吗啡的药物动力学和吗啡皮下注射丸后葡糖苷酸代谢物和皮下注入吗啡。

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引用

Stuart-Harris R,乔尔SP,麦当劳P,克鲁D,斯莱文毫升

吗啡的药物动力学和吗啡皮下注射丸后葡糖苷酸代谢物和皮下注入吗啡。

Br中国新药杂志。2000年3月,49(3):207 - 14所示。

PubMed ID
10718775 (在PubMed
]
文摘

目的:探讨吗啡的药物动力学,morphine-6-glucuronide (M6G)和morphine-3-glucuronide (M3G)在健康的志愿者管理的吗啡皮下注射丸(s.c.b)和皮下输液(南卡罗来纳州我。)/ 4 h,并比较结果与吗啡静脉团(注射)管理。方法:6个健康志愿者每收到5毫克注射硫酸吗啡。,s.c.b.和短s.c.i. / 4 h,在三个不同的场合,在随机顺序,每个隔开至少1周。血浆样本化验,吗啡,M6G M3G。结果:静脉输液吗啡后,浓度的吗啡,M6G和M3G及其药代动力学参数类似我们发现之前,在其他健康志愿者(标准化nmol l - 1时,10毫克剂量一个70公斤的话题)。s.c.b.吗啡后,得到了类似的结果,除了达峰时间值中位数吗啡和M3G输液后明显比吗啡(P < 0.001和P < 0.05),与这一趋势为M6G达峰时间较长(P = 0。09年)。外观半衰期s.c.b.吗啡后M6G和M3G也显著长于后静脉输液吗啡(P = 0.03, P < 0.05,分别)。对数转换AUC值的比较表明,静脉输液和s.c.b.吗啡管理局bioequivalent对吗啡,M6G M3G。与输液吗啡相比,由s.c.i.吗啡与吗啡大大延长值达峰时间值(P < 0.001), M6G (P < 0.001)和M3G (P < 0.05),平均标准化Cmax值明显低于吗啡静脉输液和s.c.b.吗啡后(P < 0.001, M6G P < 0.001, M3G每个比较P < 0.01)。 Comparison of log-transformed AUC values after i.v. and s.c.i. morphine indicated that the two routes were not bioequivalent for morphine (log-transformed AUC ratio 0.78, 90% CI 0.66-0.93), M6G (0.72, 90% CI 0.63-0.82), or M3G (0.65, 90% CI 0.54-0.78). A small stability study indicated no evidence of adsorptive losses from morphine infused over 4 h using the infusion devices from the study. CONCLUSIONS: Although bioequivalence was demonstrated between the s. c.b. and i.v. routes of morphine administration, the bioavailabilities of morphine, M6G and M3G after s.c.i. were significantly lower than after i.v. administration. However, despite this, the study demonstrates that the subcutaneous route is an effective method for the parenteral administration of morphine.

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