| Chitosan (1,4)-2-amino-2-deoxy-β-D-glucan, is a deacetylation derivative of chitin. It has good biocompatibility, film-forming ability, and biodegradable ability, but its poor solubility in water or organic solvents is also manifest.In this work, water soluble hydroxypropyl chitosan(HPC) was prepared through the reaction of chitosan with cyclooxypropane under gentle conditions. The process parameters including the time of basification, amount of NaOH and isopropanol, reaction temperature, and reaction time were examined in single factor test. The results showed that all the factors above can significantly influence the degree of substitution of hydroxypropyl. Based on the Uniform Design method, the reactive conditions were optimized and the product of HPC with degree of substitution of about 0.55 was obtained. We measured the physical and chemical properties of HPC, such as degree of substitution, degree of deacetylation, intrinsic viscosity, viscosity average molecular weight, bulk density, solubility, temperature of glass transition, and characteristics of infrared spectrum. The stability of HPC against high temperature, high humidity, and light was also studied.At the same time, using loxoprofen sodium as model drug, HPC or HPMC as gel skeletons, following the principles on the prolong-released and controlled-released preparation in appendix XIXD, CHP 2000, based on the results of single factors test and consulted similar products in market, we designed and screened the prescriptions of prolong-released tablets, and prepared prolong-released gel skeleton tablets of loxoprofen sodium and established its quality standard.Using loxoprofen sodium tablets as control, in vivo pharmacokinetics of prolong-released gel skeleton tablets prepared in this work in Beagle dogs was investigated. An appropriate HPLC nethod was developed for measuring the concentration of loxoprofen sodium in blood.
|
PDF Full Text Request