OBJECTIVE:To optimize the formula and preparation technique of oleanolic acid loaded polybutylcyanoacrylate nanocapsules(OA-PBCA-NC)by interfacial polymerization and to study its quality.METHODS:The preparation technique of OA-PBCA-NC prepared by interfacial polymerization were optimized by single factor design,and the formula was optimized by orthogonal design with entrapment ratio as index.Its shape,particle size and the entrapment ratio were investigated as well.RESULTS:The optimized dosage ratios were as follows∶ OA vs.BCA∶60mg∶0.1ml;acetic ether vs.BCA∶2.0ml∶0.1ml;and oil vs.water:1∶1.The prepared nanocapsules were round and regular in shape without adherence.The particle size was well-distributed with mean diameter at(214?8)nm and mean entrapment ratio at(76.8?0.4)%.CONCLUSION:The preparation technique of OA-PBCA-NC established in this study is stable and feasible.

Objective To improve the method for determination of geniposide in Fructus Gardeniae.Methods The improved method was compared with the pharmacopoeia method.The content of geniposide was determined by HPLC at 238nm detection wavelength with acetonitrile-water(15:85)as mobile phase .Results The improved method in which 50 % methanol was used as solvent was superior to the pharmacopoeia method in which methanol was adopted as solvent.A higher geniposide content was abtained from the former.Conclusion The improved method is convenient and accurate,and can be used to supply reference evidence for the assay of Fructus Gardeniae in the new edition of pharmacopoeia.

Objective To establish a HPLC method for the determination of gallic acid in Radix et Rhizoma Rhei and to study the changes of gallic acid content in Radix et Rhizoma Rhei during processing. Methods HPLC method was used to detect gallic acid content. Diamonsil C18(250 mm?4.6 mm,5?m) column was used,and the mobile phase was a mixed liquid of MeOH -0.01 %H3PO4(10∶90). The column temperature was set up at 30℃,the flow rate was 1 mL?min-1,and the detecting wave-length was 273 nm. Results There were obvious differences of gallic acid content between the crude herbal material and different kinds of processed products of Radix et Rhizoma Rhei. The content of gallic acid was decreased in Radix et Rhizoma Rhei prepared by wine,but was increased in Radix et Rhizoma Rhei prepared by steaming with wine and by stewing with wine,and in charred Radix et Rhizoma Rhei. Conclusion The different processing methods have certain effect on the content of gallic acid in Radix et Rhizoma Rhei.

OBEJETIVE:To determinate simultaneously the contents of berberine hydrochloride,palmatine hydrochloride,jatrorrhizine hydrochloride,baicalin and jasminoidin in coptis chinensis detoxication capsule by HPLC.METHODS:3different UV wavelengths were adopted simultaneous in the determination in which Diamonsil C 18 was taken as the chromatographic column and water-methanol-0.05%H 3 PO 4 (gradient elution)was taken as mobile phase,the column temperature was set at35℃and the flow rate was1.0ml/min,the detection wavelength were345nm,280nm and238nm respectively and the sample size was10?l.RESULTS:They took good linear relationships when the respective sample size of berberine hydrochloride,pal-matine hydrochloride,jatrorrhizine hydrochloride,baicalin and jasminoidin were at0.105?g～1.680?g(r=0.9999),0.045?g～ 0.720?g(r=0.9998),0.065?g～1.040?g(r=0.9997),0.190?g～3.040?g(r=0.9999)and0.145?g～2.320?g(r=0.9999);Their respective average recovery rates were99.11%,98.19%,97.21%,98.52%and99.22%.CONCLUSION:This method is fast,reproducible,sensitive,and which can provide a more reasonable and reliable quality control for coptis chinensis detoxi-cation capsule.

Objective:To compare the pharmacokinetics consistence of baicalin between traditional slice decoction and dispensing granule decoction of Huanglianjiedu decoction. Methods:After the gastric administration of the two decoctions at low, middle and high dose in rats, an HPLC method was used to detect the content of baicalin in the plasma, and then DASS 2. 1. 1 software was used to cal-culate the pharmacokinetic parameters. Results:After the administration of the two decoctions at low, middle and high dose, the phar-macokinetic parameters were as follows:Cmax of 0. 25 and 0. 27μg·ml-1 ,0. 30 and 0. 31 μg·ml-1 ,0. 40 and 0. 45 μg·ml-1;AUC of 2. 48 and 2. 59μg·ml-1 ·h,3. 59 and 3. 71μg·ml-1 ·h,5. 71 and 6. 16μg·ml-1 ·h;Tmax of 3. 0 and 3. 0 h,3. 0 and 3. 0 h, 4.0 and 4.0 h;Vd of (2 822.4 ±118.2) and (2 998.9 ±255.6) L·kg-1,(3 102.6 ±176.3) and (3 405.3 ±213.8) L·kg-1, (4 231.2 ±155.4) and (4 486.0 ±187.0) L·kg-1;CL of (2 923.3 ±215.6) and (2 767.5 ±184.6)L·h-1·kg-1,(4 921.7 ± 225.4) and (4 040.8 ±246.7)L·h-1·kg-1,(5 255.9 ±189.7) and (4 868.7 ±260.4)L·h-1·kg-1;and t1/2 of (3.88 ± 0.41) and (3.71 ±0.37)h,(4.19 ±0.36) and (3.73 ±0.51)h, (5.54 ±0.38) and (5.80 ±0.54)h. Conclusion: The pharma-cokinetic parameters of baicalin have no significant difference between traditional slice decoction and dispensing granule decoction of Huanglianjiedu decoction.

0.05). In the fever experiment,the two kinds of HJD in different doses showed antipyretic effect to various degrees,but the dispensing granule decoction of HJD had the better effect,and the effect in the middle-and high-dose groups was superior to that of the low-dose groups (P

Objective To compare the contents of berberine,palmatine,jatrorrhizine,baicalin and geniposide between traditional decoction and dispensing granule decoction of Huanglian Jiedu Decoction.Methods A HPLC method was carried out on Diamonsil C18 column(250 ? 4.6 mm,5 ?m).The mixture of H2O(A),CH3OH(B)and 0.05 % H3PO4 solution(C)was used as the mobile phase for gradient elution.The column temperature was set up at 35 ℃ and the flow rate was l mL/min.The detection wavelength was 345nm for berberine,palmtine and jatrorrhizine,280 nm for baicalin,and 238 nm for geniposide.Results This method can be used to determine 5 components in Huanglian Jiedu Decoction at the same time and the method was rapid,sensitive and accurate.Conclusion The HPLC chromatograms of traditional sliced decoction of Huanglian Jiedu Decoction are similar to the dispensing granule decoction.The contents of 5 main components in dispensing granule decoction are higher than those in traditional sliced decoction.

Experimental course for integrative life science curriculum is designed for medical students ,which integrates basic knowledge and skills of cellular biology,biochemistry,genetics,molec-ular biology,molecular genetics,and immunology disciplines. Tongji University School of Medicine start-ed to implement integration-based new curriculum system since 2010. This article discussed on teaching philosophy,teaching content,teaching methods,teaching team construction and explored the effect and significance of experimental course for integrative life science curriculum.

A series of nitrogen-containing benzoheterocyclic derivatives were synthesized and tested for their antipsychotic activities. Their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological trials showed that most of the target compounds have high affinity with D2 and 5-HT(2A) receptors. Among the tested compounds, 20 exhibited the highest affinity and D2 partial agonist activity. In vivo studies showed 20 has potent antipsychotic activities on apomorphine mice model, which is a chance to find a better precursor of D2 partial agonist for further optimization.
Animals ; Antipsychotic Agents ; chemical synthesis ; pharmacology ; Dopamine Agonists ; chemical synthesis ; pharmacology ; Drug Design ; Isoquinolines ; chemical synthesis ; pharmacology ; Mice ; Receptors, Dopamine D2 ; Structure-Activity Relationship

Objective To investigate the effects of antihypertension and reversing left ventricular hypertro- phy by carvedilol or bisoprolol in patients with mild to moderate essential hypertension.Methods 40 cases of mild to moderate essential hypertension patients were selected for this random single-blind,paralleling controlled clinical study.Results Patients were randomized to take 12.5～25mg carvedilol tablet orlce daily or bisoprolol 2.5～5mg once daily if DBP was still in the range of 12.0～14.6kPa(90～110mmHg)after 2 weeks' placebo baseline. Carvedilol group included 20 cases,bisoprolol group included 20 cases,and the course was 24 weeks.Blood pressure and heart rate were measured and symptoms and signs were recorded.At the end of placebo and in 24 weeks heart ultrasound,blood routine,serum glucose,blood lipid,hepatic function and renal function were examined.SBP,DBP and heart rate of patients in two groups decreased obviously.There were significant differences between the two groups.Ventricular hypertrophy of carvedilol group improved than that in pretherapy.There were significant differ- ences between the two groups.Conclusion Carvedilol was well-tolerated with less side effects such as mild headache,tiredness,dizziness,slightly elevating of serum glucose.Carvedilol could well treat the mild moderate essen- tial hypertension effectively and safely by 12.5～25mg once daily.