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OBJECTIVE:To prepare aspirin phospholipid complex (ASP-PC) and conduct the characterization. METHODS:Using the combination rate of ASP and PC as index,single factor test was used to screen the preparation method of ASP-PC,PC type,solvent type,reaction time,reaction temperature,solvent volume and drug-lipid ratio. The verification test was conducted. UV spectrophotometry,Thermogravimetric analysis,X-ray diffraction and Fourier transform infrared spectroscopy were used for the characterization of ASP-PC. RESULTS:Magnetic stirring-condensing reflux method was adopted,drug-soybean phospholipids ratio was 1:3 (mol/mol),solvent was tetrahydrofuran,reacting for 3 h under 58 ℃. The average combination rate of prepared ASP-PC was 83.52％(RSD=1.16％,n=3). Compared with ASP,physical mixture of ASP and PC,UV spectrum showed that ASP-PC had no new absorption peak. Thermogravimetric analysis,X-ray diffraction and Fourier transform infrared spectroscopy showed the ASP and PC in ASP-PC were interacted;and ASP-PC changed little in quality within 0-300 ℃. CONCLUSIONS:ASP-PC can be successfully prepared,in which,ASP and PC were combined successfully;while there are still trace amounts of ASP in the form of crystals.
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OBJECTIVE:To study the pharmacokinetics behaviors and the bioavailability of aspirin phospholipid complex self-microemulsion in rats in vivo. METHODS:12 SD rats were randomly divided into aspirin suspension group(10 mg/kg)and as-pirin phospholipid complex self-microemulsion group (10 mg/kg),6 in each group. Rats were intragastrically administrated,and blood sample 0.6 mL was taken from jugular vein before administration and after 0.083,0.25,0.5,0.75,1.0,2.0,3.0,4.0,6.0, 8.0,12.0 h of administration. HPLC was used to determine the concentration of salicylic acid in rats'plasma. DAS 2.0 pharmacoki-netic software was adopted to calculate the pharmacokinetic parameters and relative bioavailability. RESULTS:The pharmacokinetic processes of both aspirin suspension and aspirin phospholipid complex self-microemulsion were in line with one-compartment mod-el. The salicylic acid of cmax of rats in aspirin suspension group and aspirin phospholipid complex self-microemulsion group were (1.904 ± 0.208),(6.457 ± 1.091) μg/mL;AUC0-12 h were (12.860 ± 1.327),(47.270 ± 12.860) μg/(h·mL);tmax were (2.167 ± 0.983),(0.917±0.540)h,respectively. Compared with aspirin suspension,salicylic acid of cmax and AUC0-12 h of aspirin phospholip-id complex self-microemulsion in rats in vivo were significantly increased (P<0.01),while tmax was significantly decreased (P<0.05);the relative bioavailability was 367.57%. CONCLUSIONS:Making aspirin into phospholipid complex self-microemulsion can improve the gastrointestinal absorption,with high relative bioavailability.
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BACKGROUND:Drug treatment is the main method for the treatment of diabetes currently, but the development of the disease and occurrence of related complications are the chal enges to the effect of drugs. OBJECTIVE:To investigate the effect and feasibility of co-transplantation of bone marrow mesenchymal stem cells and islet cells for the treatment of diabetes. METHODS:The rat bone marrow mesenchymal stem cells were separated and purified, and cultured in vitro to establish the diabetes models. The rat diabetes models were injected with bone marrow mesenchymal stem cells, co-cultured mixture of bone marrow mesenchymal stem cells and islet cells, and normal saline or phosphate buffer (control). The effect of transplantation was evaluated through observing the blood glucose levels, insulin secretion, and pathological changes of pancreatic tissue in the rat diabetes models. RESUTLS AND CONCLUSION:In the diabetes rats treated with bone marrow mesenchymal stem cel transplantation, the C-peptide levels were significantly increased after transplantation, while the blood glucose levels were significantly decreased, but not lower than the normal level, and the blood glucose levels were increased again with the time prolonging. In the diabetes rats treated with co-transplantation of bone marrow mesenchymal stem cells and islet cells, the blood glucose levels were decreased significantly and lower than the normal level which was maintained in a certain time, and the decreasing degree was larger than that in the rats treated with simple bone marrow mesenchymal stem cel transplantation. Co-transplantation of bone marrow mesenchymal stem cells and islet cells is feasible for the treatment of diabetes with a certain effect.
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BACKGROUND:Compound Chinese medicine is a kind of compound drugs with the combination of minerals, plants and animals, which play the multi-target integrated treatment effects in the treatment of bone metabolic disease through various methods. OBJECTIVE:To research the effect of compound traditional Chinese medicine on the proliferation and bone mineral density of osteoblasts, and to explore the pharmacological effect of compound traditional Chinese medicine in the treatment of osteoporosis. METHODS: A retrospective analysis was performed to analyze the effect of some compound traditional Chinese medicines on the proliferation and bone mineral density of osteoblasts that identified in the previous studies, in order to analyze the factors of compound traditional Chinese medicines that can promote the bone formation. The appropriate dose of the drugs that can promote cel proliferation and differentiation and improve the bone mineral density was screened out through the in vitro culture of osteoblasts, and then compared with the results of chemical medicines. RESULTS AND CONCLUSION:Compound traditional Chinese medicines can promote the proliferation and differentiation of osteoblasts and improve the bone mineral density, and have the advantages of ful treatment and less side effect in the treatment of osteoporosis. But the effect of compound traditional Chinese medicines in improving the bone mineral density is less than the chemical drugs. The long-term and large-sample clinical studies should be performed to decrease the risk of osteoporotic fracture.