FORMULATION OF TERFENADINE CONTROLLED-RELEASE MATRICES

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HANAEI J.; BARZEGAR JALALI M.

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Journal: PHARMACEUTICAL SCIENCES Year:2005 | Volume:- | Issue:3 Page(s): 9-13

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Title

FORMULATION OF TERFENADINE CONTROLLED-RELEASE MATRICES

Author(s)

HANAEI J. | BARZEGAR JALALI M. | Issue Writer Certificate

Keywords

TEIFENADINEQ2

HPMC MATRIXQ2

COMPRESSION PRESSUREQ2

RELEASE RATEQ2

SUSTAINED-RELEASEQ2

Abstract

OBJECTIVES: Terfenadine, as an antihistaminic agent. is widely used to control seasonal allergy such as rhinitis. Terfenadine is in fact a prodrug and is rapidly absorbed from the gastrointestinal tract It undergoes extensive first-pass metabolism in the liver to its active metabolite the carboxylic acid derivative fexofenadine. Sustained or controlled- release dosage forms favor the strategy of therapy by minimizing the side effects via reducing terfenadine plasma concen1ration which is the main cause of its cardiotoxicity as well as maximizing the patient compliance. However, few studies have been conducted to formulate the controlled-release dosage forms. Thus, in the current investigation in an attempt to formulate oral controlled-release terfenadine. METHODS: We have directly compressed terfenadine with a designated mixture of hydroxypropyl methylcellulose (HPMC) and magnesium stearate using 13.5, 54.0 and 67.5 MPa COMPRESSION PRESSURE. Also two conventiona tablets (home and foreign made) as well as the drug powder were included in the release studies. The content uniformity of the matrices and the tablets were assessed. Further, the release profiles of the prepared matrices were evaluated exploiting various classical kinetics models i.e., Weibull, Hixon-Crowell cube root, Higuchi square root of time, probability linear and log linear, first-order, zero-order and polynomial model comprising erosion and diffusion terms. Among the models used, the data was fitted best to the polynomial model with lag time. RESULTS: No significant difference was detected for content uniformity. The release of the drug from the matrices was markedly dependent on the COMPRESSION PRESSURE, that is the higher the pressure the lower is the RELEASE RATE and hence the longer the complete release time. The complete release times were 480, 510 and 570 min for the COMPRESSION PRESSURE of 13.5, 54.0 and 67.5 MPa, respectively. The conventional tablets and the drug powder exhibited rapid dissolution compared to matrices. CONCLUSION: Based upon our results, it appears that the terfenadine HPMC MATRIX provides reliable sustained characteristics from RELEASE RATE point of view.

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APA: Copy

HANAEI, J., & BARZEGAR JALALI, M.. (2005). FORMULATION OF TERFENADINE CONTROLLED-RELEASE MATRICES. PHARMACEUTICAL SCIENCES, -(3), 9-13. SID. https://sid.ir/paper/48552/en

Vancouver: Copy

HANAEI J., BARZEGAR JALALI M.. FORMULATION OF TERFENADINE CONTROLLED-RELEASE MATRICES. PHARMACEUTICAL SCIENCES[Internet]. 2005;-(3):9-13. Available from: https://sid.ir/paper/48552/en

IEEE: Copy

J. HANAEI, and M. BARZEGAR JALALI, “FORMULATION OF TERFENADINE CONTROLLED-RELEASE MATRICES,” PHARMACEUTICAL SCIENCES, vol. -, no. 3, pp. 9–13, 2005, [Online]. Available: https://sid.ir/paper/48552/en

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