Prolonged-release dosage forms of mebeverine hydrochloride: clinical pharmacological and pharmaceutical aspects

Purpose of the study: Investigation and comperasion of dissolution kinetics of three mebeverine hydrochloride drugs: Duspatalin® 200 mg prolonged-release capsules, Niaspam 200 mg prolonged-release capsules and Sparex® 200 mg prolonged-release capsules. Materials and methods: For each of mebeverine trade names under test, a total of 6 prolonged-release capsules 200 mg were used in the experiment. Duspatalin® 200 mg, served as a reference product. The study was performed using three dissolution media (рН 1.2; 4.5; 6.8), which modeled GI tract parts where disintegration, release, and absorption of API take place. Sampling points (1, 2, 4, 6, 8, 10, and 12 hours) were selected in such a manner so the dissolution profile of the studied dosage forms would be fully described, including the complete release (the plateau). Results: The dissolution kinetics of generic drugs (Niaspam 200 mg and Sparex® 200 mg prolonged-release capsules) and reference product were found to be equivalent in vitro in media with pH 1.2 and 6.8. At the same time, the dissolution of these drugs was not equivalent at media with pH 4.5, which is characteristic for the stomach antrum. The results of the comparative study show that at pH 4.5 93.66% of the API was released from Niaspam capsules and 98.72% - from Sparex® capsules. The percentage of released API from Duspatalin® capsules was 83.08%. Conclusion: In vitro laboratory studies of mebeverine hydrochloride release rate from three drugs (Duspatalin® 200 mg prolonged-release capsules, Niaspam 200 mg prolonged-release capsules and Sparex® 200 mg prolonged-release capsules) showed that the dissolution kinetics at pH 4.5 of the generic drugs differs from that of the original drug, which may potentially impact on clinical practice. However, further direct comparative clinical studies are required in order to confirm this hypothesis.

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