Optimization of formulation and preparation technology of Neuritic acid oral emulsion / 中国药房

OBJECTIVE To prepare Neuritic acid oral emulsion ，to optimize its formulation and preparation technology ，and to investigate its stability. METHODS Neuritic acid oral emulsion was prepared by mechanical method. On the basis of single factor experiment ，the appearance ，centrifugal stability ，centrifugal stability constant （Ke）and particle size of the emulsion as indexes，the formulation was optimized by orthogonal design ，taking the dosage of oleic acid ，octylphenol polyoxyethylene ether-10 and propylene glycol as factors ，the preparation technology was optimized by taking emulsification temperature ，shear time，pressure of high-pressure homogenization and cycle times of high-pressure homogenization as factors. The content of neuritic acid was determined by high performance liquid chromatography. The stability of Neuritic acid oral emulsion was investigated by high temperature test ，accelerated test and long-term test. RESULTS The optimal formulation and preparation technology were as follows：neuritic acid of 1 g，oleic acid of 5％ ，octylphenol polyoxyethylene ether- 10 of 4％ ，propylene glycol of 2％ ， emulsification temperature of 60 ℃ ，shear time of 2 min，homogenization pressure of 40 MPa and cycle times of twice. After three experiments ，the average particle size of Neuritic acid oral emulsion was 158.05 nm（RSD＝1.58％，n＝3），the average Ke was 0.39（RSD＝1.49％，n＝3），and the appearance was uniform milky white ，there was no stratification. The results of high temperature test showed that Neuritic acid oral emulsion was prone to stratification in high temperature environment ，and the content of neuritic acid increased. The results of accelerated test and long-term test showed that there was no significant change in the appearance or the content of neuritic acid when Neuritic acid oral emulsion was placed at room temperature for 6 months. CONCLUSIONS The formulation and preparation technology are stable and feasible ，and can be used for the preparation of Neuritic acid oral emulsion. Neuritic acid oral emulsion should not be placed in high temperature environment. It has good stability at room temperature for 6 months.

Inhibition of ursolic acid on angiogenesis and xenografts in zebrsfish (danio rerio) / 中国药理学通报

Aim To investigate the anti-angiogenesis and anti-xenograftes of UA in zebrafish larvaes. Meth-ods 24 hour post-fertilization ( hpf ) TG zebrafish was treated with different concentration of UA for 24h, and the number of intersegmental vessels( IVS) were detec-ted under fluorescent microscope respectively;then the models of AB/TG zebrafish xenografts were established by be micro-injected with SMMC-7721 or HT-29 cell at 48hpf respectively, and after cocultured with UA for 48h, optical density (OD) of the SMMC-7721 cell and subintestinal veins ( SIVs) induced by HT-29 were e-valuated under confocal microscope. Results ISV as-say showed that UA could cause IVS missing or disap-perance, inhibition ratio reaching 20. 25% and 26. 65%. UA blocked the spread of SMMC-7721 cells in zebrafish and OD value,and inhibition ratios at three concentrations were 38. 01%, 54. 69%, 61. 88%, re-spectively; in another SIVs assay induced by xeno-grafts, UA at concentration 10 and 15mg·L-1 showed that SIVs were inhibited (P<0. 01) obviously. Con-clusion UA could inhibit the angiogenesis and the growth of SMMC-7721/HT-29 xenografts,and the anti-tumor mechanism may be related with VEGFR2 expres-sion.

Plasma concentration and pharmacokinetics of ursolic acid carried in self-microemulsifying drug delivery system in rats studied by UPLC-MS/MS / 药学学报

This study is to report the establishment of an UPLC-MS/MS method for the determination of plasma concentration of UA carried in self-microemulsifying drug delivery system (SMEDDS) and its pharmacokinetics in rats. It was used for determination and analysis when serum with internal standard was extracted from C18 solid-phase column. Acquity UPLC BEH C18 column (100 mm x 2.1 mm, 1.7 microm) was used for separation. The mobile phase was acetonitrile -0.1% ammonia with gradient elution at the flow rate of 0.2 mL x min(-1). The column temperature was 40 degrees C and the detection wave length was 210 nm. It was detected by negative ion using electrospray ionization source (ESI) and scanned by multiple reaction ion monitoring (MRM) mode. The liner relationship of UA was very good in the range of 1.19-3 815.00 ng x mL(-1) (r = 0.999 0). Recovery rate of different concentrations were 87.42%-89.95%. The precision of inter-day and intra-day were less than 11%. The method developed in our study was proved to be sensitive, rapid and simple. It is suitable for the pharmacokinetic study of UA-SMEDDS in rats.

Determination of total saponin in Semen Platycladi and defatted powder of Semen Platycladi / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the contents of total saponin in the unprocessed Semen Platycladi and defatted powder of Semen Platycladi.</p><p><b>METHOD</b>Through contrasting different coloration, proper condition was selected by using orthogonal test design. Spectrophotometry was established to determine the contents of total saponin in the unprocessed Semen Platycladi and defatted powder of Semen Platycladi.</p><p><b>RESULT</b>Coloration system of vanillin-acetic acid-sulfuric acid was determined. The proper condition of coloration was that sulfuric acid was 80%, water bathed 85 and heated for 10 minutes. The contents of total saponin in unprocessed Semen Platycladi was 0.142% the content of total saponin in the defatted powder of Semen Platycladi was 0. 319%.</p><p><b>CONCLUSION</b>This method, stable, simple and quick, is applicable to the determination of total saponin in Semen Platycladi. A Little of total saponin is lost in the processing course of Semen Platycladi.</p>

Effect of Ruhuang preparation on endotoxin and intestinal defence function of cirrhotic rats / 中华中医药杂志

Objective: To study the influence of Ruhuang(Rhubarb and Lactohacillin) preparation to endotoxin and intestinal defence function of cirrhotic rats.Methods:88 male Wister rats were randomly divided into normal group,model group,prevention group,prevention of control group,model treatment group and model treatment of control group.Liver cirrhosis model was induced by CCl4 combined with other factors,Ruhuang preparation was used for the prevention and treatment,lactulose was used as positive control drug.The level of plasma endotoxin,intestinal mucosal S-IgA and serum D-lactic acid were detected.Results : The blood plasma endotoxin level of Ruhuang prevention group and model treatment group is lower than that of model group obviously(P

Determination of ?-eudesmol in atractylis oil from Rhizomes of Atractylodes Lancea (THUNB.)DC.by gas chromatography / 中成药

AIM: To establish the determination of ? eudesmol in atractylis oil from Rhizomes of Atractylodes Lancea (THUNB.) DC. by gas chromatography. METHODS: Pentadecanol had been used as the internal standard substance in internal standard method. The GC system consisted of capillary column, 10%SF 30 as the stationary phase, nitrogen as the carrier gas, and FID as the detector. RESULTS: Both ? eudesmol in essential oil and pentadecanol had got satisfactory separation under the chromatographic condition. The mean recovery of ? eudesmol was 99.60%, and RSD was 1.30%. CONCLUSIONS: The method is sensitive, accurate and reproducible, and it can be used to control the quality of the essential oil from Rhizomes of Atractylodes Lancea (THUNB.) DC.