剂型对人体中甲苯咪唑生物利用度的影响。
The effect of dose form on the bioavailability of mebendazole in man.
作者信息
Dawson M, Watson T R
出版信息
Br J Clin Pharmacol. 1985 Jan;19(1):87-90. doi: 10.1111/j.1365-2125.1985.tb02617.x.
Abstract
Four different dose forms of mebendazole were administered to human volunteers, and urine was collected and assayed for mebendazole and unconjugated metabolites of mebendazole. Oral administration of mebendazole as an oily suspension slightly enhances the bioavailability of the drug, however mebendazole is not absorbed following rectal administration. The major urinary metabolite of mebendazole in humans is 2-amino-5(6)[alpha-hydroxybenzyl]benzimidazole (IV), not 2-amino-5(6) benzoylbenzimidazole (II), as previously reported.
摘要
将四种不同剂型的甲苯咪唑给予人类志愿者，并收集尿液检测甲苯咪唑及其未结合代谢物。甲苯咪唑以油悬液形式口服可略微提高药物的生物利用度，然而，甲苯咪唑经直肠给药后不被吸收。人类尿液中甲苯咪唑的主要代谢物是2-氨基-5(6)[α-羟基苄基]苯并咪唑（IV），而非先前报道的2-氨基-5(6)苯甲酰基苯并咪唑（II）。
相似文献
1
The effect of dose form on the bioavailability of mebendazole in man.剂型对人体中甲苯咪唑生物利用度的影响。
Br J Clin Pharmacol. 1985 Jan;19(1):87-90. doi: 10.1111/j.1365-2125.1985.tb02617.x.
2
The pharmacokinetics and bioavailability of a tracer dose of [3H]-mebendazole in man.人体中示踪剂量的[3H] - 甲苯咪唑的药代动力学和生物利用度。
Br J Clin Pharmacol. 1985 Jan;19(1):79-86. doi: 10.1111/j.1365-2125.1985.tb02616.x.
3
The metabolic and pharmacokinetic disposition of mebendazole in the rat.甲苯达唑在大鼠体内的代谢及药代动力学特性
Eur J Drug Metab Pharmacokinet. 1983 Oct-Dec;8(4):373-81. doi: 10.1007/BF03188769.
4
Identification of biliary metabolites of mebendazole in the rat.大鼠体内甲苯达唑胆汁代谢物的鉴定。
Eur J Drug Metab Pharmacokinet. 1982;7(2):131-6. doi: 10.1007/BF03188730.
5
The pharmacokinetics and bioavailability of mebendazole in man: a pilot study using [3H]-mebendazole.甲苯咪唑在人体内的药代动力学和生物利用度：一项使用[³H] - 甲苯咪唑的初步研究。
Br J Clin Pharmacol. 1982 Sep;14(3):453-5. doi: 10.1111/j.1365-2125.1982.tb02008.x.
6
Bioavailability and tolerability of mebendazole in patients with inoperable hydatid disease.甲苯达唑在无法手术的包虫病患者中的生物利用度和耐受性。
Trans R Soc Trop Med Hyg. 1982;76(4):563-4. doi: 10.1016/0035-9203(82)90163-8.
7
On the pharmacokinetics of domperidone in animals and man. IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration.多潘立酮在动物和人体中的药代动力学。IV. 静脉注射多潘立酮的药代动力学及其在肌肉注射、口服和直肠给药后的人体生物利用度。
Eur J Drug Metab Pharmacokinet. 1981;6(1):61-70. doi: 10.1007/BF03189516.
8
Metabolism and pharmacokinetics of mebendazole in Japanese pufferfish ().日本河豚（）体内的苯并咪唑的代谢和药代动力学。
Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2022 May;39(5):912-924. doi: 10.1080/19440049.2022.2052974. Epub 2022 Apr 20.
9
Mebendazole concentrations in sheep plasma.
Res Vet Sci. 1983 Jan;34(1):37-41.
10
The pharmacokinetics of mebendazole and flubendazole in animals and man.甲苯达唑和氟苯达唑在动物及人体中的药代动力学。
Arch Int Pharmacodyn Ther. 1982 Apr;256(2):180-91.
引用本文的文献
1
Docusate-Based Ionic Liquids of Anthelmintic Benzimidazoles Show Improved Pharmaceutical Processability, Lipid Solubility, and Activity against .基于双羟萘酸的驱虫苯并咪唑离子液体具有改善的药物加工性能、脂溶性和对. 的活性。
ACS Infect Dis. 2021 Sep 10;7(9):2637-2649. doi: 10.1021/acsinfecdis.1c00063. Epub 2021 Sep 1.
2
Progress in the pharmacological treatment of human cystic and alveolar echinococcosis: Compounds and therapeutic targets.人包虫病（囊型和泡型）的药物治疗进展：化合物和治疗靶点。
PLoS Negl Trop Dis. 2018 Apr 20;12(4):e0006422. doi: 10.1371/journal.pntd.0006422. eCollection 2018 Apr.
3
An alternative mebendazole formulation for cystic echinococcosis: the treatment efficacy, pharmacokinetics and safety in mice.用于囊性棘球蚴病的另一种甲苯咪唑制剂：小鼠的治疗效果、药代动力学及安全性
Parasit Vectors. 2014 Dec 10;7:589. doi: 10.1186/s13071-014-0589-0.
4
Repurposing Drugs in Oncology (ReDO)-mebendazole as an anti-cancer agent.肿瘤学中药物再利用（ReDO）——甲苯达唑作为一种抗癌剂
Ecancermedicalscience. 2014 Jul 10;8:443. doi: 10.3332/ecancer.2014.443. eCollection 2014.
5
Safety of a New Chewable Formulation of Mebendazole for Preventive Chemotherapy Interventions to Treat Young Children in Countries with Moderate-to-High Prevalence of Soil Transmitted Helminth Infections.在土壤传播性蠕虫感染中度至高度流行的国家，用一种新的阿苯达唑咀嚼剂型进行预防性化疗干预以治疗幼儿的安全性。
J Trop Med. 2012;2012:590463. doi: 10.1155/2012/590463. Epub 2012 Dec 24.
6
Dinitroaniline activity in Toxoplasma gondii expressing wild-type or mutant alpha-tubulin.表达野生型或突变型α-微管蛋白的弓形虫中二硝基苯胺活性。
Antimicrob Agents Chemother. 2010 Apr;54(4):1453-60. doi: 10.1128/AAC.01150-09. Epub 2010 Feb 9.
7
Is the exclusion of children under 24 months from anthelmintic treatment justifiable?将24个月以下儿童排除在驱虫治疗之外是否合理？
Trans R Soc Trop Med Hyg. 2002 Mar-Apr;96(2):197-9. doi: 10.1016/s0035-9203(02)90303-2.
8
The pharmacokinetics and bioavailability of a tracer dose of [3H]-mebendazole in man.人体中示踪剂量的[3H] - 甲苯咪唑的药代动力学和生物利用度。
Br J Clin Pharmacol. 1985 Jan;19(1):79-86. doi: 10.1111/j.1365-2125.1985.tb02616.x.
9
Pharmacokinetics of albendazole in man.阿苯达唑在人体中的药代动力学。
Eur J Clin Pharmacol. 1986;30(6):705-8. doi: 10.1007/BF00608219.
10
Increased systemic availability of albendazole when taken with a fatty meal.
Eur J Clin Pharmacol. 1988;34(3):315-7. doi: 10.1007/BF00540964.
本文引用的文献
1
Plasma concentrations of mebendazole during treatment of echinococcosis: preliminary results.甲苯达唑治疗包虫病期间的血浆浓度：初步结果
Eur J Clin Pharmacol. 1980 May;17(5):375-8. doi: 10.1007/BF00558451.
2
Chemotherapy of alveolar echinococcosis. Comparison of plasma mebendazole concentrations in animals and man.泡型包虫病的化疗。动物与人血浆中甲苯达唑浓度的比较。
Eur J Clin Pharmacol. 1981;20(6):427-33. doi: 10.1007/BF00542095.
3
Bioavailability and tolerability of mebendazole in patients with inoperable hydatid disease.甲苯达唑在无法手术的包虫病患者中的生物利用度和耐受性。
Trans R Soc Trop Med Hyg. 1982;76(4):563-4. doi: 10.1016/0035-9203(82)90163-8.
4
4-Amino-3-(3'-methoxycarbonyl-2'-thioureido)benzophenone, a prodrug of mebendazole.
Eur J Drug Metab Pharmacokinet. 1983 Oct-Dec;8(4):329-34. doi: 10.1007/BF03188765.
5
Mebendazole in enterobiasis. Radiochemical and pilot clinical study in 1,278 subjects.
JAMA. 1971 Jul 19;217(3):313-6.
6
The pharmacokinetics and bioavailability of a tracer dose of [3H]-mebendazole in man.人体中示踪剂量的[3H] - 甲苯咪唑的药代动力学和生物利用度。
Br J Clin Pharmacol. 1985 Jan;19(1):79-86. doi: 10.1111/j.1365-2125.1985.tb02616.x.
Zotero 插件