Development of Methods for tee Preparation and Evaluation of Chlorampeenicol Palmitate Ester and its Biopearmaceutically Effective Metastable Polymorph

Publisher Website
Google Scholar
Abstract
Polymorphism greatly influences bioavailability because among other variations, the different polymorphs of a particular compound have different solubilities due to different arrangements of molecules in the solid state giving rise to different lattice energies. Chloramphenicol palmitate (CMP) has three polymorphs with different thermodynamic stability. Polymorph A (m.p. 90°C is the stable variety; Polymorph B (m.p. 89°C) is the metastable variety and Polymorph C is the unstable variety. For the preparation of our desired polymorph B, the available literature is quite insufficient and most of them are well guarded by patent secrets. This work was directed towards the development of modified method of Preparation of CMP and subsequent polymorphic modification to give rise to the desired metastable bioavailable variety. The prepared polymorph when compared with reference standard with respect to M.P., TLC Analysis and I.R. Spectroscopy, shows equivalency in all respect. In-vitro Enzymatic Hydrolysis, Dissolution Studies and In-vivo Studies on Intestinal Absorption show superiority of polymorph B over polymorph A.

This publication has 4 references indexed in Scilit: