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首页> 外文期刊>薬物動態 >Pharmacokinetics of Buprenorphine Hydrochloride (BN centre dot HCl) (1): Absorption, Distribution, Metabolism and Excretion after Percutaneous (TSN-09: BN centre dot HCl Containing Tape Application) or Subcutaneous Administration of BN centre dot HCl
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Pharmacokinetics of Buprenorphine Hydrochloride (BN centre dot HCl) (1): Absorption, Distribution, Metabolism and Excretion after Percutaneous (TSN-09: BN centre dot HCl Containing Tape Application) or Subcutaneous Administration of BN centre dot HCl

机译：盐酸盐酸盐（BN Center Dot HCl）（1）：经皮（TSN-09：BN中心点HCl含有胶带施用）或皮下施用BN中心点HCl后吸收，分布，代谢和排泄物

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The Pharmacokinetics of ~3H- BN centre dot HCl in male rats was studied after a single percutaneous (~3H-TSN-09: ~3H- BN centre dot HCl containing tape) or subcutaneous administration of ~3H- BN centre dot HCl.1. The radioactivity level in blood reached the C_max at 21.6 hr after a single percutaneous administration, then decreased with the t_(1/2) of 4.8 days, and the unchanged drug concentration in plasma reached the C_max at 8 hr after dosing. When ~3H- BN centre dot HCl was administered percutaneously as a tape formulation (~3H-TSN-09) at the dosage of 20,40 or 80 #mu#g of ~3H- BN centre dot HCl/animal, the C_max and AUC_(0-infinity) value increased in proportion to the administered dose. From the AUC_(0-infinity) values in percutaneous and subcutaneous administration, the absorption ratio of percutaneous administration was calculated to account for about 14% of dose. The T_max of each dose was observed at around the end of application period, indicating the absorption of ~3H- BN centre dot HCl through skin to continue during application period.2. When ~3H-TSN-09 was applied to the shaved area skin in rats, the whole body autoradiogram showed high level of radioactivity of the application site of the skin, low level of radioactivity in0 the gastro-intestinal contents and little level of radioactivity in most other tissues.3. Within 168 hr after a single percutaneous administration 1.0 and 8.2% of dose was excreted into urine and feces, respectively.4. The bindign of BN centre dot HCl to plasma protein varied from 88.9 to 97.4% in rat, dog or human. BN centre dot Hclbound to human serum albumin, #gamma#-globulin and #alpha#!-acid glycoprotein and their binding ratios were 65.6, 41.5 and 84.95, respectively.After a single percutaneous administration of ~3H- BN centre dot HCl to rats, two metabolites, RP1 and RP2 were detected in plasma. The structures of RP1 and RP2 wre identified as norbuprenorphine-glucuronide and BN-glucuronide, respectively. These two metabolites were also found in rat plasma after a single subcutaneous administration. So it was considred that the metabolic pathway of BN centre dot Hclmight be the same in both administration routes.
机译：在单一经皮（〜3H-TSN-09：〜3H-BN-09：〜3H-BN-09：〜3H-BN-09：〜3H-BN-09：〜3H-BN-09：〜3H-BN-09：胶带）或皮下施用〜3H-BN中心点HCl.1后，研究了〜3H-BN中心点HCl的药代动力学。 。在单一经皮施用后，血液中的放射性水平在21.6小时以21.6小时达到C_max，然后用4.8天的T_（1/2）降低，并在给药后8小时血浆中的不变药物浓度达到C_max。当剂量为〜3H-BN-TSN-09）以20,40或80-80＃GCOR HCl / Anival，C_max和C_max和C_MAX和C_MAX和AUC_（0-无限远）与给药剂量成比例地增加。从经皮和皮下施用中的AUC_（0-无穷大）值，计算经皮给药的吸收比以占剂量约14％。在施加周期结束时观察到每种剂量的T_max，表明在施用期间吸收〜3H-BN中心点HCL以继续。当〜3H-TSN-09应用于大鼠剃屑区域皮肤时，全身放大镜显示出皮肤应用部位的高水力放射性，低放射性水平IN0胃肠内容物和放射性水平较小大多数其他组织.3。在单一经皮施用后的168小时内，分别排出8.0％的剂量，分别排入尿液和粪便。 BN中心点HCl与血浆蛋白的结合在大鼠，狗或人中的88.9％至97.4％。 BN中心点Hclbound到人血清白蛋白，#gamma＃-globulin和#alpha＃！ - 酸糖蛋白及其结合比分别为65.6,41.5和84.95。在单一经皮施用〜3H-BN中心点HCl到大鼠的单一经皮施用，在血浆中检测到两种代谢物，RP1和RP2。 RP1和RP2 WRE的结构分别鉴定为Norbuprenorphine-葡糖醛酸和BN-葡糖醛酸酯。在一次皮下给药后，还发现这两个代谢物在大鼠血浆中发现。因此，据认为，BN中心点HCLMight的代谢途径在两个管理路线中都是相同的。

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