Formulation and evaluation of enteric coated microcapsules of diclofenac sodium for modified release by combination of wet granulation and thermal change method
Keywords:Diclofenac sodium, microcapsules, factorial design, wet granulation, thermal change method
The purpose of the present work was to develop optimized novel enteric microcapsules containing diclofenac sodium, a non steroidal anti inflammatory drug (NSAID) used for rheumatoid arthritis, for improved delivery and to diminish its adverse effect after oral administration. The microcapsule was prepared by using different polymers and the enteric coating was provided by using an innovative technique combining wet granulation method and thermal change method. This work also investigated different levels of enteric polymers like cellulose acetate phthalate (CAP) (X1) and ethyl cellulose (EC) (X2) and the stirring speed during coating ethyl cellulose (X3), by using 23 full factorial design. The dependent variables assessed were % yield (Y1), Q8 (% drug released after 8 hour) (Y2), n (Diffusion coefficient) (Y3), DEE (Drug entrapment efficiency) (Y4). The main effect and interaction terms were quantitatively evaluated using a mathematical model. The prepared microcapsules were evaluated for percentage drug dissolved, scanning electron microscopy, drug excipient interaction, angle of repose, particle size. Mean dissolution time (MDT) was used to compare dissolution patterns obtained. The results showed that X1 and X2 significantly affected the release properties.
S. C Sweetman, Martindale–The complete drug reference. 33rd ed. Pharmaceutical Press, Great Britain 2002. pp. 30 – 32
T.J. Roseman, N.F. Cardinelli, in Controlled-release Technologies, Vol. 1 (A. F. Kydonieus, ed), CRC Press, Boca Raton, FL, 1980.
E.A. Hosny, G.M. el Mahrouk, M.W. Gouda, Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads, Drug Dev. Ind. Pharm. 24 (7) (1998) 661–663; DOI:10.3109/03639049809082368
J.I. Perez-Martinez, E. Morillo, C. Maqueda, J.M. Gines, Ethyl cellulose polymer microspheres for controlled release of norfluazon, Pest. Manag. Sci. 57 (2001) 688–694; DOI: 10.1002/ps.339
G.F. Palmieri, S. Michelini, P. Di Martino, S. Martelli, Polymers with pH-dependant solubility: possibility of use in the formulation of gastroresistant and controlled release matrix tablets, Drug Dev. Ind. Pharm. 26 (2000) 837–845; DOI:10.1081/DDC-100101307
J.B. Schwartz, R.E. O’Connor, Optimization techniques in pharmaceutical formulation and processing In Modern Pharmaceutics (Ed. G.S. Banker, C.T. Rhodes,) 3rd ed. Marcel Dekker, New York 1997 pp. 727–752.
M.F. Al-Omran, S.A. Al-Suwayeh, A.M. El-Helw, S.I. Saleh. Taste masking of diclofenac sodium using microencapsulation. J. Microencapsulation, 19 (1) 2002, 45 – 52 DOI:10.1080/ 02652040110055612
Subrahmanyam C.V.S, Setty J.T., Kusumdevi V., Suresh S. Laboratory manual of Pharmaceutical Engineering. 1st edition Vallabh Publications, New Delhi 2006. 27 – 34
H. Abdelkader, O.Y. Abdalla, H. Salem, Formulation of controlled release based biclofenac matrix tablets: Influence of some hydrophilic polymers on the release rate and in vitro evaluation. AAPS Pharm Sci Tech, 8(4) 2007: E100; DOI:10.1208/pt0804100
Y. Rane, R. Mashru, M. Sankalia, J. Sankalia, Effect of hydrophilic swellable polymers on dissolution enhancement of Carbamazepine solid dispersions studied using response surface methodology. AAPS PharmSciTech, 8(2) 2007 Article 27: DOI:10.1208/pt0802027
Moffat AC, Osselton MD, Widdop B, editors. Clarke’s Analysis of Drugs and Poisons. Great Britain: Pharmaceutical Press. 2004
A. Martin, Micromeritics In Physical Pharmacy (Ed. A Martin). 4th ed. B.I Waverly Pvt. Ltd., New Delhi, 1999 pp. 423 – 452
B.C. Hancock, M. Park, What is true solubility advantage for amorphous pharmaceuticals? Pharm Res 28 2000, 1001 – 1013
How to Cite
Copyright (c) 2020 Sanjib Bahadur, Pragya Baghel, Ranabir Chanda, Amit Roy, Suman Saha, Ananta Choudhury
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
In submitting an article to Journal of Applied Pharmaceutical Research (JOAPR) I certify that:
- I am authorized by my co-authors to enter into these arrangements.
- I warrant, on behalf of myself and my co-authors, that:
- the article is original, has not been formally published in any other peer-reviewed journal, is not under consideration by any other journal and does not infringe any existing copyright or any other third party rights;
- I am/we are the sole author(s) of the article and have full authority to enter into this agreement and in granting rights to JOAPR are not in breach of any other obligation;
- the article contains nothing that is unlawful, libellous, or which would, if published, constitute a breach of contract or of confidence or of commitment given to secrecy;
- I/we have taken due care to ensure the integrity of the article. To my/our - and currently accepted scientific - knowledge all statements contained in it purporting to be facts are true and any formula or instruction contained in the article will not, if followed accurately, cause any injury, illness or damage to the user.
- I, and all co-authors, agree that the article, if editorially accepted for publication, shall be licensed under the Creative Commons Attribution-NonCommercial 4.0 International License
- I, and all co-authors, agree that, if the article is editorially accepted for publication in Journal of Applied Pharmaceutical Research (JOAPR) data included in the article shall be made available under the Creative Commons 1.0 Public Domain Dedication waiver, unless otherwise stated. For the avoidance of doubt it is stated that sections 1, 2, and 3 of this license agreement shall apply and prevail.