PHARMACEUTICAL COMPOSITIONS AND METHODS

• Main Authors: JOEL FRANK, GILIYAR CHANDRASHEKAR, SRINIVASAN VENKATESHWARAN, NACHIAPPAN CHIDAMBARAM, MAHESH V PATEL, SATISH KUMAR NACHAEGARI
• Format: Patent
• Language: English; Japanese
• Published: 03.12.2020
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide compositions and dosage forms enabling high drug loading while maintaining excellent oral bioavailability for highly lipophilic drugs.SOLUTION: Disclosed is a composition which can reduce the pill burden of a hydrophobic drug such as testosterone tridecanoates, and can be formulated at advantageous drug loads (e.g., greater than 23%) while providing suitable bioavailability (e.g., capable of treating a hypogonadal male with less than 10 unit dosage forms per day) that allows the reduction in pill burden and accordingly improved patient adherence or compliance. Additionally, the composition (e.g., dosage form) has a release profile that is suitable for providing bioavailable API and stable over time (e.g., under storage conditions).SELECTED DRAWING: Figure 1 【課題】優れた経口生物学的利用性を維持しながら高親油性薬のための高い薬物負荷（ｄｒｕｇ ｌｏａｄｉｎｇ）を可能にする、組成物および投与剤形を提供する。【解決手段】テストステロントリデカノアートのような疎水性薬のピルバーデンを減少させることができ、ピルバーデンの減少、つまり患者アドヒアランスまたはコンプライアンスの改善を可能にする適切な生物学的利用性をもたらしながら（例えば、１日あたり１０未満の単位投与剤形で性腺機能低下男性を処置し得る）、有利な薬物負荷（例えば、２３％を超える）で配合され得る。加えて、該組成物（例えば、投与剤形）は、生物学的利用性のあるＡＰＩを提供するのに適し、経時的に安定している（例えば、保存条件下）、放出プロファイルを有する。【選択図】図１