| With the development of standard of living, the problem of obesity becomesmore serious every day. Obesity and obesity-related metabolic disease areincreasingly affecting our daily life. Though there were several drugs for weight loss,like fenfluramine, sibutramine and others, most of them were withdraw from themarket because of safety problem. Along with the concern about the safety of thepharmaceutical chemicals, Chinese medicine and phytochemical drug has recentlyexcited interest.Chitosan is a kind of polysaccharose which is extracted from crab shells. Ourteam previously preparaed chitosan microsphere（CTMS）, and proved that the abilityof CTMS in anti-obesity and antilipidemic was better than that of CTS.Capsaicin（CAP）, a natural anti-obesity substance, can affect obesity on energybalance, adipogenesis, lipometabolism and others. Many researchers have proved thatit could control the weight of people suffered from obesity and overweight. Thought itis a good anti-obesity substance, the pungency and bad oral bioavailability made itusage in anti-obesity. In our laboratory, we developed capsaicn-chitosanmicrosphere（CCMS）. Anti-obesity experiments have showed that CCMS was better atimproving the obesity than capsaicin and chitosan microsphere（CTMS）, and thetolerance increased. This study is to research the tissue distribution of CTMS, and thepharmacokinetic of CCMS, it can also explain the anti-obesiy mechanism of CTMSand CCMS in pharmacokinetic.For the first, the chitosan microspheres were labeled by fluorescence FITC, thefluorescence was used to detect the pharmacokinetic profile and tissue（serum, heart, liver, spleen, lung, kidney） distribution of chitosan microsphere. In order to determinethe proper condition, the pH, temperature, concentration of FITC, ratio of mass wereresearched. At last, we prepared FITC-CTMS with the labeling efficiency was2.21%.FITC-CTS and FITC-CTMS were oral administrated in SD rats, the serum, heart,liver, lung, kidney, urine, feces were collected at fixed time. The study found thatFITC-CTS and FITC-CTMS were concentrated on liver and kidney, most of themwere in liver, there were a little in heart, spleen, lung and serum. Compared withFITC-CTS, the absorption of FITC-CTMS was improved, and tissue distribution washigher than that of FITC-CTS. The exertion research showed that most of FITC-CTSand FITC-CTMS was exerted in feces with a little absorption after oral administrated,and the absorption of FITC-CTMS was better than that of FITC-CTS.The pharmacokinetic profile and tissue distribution of CCMS was researched byHPLC after CAP and CCMS were oral administrated. And the exertion of CAP andCCMS was also studied. It can provide the direction for further research about CCMS.The Tmax, Cmax, T1/2β, AUC0-tof CAP were1.33±0.26h,814.60±59.47ng·mL-1,2.22±0.47h,3830.52±667.65h·ng·mL-1. The Tmax, Cmax, T1/2β, AUC0-tof CCMS were2.75±0.27h,1257.67±99.85ng·mL-1,3.48±0.53h,5848.41±754.81h·ng·mL-1. Thetissue distribution study also showed that the concentration of CCMS in tissue werehigher than that of CAP. As can be seen by the recommendations and observations,the absorption and bioavailability were improved after CAP was made into CCMS. |
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