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新型关节内注射用类固醇THS-201在棉球肉芽肿和单关节炎模型中的选择性局部抗炎活性

Selective local anti-inflammatory activity of THS-201, a new intra-articular steroid, in cotton pellet granuloma and monoarticular arthritis.

作者信息

Kiniwa M, Miyake H

出版信息

Arch Int Pharmacodyn Ther. 1986 Mar;280(1):153-64.

PMID:3718077
Abstract

A new steroid, THS-201 was administered locally in one of a pair of inflamed sites and its local anti-inflammatory activity was compared with those of triamcinolone acetonide, methylprednisolone acetate and hydrocortisone acetate. In rats, THS-201 (80 micrograms/pellet) completely inhibited the formation of granulation tissue even after 21 days. In antigen-induced bilaterally arthritic rabbits, THS-201 (2 mg/joint) decreased the swelling of the treated knee joint for more than 24 days, but no such effect was seen in the opposite knee joint. The anti-inflammatory activity of the other steroids employed as reference drugs were weaker than that of THS-201. These results indicate that THS-201 is an anti-inflammatory steroids exclusively acting at the site of administration for a long period, and for this reason it might be suitable for intraarticular application in clinical use.

摘要

一种新的类固醇THS - 201被局部应用于一对炎症部位中的一个,并且将其局部抗炎活性与曲安奈德、醋酸甲泼尼龙和醋酸氢化可的松的抗炎活性进行比较。在大鼠中,即使在21天后,THS - 201(80微克/粒)仍能完全抑制肉芽组织的形成。在抗原诱导的双侧关节炎兔中,THS - 201(2毫克/关节)使治疗的膝关节肿胀减轻超过24天,但对侧膝关节未见此效果。用作参比药物的其他类固醇的抗炎活性比THS - 201弱。这些结果表明,THS - 201是一种仅在给药部位长期发挥作用的抗炎类固醇,因此它可能适用于临床关节腔内应用。

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