Main Article Content
HP-Î²-Cyclodextrin. The complexes of mefenamic acid with Î²-Cyclodextrin and HP-Î²-Cyclodextrin were prepared by kneading method and were characterized and evaluated to study the effect of complexation on dissolution profiles and
in vivo advantage. The complexes were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, and differential scanning calorimetry studies. Phase solubility studies indicated complex formation with possible stoichiometry of 1:1 and a stability constant of 176 M-1 for Î²-Cyclodextrin and 103.8 M-1 for HP-Î²-Cyclodextrin. The characterization studies confirmed the inclusion of mefenamic acid within the nonpolar cavity of Î²-Cyclodextrin and of HP-Î²-Cyclodextrin. Remarkable improvement was observed in the in vitro drug release profiles in 0.1-N HCl and pH-6.8 phosphate buffer with
all complexes. Mefenamic acid also showed improvement in the in vivo activity when administered orally to rats as compared
with mefenamic acid per se.
This is an Open Access article distributed under the terms of the Attribution-Noncommercial 4.0 International License [CC BY-NC 4.0], which requires that reusers give credit to the creator. It allows reusers to distribute, remix, adapt, and build upon the material in any medium or format, for noncommercial purposes only.
Duchene D, Wouessidjewe D. Pharmaceutical uses of cyclodextrins and
derivatives. Drug Dev Ind Pharm 1990;16:2487-99.
Bekers O, Uijtendaal E, Beijnen J, Bult A, Underberg W. Cyclodextrins
in the pharmaceutical field. Drug Dev Ind Pharm 1991;17:1503-49.
Duchene D, Vaution D, Glomot F. Cyclodextrins their value in
pharmaceutical technology, Drug Dev Ind Pharm 1986;12:2193-215.
Menard F, Dedhiya MG. Physicochemical aspects of the complexation of
some drug with cyclodextrins. Drug Dev Ind Pharm 1990;16:91-113.
Aithal K, Udupa N, Sreenivasan K. Physicochemical properties of drug-
cyclodextrin complexes. Indian Drugs 1995;32:293-305.
Sanghavi N, Choudhary K, Matharu R, Viswanathan L. Inclusion
complexation of lorazepam with Î²-cyclodextrin. Drug Dev Ind Pharm
Vromans H, Eissens AC, Lerk CF. Mechanism of dissolution of drug-
cyclodextrin complexes. Acta Pharm Technol 1989;35:250-5.
Derle DV, Gujar KN. A critical study of analgesic, anti-pyretic and anti-
inflammatory activity of ibuprofen vs. ibuprofen and paracetamol
combination in animals. Indian Drugs 2001;7:368.
Shenoy A, Shenoy V. Antibacterial Agents, in Handbook of
Pharmaceutical Chemicals, 1st ed, Navi Mumbai: Multi-tech Publishing
Co; 2000. p. 168-9.
Khazaimia Ahereh T, Fakhreddin J. A comparison of gastrointestinal
permeability induced by diclofenac-phospolipid complex with
diclofenac acid and its sodium salts. J Pharm Sci 2003;6:352-9.
Raynolds J. Antibacterial Agents, Martindale The Extra Pharmacopoeia,
st ed, London: Royal Pharmaceutical Society; 1996. p. 272.
Higuchi T, Connors KA. Phase solubility techniques. Adv Anal Chem
Masson M, Sigurdardottir B, Matthiasson K, Loftsson J. Investigation
of drug-cyclodextrin complexes by a phase-distribution method:
Some theoretical and practical considerations. Chem Pharm Bull
Reddy M, Murthy T, Raju G, Muralikrishna J, Seshukumar K, Sankar D.
New spectrophotometric methods for the determination of
roxithromycin. Indian J Pharm Sci 2002;64:73-5.
Derle DV, Shinde S, Gujar KN. Inclusion complexation of roxithromycin
with Î²-cyclodextrin. Int J Pharm Excipient 2003;7:95-100.
Baboota S, Dhaliwal M, Kohli K. Physicochemical characterization,
in vitro dissolution behavior and pharmacodynamic studies of roficoxib-
Î²-cyclodextrin inclusion compounds: Preparation of roficoxib-HP-Î²-
cyclodextrin inclusion complex, A technical note. AAPS PharmSciTech
Winter C, Risley E, Nuss G. Carrageenan-induced edema in hind paw
of rats as an assay for anti-inflammatory drugs. Proc Soc Exp Bio Med
Derle DV, Gujar KN. Anti-inflammatory, analgesic and anti-pyretic activity
of Acorus Calamus and Curcuma Amada. Indian Drugs 2001;8:444.
Lu W, Zhang Q, Zheng L, Wang H, Li R, Zhang L. Antipyretic, analgesic
and anti-inflammatory activities of ketoprofen Î²-cyclodextrin inclusion
complexes in animals. Biol Pharm Bull 2004;27:1515-20.
Ulaleye S, Farombi E, Adewoye E, Owayele B, Onasanso S, Elegbe R.
Analgesic and anti-inflammatory effects of Kolaviron (A Garcina Kola
Seed Extract). Afr J Biomed Res 2000;3:171-4.
Best J, Kahn J. Research in Education, 7th ed, New Delhi: Prentice-Hall
of India Private Limited; 1999. p. 362-5.
Brown M. Introduction to thermal analysis: Techniques and applications.
New York: Chapmann and Hall; 1988. p. 121-4.
Reddy N, Ramakrishna S, Chowdary K, Diwan P. Î²-cyclodextrin complex
of celecoxib: Molecular modeling, characterization and dissolution
studies. AAPS PharmSciTech 2004;6:7.
Tahereh K, Fakhreddin J. A comparison of gastrointestinal permeability
induced by diclofenac-phospolipid complex with diclofenac acid and
its sodium salts. J Pharm Sci 2003;6:352-9.
McEwen J. Clinical pharmacology of piroxicam Î²-cyclodextrin: Implications
for innovative patient care. Clin Drug Investig 2000;19:27-31.
Dolina A, Santoyo S, Ygartua S. Influence of piroxicam: HP- Î²-cyclodextrin
complexation on in vitro permeation and skin retention of piroxicam.
Skin Pharmacol Appl Skin Physiol 2001;14:97-107.