Use of the Liquisolid Technique for Improvement of the solubility and Dissolution of Clozapine
Keywords:
Liquisolid technique, Clozapine, Solubility, Dissolution rate, Mean dissolution time, Dissolution efficiency
Abstract
The aim of the present work was to enhancement of Solubility and Dissolution of Clozapine using liquisolid technique. This work aimed to study the effect of different liquid vehicles on release characteristics of Clozapine. For liquisolid technique, different amount of liquid and ratio of carrier to coating material were employed. Avicel PH 102 and Aerosil 200 were used as carrier and coating material respectively and sodium starch glycolate (5%) was used as superdisintegrant. The empirical method as introduced by Spireas and Bolton 1999 was applied strictly to calculate amount of carrier and coating materials required to prepare liquisolid tablet. Quality control test like uniformity of tablet weight, uniformity of drug content, hardness, friability test, disintegration test and in-vitro dissolution tests were performed to evaluate the each batch of prepared tablets. In vitro drug dissolution profile of the liquisolid formulation were studied and compared with the Directly Compressed tablet of Clozapine in 0.1N HCL. Stability study was carried out to evaluate the stability of the tablet under humid condition. It was found to be that the optimized liquisolid tablet has high dissolution efficiency (80.44%) and lower mean dissolution time (MDT).From present study it can be concluded that liquisolid technique shows better improvement in solubility and dissolution of Clozapine than the pure drug.
References
1.Tiong N, Elkordy A.A, ”Effect of liquisolid formulations on dissolution of naproxen” European Journal of Pharmaceutics and Biopharmaceutics, 2009, 73, 373–384.
2.C. Lipinski, Poor aqueous solubility – an industry wide problem in drug discovery, Am. Pharm. Rev. 5 (2002) 82–85.
3.D. Hörter, J.B. Dressman, Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract, Adv. Drug Deliv Rev. 46 (1997) 75–87.
4.R. Löbenberg, G.L. Amidon, Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards, Eur. J. Pharm. Biopharm. 50 (2000) 3–12.
5.Fahmy R.H, Kassem M.A, “Enhancement of femotidine dissolution rate through liquisolid tablets formulation: In vitro and In vivo evaluation” European Journal of Pharmaceutics and Biopharmaceutics, 2008, 69, 993–1003.
6.Vemula V.R, Legishetty V, Lingala S, “Solubility enhancement techniques – A Review” International Journal of Pharmaceutical Sciences Review and Research, 2010, 5(1), 41-47.
7.S. Spireas, M. Bolton, Liquisolid Systems and Methods of Preparing Same, U.S. Patent 5,968,550, 1999.
8. S. Spireas, Liquisolid Systems and Methods of Preparing Same, U.S. Patent 6,423,339 B1, 2002.
9. Sheth, C.I. Jarowski, Use of powdered solutions to improve the dissolution rate of polythiazide tablets, Int. J. Pharm. 16 (5) (1990) 769–777.
10. S. Spireas, T. Wang, R. Grover, Effect of powder substrate on the dissolution properties of methchrothiazide liquisolid compacts, Drug Dev. Ind. Pharm. 25 (2) (1999) 163–168.
11. A.Nokhodchi, The effect of type and concentration of vehicles on the dissolution rate of a poorly soluble drug (indomethacin) from liquisolid compacts, J. Pharm. Pharma. Sci. 8 (1) (2005) 18–25.
12. Y. Javadzadeh,M.R. Siahi-Shadbad, M. Barzegar-Jalali, A. Nokhodchi, Enhancement of dissolution rate of piroxicam using liquisolid compacts, Il Farmaco 60 (2005) 361–365.
13.Syed I.H, Pavani E, “The liquisolid technique: Based Drug delivery system” International Journal of Pharmaceutical Sciences and Drug Research, 2012, 4(2), 88-96.
14.Spireas S. Liquisolid System and method of preparing same. U.S Patent 6423339B1, 2002.
15.Merisko E. Liversidge nanocrystals: resolving pharmaceutical formulation issues associated with poorly soluble compounds in: J.J matty (Ed), Particles, Marcel Dekker, Orlando, 2002.
16.Jarowski CI, Rohera BD, Spireas S. Powdered solution technology: principles and mechanism. Pharm Res. 1992; 9: 1351-1358.
17.Barzegar JM, Javadzadeh Y, Nokhodchi A, Siahi-Shadbad MR. Enhancement of dissolution rate of piroxicam using liquisolid compacts. II Farmaco. 2005; 60: 361-365.
18.Nokhodchi A, Hentzschel CM, Leopord CS. Drug release from liquisolid system: speed it up, slow it down. Expert Opin Drug Del. 2011; 8: 191-205.
19.Smirnova I, Suttiruengwong S, Seiler M, Arlt M. Dissolution rate enhancement by adsorption of poorly soluble drugs on hydrophilic silica aerogels. Pharm Dev Tech 2004; 9: 443-452.
20.Spireas S, Bolton M. Liquisolid Systems and Methods of Preparing Same. U.S. Patent 5,968,550, 1999.
21.Gowda D.V., Gupta V, Khan M and Bathool A, “Encapsulation of Clozapine in to Beeswax Microspheres: Preparation, Characterization and Release Kinetics” International Journal of PharmTech Research, 2011, (3, 4) 2199-2207.
22.USP DI, Drug information for the health care professional, 12th Ed. 974 -978, 1992.
23.Falkai P., Wobrock T., Lieberman J., Glenthoj B.,Gattaz W.F., Moller H.J & Wfsbp Task Force On Treatment Guidelines For Schizophrenia. The World Journal of Biological Psychiatry, 2006; 7(1): 5- 40.
24.Maxine X. Patel and Anthony S. David. Why aren't depot antipsychotics prescribed more often and what can be done about it? Advances in Psychiatric Treatment 2005; 11:203-211.
25.Kopparam Manjunath and Vobalaboina Venkateswarlu; Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration; Journal of Controlled Release Volume 107, Issue 2, 3 October 2005, Pages 215-228
26. drugs.com/search.php?searchterm=Clozapine
27. drugbank.ca/drugs/DB00363
28. medlineindia.com
29.Spireas S, Sadu S, “Enhancement of prednisolone dissolution properties using liquisolid compacts” International Journal of Pharmaceutics, 1998, 166, 177–188.
30.Elkordy A.A, Essa E.A, Dhuppad S, Jammigumpula P, “Liquisolid technique to enhance and to sustain griseofulvin dissolution: Effect of choice of non-volatile liquid vehicles” International Journal of Pharmaceutics, 2012, 434, 122–132.
31.Hentzschel C.M, Alnaief M, Smirnova I, Sakmann A, Leopold C.S, “ Enhancement of griseofulvin release from liquisolid compacts” European Journal of Pharmaceutics and Biopharmaceutics, 2012, 80, 130–135.
32.Javadzadeh Y, Musaalrezaei, Nokhodchi A,” Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices” International Journal of Pharmaceutics, 2008, 362, 102–108.
33.Javadzadeh Y, Siahi-Shadbad M.R, Barzegar-Jalali M, Nokhodchi A, “ Enhancement of dissolution rate of piroxicam using liquisolid compacts” II Farmaco,2005, 60, 361-365.
34.Shah C.V, Patel H.K., Shah V.H, Upadhyay U.M, “Design, Development and Optimization of Valsartan Liquisolid tablets using Box-Behnken Design” International Journal of Pharmaceutical Sciences and Research, 2012, 3(8), 2741-2753.
35.El-Say M. Khalid, Samy M. Ahmed, Fetouth I. Mohamed, “Formulation and evaluation of Rofecoxib liquisolid tablets” International Journal of Pharmaceutical Sciences Review and Research, 2010, 3(1), 135-142.
36.Naveen C, Shastri N, Tadikonda R.R, “ Use of the liquisolid compact technique for improvement of the dissolution rate of Valsartan ” Acta Pharmacutica Sinica B, 2012, 2 (5), 502-508.
37.Sathali A.A.H, C Deppa C, “Formulation of liquisolid tablets of candesartan cilexetil” International Journal of Research in Pharmaceutical Sciences, 2013, 4(2), 238-249.
2.C. Lipinski, Poor aqueous solubility – an industry wide problem in drug discovery, Am. Pharm. Rev. 5 (2002) 82–85.
3.D. Hörter, J.B. Dressman, Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract, Adv. Drug Deliv Rev. 46 (1997) 75–87.
4.R. Löbenberg, G.L. Amidon, Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards, Eur. J. Pharm. Biopharm. 50 (2000) 3–12.
5.Fahmy R.H, Kassem M.A, “Enhancement of femotidine dissolution rate through liquisolid tablets formulation: In vitro and In vivo evaluation” European Journal of Pharmaceutics and Biopharmaceutics, 2008, 69, 993–1003.
6.Vemula V.R, Legishetty V, Lingala S, “Solubility enhancement techniques – A Review” International Journal of Pharmaceutical Sciences Review and Research, 2010, 5(1), 41-47.
7.S. Spireas, M. Bolton, Liquisolid Systems and Methods of Preparing Same, U.S. Patent 5,968,550, 1999.
8. S. Spireas, Liquisolid Systems and Methods of Preparing Same, U.S. Patent 6,423,339 B1, 2002.
9. Sheth, C.I. Jarowski, Use of powdered solutions to improve the dissolution rate of polythiazide tablets, Int. J. Pharm. 16 (5) (1990) 769–777.
10. S. Spireas, T. Wang, R. Grover, Effect of powder substrate on the dissolution properties of methchrothiazide liquisolid compacts, Drug Dev. Ind. Pharm. 25 (2) (1999) 163–168.
11. A.Nokhodchi, The effect of type and concentration of vehicles on the dissolution rate of a poorly soluble drug (indomethacin) from liquisolid compacts, J. Pharm. Pharma. Sci. 8 (1) (2005) 18–25.
12. Y. Javadzadeh,M.R. Siahi-Shadbad, M. Barzegar-Jalali, A. Nokhodchi, Enhancement of dissolution rate of piroxicam using liquisolid compacts, Il Farmaco 60 (2005) 361–365.
13.Syed I.H, Pavani E, “The liquisolid technique: Based Drug delivery system” International Journal of Pharmaceutical Sciences and Drug Research, 2012, 4(2), 88-96.
14.Spireas S. Liquisolid System and method of preparing same. U.S Patent 6423339B1, 2002.
15.Merisko E. Liversidge nanocrystals: resolving pharmaceutical formulation issues associated with poorly soluble compounds in: J.J matty (Ed), Particles, Marcel Dekker, Orlando, 2002.
16.Jarowski CI, Rohera BD, Spireas S. Powdered solution technology: principles and mechanism. Pharm Res. 1992; 9: 1351-1358.
17.Barzegar JM, Javadzadeh Y, Nokhodchi A, Siahi-Shadbad MR. Enhancement of dissolution rate of piroxicam using liquisolid compacts. II Farmaco. 2005; 60: 361-365.
18.Nokhodchi A, Hentzschel CM, Leopord CS. Drug release from liquisolid system: speed it up, slow it down. Expert Opin Drug Del. 2011; 8: 191-205.
19.Smirnova I, Suttiruengwong S, Seiler M, Arlt M. Dissolution rate enhancement by adsorption of poorly soluble drugs on hydrophilic silica aerogels. Pharm Dev Tech 2004; 9: 443-452.
20.Spireas S, Bolton M. Liquisolid Systems and Methods of Preparing Same. U.S. Patent 5,968,550, 1999.
21.Gowda D.V., Gupta V, Khan M and Bathool A, “Encapsulation of Clozapine in to Beeswax Microspheres: Preparation, Characterization and Release Kinetics” International Journal of PharmTech Research, 2011, (3, 4) 2199-2207.
22.USP DI, Drug information for the health care professional, 12th Ed. 974 -978, 1992.
23.Falkai P., Wobrock T., Lieberman J., Glenthoj B.,Gattaz W.F., Moller H.J & Wfsbp Task Force On Treatment Guidelines For Schizophrenia. The World Journal of Biological Psychiatry, 2006; 7(1): 5- 40.
24.Maxine X. Patel and Anthony S. David. Why aren't depot antipsychotics prescribed more often and what can be done about it? Advances in Psychiatric Treatment 2005; 11:203-211.
25.Kopparam Manjunath and Vobalaboina Venkateswarlu; Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration; Journal of Controlled Release Volume 107, Issue 2, 3 October 2005, Pages 215-228
26. drugs.com/search.php?searchterm=Clozapine
27. drugbank.ca/drugs/DB00363
28. medlineindia.com
29.Spireas S, Sadu S, “Enhancement of prednisolone dissolution properties using liquisolid compacts” International Journal of Pharmaceutics, 1998, 166, 177–188.
30.Elkordy A.A, Essa E.A, Dhuppad S, Jammigumpula P, “Liquisolid technique to enhance and to sustain griseofulvin dissolution: Effect of choice of non-volatile liquid vehicles” International Journal of Pharmaceutics, 2012, 434, 122–132.
31.Hentzschel C.M, Alnaief M, Smirnova I, Sakmann A, Leopold C.S, “ Enhancement of griseofulvin release from liquisolid compacts” European Journal of Pharmaceutics and Biopharmaceutics, 2012, 80, 130–135.
32.Javadzadeh Y, Musaalrezaei, Nokhodchi A,” Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices” International Journal of Pharmaceutics, 2008, 362, 102–108.
33.Javadzadeh Y, Siahi-Shadbad M.R, Barzegar-Jalali M, Nokhodchi A, “ Enhancement of dissolution rate of piroxicam using liquisolid compacts” II Farmaco,2005, 60, 361-365.
34.Shah C.V, Patel H.K., Shah V.H, Upadhyay U.M, “Design, Development and Optimization of Valsartan Liquisolid tablets using Box-Behnken Design” International Journal of Pharmaceutical Sciences and Research, 2012, 3(8), 2741-2753.
35.El-Say M. Khalid, Samy M. Ahmed, Fetouth I. Mohamed, “Formulation and evaluation of Rofecoxib liquisolid tablets” International Journal of Pharmaceutical Sciences Review and Research, 2010, 3(1), 135-142.
36.Naveen C, Shastri N, Tadikonda R.R, “ Use of the liquisolid compact technique for improvement of the dissolution rate of Valsartan ” Acta Pharmacutica Sinica B, 2012, 2 (5), 502-508.
37.Sathali A.A.H, C Deppa C, “Formulation of liquisolid tablets of candesartan cilexetil” International Journal of Research in Pharmaceutical Sciences, 2013, 4(2), 238-249.
Published
2014-09-01
How to Cite
[1]
Vijaykumar, G., Patel, J., Kapadiya, J. and Upadhyay, U. 2014. Use of the Liquisolid Technique for Improvement of the solubility and Dissolution of Clozapine. PharmaTutor. 2, 9 (Sep. 2014), 101-114.
Section
Articles
