Formulation, in vitro and in vivo Characterisation of Diclofenac Potassium Sustained Release Tablets Based on Solidified Reverse Micellar Solution (SRMS).
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Date
2013-01
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Abstract
Aims: To formulate sustained release diclofenac potassium tablets based on solidified
reverse micellar solution (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 Technology and Industrial
Pharmacy, University of Nigeria, Nsukka and Department of Pharmaceutics, University of
Nigeria, Nsukka 410001, Nigeria.
Methodology: SRMS, consisting of mixtures of phospholipid and triglyceride were
prepared in the ratios of 1:1, 2:1 and 1:2 (Phospholipon® 90H: Softisan® 154) respectively.
SRMS-based tablets containing 100 mg of diclofenac potassium each were prepared
using validated plastic mould. The physicochemical 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 physicochemical properties of the tablet
formulations were significantly affected by the composition/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) respectively. 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 maximum 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.
Description
Keywords
SRMS, diclofenac potassium, tablets, ulcerogenicity, Softisan 154®, Phospholipon® 90H
Citation
Chime S A, Attama A A, Kenechukwu F C, Umeyor E C, Onunkwo G C. Formulation, in vitro and in vivo Characterisation of Diclofenac Potassium Sustained Release Tablets Based on Solidified Reverse Micellar Solution (SRMS). British Journal of Pharmaceutical Research. 2013 Jan-Mar; 3(1): 90-107.