Preparation and quality evaluation of gardenoside emulsion / 中草药

Objective To prepare water-in-oil gardenoside emulsion, optimize its formulation process, and evaluate the quality. Methods The formulation was optimized based on emulsification time, oil floating time and phase separation time, and investigated the optimal gardenoside emulsion by the single factor investigation and mixture design. The properties, stability, content, and in vitro release of the emulsion were also studied. Results The mean particle size of gardenoside emulsion was (5.48 ± 0.02) μm and the value of PDI was 0.125 ± 0.096; Centrifugation accelerated test was performed at 4 000 r/min for 15 min without delamination; The average mass fraction of gardenoside emulsion was 92.14% and RSD was 1.86% (n = 3); The in vitro release of gardenoside emulsions at pH 4.5, 6.8, and 7.4 was up to 105.32%, 98.41%, and 98.70%, respectively, while the in vitro release at pH 1.2 was up to 63.45%; Finally, the law of drug release was explained by fitting equation. Conclusion The high speed shear mechanical method can be used to prepare gardenoside emulsion, and the quality evaluation of the optimized prescription meets the requirements.

Effects of baicalin-gardenoside pairing on 5-lox/CysLTs/CysLT pathway of cerebral ischemic injury rats / 中成药

AIM To study the effects of baicalin and gardenoside pairing on 5-lox/CysLTs/CysLT pathway of rats with cerebral ischemia injury.METHODS SD rats randomly assigned into control group,model group,baicalin and gardenoside pairing groups (7 ∶ 3,dosed at 30,45,60 mg/kg,respectively) in their cerebral ischemia recovery period were simulated with permanent middle cerebral artery occlusion (pMCAO) if necessary.After a week of natural recovery,the drugs' pharmacodynamic effects were evaluated by the neurofunctional scoring and HE staining,their impact on the content of CysLTs was determined by ELISA,and the influence on the expression of 5-lox,CysLT1 and CysLT2 was detected by western blot.RESULTS One-week consecutive administration of baicalin and gardenoside pairing contributed to a reduction in infiltration and tissue edema of ischemic cells.If compared with pMCAO group,the baicalin and gardenoside pairing groups were observed with significantly lowered scores of neurologic functioning,inhibited microglia activation,decreased content of CysLTs and down-regulated expression of 5-LOX,CysLT1 and CysLT2 (P ＜ 0.01).CONCLUSION Baicalin and gardenia pairing's alleviating effect to the damage of cerebral ischemia may be associated with its inhibition on microglia activation and 5-lox/CysLTs/CysLT signaling pathway,and thus an inflammatory impairment reduction.

Determination of six constituents in Qingkailing Freeze-Dried Powder for Injection by HPLC / 中成药

AIM To establish an HPLC method for the content determination of six constituents in Qingkailing Freeze-Dried Powder for Injection (cholic acid,hyodeoxycholic acid,Bubali Cornu,etc.).METHODS The content determination of adenosine,chlorogenic acid and gardenoside was performed on a 30 ℃ thermostatic XBridge C1s column (4.6 mm ×250 mm,5 μm),with the mobile phase comprising of acetonitrile-water (containing 0.1％ formic acid) flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 254 nm.The content determination of baicalin,hyodeoxycholic acid and cholic acid was performed on a 35 ℃ thermostatic XBridge C1s column (4.6 mm ×250 mm,5 μm),with the mobile phase comprising of methanol-water (containing 0.1％ formic acid) flowing at 1.0 mL/min in a gradient elution manner.RESULTS Six constituents showed good linear relationships within the ranges of 2.244-56.108,2.658-66.445,4.347-108.682,122.01-1 016.75,131.94-1 099.50,152.22-1 268.50 μg/mL (r ＞ 0.999 0),whose average recoveries (RSDs) were 101.1％ (0.46％),98.0％ (1.74％),99.7％ (0.15％),100.9％ (1.31％),98.1％(0.18％),98.2％ (1.61％),respectively.CONCLUSION This stable and reproducible method can be used for the quality control of Qingkailing Freeze-Dried Powder for Injection.

Simultaneous determination of 9 components in Xiao'er Chiqiao Qingre granules by UPLC / 中国中药杂志

To establish a method for the simultaneous determination of 9 components, namely gardenoside, paeoniflorin, forsythoside A, baicalin, forsythin, glycyrrhizic acid, rhein, honokiol, and magnolol in Xiao'er Chiqiao Qingre granules（XECQ Gra）. Ultra performance liquid chromatography (UPLC) was used on an Acquity UPLC HSS T3 C₁₈ column (2.1 mm×100 mm, 1.8 μm) with 0.1% phosphoric acid acetonitrile (A)-0.1% phosphoric acid solution (B) as mobile phase for gradient elution. The flow rate was 0.3 mL·min⁻¹ ; the column temperature was set at 30 °C, and the determination wavelength was set at 220 nm. All the 9 compounds were well separated, and showed good linear relationship within their concentrations (r>=0.999). The average recoveries were between 95.84%-101.4% and the RSD values were all less than 3.0%. The method is simple, reliable, and accurate, and could be used for the quality control of XECQ Gra.

Effects of Gardenia jasminoides extracts on cognition and innate immune response in an adult Drosophila model of Alzheimer's disease / 中国天然药物

Herbal extracts have been extensively used worldwide for their application on memory improvement, especially among aged and memory-deficit populations. In the present study, the memory loss induced by human Abeta protein over-expression in fruitfly Alzheimer's disease (AD) model was rescued by multiple extracts from Gardenia jasminoides. Three extracts that rich with gardenia yellow, geniposide, and gardenoside components showed distinct rescue effect on memory loss. Further investigation on adding gardenoside into a formula of Ganoderma lucidum, Panax notoginseng and Panax ginseng (GPP) also support its therapeutic effects on memory improvement. Interestingly, the application of GPP and gardenoside did not alter the accumulation of Abeta proteins but suppressed the expression of immune-related genes in the brain. These results revealed the importance and relevancy of anti-inflammation process and the underlying mechanisms on rescuing memory deficits, suggesting the potential therapeutic use of the improved GPP formulation in improving cognition in defined population in the future.

Simultaneous determination of eight ingredients in Bushen Qingli Granules by HPLC-QAMS / 中草药

Objective: To establish a novel method for QAMS to realize simultaneous determination of eight ingredients in Bushen Qingli Granules (BQG), including geniposidic acid (GA), chlorogenic acid, geniposide, scoparone, salvianolic acid B (SAB), baicalin, quercetin-7-O-α-L-rhamnoside (QR), and baicalein, and to verify the feasibility and technical adaptability of this method for application in BQG. Methods: Taking BQG as research objects and the above eight components as indexes, three correction methods of QAMS were used to calculate the relative correction factor (fk/s) of each tested component and 6,7-dimethoxycoumarin regarded as reference, in order to estimate the content of each component; The error and correlation evaluation was carried out by comparing the calculated values of the regression equation and three correction methods with the real data of the external reference. Results: Within certain linear ranges, eight kinds of target components showed good linear relationships (r > 0.999 9). The values of relative correction factors (RCF) of scoparone to GA, chlorogenic acid, geniposide, SAB, baicalin, QR, and baicalein respectively were 0.562, 0.818, 0.627, 0.877, 0.935, 1.113, and 2.339, and the RCF had a good reproducibility. The contents of eight components of six batches of samples were GA 1.633—1.736 mg/g, chlorogenic acid 1.777—1.950 mg/g, geniposide 6.017—6.422 mg/g, scoparone 1.765—1.851 mg/g, SAB 2.326—2.522 mg/g, baicalin 19.476—21.329 mg/g, QR 3.077—3.265 mg/g, and baicalein 0.161—0.186 mg/g. No significant difference was found in these tested results by comparing the measured values and the real values. Conclusion: The QAMS method can provide a quick and feasible method with simultaneous determination to establish multitude index quality evaluation model for BQG.

Study on Distribution and Targeting of Gardenia jasminoides Extract Niosomes in Rats / 中国药房

OBJECTIVE:To study distribution and targeting of Gardenia jasminoides extract niosomes in rats. METHODS:G. jasminoides extract niosomes were prepared by modified thin film dispersion method. 30 rats were randomly divided into G. jasmin-oides extract group(57 mg/kg)and G. jasminoides extract liposome group(131 mg/kg)according to their weight. They were given relevant medicine intragastrically,once a day,for consecutive 7 days. 1 h after last administration,heart,liver,spleen,lung and kidney tissue were isolated,and HPLC method was adopted to the contents of active ingredients gardenoside in them. The targeting of G. jasminoides extract niosomes was evaluated by DTI quantitatively. RESULTS:Compared with G. jasminoides extract group, the contents of gardenoside in heart,spleen and brain tissue of rats increased significantly in G. jasminoides extract niosomes group (P<0.01),and DTI were 1.718,1.972 and 13.071;the contents of gardenoside in liver and kidney decreased significantly (P<0.01),and DTI were 0.431 and 0.467,respectively. CONCLUSIONS:G. jasminoides extract niosomes change the distribution of gardenoside in rats,showing brain targeting effect and decreasing first pass effect for liver.

Study on Quality Standard of Qingfei Pill / 中国中医药信息杂志

Objective To set up the quality standard of TCM preparation Qingfei pill. Methods TLC methods were used to the qualitative identification of Fructus Termininaliae Immaturus and Radix Sophorae Subprostratae in the preparation. The content of Gardenoside, the effective component of Fructus Gardeniae, was determined by HPLC method, using Agilent Eclipse XDB-C18 (150 mm×4.6 mm, 5 μm) and acetonitrile-water (10∶90) as mobile phase with flow rate at 1.0 mL/min. The column temperature was room temperature, and the detection wavelength was 238 nm. Results The TLC methods for Fructus Termininaliae Immaturus and Radix Sophorae Subprostratae identifications were simple and rapid, and showed good repetitiveness. Gardenoside presented a good linear relationship within the range of 0.238-3.808 μg, and the average recovery rate was 97.24%, RSD was 1.60% (n=6). Conclusion These methods showed strong specificity and good repetitiveness, and can be used to control the quality of the product effectively.

Application of Shandong Yaosheng 1 + 1 (Ⅲ) clarificant in clarifying processof Anti-flu Nose Drops / 中草药

Object To investigate the process of flocculation impurity removal for the Anti-flu Nose Drops (AND). Methods Five kind of effective factors on flocculation impurity removal with the index of clarifying results were studied. Comparative tests for Shandong Yaosheng 1 + 1 (Ⅲ) clarificant, 50% alcohol precipitation, and 75% alcohol precipitation were performed with the quantitative index of gardenoside contents, the qualitative index of magnolin and gardenoside TLC chromatograms. The optimum process condition was selected out. Results Under the optimum process condition of flocculation impurity removal, gardenoside contents in the flocculation group is higher than those in 50% , 75% alcohol groups. TLC chromatograms showed that the spots of flocculation group are the same as those in the original liquid group. Conclusion Shandong Yaosheng 1 + 1 (Ⅲ) clarificant has following advantages; high reserved rate of active components, simple operation, cheap cost, stable process, which is a ideal method for the impurity removal.

HPLC Determination of Gardenoside in Xinxue Tablets / 中药新药与临床药理

Objective To establish a RP-HPLC method for the determination of gardenoside in Xinxue Tablets and to provide evidence for ameliorating its quality criterion.Methods HPLC conditions were as follows: C18(4.6?250 mm,5 ?m)column with temperature at 25 ℃,acetonitrile-water(15∶85) as mobile phase with flow rate of 1 mL/min,and the detection wavelength at 238 nm.Results Gardenoside was well separated from other components and had good linearity in the range of 0.128～1.024 ?g(r=0.999 2).The average recovery was 98.67 %and RSD=1.57 %.Conclusion The method is accurate,reproducible,and can be used for the quality control of Xinxue Tablets.

Determination of prim-o-glucasylcimifugin,5-o-methylvisammiosode and gardenoside in Huoxiang Qingwei Granules by HPLC / 中成药

AIM: To establish a method of determing prim-o-glucasylcimifugin,5-o-methylvisammiosode,gardenoside quantitatively in Huoxiang Gingwei Granules(Herba Pogostemonis,Fructus Gardeniae,Radix Saposhnikoviae,etc.). METHODS: Three components were determined by HPLC in the same chromatographic condition(Column: Shimadzu VP-ODS 250 mm?4.60 mm,5 ?m;mobile phase: acetonitrile-0.1% phosphoric acid gradient elution;flow rate: 1.0 mL/min: column temperature: at 30 ℃). RESULTS: Prim-o-glucasylcimifugin showed a good linear relationship at the range of 26.0-390 ng,r=(0.999 9),the average recovery was 101.7% and RSD was 1.1%.5-o-methylvisammiosode showed a good linear relationship at the range of 21.5-322.2 ng,r=(0.999 9),the average recovery was 101.9% and RSD was 1.1%.Gardenoside showed a good linear relationship at the range of 47.1-706.5 ng,r=(0.999 9),the average recovery was 101.6% and RSD was 1.1%.(CONCLUSION):() The established method can provide the content determination of 3 ingriedents at the same test condition and be used for the quality control of Huoxiang Qingwei Granules.