2.Determination of diosgenin in Shengmai Freeze-drying Preparation for Injection by RP-HPLC
Hai-Bing HE ; Xing TANG ; Ye-Miao YU ;
Chinese Traditional Patent Medicine 1992;0(06):-
AIM: To develop a new quantitative analysis method for determining diosgenin in Shengmai Freeze-drying Preparation for Injection (Radix Ophiopogonis,etc.)by RP-HPLC with UV detector. METHODS:ODS C_(18) column (5 ?m,4.6 mm?250 mm) was used with mobile phase of acetonitrile-water (88∶12).The mobile phase flow rate was 1.0 mL?min~(-1).The detection wavelength was at 204 nm. RESULTS:The linear range of HPLC was 2.46-7.38 ?g(r=0.999 9).The average recovery was 98.3%,RSD was 0.95%(n=9). CONCLUSION:This method is reliable,accurate and suitable for the determination of diosgenin in Shengmai Freeze-(drying) Preparation for Injection.
3.Clinical Pathological Features of Mesenteric and Omental Inflammatory Myofibroblastic Tumor in 5 Children
ying-zi, TANG ; hai-yan, WU ; li-li, HE
Journal of Applied Clinical Pediatrics 2006;0(19):-
Objective To study the clinical pathological features of mesenteric and omental inflammatory myofibroblastic tumor (IMT) in children.Method Clinical features,laboratory result,pathological evidence for diagnosis and treatment of 5 cases with mesenteric and omental IMT were analyzed and evaluated.Results Intra-abdominal mass was most frequently found in childhood mesenteric and omental IMT.Gastrointestinal obstruction was showed in 2 cases.Anemia,leucocytosis,thrombocytosis,polyclonal-hyperglobulinemia appeared in 5 cases.The histological pattern showed:4 cases were myxoid pattern IMT,1 case was compact spindle cells pattern IMT.Immunohistochemistry showed:the spindle cells were expressed vimentin,smooth muscle action(SMA) and desmin.Partial spindle cells were anaplastic lymphoma kinase(ALK) and cytokeratin(CK) positive,while S-100 protein,CD34 were negative.Complete surgical excision was performed on 5 cases.Follow-up studies ranged from 5 months to 3 years,and no patient developed recurrence.Conclusions Childhood mesenteric and omental IMT is a rare interstitial tumor.The diagnosis should be based on pathological and immunohistochemistry examinations.Most cases are benign,and complete surgical excision can avoid local recurrence.
4.Contrast study of assessment of Her2 gene by fluorescence in situ hybridization and immunohistochemistry technique in neoadjuvant chemotherapy breast cancer patients
Juan HUANG ; Xueli HU ; Jian HAI ; Feiyu CHEN ; Ting XIA ; Yaning HE ; Lili TANG
Journal of Chinese Physician 2012;14(1):5-8
ObjectiveTo evaluate the consistency of HER2 gene status before and after neoadjuvant chemotherapy in breast cancer by FISH (fluorescence in situ hybridization) and IHC (immunohistochemistry) techniques,and analyze the factor of the difference in the result and the feasibility of HER2 gene tested by FISH in the neoadjuvant chemotherapy breast cancer patients.Methods FISH and IHC for HER2 gene expression status was performed on the archival paraffin-embedded sections of breast cancer tissues before and after neoadjuvant chemotherapy from 135 Chinese female patients,x2 test of paired comparison of enumeration data and Kappa analysis were used to compare the difference and consistency of this two techniques.ResultsThe detection rate of HER2 status in punctured cancer tissues before neoadjuvant chemotherapy by FISH and HER2 did not show statistical difference in our research while the opposite result were showed in cancer tissues after neoadjuvant chemotherapy.Moreover,the two techniques of HER2 test were less concordant in patients accepted taxanes neoadjuvant chemotherapy than CAF treatment.ConclusionsThe consistency of FISH and IHC techniques of cancer tissues before neoadjuvant chemotherapy gained advantage compared to the ones after neoadjuvant chemotherapy.Patients received neoadjuvant chemotherapy especially taxanes should take the test of HER2 gene status by FISH technique.
5.Preparation and evaluation of risperidone-loaded microsphere/sucrose acetate isobutyrate in situ forming complex depot with double diffusion barriers.
Xia LIN ; Xing TANG ; Yu-hong XU ; Yu ZHANG ; Yan ZHANG ; Hai-bing HE
Acta Pharmaceutica Sinica 2015;50(6):775-782
In the present study, a risperidone loaded microsphere/sucrose acetate isobutyrate (SAIB) in situ forming complex depot was designed to reduce the burst release of SAIB in situ forming depot and to continuously release risperidone for a long-term period without lagime. The model drug risperidone (Ris) was first encapsulated into microspheres and then the Ris-microspheres were embedded into SAIB depot to reduce the amount of dissolved drug in the depot. The effects of different types of microsphere matrix, including chitosan and poly(lactide-coglycolide) (PLGA), matrix/Ris ratios in microspheres and morphology of microspheres on the drug release behavior of complex depot were investigated. In comparison with the Ris-loaded SAIB depot (Ris-SAIB), the complex depot containing chitosan microspheres (in which chitosan/Ris = 1 : 1, w/w) (Ris-Cm-SAIB) decreased the burst release from 12.16% to 5.80%. However, increased drug release rate after 4 days was observed in Ris-Cm-SAIB, which was caused by the high penetration of the medium to Ris-Cm-SAIB due to the hydrophilie of chitosan. By encapsulation of risperidone in PLGA microspheres, most drugs can be prevented from dissolving in the depot and meanwhile the hydrophobic PLGA can reduce the media penetration effect on the depot. The complex depot containing PLGA microspheres (in which PLGA/ drug=4 : 2, w/w) (Ris-Pm-SAIB) showed a significant effectiveness on reducing the burst release both in vitro and in vivo whereby only 0.64% drug was released on the first day in vitro and a low AUC0-4d value [(105.2± 24.4) ng.mL-1.d] was detected over the first 4 days in vivo. In addition, drug release from Ris-Pm-SAIB can be modified by varying the morphology of microspheres. The porous PLGA microspheres could be prepared by adding medium chain triglyceride (MCT) in the organic phase which served as pore agents during the preparation of PLGA microspheres. The complex depot containing porous PLGA microspheres (which were prepared by co-encapsulation of 20% MCT) (Ris-PPm-SAIB) exhibited a slightly increased AUC0-4d of (194.6±15.8) ng.mL-1d and high plasma concentration levels from 4 to 78 days [Cs(4-78d)=(7.8±1.2) ng.mL-1]. The plasma concentration on 78 day C78d was (9.0 2.5) ng.mL-1 which was higher than that of Ris-Pm-SAIB [C78d= (1.6 ± 0.6) ng.mL-1]. In comparison with Ris-Pm-SAIB, the AUC4-78d of Ris-PPm-SAIB increased from (379.0±114.3) ng.mL-1.d to (465.0 ±149.2) ng.mL-1.d, indicating sufficient drug release from the Ris-PPm-SAIB. These results demonstrate that the risperidone loaded porous PLGA microsphere/SAIB in situ forming complex depot could not only efficiently reduce the burst release of SAIB depot both in vitro and in vivo, but also release the drug sufficiently in vivo, and be capable to continuously release the drug for 78 days.
Chitosan
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Drug Carriers
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Lactic Acid
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Microspheres
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Polyglycolic Acid
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Risperidone
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chemistry
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Sucrose
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analogs & derivatives
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Technology, Pharmaceutical
6.Pharmacokinetic study of ketoprofen in rat by blood microdialysis technique.
Hai-Bing HE ; Xing TANG ; Fu-De CUI
Acta Pharmaceutica Sinica 2006;41(5):452-456
AIMTo investigate the in vitro recovery and influencing factors of ketoprofen in microdialysis probe, and study the pharmacokinetic of unbound ketoprofen in rat after iv administration.
METHODSThe recovery of ketoprofen was detected by a concentration difference method. After microdialysis probe was inserted into the jugular vein of male Wistar rats, the probe was infused with various concentrations perfusate. The in vivo recovery and the pharmacokinetics of unbound ketoprofen in rat were investigated. Dialysate samples were determined by HPLC.
RESULTSThe recovery detected by gain was as the same as that by loss; the recovery was independent of the drug concentration surrounding the probe. The in vitro recovery was 28.75% by concentration difference method and the in vivo recovery was (40.3 +/- 2.7) % by retrodialysis method. After i.v. administration of ketoprofen in rat, T 1/2, AUC and CL of unbound ketoprofen were (181 +/- 16) min, (112 +/- 27) microg x min x mL(-1) and (0.22 +/- 0.05) L x min(-1), respectively.
CONCLUSIONMicrodialysis sampling can be used for the pharmacokinetic study of unbound ketoprofen in rat.
Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; Injections, Intravenous ; Ketoprofen ; administration & dosage ; pharmacokinetics ; Male ; Microdialysis ; methods ; Rats ; Rats, Wistar
7.Applied study on optimizing therapeutic regimen of gastric cancer with the chemosensitivity test in vitro by MTT assay
Cui-Qing ZHANG ; Dong-Ping TANG ; Chuan-Min ZHANG ; Kai TANG ; Nan-Wu YANG ; Hai-Ping HE ;
Cancer Research and Clinic 2006;0(10):-
0.05. Conclusion The tumour chemosensitivity test in vitro gave some prediction and guidances for the clinic chemotherapy,and it could discover the drug resisting cases.The combined chemotherapy should be selected for gastric carcino- ma patients.
8.Rheological properties of sucrose acetate isobutyrate in situ gel.
Ya-xin LU ; Hai-bing HE ; Yue CUI ; Xing TANG
Acta Pharmaceutica Sinica 2007;42(4):445-449
To study the rheological properties of sucrose acetate isobutyrate (SAIB) in situ gel and the influencing factors. Measurements of shear stress and viscosity were carried out at different shear rate. The rheological properties of SAIB solution were similar to those of Newtonian fluid. The factors such as the type of solvent, concentration, additive, drug and temperature had effect on the rheological properties. Ethanol was a suitable solvent compared with ethyl lactate and N-methylpyrrolidone (NMP). The solution viscosity of SAIB was reduced from 1.29 to 0.11 Pa x s with only increasing the content of ethanol from 10% to 20%. Polylactic acid (PLA) and risperidone could increase the intermolecular force and viscosity. However, adding 10% (w/w) PLA, the initial release of risperidone was reduced from 20.2% to 3.5%. The solution viscosity reduced significantly by stepping up the temperature. The results obtained support the using of SAIB is satisfactorily injectable in situ gel formulation.
Antipsychotic Agents
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administration & dosage
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Delayed-Action Preparations
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Drug Carriers
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Ethanol
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Lactates
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Lactic Acid
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Polyesters
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Polymers
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Pyrrolidinones
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Rheology
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Risperidone
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administration & dosage
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Solvents
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Sucrose
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administration & dosage
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analogs & derivatives
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chemistry
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Temperature
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Viscosity
9.Preparation and in vitro and in vivo evaluation of etoposide submicro-emulsion for intravenous injection.
Ling-Ling TIAN ; Xing TANG ; Hai-Bing HE ; Jing WANG
Acta Pharmaceutica Sinica 2007;42(8):892-897
The aim of this thesis is to prepare etoposide submicro-emulsion (ESE) for intravenous injection and investigate its characteristics in vitro and in vivo. High-pressure homogenization was used to prepare ESE, using 10% (w/w) soybean oil and 10% (w/w) medium-chain triglyceride as mixed oil phase, and 1.8% (w/w) fabaceous lecithin as emulsifier. The pH was adjusted to 5.5 with 0.1 mol x L(-1) NaOH to keep the most stability of ESE. The particle size distribution and zeta potential were measured using photon correlation spectroscopy. Ultrafiltration was used to estimate the relative percentages of etoposide in each phase. Long-term storage test and accelerated isothermal test-Weibull distribution method were used to estimate the physical and chemical stability of ESE. Plasma pharmacokinetics in rats was monitored by high performance liquid chromatography by comparison with etoposide nonaqueous solution at the same time. The mean particle size, zeta potential and entrapment efficiency of ESE were (189.9 +/- 54.6) nm, - 32.6 mV and 91.7%, respectively. The emulsion was stable during 9 month storage at 4 degrees C. The shelf life (T0.9) of etoposide in lipid emulsion was estimated to be about 665 days at 4 degrees C. The drug concentration-time curves of ESE and solution were similar and could be described by two compartment model. The area under the curve of concentration versus time from zero to the last time point and the mean residence time of ESE and solution were (18.30 +/- 8.74) and (19.32 +/- 6.45) microg x h x mL(-1), and (1.46 +/- 0.32) and (1.71 +/- 0.52) h, respectively. Etoposide was incorporated in submicro-emulsion to improve its physical and chemical stability without addition of organic solvents with insignificant different characteristics in vivo when compared with solution.
Animals
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Antineoplastic Agents, Phytogenic
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administration & dosage
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pharmacokinetics
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Area Under Curve
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Drug Carriers
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Drug Compounding
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Drug Stability
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Drug Storage
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Emulsions
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Etoposide
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administration & dosage
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pharmacokinetics
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Female
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Hydrogen-Ion Concentration
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Injections, Intravenous
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Lecithins
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chemistry
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Male
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Particle Size
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Random Allocation
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Rats
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Rats, Wistar
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Solubility
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Soybean Oil
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chemistry
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Technology, Pharmaceutical
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methods
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Triglycerides
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chemistry
10.Determination of six C-Glycoside flavones and antitumor activity of water-soluble total flavonoids from Isodon lophanthoides var. gerardianus.
Yang ZHANG ; Hai-ming TANG ; Ai LI ; Lan-fang XU ; Jian-nan CHEN ; Song HUANG ; Lian HE
China Journal of Chinese Materia Medica 2015;40(8):1543-1547
This research established an HPLC method for determination of six C-Glycoside flavones of warer-soluble total flavonoids from Isodon lophanthoides var. gerardianus (Benth.) H. Hara, and studied the antitumor activity of the warer-soluble total flavonoids. The HPLC system consisted of Kromasil 100-5 C18 (4.6 mm x 250 mm, 5 microm) column and a solution system of methanol, acetonitrile and 0.5% formic acid gradient elution at a flow rate of 0. 8 mL x min(-1) and the wavelength of detector was at 334 nm. The column temperature was 25 degrees C. The antitumor activity of water-soluble flavonoids was assayed using HepG2 cell as the tested cell. The linear ranges of vicenin II, vicenin III, isoschaftoside, schaftoside, vitexin, 6, 8-di-C-a-L-arabinosylapigenin were 0.25-2.53, 0.12-1.20, 0.37-3.69, 0.16-1.63, 0.19-1.92, 0.14-1.42 microg, respectively. The average recoveries (n = 6) were 99.6% (RSD 0.87%), 100.2% (RSD 2.0%), 99.6% (RSD 1.8%), 97.9% (RSD 1.5%), 98.8% (RSD 1.2%), 98.6% (RSD 1.2%), respectively. After exposure in 24, 48, 72 h, the total flavonoids showed inhibitory effect on the proliferation of HepG2 cells with IC50 as the evaluation index, the IC50 values of 1.89, 1.71, 1.51 g x L(-1), respectively. The method is quick, simple and accurate with good re- producibility, and can be used for determination of vicenin II, vicenin III, isoschaftoside, schaftoside, vitexin, 6, 8-di-C-a-L-arabino- sylapigenin in the warer-soluble total flavonoids from L lophanthoides var. gerardianus. The warer-soluble total flavonoids from L lophanthoides have inhibitory effect on the proliferation of HepG2 cells.
Antineoplastic Agents, Phytogenic
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analysis
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pharmacology
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Cell Line, Tumor
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Cell Proliferation
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drug effects
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Chromatography, High Pressure Liquid
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Drugs, Chinese Herbal
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analysis
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pharmacology
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Flavones
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analysis
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pharmacology
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Humans
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Isodon
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chemistry
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Monosaccharides
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analysis
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pharmacology