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酮洛芬赖氨酸盐新型泡沫制剂在炎症和痛觉过敏实验模型中的作用

Effects of a new foam formulation of ketoprofen lysine salt in experimental models of inflammation and hyperalgesia.

作者信息

Daffonchio L, Bestetti A, Clavenna G, Fedele G, Ferrari M P, Omini C

机构信息

Pharmacological Department, Dompé Farmaceutici SpA, Milan, Italy.

出版信息

Arzneimittelforschung. 1995 May;45(5):590-4.

PMID:7541996
Abstract

The anti-inflammatory and analgesic profile of a new topical foam formulation of ketoprofen lysine salt (CAS 57469-78-0, Artrosilene Schiuma, KLS-foam) was characterized in comparison with marketed gel formulations containing KLS (KLS-gel) or diclofenac diethylammonium salt (DCF-gel). KLS-foam dose-dependently inhibited oedema formation and hyperalgesia induced by subplantar injection of carrageenan or substance P, being more potent than KLS-gel. At equieffective anti-inflammatory doses, KLS-foam provided a more pronounced analgesic effect than DCF-gel. KLS-foam also markedly inhibited exudate formation and prostaglandin production induced by subcutaneous implantation of carrageenan soaked sponges. In carrageenan induced paw inflammation, KLS-foam provided the same anti-inflammatory effect as orally administered KLS, but induced significantly less gastric damages. Oral administration of KLS resulted in sustained systemic absorption of ketoprofen, whereas after topical application of KLS-foam no appreciable ketoprofen plasma levels were detected. These data support the anti-inflammatory and particularly the analgesic effectiveness of the new foam formulation of KLS, a finding that, together with the high gastric tolerability, further emphasizes the usefulness of KLS-foam in the treatment of localized flogistic diseases and associated pain.

摘要

将酮洛芬赖氨酸盐(CAS 57469-78-0,Artrosilene Schiuma,KLS泡沫)的一种新型局部用泡沫制剂的抗炎和镇痛特性,与含有KLS的市售凝胶制剂(KLS凝胶)或双氯芬酸二乙铵盐(DCF凝胶)进行了比较。KLS泡沫剂量依赖性地抑制了由足底注射角叉菜胶或P物质诱导的水肿形成和痛觉过敏,其效力比KLS凝胶更强。在等效抗炎剂量下,KLS泡沫比DCF凝胶具有更显著的镇痛作用。KLS泡沫还显著抑制了由皮下植入角叉菜胶浸泡海绵诱导的渗出物形成和前列腺素产生。在角叉菜胶诱导的爪部炎症中,KLS泡沫与口服KLS具有相同的抗炎作用,但引起的胃损伤明显更少。口服KLS导致酮洛芬的持续全身吸收,而局部应用KLS泡沫后未检测到明显的酮洛芬血浆水平。这些数据支持了KLS新型泡沫制剂的抗炎尤其是镇痛有效性,这一发现连同高胃耐受性,进一步强调了KLS泡沫在治疗局部炎症性疾病及相关疼痛方面的有用性。

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