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PARTICLE CHARACTERISTICS' EFFECT ON FORMULATION CONTAINING ORAL ANTI-HYPERGLYCEMIC AGENT

IP.com Disclosure Number: IPCOM000132293D
Publication Date: 2005-Dec-06
Document File: 2 page(s) / 38K

Publishing Venue

The IP.com Prior Art Database

Abstract

(±)-5-{[[4-2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl}-2,4-thiazolidinedione hydrochloride (PH) (Figure 1), is an oral anti-hyperglycemic agent which acts primarily by decreasing insulin resistence. PH contains one asymmetric carbon. The compound is synthesized and used as a racemic mixture. No difference was found in pharmacological activity between two enantiomers. It is used in treatment of type II diabetes.

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PARTICLE CHARACTERISTICS' EFFECT ON FORMULATION CONTAINING ORAL ANTI-HYPERGLYCEMIC AGENT

(±)-5-{[[4-2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl}-2,4-thiazolidinedione hydrochloride (PH) (Figure 1), is an oral anti-hyperglycemic agent which acts primarily by decreasing insulin resistence. PH contains one asymmetric carbon. The compound is synthesized and used as a racemic mixture. No difference was found in pharmacological activity between two enantiomers. It is used in treatment of type II diabetes.

Figure 1. Structural formula of PH.

PH, used in our formulation, was prepared from base (PB). PB was suspended in lower alcohol like ethanol and heated under reflux temperature for 1-5 hours. The suspension was cooled and PB was filtered and dissolved in solution of HCl in ethanol at reflux temperature. The solution was cooled and the precipitated PH was filtered under room temperature, washed with water and dried at reduced pressure for few hours.

Recrystallization of PH

PH was dissolved in solution of 0.1-1% HCl in ethanol at reflux temperature. The solution was cooled under room temperature and the precipitated PH was filtered, washed with water and ethanol and then dried at reduced pressure for few hours at temperature below 50°C. PH, prepared as described, was essentially free of PB.

It has been well known that a large difference in size between non-cohesive particles will cause segregation (1). Selection of particle size of both active ingredient(s) and excipients is especially important in direct compression technology, where ingredients are not processed in the way of particle size reduction or enlargement (e.g. milling, grinding, granulation).

The aim of our development work was physical-chemical characterization of PH, primarily influence of particle characteristics of PH on dissolution characteristics of formulation. Ta...