Cyclodextrin inclusion cpds. of phendilin or its hydrochloride

Prodn. of inclusion cpds. of N-(1-phenethyl)-3,3-diphenylpropylamine (I) or its hydrochloride with cyclodextrin (II) comprises treating (I) or its hydro;chloride, at 4-60 deg.C with stirring, with 1 mmole (calculated as base) or 1-3 mmole (calculated as hydrochloride) of (II). Reaction is carried ou...

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Bibliographische Detailangaben
Hauptverfasser: SZOKE NATA, STADLER AGNES, VIKMON MARIA, KORBONITS DESZO, VIRAG SANDOR, SZEJTLI JOSZEF, KISS PAL, KIRALY NATA, TURCSAN ISTVAN
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Sprache:eng ; ita
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Zusammenfassung:Prodn. of inclusion cpds. of N-(1-phenethyl)-3,3-diphenylpropylamine (I) or its hydrochloride with cyclodextrin (II) comprises treating (I) or its hydro;chloride, at 4-60 deg.C with stirring, with 1 mmole (calculated as base) or 1-3 mmole (calculated as hydrochloride) of (II). Reaction is carried out in aq. and/or ethanolic medium and opt. the complex formed is treated with HCl to convert it to the hydrochloride complex. Inclusion cpds. of (I) with alpha-, beta- and gamma-(II), and of (I) hydrochloride with beta-(II) are new. (I) is a known coronary dilating (calcium antagonising) agent but both it and its hydrochloride are (almost) insoluble in water. The (II)-inclusion cpds. are more quickly and completely dissolved so that the degree of resorption is improved. The LD50 (mica) for the (I) free base inclusion cpd. is 157 mg per kg intraperitonally and 625 mg per kg orally.