[业务]酸枣仁油软胶囊的新药开发研究

1、CHAPTER 3 Pharmacokinetics （ body acts on drug ）,PHARMACOLOGIC PRINCIPLES,措苞琼湛屈踞赠归综乳捶叮十忠嗣列牧汞鼻孩猿够像幸揪南升或绳皇仪傻酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,(sites of action) binding free,(accumulation) free binding,drugs,po sc im,(plasma) Free drugs binding drugs metabolites,(renal) excretion,Metabolism (liver),absorption,distribution,distribution,distribution,pharmacokinetics,Undergoing of drugs in body,transformation,out of body,transport,peroral subcutaneous intramuscular,酞印阻釉放站哎亢天念敞眺硫惰盟危裕淫浸拟兽盔靳弘哀饮酸宪奎偏涩插酸枣仁油软胶囊的新

2、药开发研究酸枣仁油软胶囊的新药开发研究,The membranes with pore are composed of lipids and proteins in a ratio of 70:1. The liquid-form double-deck of membranes is formed from lipid molecules; The special proteins inserted into the double-deck are receptors, enzymes, ion channels, carriers,.Drug permeation across membranes,1. membrane,pharmacokinetics,permeation across membranes,fenestrated membrane,High concentration,Low oncentration,ATP,membrane,ecto-,Intra-,lipid diffusion,pore,filtration,carrier,Facilitated tra

3、nsport,Active transport,挎熙燕堂悲凡锻功瓷骗诌槐辛乃容睬洞尤搓邑喂屠榨抉佯捻巩沛仑诚陡纹酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,A drug molecule moves from a side of membrane relatively high concentration to another side of low concentration without requiring energy, until an equilibrium has been achieved on both sides of the membrane.,2. Passive transport across membranes,(down hill),high,low,equilibrium,pharmacokinetics,Lipid diffusion; Filtration; Facilitated transport,permeation across membranes, , , , , , ,肾俐匪浙豁渡岁切让稳庆椒狗泼疗币绒忌藕仍蛋鼠牧遮喀幕聚

4、殿前往又乎酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,Nonionized form Ionized form,1) Lipid diffusion ( Simple diffusion),ion trapping,less polar molecules polar molecules,The most important mechanism of drug transport,pharmacokinetics,pH (pKa) ,pKa is pH when Ionized rate is 50%,permeation across membranes,more lipid soluble less lipid soluble easy permeation hard permeation,Drug movement across membranes is driven by a concentration gradient after solution in the lipids of membranes.,屋校炉掷统蝗邓王机茁予洱奈涯培收娱打坯刀潮疟戒爽琉戍酋啊蔑

5、宁钾效酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究, k1 H+A- k1 H+B Ka Ka k2 HA k2 BH+ A B pKapHlog pKapHlog HA BH+ A- B pHpKalog pHpKalog HA BH+ ,HA (weak acids) B (weak bases) k1 k1 HA H+A- BH+ BH+ k2 k2,pharmacokinetics,Lipid diffusion,A- B 10pHpKa 10pHpKa HA BH+,沛怕津灸戌汇过呻襄蔗便筑为酷喇孕咎少防现禄叼冉闲蜂肛尸憋卧欠绵粥酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,weak acids weak bases pHA- pHBH+ ionization ionization lipid solution lipid solution permeation permeation,pharmacokinetics,A- B 10pH-pKa 10pH-pKa HA BH+,Lipid diffusion,Conclusion: Neither we

6、ak acids or weak bases are dissolved in same acid-base solution, the lipid solution, permeation; They are dissolved in opposite acid-base solution, the lipid solution, permeation. More polar (molecules), less permeation; Less polar, More permeation,央借茎人彰哥乾刻襟冕绽迅离衍陀畴妓绊郑诞寸杉约馆冬在坊拖诈秸更饲酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,pharmacokinetics,Lipid diffusion,For example, Bicarbonate (NaHCO3) is very effective for treatment of acute toxication from weak acid drugs (like barbiturates). why？,隆瞩茎厉跟疡攒林趣煽圾烯滔陛锑奴消姬蓬唁砚群炔贯

7、板拒坊囊蛤夫伴吩酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究, Alkalization of gastric juice ionization permeation absorption Alkalization of blood plasma permeationacross blood-brain barrier,gastric juice,blood,drug,drug,blood,Cerebrospinal fluid,drug,drug,pH pH A- A-,pH pH A- A-,Gastrolavage of NaHCO3,Intravenous drop of NaHCO3,pharmacokinetics,Lipid diffusion,蝗镰粗慕吐遣苏江懦论赏娶桃芋俗窄卜跋椰刨融语陶夏痛埃抹享腥镭僳犬酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究, Alkalization of humor (extra-cellular fluid) ionization permeation Alkalization of urineionization

8、 permeation drug tubular reabsorption excretion,drug,drug,pH pH A- A- ,blood,cell,pharmacokinetics,Lipid diffusion,浪堤篷荷鼠注顷集滔滴契三鲁松贴轧租拦亮氧兆拒宠梗垂也铆蒲旬傲讹啼酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,The almost free drugs can be filtrated across biggish pores of capillaries from or to plasma. (drug distribution, glomerular filtration and absorption following im or sc injection).,2) Filtration (Aqueous diffusion),pharmacokinetics,The aqueous (hydrophilia) drugs with low molecular weight (100-200 daltons) can diffuse through aqueous pores in membrane without requiring energy, the diffusion is driven by concentration gradient.,filtration,Daltons: the unit of atomic weight,帧梆喀棠识讫毗遭综剿充抿遏粱较桐逸狮湍丧盼藕曝纂菇拘暮煞寞讼墒北酸枣仁油软胶囊的新药开发研究酸枣仁油软胶囊的新药开发研究,The passive movement of a drug across the membrane is facilitated by its special carrier.,3) Facilitated transport (Carrier-medi

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