Preparation and Quality Evaluation of Azelnidipine Enteric Solid Dispersion / 中国药房

OBJECTIVE：To prepare Azelnidipine enteric solid dispersion and evaluate its quality. METHODS ：Azelnidipine enteric solid dispersion was prepared by solvent method. Taking cumulative dissolution rate as the index ，single factor test was used to optimize carrier material type and its ratio. The quality of the product was evaluated by DSC ，XRD and FTIR ，and its stability was investigated. RESULTS ：After azelnidipine and carrier material of Eudragit L 100-55 acrylic resin were prepared to enteric solid dispersion at a ratio of 1∶5（m/m），its dissolution rate was significantly improved. DSC ，XRD and FTIR method had all verified the crystal form of azelnidipine changed and it existed in amorphous form. The results of stability test showed that Azelnidipine enteric solid dispersion was stable under high temperature （60 ℃），high humidity （75％）and strong light [ （4 500±500）lx] for 10 days. CONCLUSIONS ：Azelnidipine enteric solid dispersion by solvent method with Eudragit L 100-55 acrylic resin as carrier can eliminate the influence of crystal form ，improve dissolution and has good stability.

Efficacy and Safety of Clonidine Transdermal Patch for Child Tic Disorders ：A Meta-analysis / 中国药房

OBJECTIVE： To systematically evaluate the efficacy and safety of Clonidine tansdermal patch for child tic disorders in children， and to provide evidence-based reference for clinical treatment. METHODS： Retrieved from Medline， Embase， Cochrane library， CNKI， VIP， CBM and Wanfang database， randomized controlled trials （RCTs） about Clonidine tansdermal patch （trial group） versus other therapies （control group， including placebo group， thiopride group， haloperidol group） for child tic disorders were collected from datbase estallishment to July 2018. The literatures met inclusion criteria were summarized. After quality evaluation with Cochrane system evaluation manual 5.1.0， Meta-analysis of reduction rate （amount） of YGTSS， the incidence of ADR and response rate was performed by using Rev Man 5.3 statistical software. Descriptive analysis was performed on indicators of groups that were unable to perform Meta-analysis. RESULTS： A total of 8 RCTs involving 1 320 patients were included. Among them， 2 RCTs involved placebo in control group； 2 RCTs involved thiopride， 3 RCTs involved haloperidol， and 1 RCT involved thiopride and haloperidol. Results of Meta-analysis showed that reduction rate of YGTSS in trial group were significantly higher than haloperidol group [MD＝21.94， 95％CI（21.03， 22.86）， P＜0.001]， but there was no statistical significance compared with thiopride group [MD＝10.66， 95％CI（－15.68， 37.00）， P＝0.43]. The incidence of adverse events （mainly including skin itching， redness， dry mouth， dizziness， decreased blood pressure， abnormal electrocardiogram） in trial group were significantly lower than thiopride group [OR＝0.42， 95％CI（0.22， 0.82）， P＝0.01] and haloperidol group [OR＝0.17， 95％CI（0.09， 0.32）， P＜0.001]， but there was no statistical significance compared with placebo group [OR＝0.61， 95％CI（0.29， 1.29）， P＝0.20]. There was no statistical significance in response rate of trial group compared with thiopride group [OR＝1.29，95％CI（0.38， 4.39）， P＝0.69] and haloperidol group [OR＝1.63， 95％CI（0.89， 2.96）， P＝0.11]. The results of descriptive analysis showed that reduction rate （amount） of YGTSS in trial group was significantly higher than that of placebo group （P＜0.05）， and response rate of trial group was significantly higher than that of placebo group （P＜0.01）. CONCLUSIONS： For child tic disorders in children， Clonidine tansdermal patch is better than placebo and haloperidol in reduction rate （amount） of YGTSS， and is similar to thiopride. Response rate of Clonidine tansdermal patch is better than that of placebo， and is similar to those of thiopride and haloperidol. The safety of Clonidine tansdermal patch is better than those of thiopride and haloperidol， and is similar to that of placebo.

Research on standard management for quality and safety of outpatient prescription / 中华医院管理杂志

Medication safety is a top concern for medical institutions. Outpatient prescription standard is designed to standardize prescription, dispensing, and supervision for outpatient and emergency prescriptions at medical institutions. The standard covered prescription authorization management, prescription issuance, prescription dispensing, prescription saving and supervision. These four parts focus on risk exposure of patients′medication safety, and aim at safeguarding patient medication safety, which were formulated according to China′s laws and regulations, domestic and international industrial standards and technical specifications, as well as prescription conditions at medical institutions and experts opinions. The standard covers technical requirements and guidance, management measures and system development, serving as an important basis to guide medical institutions on standardize management of outpatient prescription and emergency prescription.

Current situations of sterile and implantable medical device manufacturing in Sichuan Province:an investigation in 31 production enterprises / 中国组织工程研究

BACKGROUND:The Specification of Quality Management for Medical Device Production (for Trial Implementation) issued by the China Food and Drug Administration (CFDA) on December 16, 2009 was demanded to be initially implemented in medical device manufacturers with a higher risk in sterility and implant before January 1, 2011. The revised version was published on December 29, 2014 and came into effect on March 1, 2015. OBJECTIVE:To put forward specific suggestions through analyzing the status of 31 sterile implantable medical device manufacturers in Sichuan Province and the corresponding implementation situation of the specification for trial implementation. METHODS:The relevant data of these 31 manufacturers were collected through the quality management system assessment, supervision and inspection, flight inspection and questionnaire survey. And the data were analyzed statistically. RESULTS AND CONCLUSION:The overall size of medical device manufacturers in Sichuan Province is small. There are still some other problems, such as no advanced equipment, low quality of employees, lack of funds and inappropriate management, in these manufacturers. Considering these, we have given some guiding recommendations from the aspects of production and supervision.

Systematic evaluation on effectiveness and safety of recombinant human growth hormone in treating adult patients with severe burn / 中华烧伤杂志

Objective@#To systcmatically evaluate the effectiveness and safety of recombinant human growth hormone (rhGH) in treating adults with severe burn.@*Methods@#Databases including PubMed, Cochrane Library, and Embase were searched using key words " burns, thermal, human growth hormone, growth hormone, hGH, and somatropin (human)" , and China Biology Medicine disc, Chinese Journals Full-text Database, VIP Database, and Wanfang Database were searched using key words in Chinese version "烧伤,重组人生长激素" to obtain the randomized controlled trials about rhGH in the treatment of adults with severe burn from the establishment of each database to December 2016. The measurement indexes included hemoglobin (Hb) and plasma total protein, inflammatory factors [including interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α)], incidence rate of sepsis, incidence rate of hyperglycemia, wound healing time, length of stay, and mortality rate. Meta-analysis was conducted by RevMan 5.3 statistical software.@*Results@#A total of 8 trials involving 534 patients were included; 276 patients in rhGH group were treated with rhGH and 258 patients in placebo control group were treated with placebo. One trial had low risk of bias, while the other 7 trials had unclear risk of bias. The levels of Hb and plasma total protein of patients in rhGH group were higher than those in placebo control group, with standardized mean differences (SMDs) respectively 2.00 and 2.23 [with 95% confidence intervals (CIs) respectively 0.19-3.82 and 1.21-3.26, P<0.05 or P<0.01]. The levels of IL-6 and TNF-α of patients in rhGH group were lower than those in placebo control group, with SMDs respectively -1.46 and -1.13 (with 95% CIs respectively -2.40--0.53 and -1.75--0.51, P values below 0.05). Incidence rate of sepsis and mortality rate of patients in rhGH group were lower than those in placebo control group, with relative risks (RRs) respectively 0.60 and 0.35 (with 95% CIs respectively 0.42-0.85 and 0.15-0.83, P values below 0.05). Incidence rate of hyperglycemia of patients in rhGH group was higher than that in placebo control group, with RR of 2.39 (with 95% CI 1.79-3.18, P<0.001). The wound healing time and length of stay of patients in rhGH group were lower than those in control group, with SMDs respectively -1.54 and -2.00 (with 95% CIs respectively -2.22--0.86 and -3.51--0.49, P<0.05 or P<0.01). Hb, plasma total protein, inflammatory factors, incidence rate of sepsis, wound healing time, length of stay, and mortality rate showed no significant publication bias (P values above 0.05), while there may be publication bias in incidence rate of hyperglycemia (P=0.026).@*Conclusions@#rhGH can inhibit the breakdown of Hb and plasma total protein, reduce the level of inflammatory factors and incidence rate of sepsis, thus shorten the wound healing time and length of stay, thereby reduce mortality rate of adult patients with severe burn. However rhGH may cause hyperglycemia.

N-acetylcysteine for Idiopathic Pulmonary Fibrosis: A Systematic Review / 中国药房

OBJECTIVE:To review therapeutic efficacy of N-acetylcysteine (NAC) for idiopathic pulmonary fibrosis (IPF),and to provide evidence-based reference.METHODS:Retrieved from Central database,PubMed,EMBase,CBM,CJFD,Wanfang database and VIP,randomized controlled trials or semi-randomized controlled trials about NAC (unlimited single drug or combination) vs.placebo/blank control in the treatment of IPF were collected.Meta-analysis was performed by using Rev Man 5.3 statistical software after data extraction and quality evaluation with Cochrane collaboration's bias risk assessment tool(2014 edition).RESULTS:A total of 10 studies were included(2 RCT,8 qRCT),involving 742 patients.Results of Meta-analysis showed that compared to placebo/blank control,NAC couldn't reduce the mortality of IPF patients [OR=1.14,95％ CI(0.50,2.62),P=0.76],but could significantly improve subjective symptom remission rate[OR=3.17,95％ CI (1.98,5.07),P＜0.001] and dyspnea score [SMD =-2.54,95 ％ CI (-5.02,-0.06),P=0.04].CONCLUSIONS:For IPF,NAC can't decrease the mortality of patients,but can relieve main symptoms and dyspnea.

N-acetylcysteine for Idiopathic Pulmonary Fibrosis: A Systematic Review / 中国药房

OBJECTIVE:To review therapeutic efficacy of N-acetylcysteine (NAC) for idiopathic pulmonary fibrosis (IPF),and to provide evidence-based reference.METHODS:Retrieved from Central database,PubMed,EMBase,CBM,CJFD,Wanfang database and VIP,randomized controlled trials or semi-randomized controlled trials about NAC (unlimited single drug or combination) vs.placebo/blank control in the treatment of IPF were collected.Meta-analysis was performed by using Rev Man 5.3 statistical software after data extraction and quality evaluation with Cochrane collaboration's bias risk assessment tool(2014 edition).RESULTS:A total of 10 studies were included(2 RCT,8 qRCT),involving 742 patients.Results of Meta-analysis showed that compared to placebo/blank control,NAC couldn't reduce the mortality of IPF patients [OR=1.14,95％ CI(0.50,2.62),P=0.76],but could significantly improve subjective symptom remission rate[OR=3.17,95％ CI (1.98,5.07),P＜0.001] and dyspnea score [SMD =-2.54,95 ％ CI (-5.02,-0.06),P=0.04].CONCLUSIONS:For IPF,NAC can't decrease the mortality of patients,but can relieve main symptoms and dyspnea.

Phlebitis Induced by Alprostadil Injection with Different Administration Routes:A Systematic Review / 中国药房

OBJECTIVE:To systematically review the difference of phlebitis induced by Alprostadil injection with different ad-ministration routes,and to provide evidence-based reference for clinical rational use. METHODS:Retrieved from PubMed,EM-Base,Cochrane Library,CBM,CJFD,VIP and Wanfang database,RCTs about phlebitis induced by Alprostadil injection with dif-ferent administration routes were collected. Meta-analysis was conducted by Rev Man 5.2 statistical software after literature screen-ing,data extraction and quality evaluation according to Cochrane System Evaluator's Manual 5.1.0. RESULTS:A total of 20 RCTs were included,involving 2562 patients. The results of Meta-analysis showed that the incidence of phlebitis induced by intravenous injection was significantly higher than that induced by intravenous dripping [OR=4.11,95%CI(1.59,10.67),P=0.004] and intrave-nous pump [OR=3.50,95%CI(1.50,8.16),P=0.004]. The incidence of phlebitis induced by general apparatus infusion was signifi-cantly higher than that induced by fine filtering infusion [OR=0.03,95%CI(0.01,0.08),P<0.001],with statistical significance. CONCLUSIONS:The incidence of phlebitis induced by low-concentration of Alprostadil injection or fine filtering infusion is low-er,and that of intravenous injection is higher.

Analysis of the Chemical Compositions in Jinqiancao Granule by HPLC-ESI-Q-TOF-MS / 中国药房

OBJECTIVE:To establish a method for the analysis of chemical compositions in Jinqiancao granule. METHODS:HPLC-ESI-Q-TOF-MS was adopted. The chromatographic conditions:the column was Inertsil ODS-4 with mobile phase of 0.1%formic acid- methanol (gradient elution) at a flow rate of 0.8 ml/min,column temperature was 30 ℃,and the injection volume was 15 μl. MS conditions:ion source was ESI(negative ion mode),endplate offset voltage was -500 V,capillary electrophore-sis was 3500 V,carrier gas was helium gas,atomization and drying gas was high purity nitrogen gas at a flow rate of 6 L/min and a pressure of 1.0 bar,drying air temperature was 180℃. Scanning range was 50-1500 m/z. ChemBioDraw Ultra13.0 and Bruk-er data analysis software 4.0 were used to analyze the chemical composition molecular formula. RESULTS:A total of 27 kinds of chemical components were identified in Jinqiancao granule,involving sucrose,uridine,gallic acid,new chlorogenic acid,(-)-epi-gallocatechin,protocatechuic acid,chlorogenic acid,schaftoside,caffeic acid,schaftoside,vanillc acid,ferulic acid,hyperin,ros-marinic acid,rutin,isoquercitrin,astragalin,quercetin-3-rhamnoside,myricetin,4-hydroxybenzoic acid,quercetin,naringenin, luteolin,kaempferol,isorhmnetin,apigenin and emodin. CONCLUSIONS:Caffeic acid,rosmarinic acid,vanillic acid,(-)-epigal-locatechin,uridine and emodin are firstly found and reported in the chemical compositions in Jinqiancao granule.

Determination of rasagiline mesylate in human plasma by LC-MS/MS and its pharmacokinetics study / 中国药理学通报

Aim To develop LC-MS/MS method to de-termine rasagiline mesylate in human plasma and its application in a pharmacokinetics study .Methods Plasma samples were extracted using liquid-liquid ex-traction with clopidogrel as internal standard .The con-tent of rasagiline mesylate in human plasma was detec-ted by selectivelypositive ion reaction monitoring on a triple quadrupoles tandem mass spectrometer .The de-tected ions were m/z 172.3→117.1 ( rasagiline ) , m/z 322.3 →184.0 ( clopidogrel ) .The linear calibration curve was obtained in the concentration range of 0.1047~20.93 μg · L-1 .The lower limit of quantifi-cation was 0.1047 μg · L-1 .Indicators of the method validation were in line with requirements .The method was used to determine the concentration of rasagiline in human plasma after oral administration of rasagiline mesylate capsule to 24 healthy Chinese volunteers ( with half males and females ) and the results were compared statistically .Results The single oral dose of 0.5 ,1.0 and 2.0 mg presented linear pharmacokinetics in the health volunteers .No accumulation was observed with multiple doses .Meanwhile , no significant difference was identified between the gender groups . High fat postprandial has obvious effects on the peak serum con-centration of rasagiline , but there was no effect on the absorption amount and cumulative excretion .Conclu-sion The LC-MS/MS method is specific and sensi-tive, and can be successfully applied to the pharmaco-kinetic study of Rasagiline mesylate tablets in healthy Chinese volunteers .

Analysis of Drug Use of Chinese Government Medical Detachment in Nepal Earthquake / 中国药房

OBJECTIVE:To provide reference for rational allocation of earth quake medical rescue drugs. METHODS:The number and types of drugs used by Chinese government medical detachment in Nepal earthquake in 2015 were analyzed statistical-ly. RESULTS:Top three kinds of drugs were antipyretic analgesics,Chinese patent medicine for activating meridians to stop pain and antihypertensive drugs;among which,Yunnan baiyao capsule,Ibuprofer sustained release tablet,Nifedipine sustained release tablet were more used;main dosage form was oral preparation,followed by external application and topical preparation. CONCLU-SIONS:Foreign aid relief teams can foresee the quantity and type of rescue drugs depending on station sanitary conditions,medica-tion habits,the characteristics of patients to guarantee the medical detachment work and avoid medical resources waste.

HBsAg quantification in prediction of the long-term efficacy of interferon for chronic hepatitis B / 实用医学杂志

Objective To explore the value of serum HBsAg quantification in prediction of interferon treatment of HBeAg-positive chronic hepatitis B (CHB). Methods 75 patients with HBeAg-positive CHB received peginterferon alfa-2a (PegIFNα-2a) at a dose of 180 μg weekly for 48 weeks with 24 weeks of a pose-treatment follow-up. Serum HBsAg quantification and level of HBV DNA were measured during the treatment and the pose-treatment follow-up. Results In the post-treatment follow-up , the patients were divided into sustained response (SR) group, relapse group, and non-response group. Serum level of HBV DNA did not differ significantly between SR group and relapse group , but was lower than that in non-response group. However , there was no significant difference in HBsAg quantification between relapse group and non-response group , but the level of quantification was higher in both group than in SR group. Serum HBsAg declined more than 1 log10 IU/mL at week 12 , with sensitivity , specificity , and positive and negative predictive value of 86%, 94%, 95%and 94%. The accuracy of the cut-off with a 1 log10 IU/mL decrease in HBsAg level at week 12 of PegIFNα-2a therapy to predict SVR was assessed using receiver operating characteristic curve , and the area under the curve was 0.952. Conclusion The change in serum HBV DNA level could not predict SR effectively, but serum HBsAg quantification is an ideal parameter for predicting the efficacy of interferon therapy.

Clinical Observation of Guizhi Fuling Capsule Combined with Mifepristone in Treatment of Uterine Fibroids / 中国药房

OBJECTIVE:To observe the efficacy and safety of Guizhi fuling capsule combined with mifepristone in treatment of uterine fibroids. METHODS:116 patients with uterine fibroids were randomly divided into control group and observation group. Control group was orally given Mifepristone tablet 25 mg,2 h before meal in the first day of menstrual period,once a day,for con-tinuous 10 d;observation group was additionally given Guizhi fuling capsule 3 pills in non-menstrual period,3 times a day. 3 months was regarded as a treatment course,it lasted 2 courses. Clinical efficacy,and E2,FSH,SHBG,uterine volume,menstrual blood volume,uterine fibroid volume and incidence of adverse reactions in 2 groups before and after treatment were observed. RE-SULTS:Total effective rate in observation group was significantly higher than control group,the difference was statistically signifi-cant(P0.05). CONCLU-SIONS:The clinical efficacy of Guizhi fuling capsule combined with mifepristone in treatment of uterine fibroids is more signifi-cant than mifepristone alone,with good safety.

Comparison of the hyperlipidemic models and lipid-lowering pharmacodynamics between Dunkin Hartley albino guinea pigs and Hartley pigment guinea pigs / 中国比较医学杂志

ObjectiveTocomparethedifferencesoftwostocksofguineapigs,thealbinoguineapigsandpigment guinea pigs , in establishing dyslipidemic model , to evaluate their lipid-lowering action , and to compare their properties for development of hyperlipidemia .Methods Two stocks of the 5-week-old guinea pigs were randomly divided into two groups, normal group (NC) and model group (Model).For the NC group, 12 guinea pigs were fed with normal chew .For the model group , after fed with high-fat diet for four weeks , 24 male guinea pigs were randomly grouped and treated with vehicle (VC group) and pitavastatin (Pit group) calcium, respectively, by gavage as well as received high-fat diet.Before and after modeling and pitavastatin treatment , blood samples were collected and subjected to analysis of plasma TC , TG, HDL-C and LDL-C, respectively .Results In the normal group , the blood lipid levels of albino guinea pigs were more stable than that of the pigmented pigs with the increase of age .After fed with high-fat diet , the plasma lipid levels of TC , TG and LDL-C were significantly increased in the two strains of guinea pigs , while HDL-C showed a decrease to varying degrees .Interestingly , the lipid level in the albino guinea pigs was significantly higher than that of pigment guinea pigs . And also, after drug administration for four weeks , pitavastatin treatment significantly decreased the elevated lipid level of TC, TG and LDL-C in the albino guinea pigs compared with that in the pigment guinea pigs .Conclusions The albino guinea pigs and pigment guinea pigs demonstrate certain differences in establishing dyslipidemic model and evaluating lipid -lowering pharmacodynamics .However , compared with the pigment guinea pigs , the albino guinea pigs have obvious superiority because of easy establishment of hyperlipidemia model and are more sensitive to lipid -lowering drugs .

Transplacental transport mechanisms of drugs for transplacental treatment of fetal tachyarrhythmia of MDCKII/MDCKII-BCRP cell line / 药学学报

To study the transport mechanisms of drugs for transplacental treatment of fetal tachyarrhythmia, MDCKII-BCRP and MDCKII cell models was used. MDCKII-BCRP and MDCKII cell monolayer model was used to investigate the bi-direction transport of sotalol, propranolol, propafenone, procainamide and flecainide. Drug concentrations were measured by HPLC-UV or chemiluminescence. The apparent permeability coefficient (P(app)), efflux rate (R(E)) and net efflux rate (R(net)) were calculated. Drugs with R(net) greater than 1.5 were further investigated using cellular accumulation experiments with or without a BCRP inhibitor. The R(net) of sotalol, propranolol, propafenone and procainamide were less than 1.5, while R(net) of flecainide with concentrations of 20 and 5 μmol x L(-1) were 1.6 and 1.9, respectively. The results showed that the transport of flecainide on MDCKII-BCRP cell monolayer could be mediated by BCRP; and the affinity increased when the concentration of flecainide decreased. Cellular accumulation experiments further suggested that accumulation of flecainide in MDCKII-BCRP cells was significantly lower than that in MDCKII cells in a concentration-dependent manner. BCRP inhibitor quercetin (50 μmol x L(-1)) significantly increased the accumulation of flecainide in MDCKII-BCRP cells (P < 0.05). Our preliminary data showed that flecainide but not sotalol, propranolol, propafenone or procainamide can be a substrate of BCRP. Thus the effect of flecainide may be affected by the BCRP in the maternal placental trophoblast membrane layer when treating fetal tachyarrhythmia.

Recent advances in smoke and drugs interaction / 中国生化药物杂志

Objective Cigarette smoking remains highly prevalent in most countries.It can affect drug therapy by both pharmacokinetic and pharmacodynamic mechanisms.Correlation between smoking and drugs has been reviewed, and the future study about situation of smoking and drugs also was reviewed.

Systematic Review of the Efficacy of Agomelatine in the Treatment of Depression in Acute Phase / 中国药房

OBJECTIVE:To systematically review the efficacy of agomelatine in the treatment of depression in acute phase, and provide evidence-based reference for the clinical treatment. METHODS:Retrieved from Cochrane Library,Medline,EMBase, CJFD,VIP,CBM,Wanfang Database,WHO Clinical Trials Registry Platform and American Clinical Trials Registry Platform, the randomized controlled trials (RCT) about agomelatine versus placebo in the depression patients in acute phase. After quality evaluation and data extraction,Meta-analysis was conducted by using Rev Man 5.2 statistics software. RESULTS:A total of 7 RCT were included,involving 2 378 patients. Results of Meta-analysis showed the effective rate in agomelatine group was obviously bet-ter than placebo group [RR=1.43 ,95%CI(1.29 ,1.59),P<0.001] ,remission rate was obviously better than placebo group [RR=1.27 ,95%CI(1.03 ,1.57),P=0.02] ,and the endpoint score of depression scales was obviously lower than placebo group [MD=-2.92,95%CI(-3.65,-2.20),P<0.001],there was statistically significance. CONCLUSIONS:Agomelatine is effective in the treatment of depression patients in acute phase. However,due to the limit of methodological quality and sample size,it remains to be further verified with more rigorously designed and long-term follow-up of large-scale RCT.

Enhancers on the transmembrane transport of chlorogenic acid / 药学学报

To investigate the influence of the difference enhancers on the transport mechanism of chlorogenic acid (CGA) across Caco-2 cells model, a RP-HPLC method was adopted to detect the concentrations of CGA. At the concentrations of 20 to 80 microg x mL(-1), the difference of absorption rate constants (K(a)) was not statistically significant. At the concentrations of 40 and 20 microg x mL(-1), the ratios of apparent permeability coefficients (P(app)) of the apical to basolateral and the basolateral to apical were 1.14 and 1.18, respectively. With the effect of enhancers K(a) and P(app) increased, the absorption half-life (T1/2) decreased. CGA passed through the Caco-2 cell membrane mainly by passive transport. It showed that monocarboxylic acid transporter (MCT) could be involved in the across membrane transport process of CGA. Borneol had no effect on the cell membrane transport processes. The order of increasing absorption of CGA caused by the enhancers was sodium lauryl sulphate > sodium taurocholate > carbomer.

Determination of oxaprozin in human plasma with high performance liquid chromatography (HPLC) and its application / 生物医学工程学杂志

The present research was aimed to develop a high performance liquid chromatography (HPLC) method to determine oxaprozin in plasma and to evaluate the bioavailability of two oxaprozin enteric coated tablets. A C18 column was used to separate the plasma after protein precipitation and the mobile phase was methanol-12. 5mmol/L ammonium acetate buffer solution (pH=3.0)(71:29). The calibration curve was linear in the concentration range of 0. 50-70. 56 microg . mL-1, and the intra and inter-day RSDs were less than 12. 33% and 10. 42% respectively. A single dose of 0. 4 g reference preparation or test preparation of oxaprozin enteric coated tablets was administered to 20 healthy volunteers according to a randomized crossover study. AUC0-->264h were (4 917. 44 +/- 629. 57) microg . h . mL-1 and (4 604. 30+/-737. 83) microg . h . mL-1, respectively; Cmax were (52. 34+/-7. 68) microg . mL-1 and (48. 66+/-4. 87) microg . mL-1, respectively; Tmax were (18. 70+/-2.27) h and (19. 30+/-1. 63) h, respectively; The relative bioavailability of test preparation was 94.0% +/- 13. 7%. The method is simple, rapid and selective for oxaprozin determination. There is no significant difference in the main pharmacokinetic parameters between the test formulation and reference formulation and the two formulations are in bioequivalence.

Bioequivalence research of cyclosporin soft capsules / 生物医学工程学杂志

This paper is aimed to study the bioavailability and bioequivalence of Cyclosporin Soft Capsules (test preparation and reference preparation) in Chinese healthy volunteers. A high performance liquid chromatography-ultraviolet (HPLC-UV) method for determining the concentration of Cyclosporin A in human whole blood was developed and methodological validated. In accordance with the randomized two-period self crossover study, 24 volunteers received a single oral dose of 400 mg of test preparation or reference preparation. Multiple blood samples were collected post dose and then the concentration of Cyclosporin A in human whole blood samples was determined using the validated assay. The pharmacokinetic parameters including AUC0-t, Cmax, Tmax, and T1/2 were calculated using the non-compartmental method. The bioequivalence of the two preparations was evaluated. After receiving single dose of 400 mg of Cyclosporine A, the pharmacokinetic parameters of T1/2, Cmax, Tmax, and AUC0-t, of Cyclosporin A were (10.114 +/- 6.329) h and (9.717 +/- 4.076) h, (2021.235 +/- 298.581) ng x ml(-1) and (1992.192 +/- 1286.923) ng x ml(-1) (1.729 +/- 0.361) h and (1.813 +/- 0.323) h, (9824.811 +/- 1633.026) ng x h x ml(-1) and (10316.514 +/- 1395.955) ng x h x ml(-1) for test preparation and reference preparation, respectively. The statistical results suggested that these parameters were comparable between the two preparations. The results showed that the test preparation was bioequivalent with the reference preparation in healthy volunteers.