Nawaz Mahammed, Harshini Yadav, Ashok Thulluru, Narahari Narayana, Saravanakumar, Anna Balaji, S. Mounika
Nawaz Mahammed1, Harshini Yadav1, Ashok Thulluru2, Narahari Narayana2, Saravanakumar2, Anna Balaji2, S. Mounika1
1Department of Pharmaceutics, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, A. Rangampet, Tirupati-517102, A.P., India.
2Centre for Pharmaceutical Research, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, A. Rangampet, Tirupati-517 102, A.P., India.
Volume - 13,
Issue - 5,
Year - 2020
In the present study an effort was made to improve dissolution profile of clopidogrel bisulphate by formulating into liquisolid (LS) compact.PEG400 was taken as non volatile solvent in preparation of LS compacts. compatibility of excipients and drug was confirmed by FT-IR studies. The prepared powder blend is having good flow properties.The entrapment of drug within the excipients was confirmed by SEM studies. Disintegration time of LS compacts was decreased by the incorporation of super disintegrants (sodium starch glycolate and pvpk30).F2 formulation was chosen as best formulation based on dissolution and disintegration profiles. The release profile of F2 LS was compared with marketed product (plavix) and results revealed that, the dissolution of drug in LS compact was higher when compared with marketed product, may be due to presence of drug in non-volatile solvent PEG400.
Cite this article:
Nawaz Mahammed, Harshini Yadav, Ashok Thulluru, Narahari Narayana, Saravanakumar, Anna Balaji, S. Mounika. Formulation and Evaluation of Clopidogrel Bisulphate Tablets by Liquisolid Compact Technique. Research J. Pharm. and Tech 2020; 13(5):2427-2434. doi: 10.5958/0974-360X.2020.00435.7
Nawaz Mahammed, Harshini Yadav, Ashok Thulluru, Narahari Narayana, Saravanakumar, Anna Balaji, S. Mounika. Formulation and Evaluation of Clopidogrel Bisulphate Tablets by Liquisolid Compact Technique. Research J. Pharm. and Tech 2020; 13(5):2427-2434. doi: 10.5958/0974-360X.2020.00435.7 Available on: https://rjptonline.org/AbstractView.aspx?PID=2020-13-5-65
1. Lipinski CA, Lombardo F, Dominy BW, et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Delivery Rev 2001; 46:3–26
2. Stegemann S, Livelier F, Franchi D, et al. When poor solubility becomes an issue: from early stage to proof of concept. Eur J Pharm Sci 2007; 31: 249–261
3. Liversidge EM. Nanocrystals: resolving pharmaceutical formulation issues associated with poorly water soluble compounds. In: Marty JJ, editor. Particles. Orlando: Marcel Dekker; 2002
4. Giliyar C, Fikstad DT, Tyavanagimatt S. Challenges and opportunities in oral delivery of poorly water-soluble drugs. Drug Del Technol 2006;6: 5763
5. Amidon GL, Lennernas H, Crison JR, et al. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability.
Pharm Res 1999;12: 413–420.
6. Yadav AV, Shete AS, Dabke AP. Formulation and evaluation of orodispersibleliquisolid compacts of aceclofenac. Indian J Pharm Educ 2010;44: 227–23.
7. Aguiar AJ, Zelmer AJ, Kinkel AW. Deaggregation behavior of a relatively insoluble substituted benzoic acid and its sodium salt. J Pharm Sci 1979;56: 1243–125.
8. Craig DQM. The mechanisms of drug release from solid dispersions in water-soluble polymers. Int J Pharm 2002;231: 131–144.
9. Ebert WR. Soft gelatin capsules: unique dosage form. Pharm Tech 1977; 1:44–50.
10. Hiremath SN, Raghavendra RK, Sunil F, et al. Dissolution enhancement of gliclazide by preparation of inclusion complexes with β-cyclodextrin. Asian J Pharm 2008;2:73–76.
11. Li DX, Oh YK, Lim SJ, et al. Novel gelatin microcapsule with bioavailability enhancement of ibuprofen using spray-drying technique. Int J Pharm 2008; 355:277–284.
12. Kocbek P, Baumgartner S, Kristl J. Preparation and evaluation of nanosuspensions for enhancing the dissolution of poorly soluble drugs. Int J Pharm 2006;312:179–186.
13. Mahmoud EB, Nazrul H, Gihan F, et al. Solubility and dissolution enhancement of tadalafil using selfnanoemulsifying drug delivery system. J Oleo Sci 2014;63:567–576.
14. Müller RH, Runge S, Ravelli V, et al. Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN®) versus drug nanocrystals. Int J Pharm 2006;317:82–89.
15. Javadzadeh Y, Shariati H, Movahhed-Danesh E, et al. Effect of some commercial grades of microcrystalline cellulose on flowability, compressibility, and dissolution profile of piroxicam liquisolid compacts. Drug Dev Ind Pharm 2009;35:243–251
16. Elkordy AA, Tan XN, Essa EA. Spironolactone release from liquisolid formulations prepared with Capryol™ 90, Solutol® HS-15 and Kollicoat® SR 30 D as non-volatile liquid vehicles. Eur J Pharm Biopharm2013;83:203–223.
17. Suliman AS, Anderson RJ, Elkordy AA. Norfloxacin as a model hydrophobic drug with unique release from liquisolid formulations prepared with PEG 200 and Synperonic PE/L-61non-volatile liquid vehicles. Powder Technol 2014;257:156–167.
18. Spireas S, Bolton SM. Liquisolid systems and methods of preparing same. US5968550, 1999.
19. Spireas S. Liquisolid system and method of preparing same. U.S Patent 6423339B1, 2002.
20. Spireas SS, Jarowski CI, Rohera BD. Powdered solution technology: principles and mechanism. Pharm Res 1992;9:1351–1358.
21. Spireas S, Sadu S. Enhancement of prednisolone dissolution properties using liquisolid compacts. Int J Pharm 1998;166:177–188.
22. Fahmy RH, Kassem MA. Enhancement of famotidine dissolution rate through liquisolid tablets formulation: invitro and in vivo evaluation. Eur J Pharm Biopharm2008;69:993–1003
23. Komala DR, Janga KY, Jukanti R, et al. Competence of raloxifene hydrochloride loaded liquisolid compacts for improved dissolution and intestinal permeation. J Drug Deliv Sci Technol2015;30:232–241.
24. Sanka K, Poienti S, Mohd AB, et al. Improved oral delivery of clonazepam through liquisolid powder compact formulations: in-vitro and ex-vivo characterization. Powder Technol2014;256:336–344.
25. Javadzadeh Y, Musaalrezaei L, Nokhodchi A. Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices. Int J Pharm 2008;362:102–108.
26. Nokhodchi A, Aliakbar R, Desai S, et al. Liquisolid compacts: the effect of cosolvent and HPMC on theophylline release. Colloids Surf B Biointerfaces2010;79:262–269.
27. Pavani E, Noman S, Syed IA. Liquisolid technique based sustained release tablet of trimetazidine dihydrochloride. Drug Invention Today 2013;5:302–310.
28. El-Hammadi M, Awad N. Investigating the use of liquisolid compacts technique to minimize the influence of pH variations on loratadine release. AAPS PharmSciTech2012;13:5358.
29. Badawy MA, Kamel AO, Sammour OA. Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study.DrugDeliv2016;23:818–827.
30. Khames A. Liquisolid technique: a promising alternative to conventional coating for improve ment of drug photostability in solid dosage forms. Drug Deliv2013;10:1335–1343.
31. Gowree MP, Vedha Hari BN, Ramya Devi D (2011) Emerging Liquisolid Compact Technology for Solubility Enhancement of BCS Class-II Drug. Journal of Pharmaceutical Science and Research 3: 1604-1611.
32. Spireas S (2002) Liquisolid systems and methods of preparing same. US Patent 6423339B1.
33. Spireas S, Sadu S (1998) Enhancement of prednisolone dissolution properties using liquisolid compacts. International Journal of Pharmaceutics 166: 177-188.
34. Aparna TN, Rao AS. Liquisolid compacts: an approach to enhance the dissolution rate of domperidone. World J Pharm Pharm Sci. 2017;6(7):1219–1232.
35. Javadzadeh Y, Jafari-Navimipour B, Nokhodchi A. Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine). Int J Pharm. 2007;341:26–34.
36. Sambasiva RA, Naga AT. Liquisolid technology: an overview. Int J Res Pharm Biomed Sci 2011;2:401-9.
37. Subhramanyam CVS. Textbook of Physical Pharmaceutics. 2ndedition. Vallabh Prakashan. NewDelhi;2001
38. Lachman L, Liberman AH and KanigLJ : The theory and practice of industrial pharmacy. Mumbai, third ed. Varghese Publication House. 1987;182-184 p.
39. Spiras S, Bolton SM. Liquisolid systems and methods for preparing same, United States Patent2000;6:96,337.
40. Kapade MT. Formulation and evaluation of bilayer tablets containing floating clopidogrel layer and immediate release aspirin layer. Int J Res Pharm Chem. 2016;6(3):580–594.
41. Zhang Y, Huo M, Zhou J, Zou A, Li W, Yao C, et al. DDsolver : an add-in program for modeling and comparison of drug dissolution profiles. Am Assoc Pharm Sci. 2010;12(3):263–271.
42. Tayel SA, Soliman II, Louis D. Improvement of dissolution properties of carbamazepine through application of the liquisolid tablet technique. Eur J Pharm Biopharm. 2008;69(1):342–347.
43. Pardhi DM, Shivhare UD, Mathur VB. Liquisolid technique for enhancement of dissolution properties of carvedilol. Der Pharm Lett. 2010;2(5):412–427.
44. USP30-NF25 UP. US pharmacopoeial convention. Inc, Rockville, MD, USA. 2007
45. El-Say KM, Samy AM, Fetouh MI. Formulation and evaluation of rofecoxibliquisolid tablets. Int J Pharm Sci Rev Res. 2010;3(1):135–142.
46. Javadzadeh Y, Siahi-ShadbadMR ,Barzegar-Jalali M , Nokhodchi A. Enhancement of dissolution rate of piroxicam using liquisolid compacts. Farm. 2005;60(1):361–365.