FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention provides compositions containing clopidogrel and sulphoalkylester cyclodextrin (SAE-CD), preferentially, sulphobutylester cyclodextrin. The compositions may be liquid, suspension and solid. The compositions are prepared for ingestion, oral or enteral introduction. SAE-CD is used as an agent promoting clopidogrel dissolution and stabilisation in an aqueous media. Higher stability of clopidogrel to hydrolytic, thermal and photolytic degradation is provided. SAE-CD gives better effect as compared with the other cyclodextrin derivatives. The compositions under the invention reduce chiral inversion rate (S) of clopidogrel into (R)-clopidogrel.
EFFECT: compositions give substantial pharmacokinetic, pharmacodynamics and/or therapeutic advantages as compared with a tablet composition introduced orally and not containing SAE-CD.
58 cl, 18 dwg, 14 tbl, 27 ex
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Authors
Dates
2012-12-27—Published
2008-04-26—Filed