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The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetracomponent complexes.
Drug Dev Ind Pharm. 2005 Sep; 31(8):747-56.DD

Abstract

In an effort to improve the solubility of the insoluble drug scutellarin, a novel complexation of scutellarin with beta-cyclodextrin (beta-CD) was studied. Tetracomponent freeze-dried complex was prepared with scutellarin, beta-CD, Hydroxypropyl Methylcellulose (HPMC), and triethanolamine. To confirm complex formation, complex was characterized by Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction, and differential scanning calorimetry (DSC). Phase-solubility analysis suggested the soluble complexes having 1:1 stoichiometry. The beta-CD solubilization of scutellarin could be improved significantly by combining water-soluble polymer and pH adjuster. Comparing the binary, ternary solid systems with tetrary systems, tetracomponent freeze-dried complex showed the best effect of solubilization. A maximal solubility of scutellarin (23.65 mg/ml) was achieved with tetracomponent freeze-dried complex, up to 148-fold increase over scutellarin solubility in water, and the solubility of scutellarin is 15.35 microg/ml (up to 6-fold) in simulated gastric fluid.

Authors+Show Affiliations

Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. China.No affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

16221609

Citation

Cao, Feng, et al. "The Physicochemical Characteristics of Freeze-dried Scutellarin-cyclodextrin Tetracomponent Complexes." Drug Development and Industrial Pharmacy, vol. 31, no. 8, 2005, pp. 747-56.
Cao F, Guo J, Ping Q. The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetracomponent complexes. Drug Dev Ind Pharm. 2005;31(8):747-56.
Cao, F., Guo, J., & Ping, Q. (2005). The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetracomponent complexes. Drug Development and Industrial Pharmacy, 31(8), 747-56.
Cao F, Guo J, Ping Q. The Physicochemical Characteristics of Freeze-dried Scutellarin-cyclodextrin Tetracomponent Complexes. Drug Dev Ind Pharm. 2005;31(8):747-56. PubMed PMID: 16221609.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetracomponent complexes. AU - Cao,Feng, AU - Guo,Jianxin, AU - Ping,Qineng, PY - 2005/10/14/pubmed PY - 2006/6/10/medline PY - 2005/10/14/entrez SP - 747 EP - 56 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 31 IS - 8 N2 - In an effort to improve the solubility of the insoluble drug scutellarin, a novel complexation of scutellarin with beta-cyclodextrin (beta-CD) was studied. Tetracomponent freeze-dried complex was prepared with scutellarin, beta-CD, Hydroxypropyl Methylcellulose (HPMC), and triethanolamine. To confirm complex formation, complex was characterized by Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction, and differential scanning calorimetry (DSC). Phase-solubility analysis suggested the soluble complexes having 1:1 stoichiometry. The beta-CD solubilization of scutellarin could be improved significantly by combining water-soluble polymer and pH adjuster. Comparing the binary, ternary solid systems with tetrary systems, tetracomponent freeze-dried complex showed the best effect of solubilization. A maximal solubility of scutellarin (23.65 mg/ml) was achieved with tetracomponent freeze-dried complex, up to 148-fold increase over scutellarin solubility in water, and the solubility of scutellarin is 15.35 microg/ml (up to 6-fold) in simulated gastric fluid. SN - 0363-9045 UR - https://www.unboundmedicine.com/medline/citation/16221609/The_physicochemical_characteristics_of_freeze_dried_scutellarin_cyclodextrin_tetracomponent_complexes_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639040500216220 DB - PRIME DP - Unbound Medicine ER -