Objective: To optimize the preparation technique for bifonazole suppositories and evaluate the quality.Methods: The appearance, hardness and melting time of suppositories were used as the evaluation indices to optimize the process conditions, such as suppository matrix, drug particle size, injection molding temperature and stirring conditions, etc.The content of bifonazole was determined by HPLC.Results: The best formula was as follows: the matrix was multiplicated monofatty glyceride-36, bifonazole was sieved by 100 mesh sieve and the best molding temperature was 45 ℃.The quality of the prepared suppositories with the above conditions was controllable in the appearance, melting time limit, hardness and content determination, etc.Conclusion: The formula of bifonazole suppositories is reasonable, the preparation process is feasible, and the quality control methods are reliable.

This study examined the effect of self-microemulsiflying drug delivery system (SMEDDS) containing Cremophor RH40 or Tween 80 at various dilutions on cytochrome P450 3A (CYP3A) enzymes in rat hepatocytes, with midazolam serving as a CYP3A substrate. The particle size and zeta potential of microemulsions were evaluated upon dilution with aqueous medium. In vitro release was detected by a dialysis method in reverse. The effects of SMEDDS at different dilutions and surfactants at different concentrations on the metabolism of MDZ were investigated in murine hepatocytes. The cytotoxicity of SMEDDS at different dilutions was measured by LDH release and MTT technique. The effects of SMEDDS on the CYP3A enzymes activity were determined by Western blotting. Our results showed that dilution had less effect on the particle size and zeta potential in the range from 1:25 to 1:500. The MDZ was completely released in 10 h. A significant decrease in the formation of 1'-OH-MDZ in rat hepatocytes was observed after treatment with both SMEDDS at dilutions ranging from 1:50 to 1:250 and Cremophor RH 40 or Tween 80 at concentrations ranging from 0.1% to 1% (w/v), with no cytotoxicity observed. A significant decrease in CYP3A protein expression was observed in cells by Western blotting in the presence of either Cremophor RH40 or Tween 80-based SMEDDS at the dilutions ranging from 1:50 to 1:250. This study suggested that the excipient inhibitor-based formulation is a potential protective platform for decreasing metabolism of sensitive drugs that are CYP3A substrates.

Objective To observe the effect of treating Diabetic Peripheral Neuropathy with Acupoint Injection. Methods 65 patient with DPN were randomly recruited into a control group and a treatment group after adjusting stage. The control group was treated with acupuncture, while the treatment group was treated with the Safflower inoculation fluid acupuncture point injects. Nerve function parameter (MDNS、 NCV) and clinical symptoms were observed after 3 therapeutic courses. Results Nerve function parameter (MDNS、 NCV) and clinical symptoms in the treatment group were apparently improved after treatment (P<0.05) . Conclusion Acupuncture point injected with Safflower inoculation fluid may improve clinical symptoms and nerve functions of DPN patients.

AIM: To investigate the role of CD134 (OX40) and NF-?B in the pathogenesis of lupus nephritis (LN). METHODS: Renal in situ CD134 and NF-?B expression were examined in 40 biopsy specimens from LN patients by immunohistochemistry and microwave-based immunohistochemistry, respectively. The relationship between expression of CD134 and NF-?B was analyzed. RESULTS: The expression of glomerular and tubular CD134 and NF-?B in LN were higher than that in normal control, especially in class Ⅳ LN, where there was intense staining of endothelial cell, distal tubules, and interstitial mononuclear cell. The CD134 expression of glomerular and tubular was closely related to NF-?B expression, respectively ( r=0.5542,P

Objective: To observe the clinical therapeutic effect of Tang Shen Ning(TSN,a prescription of traditional Chinese medicine)for curing the early stage of diabetic nephropathy(DN).Methods: Adopting random and double-blind controlled trial methods,several indexes were observed in terms of uric micro-amount albumin excretion rate,creatinine clearance,hemorheology and platelet function et al.Results: TSN could significantly reduce urinary albumin,glomerulus's hyper-filtration,improve blood stream transform and inhibit platelet aggregation.Conclusion: TSN could protect renal functions during the early stage of DN.

This study examined the effect of self-microemulsiflying drug delivery system (SMEDDS) containing Cremophor RH40 or Tween 80 at various dilutions on cytochrome P450 3A (CYP3A) enzymes in rat hepatocytes, with midazolam serving as a CYP3A substrate. The particle size and zeta potential of microemulsions were evaluated upon dilution with aqueous medium. In vitro release was detected by a dialysis method in reverse. The effects of SMEDDS at different dilutions and surfactants at different concentrations on the metabolism of MDZ were investigated in murine hepatocytes. The cytotoxicity of SMEDDS at different dilutions was measured by LDH release and MTT technique. The effects of SMEDDS on the CYP3A enzymes activity were determined by Western blotting. Our results showed that dilution had less effect on the particle size and zeta potential in the range from 1:25 to 1:500. The MDZ was completely released in 10 h. A significant decrease in the formation of 1'-OH-MDZ in rat hepatocytes was observed after treatment with both SMEDDS at dilutions ranging from 1:50 to 1:250 and Cremophor RH 40 or Tween 80 at concentrations ranging from 0.1% to 1% (w/v), with no cytotoxicity observed. A significant decrease in CYP3A protein expression was observed in cells by Western blotting in the presence of either Cremophor RH40 or Tween 80-based SMEDDS at the dilutions ranging from 1:50 to 1:250. This study suggested that the excipient inhibitor-based formulation is a potential protective platform for decreasing metabolism of sensitive drugs that are CYP3A substrates.

OBJECTIVE To prepare curcumin /berberine co -loaded self -microemulsion drug delivery system （CUR/BER- SMEDDS）and evaluate its physicochemical properties and in vitro anti-tumor effects . METHODS Using CUR and BER as model drug，based on the screening of the type of oil phase ，emulsifier，co emulsifier and their mass ratio ，the formulation of CUR/BER - SMEDDS were optimized by central composite design -response surface methodology ，taking particle size and drug loading as evaluation parameters ，with the mass percentage of oil phase and the mass ratio of emulsifier to co emulsifier as factors ，and verification test was conducted . CUR/BER-SMEDDS prepared by optimized formulation were evaluated in terms of physicochemical properties，in vitro dissolution and in vitro anti-tumor effects . RESULTS The optimized formulation of CUR/BER -SMEDDS included that the oil phase was medium chain triglyceride （30.97%），the emulsifier was polyoxyl 40 hydrogenated castor oil （46.77%），the co emulsifier was polyethylene glycol 400（22.26%），and the mass ratio of emulsifier to co emulsifier was 2.10∶1. The validation experiments showed that mean particle size of CUR/BER -SMEDDS was（58.90±5.41）nm，the average drug loading was（94.94±3.87）mg/g，and the relative deviations from the predicted values were －2.90% and －0.14%，respectively. The CUR/ BER-SMEDDS prepared by optimal formulation was light yellow ，clear and transparent liquid after emulsified with water ，and its particles were spherical . The results of dissolution test in vitro showed that after SMEDDS was made ，the cumulative dissolution of CUR in artificial intestinal fluid and artificial gastric fluid and that of BER in artificial intestinal fluid were significantly higher than those of its raw material . Results of in vitro anti-tumor experiment showed that IC 50 values of CUR/BER -SMEDDS for PC -3 cells and DU -145 cells were （17.38±2.84）and（20.89±1.26）μmol/L，which were all lower than those of CUR and EBR significantly （P＜0.05）.CONCLUSIONS The optimized prepar ation process of CUR/BER -SMEDDS is stable and feasible . The drug release of CUR/BER-SMEDDS is more complete than that of single drug，and has stronger anti -prostate cancer effect in vitro .