Development and Optimization of Coated Tablet Containing Amlodipine and Valsartan for Hypertension Treatment

Objective: To develop and optimize the formulation of coated tablets containing these Active Pharmaceutical Ingredients (APIs) with in vitro equivalence to that of the original drug. Methods: Design Expert and BCPharSoft OPT softwares were applied in the development and optimization of film-coated tablets of amlodipine 5 mg and valsartan 80 mg, in order to obtain a tablet formulation with in vitro equivalence to the original drug in three dissolution testing environments. Evaluating through appearance, identification, medium hardness, weight uniformity, in vitro equivalence, assay. Results: An optimized formulation of film-coated tablets with in vitro equivalence to the referent drug was obtained. For the tablet core, it is composed of amlodipine besylate 6.94 mg (equivalent to 5 mg amlodipine) and valsartan 80 mg with excipients of 9.77% crospovidone XL, 2% aerosil, 2.75% magnesium stearate, 42.01% avicel PH 112, with a hardness of 70-90 N. The film-coating suspension comprises 4.75% Hydroxypropyl Methylcellulose 6cps (HPMC 6cps), 0.42% polyethylene glycol 6000 (PEG 6000), 0.84% talc, 1.77% titanium dioxide (TiO2), 0.12% yellow iron oxide, in 92.1% ethanol 96%-water (2:1). Conclusion: In the current study, a film-coated tablet formulation with in vitro equivalence of two APIs to the original drug in all three environments was successfully developed and optimized. The obtained results are an important premise for the development of related generic drugs in the pharmaceutical market of developing countries, which not only reduces the product price but also help less wealthy patients in developing countries to better control hypertension disease.