Differential effect of benexate hydrochloride betadex on prostaglandin levels in stomach and inflammatory site in rats

Differential effect of benexate hydrochloride betadex on prostaglandin levels in stomach and inflammatory site in rats
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DOI:
10.1254/jjp.72.183
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发表时间:
1996-10-01
期刊:
JAPANESE JOURNAL OF PHARMACOLOGY
影响因子:
--
通讯作者:
Mizui, T
Mizui, T
中科院分区:
其他
文献类型:
--
作者:
Hori, Y;Odaguchi, K;Mizui, T

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我们比较了抗溃疡药物盐酸苯海索(BHB)对未治疗和消炎痛治疗的大鼠胃组织和炎性渗出物中前列腺素(PG)水平的影响。BHB(100、300和1000 mg/kg,P.O.)对消炎痛(30 mg/kg,P.O.)所致的胃粘膜损伤有剂量依赖性抑制作用。胃壁前列腺素(PGE(2)和6-keto-PGF(1α))在消炎痛治疗后0.5~6小时持续下降。BHB(300和1000 mg/kg)在给药后1小时和6小时可剂量依赖性地恢复消炎痛引起的胃PGs下降。但不能拮抗消炎痛引起的角叉菜胶性胸膜炎胸腔渗出液中PG含量的降低,也不影响消炎痛的抗炎作用。BHB(100~1000 mg/kg)单独给药后6h,胃PGE(2)升高61%~113%,胸腔积液PGE(2)降低9%~71%。这些结果提示,BHB持续升高胃PGE(2)对消炎痛所致的胃粘膜损伤具有保护作用,BHB在不影响其抗炎作用的前提下,是一种较好的非甾体抗炎药物。
We compared the effects of an anti-ulcer agent, benexate hydrochloride betadex (BHB), on prostaglandin (PG) levels in gastric tissue and inflammatory exudate in untreated and indomethacin-treated rats. BHB (100, 300 and 1000 mg/kg, p.o.) showed dose-dependent inhibition of gastric mucosal lesions induced by indomethacin (30 mg/kg, p.o.). Sustained decrease of PGs (PGE(2) and 6-keto-PGF(1 alpha)) in the gastric wall was observed from 0.5 to 6 hr after indomethacin treatment. BHB (300 and 1000 mg/kg) dose-dependently led to recovery of the indomethacin-induced decrease of gastric PGs at 1 and 6 hr after dosing. It did not antagonize the indomethacin-induced decrease of PG levels in the pleural exudate of carrageenin pleurisy nor did it affect the anti-inflammatory effects of indomethacin. BHB (100 to 1000 mg/kg) alone increased gastric PGE(2) by 61% to 113%, while it decreased PGE(2) levels in the pleural exudate by 9% to 71% at 6 hr after dosing. These results suggest that sustained increase of gastric PGE(2) by BHB could be responsible for protection against indomethacin-induced gastric mucosal lesions and that BHB is a suitable anti-ulcer agent for NSAIDs without compromising their anti-inflammatory effects.