Gastroretentive floating microspheres for the management hypertension based on drug combination of amlodipine /losartan

Abstract

Background: Hypertension is one of the serious global health issues that affect millions of people and leads to cardiovascular damage if remain untreated. Various antihypertensive drugs have been developed but it is difficult to achieve better control of blood pressure by using mono-therapy so in this research work, combination therapy having sustained effect for the treatment of hypertension was developed. Method: Gastroretentive floating microspheres of amlodipine besylate and losartan potassium were formulated for the purpose of increasing the time of retention of drugs in the upper gastrointestinal tract and ultimately extend drug release. Eudragit RS100 was used as release controlling agent. The method adopted to prepare microspheres was solvent extraction. Formulated microspheres after that tested for assessing flow properties, buoyancy (%), percentage yield, drug release, surface morphology, by FTIR drug and polymer compatibility, size analysis and entrapment efficiency. Release kinetics on cumulative release data were applied. Results: It was observed from the findings that all the formulation remained buoyant in 1.2 pH buffer up to 12 hrs. It was also found that release of drug from formulation was prolonged which indicates sustained effect of dosage form. All the other results were satisfactory and it was also found that entrapment efficiency of formulation increased when concentration of polymer increased. On the basis of results, formulation 1 with 1:1 drug polymer ratio was selected as optimum formulation. Conclusion: It was concluded from the study that gastroretentive floating microspheres could be a one of best approach to extend the release of drug delivery system.

Keywords

• Gastroretentive drug delivery system
• Floating microspheres
• Amlodipine besylate
• Losartan potassium
• Sustained release drug delivery