AIM: To explore the correlativity of the oil/water partition of hydroxycamptothecin and its absorp-tion coefficiency in small intestine in rats.METHODS: pH value of water phase in buffer solution in turn took 2.2,4.6,7.4,9.6 and 11,while octanol was adopted as oil phase.After phase equilibrium,HPLC was used to determine the concentration of hydro-xycamptothecin,and oil/water partition coefficient was calculated with the phenol red as volume calibration agent,small intestinal absorption coefficients of rats in different pH were plotted against its oil/water partition coefficients.RESULTS: Oil/water partition coefficient(x) of hydroxycamptothecin and small intestinal absorption(y) altered with the change of pH value of the dispension medium.The linear re-gress equation was constructed as y = 0.001 3x + 0.009 1 with its correlation coefficient R2 being 0.959 7.CONCLUSION: There exists a good linear dependence between oil/water partition coefficient of hydroxycamptoth-ecin and its absorption coefficient in small intestines of rats.Oil/water partition coefficient can be used to design the new oral preparations.

OBJECTIVE:To compare therapeutic efficacy and safety of 3 ornidazole regimens in the treatment of chronic pel-vic inflammatory disease(PID). METHODS:A total of 120 chronic PID patients were randomly divided into ornidazole group(40 cases),combined with levofloxacin group(40 cases)and combined with cefdinir group(40 cases). Based on routine treatment,or-nidazole group was given Ornidazole tablet 0.5 g orally,day and night. Combined with levofloxacin group was additionally given Levofloxacin hydrochloride tablet 0.1 g orally,tid,on the basis of ornidazole group. Combined with cefdinir group was additional-ly given Cefdinir dispersible tablet 0.1 g orally,tid,on the basis of ornidazole group. Treatment course of 3 groups lasted for 10 d. Clinical efficacies of 2 groups were observed,and plasma viscosity (PV),hematocrit,CRP,IL-1,leucocyte count,lympho-cyte count,lymphocyte percentage and the occurrence of ADR were observed before and after treatment. RESULTS:Total response rate was in descending order:combined with cefdinir group(95.00%)>combined with levofloxacin group(82.50%)>ornidazole group(62.50%),with statistical significance(P<0.05). Before treatment,there was no statistical significance in PV,hematocrit, CRP,IL-1,leucocyte count,lymphocyte count or lymphocyte percentage among 3 groups(P>0.05). After treatment,above inel-exes of 3 groups were significantly lower than before;combined with cefdinir group0.05). CONCLUSIONS:Therapeutic efficacy of ornidazole combined with cefdinir is better than that of ornidazole combined with levofloxacin in the treatment of chronic PID,and its safety is similar to that of ornidazole alone.

This paper explore the possibility of using the partition of 10-hydroxycamptothecin in the phases of liposome and water to predict the absorption of the drug in small intestine of rats. In order to certify this theory, the in vivo absorption model have been used to study the absorption of 10-hydroxycamptothecin in the small intestine of rats while altering the pH of the medium. The correlation has been explored between the partition of drug in the phases of liposome and water and the absorption of drug in the small intestines of rats. And it was found that the partition of 10-hydroxycamptothecin in the phases of liposome and water and the absorption of the drug in small intestines of rats altered with the changes of pH, and there existed a good relative coefficient between them. All of these indicated that partition of 10-hydroxycamptothecin in phases of liposome and water can be used to predict its absorption in small intestines of rats.
Animals ; Camptothecin ; analogs & derivatives ; chemistry ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Hydrogen-Ion Concentration ; Intestinal Absorption ; physiology ; Intestine, Small ; metabolism ; Liposomes ; chemistry ; Rats ; Water ; chemistry

ABSTRACT OBJECTIVE：To study the improvement effect of Periplaneta americana extract Ento-A on damp-heat ulcerative colitis（UC）model rats. METHODS：Totally 70 rats were randomly divided into normal control group（n＝8）and modeling group （n＝62）. The damp-heat UC model was induced in modeling group by high sugar，high fat，spicy diet combined with 2，4， 6-trinitrobenzene sulfonic acid enema. 48 modelrats were randomly divided into model control group，mesalazine group （300 mg/kg），Changyanning group（300 mg/kg）and Ento-A low-dose，medium-dose and high-dose（50，100，200 mg/kg，calculated by the extract），with 8 rats in each group. Normal control group and model control group were given normal saline intrsgastrically，and other groups were given relevant medicine intragastrically，once a day，for consecutive 14 days. After last administration， disease activity index （DAI）， colonic mucosal injury index （CMDI） and histopathological score （HS）of rats were determined. The spleen index，liver index and colon index in rats were determined. The serum levels of IL-8，IL-17，SOD and MDA，colonic levels of IL-2，PGE2 and MPO were detected by ELISA. RESULTS：Compared with normal control group，the DAI score，CMDI score，HS score，colonic index，the serum levels of IL-8，IL-17 and MDA， colonic levels of MPO and PGE2 were increased significantly（P＜0.01）；serum level of SOD and colonic level of IL-2 were decreased significantly （P＜0.01）. Compared with model control group，DAI score，CMDI score，serum levels of IL-17 and MDA，colonic levels of PGE2 were decreased significantly in Ento-A high-dose groups（P＜0.05 or P＜0.01），while serum level of SOD and colonic level of IL-2 were increased significantly（P＜0.01）. CMDI score and HS score，serum levels of IL-8，IL-17 and MDA，colonic levels of PGE2 and MPO were decreased significantly in Ento-A medium-dose group（P＜0.05 or P＜0.01）， while colonic level of IL-2 was increased significantly（P＜0.01）. HS score，serum levels of IL-17 and MDA，colonic levels of MPO and PGE2 were decreased significantly in Ento-A low-dose group（P＜0.05 or P＜0.01），while serum level of IL-2 was increased significantly（P＜0.01）. CONCLUSIONS：P. americana extract Ento-A may play improvement effect on damp-heat UC rats by regulating immune system balance and reducing inflammatory damage.