Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Formulation and Evaluation of pH-Responsive Mini-Tablets for Ileo-Colonic Targeted Drug Delivery

Mohd Abdul Hadi¹ , Raghavendra NG Rao², Srinivasa A Rao³

¹Department of Pharmaceutics, Bhaskar Pharmacy College (JB Group of Educational Institutions), Yenkapally (V), Moinabad (M), R.R.District, Hyderabad-500075; ²Jyothishmathi Institute of Pharmaceutical Science, LMD colony, Karimnagar -505481; ³Bhaskar Pharmacy College (JB Group of Educational Institutions), Yenkapally (V), Moinabad (M), R.R.District, Hyderabad-500075, Andhra Pradesh, India.

For correspondence:- Mohd Hadi Email: hadi.lcp@gmail.com Tel:+919949444787

Received: 22 April 2013 Accepted: 12 December 2013 Published: 25 July 2014

Citation: Hadi MA, Rao RN, Rao SA. Formulation and Evaluation of pH-Responsive Mini-Tablets for Ileo-Colonic Targeted Drug Delivery. Trop J Pharm Res 2014; 13(7):1021-1029 doi: 10.4314/tjpr.v13i7.3

© 2014 The authors.
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Abstract

Purpose: To formulate and evaluate a novel pH-responsive mini-tablet for ileo-colonic targeted delivery of naproxen in chronotherapeutic treatment of rheumatoid arthritis.

Methods: Core mini-tablets were prepared by direct compression method. These prepared core mini-tablets were then coated with enteric coating polymers, i.e., Eudragit L100 and Eudragit S100 in different ratios and concentrations and filled into an empty hydroxypropyl methylcellulose (HPMC) capsule. Fourier transform infrared spectroscopy (FTIR) and diffraction scanning calorimetry (DSC) studies on the pure drug and its combination with polymers were performed to assess compatibility. The formulations were also characterized for drug content, in-vitro drug release and stability.

Results: FTIR and DSC data show that there was no interaction between the drug and the polymers. All the physicochemical properties of the core mini-tablets were within acceptable limits. Drug content was 99.42 ± 0.15 %. Optimized formulation F12 released drug after a lag time of 5.02 ± 0.4 h, with 99.40 ± 0.4 % of the drug released at the end of 8 h. It was also stable for a period of 6 months based on International Conference on Harmonization ICH guidelines.

Conclusion: A novel pH-responsive mini-tablet formulation of naproxen has been successfully developed for the chronotherapeutic treatment of rheumatoid arthritis.

Keywords: Ileo-colonic targeted delivery, Naproxen, Mini-tablets, Hydroxypropyl methylcellulose , Chronotherapeutic, Enteric coat, Rheumatoid arthritis