 mg can inhibit gastric acid secretion up to 6 hours but not up to 12 hours. An alternative dose of 40 mg leads to plasma fluctuations; thus a sustained release dosage form of famotidine is desirable. The short biological half-life of drug (2.5-4 hours) also favors development of a sustained release formulation. Thus objective of present study to reduce the dosing frequency by developing, optimizing and evaluating gastroretentive mucoadhesive tablet for sustain release. A 32 full factorial design is employed to study the effect of independent variables like Carbopol-940 and HPMC K100M, which significantly influence characteristics like  ex-vivo mucoadhesive strength and in-vitro drug release. Tablets were prepared by direct compression technique. No significant change was observed in physical appearance, drug content, hardness, mucoadhesive strength, in vitro dissolution pattern after the stability tasting for one month.
Pharmaceutical Advances in Cyclodextrin Inclusion Complexes for Improved Bioavailability of Poorly-Soluble Drugs
Authors: Godge Ganesh Raosaheb , Hiremath Shivanand , Sonawale Bhakti , Shirsath Rani
Published: August 2020

Cyclodextrins (CDs) are commonly used in drug formulations as solubility enhancers because of their ability to form water-soluble inclusion complexes with poorly water-soluble drugs. Cyclodextrins are useful molecular chelating agents. The cyclodextrins have a wide range of applications in different areas of drug delivery and pharmaceutical industry due to their complexation ability and other versatile characteristics. Orally administered drugs completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs play an important role in the process of formulation development. The most common pharmaceutical application of cyclodextrin is to enhance the solubility, stability, safety and bioavailability of drug molecules. Cyclodextrins are cyclic oligosaccharides which have recently been recognized as useful pharmaceutical excipients. As a result of molecular complexation phenomena CDs are widely used in many industrial products, technologies and analytical methods. The negligible cytotoxic effects of CDs are an important attribute in applications such as drug carrier, food and flavors, cosmetics, packing, textiles, separation processes, environment protection, fermentation and catalysis. The objective of this review is to discuss and summarize some of the findings and applications of cyclodextrin and their derivatives indifferent areas of drug delivery. The paper also highlights important CD application in drug solubility and dissolution, bioavailability, safety and stability, their use as excipients in drug formulation, design of various novel delivery systems like liposome, microspheres, microcapsules, and nanoparticles.
A Review of Dendrimer-based Approach to Novel Drug Delivery Systems
Authors: Verma Navneet Kumar , Alam Gulzar , Mishra J N
Published: August 2020

Dendrimers are synthetic macromolecules having highly branched, three-dimensional nanoscale architecture with very low polydispersity and higher functionality. They are polymers bearing regular dendritic architectures and represent a novel class of systems which features modifiable surface groups, multi-functionality and nanoscale monodispersed size. These molecules can form covalent or noncovalent complexes with pharmaceutical compounds and act as vehicles for targeted drug delivery and controlled-release purposes. Complex formation with other compounds can be promoted, for example, by solvophobic/solvophilic interactions, hydrogen bonding, or ionic pairing or through chemical binding (conjugation) to their surface groups. This review discusses the advantages, properties, different type of dendrimers, their characterization, dendrimers-based products and their pharmaceutical application in drug delivery systems. Recent advances of dendritic polymers (targeting dendrimers to HIV infected macrophages in vitro and plasmid and doxorubicin co-delivery targeting to tumor) and future prospects of dendrimers are also briefly discussed. Overall, dendrimers are most important macro-molecules in the novel drug delivery system and they have various pharmaceutical as well as non-pharmaceutical applications.
Formulation and Evaluation of Mouth Dissolving Tablets of Piroxicam
Authors: Singh Sudarshan , Shyale S S , Bhosale G
Published: August 2020

Piroxicam, a non-steroidal anti-inflammatory agent, is widely used in rheumatoid arthritis, osteoarthritis, musculo-skeletal disorders, dysmenorrhoeal and post-operative pain. It has poor bioavailability due to its inherent properties. The objective of present study is to enhance water solubility of Piroxicam by solid dispersion technique and to develop novel method of preparing compressed tablets for Piroxicam with high porosity which dissolves rapidly in mouth, using camphor as sublimating agent and super disintegrants such as Crosscarmellose sodium and sodium starch glycollate. The tablets were evaluated for hardness, thickness, friability, weight variation, wetting time, disintegration time, drug content and in vitro drug release. Optimized formulation was evaluated for stability according to ICH guideline. All tablets had hardness in range of 2.8-3.1 kg/cm2 and friability of all formulations was less than 1.0%. Weight variation and drug content were within USP limits. A stability study for optimized F6 formulation 40 °C / 75 % RH for 30 days showed little change in drug content. Therefore, it is concluded that enhance solubility and increased levels of the super disintegrants Cross carmellose sodium and sodium starch glycollate increases the rate of Piroxicam release. Camphor decreases disintegration time of tablets and create high porosity which dissolve rapidly in mouth and could be industrially feasible.
Formulation and Evaluation of Gastro-Retentive Floating Extended Release Metoprolol Tablets using Sodium Alginate and HPMC K-100M Combination
Authors: Thulluru Ashok , Varma M. Mohan , Setty C M , Chintamaneni Pavan Kumar , Vardhan S. Sriharsha
Published: August 2020

The present study was aimed to convert Metoprolol Succinate convert into Gastro Retentive Floating Tablet (GRFT). The gas generating floating tablets of Metoprolol Succinate were prepared to increase the gastric retention and to extend the drug release up to 12 hr. and thereby enhancing its bioavailability. The floating tablets were formulated using HPMCK 100M alone and with the combination of sodium alginate to the polymer of varying concentrations. The tablets were prepared by non-aqueous wet granulation method. The formulated granules were evaluated for pre-compression studies, after the compression of tablets they were subjected to various post-compression studies: Average weight, thickness, density, hardness, % friability, % drug content, (In vitro buoyancy studies: floating time, total floating time and matrix integrity up to 12 hr) and the In vitro drug release studies. The optimized formulation (F4) was found to follow a near perfect zero order kinetics (regression coefficient,      r2 = 0.978). Higuchi plot for formulation, F4, showed r2 value of 0.978, suggesting that the diffusion and erosion plays an important role in the controlled release of the drug. The data was fitted to the Korsemeyer-Peppa’s equation; and the value of the diffusion component (n=0.654), for the formulation F4, indicated that the drug release follows non-Fickian diffusion.
Formulation and Evaluation of Floating Pulsatile Drug Delivery System of Ibuprofen and Ranitidine Combination
Authors: Raj Behin Sundara , Punitha I S R , Gifty M J
Published: August 2020

Since rheumatoid arthritis patients experience severe pain, inflammation, and joint stiffness in the early morning hours a pulsatile drug delivery system of a suitable anti-inflammatory drug that is administered at bedtime but release the drug in the early morning would be a promising system. The objective of this work was to develop a pulsatile release tablet containing a combination of ibuprofen and ranitidine HCl from which ibuprofen gets released after a lag time of 6-7 hours. The methodology involves; analytical method development for simultaneous estimation of combination drugs, development of pulsatile release tablet and an in vivo study in rats. Lag time was controlled by coating the rapid release core tablet with different grades and concentrations of HPMC polymer. A floating gastroretentive layer was applied on top to prevent metabolism of ranitidine at the last part of the intestine. Six different formulations were prepared with three different concentrations of HPMCK4M and HPMCK100M. In vitro studies showed that the lag time increased with an increase in both concentration and viscosity of polymers. The formulation where the core tablet was coated with 100 mg of HPMCK100M had an optimum lag time of 6.3 hrs. In vivo study evaluated the ulcer protection of the formulation in four animal groups; first group remained as control, the second group received ibuprofen at a dose of 180 mg/kg, third and fourth groups received a combination of both the drugs but ranitidine in different doses. Based on this research, it can be concluded that pulsatile release of ibuprofen tablets can be successfully formulated by using HPMC polymers. The usage of ranitidine along with ibuprofen reduces the ulcerogenecity of the later.
Anticancer Activity of Zinc Nanoparticles Made using Terpenoids from Aqueous Leaf Extract of Andrographis Paniculata
Authors: Dhamodaran M , Kavitha S
Published: August 2020

In recent years, the evolution of green chemistry in the production of nanoparticles has wrapped up an immense consideration because traces of chemicals left unreacted in the chemical synthesis process can be precarious. Green synthesis of metal nanoparticles is an interesting issue of the nanoscience and nanobiotechnology. There is a growing attention to biosynthesis the metal nanoparticles using organisms. Among these organisms, plants seem to be the best candidate and they are suitable for large scale biosynthesis of nanoparticles. Nanoparticles produced by plants are more stable, and the rate of synthesis is faster than that in the case of other organisms. Natural products, especially of plant origin, represent an excellent starting point for research. In traditional medicine there are also several plants that are used to treat many diseases. Therefore, a competent protocol for the production of Zn- NPs without calcinations was developed by green synthesis method using one of the major constituents, terpenoids from aqueous leaf extracts of Andrographis paniculata. Among the single compounds extracted from Andrographis paniculata, andrographolide is the major one in terms of bioactive properties and abundance. The anticancer activities of Zn-TAP NPs have been evaluated in cancer models such as HeLa, Hep-2 cells and were examined in different concentrations by MTT assay method. The Zn-TAP NPs showed a maximum activity against HeLa (human cervical cancer cells) and Hep-2 (human liver cancer cells) with maximal inhibition of 59% and 63% at 250 µg/ml, respectively. This approach offers environmentally beneficial alternatives to more hazardous chemicals and processes and promotes pollution prevention by the production of nanoparticle in their natural environs.
Chronomodulated Delivery of Pantoprazole for Nocturnal Hyperacidity
Authors: P Mahalakshmi , T N K Suriyaprakash , Prabu S. Lakshmana
Published: August 2020

The objective of this work was to design and evaluate an oral site-specific, pulsatile drug delivery system containing Pantoprazole sodium which can be targeted to colon in a pH and time dependent manner, to modulate the drug level in synchrony with the circadian rhythm of nocturnal hyperacidity. Five different composition of Core tablets were prepared by direct compression technique. Based on the release studies of core tablets, nine different compositions of press coated tablets were prepared and analyzed. The press coated tablet further coated by using five different proportions of Eudragit RS PO for providing consistent, reproducible chronomodulated release profile. Formulation FPC3 is more suitable among the formulations to design pulsatile release formulations of pantoprazole sodium for 6 hours lag time. After this lag time burst release was observed which exhibited sigmodial release pattern and that was considered to be an ideal for the pulsatile drug delivery system. The chronomodulated drug delivery systems for pantoprazole sodium for the treatment of hyperacidity was successfully developed and the release of the drug was sharp and complete after the lag time which is necessary for any pulsatile drug delivery systems.
Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques
Authors: Singh Sudarshan , Shyale S S , Sandip H G
Published: August 2020

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.
Antibacterial and Hemolytic Activity of Green Silver Nanoparticles from Catharanthus roseus
Authors: Raja A. , Salique S. Mohamed , Gajalakshmi P. , James Arthur
Published: August 2020

The objective of this research was to standardize the Green synthesis of silver nanoparticles by C.roseus and to evaluate them for their potential against Mycobacteral tuberculosis. Phytochemical study realized the presence flavonoids, saponins, alkaloids, cardiac glycosides, steroids and tannins. Colloidal silver nanoparicle was synthesized by one step green reduction at room temperature and characterized by UV and TEM. An effort made to find out the capping agent revealed that the TLC fraction with 0.7 Rf value showed the reduction of silver ions. GCMS analysis of TLC fraction showed the presence of nine different phytochemical which includes pentadecane and piperdine carboxylic acid as major constituent. The nanoparticle diameter is in the range of 38- 52 nm and stable for 30 days under room temperature. The bactericidal activity of synthesized nanoparticle was  24 ± 0.04 and 22 ± 0.62 mm respectively against M.smegmatis and M.tuberculosis. The in vitro hemolytic assessment of silver nanoparticles was found to be safe at maximum of 1-5 µg/mL and toxic between 15- 50 µg/ml. Further this data encourages that theses biologically synthesized nanoparticles were found to be less toxic and more effective against mycobacterial strains.
Development and Optimization of Mouth Dissolving Film of Granisetron using 32 Factorial Design and Response Surface Methodology
Authors: Sapavadiya Vipul K. , Sapavadiya Miral V. , Shelat Pragna K. , Lalwani Anita N.
Published: August 2020

Granisetron is a highly selective serotonin (5-HT3) receptor blocker which prevents the vomiting reflex induced by serotonin during cancer chemotherapy. The objective of present research work was development and optimization of mouth dissolving film of granisetron hydrochloride. Solvent casting method was used for preparation of mouth dissolving film. Various film forming polymers like PVP K-30, PVA, maltodextrin, HPMC E5 LV and lycoat RS 720 along with and plasticizer like Propylene glycol, Poly ethylene glycol 400 and glycerin were used for selection of suitable polymer plasticizer combination. Film prepared using lycoat RS 720 and PEG-400 was found satisfactory and further factorial design and desirability function was used for optimization. Regression equation and counter plots were executed to dependent variables i.e., tensile strength, % elongation, elastic modulus and % drug release in 1 minutes to independent variables. Results of experimental design revealed that the independent factors lycoat RS 720 and PEG-400 significantly influenced the mechanical properties and % drug release from the film which was ultimately reflected in this formulation of optimized batch. All experimental design formulations were evaluated for weight variation, thickness, drug content, % moisture loss, pH, folding endurance and stability study at 40˚ ± 2˚ C/75 ± 5% RH. From the result of optimized batch it can be concluded that an optimized formulation was stable with suitable packaging and the high % drug release of film in simulated saliva indicate that it can be used for drug delivery system of granisetron hydrochloride having first pass metabolism
Development and Evaluation of Nanoparticle-Loaded Hydrogel of Co-trimoxazole
Authors: Kumar Prajeesh , Narang Raj K. , Swamy Shivansh
Published: August 2020

In this study, development of nanoparticle loaded hydrogel of Cotrimoxazole that could simultaneously deliver trimethoprim and sulfamethoxazole at the site of wound to promote and accelerate wound healing is planned. Chitosan nanoparticles loaded with Co-trimoxazole were prepared by ionic gelation method. Chitosan nanoparticles were optimized and F5 formulation was selected 5:1 Chitosan TPP ratio for this Homogenization speed was kept at 5000 rpm and an average size of 209.8 ± 34.6 was obtained, PDI was found to be 0.26 ± 0.04, the zeta potential of the nanoparticles was found to be + 24.7 ± 3.12 and the entrapment efficiency of 89.7 ± 3.1 % was seen. Hydrogel was prepared and optimized on the basis of Conc. of Carbopol 940 1.2%, viscosity 14.953 ± 0.51, pH 5.9 ± 0.04, Swelling index 250 ± 4.71 and Spreadability 34 ± 3.5. Antimicrobial study and Minimum Inhibitory Concentration (MIC) were performed and it was observed that the MIC of Co-trimoxazole was 2 µg/mL and the hydrogel formulation showed maximum zone of inhibition 3.7 ± 0.3 after 72 hours against plain drug and marketed formulation. The rate of wound contraction was calculated in percentage and at 15th day the control group had 72% ± 3.9%, Marketed formulation group had 36% ± 5.2% and the hydrogel formulation had reduced the wound size to mere 4% ± 1.3% only. Hydrogel loaded with nanoparticles of Co-trimoxazole that possessed optimum rheology and provided sustained drug release was successfully prepared. The developed hydrogel formulation was found to heal the wound 1.5 times faster than the marketed formulation thus providing us with a better alternative to other conventional wound dressings.
Design, in vitro and in vivo Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets
Authors: Appala Sushma , Bomma Ramesh , Veerabrahma Kishan
Published: August 2020

Objective of the investigation was to develop gastro retentive dosage form of gemifloxacin mesylate for local action in the stomach as it has antibacterial activity against Helicobacter pylori. Gemifloxacin mesylate is a synthetic broad-spectrum antibacterial agent for oral administration, having 7 hrs half-life and 71% oral bioavailability. In present study, gemifloxacin mesylate floating matrix tablets were prepared by direct compression method using polymers (HPMC K4M, HPMC K15M and polyox WSR 1105) and evaluated for various parameters like drug content, floating behavior (floating lag time and total floating time), in vitro drug release, swelling index, weight variation, friability, hardness and thickness. Sodium bicarbonate was incorporated as gas generating agent in all formulations. Drug-excipients compatibility was studied by Differential Scanning Calorimetry. Results have shown that the amount of polymer in the formulation affected the drug release. Optimized formulation (F8 containing polyox WSR1105 as release retarding agent) was selected based on in vitro drug release, floating lag time, floating time and other parameters. This formulation followed zero order kinetics and non-Fickian mechanism of drug release. In vivo radiographic study was conducted in healthy human volunteers using tablets containing BaSO4 as radio opaque agent. The average residence time was found to be 4.5± 0.86 h (n=3). This design of gastro retentive drug delivery system helps in increasing the local delivery of drug in patients with Helicobacter pylori infection
Hydrogel Scaffolds - Emerging Biomaterial for Regenerative Medicine
Authors: Kumar Prajeesh , Swamy Shivansh , Narang Raj K.
Published: August 2020

The regenerative medicine field has led to the development of various biomaterials. One such development is in the form of Hydrogel Scaffold for Tissue regeneration. This review describes the biomedical advances in Hydrogel Scaffolds as emerging biomaterial for regenerative medicine.  Their unique ability to mimic the extra cellular environment, biocompatibility, flexible method of synthesis, desirable framework for cellular proliferation and survival has made them the material of choice. Hydrogels have demonstrated features which exemplify many of the broad-based manifestations of tissue engineering, providing realized as well as potential commercial value. Direct incorporation of cells and growth factors has led to efficient and more promising results in regenerative medicine. This review gives an overview of the various kinds of hydrogels, fabrication methods with specific features and few of the recent applications of hydrogels in the field of regenerative medicine.
Bioenhancing Effect of Cow Urine Distillate and Pepper Extract on Antibacterial Activity of Azadirachta Indica Leaves
Authors: Dhakal Pramod , Achary Ankit a , Joshi Vedamurthy
Published: August 2020

Bioenhancers are drug facilitator which do not show the typical drug activity but in combination to enhance the activity of other molecule in several way including increase the bioavailability of drug across the membrane, potentiating the drug molecules by conformational interaction, acting as receptor for drug molecules and making target cell more receptive to drugs and promote and increase the bioactivity or bioavailability or the uptake of drugs in combination therapy. The objective of the present study was to evaluate the antibacterial and activity of combination in Azadirachta indica extract with cow urine distillate and pepper extract against common pathogenic bacteria, a causative agent of watery diarrhea. It has been found that Indian indigenous cow urine and its distillate also possess bioenhancing ability. Bioenhancing role of cow urine distillate (CUD) and pepper extract was investigated on antibacterial activity of ethanol extract of Azadirachta indica. Antibacterial activity of ethanol extract neem alone and in combination with CUD and pepper extract were determined the ATCC strains against Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and E-coli by cup plate diffusion method. Ethanol extract of neem has showed more effect on P. aeruginosa, E-coli than S. aureus and K. pneumonia with combination of CUD and pepper extract. CUD and pepper did not show any inhibition of test bacteria in low concentration. The antibacterial effect of combination of extract and CUD was higher than the inhibition caused by extract alone and is suggestive of the bioenhancing role of cow urine distillate and pepper. Moreover, inhibition of test bacteria was observed with less concentration of extract on combining with CUD
Recent Advances in Gastro-Retentive Drug Delivery Systems
Authors: Venkateswara Rao Korlapati , Venkatachalam V.V.
Published: August 2020

Controlled  gastric  retention  of  solid  dosage  form  may  be  achieved  by  the  mechanisms  of  floatation,  muco-adhesion,  sedimentation,  expansion  or  by  a  modified  shaped  system. The purpose of this paper is to review the recent literature and current technology used in the development of gastroretentive drug delivery systems. Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by a narrow absorption window. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. So, gastroretention could help to provide greater availability of new products and consequently improved therapeutic activity and required benefits to patients. The purpose of writing the article was to compile the recent literature with special focus on various gastroretentive approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. In particular, bioadhesive, size-increasing and floating drug delivery systems are presented and their major advantages and shortcomings are critically discussed in this review. Thus, gastroretention could help to provide greater availability of new products  and  consequently  improved  therapeutic  activity  and  substantial  benefits  to  patients
Formulation and Evaluation of Fast-Dissolving Film of Cetirizine and Dextromethorphan
Authors: Patel Dipal M. , Patel Dhaval J. , Darji Palak J.
Published: August 2020

Fast dissolving dosage forms are gaining popularity in recent time, as this dosage forms requires no water for administration. Cetirizine is widely used in allergic induced asthma and Dextromethorphan is used in sore throat condition. Combination of both the drugs will have more potent effect compared to single drug. The objective of the study was to design and optimize fast dissolving film by casting method using HPMC E5 LV, polyethylene glycol 400, aspartame- neotam-tartaric acid- citric acid- menthol- ion exchange resins for taste masking of cetirizine and dextromethorphan. Films were formulated using plasticizers and also citric acid and tartaric acid as saliva stimulating agent along with, menthol as flavoring agent. Aspartame and Neotame were used as sweeteners and Kyron T111 as ion exchange resin to mask bitterness of drugs. Fast dissolving films contain more than 95% of drugs as per percent drug content study. Formulated film showed mouth dissolving time 17 seconds with more than 96% of drugs release occurs within 30 min. Films were prepared by solvent casting method without any organic solvent and found to satisfy the mouth dissolving time and other film parameters. Our results show that all the four formulated films showed satisfactory film parameters. It can be concluded that, fast dissolving film containing Cetirizine and Dextromethorphan can be casted by solvent casting method without any organic solvents.
The Novel Drugs of 2015 – An Extraordinary Growth of Innovative Pharmaceuticals
Authors: Reddy D. Samba , Reddy Savitha
Published: August 2020

The FDA has approved 45 new drugs in 2015, a record approval in two decades, indicating another year of excellent innovation and productivity. There are many regulatory pathways at the FDA for the approval of novel drugs. Sixteen drugs (36%) were First-in-Class with a new or unique mechanism of action for treating a disease. About 29% of the new drugs are biologics. Moreover, 21 of 45 (47%) are orphan drugs for the treatment of rare diseases. The FDA approved many new drugs to treat various forms of cancer, urinary tract infections, chronic hepatitis C, cystic fibrosis, irritable bowel syndrome, heart failure, and high cholesterol, as well as the first approved reversal agent for a commonly-used blood thinner.  For the second consecutive year, the FDA approved more “orphan” drugs for rare diseases than any previous year in recent history. From 2006 through 2014, the FDA averaged about 28 novel drug approvals per year. Such products represent innovation and provide important new therapies for patients worldwide. Despite such record new drug approvals, there is a continued productivity crisis in R&D due to a progressive rise in cost for drug discovery and development. The U.S. pharmaceutical market is forecasted to reach $548 billion by 2020. The prices appear to be increasing faster for generic and branded prescription drugs. Overall, faster development and regulatory review contributed to a spike in record approval of innovative pharmaceutical products in 2015
Colon Delivery of Naproxen: Preparation, Characterization and Clinical Evaluation in Healthy Volunteers
Authors: Rajitha R. , Narendar D. , Arjun N. , Nagaraj B.
Published: August 2020

Naproxen is a steroidal anti-inflammatory drug and is used in the treatment of rheumatoid arthritis, osteoarthritis and colitis. When administered orally in conventional form results in undesirable gastrointestinal toxicity and poor delivery of the drug to the colonic region. In this study, colon targeted delivery system of naproxen was developed to reduce side effects and achieve high local drug concentration at the afflicted site in the colon. Core tablets of naproxen were formulated with HPMC K4M polymer by wet granulation method. The prepared tablets were evaluated for physical parameters and in vitro drug release. The tablets were coated with Eudragit S100 and Eudragit L100 with triethyl citrate as a plasticizer. The coated tablets were evaluated for physical parameters and in vitro drug release. Drug excipient compatibility studies by using FTIR were analysed. Further, in vivo colon residence time of naproxen in healthy human volunteers was performed by radio imaging study. From the results, formulation EL4 also performed better in vitro release but ES2 was considered more superior because of the former’s dependence on GI transit time for drug release and total weight gain of 7.5% at a concentration of 20% dry weight of the polymer with plasticizer and was not specific to pH of the colon and a weight gain of 20% is needed in case of tablets coated with Eudragit L100. Hence ES 2 was considered as the optimized formulation for colonic drug delivery. These results were confirmed with the results of X-ray studies in three healthy human volunteers
Current Status and Future Prospects of Application Specific Engineered Nanocurcumin Compounds
Authors: Ahmad Shamim
Published: August 2020

Establishing chemical conjugations among complex macromolecules and nanostructured material species with the help of activity-specific chemical moieties either acquired during chemical synthesis of the backbone structures or attaching them later along with the targeting ligands on to the nanoparticulate surfaces by surface functionalization are currently being used in preparing functional compounds appropriate for targeted drug/gene delivery applications. Current drug discoveries involving phytochemicals in place of purely synthetic molecules are getting translated faster into relatively cost-effective formulations that are free from meeting most of the requirements of the stringent test-conditions set by the regulatory authorities as they use the constituents with known toxicity profiles already established through traditional experience of using them as medicine over a long period of time in the past. Moreover, the knowledge of their physico-chemical attributes like hydrophilicity, hydro-phobicity, and amphiphilicity of these constituents is easy to put to use in controlling the shape and size of the nanoparticulate formulations through self-organized nano/microstructures like micelles and other hierarchical supramolecular assemblies in different solvent media as discussed in this review. The structure activity relationships (SARs) of curcumins have shown enough indications that they are going to emerge as an intelligent drug design platforms where the synergistic combinations with natural and benign phytochemicals with numerous biomedical activities would certainly produce smarter but affordable treatments of human ailments in near future.
Formulation and Evaluation of Trilayered Tablets of Zolmitriptan
Authors: Mohammad Abdul Saleem , Farheen Seema , Rasheed Nuha
Published: August 2020

The present study outlines a systematic approach to formulate and evaluate trilayered tablets of zolmitriptan by geomatrix technology by using different concentrations of HPMC, xanthangum and ethyl cellulose by direct compression method for controlled release, which may produce the controlled drug release in the treatment of migraine disorder. The different release rates from these formulations were obtained from in vitro dissolution studies. From the results it was observed that the release rate was greatly influenced by the polymer concentration. In order to obtain a formulation which releases more than 90% of drug within 12-14hrs, sixteen formulation trials of the active layer have been prepared and the drug release follows first order kinetics. Hence, the formulation trial F14  showed about 99% drug release in 12 hrs, where the drug release was dependent on concentration of drug in tablets  and showed various physiochemical evaluation parameters like hardness, thickness and also showed  drug excipient compatibilities by DSC and FTIR studies.
Lacidipine Loaded Solid Lipid Nanoparticles for Oral Delivery: Preparation, Characterization and In vivo Evaluation
Authors: V. Kishan , V Sandeep , D Narendar , N Arjun
Published: August 2020

The objective of this study was to develop and evaluate lacidipine (LD) loaded solid lipid nanoparticles (LD-SLNs) for improving the oral bioavailability. LD-SLNs were prepared in two steps. First step was hot homogenization and next by ultrasonication method, using triglycerides (tripalmitin and tristearin), monoglyceride and surfactants (Poloxamer 188 and egg lecithin E80). The prepared LD-SLNs were characterized for particle size, PDI, zeta potential, drug content, entrapment efficiency (EE %).         In vitro drug release studies using a dialysis bag method in 0.1N HCl and pH 6.8 phosphate buffer were conducted. In addition, long-term physical stability of the optimized SLNs was investigated at refrigerated and room temperature for 60 days. FTIR and DSC studies revealed that no interaction between the drug and lipids. LD-SLNs prepared with Dynasan-116 (F3), having the size of 141.86nm, PDI of 0.293, ZP of -22.3 m with 94.75% of EE was optimized and was stable for 60days. Scanning electron microscopic studies showed nearly spherical shaped particles. Further, pharmacokinetic studies were conducted in wistar rats. The relative bioavailability of LD in SLNs was 2.03 times when compared with that of the LD suspension. The results are indicative of SLNs as suitable lipid based carrier system for improving the oral bioavailability of LD.
Simultaneous Estimation of Ilaprazole and Domperidone in Pharmaceutical Dosage Form
Authors: Patel Gopi , Prajapati Kiral M , Prajapati Bhavesh , Shah Samir K
Published: August 2020

A simple, accurate and precise stability-indicating RP-HPLC method was developed and subsequently validated for simultaneous determination of ilaprazole and domperidone in bulk and pharmaceutical dosage form. The proposed HPLC method utilizes  C18  (250 mm × 4.6 mm × 5 µm) column with mobile phase comprising of 0.5 % glacial acetic acid in water pH 5.5 adjusted with ammonia solution: methanol in the ratio 45:55 v/v at a flow rate of 1.0 ml/min. Quantitation was achieved with UV detection at 286 nm based on peak area with linear calibration curves at concentration  ranges 80-120µg/ml for ilaprazole and 240-360 µg/ml for domperidone  with correlation coefficient of 0.999.The retention times of ilaprazole and domperidone  were found to be 3.0 min, 5.4 min respectively. The mean recoveries obtained for ilaprazole and domperidone were found to be 99.76 ± 0.6463 % and 100.7 ± 0.2424 % respectively. Stress testing which covered acid, alkali hydrolysis, and peroxide, photolytic, thermal degradation was performed to prove the specificity of the proposed method and degradation was achieved. The proposed method was successfully applied for the stability indicating simultaneous estimation of ilaprazole and domperidone in routine quality control analysis in bulk and pharmaceutical formulation.
Isolation and Determination of the Major Principle or Causative Agent behind the 2016 Published Break through Discovery of Dr. M.S. Reddy’s “Multiple Mixed Strain Probiotic Therapy”, in Successfully Treating the Lethal Hospital Acquired Infections Due to
Authors: Reddy Malireddy S , Reddy D.R.K
Published: August 2020

A multiple mixed strain Probiotic culture was compounded using several naturally antibiotic resistant beneficial microorganisms belonging to different genera and species, along with their bacteriocins and growth end products or metabolites. Prior to mixing several individually grown single strains of Probiotics, compatibility studies were conducted to eliminate the strain dominance in the mixed cultures using direct differential plating techniques and strain specific bacteriophages,using the procedures  outlined in our earlier publication. The multiple mixed stain Probiotics thus prepared were studied to see weather Probiotic bacteria by themselves or their bacteriocins and other end products of growth (without the live Probiotics) or the combination of live Probiotics and their bacteriocins and other growth end products, were responsible to inhibit the growth and proliferation of the lethal hospital acquired infections i.e., Clostridium difficile (C. diff) and Methicillin Resistant Staphylococcus aureus (MRSA). In addition, several procedures of preparing the functional mixed strain Probiotics, using liquid nitrogen freezing and freeze drying (lyophilization)were evaluated,tocomeupwiththebest

procedure suitable to maximize their subsequent inhibitory effect on C. diff and MRSA, both under the laboratory conditions and in the practical clinical hospital conditions. Community based clinical trials were conducted to check the effect of multiple mixed strain Probiotics with and without their bacteriocins and their other growth end products, to cure the lethalC. diff infection under practical hospital conditions. The results revealed and confirmed that our 2016 novel discovery is still the best way to prepare and administer the multiple mixed strain Probiotics to treat the lethal hospital acquired infections. Also this study reconfirmed that the liquid nitrogen freezing is far superior to freeze drying or lyophilization to preserve the maximum efficiency of multiple mixed strain Probiotics. In conclusion, it proved that even the concentrated high bacterial cell number multiple mixed strain Probiotics (without their bacteriocins and other growth metabolites) are not as effective compared to the multiple mixed strain Probiotics frozen using liquid nitrogen, along with their bacteriocins and growth metabolites, to cure the lethal C. diff infection under practical clinical hospital conditions.
Creating and Implementing Communicative Tasks According to VanPatten’s Principles
Authors: Clarke Stephen , Hastings Chris
Published: August 2020

In this paper aimed at practitioners, the authors introduce their interpretation of an approach to communicative language teaching proposed by the SLA scholar Bill VanPatten that involves the use of Tasks as key elements in the curriculum. While the notion of task-based learning is not new, VanPatten’s approach differs fundamentally from other conceptions, especially in the way it focuses on a definition of communication and in its rejection of the explicit teaching of grammar. VanPatten (2017) introduces six principles of communicative language teaching which can be used as a framework for designing and implementing Tasks. In the following order, this paper outlines the principles as they relate to Task design, gives an example of a communicative Task created by the authors which reflects VanPatten’s principles, and finally offers considerations for classroom implementation.
実践者を対象とした本論文では、SLAの学者であるBill VanPattenによって提案された、カリキュラムの主な要素としてタスクを使用することを含む、コミュニカティブ・ランゲージ・ティーチングへのアプローチの解釈を紹介する。タスクに基づく言語指導法の概念は新しいものではないが、VanPattenのアプローチは他の概念とは根本的に異なり、特にコミュニケーション定義に焦点を当てている点と、文法の明白な指導を否定している点が異なっている。VanPatten（2017）は、タスク設計および実践するための枠組みとして活用できるコミュニカティブ・ランゲージ・ティーチングの６つの原理を紹介している。次の順序で、本論では、タスク設計に関連した原則の概要を述べ、VanPatten氏の原則を反映した著者によるコミュニカティブタスクの例を示し、最後に授業での実践に関する考慮事項を提案する。
Error Analysis: A Methodological Exploration and Application
Authors: McDowell Leigh
Published: August 2020

Error Analysis (EA) was initially conceived in early Second Language Acquisition research in the 1960s to investigate the systems underlying learner language and has since gained wider application in English Language Teaching research. However, for many language teachers, the practical and technological barriers to employing EA in their professional practices remain restrictively high. This paper demonstrates a simple yet robust procedure for EA that can be applied by anyone with access to the commonly available tools of Microsoft Word and Excel. Additionally, by drawing on data from an EA of 18 texts written by Japanese materials scientists, the paper illustrates how this procedure can inform language teaching practices by identifying the most pressing grammatical needs within a population of L2 English users.
本来、誤答分析（Error Analysis）は、語学学習者の言語の根本にあるシステムを調査する為に1960年代の初期第二言語習得（SLA）研究中に提案されていて、その後英語教授法（ELT）研究に広く使われるようになった。しかし、多くの語学教師等にとっては、仕事に誤答分析を用いるには技術的な壁が未だに高い。本論文では、一般的に使われているワードやエクセル等によって簡単で確実に誤答分析が出来る方法を紹介する。また、18名の日本人の材料科学研究者の文章の誤答分析のデータを用いて、どのようにしてこの方法を使って言語教育法を明確に出来るかを、第二言語として英語を話すグループの課題となる文法の必要性を示しながら、を説明する。