Development of trilayered mucoadhesive tablet of itraconazole with zero-order release

Main Article Content

Ashwini Madgulkar
Shivajirao Kadam
Varsha Pokharkar


Itraconazole is practically insoluble in water; large interindividual and intraindividual variations of its oral bioavailability are reported. A mucoadhesive drug delivery system is useful to prolong the retention time of a dosage form in the stomach,thereby improving the oral bioavailability of the drug. Solid dispersion of itraconazole with Eudragit E100 was prepared by spray-drying method to improve dissolution. Trilayered mucoadhesive tablet was prepared, with inner core containing solid dispersion of the drug and with carbopol and HPMC sandwiched between two layers of hydrophilic mucoadhesive polymer mixture of carbopol and Hydroxypropyl methyl cellulose (HPMC). Amounts of Carbopol 934P (CP) and Methocel K4M (HPMC) were varied in the outer coat around the solid dispersion. The drug-release pattern for all the formulation combinations was found to be nonfickian, approaching zero-order kinetics. Suitable combination of two polymers provided adequate bioadhesive strength and sustained-release profile with zero-order kinetics.


Download data is not yet available.

Article Details

How to Cite
Madgulkar, A., Kadam, S., & Pokharkar, V. (2014). Development of trilayered mucoadhesive tablet of itraconazole with zero-order release. Asian Journal of Pharmaceutics (AJP), 2(1).


Grant S, Clissold S. Itraconazole: A review of pharmacodynamics and

pharmacokinetic properties and therapeutic use in superficial and

systemic mycosis. Ind Drugs 1989;37:310-4.

Jacob J, Bassett M, Carter B. Pharmacokinetics of bioadhesive,

gastroretentive, controlled release tablets of itraconazole. Available

from: DS, Fessi H, Devissaguet JP, 3. Puisieux F. Comparative study of the association of itraconazole with colloidal drug carriers. Drug Dev Res 1996;38:125-33.

Nur AO, Zhang JS. Captopril floating and/or bioadhesive tablets: Design

and release kinetics. Drug Dev Ind Pharm 2000;26:965-9.

Khanna R, Agarwal SP, Ahuja A. Muco-adhesive buccal tablets of

clotrimazole for oral candidiasis. Drug Dev Ind Pharm 1997;23:831-7.

Narendra C, Shrinath MS. Development of three layered buccal compact

containing metoprolol tartrate by stastical optimization technique. Int

J Pharm 2005;304:102-14.

Ceschel GC, Maffei P, Badiello R. Optimization of hydrochlorothiazide

tablets. Drug Dev Ind Pharm 1999;25:1167-76.

Kim J. Method and composition of an oral preparation of itraconazole.

United States Patent 6485743.

Gupta A, Garg S, Khar RK. Measurement of bioadhesive strength of

mucoadhesive buccal tablets: Design of an in vitro assembly. Ind Drugs


Junginger HE. Bioadhesive polymer systems for peptide delivery. Acta

Pharm Technol 1993;36:110-26.

Li C, Bhatt PP, Johnston TP. Evaluation of a mucoadhesive buccal patch

for delivery of peptides: In vitro screening of bioadhesion. Drug Dev

Ind Pharm 1998;24:919-26.

Machida Y, Nagai T. Bioadhesive preparation as topical dosage forms.

In: Bioadhesive Drug Delivery Systems. Athiowitz E, Chickering DE,

Lehr CM, editors. New York: Marcel Dekker; p. 646-7.

Perez-Marcos B, Ford D, Jajafi M, Adrangni M. Release of propranolol

HCl from matrix tablets containing hydroxy propyl methyl cellulose K4

M and carbopol 974. Int J Pharm 1994;111:251-9.