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COMPOSITIONS PHARMACEUTIQUES À FORTE CHARGE DE MÉDICAMENT
专利权人:
Acryspharm LLC
发明人:
申请号:
EP17919134.1
公开号:
EP3658123A1
申请日:
2017.11.03
申请国别(地区):
EP
年份:
2020
代理人:
摘要:
A pharmaceutical composition of high drug loading comprising an active pharmaceutical ingredient (API) and pharmaceutical acceptable additives, which include glass-solution forming additive and/or eutectic-mixture forming additive, is provided. The composition is dispersed uniformly to form a hybrid solid dispersion consisting of crystalline-suspension, glass-solution and/or eutectic-mixture, where the crystalline API is uniformly distributed in the hybrid solid dispersion and exists in nano/micro particle size range. The amorphous API, when present, is uniformly distributed in the hybrid solid dispersion. The API may exist in different chemical and/or physical forms. The API is present in an amount of from more than about 50% wt/wt to about 90% wt/wt with respect to the total amount of the active pharmaceutical ingredient and the pharmaceutically acceptable glass-solution forming and/or eutectic-mixture forming additives. At least about 50% wt/wt of the API is dispersed in the crystalline-suspension and at least about 5% wt/wt of the API is dispersed in the glass-solution and/or eutectic-mixture. The pharmaceutical composition offers excellent dissolution rate, superior chemical and physical stability, and minimum drug-drug/drug-excipient incompatibility. The composition is beneficial for reducing the overall tablet/capsule size for low water-soluble drugs requiring high drug loading or dosage, including combination drugs.L'invention concerne une composition pharmaceutique à forte charge de médicament comprenant un agent pharmaceutique actif et des additifs pharmaceutiquement acceptables qui comprennent des additifs formant une solution vitreuse et/ou un additif formant un mélange eutectique. La composition pharmaceutique offre un excellent taux de dissolution, une stabilité chimique et physique supérieure et une incompatibilité minimale médicament-médicament/ médicament-excipient.
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中国工程科技知识中心
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