Abstract

CAPTOPRIL-EXCIPIENT PREFORMULATION STUDIES FOR MOUTH DISSOLVING TABLETS DEVELOPMENT

Ahmed Mohamed Othman, Mahmoud Mahyoob Alburyhi* and Ghada Hassan Al-

Abstract

Captopril is a sulfhydryl-containing angiotensin-converting enzyme inhibitor which is the enzyme that converts angiotensin-I to angiotensin II and may also reduce the degradation of bradykinin. It is used in the management of hypertension, heart failure, myocardial infarction and in diabetic nephropathy. Therefore, it can be used as a model of mouth dissolving tablets MDTs as a more bioavailable form than conventional tablets. The main objective of the present study was to the preformulation studies were performed to know the development of formulation and evaluation of Captopril mouth dissolving tablets MDTs to improve the bioavailability of Captopril. In API development process, a detailed characterization of the API and other formulation components is usually carried out during the preformulation stage. The drug-excipient compatibility studies were conducted to characterize the drug Captopril present in mouth dissolving tablets MDTs. Preformulation, formulation and evaluation of Captopril to avoid problems associated with conventional delivery system and one of the most recent antihypertensive agents. In the present study that the compatibility was assessed by, FTIR spectroscopy, and melting point apparatus, precompression parameters and powder flow properties. Results showed that physical mixtures physical mixtures of Captopril with different used excipients such as Microcrystalline cellulose, Mannitol, Maize starch and Lactose monohydrate as diluent, and Croscarmellose sodium and Sodium starch glycolate as superdisintegrants were evaluated for preformulation studies parameters. It was concluded that the drug Captopril was found to be compatible with most Captopril MDTs formulations which were selected for the formulation development of the Captopril mouth dissolving tablets MDTs. Formulation scientist from his experience and knowledge have to significantly in the preformulation study stage and is an important factor in the ADDS (Advanced Drug Delivery Systems) product development process.

Keywords: Captopril, Compatibility, Excipients, Development, Preformulation, Formulation.