CAS: 1225-55-4; Protriptyline Hydrochloride

📜普罗替林置于盐酸体系中,用 乙醚,二氯甲烷 用作溶剂,化学反应生成普罗替林盐酸盐
参考文献:Process For Preparation Of 5H-Dibenzo[a,D] Cycloheptene Derivatives
标题:Process For Preparation Of 5H-Dibenzo[a,D] Cycloheptene Derivatives
摘要:从式(1)的5-二氢苯并环庚三烯与氯丙醇在四氢呋喃中过量正丁基锂存在下偶联的制备普曲林盐酸盐的方法,随后制备式(3)的甲磺酸酯衍生物,最后通过在甲醇中与甲胺溶液反应,进行甲磺酸酯基的亲核置换,得到式(4)的普曲林游离碱.此外,该方法还揭示了盐酸盐的形成和纯化过程,以获得纯度高于0.1%(重量百分比)的纯制药级普曲林盐酸盐.

专利信息

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-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-2013303495-A1
优先权日:2009-12-31
标题:Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES 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-2009304615-A1
优先权日:2007-11-14
标 题 :Tricyclic compounds as melanogenesis modifiers and uses thereof
发明人：ORLOW SETH J; KOMATSU LI NI
权利人:ORLOW SETH J; KOMATSU LI NI
摘要:A method of identification of tricyclic compounds (formula I) that control melanin synthesis (melanogenesis), and the use of such compounds and compositions thereof to modify (e.g., inhibit) melanin production are disclosed. n n n n n n n n n n The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to aberrant melanogenesis activity including by way of non-limiting example, hyperpigmentation and others.

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.