FORMULATION AND IN VITRO EVALUATION OF RITONAVIR FLOATING TABLETS BY MELT GRANULATION TECHNIQUE
DOI:
https://doi.org/10.22159/ijap.2016v8i3.11113Keywords:
Gelucire 4301, Gelucire 5002, Geleol pellets, Swelling behaviorAbstract
Objective: The purpose of this study was to formulate Ritonavir floating matrix tablets by melt granulation technique in order to prolong its gastric residence time thereby increasing its bioavailability.
Methods: The Ritonavir tablets were prepared by melt granulation technique, using carriers such as Gelucire 43/01, Gelucire 50/02 and Geleol pellets alone or in combinations. Ethyl cellulose was used as drug release rate retarding agent and sodium bicarbonate was used as gas generating agent. The prepared granules were subjected to pre and post compressional parameters. The formulations were optimized on the basis of matrix integrity, duration of floating, swelling behavior and In vitro drug release.
Results: The drug-excipients compatibility studies were performed by FT-IR and the study revealed that there is no drug excipients interaction. A combined matrix system containing Gelucire 43/01: Gelucire 50/02 with 1:1 concentration along with HPMC K 15 M shows good drug release pattern with less floating lag time and increased floating duration.
Conclusion: The in vitro drug release pattern of Ritonavir floating tablets was fitted to different kinetic models which showed the highest regression for Zero order kinetics with Higuchi mechanism.
Keywords: Gelucire 43/01, Gelucire 50/02, Geleol pellets, Swelling behavior
Downloads
References
Bulgarelli E, Forni F, Bernabei MT. Effect of matrix composition and process conditions on casein-gelatin beads floating properties. Int J Pharm 2000;198:57-65.
Singh BN, Kim KH. Floating drug delivery system: an approach to the controlled drug delivery via gastric retention. J Controlled Release 2000;63:235â€59.
Nur AO, Zhang JS. Captopril floating and/or bioadhesive tablets: design and release kinetics. Drug Dev Ind Pharm 2000;26:965-9.
Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a novel controlled-release system for gastric retention. Pharm Res 1997;14:815–9.
Kumar K, Shah MH, Ketkar AR, Kadam SS, Paradkar A. Effect of drug solubility and different excipients on floating behavior and release from glyceryl mono-oleate matrices. Int J Pharm 2004;272:151-60.
S Sarojini, R Manavalan. An overview on various approaches to gastro retentive dosage formsâ€. Int J Drug Dev Res 2012;4:1-13.
Dasharath M Patel, Natavarlal M Patel, Viral F Patel, Darshini A Bhatt. Floating granules of rantidine hydrochloride-gelucire 43/01: formulation optimization using factorial design. AAPS PharmSciTech 2007;8:E1-E7.
Dennis AB, Farr SJ, Kellaway IW, Taylor G, Davidson R. In vivo evaluation of rapid release and sustained release gelucire capsule formulations. Int J Pharm 1990;65:85-100.
Sutananta W, Craig DQM, Newton JM. The effects of aging and thermal behaviour and mechanical properties of pharmaceutical glycerides. Int J Pharm 1994;111:51-62.
Ainaoui A, Ouriemchi EM, Bidah D, EI Amram MK, Vergnaud JM. The process of drug releases with oral dosage forms with lipidic gelucire matrix. J Polym Eng 1997;17:245-57.
Ainaoui A, Vergnaud JM. Modeling the plasma drug level with oral dosage forms with lipidic gelucire matrix. Int J Pharm 1998;168:155-62.
Shyam Shimpi, Bhaskar Chauhan, KR Mahadik, Anat Paradkar. Preparation and evaluation of diltiazem hydrochloride-gelucire 43/01 floating granules prepared by melt granulation. AAPS PharmSciTech 2004;5:1-6.
Mahaparele PR, Kasture PV, Deshmukh SS, Kuchekar BS. Sustained release matrices of metoprolol succinate using compritol 888 ATO and precirol ATO 05. J Pharm Res 2006;5:10-4.
Paradkar AR, Maheswari M, Chauhan MB. Sustained release matrices of Metformin hydrochloride and glyceryl behenate. Indian Drugs 2004;41:350-3.
Patel NM, Soniwala MW. Influence of release enhancer on the release of Vanlafaxine hydrochloride from glyceryl behenate matrix tablet. Indian Drugs 2008;45:98-104.
Richard W Korsmeyer, Robert Gurny, Eric Doelker, Pierre Buri, Nikolaos A Peppas. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.
Peppas NA. Analysis of fickian and non-fickian drug release from polymers. Pharm Acta Helv 1985;60:110-1.
Published
How to Cite
Issue
Section
