Investigation and Physicochemical Characterization of Vinpocetine-Sulfobutyl Ether .BETA.-Cyclodextrin Binary and Ternary Complexes
- 1 January 2003
- journal article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 51 (8), 914-922
- https://doi.org/10.1248/cpb.51.914
Abstract
The purpose of this study was to investigate the interactions between vinpocetine (VP), sulfobutyl ether beta-cyclodextrin (SBEbetaCD) and the water-soluble polymers polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC). The water-soluble polymers were shown to improve the complexation efficiency of SBEbetaCD, and thus less SBEbetaCD was needed to prepare solid VP-SBEbetaCD complexes in the presence of the polymers. The interactions between VP and SBEbetaCD, with or without PVP or HPMC, were thoroughly investigated in aqueous solutions using the phase-solubility method as well as in the solid state. The amount of VP solubilized in water or aqueous polymer solution increased linearly with increasing SBEbetaCD concentration, demonstrating A(L)-type plots. We estimated the apparent stability constant (K(c)) at room temperature of VP-SBEbetaCD binary complex to be 340 M(-1) and this value increased to 490 M(-1) or 390 M(-1), respectively, with the addition of PVP and HPMC, assuming a 1 : 1 VP-SBEbetaCD molar ratio. Improvement in the K(c) values for ternary complexes clearly confirmed the benefit of the addition of water-soluble polymers to promote higher complexation efficiency. Solid VP-SBEbetaCD binary and ternary systems were prepared by physical mixing, kneading, coevaporation, and lyophilization methods and fully characterized by scanning electron microscopy, differential scanning calorimetry, and X-ray diffractometry. The results obtained suggest that coevaporation and lyophilization methods yield a higher degree of amorphous entities and indicated formation of VP-SBEbetaCD binary and ternary complexes.Keywords
This publication has 31 references indexed in Scilit:
- Effect of the Hydrophobic Nature of Triacetyl-.BETA.-cyclodextrin on the Complexation with Nicardipine Hydrochloride: Physicochemical and Dissolution Properties of the Kneaded and Spray-dried Complexes.CHEMICAL & PHARMACEUTICAL BULLETIN, 2002
- Interactions of Griseofulvin with Cyclodextrins in Solid Binary SystemsJournal of Pharmaceutical Sciences, 1998
- Pharmaceutical Applications of Cyclodextrins. III. Toxicological Issues and Safety EvaluationJournal of Pharmaceutical Sciences, 1997
- Pharmaceutical Applications of Cyclodextrins. 2. In Vivo Drug DeliveryJournal of Pharmaceutical Sciences, 1996
- Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and StabilizationJournal of Pharmaceutical Sciences, 1996
- Analytical applications of retinoid—cyclodextrin inclusion complexes: 1. Characterization of a retinal—β—cyclodextrin complexJournal of Pharmaceutical and Biomedical Analysis, 1996
- The effect of water-soluble polymers on aqueous solubility of drugsInternational Journal of Pharmaceutics, 1996
- The effect of water-soluble polymers on drug-cyclodextrin complexationInternational Journal of Pharmaceutics, 1994
- Psychopharmacological effects of vinpocetine in normal healthy volunteersEuropean Journal of Clinical Pharmacology, 1985
- Inclusion compounds of non-steroidal antiinflammatory and other slightly water soluble drugs with .ALPHA.- and .BETA.-cyclodextrins in powdered form.CHEMICAL & PHARMACEUTICAL BULLETIN, 1975