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Application of a ternary HP-β-CD-complex approach to improve the dissolution performance of a poorly soluble weak acid under biorelevant conditions.
Int J Pharm. 2012 Jul 01; 430(1-2):176-83.IJ

Abstract

Over the last decades the poor solubility of new drugs has become an important issue, with one of the main challenges being to develop oral dosage forms with acceptable bioavailability for such compounds. The specific purpose of our study was to combine the advantages of cyclodextrins with those of solid dispersion approaches to improve the bioavailability of poorly soluble weak acids. Glyburide, an antidiabetic, was used as a model drug. First, binary drug inclusion complexes were prepared with 2-hydroxypropyl-β-cyclodextrin. Next, solid glyburide dispersions were prepared with polyvinylpyrrolidone (PVP) and a relatively new hydrophilic copolymer, Kollicoat IR. Finally, to check for potential synergistic effects of the two types of excipients, ternary inclusion complexes were formulated by keeping the 1:2 drug:CD ratio constant but varying the polymer concentration (5-20%). The formulations were analyzed by differential scanning calorimetry and subjected to solubility and dissolution experiments in compendial and biorelevant media. The results of the study clearly indicate that all formulations result in better in vitro performance of the drug. Best results were obtained with the ternary inclusion complexes containing 10% Kollicoat IR or 20% PVP K30. This formulation approach, particularly with the new polymer, appears to be promising in terms of enhancing the bioavailability of BCS class II drugs.

Authors+Show Affiliations

Johann Wolfgang Goethe University, Institute of Pharmaceutical Technology, 9 Max von Laue Street, Frankfurt am Main 60438, Germany.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22531855

Citation

Zoeller, Thomas, et al. "Application of a Ternary HP-β-CD-complex Approach to Improve the Dissolution Performance of a Poorly Soluble Weak Acid Under Biorelevant Conditions." International Journal of Pharmaceutics, vol. 430, no. 1-2, 2012, pp. 176-83.
Zoeller T, Dressman JB, Klein S. Application of a ternary HP-β-CD-complex approach to improve the dissolution performance of a poorly soluble weak acid under biorelevant conditions. Int J Pharm. 2012;430(1-2):176-83.
Zoeller, T., Dressman, J. B., & Klein, S. (2012). Application of a ternary HP-β-CD-complex approach to improve the dissolution performance of a poorly soluble weak acid under biorelevant conditions. International Journal of Pharmaceutics, 430(1-2), 176-83. https://doi.org/10.1016/j.ijpharm.2012.04.029
Zoeller T, Dressman JB, Klein S. Application of a Ternary HP-β-CD-complex Approach to Improve the Dissolution Performance of a Poorly Soluble Weak Acid Under Biorelevant Conditions. Int J Pharm. 2012 Jul 1;430(1-2):176-83. PubMed PMID: 22531855.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Application of a ternary HP-β-CD-complex approach to improve the dissolution performance of a poorly soluble weak acid under biorelevant conditions. AU - Zoeller,Thomas, AU - Dressman,Jennifer B, AU - Klein,Sandra, Y1 - 2012/04/15/ PY - 2012/01/13/received PY - 2012/04/05/revised PY - 2012/04/08/accepted PY - 2012/4/26/entrez PY - 2012/4/26/pubmed PY - 2012/9/29/medline SP - 176 EP - 83 JF - International journal of pharmaceutics JO - Int J Pharm VL - 430 IS - 1-2 N2 - Over the last decades the poor solubility of new drugs has become an important issue, with one of the main challenges being to develop oral dosage forms with acceptable bioavailability for such compounds. The specific purpose of our study was to combine the advantages of cyclodextrins with those of solid dispersion approaches to improve the bioavailability of poorly soluble weak acids. Glyburide, an antidiabetic, was used as a model drug. First, binary drug inclusion complexes were prepared with 2-hydroxypropyl-β-cyclodextrin. Next, solid glyburide dispersions were prepared with polyvinylpyrrolidone (PVP) and a relatively new hydrophilic copolymer, Kollicoat IR. Finally, to check for potential synergistic effects of the two types of excipients, ternary inclusion complexes were formulated by keeping the 1:2 drug:CD ratio constant but varying the polymer concentration (5-20%). The formulations were analyzed by differential scanning calorimetry and subjected to solubility and dissolution experiments in compendial and biorelevant media. The results of the study clearly indicate that all formulations result in better in vitro performance of the drug. Best results were obtained with the ternary inclusion complexes containing 10% Kollicoat IR or 20% PVP K30. This formulation approach, particularly with the new polymer, appears to be promising in terms of enhancing the bioavailability of BCS class II drugs. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/22531855/Application_of_a_ternary_HP_β_CD_complex_approach_to_improve_the_dissolution_performance_of_a_poorly_soluble_weak_acid_under_biorelevant_conditions_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(12)00375-4 DB - PRIME DP - Unbound Medicine ER -