Stereoselective behavior of a novel biodegradable racemic ketoprofen injectable implant in rats | Zendy

Wang ShengHao | Zendy; Yin LiNa | Zendy; Liang ZeHua | Zendy; Lu SiJie | Zendy; Zeng Su | Zendy

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Stereoselective behavior of a novel biodegradable racemic ketoprofen injectable implant in rats

Author(s) -

Wang ShengHao,

Yin LiNa,

Liang ZeHua,

Lu SiJie,

Zeng Su

Publication year - 2007

Publication title -

chirality

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.43

H-Index - 77

eISSN - 1520-636X

pISSN - 0899-0042

DOI - 10.1002/chir.20453

Subject(s) - chemistry , enantiomer , stereoselectivity , ketoprofen , in vivo , implant , derivatization , bioavailability , racemic mixture , high performance liquid chromatography , stereochemistry , pharmacology , chromatography , organic chemistry , catalysis , surgery , medicine , microbiology and biotechnology , biology

The stereoselectivity of release of ketoprofen (KET) enantiomers from a biodegradable injectable implant containing racemic KET ( rac ‐KET) was investigated in vivo. A pre‐column chiral derivatization RP‐HPLC method was employed to assay diastereoisomeric derivatives of R ‐ and S ‐KET. The rac ‐KET injectable implant, once injected subcutaneously in rats, produced long‐lasting plasma levels of S ‐KET, which were always greater than those of R ‐KET. The difference in enantiomer concentration was to be related to stereoselective release, due to stereoselective interaction between D , L ‐PLG in the implant and KET enantiomers, as well as the chiral inversion of KET in vivo. The rac ‐KET injectable implant provided the sustained release of S ‐KET with effective plasma levels maintained for about 8 wk after a single injection. Chirality 2007. © 2007 Wiley‐Liss, Inc.

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