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概要

Formulation and Evaluation of Licozinat Matrix Tablet

Otgonsuren D, Davaasuren TS, Enkhtuul B, Davaadagva D and Jambaninj D

Objective: Monoammonium glycyrrhizinate of Glycyrrhiza root has been used as an expectorant, detoxificator, anti-allergic, and antioxidant. Japanese researchers have been determined it has anti-viral activity in case of hepatitis A, B, C, D. We have isolated monoammonium glycyrrhizinate from Glycyrrhiza root, grown in Mongolia through a method presented in a previous study. The objective of the study was to develop prolonged release matrix tablet with hepatoprotective effect and to evaluate their pharmacotechnical qualities and the in vivo performance. Licozinat matrix tablets contained monoammonium glycyrrhizinate 140 mg; glycine 50 mg; LD-methionin 50 mg in each tablet.

Methods: In the present study the matrix tablet were prepared using HPMC K4000, lactose, glucose, microcrystalline cellulose, PVP-K30, talc and magnesium stearate in different ratios. The matrix tablet were prepared by wet granulation method and evaluated for weight variation, hardness, friability, in-vitro release, and in vivo study.

Results: Appropriate excipients were chosen for the matrix tablets: lactose as a diluent, 5% of PVP-K30 as a binder, HPMC as a matrix former, 3% of talc and 1% of magnesium stearate as a glidiant or lubricant. We have prepared the matrix tablets by wet granulation method and compressed the tablet mixture by a 2.5 kPa pressure. Formulation 5 (F5) was determined to be the most appropriate tablet design and it released the drug in a prolonged way during the in vitro testing. The hepatoprotective effect of matrix tablet in comparison to Glycyron tablet, were studied on CCl₄ induced hepatotoxicity in rats. The effect of Licozinat matrix tablet were compared with the Glycyron tablet that were administered to CCl₄ treated rats. On administration Licozinat matrix tablet decreased the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin and alkaline phosphatise (ALP).

Conclusion: We have developed and evaluated prolonged/controlled release matrix tablets with hepatoprotective effect. The Licozinat matrix tablets satisfied the quality criteria. On administration Licozinat matrix tablet decreased the level of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin and alkaline phosphatise (ALP).