Abstract

DROTAVERINE-EXCIPIENT COMPATIBILITY STUDIES FOR ADVANCED DRUG DELIVERY SYSTEMS DEVELOPMENT

Mokhtar Abd-hafiz Al-Ghorafi, Mahmoud Mahyoob Alburyhi*, Abdalwali Ahmed Saif, Maged Alwan Noman and Tawfeek A. A. Yahya

Abstract

Drotaverine HCl is used as antispasmodic drug in the treatment of various spastic conditions such as gastrointestinal diseases, biliary dyskinesia, and vasomotor diseases associated with smooth muscle spasms. These spasms are painful and leave uncomfortable feeling. Drotaverine HCl needs about 15 minutes to start giving its effect, so to improve the drug onset of action and increase the drug release. The safety, efficacy, quality and stability of a formulation are major concepts of any API development process. In API development process, a detailed characterization of the API and other formulation components is usually carried out during the preformulation stage. The main objective of the present study was to the preformulation studies were performed to know the physico-chemical and mechanical properties of Drotaverine Hydrochloride for formulation development of Drotaverine Hydrochloride ODTs. The drug-excipient compatibility studies were conducted to characterize the drug Drotaverine Hydrochloride present in Orodispersible Tablets Delivery System ODTDS. Preformulation, formulation and evaluation of Drotaverine Hydrochloride to avoid problems associated with conventional delivery system such as limited permeation, low dissolution and bioavailability and also to improve bioavailability and as an antispasmodic agent. 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 of Drotaverine Hydrochloride and various excipients as mannitol, microcrystalline cellulose as diluents, and sodium starch glycolate and croscarmellose sodium, as superdisintegrants were evaluated for preformulation studies parameters. It was concluded that the drug Drotaverine Hydrochloride was found to be compatible with various excipients which were selected for the formulation development of the Drotaverine Hydrochloride ODTs. 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: Drotaverine Hydrochloride, Antispasmodic agent, Compatibility, Excipients, Development, Preformulation, Formulation.