Formulation and Development of Gastroretentive Drug Delivery System of Efavirenz
Abstract
Efavirenz, a non-nucleotide reverse transcriptase inhibitor is an important drug for treating patients with Human Immunodeficiency Virus infections. It belongs to BCS class II have low solubility and poor intrinsic dissolution rate. It is highly basic (pKa 10.2) which makes it suitable candidate for floating dosage form for continuous delivery in stomach.The study was aimed to improve the solubility by solid dispersion technique.Saturation solubility study and drug content were evaluated for solid dispersion preparation. Saturation solubility shows 8 fold increases in 0.1 N HCL compared to plain drug and drug content was found to be between 95%-102%. Further effervescent floating gastroretentive drug delivery system was prepared by 32 full factorial design with independent variables i.e., concentration of HPMC K100 as matrix forming agent and citric acid as gas generating agent. Lag time, floating time, percent drug release were studied as responses. The optimized batch exhibited floating lag time of 40 sec and the in vitro release studies showed 89.5% drug release in 9 h and tablet remained floating for greater than 8 h. The study thus demonstrated that solubility is increased by solid dispersion technique and floating delivery systems may increase solubility and bioavailability of Efavirenz.
Keywords:
Efavirenz, GRDDS, Solid dispersion (SD), Solvent evaporation method, Solubility enhancement, Percent drug releaseDOI
https://doi.org/10.25004/IJPSDR.2019.110513References
Shaha SH, Patel JK, Pundarikakshudu K. An overview of a gastroretentive floating drug delivery system. Asian J Pharm Sci 2009;4:65-80.
Nayak AK, Maji R, Das B. Gastroretentive drug delivery systems: a review. Asian J Pharma Clinical Res. 2010; 3(1):2-10.
Moes AJ. Gastroretentive dosage forms. Crit Rev Ther Drug Carrier Syst. 1993;10:143-195.
Baumgartner S, Kristl J, Vrecer F. Optimization of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm. 2000;195:125-135.
Hoffman A. Pharmacodynamic aspects of sustained release preparations. Adv Drug Deliv Rev. 1998;33:185-199.
Klausner EA, Lavy E, Friedman M, et al. Expandable gastroretentive dosage forms. J Control Release. 2003;90:143-162.
Rouge N, Allemann E, Gex-Fabry M, et al. Comparative pharmacokinetic study of a floating multiple-unit capsule, a high-density multiple-unit capsule and an immediate release tablet containing 25 mg atenolol. Pharm Acta Helv. 1998;73:81-87.
Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release. 2000;63:235-239.
https://www.medinstitute.org/sti-wizard/hiv 17/6/2019.
http://pubchem.ncbi.nlm.nih.gov/compound/efavirenz#section=Depositor-Supplied-Synonyms.(access date: 25/06/2018)
Chiou WL, Riegalman S. Pharmaceutical Applications Of Solid Dispersion Systems. J Pharm Sci1971;60:1281–1302.
Patil AN, Shinkar DM, Saudagar RB. Review Article: Solubility Enhancement by Solid Dispersion. Int J Curr Pharm Res. 9(3): 15-18.
Shinde SS, Shete AS , PatilMV, SalunkheS, Indapure D. Preparation & Physicochemical Characterization Of Poorly Water Soluble Drug By Using Spray Drying And Solvent Evaporation Methods. Int J Pharma Sci Res. 2014; 5(3): 1035-1044.
Das SK, et al. Solid Dispersions: An Approach to Enhance the Bioavailability of Poorly Water-Soluble Drugs. Int J Pharmaco and Pharma Tech. 2011;1(1): 2277–3436.
Meka L, Vobalaboine V. Enhancement of solubility and dissolution rate of poorly water soluble drugs using cosolvency and solid dispersion techniques. Int J Pharm Sci Nanotech 2009;1:349-56.
Mogal SA, et al. Solid dispersion technique for improving solubility of some poorly soluble drugs. Der Pharmacia Lettre. 2012; 4(5): 1574-1586.
Rao M, et al. Dissolution Improvement of Simvastatin by Surface Solid Dispersion Technology. Dissolution Technologies. 2010; 27-34.
Reddy BV, Ramana Murthy KV. Enhancement Of Dissolution Rate Of Efavirenz By Solid Dispersion Technique. Int J Pharm Bio Sci. 2012; 2( 2):185-190.
Ganapuram BR, et al. Development, evaluation and characterization of surface solid dispersion for solubility and dispersion enhancement of irbesartan. J Pharmacy Res. 2013; 472-477.
Chan S, et al. The characterization and dissolution performances of spray dried solid dispersion of ketoprofen in hydrophilic carriers. As J Pharma Sci. 2015; 10: 372–385.
Guleria R, et al. Polyethylene Glycol Enhances Solubility of Domperidone Through Solid Dispersion. Am J Pharmtech Res. 2012; 2(2): 630-638.
Bhole PG, Patil VR. Enhancement of water solubility of felodipine by preparing solid dispersion using poly-ethylene glycol 6000 and poly-vinyl alcohol. As J Pharm. 2009; 240-244.
Shinde AJ, Harinath MN. Gastroretentive Drug Delivery System: An Overview. 2008;6(1):1-12.
Begum MY, Avanthi J, Shwetha A, Madhuri T, Sudhakar M and Naveen D, Formulation And Evaluation Of Sustained Release Floating Tablets Of Loratadine. Int J Pharma Sci and Res. 2014;5(10): 4375-4385.
Patel GM, Patel HR, Patel M. Floating Drug Delivery System: An Innovative Approach to Prolong Gastric Retention. Pharmainfo.net 2007;5(6).
Shirwalkar AA, Kumar SMR, Jacobs. Recent developments in floating drug delivery systems for gastric retention of drugs. An overview. Ind Drugs 2006;43(9):697-704.
Charyulu NR, et al. Formulation and evaluation of bilayer floating tablets of Diltiazem hydrochloride for bimodal release. Int J Res Pharm Sci. 2012;3(2):301-306.
Gambhire MN, et al. Development and In Vitro Evaluation of an Oral Floating Matrix Tablet Formulation of Diltiazem Hydrochloride. AAPS Pharm Sci Tech 2007; 8 (3) E1-E9.
Nipun TS, Islam SA. SEDDS of gliclazide: Preparation and characterization by in-vitro, ex-vivo and in-vivo techniques. Saudi pharma J. 2014;22(4):343-348.
Bhusnure OG, Kazi PA, Gholve SB, Ansari A, Kazi SN. Solid Dispersion: An Ever Green Method for Solubility Enhancement of Poorly Water Soluble Drugs. Int J Res Pharm chem. 2014;4(4):906-918.
Kumari B, Bishnoi HK. Solid Dispersion: Its Types and Mechanism of Enhancement of Solubility by Solid Dispersion. J Pharm Res. 2019;8(3):65-71.
Gomes EC et al., A Chemical Interactions Study of Antiretroviral Drugs Efavirenz and Lamivudine Concerning the Development of Stable Fixed-Dose Combination Formulations for AIDS Treatment. J BrazChem Soc. 2013; 24(4): 573-579.
Kolhe S, Chaudhari P, More D. Dissolution Enhancement of Poorly Water Soluble Efavirenz by Hot Melt Extrusion Technique. Int. J. Drug Dev. & Res. 2013;5(2): 368-381.
Senjoti FG, Mahmood S, Jaffri JM, et al. Design and in-vitro evaluation of sustained release floating tablets of metformin HCl based on effervescence and swelling. Iran J Pharm Res. 2016;15:53–70.
Indian Pharmacopoeia 2010, Govt of India, Ministry of health and family welfare. Delhi: Indian Pharmacopoeial Commission, Ghaziabad, 2010.
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