Formulation, in vitro and in vivo Characterisation of Diclofenac Potassium Sustained Release Tablets Based on Solidified Reverse Micellar Solution (SRMS)

Abstract

Aims: To formulate sustained release diclofenac potassium tablets based on solidified reverse micellar soln. (SRMS) and to evaluate the in vitro and in vivo properties of the tablets. Study Design: Formulation, in vitro and in vivo evaluation of sustained release diclofenac potassium. Place and Duration of Study: Department of Pharmaceutical Technol. and Industrial Pharmacy, University of Nigeria, Nsukka and Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria. Methodol.: SRMS, consisting of mixts. of phospholipid and triglyceride were prepd. in the ratios of 1:1, 2:1 and 1:2 (Phospholipon 90H:Softisan 154) resp. SRMS-based tablets contg. 100 mg of diclofenac potassium each were prepd. using validated plastic mold. The physicochem. properties of the tablet formulations were studied and compared with the market brands of the drug for sustained release properties. In vitro release was carried out in simulated intestinal fluid (SIF, pH 7.5) using the USP paddle method. Anti-inflammatory, analgesic/anti-nociceptive and ulcerogenic properties of the formulated tablets were studied using adult Wistar rats. Results: The results showed that the physicochem. properties of the tablet formulations were significantly affected by the compn./ratio of the lipid matrix (LM) used (p < 0.05). The hardness of the tablets ranged from 4.55 ± 0.50 to 5.10 ± 0.39 kgf for tablets formulated with LM 1:2 and 1:1 (M3 and M1) resp. Friability results indicated that all the SRMs tablets exhibited friability values less than 1%. The erosion time ranged from 35.8 ± 1.10 to 120.3 ± 0.32 min. The release profile of the tablets showed max. release between 8-11 h for all the batches. Diclofenac potassium tablets based on SRMS had good anti-inflammatory and analgesic properties and also inhibited the ulcerogenicity of the NSAID by up to 85%. Conclusion: Diclofenac potassium tablets based on SRMS could be used for once daily administration. [on SciFinder(R)]