Characterization and in vivo evaluation of lacidipine inclusion complexes with β-cyclodextrin and its derivatives
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- 作者：T. Darekar ; K. S. Aithal ; R. Shirodkar…
- 关键词：Lacidipine ; Sulfobutyl ether β ; cyclodextrin ; Solubility ; Complexation
- 刊名：Journal of Inclusion Phenomena and Macrocyclic Chemistry
- 出版年：2016
- 出版时间：April 2016
- 年：2016
- 卷：84
- 期：3-4
- 页码：225-235
- 全文大小：1,086 KB
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K. S. Aithal (2)
R. Shirodkar (1)
L. Kumar (1)
Z. Attari (1)
S. Lewis (1)
1. Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, 576 104, India
2. Department of Physics, Manipal Institute of Technology, Manipal University, Manipal, 576 104, India - 刊物类别：Chemistry and Materials Science
- 刊物主题：Chemistry
Organic Chemistry
Food Science
Crystallography - 出版者：Springer Netherlands
- ISSN：1573-1111
文摘
The objective of the study was to explore the possible formation of the inclusion complex of lacidipine (LCDP), a class II drug under biopharmaceutics classification system (BCS) with beta-cyclodextrin (β-CD) and modified β-CDs: hydroxy propyl- beta-cyclodextrin (HP-β-CD) and sulfobutyl ether-beta-cyclodextrin (SBE-β-CD) in order to enhance the solubility and the dissolution rate of the drug with an intention to improve its bioavailability. The stability constants found using phase solubility studies showed that SBE-β-CD formed the most stable inclusion complex with the drug (K = 348 ± 4 M−1) compared to the other cyclodextrins (CDs). The thermal analysis confirmed this finding. IR spectral analysis indicated the involvement of the hydroxyl function of CDs with the COOH of the drug. H1 NMR and 13C NMR spectral analysis indicated that the aromatic ring of drug included deeply in the CD cavity leaving the side chain protruding outside the CD cage and hydrogen bonds are formed which stabilizes the complex formation. The dissolution of the drug was improved on complexation with SBE-β-CD more effectively compared to the other CDs. The in vivo pharmacokinetic study of the complexes in Wistar rats showed an increase in AUC value by 1.5–2 times in case of (HP-β-CD) and SBE-β-CD compared to the plain drug and maximum with SBE-β-CD complex (Cmax = 242 ± 150 ng/ml, AUC = 1506.95 ± 0.505 ng/ml h).