专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-6110906-A 优先权日:1989-03-10 标题:Androgen derivatives for use in the inhibition of sex steroid activity 发明人:LABRIE FERNAND; MERAND YVES 权利人:ENDORECHERCHE INC 摘要:Methods for treating sex steroid-dependent diseases by inhibiting sex steroid activity include administration of novel compounds which include an androgenic nucleus substituted at a ring carbon with at least one substituent specified herein. Such compounds may function by inhibiting sex steroid synthesis (both estrogen and androgen synthesis) and/or by antagonistically blocking androgen receptors.
专利号:US-11617758-B2 优先权日:2009-12-31 标 题 :Emulsion formulations 发明人:DHINGRA OM; BERNSTEIN JAMES S 权利人:MARIUS PHARMACEUTICALS LLC 摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-11498061-B2 优先权日:2018-11-14 标题 :Preparation method of mesoporous Fe—Cu-SSZ-13 molecular sieve 发明人:YUE YUANYUAN; LIU BEN; Lv Nangui; BAO XIAOJUN; LIU JIE; WANG TINHAI; YUAN PEI; ZHU HAIBO; BAI ZHENGSHUAI; CUI QINGYAN 权利人:UNIV FU ZHOU 摘要:A method of preparing a mesoporous Fe—Cu—SSZ-13 molecular sieve includes activating an aluminum source, a silicon source, an iron source and a copper source respectively; mixing the activated minerals with sodium hydroxide, water and a seed crystal at 25-90° C., while controlling feeding amounts of respective raw materials so that molar ratios of respective materials in a synthesis system are as follows: SiO 2 /Al 2 O 3 =10-100, SiO 2 /Fe 2 O 3 =30-3000, SiO 2 /CuO=1-100, Na 2 O/SiO 2 =0.1-0.5, H 2 O/SiO 2 =10-50, template/SiO 2 =0.01-0.5; adding an acid source to adjust pH of the system for first aging; and adding the acid source again to adjust the pH of the system for second aging to obtain aged gel; pouring an aged mixture into a kettle; cooling a crystallized product and filtering to remove a liquor; washing a filter cake; drying to obtain a solid; performing ion exchange; and filtering, washing and drying the solid to obtain powder; and placing the powder in a muffle furnace.
专利号:US-2025281509-A1 优先权日:2021-04-26 标 题 :Sequential hormone therapy to improve survival and enhance response to immune therapy in men with prostate cancer 发明人:DENMEADE SAMUEL R; ISAACS JOHN T; ANTONARAKIS EMMANUEL S; KACHHAP SUSHANT; MARKOWSKI MARK CHRISTOPHER 权利人:UNIV JOHNS HOPKINS 摘要:Disclosed are methods for treating men with castrate resistant prostate cancer with a sufficient dose of testosterone to achieve supraphysiologic serum levels of testosterone in sequence with androgen ablative treatment or androgen synthesis inhibitors for one or more cycles until evidence of radiographic progression, at which point the subject will receive immune checkpoint blockade therapy.