Enhancement of Solubility And Dissolution Profile of Clopidogrel By Various Solid Dispersion Formulations

Authors

  • Mohammed Abdul Khader Department of Pharmacy, Mewar University, Chittorgarh-312901, Rajasthan, India
  • Roshan Salfi Department of Pharmacy, Mewar University, Chittorgarh-312901, Rajasthan, India

Abstract

The present research is aimed at enhancing solubility and drug dissolution of clopidogrel (CPG) used as oral antiplatelet agent by employing solid dispersion (SD) technique. Total 40 SDs formulated with  drug: polymers (pluronic F127, poloxamer 407, labrafil PG, PEG 6000, gelucire 50/13), in varying ratios (1:0.5, 1:1, 1:2, 1:3, 1:4) of which CPG1 to CPG20 and CPG21 to CPG40 prepared by adopting solvent evaporation  method fusion (melt) method respectively. The formulation CPG40 containing pluronic F127 as polymer showed highest solubility of 6.57±0.04 mg/ml) that is 45 folds than pure drug. Similar results  reflected in the dissolution studies where CPG40 containing CPG: pluronic F127 in 1:4 ratio showed maximum % drug content, % practical yield and drug dissolution of 99.14% in 60 minutes when compared with other formulations and pure drug (32.76%) obtained  by fusion melt method. From FTIR studies the optimized formulation CPG40 showed the compatibility between drug and polymers. XRD and SEM studies showed CPG40 exists in amorphous form that fetched in better drug release from the SD formulation in comparison to pure drug.

Keywords:

Clopidogrel, solid dispersion, fusion (melt) method, pluronic F127, platelet aggregation inhibitor.

DOI

https://doi.org/10.25004/IJPSDR.2020.120410

References

Vasconcelos T, Sarmento B, Costa P.Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Dis Today. 2007; 12(23-24):1068-1075.

Perioli L, D'Alba G,Pagano C.New oral solid dosage form for furosemide oral administration. Eur J Pharm Biopharm. 2012; 80(3):621-9.

Ali AA, Gorashi AS. Absorption and dissolution of nitrofurantoin from different experimental formulations. Int J Pharm.1984;19: 297-306.

Ahire BR, Rane BR, Bakliwal SR, Pawar SP. Solubility Enhancement of Poorly Water Soluble Drug by Solid Dispersion Techniques. Int J Pharm Tech Res. 2010; 2:2007-2015.

Bang LM, Chapman TM, Goa KL. Clopidogrel: A review of its efficacy in the management of hypertension. Drugs. 2003; 63:2449-72.

Borghi C. Clopidogrel in Hypertension. Vasular Health and Risk Management. 2005; 1(3):173-182.

Patel J, Kevin G, Anjali P, Mihir R, Navin S. Design and development of a self-nanoemulsifying drug delivery system for Telmisartan for oral drug delivery. Int J Pharm Investig. 2011; 1(2):112-118.

Arora SC, Sharma PK, Irchhaiya R, Khatkar A, Singh N, Gagoria J. Development, characterization and solubility study of solid dispersions of Cefuroxime Axetil by the solvent evaporation method. J Adv Pharm Technol Res. 2010;1(3):326-9.

Anant P, Manish M, Amit Kumar T, Bhaskar C, Kadam SS. Preparation and characterization of flurbiprofen beads by melt solidification technique. AAPS Pharm Sci Tech. 2003; 4 (4): 65.

Saravanan M, Natraj KS, Ganesh KS. The effect of tablet formulation and hardness on in vitro release of cephalexin from Eudragit L100 based extended release tablets. Biol Pharm Bull. 2002; 25: 4541-5.

Afrasim M, Shivakua HG. Formulation of Sustained-release diltiazem matrix tablets using hydrophilic gum blends.Trop J Pharm Res. 2010; 9: 283-291.

Mohammadi H, Hemanath Kumar V. Formulation and Evaluation of Solid Dispersion Incorporated Fast Disintegrating Tablets of Tenoxicam Using Design of Experiment. Int J Pharm Sci Drug Res. 2019; 11(1):35-44.

Vanshiv SD, Rao MRP, Sonar GS. Physicochemical characterization and in vitro dissolution of Domperidone by solid dispersion technique. Ind J Pharm Edu Res. 2009; 43(1):86-90.

Subhash K, Bidkar SJ, Dama GY. Formulation& Evaluation of Ciprofloxacin Solid Dispersion Controlled Release Floating Capsules for Solubility Improvement. Indian J Pharm Biol Res. 2017; 5(3):7-16.

Batra V, Shirolkar VS, Mahaparale PR. Solubility and dissolution enhancement of glipizide by solid dispersion technique. Ind J Pharm Edu Res. 2008; 42(4):373-378.

Yadav B, Tanwar YS.Development, Characterization and In Vitro Evaluation of Flurbiprofen Solid Dispersions using Polyethylene Glycols as Carrier. J App Pharm Sci. 2016; 6(04): 060-066.

Mohammadi Ghobad, Barzegar-Jalali Azim, Khosro Adibkia. Development and Characterization of Solid Dispersion for Dissolution Improvement of Furosemide by Co grinding Method. Adv Pharm Bull. 2014; 4(4): 391-399.

Soliman MS, Khan MA. Preparation and in vitro characterization of a semi-solid dispersion of flurbiprofen with Gelucire44/14 and Labrasol. Pharmazie. 2005; 60(4): 288-293.

Shailendra Kumar Singh, SoukaryaSom, Shankhwar U. Formulation and optimization of solid dispersion of Clopidogrel with PEG 6000. J Appl Pharm Sci. 2011; 1(8):217-26.

Shaikh FI, Patel VB. Enhancement of dissolution of Clopidogrel Hydrochloride using solid dispersion technique. Res J Recent Sci. 2015; 4: 299- 307.

Valizadeh H, Nokhodchi A, Qarakhani N, Zakeri-Milani P, Azarmi S, Hassanzadeh D, Löbenberg R. Physicochemical characterization of solid dispersions of indomethacin with PEG 6000, Myrj 52, lactose, sorbitol, dextrin, and Eudragit E100. Drug Dev Ind Pharm. 2004; 30(3):303-317.

Published

30-07-2020
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How to Cite

“Enhancement of Solubility And Dissolution Profile of Clopidogrel By Various Solid Dispersion Formulations”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 12, no. 4, July 2020, pp. 377-83, https://doi.org/10.25004/IJPSDR.2020.120410.

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Section

Research Article

How to Cite

“Enhancement of Solubility And Dissolution Profile of Clopidogrel By Various Solid Dispersion Formulations”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 12, no. 4, July 2020, pp. 377-83, https://doi.org/10.25004/IJPSDR.2020.120410.

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