AIM:To optimize the formulation of Fuyankang Dispersible Tablets and study the in vitro release characteristics of them. METHODS: The orthogonal design was used to obtain the optimal formulation with the disintegration,hardness and weight of tablets as markers,and then dispersible uniform and the in vitro release characteristics of the optimal formulation were studied with dispersed experiment and PR-HPLC,respectively.(RESULTS:)The proportion of each adjuvant in the optimal formulation consisted of 10% MCC,4% L-HPC,12% PVPP.The optimized dispersible tablets disintegrated in 1 min,the hardness was 5.24 kg,the average weight was 0.407 g;the dispersible uniform was excellent,and the settling velocity equation was logF=-0.028-1.001?10~(-3)t;The released rate parameters of Fuyankang Dispersible Tablets were T_(50)=3.0 min and T_d=4.0 min,which were remarkly less than that of the control group,T_(50)=14.28 min and T_d=16.62 min(P

OBJECTIVE:To optimize the preparation technique of norcantharidin liposome(NL) and study its pharmaceutical properties. METHODS: With envelopment efficiency(EE), mean particle size and span of the liposome as indexes, the effects of thin-film dispersion method, injection method, reverse phase evaporation and reverse phase film-evaporation method on the EE and particle size of the NL were evaluated. And the uniform design was used to optimize the reverse phase film-evaporation preparation technique of NL with the amount of phospholipid (X1), the mass ratio of phospholipid/ cholesterol (X2), the sonde-type ultrasounding times (X3), the dilution times of buffer phosphate (X4), the volume ratio of oil/water phase (X5) and the mass ratio of lipoids/ drug (X6) as integrated indexes. A verification test was performed on the optimal technique. RESULTS: The formulation prepared by reverse phase film-evaporation technique exhibited the best EE. The preparation conditions of the optimized NL were as follows: X1=200 mg; X2=7∶1; X3=20 times; X4=50 times; X5=1∶4; X6=30∶1. The verification test showed that the EE, the mean particle size and the span of the liposome were (42.5?1.3)%, (210.9?2.1) nm and (0.61?0.12), respectively. CONCLUSION: NL was prepared successfully.

Objective:To select the binding-peptide of the cell surface marker CD133 of cancer stem cells from phage peptide library,and to find a new tool for research on stem cells,tumor therapy and anti-metastasis of cancer.Methods:Biotined mouse CD133 extracellular fraction was used as a target to screen phage 7-peptide library by the high affinity of streptavidin and biotin,and the clones were identified by sandwich ELISA and competitive experiment.Single strand DNA was extracted from these positive clones and was analyzed by single-strand dideoxy-sequencing.Results:After three turn solution panning,five peptides with high affinity shared the same amino acid sequence:APSPMIW and three identical peptides with high affinity shared the same amino acid sequence:LQNAPRS.Conclusion:The peptides that bind with mouse CD133 extracellular fraction with high affinity and specificity were first screened from the phage peptide library for the first time,which initially indicates that the feasibility of screening from phage peptide library with small molecule polypeptide biotined as a target.

Objective:To investigate the curative effect of electroacupuncture on urine retention following cervical cancer operation. Methods: A treatment group was treated with electroacupuncture according to classification based on syndrome differentiation and a control group, by a conventional method. One course of treatment consisted of 5 days. Results: The curative rate and cure rate were 96.67% and 76.67%, respectively, in the treatment group and 70% and 36.67%, respectively, in the control group. There were significant differences in curative rate and cure rate between the two groups (P＜0.01). Conclusion:Electroacupuncture is a good method for treating urine retention subsequent to cervical cancer operation.

AIM: To screen and optimize the preparation conditions of irisquinone-hydroxypropyl-?-cyclodextrin inclusion complex (Irisquinone-HP-?-CD) with stiring method. METHODS: The load-drug and recovery of irisquinone were adopted as the index, host-guest molar ratio, alcohol concentration and stiring rate as factors, have been investigated in the techniques of irisquinone-HP-?-CD. RESULTS: The load-drug and recovery of irisquinone-HP-?-CD were respective ( 15.79 ?0.22)% and ( 92.03 ?6.26)% by optimizing conditions which were host-guest molar ratio 2∶1, 90% EtOH and stiring rate 800r?min -1. At the same time, the dissolution test showed that irisquinone was faster released from inclusion complex than that from capsules and mixture dosage form. CONCLUSION: The optimizing techniques fit to prepare irisquinoe-HP-?-CD in industry.

Objective To parperare and identify the irisquinone-hydroxypropyl-?-cyclodextrin (irisquinone-HP-?-CD) inclusion compound. The inclusion mechanism and mol ratio of irisquinone and HP-?-CD were studied simultaneously. Methods The irisquinone-HP-?-CD was prepared with lyophilization technique. The mol ratio between host and guest moleculars was also researched by molecular gradient and continuing variational methods in inclusion processing. At the same time, the inclusion compound was identified by X-ray diffraction (XRD) and differential scanning calorimetry (DSC) methods, respectively. Results The above-mentioned systems showed the mol ratio of HP-?-CD-irisquinone (2 : 1) and the inclusion compound enhanced remarkably the most solubilization and more combined constant of irisquinone in 25, 35, and 45℃. The lyophilized powder had been formed inclusion compound by identifying. Conclusion It is advantageous to increase the solubilization and to strengthen the stability of irisquinone by preparing inclusion compound.

Objective To investigate the solubilitization effect of macromolecular paclitaxel with cyclodextrin and mechanism between inclusion complex and drugs. Methods The influence effects on paclitaxel solubility were studied with ?-cyclodextrin (?-CD) and hydroxypropyl-?-cyclodextrin (HP-?-CD) as inclusion carriers. The chemical shifts of hydrogen atom in host and guest molecules were also investigated with 1H-NMR. Results The form of inclusion complex was responsible by host molecules and the enhancement solubility of paclitaxel in HP-?-CD was larger than that in ?-CD and increased with the ratio increasing. The benzene ring in the molecular of HP-?-CD and paclitaxel showed the most significant effect. Conclusion The solubility of diossolved paclitaxel is improved by hydroxypropyl-?-cyclodextrin.

AIM: To investigate the intestinal uptake of risquinone in two dosage forms-capsule and irisquinone-?-hydroxyprol-?-cyclodextrin(HP-?-CD) in rats and its pharmacokinetics. METHODS: Comparing with capsule,the accumulation uptake of irisquinone from HP-?-CD inclusion complex were tested in suit in vivo and the correspondence between pharmacokinetics behavior and uptake of irisquinone in rats were simultaneously analysised. RESULTS: The intestinal absorption rate of irisquinone were 0.047 h~(-1) to capsule and 0.180 h~(-1) to irisquinone-HP-?-CD,respectively.The intestinal uptake of irisquinone in rats was positive correlation with its release from capsule in vitro.The accumulated uptake of irisquinone were 29.58% from capsule and 69.63 % from irisquinone-HP-?-CD.The pharmacokinetics of irisquinone in two formulas were coincidence with one-compartment model in rats.The absorption half life(T_(1/2(ka))) was 0.23 h to irisquinone-HP-?-CD and 0.49 h to capsule.The relative bioavailability of irisquinone-HP-?-CD was 133.9%. CONCLUSION: Inclusion complex may enhance intestinal uptake of drug and improve its bioavailability.

Objective To prepare the chitosan nanoparticles(particle-diameter

Objective To synthesize N-galactosylated chitosan as hepatocyte-targeting carrier and prepare loading norcantharidin nanoparticles.Methods N-Galactosylated chitosan was prepared by carbodiimide condensation reaction;loading norcantharidin nanoparticles were achieved by ionic cross-linkage process with N-galactosylated chitosan as carrier.Taking distribution of particle size,entrapment efficiency,and drug-loading capacity as comprehensive indexes,the orthogonal test design was used to optimize the preparation process and the in vitro release was investigated.Results Substitution degree of N-galactosylated chitosan reached to 8.92%.Novel nanoparticles were spherical,average in particle size(118.7?8.84)nm,entrament efficiency(57.92?0.40)%,drug-loading capacity(10.38?0.06)%,and the in vitro release followed Higuchi equation.Conclusion Effect of drug sustained release of galactosylated chitosan nanoparticles is significant.