Термогравиметрические исследования суппозиториев с клопидогрелем

Abstract

During the last years clopidogrel has been ranked the leading place of the medications with antiplatelet mechanism and together with strong polyvalent antiaggregatory action on platelets decreases the level of triglycerides and optimizes other indexes of lipidogramm. Alternative to oral administration of clopidogrel is rectal route which thanks to increasing of medical substance bioavailability allows to decrease the dose of active ingredient and to minimize the risks of unwanted drug side eff ects in the organism. On the department of technology of medications in Zaporozhye State Medical University as a result of complex physico-chemical, microbiological and biopharmaceutical investigations the rational composition of clopidogrel rectal dosage form – suppository on hydrophilic base for prevention of atherothrombosis for the patients with myocardial infarction, acute coronary syndrome, ischemic stroke, occlusive arterial disease – was developed. The aim of present work is the study of thermal treatment eff ects of suppository mass with clopidogrel in the temperature range of technological process of suppository manufacturing. As the objects for thermogravimetric investigations the rectal suppositories with clopidogrel 0,075 g (containing 2% surfactants) and also the active substance (clopidogrel) and excipients (twin-80, polyethyleneoxyde base) of this dosage form were used. Thermogravimetric analysis was carried out on the derivatograph "Shimadzu DTG-60" (Japan) with the platinum and platinum-rhodium thermopair with samples heating in aluminium crucibles. It was revealed that developed rectal dosage form of clopidogrel – suppository on hydrophilic polyethylene oxide base containing 2% of twin-80 is a mechanical mixture of active substances and excipients because its components do not interact with each other. Manufacturing of suppositories with clopidogrel at the temperature range generally used in technological process for suppository mass (70–80º) does not lead to destruction of the components of this dosage form.