Deciphering molecular mechanics in the taste masking ability of Maltodextrin: Developing pediatric formulation of Oseltamivir for viral pandemia.

Present research work was aimed at masking the bitter taste of anti- viral drug Oseltamivir phosphate (Ost) by complexing it with pea starch maltodextrin- Kleptose Linecaps® (Mld). The Ost groups involved in triggering the bitter sensation were identified by computationally assessing its interaction with human bitter taste receptor hTAS2R 38. A series of exhaustive molecular dynamics (MD) simulation was run using Schrodinger® suite to understand the type of interaction of Ost with Mld. Experimentally, complexes of Ost with Mld were realized by solution method. The complexes were characterized using differential scanning colorimetry (DSC), fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), hot stage microscopy (HSM), scanning electron microscopy (SEM), proton NMR (1H-NMR) and Carbon-13 nuclear magnetic resonance (13C-NMR). Ost-oral dispersible mini tablets (ODMT) were prepared by direct compression and optimised using mixture designs. Finally, bitter taste perception of Ost-ODMT was evaluated in healthy human volunteers of either sex. Computational assessment, involving interaction of Ost with bitter receptor, predicted the involvement of free amino group of Ost in triggering the bitter response whereas, MD simulation predicted the formation of stable complex between Ost and double helical confirmation of Mld. Different characterization techniques confirmed the findings of MD simulation. Results from the taste assessment in human volunteers revealed a significant reduction in bitter taste of prepared Ost-ODMT.

Microemulsion-Based Topical Hydrogels of Tenoxicam for Treatment of Arthritis.

Tenoxicam (TNX) is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, backache and pain. However, prolonged oral use of this drug is associated with gastrointestinal adverse events like peptic ulceration, thus necessitating its development as topical formulation that could obviate the adverse effects and improve patient compliance. The present study was aimed at development of microemulsion-based formulations of TNX for topical delivery at the affected site. The pseudoternary phase diagrams were developed and microemulsion formulations were prepared using Captex 300/oleic acid as oil, Tween 80 as surfactant and n-butanol/ethanol as co-surfactant. Optimized microemulsions were characterized for drug content, droplet size, viscosity, pH and zeta potential. The ex vivo permeation studies through Laca mice skin were performed using Franz diffusion cell assembly, and the permeation profile of the microemulsion formulation was compared with aqueous suspension of drug and drug incorporated in conventional cream. Microemulsion formulations of TNX showed significantly higher (p < 0.001) mean cumulative percent permeation values in comparison to conventional cream and suspension of drug. In vivo anti-arthritic and anti-inflammatory activity of the developed TNX formulations was evaluated using various inflammatory models such as air pouch model, xylene-induced ear edema, cotton pellet granuloma and carrageenan-induced inflammation. Microemulsion formulations were found to be superior in controlling inflammation as compared to conventional topical dosage forms and showed efficacy equivalent to oral formulation. Results suggest that the developed microemulsion formulations may be used for effective topical delivery of TNX to treat various inflammatory conditions.

Issues impacting therapeutic outcomes in pediatric patients: an overview.

The quest for achieving optimal therapeutic outcomes in pediatric patients has evaded the healthcare professionals for long and often lack of child specific dosage forms and the associated events that follow with it have been considered to be major contributor towards suboptimal outcomes. Consequently, there have been sustained efforts over the years to address this issue with the enactment of legislations like Best Pharmaceutical for Children Act (BPCA), Pediatric Research Equity Act (PREA) and Pediatric Regulation by European Union (EU) to incentivise the participation of pharmaceutical industry towards development of child friendly dosage forms. Initiatives taken in past by organisations like World Health Organisation (WHO) and Drugs for Neglected Diseases Initiative (DNDi) to spur the development of child friendly dosage forms has helped to address issues pertaining to management of Human Immunodeficiency Virus (HIV) and malaria in pediatric patients. Present efforts aimed at developing child friendly dosage forms include oro-dispersible platforms including thin films and mini-tablets. Despite these leaps and advancements in developing better dosage forms for children, lower therapeutic outcomes in pediatric patients continue to remain an unresolved issue because of detrimental effects of additional factors such as parents understanding of label instructions and complexities involved in executing pediatric clinical studies thus requiring a concerted effort from pharmaceutical companies, academic researchers, parents and healthcare providers to work for better treatment outcomes in children.

Development of novel floating delivery system based on psyllium: application on metformin hydrochloride.

psyllium, a medicinally active gel forming natural polysaccharide and a dietary fiber has been used as a medicine in myriad of conditions such as constipation and inflammatory bowel syndrome. One of its more recent uses that have received attention has been its ability to reduce blood sugar levels in diabetics. Therefore present work is an attempt to formulate anti diabetic drug Metformin as a controlled release floating delivery making use of pysllium as release retardant and to assist the drug in stabilizing blood sugar level in type II diabetics. Drug and excipients compatibility studies were monitored by thermal analysis using differential scanning calorimeter (DSC) and Fourier transform infra red (FTIR). The DSC thermogram and FTIR of drug and drug-polymer mixture did not reveal any incompatibility. psyllium was tried in different concentrations along with other polymers like HPMC K15M and carbopol 940 to achieve the desired release profile. The total drug: polymer ratio was kept between 1:0.4 to 1:0.5, and different polymer combinations were tried to achieve desired drug release for 12 hours. The prepared tablets were evaluated for in vitro release studies and floating behavior. Our conclusion from the present study indicated that pysllium could potentially be used in conjunction with other polymers to formulate controlled release formulations of anti-diabetic drugs to provide better control over blood glucose levels.

Oseltamivir: a first line defense against swine flu.

Oseltamivir (has known by its brand name 'Tamiflu') is a prodrug, requiring ester hydrolysis for conversion to the active form, Oseltamivir carboxylate. Oseltamivir was the first orally active neuraminidase inhibitor commercially developed by US based Gilead Sciences and is currently marketed by F. Hoffmann-La Roche (Roche). Oseltamivir is an antiviral drug which works by blocking the function of the viral neuraminidase protein. US FDA approved Oseltamivir for prophylaxis of uncomplicated influenza A and B. Currently, Oseltamivir is the only first line defense drug available for the treatment of Swine Flu. Orally Oseltamivir is well tolerated and effective in treatment of influenza in adolescents and adults, including the elderly and patients with chronic cardiac and/or respiratory disease. Many of the pharmaceutical companies targeted Oseltamivir as a block buster molecule. In present review, we have tried to cover chemistry, mode of binding, total synthesis, current patent status, adverse effect and clinical status of Oseltamivir giving emphasis on medicinal chemistry aspect.

Hypolipidemic effect of ethanolic extract from the leaves of Hibiscus sabdariffa L. in hyperlipidemic rats.

The present study is designed to investigate the hypolipidemic effect of ethanolic extract from the leaves of Hibiscus sabdariffa L. (HSEE) in hyperlipidemic rats. In the present work, HSEE was evaluated at three doses (i.e. 100, 200 and 300 mg/kg, orally) in cholesterol-induced (2 g/kg, orally) hyperlipidemic Wistar rats. Atorvastatin (10 mg/kg, orally) was used as the standard drug. Administration of HSEE (200 mg/kg and 300 mg/kg) together with continuous cholesterol feeding for four weeks showed significant reduction in serum cholesterol level by 18.5% and 22%, respectively (p < 0.05); serum triglyceride level by 15.6% and 20.6%, respectively (p < 0.05); serum LDL level by 24% and 30%, respectively (p < 0.05), and serum VLDL level by 15.5% and 20.5%, respectively (p < 0.05), as compared to cholesterol group. However, no significant change in HDL level was observed. HSEE 300 mg/kg was more effective than HSEE 200 mg/kg dose but less effective than the standard drug, atorvastatin. HSEE 100 mg/kg did not show any significant reduction in lipid levels. These results indicate that HSEE exhibit the hypolipidemic effect and among all HSEE groups investigated, HSEE 300 mg/kg has the best hypolipidemic effect.