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The Basic Research of Cholic Acid in Nasal Drug Delivery System

Author: SuZuoZuo
Tutor: YangMing
School: Chengdu University of Traditional Chinese Medicine
Course: Pharmacy
Keywords: Cholic acid Hydroxypropyl-β- cyclodextrin Pernasal administration system Nasal irritation
CLC: R944
Type: Master's thesis
Year: 2009
Downloads: 27
Quote: 0
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Abstract


The basic problems of the system by the nasal administration purposes cholic solve critical issues cholic pernasal administration, ensuring cholic acid through the nasal administration security, stability and effectiveness of the medicine containing cholic good service in clinical, to provide strong support to highlight its advantages in the treatment of rhinitis, stroke and other illnesses. Bile acid inclusion compound was prepared using HP-β-CD method to solve the bile acid after intranasal administration of key issues, the application of orthogonal test to identify conclusive evidence of the inclusion complex optimization Technique for Preparing and phase identification, and design to ease the actual effect of the bile acid nasal irritation nasal irritation evaluation tests on HP-β-CD were evaluated, in addition to the corresponding tests examine HP-β-CD solubility of bile acids, nasal permeability in vitro the impact of the anti-inflammatory effects and stability. The best preparation: feed ratio of 1:3, the inclusion temperature of 60 ° C, stirring time 60min liquid medicine drops acceleration 1.6ml · min -1 ; differentiated through four objects confirmed success of bile acid - hydroxypropyl-β-cyclodextrin inclusion complex formation; cilia toxicity test, acute irritant morphological evaluation of the results of the bile acids after HP-β-CD inclusion, nasal irritation evident improvement (p lt; 0.05). Sequential administration containing bile acid 0.5mg · ml -1 clathrate is very weak solution of rat nasal irritation, and after stopping the treatment nasal self-recovery; inclusion constant K = 564.30 L.mol -1 , HP-β-CD concentration of 40mM, bile acid solubility was 11.81 ± 0.10 times the original solubility; sheep nasal penetration test, inclusion The permeability coefficient, respectively, and steady-state flow of bile acids 1.46,1.44 times; bile acids by hydroxypropyl-β-cyclodextrin inclusion after its anti-inflammatory effects are not affected (p gt; 0.05); bile acids by hydroxypropyl-β-cyclodextrin inclusion will not result in high temperature, high humidity, high light environment unstable, it will not result in the relative humidity 75%, temperature 40 ℃ under the conditions placed without stable. Conclusion hydroxypropyl-β-cyclodextrin can improve the cholic nasal irritation, increased bile acids in vitro solubility and nasal permeability, the cholic acid anti-inflammatory effects as well as stability and does not affect, and show that HP-β-CD bile acid inclusion complex was prepared to address the key issues of the bile acid nasal administration feasible.

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