Effect of Quaternization of N-trimethyl Chitosan on Properties of Insulin Liquid Suppositories in vitro
ZHANG Hong1，DAI Wen-bing2， HE Wen1， LI Jing2，ZHANG Mian2
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1.Department of Pharmacy，Renmin Hospital of Wuhan University，Wuhan 430072，China； 2.Department of Pharmacy，Wuhan University，Wuhan 430060，China
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Received
Published
2005-03-21
2006-02-10
Issue Date
2006-02-10
Abstract
OBJECTIVE To study the effect of quaternization and concentration of N-trimethyl chitosan on the physicochemical properties of insulin liquid suppositories in vitro.METHODS Two kinds of TMC with different degrees of quaternization,ie.TMC40 and TMC60,were synthesized by a two-step method using chitosan and methyl-iodide.The degrees of quaternization of TMC was determined by1H-NMR.P407 and P188 were used as liquid suppository bases to prepare insulin liquid suppository with TMC as the absorption enhancer.The changes of the characters of the liquid suppository in vitro were determined by measuring gel temperature,gel strength and bioadhesive force with different concentrations(0%,0.1%,0.5%,1%)and degrees of quaternization of TMC.RESULTS The degree of quaternization of TMC40 and TMC60 was 38.8% and 67.2%,respectively.With the increase of TMC concentration,there was an decrease in gelation temperature,while an increase in both of gel strength and bioadhesive force.With an increase in the degree of quaternization of the TMC,there was an increase in gelation temperature and an decrease in both of gel strength and bioadhesive force.CONCLUSION The degree of quaternization and concentration of TMC had significant influence on the properties of the liquid suppository in vitro.Adjusting of degrees of quaternization and concentration of TMC maybe improve the properties in vitro and enhance the rectal absorption of insulin.
ZHNG Hong;DI Wen-ing;HE Wen;LI Jing;ZHNG Min.
Effect of Quaternization of N-trimethyl Chitosan on Properties of Insulin Liquid Suppositories in vitro[J]. Chinese Pharmaceutical Journal, 2006, 41(04): 281-283
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