Development and validation of discriminatory dissolution procedure for poorly soluble glyburide

S. Singh, K. Srinivasan, K. Gowthamarajan, G. Narayan

Research output: Contribution to journalArticle

Abstract

In the present study, parameters such as solubility, medium pH, surfactant type and dissolution behavior of formulations, influence of sink conditions, stability and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium for glyburide (BCS Class II drug). Results of solubility data revealed that solubility increased with an increase in pH. Sink conditions were exhibited in the 0.05 M borate buffer pH 9.6, 0.05 M phosphate buffer pH 6.5 containing 0.1-2% (w/v) cetyl trimethyl ammonium bromide (CTAB) and 0.05 M phosphate buffer pH 7.4 containing 0.1-2% CTAB (w/v), respectively. The 0.05 M phosphate buffer at pH 6.5 containing 0.1% CTAB (w/v) with an agitation speed of 50 rpm (USP II) showed a more discriminating drug release profile when compared with 0.05 M phosphate buffer at pH 7.4 containing 0.1% CTAB (w/v) with an agitation speed of 75 rpm. The spiked samples have shown better recovery at 50, 100 and 150% levels. There was no degradation, as observed in the mass spectrum of recovered dissolution samples when compared with the mass spectrum of standard drug solution, which promised that the method was specific and can be used for routine Quality Control analysis as well as for assessment of formulation variables in future dissolution studies of glyburide.
Original languageEnglish
Pages (from-to)205-212
Number of pages8
JournalAsian Journal of Pharmaceutics
Volume4
Issue number4
DOIs
Publication statusPublished - 2010

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Glyburide
Buffers
Phosphates
Solubility
Borates
Surface-Active Agents
Quality Control
Pharmaceutical Preparations
cetyl ammonium bromide

Cite this

Singh, S. ; Srinivasan, K. ; Gowthamarajan, K. ; Narayan, G. / Development and validation of discriminatory dissolution procedure for poorly soluble glyburide. In: Asian Journal of Pharmaceutics. 2010 ; Vol. 4, No. 4. pp. 205-212.
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abstract = "In the present study, parameters such as solubility, medium pH, surfactant type and dissolution behavior of formulations, influence of sink conditions, stability and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium for glyburide (BCS Class II drug). Results of solubility data revealed that solubility increased with an increase in pH. Sink conditions were exhibited in the 0.05 M borate buffer pH 9.6, 0.05 M phosphate buffer pH 6.5 containing 0.1-2{\%} (w/v) cetyl trimethyl ammonium bromide (CTAB) and 0.05 M phosphate buffer pH 7.4 containing 0.1-2{\%} CTAB (w/v), respectively. The 0.05 M phosphate buffer at pH 6.5 containing 0.1{\%} CTAB (w/v) with an agitation speed of 50 rpm (USP II) showed a more discriminating drug release profile when compared with 0.05 M phosphate buffer at pH 7.4 containing 0.1{\%} CTAB (w/v) with an agitation speed of 75 rpm. The spiked samples have shown better recovery at 50, 100 and 150{\%} levels. There was no degradation, as observed in the mass spectrum of recovered dissolution samples when compared with the mass spectrum of standard drug solution, which promised that the method was specific and can be used for routine Quality Control analysis as well as for assessment of formulation variables in future dissolution studies of glyburide.",
author = "S. Singh and K. Srinivasan and K. Gowthamarajan and G. Narayan",
note = "Export Date: 10 November 2017 Correspondence Address: Singh, S.; Department of Pharmaceutical Analysis, Bharathi College of Pharmacy, Bharathinagara, Maddur Taluk, Mandya Dist, Karnataka-571 422, India; email: sachin_pharma06@yahoo.co.in Chemicals/CAS: boric acid, 10043-35-3, 11113-50-1, 11129-12-7, 14213-97-9; cetrimide, 57-09-0, 6899-10-1, 8044-71-1; glibenclamide, 10238-21-8; phosphate, 14066-19-4, 14265-44-2 Manufacturers: Reddy, India References: Carstensen, J.T., Physico-chemical aspects of drug release (1977) Proceedings of the 37th International Congress of Pharmaceutical Sciences of F.I.P., the Hague, Netherlands, , Formulation and Preparation of Dosage Forms Elsevier: Amsterdam; Sept 5-9; Shah, V.P., Konecny, J.J., Everett, R.L., McCullough, B., Noorizadeh, A.C., Skelly, J.P., In vitro dissolution profile of water-insoluble drug dosage forms in the presence of surfactants (1989) Pharm Res, 6, pp. 612-618; Amidon, G.L., Lennernas, H., Shah, V.P., Crison, J.R., A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability (1995) Pharm Res, 12, pp. 413-420; Jinno, J., Oh, D.-M., Crison, J.R., Amidon, G.L., Dissolution of ionizable water-insoluble drugs: The combined effect of pH and surfactant (2000) Journal of Pharmaceutical Sciences, 89 (2), pp. 268-274. , DOI 10.1002/(SICI)1520-6017(200002)89:2<268::AID-JPS14>3.0.CO;2-F; Hoener, B., Benet, L.Z., (1990) Modern Pharmaceutics, p. 143. , Banker GS, Rhodes CT, editors New York: Marcel Dekker; Jorgensen, E.D., Bhagwat, (1998) Pharm Sci Technol Today, 1, pp. 128-135; http://www.drugscard.com, Available from cited in 2009; (2004) Dissolution Method for Drugs, , U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER); Klein, S., Wunderlich, M., Dressman, J., Stippler, E., Development of dissolution tests the basis of gastrointestinal physiology (2005) Taylor and Francis, p. 195. , Pharmaceutical dissolution testing. In: Dressman J, editor. 1 st ed; Gray, V., Compendial testing equipment: Calibration, qualification and sources of pharmaceutical dissolution testing (2005) Taylor and Francis, p. 63. , Dressman J, editor. 1st ed; Kramer, J., Grady, L., Gajendran, J., Historical development of dissolution testing (2005) Taylor and Francis, p. 28. , Pharmaceutical Dissolution Testing. In: Dressman J, editor. 1 st ed; Moore, J.W., Flanner, H.H., Mathematical Comparison of Dissolution Profiles (1996) Pharmaceutical Technology, 20 (6), pp. 64-74; Brown, C.K., Dissolution method development: An industry perspective (2005) Taylor and Francis, p. 28. , Pharmaceutical Dissolution Testing Dressman J, editor. 1st ed",
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Development and validation of discriminatory dissolution procedure for poorly soluble glyburide. / Singh, S.; Srinivasan, K.; Gowthamarajan, K.; Narayan, G.

In: Asian Journal of Pharmaceutics, Vol. 4, No. 4, 2010, p. 205-212.

Research output: Contribution to journalArticle

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AU - Gowthamarajan, K.

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N1 - Export Date: 10 November 2017 Correspondence Address: Singh, S.; Department of Pharmaceutical Analysis, Bharathi College of Pharmacy, Bharathinagara, Maddur Taluk, Mandya Dist, Karnataka-571 422, India; email: sachin_pharma06@yahoo.co.in Chemicals/CAS: boric acid, 10043-35-3, 11113-50-1, 11129-12-7, 14213-97-9; cetrimide, 57-09-0, 6899-10-1, 8044-71-1; glibenclamide, 10238-21-8; phosphate, 14066-19-4, 14265-44-2 Manufacturers: Reddy, India References: Carstensen, J.T., Physico-chemical aspects of drug release (1977) Proceedings of the 37th International Congress of Pharmaceutical Sciences of F.I.P., the Hague, Netherlands, , Formulation and Preparation of Dosage Forms Elsevier: Amsterdam; Sept 5-9; Shah, V.P., Konecny, J.J., Everett, R.L., McCullough, B., Noorizadeh, A.C., Skelly, J.P., In vitro dissolution profile of water-insoluble drug dosage forms in the presence of surfactants (1989) Pharm Res, 6, pp. 612-618; Amidon, G.L., Lennernas, H., Shah, V.P., Crison, J.R., A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability (1995) Pharm Res, 12, pp. 413-420; Jinno, J., Oh, D.-M., Crison, J.R., Amidon, G.L., Dissolution of ionizable water-insoluble drugs: The combined effect of pH and surfactant (2000) Journal of Pharmaceutical Sciences, 89 (2), pp. 268-274. , DOI 10.1002/(SICI)1520-6017(200002)89:2<268::AID-JPS14>3.0.CO;2-F; Hoener, B., Benet, L.Z., (1990) Modern Pharmaceutics, p. 143. , Banker GS, Rhodes CT, editors New York: Marcel Dekker; Jorgensen, E.D., Bhagwat, (1998) Pharm Sci Technol Today, 1, pp. 128-135; http://www.drugscard.com, Available from cited in 2009; (2004) Dissolution Method for Drugs, , U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER); Klein, S., Wunderlich, M., Dressman, J., Stippler, E., Development of dissolution tests the basis of gastrointestinal physiology (2005) Taylor and Francis, p. 195. , Pharmaceutical dissolution testing. In: Dressman J, editor. 1 st ed; Gray, V., Compendial testing equipment: Calibration, qualification and sources of pharmaceutical dissolution testing (2005) Taylor and Francis, p. 63. , Dressman J, editor. 1st ed; Kramer, J., Grady, L., Gajendran, J., Historical development of dissolution testing (2005) Taylor and Francis, p. 28. , Pharmaceutical Dissolution Testing. In: Dressman J, editor. 1 st ed; Moore, J.W., Flanner, H.H., Mathematical Comparison of Dissolution Profiles (1996) Pharmaceutical Technology, 20 (6), pp. 64-74; Brown, C.K., Dissolution method development: An industry perspective (2005) Taylor and Francis, p. 28. , Pharmaceutical Dissolution Testing Dressman J, editor. 1st ed

PY - 2010

Y1 - 2010

N2 - In the present study, parameters such as solubility, medium pH, surfactant type and dissolution behavior of formulations, influence of sink conditions, stability and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium for glyburide (BCS Class II drug). Results of solubility data revealed that solubility increased with an increase in pH. Sink conditions were exhibited in the 0.05 M borate buffer pH 9.6, 0.05 M phosphate buffer pH 6.5 containing 0.1-2% (w/v) cetyl trimethyl ammonium bromide (CTAB) and 0.05 M phosphate buffer pH 7.4 containing 0.1-2% CTAB (w/v), respectively. The 0.05 M phosphate buffer at pH 6.5 containing 0.1% CTAB (w/v) with an agitation speed of 50 rpm (USP II) showed a more discriminating drug release profile when compared with 0.05 M phosphate buffer at pH 7.4 containing 0.1% CTAB (w/v) with an agitation speed of 75 rpm. The spiked samples have shown better recovery at 50, 100 and 150% levels. There was no degradation, as observed in the mass spectrum of recovered dissolution samples when compared with the mass spectrum of standard drug solution, which promised that the method was specific and can be used for routine Quality Control analysis as well as for assessment of formulation variables in future dissolution studies of glyburide.

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