フルルビプロフェン水性製剤の局所刺激性に及ぼすシクロデキストリンの緩和効果

概要

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The inclusion complexations of flurbiprofen (FP) with three cyclodextrins (α-, β-, and γ-CyD) were assessed by solubility method, optical rotatory dispersion (ORD), ultraviolet spectra (UV) and circular dichroism (CD) in aqueous solution. FP was included with β-CyD or γ-CyD in the molecular ratio of 1 : 1. Their stability constants and mutual effects were in the order of β-, >γ-, >α-CyD. To improve the local irritation induced by intramuscular injection or eye dropping of FP, CyD complexation was utilized. CyDs were found to protect the erythrocytes from the hemolysis and shape changes induced by FP in vitro. Their protective effects on whole blood of human and rabbit increased in the order of β-, >γ-CyD. The irritative effects of FP or its CyD complexes on the M. vastus lateralis of rabbits were studied on the gross examination. The irritation of β-CyD complex was found to be the mildest in all other CyD complexes. The effects of FP aqueous ophthalmic solution was studied for the reduction of local irritation and the inhibition of the increase of aqueous humor protein induced by the paracentesis to rabbit eyes. The complexation of FP with β-CyD was found to be the mildest in all FP ophthalmic solution studied on the eye irritation. Furthermore, the aqueous ophthalmic solution of 0.1% FP containing β-CyD indicated the inhibition about 75% of increasing protein in the intraocular surgery.
公益社団法人日本薬学会の論文
1984-10-25