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抗酸剂对合成前列腺素(8R,11R,12S,15R,5Z,13E)-15-(乙酰氧基)-11,16,16-三甲基-9-氧代前列腺-5,13-二烯-1-酸在犬体内胃抗分泌活性的影响。

Influence of antacids on the gastric antisecretory activity of the synthetic prostanoid (8R,11R,12S,15R,5Z,13E)-15-(acetyloxy)- 11,16,16-trimethyl-9-oxoprosta-5,13-dien-1-oic acid in dogs.

作者信息

Gaginella T S, Bertko R J

出版信息

J Pharm Sci. 1985 Dec;74(12):1334-6. doi: 10.1002/jps.2600741217.

Abstract

Liquid antacids that contain aluminum-magnesium hydroxides reduce the absorption of various therapeutic agents. To assess the potential for such an interaction with the synthetic anti-ulcer prostanoid (8R,11R,12S,15R,5Z,13E)-15-(acetyloxy)-11, 16,16-trimethyl-9-oxoprosta-5,13-dien-1-oic acid (1; Ro 22-6923), we studied the effect of Mylanta and DiGel liquid on the gastric antisecretory activity of this drug in dogs. Dogs were prepared with a modified Pavlov (innervated) pouch. Compound 1 was administered alone or with liquid antacid into the main stomach while acid secretion into the pouch was measured. Mylanta (30 mL) and DiGel (35 mL) failed to significantly reduce the ability of 1 (0.5 mg/kg, orally) to inhibit histamine (25 micrograms/kg/h)-stimulated secretion. Neither the onset nor the duration of action of 1 was affected by either antacid. The total acid output over the 4 h after administration of 1 was not significantly affected by the antacids. The results suggest that Mylanta and DiGel, or antacids of a composition similar to that of these products are not likely to interfere with the antisecretory activity of 1 in humans.

摘要

含有氢氧化铝镁的液体抗酸剂会降低多种治疗药物的吸收。为了评估与合成抗溃疡前列腺素(8R,11R,12S,15R,5Z,13E)-15-(乙酰氧基)-11,16,16-三甲基-9-氧代前列腺-5,13-二烯-1-酸(1;Ro 22-6923)发生这种相互作用的可能性,我们研究了胃得乐和迪吉尔液体对该药物在犬类中的胃抗分泌活性的影响。犬类通过改良的巴甫洛夫(有神经支配)胃小囊进行制备。化合物1单独给药或与液体抗酸剂一起给药至主胃中,同时测量进入胃小囊的胃酸分泌。胃得乐(30 mL)和迪吉尔(35 mL)未能显著降低1(0.5 mg/kg,口服)抑制组胺(25微克/千克/小时)刺激分泌的能力。两种抗酸剂均未影响1的起效时间和作用持续时间。给药后4小时内的总酸分泌量未受到抗酸剂的显著影响。结果表明,胃得乐和迪吉尔或与这些产品成分相似的抗酸剂不太可能干扰1在人体中的抗分泌活性。

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