1.Absolute bioavailability of ginkgolide compounds in rats.
Hai-hong SI ; Ting GENG ; Xiao-ping SUN ; Jie ZHAO ; Jia XUE
China Journal of Chinese Materia Medica 2015;40(14):2882-2886
To investigate the pharmacokinetic characteristics and absolute bioavailability of ginkgolide A (GA), ginkgolide B (GB) and bilobalide (BB) in rats. In this experiment, a high-performance liquid chromatography-tandem mass spectrometry (LC-MS/ MS) method was established to determine the plasma concentrations of GA, GB and BB in rats after rats were administrated with the three drugs through ig and iv respectively. The main pharmacokinetic parameters and absolute bioavailability of three ginkgolide compounds were obtained by using pharmacokinetic software DAS 2. 0. After the inject of GA, GB and BB, the results showed Cmax at (513.9 ± 116.9), (701.3 ± 76.0), (5,255.6 ± 476.8) µg · L(-1) and AUC0.24h of (960.9 ± 268.5), (779.5 ± 140.6), (7,409.3 ± 1,181.1) µg · h · L(-1), respectively; after the oral administration, the results showed Cmax at (522.9 ± 39.9), (146.8 ± 31.6), (2,711.9 ± 588.9) µg · L(-1) and AUC0-24 h of (1,760.4 ± 300.7), (636.6 ± 180.3), (16,651.4 ± 1,306.5) µg · h · L(-1), respectively. The absolute bioavailability of GA, GB and BB in rats was (61.1 ± 10.4)%, (27.2 ± 7.7)%, (56.2 ± 4.4)%, respectively. The method established in this experiment has a good specificity and sensitivity and so can be used to study the pharmacokinetics and absolute bioavailability of GA, GB and BB in rats.
Animals
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Biological Availability
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Chromatography, High Pressure Liquid
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Cyclopentanes
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pharmacokinetics
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Furans
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pharmacokinetics
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Ginkgolides
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pharmacokinetics
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Lactones
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pharmacokinetics
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Male
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Rats
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Rats, Sprague-Dawley
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Tandem Mass Spectrometry
2.Determination of five kinds of trace ginkgolic acids in diterpene ginkgolides meglumine injection materials by LC-MS/MS.
Hai-hong SI ; Yan-jing LI ; Jia XUE ; Wen-zhe HUANG ; Zhen-zhong WANG ; Wei XIAO
China Journal of Chinese Materia Medica 2015;40(14):2832-2836
To develop a LC-MS/MS method for the determination of five kinds of trace ginkgolic acids in diterpene ginkgolides meglumine injection materials, the column was Agilent ZORBAX Eclipse plus C18 (3.0 mm x 50 mm, 1.8 µm), and the mobile phase consisted of methanol-water (containing 0.2% formic acid) (95:5) at a flow rate of 0.5 mL · min(-1). The multiple reaction ion monitoring (MRM) with an ESI interface in the negative ion mode was selected. The results showed that the linear ranges of five kinds of ginkgolic acids were in the range of 0.2-36.0 µg · L(-1) (r ≥ 0.999 5). The lowest limit of quantification (LOQ) of ginkgo acid C13: 0, C15:1, C17:2, C15:0 and C17:1 were 0.18, 0.18, 0.21, 0.10 and 0.20 µg · L(-1), respectively. The average recovery was between 73.28% and 87.56%, and the average content of total ginkgolic acids in three batches of samples was in the range of 0.023-0.028 µg · g(-1), which was much lower than 2 µg · g(-1) prescribed in drug registration standards. This method is simple and rapid with high sensitivity, which can be used for the determination of five kinds of trace ginkgolic acids in diterpene ginkgolides meglumine injection materials.
Chromatography, Liquid
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methods
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Ginkgolides
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analysis
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Injections
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Limit of Detection
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Salicylates
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analysis
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Tandem Mass Spectrometry
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methods
3.Effect of brain-derived neurotrophic factor genetically modified neural stem cells transplantation on cerebral ischemic injury in rats
Xiao-Ying BI ; Su-Ju DING ; Jia-Si LI ; Yi TAO ; Li CAO ; Yong ZHANG
Chinese Journal of Neurology 2000;0(04):-
Objective To investigate the effect of brain-derived neurotrophic factor (BDNF) gene modified neural stem cells (NSCs)transplantation on cerebral ischemic injury in rats.Methods NSCs from newborn rat hippocampus were isolated,cultured in a medium containing fibroblast factor (FGF) in vitro. Their proliferation and differentiation were detected by immunohistochemistry.Virus vectors pLXSN-BDNF were built and BDNF were transfected into NSCs.Biological activity were detected to obtained engineering stem cells of BDNF protein with secretary activity.Middle cerebral artery occlusion (MCAO) models were made and transplanted with NSCs-BDNF by stereotaxic technique.The effect of transplantation on MCAO models was evaluated histologically and behaviorally.Results Statistical analysis showed that the behavioral performance of the animals improved after transplantation (Longa mark being 1.343?0.293 four weeks after stem cell transplantation).The number of hippocampal dentate gyrus neurons increased to 87.5%?6.6% , four weeks after stem cell transplantation on Nissle stained hippocampal sections,which was significantly different from that of controls.Positively BrdU stained neural stem cells revealed by immunohistochemistry in the cultured cells and in the transplanted brain sections,indicated that the engineering cells transplanted had survived in the host brain and began to proliferate.Conclusion Transplantation of BDNF genetically modified NSCs can effectively promote the recovery from cerebral ischemic injury.
4.Effect of Warm and Hot Water Bath on Rang of Motion of Knee
Long JIN ; Fang CONG ; Fengshan SI ; Bin YAO ; Wei JIA ; Dengwu XIAO
Chinese Journal of Rehabilitation Theory and Practice 2012;18(5):461-462
Objective To compare the effect of water bath in different temperature on rang of motion (ROM) of injuried knees. Methods30 patients with limited knee ROM were divided into hot water group (42 ℃) and warm water group (38 ℃) randomly. On the base of routinerebabilitation, patients accepted lower limb special bubbles and swirl bath in their temperature 20 times. Their positive ROM of kneewere measured before and after the treatment. Results The ROM of knee increased in both groups (P<0.001), and increased more in hot watergroup than in warm water group (P<0.05). Conclusion Hot water bath is more effective on ROM of injuried knees.
5.Effect of Underwater Treadmill Training on Hemiplegics after Stroke
Qiong WU ; Fang CONG ; Long JIN ; Fengshan SI ; Bin YAO ; Wei JIA ; Dengwu XIAO
Chinese Journal of Rehabilitation Theory and Practice 2011;17(12):1145-1147
Objective To investigate the effect of underwater treadmill training (UWTT) on patients with hemiplegia after stroke. Methods Based on routine rehabilitation, 15 hemiplegic patients after stroke were treated with UWTT system 20 min/d, 5 times a week for 4 weeks. Walking distance and speed in water were tested before and after UWTT. Dynamic balance function and static balance function were also assessed by Active Balancer assessment. Results All the items improved significantly after treatment (P<0.01), except deflection center displacement of X and Y axis (P>0.05). Conclusion UWTT can improve the walking ability and balance function of hemiplegic patients after stroke.
6.Effects of irradiation and W11-a12 on anion-selective channel of mouse peritoneal macrophage
Chong-Xiang SHU ; Ben-Lan YE ; Tian-Min CHENG ; Jia-Si XIAO
Journal of Third Military Medical University 2001;23(3):290-292
Objective To study the effects of irradiation and W11-a12,a kind of repair-promoting drug,on anion-selective channel in membranes of mouse peritoneal macrophage. Methods The activity of anion-selective channel was recorded from cell-attached patches with patch clamp techniques. Results The effects of irradiation on anion-selective channel in membranes of peritoneal macrophage included:①decreasing the mean number of activated channels by the presence of zymosan; ②prolonging the mean time from stimulus to the opening of channels; ③depressing the opening of channels by decreasing open-state probability,shortening open-time and prolonging close-time. The effects of irradiation could partly be depressed by W11-a12. Conclusion Irradiation will depress the anion-selective channel of peritoneal macrophage, which may be an important way to depress the function of macrophage.
7.Reliability and Validity of Chinese Version ofWater Orientation Test of Alyn 1
Long JIN ; Fang CONG ; Yao CUI ; Dunwu XIAO ; Fengshan SI ; Bin YAO ; Wei JIA ; Youlin LI ; Shuzeng ZHANG
Chinese Journal of Rehabilitation Theory and Practice 2015;21(5):539-543
Objective To translate the Water Orientation Test of Alyn 1 (WOTA1) into Chinese and investigate the test-retest reliability, inter-rater reliability and validity of this Chinese Version. Methods The Water Orientation Test of Alyn 1 was translated from English into Chinese. 25 children with cerebral palsy were tested with Chinese Version of WOTA1 by 2 raters. One of the raters accessed the same children again after 2 days. While the children were assessed with Brief Assessment of Motor Function (BAMF). The scores from both raters, twice of one rater, and of WOTA1 and of BAMF were analyzed with Pearson correlation coefficient. Results The correlation coefficient of test-retest of WOTA1 total score is 0.992 (95% CI: 0.982-0.996), and it was 0.887 to 1.000 of the scores of items. The correlation coefficient of inter-rater of total score is 0.992 (95% CI: 0.980-0.998), and it was 0.748 to 1.000 of the scores of items. The correlation coefficient between scores of WOTA1 and BAMF was 0.926 (P<0.01). Conclusion The Chinese Version of WOTA1 is good reliable and valid to assess the motor function in hydrotherapy pool.
8.Etiology of hand, foot and mouth disease in Guangzhou in 2008.
Bing ZHU ; Jia-yu ZHONG ; Hui-min XIA ; Si-tang GONG ; Mi-si XIAO ; Jia-hui XIE ; Ying-ying ZHANG ; Liang HUA ; Guang-wan LIAN
Chinese Journal of Pediatrics 2010;48(2):127-130
OBJECTIVETo understand the etiology of hand, foot and mouth disease (HFMD) in Guangzhou area in 2008.
METHODTotally 1023 clinical specimens were collected from pediatric patients suspected of HFMD in 2008. TaqMan real-time RT-PCR were used for detection of enterovirus 71 (EV71), Coxsackievirus A16 (CA16) and other enteroviruses. The specimens which were enterovirus positive by RT-PCR method with universal primer but EV71 and CA16 negative, were amplified and sequenced for 5'untranslated region.
RESULTEnterovirus was identified from 434 of 1023 samples and detection rate of enterovirus was 42.42%; of the 434 samples, 276 were positive for EV71 (63.6%), 126 for CA16 (29%), 4 samples for enterovirus 84, 3 for Echovirus 11, 2 for Echovirus 9, 3 for Coxsackievirus B3, 4 for Coxsackievirus A10, 3 for Coxsackievirus A6, 6 for Coxsackievirus A12 or A5, and for 7 samples typing was difficult.
CONCLUSIONThe major causative agents of HFMD in Guangzhou were EV71 and CA16 in 2008, and EV84, CA10, CA12, CA6, COSB3, ECHV11, ECHV9 were also the pathogens for smaller proportions of patients.
Child ; Child, Preschool ; China ; epidemiology ; Coxsackievirus Infections ; epidemiology ; DNA Primers ; Enterovirus A, Human ; classification ; genetics ; isolation & purification ; Female ; Hand, Foot and Mouth Disease ; epidemiology ; virology ; Humans ; Infant ; Male ; RNA, Viral ; Reverse Transcriptase Polymerase Chain Reaction
9.Preparation and in vitro and in vivo evaluations of topically applied capsaicin transfersomes.
Long XIAO-YING ; Jia-Bo LUO ; Zhi-Hong YAN ; Hui-Si RONG ; Wei-Min HUANG
Acta Pharmaceutica Sinica 2006;41(5):461-466
AIMTo prepare capsaicin transfersomes and evaluate them in vitro and in vivo.
METHODSCapsaicin transfersomes were prepared by high shear dispersing machine and evaluated by entrapment efficiency, release rate, in vitro skin permeation and distribution in different tissues in vivo.
RESULTSCapsaicin transfersomes were composed of single unilamellar vesicles with an average diameter of 150.6 nm. Capsaicin entrapment efficiency increased distinctly with increasing of concentration of lecithin and entrapment efficiency is 96.7% while concentration of lecithin to 8%. Cumulative release amount of capsaicin is in direct proportion to the ethanol concentration in the receptor medium. In vitro capsaicin cumulative penetration amount showed higher levels in transfersomes than cream and suspension in rat abdominal skin. Abdominal skin cumulative penetration amount in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men. In the same way, abdominal skin epidermal membrane cumulative penetration amount in vitro of capsaicin transfersomes was significantly higher than that from derma and full skin in human abdominal skin. The capsaicin tissue distribution of capsaicin injection by multiple celiac injections in rats is different: bone > plasma > skin > muscle. There is a similar result by multiple thigh topical application of capsaicin transfersomes: bone > skin > plasma > muscle.
CONCLUSIONEntrapment efficiency of capsaicin transfersomes reached the criterion of China Pharmacopoeia (> 80%) and capsaicin skin penetration can be increased by capsaicin transfersomes. It should be noted that the diverse characters and levels of skin may probably affect the permeating capability of capsaicin. Capsaicin tissue distribution in bone and muscle is similar and is different in plasma and skin by multiple injections and topical skin apply.
Administration, Cutaneous ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; pharmacokinetics ; Capsaicin ; administration & dosage ; pharmacokinetics ; Drug Carriers ; Drug Delivery Systems ; Humans ; Lecithins ; chemistry ; Male ; Mice ; Particle Size ; Rats ; Rats, Sprague-Dawley ; Skin Absorption ; Sodium Cholate ; chemistry ; Tissue Distribution
10.Preparation and in vitro evaluations of topically applied capsaicin transfersomes.
Xiao-ying LONG ; Jia-bo LUO ; Li-ren LI ; Dan LIN ; Hui-si RONG ; Wei-min HUANG
China Journal of Chinese Materia Medica 2006;31(12):981-984
OBJECTIVECapsaicin transfersomes were prepared and its quality specifications were evaluated.
METHODCapsaicin transfersomes were prepared by high shear dispersing machine and evaluated on the entrapment efficiency, drugs release rate and in vitro skin permeation.
RESULTCapsaicin transfersomes is composed of single unilamellar vesicles, with average size of 150.6 nm. Capsaicin entrapment efficiency achieved 96.7% while concentration of lecithin used was 8%. cumulative release amount of capsaicin was in direct proportion to the ethanol concentration in the medium. The in vitro rate cumulative penetration rate of capsaicin was higher in transfersomes than in cream and suspension in rats. Adomen skin cumulative penetration rate in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men. In the same way,cumulative penetration rate in vitro of capsaicin transfersomes through abdomen skin epidermal membrance was significantly higher than that with derma and full skin in men.
CONCLUSIONEntrapment efficiency of capsaicin transfersomes reached 96.7%, meeting the criterion of China pharmacopia( > 80%), skin penetration of capsaicin was enhanced by a capsaicin transfersomes preparation and was affected by diverse characters and levels of skin.
Administration, Cutaneous ; Analgesics, Non-Narcotic ; administration & dosage ; pharmacokinetics ; Animals ; Capsaicin ; administration & dosage ; pharmacokinetics ; Drug Carriers ; Drug Delivery Systems ; methods ; Humans ; In Vitro Techniques ; Male ; Mice ; Particle Size ; Phosphatidylcholines ; administration & dosage ; chemistry ; pharmacology ; Rats ; Skin ; drug effects ; metabolism ; Skin Absorption ; drug effects