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在健康志愿者中通过联合使用水杨酸钠或辛酸钠对头孢西丁进行速率控制的直肠吸收增强作用。

Rate-controlled rectal absorption enhancement of cefoxitin by co-administration of sodium salicylate or sodium octanoate in healthy volunteers.

作者信息

Van Hoogdalem E J, Wackwitz A T, De Boer A G, Cohen A F, Breimer D D

机构信息

Division of Pharmacology, Sylvius Laboratories, State University of Leiden, The Netherlands.

出版信息

Br J Clin Pharmacol. 1989 Jan;27(1):75-81. doi: 10.1111/j.1365-2125.1989.tb05337.x.

DOI:10.1111/j.1365-2125.1989.tb05337.x
PMID:2706190
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1379707/
Abstract
  1. The effects of sodium octanoate and sodium salicylate on the rectal absorption of cefoxitin were investigated in healthy volunteers. Drug solutions were given either as a bolus or as a zero-order infusion. 2. On rectal infusion sodium octanoate and sodium salicylate both enhanced mean cefoxitin bioavailability (+/- s.d.) from 5.0 +/- 1.2% to 9.1 +/- 1.3% and 9.2 +/- 1.5%, respectively. After rectal bolus delivery octanoate increased the mean cefoxitin bioavailability from 7 +/- 3% to 17 +/- 3%, whereas bolus salicylate did not produce a statistically significant effect. All formulations were well tolerated by the volunteers. 3. It is concluded that both octanoate and salicylate are capable of enhancing rectal cefoxitin absorption in man; rate of delivery seems to be an important factor.
摘要
  1. 在健康志愿者中研究了辛酸钠和水杨酸钠对头孢西丁直肠吸收的影响。药物溶液以推注或零级输注的方式给药。2. 直肠输注时,辛酸钠和水杨酸钠均提高了头孢西丁的平均生物利用度(±标准差),分别从5.0±1.2%提高到9.1±1.3%和9.2±1.5%。直肠推注给药后,辛酸盐使头孢西丁的平均生物利用度从7±3%提高到17±3%,而推注水杨酸盐未产生统计学上的显著影响。所有制剂志愿者均耐受性良好。3. 得出的结论是,辛酸盐和水杨酸盐均能够提高人体直肠中头孢西丁的吸收;给药速率似乎是一个重要因素。

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引用本文的文献

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Pharmacokinetics of rectal drug administration, Part II. Clinical applications of peripherally acting drugs, and conclusions.直肠给药的药代动力学,第二部分。外周作用药物的临床应用及结论。
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本文引用的文献

1
Effects of surfactants on the GI absorption of beta-lactam antibiotics in rats.表面活性剂对大鼠胃肠道中β-内酰胺类抗生素吸收的影响。
J Pharm Sci. 1983 Jun;72(6):651-4. doi: 10.1002/jps.2600720615.
2
Drug biotransformation interactions in man. I. Mutual inhibition in glucuronide formation of salicylic acid and salicylamide in man.人体中的药物生物转化相互作用。I. 人体中水杨酸和水杨酰胺葡萄糖醛酸苷形成的相互抑制作用。
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Studies on the promoting effects of carboxylic acid derivatives on the rectal absorption of beta-lactam antibiotics in rats.羧酸衍生物对大鼠体内β-内酰胺类抗生素直肠吸收促进作用的研究。
Chem Pharm Bull (Tokyo). 1985 Jan;33(1):282-91. doi: 10.1248/cpb.33.282.
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Enamine formation of various amino acids with ethyl acetoacetate in aqueous solution in relation to colonic absorption of cefmetazole.各种氨基酸与乙酰乙酸乙酯在水溶液中形成烯胺与头孢美唑结肠吸收的关系。
Chem Pharm Bull (Tokyo). 1985 Jul;33(7):3027-30. doi: 10.1248/cpb.33.3027.
5
Improvement of bioavailability of poorly absorbed drugs. II. Effect of medium chain glyceride base on the intestinal absorption of cefmetazole sodium in rats and dogs.难吸收药物生物利用度的改善。II. 中链甘油酯基质对大鼠和犬体内头孢美唑钠肠道吸收的影响。
J Pharmacobiodyn. 1985 Apr;8(4):286-95. doi: 10.1248/bpb1978.8.286.
6
Use of adjuvants for enhancement of rectal absorption of cefoxitin in humans.佐剂用于增强头孢西丁在人体直肠吸收的研究。
Antimicrob Agents Chemother. 1985 Aug;28(2):211-5. doi: 10.1128/AAC.28.2.211.
7
Enhanced small intestinal absorption of beta-lactam antibiotics in rats in the presence of monodesmosides isolated from pericarps of Sapindus mukurossi (Enmei-hi).在存在从无患子果皮(菩提子)中分离出的单糖苷的情况下,大鼠小肠对β-内酰胺类抗生素的吸收增强。
J Pharmacobiodyn. 1986 Feb;9(2):211-7. doi: 10.1248/bpb1978.9.211.
8
Enhancement of the rectal absorption of sodium ampicillin by N-acylamino acids in rats.N-酰基氨基酸对大鼠氨苄西林钠直肠吸收的促进作用。
J Pharm Sci. 1987 Jul;76(7):508-12. doi: 10.1002/jps.2600760703.
9
Absorption enhancement of rectally infused cefoxitin sodium by medium-chain fatty acids in conscious rats: concentration-effect relationship.中链脂肪酸对清醒大鼠直肠灌注头孢西丁钠吸收的增强作用:浓度-效应关系
Pharm Res. 1988 Jul;5(7):453-6. doi: 10.1023/a:1015948720256.
10
Rate-controlled absorption enhancement of rectally administered cefazolin in rats by a glyceride mixture (MGK).甘油酯混合物(MGK)对大鼠直肠给药头孢唑林的速率控制吸收增强作用。
J Pharm Pharmacol. 1988 May;40(5):329-32. doi: 10.1111/j.2042-7158.1988.tb05261.x.