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一系列氨基甲酸正烷基酯在膀胱中的快速吸收:药物再循环的一条途径。

Rapid absorption from the urinary bladder of a series of n-alkyl carbamates: a route for the recirculation of drugs.

作者信息

Bridges J W, Sargent N S, Upshall D G

出版信息

Br J Pharmacol. 1979 Jun;66(2):283-9. doi: 10.1111/j.1476-5381.1979.tb13677.x.

Abstract

1 The rate of loss of a series of n-alkyl carbamates from the lumen of the urinary bladders of female rats has been studied. 2 The rate of loss obeys first order kinetics and was not affected by water flux across the bladder wall nor by binding of the carbamates to it. 3 The rate of loss of octyl carbamate was reduced by about 76% by the presence of 5% Tween 80. Histological evidence indicates that this may be due to the formation of a thin luminal lining which may be adsorbed Tween 80 or mucopolysaccharide material. 4 The absorption rate of the carbamates was limited by their hydrophilicity but reached a plateau for the more lipophilic homologues with a half life for loss of approximately 10 min. 5 The implications of these results with regard to the recirculation of unmetabolized drugs and hydrolysed conjugates of drugs, the systemic absorption of intravesically applied cancer chemotherapeutic agents and bladder wall permeability to carcinogens are discussed.

摘要
  1. 研究了一系列正烷基氨基甲酸酯类物质从雌性大鼠膀胱腔内的损失速率。2. 损失速率符合一级动力学,不受跨膀胱壁的水通量影响,也不受氨基甲酸酯类与膀胱壁结合的影响。3. 5%吐温80的存在使氨基甲酸辛酯的损失速率降低了约76%。组织学证据表明,这可能是由于形成了一层薄的腔内衬里,其可能是吸附的吐温80或粘多糖物质。4. 氨基甲酸酯类的吸收速率受其亲水性限制,但对于亲脂性更强的同系物达到一个平台期,损失的半衰期约为10分钟。5. 讨论了这些结果对于未代谢药物和药物水解共轭物的再循环、膀胱内应用的癌症化疗药物的全身吸收以及膀胱壁对致癌物的通透性的意义。

相似文献

2
Absorption of drugs from the urinary bladder [proceedings].
Biochem Soc Trans. 1979 Feb;7(1):129-30. doi: 10.1042/bst0070129.
4
The absorption of aliphatic carbamates from the rat colon.
J Pharm Pharmacol. 1978 Oct;30(10):638-41. doi: 10.1111/j.2042-7158.1978.tb13346.x.

本文引用的文献

1
Movement of electrolytes across the wall of the urinary bladder in dogs.狗膀胱壁电解质的移动
Am J Physiol. 1960 Jan;198:191-4. doi: 10.1152/ajplegacy.1960.198.1.191.
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Further studies on absorption through the human bladder.
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Drug absorption from the urinary tract of the rat. Nicotine.
Arch Int Pharmacodyn Ther. 1963;143:595-602.
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Thiotepa in the treatment of tumours of the bladder.
Lancet. 1961 Sep 16;2(7203):615-8. doi: 10.1016/s0140-6736(61)90304-x.
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Absorption of radioiodine through the bladder-wall in the rabbit.
Nature. 1959 Mar 28;183(4665):893-4. doi: 10.1038/183893a0.
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Transfer of electrolytes across the urinary bladder in the dog.狗膀胱中电解质的转运
Am J Physiol. 1956 Feb;184(2):406-11. doi: 10.1152/ajplegacy.1956.184.2.406.
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N-hydroxylation of arylamines by bladder mucosa.
Life Sci. 1966 Aug;5(16):1489-94. doi: 10.1016/0024-3205(66)90223-2.

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