NDLI: Floating Tablet of Trimetazidine Dihydrochloride: An Approach for Extended Release with Zero-Order Kinetics

Content Provider	Springer Nature Link
Author	Abdelbary, Ahmed El Gazayerly, Omaima N. El Gendy, Nashwa A. Ali, Adel A.
Copyright Year	2010
Abstract	Trimetazidine dihydrochloride is an effective anti-anginal agent; however, it is freely soluble in water and suffers from a relatively short half-life. To solve this encumbrance, it is a prospective candidate for fabricating trimetazidine extended-release formulations. Trimetazidine extended-release floating tablets were prepared using different hydrophilic matrix forming polymers including HPMC 4000 cps, carbopol 971P, polycarbophil, and guar gum. The tablets were fabricated by dry coating technique. In vitro evaluation of the prepared tablets was performed by the determination of the hardness, friability, content uniformity, and weight variation. The floating lag time and floating duration were also evaluated. Release profile of the prepared tablets was performed and analyzed. Furthermore, a stability study of the floating tablets was carried out at three different temperatures over 12 weeks. Finally, in vivo bioavailability study was done on human volunteers. All tablet formulas achieved <0.5 min of floating lag time, more than 12 h of floating duration, and extended t $_{1/2}$. The drug release in all formulas followed zero-order kinetics. T4 and T8 tablets contained the least polymer concentration and complied with the dissolution requirements for controlled-release dosage forms. These two formulas were selected for further stability studies. T8 exhibited longer expiration date and was chosen for in vivo studies. T8 floating tablets showed an improvement in the drug bioavailability compared to immediate-release tablets (Vastrel® 20 mg).
Starting Page	1058
Ending Page	1067
Page Count	10
File Format	PDF
Journal	AAPS PharmSciTech
Volume Number	11
Issue Number	3
e-ISSN	15309932
Language	English
Publisher	Springer US
Publisher Date	2010-06-26
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Pharmacy Biochemistry Biotechnology Pharmacology/Toxicology
Content Type	Text
Resource Type	Article

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