bluuebunny/crossref_metadata_2025_split huggingface dataset:
Recent Advances in the Management of Viral Flu Infections
Authors: P Pitliya , Garg S K , Saini P , Pareek A K , Trivedi S K , Puri D , Bhambu S 
Published: August 2020

Flu is an infectious respiratory disease which is caused by influenza viruses. The most common symptoms of flu are nausea, vomiting and diarrhoea. Different subtypes of influenza viruses are identified based on the combinations of these antigenic structures. Influenza viruses are negative-sense, single-strand RNA viruses that belong to the family Orthomyxoviridae. Antiviral medications are the current pharmacotherapy of flu because they are approximately 70% to 90% effective in preventing influenza. Influenza virus type A is readily prone to mutations, which can lead to minor antigenic changes (antigenic drift) or major antigenic changes (antigenic shift). These changes can result in viral strains capable of causing either an epidemic or a pandemic, because overall immunity in the population is lower. Flublok is the first trivalent influenza vaccine made using an insect virus (baculovirus) expression system and recombinant DNA technology (i.e., without the use of actual influenza virus), so there is little risk of getting the flu from the vaccine. Flublok is highly purified, has three times the amount of active ingredient in traditional influenza vaccines, and contains no preservatives, antibiotics or adjuvants. It provides protection against the latest strains of influenza by containing the corresponding hemagglutinin antigens for those strains. This review article provides brief information of influenza and its treatment by biotechnology-based vaccines introduced within the past few years.
Rifampicin and Ketoconazole Modulation of Intestinal Transport of Carbamazepine in Rats
Authors: Rao Y.M , Devandla Adukondalu , Yamsani Shravan Kumar 
Published: August 2020

Many drug substances interact with each other and affect the CYP enzyme system and transport properties of other drugs. The present study was aimed to investigate the effect of ketoconazole and rifampicin pre-treatment on the transport of carbamazepine across the intestine in rats. The transport of carbamazepine across different parts of intestine was studied by the everted and non-everted sac methods. The control and ketoconazole (80 mg/kg) and rifampicin (60 mg/kg) pre-treated rats were sacrificed and the intestine was harvested. The sacs of intestine were prepared, treated with carbamazepine solution and then placed in Dulbecco’s buffer. Samples were collected periodically and the drug content was estimated using HPLC method. The results show that there was a significant (p<0.05) difference in the transport of carbamazepine from the intestinal sacs of pretreated with ketoconazole and rifampicin as compared to control. It appears that ketoconazole and rifampicin may affect the intestinal transport of carbamazepine and hence may result in pharmacokinetic interactions.
Development and In vivo Evaluation of Cefdinir Nanosus-pension for Improved Oral Bioavailability
Authors: V. Kishan , Thota Suman , Syed Muzammil Afzal , Bomma Ramesh 
Published: August 2020

Cefdinir belongs to III generation cephalosporins and is an oral extended spectrum antibiotic. It is a BCS class IV drug, with low solubility resulting in a low oral bioavailability of about 21% for capsules and 25% for suspension. The aim of this work was to develop cefdinir nanosuspension to improve the oral bioavailability. Nanosuspensions were prepared by using single stabilizer and combination of two stabilizers by employing high speed homogenization followed by sonication method and the prepared nanosuspensions were characterized. Initially, the drug excipient compatibility was checked by Differential Scanning Calorimeter (DSC). In trial experiments, tween80 concentration was varied from 0.25 to 0.75% and homogenization time was varied from 2.5 min to 10 min, and 0.5% surfactant concentration was found optimal. Further, trials were conducted with SLS and poloxamer 188 at the same concentration to know the role of stabilizers. Trials were also done by preparing cefdinir nano-suspensions with different techniques for comparative studies and their size and poly dispersity indices (PDI) were found. The mean size and zetapotential (ZP) of nanosuspensions, prepared by high speed homogenization followed by sonication varied from 541.7 to 947.2 and-13.7mV to -22.4mV respectively. Results of saturation solubility and dissolution studies were used to optimize the nanosuspension. Optimized nanosuspension showed improved saturation solubility, dissolution rate and oral bioavailability by 1.752 fold when compared to marketed suspension and found to be stable at RT for 2 months.The bioavailability improvement was significant at a level of P value < 0.05 when student unpaired t-test was used. Hence, cefdinir nanosuspension formulation holds a great promise in improving dissolution rate and oral bioavailability.
Antioxidant Activity of Selected Chemical Constituents of Quinchamaliumchilensis
Authors: Muñoz Orlando , Aquino Rita , Mencherin Teresa , Picern Patrizia , Christen Philippe , Castro Consuelo , Villarroel Pamela , Delporte Carla 
Published: August 2020

Antioxidant compounds from plant sources have been used worldwide for a variety of indications. In this study, phytochemical investigation of the aerial parts of QuinchamaliumchilensisMol. (Santalaceae) resulted in the isolation and identification of fourflavonol glycolsides, quercetin-3-O-β-D-glucopyranosyl-(1→2)-[α-L-rhamnopyra-nosyl-(1→6)]-β-D glucopyranoside(1), kaempferol-3-O-β-D-glucopyranosyl-(1→2)-[α-L-rhamn opyranosyl-(1→6)]-β-D-glucopyranoside(2),quercetin-3-O-xylosyl-(1→2)-[α-L-rha-mnopyranosyl-(1→6)]-β-D-glucopyranoside(3) and rutin(4), as well as one flavanone glycoside, pinocembroside(5). The compounds were identified by 1D- and 2D-NMR experiments, mass spectrometry and UV spectra by comparison with those reported in literature. These compounds were isolated for the first time from the leaves of Q. chilensis. The antioxidant properties of the extract were investigated using DPPH and ferric reducing antioxidant potential (FRAP) assays. Total phenolic content was determined by the Folin-Ciocalteau method. Significant relationship between antioxidant capacity and total phenolic content was found, indicating that phenolic compounds are the major contributors to the antioxidant properties of this plant. These active molecules have therapeutic potential in treating conditions associated with oxygen free radicals.
Preparation, Characterization and In vivo Evaluation of Rosuvastatin Calcium Loaded Solid Lipid Nanoparticles
Authors: V Kishan , G Suvarna , D Narender 
Published: August 2020

Rosuvastatin calcium (RC), is a hypolipidemic drug, and has poor oral bioavailability of about 20% due to first-pass effect. For improving the oral bioavailability of RC, solid lipid nanoparticles (SLNs) were developed using triglycerides (tristearin, tripalmitin, and trimyristin). Hot homogenization followed by ultrasonication method was used to prepare RC-SLNs. The prepared SLNs were characterized for particle size, PDI, zeta potential (ZP), entrapment efficiency (EE) and drug content. In vitro release studies were performed in 0.1N HCl and pH 6.8 phosphate buffer of by open tube method. Physical stability the SLNs was observed at refrigerated temperature and room temperature for 60 days. Pharmacokinetics of RC- SLNs after oral administration, in male Wistar rats was studied. SLNs prepared with tristearin (Dyanasan-118) having size of 207.3 ± 8.52 nm, PDI of 0.344 ± 0.084, ZP of – 20.9 ± 4.88 mV with 97.06 ± 0.210 % EE were optimized. Differential scanning calorimetric (DSC) study revealed that no interaction between drug and lipid. In vitro release studies showed that more cumulative release of RC in pH 6.8 phosphate buffer than in 0.1NHCl during 24 hours. The lyophilized SLN formulation was used in knowing morphology of SLNs and was found to have spherical shape with increased polydispersity by Scanning electron microscopy. Pharmacokinetic studies showed the relative oral bioavailability of SLNs was 2.2 fold when compared to that of a suspension (p<0.001). Taken together, the results are indicative of SLNs as lipid based carriers for improving the oral bioavailability of this drug by minimizing first pass metabolism.
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.
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.
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.
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.
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.
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
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
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.