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Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with beta-cyclodextrin and its sulfobutyl ether derivative in solution and solid state.
Eur J Pharm Sci. 2003 Nov; 20(3):253-66.EJ

Abstract

The studies reported in this work aimed to elucidate the inclusion complex formation of vinpocetine (VP), a poorly water-soluble base type drug, with beta-cyclodextrin (betaCD) and its sulfobutyl ether derivative (sulfobutyl ether beta-cyclodextrin (SBEbetaCD)), with or without water-soluble polymers (PVP and HPMC), by thoroughly investigating their interactions in solution and solid state. Phase solubility studies were carried out to evaluate the solubilizing power of both cyclodextrins (CDs), in association with water-soluble polymers, towards VP and to determine the apparent stability constants (Kc) of the complexes. SBEbetaCD showed higher solubilizing efficacy toward VP than the parent betaCD due to its greater solubility and complexing abilities, what was reflected in higher Kc values. Improvement in Kc values for ternary complexes clearly proves the benefit on the addition of water-soluble polymers to promote higher complexation efficiency. VP-CDs (1:1) binary and ternary systems were prepared by physical mixing, kneading, co-evaporation, and lyophilization methods. In the solid state, drug-carrier interactions were studied by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and Fourier-transform infrared spectroscopy. The results of these analysis suggested the formation of new solid phases, some of them in amorphous state, allowing to the conclusion of strong evidences of binary and ternary inclusion complex formation between VP, CD and water-soluble polymers, particularly for co-evaporated and lyophilized binary and ternary products.

Authors+Show Affiliations

Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Coimbra 3000, Portugal.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

14592691

Citation

Ribeiro, Laura S S., et al. "Physicochemical Investigation of the Effects of Water-soluble Polymers On Vinpocetine Complexation With Beta-cyclodextrin and Its Sulfobutyl Ether Derivative in Solution and Solid State." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 20, no. 3, 2003, pp. 253-66.
Ribeiro LS, Ferreira DC, Veiga FJ. Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with beta-cyclodextrin and its sulfobutyl ether derivative in solution and solid state. Eur J Pharm Sci. 2003;20(3):253-66.
Ribeiro, L. S., Ferreira, D. C., & Veiga, F. J. (2003). Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with beta-cyclodextrin and its sulfobutyl ether derivative in solution and solid state. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 20(3), 253-66.
Ribeiro LS, Ferreira DC, Veiga FJ. Physicochemical Investigation of the Effects of Water-soluble Polymers On Vinpocetine Complexation With Beta-cyclodextrin and Its Sulfobutyl Ether Derivative in Solution and Solid State. Eur J Pharm Sci. 2003;20(3):253-66. PubMed PMID: 14592691.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical investigation of the effects of water-soluble polymers on vinpocetine complexation with beta-cyclodextrin and its sulfobutyl ether derivative in solution and solid state. AU - Ribeiro,Laura S S, AU - Ferreira,Domingos C, AU - Veiga,Francisco J B, PY - 2003/11/1/pubmed PY - 2004/8/6/medline PY - 2003/11/1/entrez SP - 253 EP - 66 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 20 IS - 3 N2 - The studies reported in this work aimed to elucidate the inclusion complex formation of vinpocetine (VP), a poorly water-soluble base type drug, with beta-cyclodextrin (betaCD) and its sulfobutyl ether derivative (sulfobutyl ether beta-cyclodextrin (SBEbetaCD)), with or without water-soluble polymers (PVP and HPMC), by thoroughly investigating their interactions in solution and solid state. Phase solubility studies were carried out to evaluate the solubilizing power of both cyclodextrins (CDs), in association with water-soluble polymers, towards VP and to determine the apparent stability constants (Kc) of the complexes. SBEbetaCD showed higher solubilizing efficacy toward VP than the parent betaCD due to its greater solubility and complexing abilities, what was reflected in higher Kc values. Improvement in Kc values for ternary complexes clearly proves the benefit on the addition of water-soluble polymers to promote higher complexation efficiency. VP-CDs (1:1) binary and ternary systems were prepared by physical mixing, kneading, co-evaporation, and lyophilization methods. In the solid state, drug-carrier interactions were studied by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and Fourier-transform infrared spectroscopy. The results of these analysis suggested the formation of new solid phases, some of them in amorphous state, allowing to the conclusion of strong evidences of binary and ternary inclusion complex formation between VP, CD and water-soluble polymers, particularly for co-evaporated and lyophilized binary and ternary products. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/14592691/Physicochemical_investigation_of_the_effects_of_water_soluble_polymers_on_vinpocetine_complexation_with_beta_cyclodextrin_and_its_sulfobutyl_ether_derivative_in_solution_and_solid_state_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928098703001994 DB - PRIME DP - Unbound Medicine ER -