FORMULATION DEVELOPMENT AND EVALUATION OF SUSTAINED RELEASE GASTRO-RETENTIVE TABLET FORMULATION OF EMTRICITABINE
Objective: The study aims for the design and evaluation of floating tablets of emtricitabine (EMT), post oral administration to sustain the release and enhance gastric residence time (GRT).
Methods: EMT is a nucleoside reverse-transcriptase inhibitor for the prevention and treatment of human immunodeficiency virus (HIV) infection. The investigation was considered to formulate a floating tablet of EMT with various agents. The formulation included with various concentrations of hydroxypropyl methylcellulose (HPMC) k4m, ethyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone (PVP) by wet granulation method. Various parameters for the prepared formulations were evaluated for weight variation, thickness, hardness, friability, floating lag time (FLT), total floating time (TFT), swelling index, in vitro drug release, and fourier-transform infrared spectroscopy (FTIR) studies.
Results: The best formulation F1 exhibited 88.28% release in 24 h duration, with a floating lag time of 7 min and swelling index of 52.1% and drug content was determined to be 98.27%. The release mechanism was determined to be first order with higuchi release kinetics displaying diffusion along with the dissolution of the EMT from the tablet by non fickian mechanism.
Conclusion: EMT tablets showed an increased GRT with a sustained release for 24 h thereby allowing a better window for absorption consequently improve the therapeutic effect of the drug.
2. Hirtz J. The GIT absorption of drugs in man: a review of current concepts and methods of investigation. Br J Clin Pharmacol. 1985;19:77S-83S.
3. Streubel A, Siepmann J, Bodmeier R. Drug delivery to the upper small intestine window using gastroretentive technologies. Curr Opin Pharmacol 2006;6:501-8.
4. Huldrych F. Gunthard, Michael S. Saag, Constance A. Benson, Carlos del Rio, Joseph J. Eron, Joel E. Gallant et al. Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults. JAMA 2016;316:191-210.
5. Eric J. Arts, Daria J. Hazuda. HIV-1 Antiretroviral Drug Therapy. Cold Spring Harb Perspect Med 2012;2:1-23.
6. M A Mozaini, T Alrahbeni, R Al-Mograbi, A Alrajhi. Antiretroviral resistance in HIV-1 patients at a tertiary medical institute in Saudi Arabia: a retrospective study and analysis. BMC Infect Dis 2018;18:2-10.
7. S.Daisy c k, S.Vengatesh, K Elango , R D Damayanthi , N Deattu, P Christina. Formulation and Evaluation of Floating tablets of Ondansetron Hydrochloride. Int J Drug Dev Res 2012;4:265-74.
8. Swati C Jagdale, Somnath, A Patil, Bhanudas, S Kuchekar. Design, development and evaluation of floating tablets of tapentadol hydrochloride using chitosan. Asian J Pharm Clin Res 2012;5:163-8.
9. AA Kharia, S N Hiremath, A K Singhai, L K Omray, S K Jain. Design and Optimization of Floating Drug Delivery System of Acyclovir. Indian J Pharma Sci 2010;72:599–606.
10. J Padmavathy, D Saravanan, D Rajesh. Formulation and evaluation of Ofloxacin floating tablets using HPMC. Int J Pharm Pharm Sci 2011;3:170–3.
11. Albadry AA, WK Ali, FA Al-saady. Formulation and evaluation of prochlorperazine maleate sustained release floating tablet. Int J Pharm Pharm Sci 2017;9:89-98.
12. Aniruddha M R, Joseph B S. Use of a moist granulation technique (MGT) to develop controlled - Release Dosage forms of Acetaminophen. Drug Dev Ind Pharm 2001;27:337-44.
13. Sharma VK. Meloxicam loaded floating sustained release matrix tablet. J Adv Pharm Edu Res 2012;2:18-24.
14. Asnaashari S, Khoei NS, Zarrintan MH, Adibkia K, Javadzadeh Y. Preparation and Evaluation of Novel Metronidazole Sustained Release and Floating Matrix Tablets. Pharm Dev Technol 2011;16:400-7.
15. Haritha S, Niranjan G K, Balaji M, Sima S, Omprakash S, A Kumar et al. Formulation and evaluation of atenolol floating bioadhesive system using optimized polymer blends. Int J Pharm Investig 2016;6:116-22.
16. Yadav KS, Satish CS, Shivkumar HG. Preparation and evaluation of chitosan-Poly (Acrylic acid) Hydrogel as Stomach specific delivery for amoxicillin and Metronidazol. Indian J Pharm Sci 2007;69:91-5.
17. S Singh, K Prajapati, A K Pathak, A Mishra. Formulation and evaluation of floating tablet of Captopril. Int J PharmTech Res 2011;3:333–41.
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