Formulation and Evaluation of Floating Microspheres for an Antihypertensive drug Telmisartan

Abstract

Telmisartan is one of the best options either in combination or alone, to treat hypertension. telmisartan belongs to class II antagonist angiotensin converting enzyme inhibitor. One of the main causes of hypertension is vasoconstriction of blood vessels hence increasing blood pressure which can be controlled by drugs that have vasoconstriction property and telmisartan is one of them, and it also relaxes the blood vessels. The dosage form opted here is floating microspheres as it can provide sustain release of drug over long period of time. Floating microspheres have a tendency to float over gastric fluid hence increasing gastric retention time. These are preferred over conventional form as they provide advantage of reducing gastric irritation, lesser dosing frequency will be required as it provide slow continuous release for prolong period of time. The present research aims to formulate telmisartan floating microspheres and its evaluation. The technique used is solvent evaporation method by using magnetic stirrer. Already formulated telmisartan microspheres have lower bioavailability, drug entrapment and lower release kinetics so our main aim is to formulate such a preparation which have greater bioavailability, drug entrapment and greater kinetic release, and to formulate such a formulation we have opted using variant ratios of polymer Eudragit RS 100, Ethyl Cellulose with constant dose of drug. After formulation, various characterization is done that include micromeritics properties, floating efficiency, solubility, drug entrapment efficiency along with yield and release kinetics. The study revealed that, using a more than one polymer in a different ratio have an impact on every parameter of microspheres.