谈《生物药剂学与药物动力学》教学体会

为促进《生物药剂学与药物动力学》教学质量的提高,近年来笔者通过教学实践,师生反馈及参考他人教学成功经验,总结不足,肯定成绩,学以致用。虽然在教学过程中取得点滴成绩,尚存在许多需要改进之处。因此在以后的工作中需以现实为起点,加强教师队伍自身建设,提高自身素质和业务水平,“以生为本”,博采众长,不断提高教学水平。     

关于生物药剂学与药物动力学教材的讨论

现在全国高等药学院校药学专业本科使用的教材，是人民卫生出版社出版的第五轮规划教材，这套教材共25本。生物药剂学与药物动力学是其中之一，它是从原药剂学教材章节中分化出来经充实扩展而成的一门独立学科。现在使用的是第2版，内容已经很丰富，体系也很完整。在教学过程中，发现有些非印刷质量的欠妥之处，与作者、读者共同讨论。     

提高生物药剂学与药物动力学教学效果探讨

生物药剂学与药物动力学是一门药学交叉学科。结合课程特点,改进教学方法,丰富教学内容,加强实验教学,提高学生的学习效率和实践能力,从而达到提高教学效果的目的。     

生物药剂学与药物动力学教学中本科生科研能力的培养

本科生科研能力的培养是高等教育的一个重要内容,针对生物药剂学与药物动力学教学的现状,通过更新课堂内容、改革实验教学、开展大学生科研训练计划和毕业专题实习等多环节的科研训练,来提高本科生的科研能力。这种科研训练模式是本科生创新思维、创新意识、创造能力和科研创新能力培养的有效途径。     

生物药剂学与药物动力学创新课堂建设

生物药剂学和药物动力学是一门实践性和应用性很强的药物制剂专业必修课,基于超星平台课程网站资源,采用全线上教学,并请行业专家走进大学课堂,通过问卷调查对教学效果进行总结。多种教学方法、教学手段的创新课堂建设取得了较好的教学效果,提高了学生学习积极性和自主学习能力。     

基于创新能力提升的生物药剂学与药物动力学实验教学改革

将设计性教学理念引入生物药剂学与药物动力学实验教学,学生在系统掌握生物药剂学与药物动力学实验相关理论知识的基础上,充分发挥主观能动性,培养学生其创新精神与实践能力。围绕"对乙酰氨基酚大鼠体内生物药剂学药动学研究"这一课题,从实验设计、实验准备、实验内容、实验方法、实验结果、并针对实验过程中的关键点对学生进行自主式启发式教学,开展基于创新能力提升的生物药剂学与药物动力学实验教学改革。     

案例教学巩固《生物药剂学与药物动力学》在线教学效果探讨

为应对突如其来的新型冠状病毒肺炎疫情,教师通过在线教学、交互讨论等形式,积极探索有效的线上教学方式,为居家自主学习的学生提供高效的学习体验.该文以抗新型冠状病毒药物为案例,面对疫情期间的特殊性,基于以往的"线上线下融合"的互动式讨论课堂,提供给大家"完全线上"的混合式教学案例,巩固《生物药剂学与药物动力学》在线教学,以...     

药物研究中的生物药剂学和药代动力学

随着合理药物设计、重组生物技术、组合化学和高通量筛选等学科的相互融合和相互推动,大量的化合物被合成出来,但由于生物药剂学和药代动力学的制约,这些药物候选物的开发时间长、成本高、西文主要介绍一些重要的生物药学和药代动力学方法,这些方法将有助于降低药物的一切时间和成本,推动安全、有效的药物开发。     

PBL教学法在生物药剂学与药物动力学实验教学能力提升中的探索性研究

目的改革生物药剂学与药物动力学实验教学方法。方法以云南中医学院2013级药学、制药工程、药物制剂专业学生为考察对象,运用PBL和LBL教学法对比研究教学效果。结果研究显示PBL教学法在学生预习成绩及总成绩提高方面明显优于传统的LBL教学法。结论 PBL教学法在生物药剂学与药物动力学实验教学中效果优于LBL教学法,值得推广应用。     

我国生物医药发展模式研究

目的:探索我国生物医药的发展模式,供高校、科研机构、企业和政府部门参考。方法:分析我国生物医药研发和生物医药产业化存在的问题,提出适合我国生物医药发展的各种模式。结果与结论:我国可以运用生物医药的人才储备模式、产学研合作模式、研发模式、阶梯式开发模式、市场营销模式、现代企业运营模式、产业集群模式及国际间合作模式等,有效地促进我国生物医药的发展。     

Positioning of Rifampicin in the Biopharmaceutics Classification System (BCS)

The position of rifampicin with respect to the biopharmaceutics classification system (BCS) was explored on the basis of its aqueous solubility and intestinal permeability. The aqueous solubility was determined between pH 1 and 7 by the conventional shake-flask method. Permeability coefficients of rifampicin and the US FDA listed low (furosemide, ranitidine) and high permeable (caffeine, naproxen) model drugs were determined in the three segments of the rat intestine by employing the everted gut sac model. The samples were analyzed by HPLC. The maximum human single dose of rifampicin (600 mg) was insoluble in 250 ml of aqueous media between pH 3 and 7. The determined apparent permeability coefficient (Papp) values for rifampicin were 4.856×10^?6, 2.117×10^?6, and 2.149×10^?6 cm/sec in the rat duodenum, jejunum and ileum, respectively. These values were similar to those of the low permeable drugs, ranitidine and furosemide, for which Papp values were determined to be 1.767×10^?6?2.426×10^?6 and 2.469×10^?6?3.008×10^?6 cm/sec, respectively. The determined values for high permeable model drugs, viz., caffeine and naproxen, were ～10–20 folds higher than rifampicin or even ranitidine and furosemide. The study suggests that rifampicin is a drug with low solubility and even low intestinal permeability and hence qualifies to be classified in BCS Class IV, instead of Class II where it is being categorized presently. The contention is supported by the reported data on the permeability of the drug through cell monolayers, the mass balance and the absolute bioavailability values in the literature, and the data for rifampicin according to “Lipinski's rule of five”.     

对《中药药剂学》有关问题的质疑

对中国中医药出版社2006年第一版,新世纪全国中医药高职高专规划教材（供中药学专业用）《中药药剂学》有关定义、论述及观点、技术等提出质疑,与同行切磋,使学术正本清源,教科书科学严谨。     

临床药学专业教材建设的思考与建议

我国临床药学专业尚处于初创和发展阶段,课程设置和教学内容比较混乱,教材建设严重滞后。要办好临床药学专业,实现培养目标,专业课程教材的建设及其教学内容的规范至关重要。这些教材包括临床各科的《药物治疗学》以及《临床药理学》、《药物流行病学》等教材,就该专业教材的编写人员组成、编写内容、编写重点以及编写思路提出思考。     

RP-HPLC法测定人血浆中奥卡西平浓度及其药动学研究

目的:建立以反相高效液相色谱法测定人血浆中奥卡西平浓度的方法,并研究其药动学。方法:血样经二氯甲烷提取并速浓采缩用后流进样量分时析间,程色序谱,柱紫为外检Hy测pe波rsi长lC为18,2流57动n相m,为柱甲温醇为-205.1℃m,o固l·L定-进1醋样酸量铵为溶5液0(μ用L,H内3P标O为4调地p西H值泮至。约另4以.8)3p-9三7软乙件胺(计60算∶480名∶0受.1)试,流者清晨空腹单剂量口服奥卡西平胶囊300mg后的平均药动学参数。结果:奥卡西平血药浓度在0.0351～2.245μg·mL-1范围内线性关系良好(r=0.9994),最低定量浓度0.0351μg·mL-1;方法回收率为93.48%～107.29%;日内RSD为1.17%～7.54%,日间RSD为5.88%～10.32%。t1/2Ke为(16.93±5.80)h,tma(x5.88±3.00)h,Cma(x0.56±0.38)μg·mL-1,AUC0～48为(12.11±5.76)ng·h·mL-1。结论:本方法灵敏、准确,可用于奥卡西平的临床血药浓度测定及药动学研究。     

Biopharmaceutics: Formulation-dependent Pharmacokinetics and Pharmacodynamics of Propofol in Rats

Propofol, a highly lipophilic anaesthetic, is commercially formulated as a lipid emulsion (diprivan) for intravenous use. This formulation is characterized by rapid onset and offset of effect after rapid intravenous administration and an effect-site equilibration half-life (t 1/2 k_E0) of 1.7min in rats. Paradoxically these characteristics are usually associated with relatively water-soluble anaesthetics. To test the influence of the formulation on propofol pharmacokinetics, effect-site equilibration kinetics and pharmacodynamics we performed a pharmacokinetic-pharmacodynamic study of propofol in chronically instrumented rats after administration in a lipid-free formulation. In this report we present the results of this study and compare these results with previous data obtained with rats receiving propofol in the emulsion formulation. Compared with the emulsion formulation the distribution volumes (Vd_c and Vd_ss) were significantly higher but the t 1/2 k_E0 (2.0 min) was similar for the lipid-free formulation. The concentration-effect relationship was biphasic. Propofol effect-site concentrations required to achieve 50% activation, peak activation, 50% inhibition of peak activation effect and maximum inhibition were significantly lower, indicating a higher apparent steady-state potency for the lipid-free formulation compared with the emulsion formulation. The evanescent characteristics of propofol's effect-time-course disappeared when the anaesthetic was administered in the lipid-free formulation. These results suggest that the nature of the formulation can profoundly influence the clinical characteristics of intravenously administered drugs by modifying the pharmacokinetics or pharmacodynamics or both.     

佳木斯市医药连锁经营现状调研与建议

目的:为规范医药连锁企业经营行为,促进医药连锁行业健康发展寻找切入点。方法:通过对佳木斯市10家医药连锁企业进行实地调研,分析本地医药连锁企业存在的问题,并提出相关建议。结果:目前医药加盟连锁企业素质欠佳,管理混乱,严重影响医药市场的健康发展。结论:医药连锁经营不能一哄而上搞盲目扩张,企业应注重经营质量,强化管理。政府部门应严格审批,加强监督检查,防止和清理不规范的连锁行为。     

Biopharmaceutics: Drug Metabolism and Pharmacokinetics: Circadian Variations in the Pharmacokinetics of Pentoxifylline in Man

Optimization of therapy by chronopharmacology requires knowledge of rhythmic manifestations of disease activity and chronopharmacokinetic data of the drugs prescribed. Rhythmic functioning of the cardiovascular system in healthy and diseased subjects is manifested as circadian rhythms in blood pressure, cardiac output, heart rate, etc. The disposition of several cardiovascular drugs in man has been reported to be time-dependent. This study reports the effect of time of administration on the disposition of pentoxifylline. Twelve healthy volunteers were treated with 400 mg pentoxifylline orally at 0100, 0700, 1300 and 1900 h in a randomized crossover Latin-square design with a wash-out period of one week. Serum samples were analysed for unchanged pentoxifylline by HPLC. Pharmacokinetic parameters were calculated using a model-independent method. The mean values of various pharmacokinetic parameters after drug treatment at these times were, respectively: maximum plasma concentration (C_max) 485 ± 174, 646 ± 175, 735 ± 271 and 781±217 ng mL^?1; time to reach the maximum plasma concentration (T_max) 1.90±0.39, 1.66±0.4, 1.31 ± 0.41 and 1.32 ± 0.44 h, mean residence time (MRT) 3.8 ± 0.8, 2.9 ± 0.5, 2.9 ± 0.4 and 2.7 ± 0.3 h, elimination half-life (t1/2) 1.93 ± 0.86, 1.23 ± 0.3, 1.39 ± 0.3 and 1.23 ± 0.18 h and volume of distribution at steady state (Vd_ss/f) 11991 ± 4862, 8823 ± 3484, 8275 ± 2357 and 7063 ± 1950 mL kg^?1. The mean C_max value was significantly (P < 0.05) lower after drug administration at 0100 h than after other time-points whereas mean T_max, MRT, Vd_ss/f and t1/2 values were significantly (P < 0.05) higher. These variations might be because of time-dependent changes in absorption and biliary excretion of pentoxifylline and should be borne in mind when designing sustained action dosage forms for the drug.     

Biopharmaceutical evaluation of carprofen following single intravenous, oral, and rectal doses in dogs

Absorption and disposition characteristics of carprofen were compared in the dog after intravenous, oral, and rectal administrations. Rectal formulations included an aqueous solution and a suppository. Single doses of 100 mg carprofen were given in a cross-over design and plasma concentrations of unchanged drug were determined by HPLC. Plasma concentration-time profiles could be adequately described after intravenous and extravascular administrations by tri-and biexponential functions, respectively. After intravenous applications the basic disposition parameters could be determined: mean (+/- S.D.) elimination half-life was about 11.7 (+/- 3.1) h; volume of distribution ranged from 0.12 to 0.22 l kg-1 and total plasma clearance was about 0.017 +/- 0.003 l h kg-1. After oral dosing, carprofen was rapidly absorbed (time of maximum concentration: 0.83 +/- 0.61 h) and comparison with the intravenous solution indicated complete bioavailability. After rectal administration, the rate of absorption evaluated through tmax and calculation of mean absorption times was always slower than after oral dosing. Relative bioavailabilities of the drug from the suppository were about 20 per cent lower than from rectal solutions. No significant difference in rates of absorption of carprofen from rectal solution and suppository was seen; this allowed the conclusion that drug release from the semi-solid dosage form was not the rate-limiting step in carprofen absorption from the suppository. From the present study, it is concluded that rectal administration of carprofen offers an alternative to the oral route of drug intake.