The physicochemical characteristics of freeze-dried scutellarin-cyclodextrin tetracomponent complexes

被引：29

作者：

Cao, F ^{[1
]}

Guo, JX ^{[1
]}

Ping, QN ^{[1
]}

机构：

[1] China Pharmaceut Univ, Dept Pharmaceut, Nanjing 210009, Peoples R China

来源：

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | 2005年 / 31卷 / 08期

基金：

中国国家自然科学基金;

关键词：

scutellarin; beta-cyclodextrin; tetracomponent complexes; Fourier transform infrared spectroscopy; powder X-ray diffraction; differential scanning calorimetry; phase solubility; solubility;

D O I：

10.1080/03639040500216220

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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 ug/ml (up to 6-fold) in simulated gastric fluid.

引用

页码：747 / 756

页数：10

共 25 条

[1]

Solubilization of tropicamide by hydroxypropyl-β-cyclodextrin and water-soluble polymers:: in vitro/in vivo studies [J].

Cappello, B ;

Carmignani, C ;

Iervolino, M ;

La Rotonda, MI ;

Saettone, MF .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 213 (1-2) :75-81

[2]

CHEN XX, 1998, J CHIN PHARM SCI, V7, P91

[3]

Cyclodextrin-based pharmaceutics: Past, present and future [J].

Davis, ME ;

Brewster, ME .

NATURE REVIEWS DRUG DISCOVERY, 2004, 3 (12) :1023-1035

[4]

Study of flavonoids/β-cyclodextrins inclusion complexes by NMR, FT-IR, DSC, X-ray investigation [J].

Ficarra, R ;

Tommasini, S ;

Raneri, D ;

Calabrò, ML ;

Di Bella, MR ;

Rustichelli, C ;

Gamberini, MC ;

Ficarra, P .

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2002, 29 (06) :1005-1014

[5]

Study of the inclusion complex of atenolol with β-cyclodextrins [J].

Ficarra, R ;

Ficarra, P ;

Di Bella, MR ;

Raneri, D ;

Tommasini, S ;

Calabrò, ML ;

Villari, A ;

Coppolino, S .

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2000, 23 (01) :231-236

[6]

Thermal analysis of hydroxypropylmethylcellulose and methylcellulose: powders, gels and matrix tablets [J].

Ford, JL .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 179 (02) :209-228

[7]

The effect of pH and triethanolamine on sulfisoxazole complexation with hydroxypropyl-β-cyclodextrin [J].

Gladys, G ;

Claudia, G ;

Marcela, L .

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2003, 20 (03) :285-293

[8]

Industrial applications of cyclodextrins [J].

Hedges, AR .

CHEMICAL REVIEWS, 1998, 98 (05) :2035-2044

[9]

Higuchi T., 1965, Interscience, New York, V4, P117

[10]

The physicochemical characteristics and bioavailability of indomethacin from β-cyclodextrin, hydroxyethyl-β-cyclodextrin, and hydroxypropyl-β-cyclodextrin complexes [J].

Jambhekar, S ;

Casella, R ;

Maher, T .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 270 (1-2) :149-166

← 1 2 3 →