Dissolution enhancement of gliclazide by preparation of inclusion complexes with β-cyclodextrin

S N Hiremath, R K Raghavendra, F Sunil, L S Danki, M V Rampure, P V Swamy, U V Bhosale

Abstract


Gliclazide is an oral hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus. The drug is
practically insoluble in water and exhibits an exceedingly slow intrinsic dissolution rate and poor bioavailability. The
present study has emphasized on improving the solubility and dissolution rate of the drug by forming inclusion complex
with β-cyclodextrin. Phase solubility studies indicated the formation of 1:2 M complex in solution. The value of apparent
stability constant Kc was found to be 691.45 M–1. The inclusion complexes were prepared by physical mixture and kneading
method. Prepared complexes were characterized by infrared (IR) spectroscopy and differential scanning calorimetry (DSC)
studies, which indicated formation of 1:2 M complex. The gliclazide:β-CD (1:2 M) complex prepared by kneading method
exhibited higher dissolution rate and dissolution efficiency values in 0.1-N HCl. A 20.31-fold increase in dissolution rate
and 16.50-fold increase in dissolution efficiency values were observed in the kneading method.
Key words: β-cyclodextrin, gliclazide, kneading method, physical mixture

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References


Loftssan T, Brewster ME. Pharmaceutical applications of cyclodextrins 1:

Solubilizations and stabilization. J Pharma Sci 1996;85:1017-25.

Rajewski RA, Stella VJ. Pharmaceutical applications of cyclodextrins 2:

In vivo drug delivery. J Pharma Sci 1996;85:1142-69.

British Pharmacopoeia, Department of health and social services.

London: HMSO; 1993, (International edition addendum 1996), 1782.

Available from: http://www.medsafe.govt.nz/profs/datasheet/a/

apoglyclazidetab.htm.

Martindale, The complete drug reference, 33rd ed. London:

Pharmaceutical Press; 2002. p. 321-2.

Higuchi T, Connors KA. Phase-solubility techniques. Adv Anal Chem

Instr 1965;4:117-22.

Aithal KS, Udupa N, Sreenivasan KK. Physicochemical properties of

drug cyclodextrin complexes. Indian Drugs 1995;32:293-303.

Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol

;27:27-48.




DOI: http://dx.doi.org/10.22377/ajp.v2i1.335

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