吗啡在健康志愿者中静脉注射、口服和颊部给药后的生物利用度和药代动力学。
The bioavailability and pharmacokinetics of morphine after intravenous, oral and buccal administration in healthy volunteers.
作者信息
Hoskin P J, Hanks G W, Aherne G W, Chapman D, Littleton P, Filshie J
机构信息
Continuing Care Unit, Royal Marsden Hospital, Sutton, Surrey.
出版信息
Br J Clin Pharmacol. 1989 Apr;27(4):499-505. doi: 10.1111/j.1365-2125.1989.tb05399.x.
Abstract
- The absolute bioavailability of morphine from oral aqueous solution, a controlled release oral tablet (MST-Continus) and a controlled release buccal tablet has been investigated in six healthy volunteers. 2. Analysis of plasma samples for morphine and its active metabolite morphine-6-glucuronide (M6G) was by means of a differential radioimmunoassay technique. Absolute bioavailability for morphine was estimated to be 23.9% after oral solution, 22.4% after MST-Continus and 18.7% after the buccal tablet. Maximum plasma morphine concentrations were seen at 45 min (oral solution), 2.5 h (MST) and 6 h (buccal). 3. There was no difference in the amount of M6G appearing in plasma after intravenous, oral or buccal administration but the mean ratio of AUCs for M6G: morphine in plasma after intravenous morphine was 2 : 1 compared with 11 : 1 after oral and buccal morphine.
摘要
- 在六名健康志愿者中研究了口服水溶液、控释口服片剂（美施康定）和控释颊含片吗啡的绝对生物利用度。2. 通过差分放射免疫分析技术分析血浆样本中的吗啡及其活性代谢物吗啡-6-葡萄糖醛酸苷（M6G）。吗啡的绝对生物利用度估计为：口服溶液后为23.9%，美施康定后为22.4%，颊含片后为18.7%。最大血浆吗啡浓度在45分钟（口服溶液）、2.5小时（美施康定）和6小时（颊含片）时出现。3. 静脉注射、口服或颊内给药后血浆中出现的M6G量没有差异，但静脉注射吗啡后血浆中M6G与吗啡的AUC平均比值为2:1，而口服和颊内给予吗啡后为11:1。
相似文献
1
The bioavailability and pharmacokinetics of morphine after intravenous, oral and buccal administration in healthy volunteers.吗啡在健康志愿者中静脉注射、口服和颊部给药后的生物利用度和药代动力学。
Br J Clin Pharmacol. 1989 Apr;27(4):499-505. doi: 10.1111/j.1365-2125.1989.tb05399.x.
2
Bioavailability of morphine after administration of a new bioadhesive buccal tablet.新型生物黏附性口腔片给药后吗啡的生物利用度
Biopharm Drug Dispos. 1998 Sep;19(6):401-5. doi: 10.1002/(sici)1099-081x(199809)19:6<401::aid-bdd116>3.0.co;2-u.
3
Relative bioavailability of controlled release morphine tablets (MST continus) in cancer patients.控释吗啡片（美施康定）在癌症患者中的相对生物利用度。
Br J Anaesth. 1988 Nov;61(5):569-74. doi: 10.1093/bja/61.5.569.
4
Morphine pharmacokinetics and metabolism in humans. Enterohepatic cycling and relative contribution of metabolites to active opioid concentrations.吗啡在人体内的药代动力学与代谢。肠肝循环及代谢产物对活性阿片类药物浓度的相对贡献。
Clin Pharmacokinet. 1993 Apr;24(4):344-54. doi: 10.2165/00003088-199324040-00007.
5
Pharmacokinetic modeling of M6G formation after oral administration of morphine in healthy volunteers.健康志愿者口服吗啡后M6G形成的药代动力学建模。
Anesthesiology. 1999 Apr;90(4):1026-38. doi: 10.1097/00000542-199904000-00016.
6
Plasma concentrations of morphine, morphine-3-glucuronide, and morphine-6-glucuronide after intravenous and oral administration to healthy volunteers: relationship to nonanalgesic actions.健康志愿者静脉注射和口服吗啡后血浆中吗啡、吗啡-3-葡萄糖醛酸苷和吗啡-6-葡萄糖醛酸苷的浓度：与非镇痛作用的关系。
Ther Drug Monit. 1995 Jun;17(3):287-301. doi: 10.1097/00007691-199506000-00013.
7
Disposition of morphine and its glucuronide metabolites after oral and rectal administration: evidence of route specificity.
Clin Pharmacol Ther. 1993 Sep;54(3):286-92. doi: 10.1038/clpt.1993.149.
8
Systemic availability of oral slow-release morphine in man.
Ann Clin Biochem. 1985 May;22 ( Pt 3):226-31. doi: 10.1177/000456328502200303.
9
Morphine and metabolite behavior after different routes of morphine administration: demonstration of the importance of the active metabolite morphine-6-glucuronide.
Clin Pharmacol Ther. 1990 Jan;47(1):12-9. doi: 10.1038/clpt.1990.2.
10
Age and the pharmacokinetics of morphine.年龄与吗啡的药代动力学
Age Ageing. 1989 Jul;18(4):258-62. doi: 10.1093/ageing/18.4.258.
引用本文的文献
1
Scoping Review of Paediatric Population Pharmacokinetic Models of Morphine.吗啡儿科群体药代动力学模型的范围综述
Clin Pharmacokinet. 2025 May 1. doi: 10.1007/s40262-025-01477-5.
2
Evaluation of the Drug-Drug Interaction Potential of Cannabidiol Against UGT2B7-Mediated Morphine Metabolism Using Physiologically Based Pharmacokinetic Modeling.使用基于生理的药代动力学模型评估大麻二酚对UGT2B7介导的吗啡代谢的药物-药物相互作用潜力。
Pharmaceutics. 2024 Dec 16;16(12):1599. doi: 10.3390/pharmaceutics16121599.
3
Opioid-Based Haptens: Development of Immunotherapy.基于阿片类药物的半抗原：免疫疗法的发展。
Int J Mol Sci. 2024 Jul 16;25(14):7781. doi: 10.3390/ijms25147781.
4
Physiologically Based Pharmacokinetic (PBPK) Model Predictions of Disease Mediated Changes in Drug Disposition in Patients with Nonalcoholic Fatty Liver Disease (NAFLD).基于生理学的药代动力学（PBPK）模型预测非酒精性脂肪性肝病（NAFLD）患者疾病导致药物处置改变。
Pharm Res. 2024 Mar;41(3):441-462. doi: 10.1007/s11095-024-03664-8. Epub 2024 Feb 13.
5
Anterior cingulate cortex and its projections to the ventral tegmental area regulate opioid withdrawal, the formation of opioid context associations and context-induced drug seeking.前扣带回皮质及其向腹侧被盖区的投射调节阿片类药物戒断、阿片类药物情境关联的形成以及情境诱导的药物寻求。
Front Neurosci. 2022 Aug 5;16:972658. doi: 10.3389/fnins.2022.972658. eCollection 2022.
6
Establishment to measure oxycodone in plasma with liquid chromatography-tandem mass spectrometry.建立液相色谱-串联质谱法测定血浆中羟考酮的方法。
Neuropsychopharmacol Rep. 2022 Sep;42(3):299-305. doi: 10.1002/npr2.12268. Epub 2022 Jun 11.
7
Clinical pharmacology and dosing regimen optimization of neonatal opioid withdrawal syndrome treatments.新生儿阿片类戒断综合征治疗的临床药理学和剂量方案优化。
Clin Transl Sci. 2021 Jul;14(4):1231-1249. doi: 10.1111/cts.12994. Epub 2021 May 1.
8
Transmucosal drug administration as an alternative route in palliative and end-of-life care during the COVID-19 pandemic.经黏膜给药剂型作为 COVID-19 大流行期间姑息治疗和临终关怀的一种替代途径。
Adv Drug Deliv Rev. 2020;160:234-243. doi: 10.1016/j.addr.2020.10.018. Epub 2020 Nov 1.
9
Simultaneous Detection of Morphine and Codeine in the Presence of Ascorbic Acid and Uric Acid and in Human Plasma at Nafion Single-Walled Carbon Nanotube Thin-Film Electrode.在Nafion单壁碳纳米管薄膜电极上同时检测抗坏血酸、尿酸存在下以及人血浆中的吗啡和可待因。
ACS Omega. 2019 Oct 16;4(18):17726-17734. doi: 10.1021/acsomega.9b02147. eCollection 2019 Oct 29.
10
Could Postnatal Age-Related Uridine Diphosphate Glucuronic Acid Be a Rate-Limiting Factor in the Metabolism of Morphine During the First Week of Life?生后年龄相关尿苷二磷酸葡萄糖醛酸是否为生命最初一周吗啡代谢的限速因素？
CPT Pharmacometrics Syst Pharmacol. 2019 Jul;8(7):469-477. doi: 10.1002/psp4.12407. Epub 2019 May 10.
本文引用的文献
1
Morphine kinetics in cancer patients.
Clin Pharmacol Ther. 1981 Nov;30(5):629-35. doi: 10.1038/clpt.1981.214.
2
Controlled-release morphine tablets. A double-blind trial in dental surgery patients.
Br J Anaesth. 1981 Dec;53(12):1259-64. doi: 10.1093/bja/53.12.1259.
3
Age-related morphine kinetics.与年龄相关的吗啡动力学。
Clin Pharmacol Ther. 1983 Sep;34(3):364-8. doi: 10.1038/clpt.1983.180.
4
Morphine metabolism in cancer patients on increasing oral doses--no evidence for autoinduction or dose-dependence.癌症患者口服剂量增加时的吗啡代谢——无自身诱导或剂量依赖性的证据
Br J Clin Pharmacol. 1983 Jul;16(1):85-93. doi: 10.1111/j.1365-2125.1983.tb02148.x.
5
Pharmacokinetics and analgesic effect of slow-release oral morphine sulphate in volunteers.口服硫酸吗啡缓释片在志愿者体内的药代动力学及镇痛效果
Br J Anaesth. 1984 Aug;56(8):821-7. doi: 10.1093/bja/56.8.821.
6
STRIPE: an interactive computer program for the analysis of drug pharmacokinetics.STRIPE：一款用于药物药代动力学分析的交互式计算机程序。
J Pharmacol Methods. 1983 May;9(3):193-9. doi: 10.1016/0160-5402(83)90038-4.
7
Oral morphine in cancer patients: in vivo kinetics and in vitro hepatic glucuronidation.癌症患者口服吗啡：体内动力学与体外肝脏葡萄糖醛酸化
Br J Clin Pharmacol. 1985 Apr;19(4):495-501. doi: 10.1111/j.1365-2125.1985.tb02675.x.
8
Steady-state pharmacokinetics of controlled release oral morphine sulphate in healthy subjects.
Clin Pharmacokinet. 1986 Nov-Dec;11(6):505-10. doi: 10.2165/00003088-198611060-00006.
9
Potential pulmonary uptake and clearance of morphine in postoperative patients.术后患者吗啡的潜在肺摄取和清除情况。
Eur J Clin Pharmacol. 1986;30(5):567-74. doi: 10.1007/BF00542416.
10
Analysis of morphine and its major metabolites by differential radioimmunoassay.
Ann Clin Biochem. 1987 Mar;24 ( Pt 2):153-60. doi: 10.1177/000456328702400205.
Zotero 插件