Development and Evaluation of Immediate Release Tablets of Dolutegravir Sodium by Solid Dispersion Technique
DOI:
https://doi.org/10.63682/jns.v14i15S.3551Keywords:
Antiretroviral, bioavailability, immediate release, solubility etc.Abstract
The Dolutegravir Sodium is an antiretroviral drugs bear some significant drawbacks such as, low solubility, low bioavailability, and undesirable side effects. Efforts have been made to design immediate release drug delivery systems for anti-HIV agents to increase the solubility & bioavailability and decrease the degradation/metabolism in the gastrointestinal tract, and to deliver them to the target cells selectively with minimal side effects. The half-life of Dolutegravir is 15 hours. It gets metabolized mainly in the liver, dolutegravir is a BSC class-II drug, it has low solubility and high permeability, hence need to enhance the solubility of by using different solid dispersion techniques. Solid dispersion of dolutegravir is prepared by rotary solvent evaporation method. The purpose of this study was to develop immediate release tablets of poorly water soluble dolutegravir. In this study dolutegravir immediate release tablet were prepared by direct compression method using superdisintegrants at a concentration range 0.5-5% .The tablet is based on interactive mixture of components, consisting of carrier particles covered by fine particles of dolutegravir. The tablets were evaluated for hardness, friability, DT, swelling index ratio and in-vitro drug release. FT-IR, XRD and physical compatibility study were conducted for drug excipient interactions.
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Coffin, J. M. Molecular biology of HIV. In The Evolution of HIV, ed. K. A. Crandall, 1999; 340.Fried land, G. and Klein R. Transmission of HIV. Nejm 1987; 317:18: 1125-1135.
Downs, A.M. and De I.Vincenzi. Probability of heterosexual transmission of HIV: relationship to the number of unprotected sexual contacts. Europeon study Group in heterosexual transmission of HIV. J. A cquir Immune Defic Syndr Hum Retroviral 1996; 11(4): 388- 95.
Amborzia, J. and Levy J. A. Epidemiology, natural history and Pathogenesis of HIV Infection. In Sexually Transmitted Diseases, 3d ed, ed. K.K. Holmes, P.F. Sparling, P.A. Mardh, S.M. Lemon, W.E. Stamm, P. Piot, and J.N. Wasserheit, 1998; 251–58.
Palella, F.J., Delaney, K.M., Moorman, A.C., Loveless, M.O., Fuhrer, J., Satten, G.A., Aschman, D.J. and Holmberg, S.D. Declining Morbidity and Mortality among Patients with Advanced Human Immunodeficiency Virus Infection; N England Journal of Medicine 1998; 338: 853–860.
Pope, M. and Haase, A. Transmission; acute HIV-1 infection and the quest for strategies to prevent infection. Natural Medicine 2003; 9(7): 847–852.
https://www.who.int/hiv/topics/treatment/art/en/#:~:text=HIV,Antiretroviral%20therapy,the%20 progression%20of%20HIV%20disease.
Lieberman H.A., Lachman L., The Theory and Practice of Industrial Pharmacy, Indian Edition, CBS Publishers, and Distributors Pvt. Ltd., 2009, 293, 457, 479-501
Martin EW, Osol A, Alfonso R. Gennaro. Remington's pharmaceutical sciences. Mack Publishing Company; 1990.
Cooper. J, Gunn 1986, “Tutorial pharmacy”, New Delhi, CBS publishers and distributors: New Delhi: pp 211-233.
Gilbert S. banker, Vhristopher T.rhodes, “ Modern Pharmaceuticals”, Fourth edition, Marcel Decker , New York pp:221-233.
H.S. Bean & A.H. Beckett, Advances in Pharmaceutical Sciences Vol. 1-5
Alfred martin, Martin's physical pharmacy and pharmaceutical sciences: physical chemical and biopharmaceutical principles in the pharmaceutical sciences. —6th ed.1,231 pages
Rawlins Bentley‟s Textbook of Pharmaceutics, page no.958
Sidney H. Willig.,Good manufacturing practices for Pharmaceuticals: A plan for total quality control, Second edition; By Quality Assurance Guide; By Organization of Pharmaceutical producers of India.
Kumar S, Singh P. Various techniques for solubility enhancement: An overview. The Pharma Innovation. 2016;5(1, Part A):23.
Vemula VR, Lagishetty V, Lingala S. Solubility enhancement techniques. International journal of pharmaceutical sciences review and research. 2010 Nov;5(1):41-51.
Gibaldi M. Biopharmaceutics and clinical pharmacokinetics. Lea & Febiger; 1977.
Alhayyan AM, Alazmi AH, Albayabi MS, Al Nass AA, Alhafufi HR, Alanezi MT, Al-Mutawa BA, Alanazi AS, Alameer I, Alshammari AD. Techniques for Improving Solubility.
Shargel. Land Yu, Applied Biopharmaceutics and Pharmacokinetics 2nd edition, Connecticut Appleton Century Crofts, 1985
MS AK, RAJESH M, SUBRAMANIAN L. Solubility enhancement techniques: A comprehensive review. World Journal of Biology Pharmacy and Health Sciences. 2023;13(3):141-9.
Thorat YS, Gonjari ID, Hosmani AH. Solubility enhancement techniques: a review on conventional and novel approaches. International journal of pharmaceutical sciences and research. 2011 Oct 1;2(10):2501.
Kadam SV, Shinkar DM, Saudagar RB. Review on solubility enhancement techniques. IJPBS. 2013;3(3):462-75.
Varandal AB, Magar DD, Saudagar RB. Different approaches toward the enhancement of drug solubility: A review. Journal of Advanced Pharmacy Education & Research Oct-Dec. 2013;3(4).
Jörgensen AM, Friedl JD, Wibel R, Chamieh J, Cottet H, Bernkop-Schnürch A. Cosolvents in self-emulsifying drug delivery systems (SEDDS): do they really solve our solubility problems?. Molecular Pharmaceutics. 2020 Jul 13;17(9):3236-45.
Chandel P, Kumari R, Kapoor A. Liquisolid technique: an approach for enhancement of solubility. Journal of drug delivery and therapeutics. 2013 Jul 13;3(4):131-7.
Patel BB, Patel JK, Chakraborty S, Shukla D. Revealing facts behind spray dried solid dispersion technology used for solubility enhancement. Saudi Pharmaceutical Journal. 2015 Sep 1;23(4):352-65.
James Swarbrick, James. G.Boylan, Marcel Dekker Inc, Encyclopedia of Pharmaceutical Technology, Vol 13, New York, 1996.
H.C. Ansel et al., Pharmaceutical Dosage Form and Drug Delivery System, Lippincott Williams and Walkins, New Delhi.
Carter S.J., Cooper and Gunn’s-Dispensing for Pharmaceutical Students, CBS publishers, New Delhi.
M.E. Aulton, Pharmaceutics, The Science& Dosage Form Design, Churchill Livingstone, Edinburgh.
Hasegawa S, Hamaura T, Furuyama N, Kusai A, Yonemochi E, Terada K. Effects of water content in physical mixture and heating temperature on crystallinity of troglitazone-PVP K30 solid dispersions prepared by closed melting method. International journal of pharmaceutics. 2005 Sep 30;302(1-2):103-12.
Bhujbal SV, Mitra B, Jain U, Gong Y, Agrawal A, Karki S, Taylor LS, Kumar S, Zhou QT. Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies. Acta Pharmaceutica Sinica B. 2021 Aug 1;11(8):2505-36.
Singh S, Baghel RS, Yadav L. A review on solid dispersion. International journal of pharmacy & life sciences. 2011 Sep 1;2(9).
Singh A, Van den Mooter G. Spray drying formulation of amorphous solid dispersions. Advanced drug delivery reviews. 2016 May 1;100:27-50.
Isaac Ghebre Sellassie: Pharmaceutical Pelletization Technology, Marcel Dekker, INC, New York. Francoise Nieloud and Gilberte Marti-Mestres: Pharmaceutical Emulsions and Suspensions, Marcel Dekker, INC, New York.
Ansari MT, Hussain A, Nadeem S, Majeed H, Saeed-Ul-Hassan S, Tariq I, Mahmood Q, Khan AK, Murtaza G. Preparation and characterization of solid dispersions of artemether by freeze-dried method. BioMed research international. 2015 May 17;2015.
DiNunzio JC, Brough C, Hughey JR, Miller DA, Williams III RO, McGinity JW. Fusion production of solid dispersions containing a heat-sensitive active ingredient by hot melt extrusion and Kinetisol® dispersing. European journal of pharmaceutics and biopharmaceutics. 2010 Feb 1;74(2):340-51.
Singh A, Sharma PK, Meher JG, Malviya R. Evaluation of enhancement of solubility of paracetamol by solid dispersion technique using different polymers concentration. Asian journal of Pharmaceutical and Clinical research. 2011;4(1):117-9.
Zawar L, Bari S. Microwave induced solid dispersion as a novel technique for enhancing dissolution rate of repaglinide. Adv Pharmacol Pharm. 2013;1:95-101.
Taral Mayur N. Solubility enhancement of atorvastatin calcium by using microwave assisted solid dispersion preparation method. International Journal of Pharmaceutical Research & Allied Sciences. 2015;4:51-6.
Stocklosam J. Pharmaceutical Calculations, Lea &Febiger, Philadelphia.
Liberman H.A, Lachman C, Pharmaceutical Dosage forms. Disperse systems, volume 1, 2, 3. Marcel Dekkar Inc.
Mohanachandran PS, Sindhumol PG, Kiran TS. Superdisintegrants: an overview. International journal of pharmaceutical sciences review and research. 2011 Jan 1;6(1):105-9.
Reshma KJ, Senthila S. Superdisintegrants and Their Inevitable Role in Orodispersible Tablet. IJRR. 2020;7:462-71.
Shihora H, Panda S. Superdisintegrants, utility in dosage forms: a quick review. J. Pharm. Sci. Biosci. Res. 2011;1(3):148-53.
Dhiman J, Dev D, Prasad DN. Superdisintegrants: Brief Review. Journal of Drug Delivery and Therapeutics. 2022 Jan 15;12(1):170-5.
Pahwa R, Gupta N. Superdisintegrants in the development of orally disintegrating tablets: a review. International journal of pharmaceutical sciences and research. 2011 Nov 1;2(11):2767.
Leon Lachman, Herbert A, Liberman and Joseph L. Kaing. The Theory and Practice of Industrial Pharmacy, Varghese publication house, 3 rd edition, 2009, 293-303.
Aulton’S. Pharmaceutics, The Design and Manufacture of Medicines, Biopharmaceutics and Pharmacokinetics, a Treatise, Valabh Prakashan, Delhi, 2nd edition, 2002, 315-384.
Ansel’S. Pharmaceutical Dosage Forms and Drug Delivery Systems, Valabh Prakashan, Delhi, 8 th Edition, 2000, 227-260.
Vaishali Kilor, Nidhi Sapkal, Jasmine Awari and Bharti Shewale. Development and Characterization of Enteric-Coated ImmediateRelease Pellets of Aceclofenac By Extrusion/Spheronization Technique Using Carrageenan As A Pelletizing Agent, AAPS Pharmscitech, 11(1), 2010, 336-343.
Susijit Sahoo, Mishra B, Biswal P I K, Omprakash Panda, Satosh Kumar Mahapatra and Goutam Kumar Jana. Fast Disslving Tablet: As a Potential Drug Delivery System, Drug Invention Today, 2(2), 2010, 130-133.
Jon Gabrielsson, Nils-Ol of Lindberg and Torbjorn Lundstedt. Multivariate Methods in Pharmaceutical applications, J. Chemom, 16(3), 2002, 141-160.
Ustavpatel, Khusbhupatel, Darshan Shan. “A review on immediate release drug delivery system”, IJPRBS, 1(5), 2012, 37-66.
Gupta A, Mishra A K, Gupta V, Bansal P, Singh R and Singh A K. Review Article, Recent Trends of Fast Dissolving Tablet – An Overview of Formulation Technology, International Journal Of Pharmaceutical and Biological Archives, 1(1), 2010, 1-
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