Moisture Sorption-desorption Characteristics and the Corresponding Thermodynamic Properties of Carvedilol Phosphate.

Aims: Carvedilol phosphate (CDP) is a nonselective beta-blocker used for the treatment of heart failures and hypertension. In this work, moisture sorption-desorption characteristics and thermodynamic properties of CDP have been investigated.

Materials And Methods: The isotherms were determined using dynamic vapor sorption analyzer at different humidity conditions (0%-90% relative humidity) and three pharmaceutically relevant temperatures (20°C, 30°C, and 40°C).

Physical characterization and dissolution performance assessment of Etravirine solid dispersions prepared by spray drying process.

The aim of the current exertion was to prepare Solid Dispersion of Etravirine by Spray drying technique to enhance aqueous solubility and dissolution rate. Solid dispersions (SD) of Etravirine were prepared using Copovidone and Povidone-Copovidone in dichloromethane and physical properties were characterized by Scanning electron microscopy (SEM), X-Ray diffractometry (PXRD), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC). SD's were evaluated for equilibrium solubility and in vitro drug release profile by dissolution testing.

Trace Level Quantification of the (-)2-(2-amino-5-chlorophenyl)-4-cyclopropyl-1,1,1-trifluoro-3-butyn-2-ol Genotoxic Impurity in Efavirenz Drug Substance and Drug Product Using LC-MS/MS.

Efavirenz is a non-nucleoside reverse transcriptase inhibitor used in the treatment of human immunodeficiency virus type-1 (HIV). (2S)-(2-Amino-5-chlorophenyl)-4-cyclopropyl-1,1,1-trifluoro-3-butyn-2-ol (AMCOL), used as an intermediate in the synthesis of efavirenz and a degradation impurity, has an aminoaryl derivative which is a well-known alerting function for genotoxic activity. Upon request from a regulatory agency, a selective and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for trace level quantitative determination of AMCOL related compound of efavirenz, for a risk assessment and comparison of impurity levels with the commercially available innovator product (brand name: Sustiva).

Simultaneous estimation of degree of crystallinity in combination drug product of abacavir, lamivudine and neverapine using X-ray powder diffraction technique.

Objective: In the present study, simultaneous determination of degree of crystallinity content in abacavir (ABC), lamivudine (3TC) and neverapine (NVP) from there combination drug product using X-ray powder diffraction (XRPD) technique is developed and validated.

Methods: The X-ray procedure for the identification and determination of the degree of crystallinity in ABC, 3TC and NVP drug product is developed and validated. It is based on the X-ray diffraction from crystalline region of the drug product.