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Preparation, Characterization Evaluation on Murraya Exotica L. Leaves Flavones-hydroxypropyl-β-cyclodextrin Inclusion Complex

Author: ZhangJianFang
Tutor: GaoJianQing
School: Zhejiang University
Course: Pharmacy
Keywords: Guri geraniol total flavonoids Hydroxypropyl-β- cyclodextrin Inclusion Complex Phase solubility Dissolution Bioavailability
CLC: TQ461
Type: Master's thesis
Year: 2010
Downloads: 201
Quote: 2
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Abstract


Guri geraniol total flavonoids (JK) is from the traditional Chinese medicine Guri fragrant leaf extract separation of flavonoids as the main component of an effective site, more than 90% of total flavonoids, significant therapeutic effect of acute myocardial infarction and diabetes. But due to the the Guri the geraniol total flavonoids polarity, poor water solubility, seriously affect the absorption, thus limiting its clinical application. , Such as preparation of a water-soluble good new formulations, will help improve the Guri the geraniol total flavonoid bioavailability, to create the conditions for its wide range of clinical applications. Cyclodextrins (CDs) having an annular hollow cylindrical structure, and able to form inclusion complexes with certain small molecule drugs. Cyclodextrin external polyhydroxy hydrophilic so the clathrate has good wettability, so as to achieve the effect on the solubilization of insoluble drugs. The most commonly used as a solubilizer is hydroxypropyl-β-cyclodextrin (HP-β-CD), having a good water-soluble, stable to heat, toxicity characteristics. Insoluble drug is its clathrate, can increase the drug solubility, dissolution rate and bioavailability. At home and abroad there is no Guri geraniol total flavonoids cyclodextrin reported. First hydroxypropyl-β-cyclodextrin inclusion material using solution - prepared by stir Guri geraniol total flavonoids - hydroxypropyl-β-cyclodextrin inclusion complex (JK-HP-β-CD ), basic research and the results are as follows: (1) to inspect the various factors affecting the inclusion reaction to identify the main factors, orthogonal design the best process. The results show that the best conditions for the inclusion reaction: HP-β-CD and JK molar ratio of 1:1, inclusion temperature 25 ℃, inclusion time 2h. The inclusion complex by differential scanning calorimetry, X-ray diffraction, and infrared spectroscopy identification, and confirmation of the formation of clathrate. (2) by phase solubility method confirmed JK and HP-β-CD formed between the molar ratio of 1:1 inclusion complexes belonging to the AL-type phase solubility diagram. Form a clathrate the JK at 25 ° C the solubility increased by 43.9 times. Dissolution medium sodium 0.2% sodium dodecyl sulfate solution, with reference to the rotating basket method for the determination of the Chinese Pharmacopoeia 2005 edition in vitro dissolution results clathrate dissolution rate significantly faster than the physical mixture and drug completely 15min minutes released. (3) the establishment of the plasma concentration was measured by high performance liquid chromatography analysis method, and preliminary investigation JK their inclusion in rats in vivo pharmacokinetic process. The results showed that after clathrate, JK blood concentrations can significantly improve their bioavailability in rats.

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