Abstract

Abstract

Abstract

Abstract

Abstract

Amorphous systems have attracted considerable attention due to their favorable properties; however, their stability issues still pose a major challenge. The purpose of the present work was to investigate the role of molecular mobility and moisture in the physical stability of a selected pharmaceutical amorphous system. Irbesartan (IBS), a relatively stable glass, was chosen as the model drug, as it exhibits a good physical stability (resistance to crystallization) at temperatures below the glass transition (Tg-50 K).

The present investigation describes the design and development of self-correcting monolithic Gastroretentive system of baclofen. Tablets were prepared by direct compression method. Optimization was carried out using simplex lattice design. Drug released at 2h, 4h, 8h, and floating lag time were considered as response variables related to percentages of diluent (MCC), Polyethylene oxide (PEO) and sodium bicarbonate. Tablets were evaluated for in-vitro buoyancy, in-vitro drug release, swelling index and ex-vivo bioadhesion studies.

The probiotic formulations are susceptible to loss in viability due to formulation, processing, storage and in vivo environment. The aim of the present study was to perform preformulation studies of probiotic Bacillus coagulans spores to aid designing of stable formulations. Bacillus coagulans spores were studied for hygroscopicity, resistance to compaction force, aqueous pH stability, and excipient compatibility. The spores were found to be moderately hygroscopic with a significant loss of microbiological assay at water activity value of more than 0.5.

Knowledge about therapy with insects in Mongolian traditional medicine is less studied even they have been used broadly since ancient time. Several orthodox practitioners have surveyed the therapeutic potentials of defensive agents in Blaps femoralis known as “stink beetle” in the past. We present results about content of defensive secretion and surface lipids, both a biologically active principle in insect, used in traditional Mongolian medicine.

During the process development of Salmeterol, an unknown impurity was detected at 2.08 Relative Retention Time (RRT) at a level of 0.11% by a gradient Reverse Phase-High Performance Liquid Chromatography (RP-HPLC). The impurity was isolated from the salmeterol drug substance using preparative HPLC. The separation was achieved with an Inertsil C8 column, using acetonitrile–trifluroacetic acid buffer pH 2.7 as mobile phase. The isolated impurity was characterized by NMR and MS techniques.

With an aim to identify the structural requirements for selective AT1 angiotensin antagonistic activity, a quantitative structure activity relationship (QSAR) analysis was carried out on a series of 6-substituted benzimidazole derivatives. The QSAR expressions were generated using 28 compounds and the predictive ability of the resulting model was evaluated against a test set of 12 compounds. The internal (cross validated squared correlation coefficient) and external consistency (predictive correlation coefficient) of the QSAR model was 0.78 and 0.40 respectively.