Journal :   Research Journal of Pharmacy and Technology

Volume No. :   2

Issue No. :  2

Year :  2009

Pages :   396-404

ISSN Print :  0974-3618

ISSN Online :  0974-360X


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Formulation and In-vitro Evaluation of Buccoadhesive Tablets containing Ketoconazole inclusion complex with β- Cyclodextrin



Address:   Dattatreya B Udgirkar1*, SN Hiremath2, K Sreenivasa Rao1 and Dilip Pawar2
1Dept. of Pharmaceutics. R.R.K. Samithi’s College of Pharmacy, Bidar, Karnataka, India.
2Dept. of Pharmaceutics. Pravara Rural Education Society’s, College of Pharmacy, Chincholi, Nasik, (MS) India
*Corresponding Author
DOI No:

ABSTRACT:
The Goal of the present investigation was to design and evaluate a tablet for buccal delivery of poorly water-soluble drug Ketoconazole (KTZ). This is a broad spectrum imidazole derivative useful in treatment of oropharyngeal candidiasis, the most common infection in AIDS patients. Hydroxypropyl methylcellulose (HPMC K4M) and Carbopol 934P (C934P) were used as candidate of bioadhesive polymers and Ethyl cellulose (EC) as backing material. Solubility of KTZ is increased by complexation with ß-Cyclodextrin (ß-CD) and then delivery via buccal mucosa. The solubility studies demonstrated the formation of KTZ- ß-CD inclusion complex with 1:1 stoichiometry. The complexation was characterized by differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR) and X-ray diffractometry (X-RD). The buccoadhesive tablets for the delivery of KTZ were prepared by 32 factorial designs; direct compression of HPMC K4M and Carbopol 934P. The tablets were evaluated for their dissolution, surface pH, swelling study and mucoadhesive properties. The In-vitro release results demonstrated that drug is released by non-Fickian diffusion mechanism with zero order kinetics. From the drug release data, formulation F1 has shown highly satisfactory values for dissolution parameters and considered as the optimized buccal tablet for improved bioavailability. The feasibility of buccal administration of KTZ was assessed by permeation experiments on sheep excised mucosa. Our results demonstrate that, as there was increase in drug release rate from the tablets in solution as well as permeated through sheep buccal mucosa. This study shows great potential for buccal administration.
KEYWORDS:
Ketoconazole; β- Cyclodextrin; Optimization; Buccal delivery.
Cite:
Dattatreya B Udgirkar, SN Hiremath, K Sreenivasa Rao, Dilip Pawar. Formulation and In-vitro Evaluation of Buccoadhesive Tablets containing Ketoconazole inclusion complex with β- Cyclodextrin. Research J. Pharm. and Tech.2(2): April.-June.2009,;Page 396-404.
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