DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEM FOR RITONAVIR TABLETS USING NATURAL POLYMERS

Saritha Chukka; Shayeda Shaik

doi:10.22159/ajpcr.2017.v10i5.17266

Authors

Saritha Chukka Kakatiya university
Shayeda Shaik University College of Pharmaceutical Sciences, Kakatiya University, Warangal

DOI:

https://doi.org/10.22159/ajpcr.2017.v10i5.17266

Keywords:

Ritonavir, floating tablets, gastric residence time, gastroretentive drug delivery system

Abstract

Objective: The present study involves preparation and evaluation of floating tablets of ritonavir for improving the drug bioavailability by prolongation of gastric residence time.

Ritonavir is an antiretroviral agent used in treatment of HIV and viral diseases has been taken as a model drug in the present investigation because of its low biological half life (3-5h). Moreover it is primarily absorbed from stomach.

Materials and Methods: Ritonavir floating tablets were prepared by the dry granulation technique, using guar gum and xanthan gum as polymers, sodium bicarbonate as effervescent agent, PVP as binding agent, Di calcium phosphate as diluents, Crospovidone as swelling agent and magnesium stearate as lubricant. The prepared tablets were evaluated for various physico-chemical parameters.

Â Results: Drug-excipient interaction studies were conducted by FTIR and DSC. The results suggested that there was no incompatibility between the drug and polymers. The prepared tablets were evaluated for their physical characteristics. All the parameters were within the pharmacopoeial limits.Â Further, tablets were also studied for their floating properties and in vitro drug release characteristics. The tablets exhibited controlled and prolonged drug release profiles. The developed formulation was found to be stable.Â

Conclusion: The developed floating tablets of ritonavir exhibit prolonged release upto 12 h, and thus may improve bioavailability and minimize fluctuations in plasma drug concentrations.

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Author Biography

Saritha Chukka, Kakatiya university

Pharmaceutics

References

REFERENCES

Streubel, A., Siepmann, J., Bodmeier, R. Gastroretentive drug delivery systems.

Expert Opin. Drug Deliv. 2006; 3 (2): 217-233.

Streubel, A., Siepmann, J., Bodmeier, R., Drug delivery to the upper small intestine window using gastroretentive technologies. Curr. Opin. Pharmacol. 2006; 6: 501-508.

Groning, R., Heun, G. Oral dosage forms with controlled gastrointestinal transit. Drug Develop. Indust. Pharm. 1984; 1: 527-539.

Fujimori, J., Machida, Y., Tanaka, S., Nagai, T. Effect of magnetically controlled gastric residence of sustained release tablets on bioavailability of acetaminophen. Int. J. Pharm. 1995; 119: 47-55.

Dhaliwal, S., Jain, S., Singh, H.P., Tiwary, A.K. Mucoadhesive microspheres for gastroretentive delivery of acyclovir. In vitro and in vivo evaluation. AAPS J. 2008; 10: 322-330.

Deshpande, A.A., Shah, N.H., Rhodes, C.T., Malick, W. Development of a novel controlled-release system for gastric retention. Pharm. Res. 1997; 14: 815-819.

Baumgartner, S., Kristl, J., VrecË‡er, F., Vodopivec, P., Zorko, B. Optimisation of floating matrix tablets and evaluation of their gastric residence time. Int. J. Pharm. 2000;195: 125-135.

Devereux, J.E., Newton, J.M., Short, M.B. The influence of density on the gastrointestinal transit of pellets. J. Pharm. Pharmacol. 1990;42: 500-501.

Pistell PJ, Gupta S, Knight AG, Domingue M, Uranga RM, Ingram DK, Kheterpal I, Ruiz C, Keller JN, Bruce-Keller AJ, Metabolic and neurologic consequences of chronic lopinavir/ritonavir administration to C57BL/6 mice, Antiviral Research. 2010;88: 334-342.

Law D, Schmitt EA, Marsh KC, Everitt EA, Wang W, Fort JJ, Krill SL, Qiu Y, Ritonavir- PEG 8000 Amorphous Solid Dispersions: In Vitro and In Vivo Evaluations, J Pharm Sci. 2004; 93: 563-570.

Law D, Krill SL, Schmitt EA, Fort JJ, Qiu Y, Wang W, Porter WR, Physicochemical Consideration in the preparation of Amorphous Ritonavir- Poly(ethylene glycol) 8000 Solid Dispersions, J Pharm Sci 2001;90:1015-1026.

United States Pharmacopoeia. US Pharmacopoeial Convention. Inc. Rockville MD. Asian ed; XXXI: pp. 2008; 3200-3201.

Williams GC, Sinko PJ, Oral absorption of the HIV protease inhibitors: a current update, Adv Drug Del Rev. 1999; 39: 211-238.

Kim RB, From MF, Wandel C, Leake B, Wood AJJ, Roden DM, The drug transporter P-Glycoprotein limits oral absorption and brain entry of HIV-1 Protease Inhibitors, J Clin Invest. 1998; 101: 289-294.

Aungst BJ, P-glycoprotein, secretory transport, and other barriers to the oral delivery of anti-HIV drugs, Adv Drug Del Rev. 1999; 39: 105-116.

T. Higuchi, Mechanism of sustained action medication, J. Pharm. Sci. 1963; 52: 1145-1149.

R.W. Korsmeyer, R. Gurny, E. Docler, P. Buri, N.A. Peppas, Mechanism of solute release from porous hydrophilic polymers, Int. J. Pharm. 1983; 15: 25-35.

Mathews BR. Regulatory aspects of stability testing in Europe. Drug Dev. Ind. Pharm. 1999; 25: 831-856.

M.N. Gambhire, K.W. Ambade, S.D. Kurmi, V.J. Kadam, K.R. Jadhav, Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride, AAPS PharmSciTech. 2007; 8 (3): E1â€“E9 (Article 73).

United States Pharmacopeia 27 and National Formulary 22, Asian Edition, United States Pharmacopeial convention, Inc., Rockville, 2004 (electronic version).

Brahma NS, Know HK. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J. Control. Release 2000; 63(1-2): 235-259.

Cheong LLWS, Heng PWS, Wong LF. Relationship between polymer viscosity and drug release from a matrix system. Pharm. Res. 1992; 9(11): 1510-1514.