Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Comparative in vitro dissolution and in vivo bioavailability of commercial amlodipine tablets

Helgi Jung-Cook¹ , Lourdes Mayet-Cruz¹, Maria Elena Girard-Cuesy²

¹Departamento de Farmacia, Facultad de QuÃmica, Universidad Nacional AutÃ³noma de México. Ciudad de México; ²Investigación, Ciencia y TecnologÃa (ICT) Internacional, México.

For correspondence:- Helgi Jung-Cook Email: helgi@unam.mx

Accepted: 24 August 2018 Published: 30 September 2018

Citation: Jung-Cook H, Mayet-Cruz L, Girard-Cuesy ME. Comparative in vitro dissolution and in vivo bioavailability of commercial amlodipine tablets. Trop J Pharm Res 2018; 17(9):1685-1691 doi: 10.4314/tjpr.v17i9.1

© 2018 The authors.
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Abstract

Purpose: To evaluate the in vivo and in vitro behavior of amlodipine immediate release products.

Methods: Three Mexican amlodipine products and the innovator (Norvasc®) were evaluated. Three bioequivalence studies were performed in 24 healthy male and female volunteers each. Plasma concentrations were determined using a liquid chromatographic method coupled with tandem mass spectrometry (LC/MS/MS). Dissolution profiles were evaluated using USP type apparatus 2 at 75 rpm and 500 mL of HCl 0.1N, pH 4.5 and pH 6.8. Also, the dissolution behavior of different lots of the innovator product was evaluated using apparatus 1 or 2 and 900 mL of buffer pH 6.8.

Results: All the generic products under study were bioequivalent to the innovator. In vitro data showed that although at pH 1.2 and 4.5, the products met the specifications for very rapidly dissolving products but at pH 6.8, neither the innovator nor the test products complied with the criteria for rapidly dissolving products. When the study was performed at pH 6.8 in 900 mL of medium, the innovator showed a rapid dissolution behavior.

Conclusion: The results show that the use of WHO conditions (900 mL of media, apparatus 2 at 75 rpm) are more adequate to predict the in vivo behavior of the amlodipine products.

Keywords: Biopharmaceutics Classification System (BCS), Dissolution, Bioequivalence, Solubility, Permeability