SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF TELMISARTAN BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING KOLLIDON VA 64 AS CARRIER
Keywords:Telmisartan, KollidonVA64, Solid dispersions, Pellets
Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets.
Methods: Telmisartan solid dispersions were prepared by solvent evaporation technique using Kollidon VA64 as binder and solubility enhancer, Crospovidone as disintegrant and ethanol was used as the solvent. Telmisartan pellets were prepared by dissolving telmisartan, kollidonVA64, Crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. All the formulations were further evaluated for physicochemical parameters such as particle size, friability, angle of repose and drug content. In vitro dissolution studies were carried out in pH 7.5 phosphate buffer by using USP apparatus II.
Results: It was observed that the dissolution rate of the solid dispersion formulation TSD5 showed a better dissolution rate to the extent of 1.113 folds and 1.979 folds when compared to a marketed formulation and pure drug, respectively. Similarly, the formulation TPL3containing 1:3 ratio of Telmisartan to Kollidon VA64 showed an improved dissolution rate to the extent of 1.150 folds and 2.045 folds when compared to the marketed formulation and pure drug, respectively. Majority of the formulations displayed first-order release kinetics and were found to be linear with R2 values in the range of 0.905 to 0.994. FTIR analysis and DSC analysis revealed that there was no major interaction between the drug and the excipients used in the design of the formulation. SEM analysis was performed for solid dispersions, pellet formulations and its polymers to determine the surface characteristics.
Conclusion: From the present study, it was observed that the solubility of Telmisartan was enhanced by Kollidon VA 64 in pellet formulations when compared to solid dispersions.
Follonier N, Doelker E. Biopharmaceutical comparison of oral multiple-unit and single unit sustained release dosage forms. STP Pharm Sci. 1992;2:141-5.
Vial Bernasconi AC, Doelker E, Buri P. Prolonged-release capsules divided and monolithic forms. STP Pharm Sci. 1988;4:397-409.
Malinowski HJ, Smith WE. Effects of spheronization process variables on selected tablet properties. J Pharm Sci. 1974;63(2):285-8. doi: 10.1002/jps.2600630225.
Jackson IM, Roberts S, Timmins P, Sen H. Comparison of laboratory scale processing in the production of coated pellets. Pharmaceutical Technology. International. 1989;1:29-32.
Gamlen MJ. Pellet manufacture for controlled release. Manuf Chem. 1985 Jun:56-9.
Nastruzzi C, Cortesi R, Esposito E, Genovesi A, Spadoni A, Vecchio C. Influence of formulation and process parameters on pellet production by powder layering technique. AAPS PharmSciTech. 2000;1(2):9. doi: 10.1208/pt010209, PMID 14727842.
Dow commercial information. Using Methocel cellulose ethers for controlled release of drugs in hydrophilic matrix systems. Dow Chemical Company; 2002. p. 1-36.
Olsen K. Fluid bed equipment. In: Ghebre Sellassie I, editor Pharmaceutical pelletization technology. New York: Marcel and Dekker; 1989. p. 39-69.
Bauer KH, Lehmann K, Osterwald HP, Rothgang G. Equipment for sugar coating and film coating processes coated pharmaceutical dosage forms. Stuttgart: Medpharm Scientiphic Publishers; 1998.
Felton LA. Film coating of oral solid dosage form. In: Swarbrick J, editor Encyclopedia of pharmaceutical technology. Informa Helathcare. 3rd ed; 2007. p. 1729-47.
Stangier J, Su CA, Roth W. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients. J Int Med Res. 2000;28(4):149-67. doi: 10.1177/147323000002800401.
Tirumalesh N, Chowdary KPR. Formulation development and optimization of telmisartan tablets employing βcd starch 1500 and soluplus. Indo Am J Pharm Sci. 2017;4(6):1630-5.
Sucheta B, Dyandevi M, Mithun VK, Rajendra DP. Solubility enhancement of anti-hypertensive agent by solid dispersion technique. Int J Pharm Life Sci. 2011;2(8):970-5.
Kausalya J, Suresh K, Padmapriya S, Anusha R, Senthilnathan B. Solubility and dissolution enhancement of telmisartan using various techniques. Int J Pharm Technol Res. 2011;3(3):1737-49.
Gordon RE, Rosanske TW, Fonner DE, Anderson NR, Banker GS. Granulation technology and tablet characterization. Pharmaceutical Dosage Forms: Tablets. 1990;2:324.
Train D. Some aspects of the property of angle of repose of powders. J Pharm Pharmacol. 1958 Dec 1;10Suppl 1:127-35T. doi: 10.1111/j.2042-7158.1958.tb10391.x, PMID 13611662.
Kothawade PC, Belgamwar VS, Deshmukh S. Solid dispersions of telmisartan for enhancing solubility, dissolution rate and oral bioavailability. Indo Am J Pharm Res. 2013;3(9):7035-45.
Vishal D, Gaurav J, Vaibhav J, Sheorey RV. Formulation and in vitro evaluation of fast-dissolving tablets of telmisartan. Int J Pharm Life Sci. 2012;3:2159-64.
Niranjan C, Anuradha C, Shubahngi S, Jagdish S. Improvement of Bioavailability and solubility of telmisartan by solid dispersion technique using various carriers. Int J Pharm Sci Rev Res. 2013;19(2):36-41.
Jain AJ, Gohel DK, Patel KN, Patel BA, Patel PA. Use of combined techniques of solubilization for improving solubility and dissolution of immediate release tablet containing telmisartan. Int J Pharm Res Scholars. 2012;1(2):221-31.
Kunam V, Suryadevara V, Rao Garikapati D, Mandava VBR, Sunkara SP. Solubility and dissolution rate enhancement of ezetimibe by solid dispersion and pelletization techniques. Asian J Pharm Clin Res. 2019;12(3):407-13. doi: 10.22159/ ajpcr.2019.v12i3.30772.
Viswanadh K, Devala RG, Vidyadhara S, Venkata BR, Ramesh BJ, Siva PS. Solubility and dissolution rate enhancement of telmisartan by solid dispersion and pelletization techniques using soluplus as the carrier. Int J Appl Pharm. 2020;12:50-8.
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