Abstract

FORMULATION, DEVELOPMENT, AND EVALUATION OF SUSTAINED RELEASE TABLETS OF FELODIPINE BY USING HYDROPHILIC POLYMERS.

Deepshi Srivastava*, Abhishek Mishra, Mohd Lateef Khan and
Suraj Mishra Ramnivas

ABSTRACT

Felodipine is a long-acting 1, 4-dihydropyridine calcium channel blocker, used to control hypertension by selective action on peripheral resistance. The conventional felodipine tablet gives a rather high peak and comparatively low trough levels, due to rapid absorption and distribution. More sustained plasma concentrations might thus produce a more even effect on blood pressure. The main objective of the present research was to formulate and evaluate sustained release matrix tablets of antihypertensive drug Felodipine (FEL). Coating of the optimized batch was done using Opadry seal coat and sunset yellow because FEL has problem of light as well as moisture sensitivity. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated for hardness, friability, weight variation, drug content, swelling index and in vitro release study. The optimized formulations were selected on the basis of acceptable tablet properties and in vitro drug release compared with innovator tablet. Optimized batch tablet was coated using Opadry seal coat and sunset yellow by Pan coating method to give protection against light and moisture. Accelerated stability study was performed on optimized batch. The resulting formulation produced robust tablets with optimum hardness, consistent weight uniformity and friability. Tablets containing only Kollidon SR was not give similar release profile with innovator tablet. Addition of hydrophilic polymer and optimization of their concentration gave similar release profile with innovator tablet. The optimized tablets exhibited gradual and extended release of drug up to 12 hr. The results of dissolution studies indicated that formulation F2 (KSR-40mg and HPMC-50mg) and F7 (KSR-60mg and HPMC-30mg), exhibited drug release pattern very close to innovator release profile. So. From that F10(KSR-50mg and HPMC-50mg) was prepared, exhibited same release profile to that of innovator product.

Keywords: Felodipine, Dibasic Calcium Phosphate, PVP K 30, Magnesium Stearate.