OBJECTIVE:To prepare Fluconazole adhesive gel.METHODS:Using carbopol934p,glycerine and other inor?ganic solvents as adjuvant,the Fluconazole adhesive gel was prepared.Then the pharmaceutic study and quality standard es?tablishment were carried out.RESULTS&CONCLUSION:The Fluconazole adhesive gel was simple in preparation and stable in property.The adhesive gel may become an ideal antifungal preparation for topical application.

Bioavailable studies were performed based on plasma concentrations of captopril in 5 Beagle dogs and 5 male healthy volunteers after a single oral administration of captopril sustained-release tablet and sugar-coated tablet. A one-compartment model was adopted. Relative bioavailability of sustained-release tablet to sugar-coated one was 131.6% for dogs and 111.0% for humans. Their mean residence times (MRTs) were 4.52 h and 1.96 h in dogs, 4.28 h and 2.77 h in humans, respectively. The maximum concentrations were 995.9 ng/ml and 2470.8 ng/ml in dogs, 126.2 ng/ml and 251.2 ng/ml in humans for two kinds of tablets, respectively. The duration time, in which plasma concentration staved above 50% inhibitory concentration of angiotensin converting enzyme activity, was more than 10 h for sustained-release tablets and 6h for sugar-coated tablets at the same dose (37.5 mg). consequently, it could be expected that the sustained-release tablet dosed twice a day should have a greater efficiency than marketed sugar-coated tablet taken 3 times daily.

Lappaconitine hydrobromide can remove inflammation and swelling, lower temperature and relieve heat. It also can be used for local anesthesia. Clinically lappaconitine hydrobromide can be applied via i.v., i.m. or p.o. for analgesic treatment. Lappaconitine has better effect for moderate pain than for severe pain, which may be associated with the low dose. Future efforts should be made in increasing dosage, combining lappaconitine hydrobromide with other drugs and improving drug delivery technique.

To prepare bio-degradable albumin microspheres containing carboplatin. METHODS: Bovin serum albumin microspheres containing carboplatin were prepared by using emulsion-direct heat cross linking techniques. RESULTS: The microsphere was yellow, powdery, with a mean diameter of 58.2 μm. The microphere loaded (11.26±0.48)% carboplatin. The trapping efficiency was (84.5±3.6)%. The pattern of drug releasing from the microspheres in vitro fitted to zero order release plot, with an initial burst in the first 2 hours. The releasing rate can be expressed by the follow equation: Q=21.90+8.50 t (d), r=0.995 8. t50=3 d. Stored at 4 ℃ and 37 ℃ respectively for 3 months, the microspheres did not alter much in shape, size and drug content. CONCLUSIONS: This method is simple, reproducible, having high drug trapping efficiency. The microsphere obtained is stable and release drug at a consistant rate in vitro, leading to a prosperity in clinical use.

Objective: To study the pharmacokinetic progress of diclofenac sodium microemulsions in rabbits. Methods: Diclofenac sodium microemulsion and diclofenac sodium suspension were single orally given to rabbits. Diclofenac sodium concentrations in plasma were measured by HPLC method. Results: AUC 0 ∞ , c max1 and t max1 were 13.456 ?g?h?ml -1 , 2.852 ?g/ml and 1.438 h after po diclofenac sodium microemulsion and 10.584 ?g?h?ml -1 , 3.145 ?g/ml and 0.750 h after po diclofenac sodium suspension. Conclusion: The absorption of diclofenac sodium microemulsions in rabbits is slower and can keep a higher concentration in plasma for a long time compared with those of the suspension. [

Objective: To prepare ibuprofen dispersible tablet and compare its pharmacokinetics and bioavailability with market tablets in rabbits. Methods: According to inspection of factors and orthogonal design, optimal formulation was decided. A randomized crossover and self control design was used. Eight healthy rabbits were single oral dosed with 100 mg ibuprofen dispersible tablet or market tablet, respectively. The plasma drug concentration was determined by HPLC method. The pharmacokinetic parameters were calculated by 3P87 program and the bioequivalence was assessed by NDST5.0 program. Results: A one compartment open model was adopted and the pharmacokinetic parameters of dispersible tablet and market tablet were as follows: c max were (9.79?2.25) and (4.54?1.50) ?g/ml; t max were (0.27?0.07) and (2.03?0.53) h; t 1/2 were (6.65? 2.14) and (9.17?4.38) h; AUC 0~∞ were (94.11?28.38) and (65.20?18.38) ?g?h?ml -1 , respectively. Ralative bioavailability of the dispersible tablet was 164.11% compared to market tablet. Conclusion: Ibuprofen dispersible tablet is administrated easily and absorbed quickly, and its bioavailability is far more better than the market one. [

Objective: To prepare silibinin solid dispersion and measure its dissolution in vitro .Methods: Silibinin solid dispersions were obtained with urea, PVP and poloxamer188 as carriers by melting and coevaporation methods. Differential thermal analysis and powder X ray diffraction were used to determine the status of drug in carriers, and the dissolution characteristics in vitro were studied in simulated gastric juice. Results: In PVP silibinin solid dispersions drug was amorphous; in poloxamer188 silibinin solid dispersions, drug existed as fine crystal, while in urea silibinin solid dispersions most of silibinin existed as crystal, only a little as molecule. Poloxamer188 was the better carrier in improving the solution and dissolution rate of the drug. Conclusion: Poloxamer188 is a very useful carrier in improving the solubility and dissolution of silibinin. [

OBJECTIVE:To prepare transferrin(TF)modified tetrandrine(TET)and vincristine(VCR)active targeting lipo-somes,and to optimize its formulation. METHODS:TF modified TET and VCR liposomes were prepared by ammonium sulfate gradient method. Using comprehensive score of encapsulation efficiency of TET and VCR as index,central composite design-re-sponse surface method was used to optimize and validate mole ratio of EPC/Chol,mole ratio of EPC/PEG2000-DSPE and TF mass fraction. RESULTS:The optimal formulation was that the mole ratios of EPC/Chol and EPC/PEG2000-DSPE were 1.5:1 and 20:1, TF mass fraction was 0.10%. The encapsulation efficiency of TET and VCR were 97.80% and 93.00%,respectively. The compre-hensive score was 94.44(n=3)which was close to the predicted value of 93.81. CONCLUSIONS:The optimal formulation is sta-ble and can be used for the preparation of TF modified TET and VCR liposomes.

OBJECTIVE:To study the anti-tumor effects of Vinblastine (VLB) hydrophilic group modified cationic liposomes in tumor-bearing mice. METHODS:Tumor-bearing model were induced by inoculating yellow ascites of S180 ascites tumor mice. Tumor-bearing mice were randomly divided into model group,VLB sulfate injection group,VLB liposomes group,VLB hydrophil-ic group modified liposomes group,VLB cationic liposomes group and VLB hydrophilic group modified cationic liposomes group, i.e. group A,B,C,D,E and F,with 18 mice in each group. Group A was given normal saline intravenously via mice tail,other groups were given VLB 1.5 mg/kg every 2 days for consecutive 5 times. The anti-tumor effects of different VLB preparations were compared,using living conditions,survival time,tumor volume and weight,and tissue pathological section as indexes. RE-SULTS:Compared with group A,B,C,D and E,the mice of group F were more active,and had longer survival time,smaller tumor volume and lighter tumor weight,with statistical significance(P<0.05). The tissue pathological section of mice in group F indicated that coagulation necrosis,disintegration,and dissolution of tumor cell nucleus. CONCLUSIONS:VLB hydrophilic group modified cationic liposomes have obvious anti-tumor effect,which are better than other VLB preparations.

OBJECTIVE:To establish the method for the determination of main components content and entrapment efficiency of transferrin modified vincristine-tetrandrine liposomes. METHODS:HPLC method was adopted to determine the content of vin-cristine. The determination was performed on ELITE C18 column with mobile phase consisted of methanol-15%triethylamine (70∶30)at a flow rate of 1.0 ml/min. The determination wavelength was set at 297 nm and column temperature was 30 ℃. The sample size was 20 μl. Free drug was isolated from liposomes by dextran gel column chromatography,and entrapment efficiency was deter-mined. RESULTS:The linear range of vincristine was 160-1 600 μg/ml (r=0.999 8,n=5) with average recovery of 99.20%(RSD=0.26%,n=9). RSD of precision test was 0.070%(n=5). The average content of vincristine in liposomes was 0.790 mg/ml(RSD=0.15%,n=3),and the average entrapment efficiency was 85.94%(RSD=2.08%,n=3). CONCLUSIONS:The method is accurate,reliable,simple and rapid,and can be used for the determination of the content and entrapment efficiency of vincristine in transferrin modified vincristine-tetrandrine liposomes.