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1. 发明授权

US06951655B2 Pro-micelle pharmaceutical compositions 失效
标题翻译：原胶束药物组合物
公开(公告)号：US06951655B2
公开(公告)日：2005-10-04
申请号：US09974942
申请日：2001-10-11
申请人： Young W. Cho , Kwang-Ho Lee
发明人： Young W. Cho , Kwang-Ho Lee
IPC分类号： A61K9/107 , A61K9/00 , A61K9/127 , A61K9/14 , A61K9/48 , A61K9/50 , A61K9/64 , A61K38/28 , A61K47/14 , A61K47/24 , A61K47/42 , A61K37/18
CPC分类号： A61K9/5073 , A61K9/0095 , A61K9/1075 , A61K9/127 , A61K9/5015 , A61K9/5042 , A61K9/5057 , A61K38/28
摘要： The present invention provides pro-micelle compositions comprising a pharmaceutically active agent encapsulated with a membrane of esterified C12-C18 fatty acids. In the mammalian intestine, exposure to C12-C18 fatty acids results in conversion of the pro-micelle to a stable micelle that effectively delivers the pharmaceutically active agent to the systemic circulation. The present invention further provides methods of making and using such compositions.
摘要翻译：本发明提供包含用酯化的C 12 -C 18脂肪酸膜包封的药物活性剂的原胶束组合物。在哺乳动物肠中，暴露于C 12 -C 18脂肪酸导致原胶束转化为稳定的胶束，其有效地将药物活性剂递送到系统性循环。本发明还提供制备和使用这些组合物的方法。

2. 发明授权

US5656289A Pharmaceutical formulations that have a biologically active hydrophilic phase and a chylomicra-containing hydrophobic phase 失效
标题翻译：具有生物活性亲水相和含乳木糖含量的疏水相的药物制剂
公开(公告)号：US5656289A
公开(公告)日：1997-08-12
申请号：US207236
申请日：1994-02-16
申请人： Young W. Cho , Michael John Flynn
发明人： Young W. Cho , Michael John Flynn
IPC分类号： A61K9/107 , A61K9/127 , A61K9/16 , A61K9/50 , A61K35/16 , A61K38/00 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/36 , A61K38/49 , B05C5/02 , A61K9/48
CPC分类号： A61K38/28 , A61K38/215 , A61K38/23 , A61K38/27 , A61K38/36 , A61K38/49 , A61K9/1075 , A61K9/1275 , A61K9/1676 , A61K9/5078 , Y10S514/866 , Y10S514/937 , Y10S514/938 , Y10S514/941 , Y10S514/943
摘要： Orally or rectally administrable formulations of biologically active material comprise a water-in-oil microemulsion, wherein the hydrophilic phase of the microemulsion comprises the biologically active material and the hydrophobic phase comprises chylomicra or material capable of forming chylomicra in the intestinal mucosa after administration. The biologically active material may be any of a wide range of substances including insulin, calcitonin and somatotrophin or growth hormone. Formulations of the invention are particularly suitable for the oral administration of insulin in the treatment of diabetes.
摘要翻译：口服或直肠给药的生物活性物质制剂包括油包水微乳液，其中微乳液的亲水相包含生物活性物质，疏水相包括乳糖微粒或能够在施用后在肠粘膜中形成乳糜微粒的物质。生物活性物质可以是包括胰岛素，降钙素和生长激素营养素或生长激素在内的各种物质中的任何一种。本发明的制剂特别适用于口服胰岛素治疗糖尿病。

3. 发明授权

US5858398A Microparticular pharmaceutical compositions 失效
标题翻译：微关节药物组合物
公开(公告)号：US5858398A
公开(公告)日：1999-01-12
申请号：US635945
申请日：1996-05-02
申请人： Young W. Cho
发明人： Young W. Cho
IPC分类号： A61K9/107 , A61K9/113 , A61K9/14 , A61K9/127 , A61K9/48
CPC分类号： A61K9/1075 , A61K9/113 , Y10S514/937 , Y10S514/941
摘要： A pharmaceutical composition comprises microparticles in micelle. The microparticles contain at least one pharmaceutically-active agent, at least one water soluble or miscible phospholipid, at least one lipid soluble or miscible phospholipid, at least one non-ionic surfactant having an HLB value of about 15 or greater, at least one non-ionic surfactant having an HLB value of about or less, and at least one water soluble or miscible sterol compound. The microparticles are suspended in at least one fatty acid having a chain length of C.sub.14 or less. The composition may optionally contain at least one fatty acid having a chain length of C.sub.16 or greater in a concentration of about 5 w/v % or less. The composition is prepared by admixing the pharmaceutically-active agent, phospholipids, surfactants, and sterol, micronizing the admixture to form microparticles, and suspending the microparticles in at least one fatty acid of chain length of C.sub.14 or less to form microparticles in micelle. The invention may be useful in the oral administration of drugs and other therapeutic agents, as well as for the trans-umbilico-dermal administration of such drugs and therapeutic agents.
摘要翻译： PCT No.PCT / US94 / 12351 Sec。 371日期：1996年5月2日 102（e）日期1996年5月2日PCT 1994年11月3日PCT PCT。公开号WO95 / 12385 PCT 日期1995年5月11日药物组合物包含胶束中的微粒。所述微粒含有至少一种药物活性剂，至少一种水溶性或可混溶磷脂，至少一种脂溶性或可混溶磷脂，至少一种HLB值为约15或更大的非离子表面活性剂，至少一种非可溶性磷脂， HLB值约为或更小的离子表面活性剂和至少一种水溶性或可混溶的固醇化合物。将微粒悬浮在链长为C14以下的至少一种脂肪酸中。组合物可任选地含有浓度为约5w / v％或更低的链长为C16或更大的至少一种脂肪酸。通过混合药物活性剂，磷脂，表面活性剂和固醇，将混合物微粉化以形成微粒，并将微粒悬浮在链长为C14以下的至少一种脂肪酸中以在胶束中形成微粒来制备组合物。本发明可用于药物和其它治疗药物的口服给药，以及用于这些药物和治疗剂的反式 - 真皮 - 皮肤给药。

4. 发明授权

US5665700A Pharmaceutical formulations 失效
标题翻译：药物制剂
公开(公告)号：US5665700A
公开(公告)日：1997-09-09
申请号：US290293
申请日：1994-08-15
申请人： Young W. Cho , Michael John Flynn , Thomas Smith Shepherd
发明人： Young W. Cho , Michael John Flynn , Thomas Smith Shepherd
IPC分类号： A61K9/00 , A61K9/107 , A61K9/16 , A61K38/18 , A61K38/22 , A61K38/23 , A61K38/27 , A61K38/28 , A61K47/00 , A61K47/24 , A61K38/02
CPC分类号： B82Y5/00 , A61K38/1816 , A61K38/23 , A61K38/27 , A61K38/28 , A61K47/24 , A61K9/1075 , A61K9/1617 , Y10S514/937
摘要： A Pharmaceutical formulation comprises a biologically active material such as insulin, erythropoietin, calcitonin and growth hormone, and, associated with it, a phospholipid for forming a material which participates in the alpha-glycerol or other pathways for the formation of lecithins which are found in the intestinal epithelial cell. Biologically active protein orally administered in such a formulation are bioavailable and bioactive.
摘要翻译：药物制剂包含生物活性物质，例如胰岛素，促红细胞生成素，降钙素和生长激素，并且与其相关联，用于形成参与α-甘油或其它途径的磷脂用于形成卵磷脂，所述磷脂用于形成卵磷脂肠上皮细胞。在这种制剂中口服给药的生物活性蛋白质是生物可利用的和生物活性的。

5. 发明授权

US4849227A Pharmaceutical compositions 失效
标题翻译：药物组合物
公开(公告)号：US4849227A
公开(公告)日：1989-07-18
申请号：US21625
申请日：1987-03-03
申请人： Young W. Cho
发明人： Young W. Cho
IPC分类号： A61K9/16 , A61K9/50
CPC分类号： A61K9/16 , A61K9/50
摘要： A composition adapted to administer a pharmocologically effective amount of a pharmaceutical agent when ingested orally comprising (a) a pharmaceutical agent; (b) a lipid coating materials; and (c) an enteric coating materials optionally comprising water soluble coating materials; emulsifying and solubilizing agents; binding agents; stabilizing and enzyme inhibiting agents surfactants and antimicrobial agents. The composition can also include a low density lipoprotein composition and lipolytic enzymes.
摘要翻译：适于在口服摄取时施用药学有效量的药剂的组合物，其包含（a）药剂; （b）脂质涂层材料; 和（c）任选地包含水溶性涂层材料的肠溶衣材料; 乳化剂和增溶剂; 粘合剂; 稳定和酶抑制剂表面活性剂和抗微生物剂。组合物还可以包括低密度脂蛋白组合物和脂肪分解酶。

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