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Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate.
J Pharm Sci. 1997 Mar; 86(3):384-8.JP

Abstract

The intrinsic dissolution rate and solubility of carbamazepine was measured in aqueous solutions of sodium lauryl sulfate (SLS) prepared with two different grades of purity, 95 and 99%, and 95% SLS in 0.15 M NaCl to determine the effect of surface-active impurities and electrolytes. Four significant observations resulted from this work: (1) the equilibrium coefficients calculated from the solubility experiments in the 99% SLS, 95% SLS, and 95% with 0.15 M NaCl SLS solutions were 295, 265, and 233 L/mol, respectively; (2) the dissolution rate enhancement in the 99% SLS was 10% greater than that in the 95% SLS and 95% with 0.15 M NaCl solutions, which were not significantly different; (3) the diffusion coefficients of the drug-loaded micelles estimated from the dissolution experiments were 8.4 x 10(-7) cm2/s for the 99% SLS, 9.5 x 10(-7) cm2/s for the 95% SLS, and 1.2 x 10(-6) cm2/s for the 95% with 0.15 M NaCl; and (4) the critical micelle concentrations for the 99% SLS, 95% SLS, and 95% SLS with 0.15M NaCl were 6.8, 4.2, and 0.35 mM, respectively. The results of this study clearly illustrate the sensitivity of the micelle to impurities and electrolytes with regard to size and loading capacity and the effect these changes have on the solubility and dissolution rate. Therefore, when using surfactants in dissolution media for in vitro testing of dosage forms, consideration must be given to the level of impurities present so that the results are consistent and reliable. Intrinsic dissolution rate, surface tension, or solubility measurements may be useful, convenient methods for identifying changes in the surfactant due to either degradation or lot-to-lot variability.

Authors+Show Affiliations

TSRL, Inc., Ann Arbor, MI 48108, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

9050810

Citation

Crison, J R., et al. "Dissolution Media for in Vitro Testing of Water-insoluble Drugs: Effect of Surfactant Purity and Electrolyte On in Vitro Dissolution of Carbamazepine in Aqueous Solutions of Sodium Lauryl Sulfate." Journal of Pharmaceutical Sciences, vol. 86, no. 3, 1997, pp. 384-8.
Crison JR, Weiner ND, Amidon GL. Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. J Pharm Sci. 1997;86(3):384-8.
Crison, J. R., Weiner, N. D., & Amidon, G. L. (1997). Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. Journal of Pharmaceutical Sciences, 86(3), 384-8.
Crison JR, Weiner ND, Amidon GL. Dissolution Media for in Vitro Testing of Water-insoluble Drugs: Effect of Surfactant Purity and Electrolyte On in Vitro Dissolution of Carbamazepine in Aqueous Solutions of Sodium Lauryl Sulfate. J Pharm Sci. 1997;86(3):384-8. PubMed PMID: 9050810.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. AU - Crison,J R, AU - Weiner,N D, AU - Amidon,G L, PY - 1997/3/1/pubmed PY - 2000/7/19/medline PY - 1997/3/1/entrez SP - 384 EP - 8 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 86 IS - 3 N2 - The intrinsic dissolution rate and solubility of carbamazepine was measured in aqueous solutions of sodium lauryl sulfate (SLS) prepared with two different grades of purity, 95 and 99%, and 95% SLS in 0.15 M NaCl to determine the effect of surface-active impurities and electrolytes. Four significant observations resulted from this work: (1) the equilibrium coefficients calculated from the solubility experiments in the 99% SLS, 95% SLS, and 95% with 0.15 M NaCl SLS solutions were 295, 265, and 233 L/mol, respectively; (2) the dissolution rate enhancement in the 99% SLS was 10% greater than that in the 95% SLS and 95% with 0.15 M NaCl solutions, which were not significantly different; (3) the diffusion coefficients of the drug-loaded micelles estimated from the dissolution experiments were 8.4 x 10(-7) cm2/s for the 99% SLS, 9.5 x 10(-7) cm2/s for the 95% SLS, and 1.2 x 10(-6) cm2/s for the 95% with 0.15 M NaCl; and (4) the critical micelle concentrations for the 99% SLS, 95% SLS, and 95% SLS with 0.15M NaCl were 6.8, 4.2, and 0.35 mM, respectively. The results of this study clearly illustrate the sensitivity of the micelle to impurities and electrolytes with regard to size and loading capacity and the effect these changes have on the solubility and dissolution rate. Therefore, when using surfactants in dissolution media for in vitro testing of dosage forms, consideration must be given to the level of impurities present so that the results are consistent and reliable. Intrinsic dissolution rate, surface tension, or solubility measurements may be useful, convenient methods for identifying changes in the surfactant due to either degradation or lot-to-lot variability. SN - 0022-3549 UR - https://www.unboundmedicine.com/medline/citation/9050810/Dissolution_media_for_in_vitro_testing_of_water_insoluble_drugs:_effect_of_surfactant_purity_and_electrolyte_on_in_vitro_dissolution_of_carbamazepine_in_aqueous_solutions_of_sodium_lauryl_sulfate_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)50267-0 DB - PRIME DP - Unbound Medicine ER -