OBJECTIVE：To study the effcet of Nitric oxide (No) on transcriptional expression of c-fos and c-jun oncogene of cultured rabbit arterial smooth muscle cells (ASMC),and its mechanism.METHODS:(1)To culture rabbit ASMC from explants;(2) To determine if NO,FeSO4,and methylene blue have toxic effect on ASMC by cell counting;(3)RNA isolation from ASMC by Guanidinium Thiocyanate-phenol-chloroform method;(4)RNA-DNA blot hybridization.RESULTS:Under the condition of no toxic effects,NO inhibited the expression of c-fos and c-jun oncogene of ASMC apparently,FeSO4 and methylene blue antagonized the inhibition effcet.CONCLUSION:NO inhibited the expression of c-fos and c-jun oncogene of ASMC through cGMP.This may be related to the important mechanism that NO inhibits the proliferation of ASMC.

OBJECTIVE:To prepare diclofenac sodium controlled release tablet,and to evaluate the mechanism of drug release.METHODS:Stearic acid and ethyl cellulose were used as blocking agents and sodium carboxylmethyl starch was used as disintegrating agent.Tablets were made after drying the granules prepared.The dissolution rates were acquired according to Chinese Pharmacopoeia(1995).RESULTS:Drug release from the tablets prepared was of zero-order release before 90% of drug released.No significant influences were observed from the dissolution rates of the different pressure of tablet(5～10kg),amount of drugs contained in the tablet(35%～60%)and different geometry of the tablets,respectively.The remarkable difference waw observed between the disintegrating and blocking agents contained in the tablets.CONCLUSION:The time of 50% of durg released could be changed as the amount of disintegrating or blocking agents were changed.

OBJECTIVE:To study the chemical constituents of Glycyrrhiza pallidiflora.METHOD:IR, 1 H-NMR,13C-NMR,MS and TLC were used to identify conpounds .RESULTS:Five compounds were elucidated as homopterocarpin,β-sitosterol,4＇,7-dimethoxyisoflavone,medicarpin and isoglabrol. CONCLUSION:The 4＇,7-dimethoxyisoflavone was first separated from this plant .

OBJECTIVE:To study the change regular of esterase isozyme and peroxidase isozyme of Polyporus umbellatus. METHOD:Using polypropylene amide circle electrophoresis.RESULTS：The pattern and activity of isozyme in same strain had some difference at different culture days,but some of isozyme pattern bands of the Rf value were visible in whole culture stage.Every strain had its peculiar pattern bands.CONCLUSION:The number of isozyme pattern bands and enzyme activity were proportional to the growing rate of myceliun,as well as its metabolic activity.

OBJECTIVE: To enhance the dissolution rate and efficacy of nimodipine (NMDP) which is a poorly water-soluble substance, and to design the formulations with fast-release properties. METHOD: NMDP-PVP-k30 coprecipitate and physical mixture were prepared. The physical states of NMDP in both newly-made and one-year-old samples were investigated by X-ray diffraction analysis. The dissolution rates of NMDP from coprecipitate and from physical mixture were also compared. Five formulations were prepared on the basis of NMDP-PVP-k30 coprecipitate and their in vitro drug dissolution behaviors were examined. Also, the dissolution property of the capsules with one selected composition was examined. The selected capsules were compared with two commercial tablets on their drug release processes. RESULTS: NMDP-PVP-k30 coprecipitate gave much higher improvement in the dissolution rate than the physical mixture, and NMDP was released 89% from the coprecipitate and 45% from the physical mixture in five minutes respectively. There was no appearance of crystallization in the coprecipitate after one year storage under experimental conditions. The tablet formulation with the highest drug dissolution rate was selected. The capsules with the same composition as the selected tablet showed a higher drug dissolution rate, which indicated that drug release property was influenced by the compressing pressure. The results showed that the dissolution rate of NMDP from the selected capsules was about three to four times of that from the two commercial tablets.CONCLUSION: The dissolution rate of NMDP can be improved greatly by coprecipitation using PVP-k30 as a carrier.

To investigate the protective effects of OLA-PENa on experimental hepatic injury in rats and compare it with OLA in the dose-response relationships. METHODS: Biochemical indexes and histopathological examination of hepatic injury in rats caused by toxicant chemicals ［D-galactosamine (D-Galn) and CCl4］ were determined. RESULTS: OLA-PENa obviously inhibited the rising of serum alanine transaminase (ALT) caused by D-Galn and CCl4 and dramatically decreased liver fat storage as well in a dose-dependent manner. Histopathological examination showed that OLA-PENa can evidently alleviate the condition of the degeneration of hepatic cells and that of necrosis. CONCLUSION: The protective effects of OLA-PENa on experimental liver injury in rats, all the mentioned effects, are more powerful than those of OLA with the same dosage.

OBJECTIVE: To study the effect of samples having different pH values in the bacterial endotoxins test (BET). METHODS: The BET was conducted as an assay of the concentration of endotoxins by using kinetic-turbidimetric technique. Samples having different pH values but containing same concentration reference standard endotoxin (RSE) were tested by TAL/LAL reagents. The average result on the standard curve was calculated and the mean recovery observed. RESULTS: The reagents had three highly sensitivities in pH 5.20, pH 7.83/pH 6.23 and pH 10.55. After adjustment to pH 6 to 8, the mean recovery was 76.5%～115.9% or 85.8%～99.8%. When the sample pH value was less than 3 or more than 12, the test was unsuitable for the inhibition test, and the mean recovery was less than 56.8%. CONCLUSION: It is necessary to adjust the pH of the solution to be tested in the BET, adjust the sample to pH (6.5～7.5) when using TAL reagents, and adjust to pH (6.2±0.1) or pH(6.7～7.8) when using LAL reagents.

To study a method for determination of sulfamethoxazole, sulfadiazine and trimethoprim tablets, a compound tablet of sulfamethoxazole, sulfadiazine and trimethoprim. METHOD: A capillary zone electrophoresis (CZE) method was used to assay three components of this compound preparation. RESULTS: The complete separation of components was achieved with 0.05 molL-1 pH 6.0 running phosphate buffer and a constant voltage of 20 kV (current of 95 μA～105 μA). The retention times of individual components were between three and eight minutes and a good linearity was shown between concentration and peak area in the concentration range over 70 μgml-1～750 μgml-1. When acetanilide was used as internal standard, the relative standard deviation (RSD) of each component determined in a batch was less than 1% (n=9). The recovery of each component was not less than 96.45% with RSD less than 3%. The analytical results obtained from 6 samples of clinical use were inconsistent with those by standard method, however the quantity of each sulfa drug was obtained by CZE method. CONCLUSION: The results showed this method is accurate, simple, and rapid. When this method is used, the quantity of each three components is determined, but by the standard method, only the total quantity of the two sulfa drugs is obtained.

To prepare and study the pharmacokinetics and release bioavailability in olunteers and concentrations in plasma in patients. METHODS: Ethylcellulose was used matrix in phase separation-coacervation for preparation of microencapsulation. The release experiments were performed in a rotating shaker. The isoniazid concentration in plasma was determined by spectrophotometrical method following a single oral dose of sustained-release cupsule and ordinary tablet respectively given to 10 volunteers in a open randomized cross-over test. MCP86 was used to process main pharmacokinetic parameters. RESULTS: The sustained-release of capsule and ordinary teblet in vitro, T50 was 1 h and 0.032 h respectively. The drug in sustained-release capsule was sustained release over 10 h. The main parameters in body: ordinary tablets: cmax=11.12 μgml-1, tmax=1.41 h, K=0.201 h-1; sustained release capsule: cmax=4.99 μgml-1, tmax=1.80 h, K=0.03 h-1. The concentration of blood at 36 h was (0±0)μgml-1 and 1.63 μgml-1 respectively. Except tmax, there was significant difference between the two fomulations (P＜0.01). The concentration of blood in patient at 1.5 h and 36 h. ordinary tablet and sustained-release capsule respectively were (8.24±2.60)μgml-1, (0±0)μgml-1and (3.69±0.86)μgml-1, (2.09±0.56)μgml-1. CONCLUSION: The sustained-release capsule will play an important part in prevention and treatment of tuberculosis as the result of its reasonable formulation and simple technology.

OBJECTIVE: To develop a HPLC method for assaying strychnine and brucine in traditional Chinese drug Maqianzi San. METHODS: With μBondapak C18 (10 μm) column (4 mm×300 mm), MeOH-H2O-HAc-(C2H5)3N(70∶230∶2.4∶0.3) as mobile phase, we set a detector at 254 nm. RESULTS: Linear range of strychnine and brucine was 0.367 2 μg～0.061 2 μg and 0.945 0 μg～0.157 5 μg respectively. The recovery rate of strychnine and brucine was 100.36% (RSD=1.09%) and 100.01% (RSD=1.46%) respectively. CONCLUSION: This method provides a simple and feasible way to control the quality of Maqianzi San.