Research on analgesic effect and prospect of clinical application of rutin / 中国药理学通报

Rutin is extracted from Ruta graveolens L. with many pharmacological activities such as anti-inflammation, anti-oxidation , protecting cardiovascular system and analgesia. As a natural product, rutin has the advantages of low side effects and difficult tolerance, but its instability and low bioavailability still limit its clinical application. This paper summarizes the analgesic mechnism of rutin, and looks forward to the clinical applica¬tion of rutin based on its derivative and dosage forms. It is expected to provide ideas for further analgesic research and drug development and application of rutin in the future.

Percentile normal values of BMI for children and adolescents in Shanghai / 预防医学

Objective To fit children and adolescents' normal values and curves of BMI with coefficient of skewness-median-coefficient of variation (LMS) method, so as to provide a reference for the monitoring of obesity in children and adolescents. Methods 15259 children and adolescents aged 7 to 18 years old were selected in Shanghai, and the height and weight of the subjects were measured . The LMS Chartmaker software was used to fit the percentile curves of BMI of boys and girls with age. With P3, P5, P10, P15, P25, P50, P75, P85, P90, P95, P97 as the reference curve. Results The percentile of students showed an increasing trend with the age increases, and the boys are higher than girls. The P50 of all age groups of boys and girls in Shanghai was higher than that of the national level. The P85 and P95 of BMI were basically equal to the national level in the early stage, and was higher than the national level in the later period. The curve of boys has entered the peak of BMI growth since 9 years old, after 12 years old, the growth rate is slow, the curve is still rising at 18 years old. The curve of girls has entered the peak since 10 years old, after 14 years old, the growth rate is slow, after 16 years old, the curve tends to be stable. Conclusion The BMI percentile curve constructed by LMS method can correctly reflect the growing development of children and adolescents, and the BMI of children and adolescents in Shanghai is higher than the national level.

Expression of recombinant human acetylcholinesterase and its application in screening its inhibitors / 药学学报

This study is designed to obtain recombinant human acetylcholinesterase (rhAChE) and apply it in screening acetylcholinesterase inhibitors. The rhAChE was overexpressed in HEK293 cells transfected by plasmid of pCMV-AChE with the cationic liposome and rhAChE was found to be secreted into cell culture medium. AChE activity was assayed according to modified Ellman method to obtain kinetic parameters. IC so50 values for donepezil compounds of rhAChE were calculated to determine their activities of inhibition. The results showed that Km value was 151.9 micromol.L-1 donepezil inhibited rhAChE in a mixed competitive-noncompetitive way (Ki= 16.03 nmol.L-1, Ki = 18.36 nmol.L-1) and that most new compounds tested exhibited high activities of inhibition on rhAChE. The study suggests that rhAChE is available to be applied in screening AChE inhibitors in vitro.

Pharmacokinetics and plasma protein binding of rutin deca (H-) sulfate sodium / 药学学报

Rutin deca (H-) sulfate sodium (RDS) possesses very good activity as an inhibitor of the complement system of warm-blooded animals and HIV. An ion-pair coupled with solid-phase extraction technique (IP-SPE) was developed to extract RDS from rat plasma, urine, bile and protein solution samples. The assay was applied to pharmacokinetics of RDS, including plasma pharmacokinetics, excretion and protein binding studies. After i.v. 5, 20 and 100 mg x kg(-1) RDS via tail vein in rats, the plasma concentration-time profiles were fitted using 3P97 software. The average terminal half-life (t(1/2)) was 3.432 +/- 0.185 2 h. The relationship of dose and AUC of RDS was linear within the dosage range. This suggested that the disposition of RDS in rats belong to linear kinetics and the pharmacokinetic parameters of RDS were dose independent. After iv RDS 20 mg x kg(-1) in rats, the biliary excretion amount of parent drug amount was only 0.3181% +/- 0.2087% of given dosage, and the urinary excretion was 86.0% +/- 6.1% in 36 h. Ultrafiltration techniques were applied to determine the protein binding of RDS in plasma (from SD rat, Beagle dog and human), human serum albumin (HSA) and human alpha1-acid glycoprotein (AGP). The mean protein binding rate in plasma of SD rat, Beagle dog and human plasma of RDS were 80%-90%, in which the range of concentration of RDS was 5 to 100 microg x mL(-1). The protein binding to HSA was 85.7% +/- 1.3% and 14.0% +/- 3.2% to AGP.

HPLC determination of zolmitriptan and its related substances / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To develop an analytical method and quality control for determination of zolmitriptan and related substances.</p><p><b>METHODS</b>Zolmitriptan and related substances were separated and determined on a shimadzu CLC-C(8) column (150 mm x 6 mm, 10 microm) with a mobile phase of acetonitrile-10 mmol/L phosphate buffer (25:75 pH 7.5) and a flow-rate of 1 ml/min; the UV-VIS detector was operated at 229 nm.</p><p><b>RESULT</b>The limit of detection for the related substances was 0.5 ng on the zolmitriptan basis (S/N >3). Linear calibration curve was gene rated from 4 - 40 microg/ml with a correlation coefficient of 0.9999. The recovery rate of zolmitriptan was 99.1% with a standard deviation of 0.2%. The results of HPLC method were consistent with those of nonaqueous titration method.</p><p><b>CONCLUSION</b>HPLC method is a rapid sensitive and accurate method for the determination of zolmitriptan and its related substances.</p>

Determination of three formulations of pilocarpine in rabbit ocular aqueous by RP-HPLC / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To develop an RP-HPLC method for assay of pilocarpine in rabbit ocular aqueous humor.</p><p><b>METHODS</b>The RP-HPLC method was performed on a column of ODS-C(18) with the mobile phase consisting of 0.5% of triethylamine (TEA) of phosphate solutions (10 mmol/L, pH 2.5) and acetonitrile (98/2,v/v). The detection wavelength was 215 nm and flow rate was 1.0 ml/min. Ninety albino rabbits were divided into 3 groups (30 in each):group 1 received 50 microl of eye drops containing 1% generic pilocarpine, group 21% mixture pilocarpine solution consisting of aqueous sample and liposome and group 31% liposome pilocarpine, respectively. The aqueous humor was withdrawn at 5, 10, 30, 40, 60, 90, 120, 180, 240 and 360 min. Pilocarpine was extracted from aqueous humor with dichloromethane.</p><p><b>RESULT</b>The linear calibration curve was obtained in the concentration range of 0.1 - 20 microg/ml. The average recovery was (68.1+/-2.7)% (n=9). Inter-day and intra-day RSD were 4.33% and 2.87%, respectively. In three formations 1% liposome pilocarpine was the best for the areas under curve and measurable amounts.</p><p><b>CONCLUSION</b>The RP-HPLC method is simple and reliable for pilocarpine measurement in ocular aqueous. Liposome formulation can significantly increase the bioavailability of pilocarpine in ocular aqueous.</p>

Enatiomeric separation of beta-blocking agents and analogs / 浙江大学学报·医学版

OBJECTIVE: To evaluate enantiomeric separation methods for beta-blocking agents and analogs. METHODS: Enantiomeric separation of racemates of 11 beta-blocking agents and their analogs was performed using chiral stationary phases and 2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl isothiocyanate (GITC). RESULTS: These beta -blocker racemates were separated into enantiomers in one or several chormatographic states such as propranolol, bisoprolol, metoprolol, celiprolol, carvedilol, sotalol, propafenone, ephedrine, and zomitriptan. Temperature had a significant effect on the resolution of the drugs when using chiralcel OD. Lower temperatures were associated with higher resolutions. CONCLUSION: When separating beta-blocking agents and their analogs, Chiralcel OD, Chiralpak AD, Chiral stationary phases and GITC chiral derivative reagents have complementary functions.