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公开(公告)号：US6162459A
公开(公告)日：2000-12-19
申请号：US801885
申请日：1997-02-18
申请人： Oliver Yoa-Pu Hu
发明人： Oliver Yoa-Pu Hu
IPC分类号： A61K9/00 , A61K31/13 , A61K31/19 , A61K31/522 , A61K31/7016 , A61K31/7076 , A61K31/708 , A61K47/12 , A61K47/26 , A61K9/70 , A61F13/00 , A61F13/02 , A61L15/16
CPC分类号： A61K9/0014 , A61K31/13 , A61K31/19 , A61K31/522 , A61K31/7016 , A61K31/7076 , A61K31/708 , A61K47/12 , A61K47/26 , A61K2300/00
摘要： A transdermal formulation for providing antiviral effect in dermis or epidermis, wherein comprising (a) 0.01 to 30 weight percent of antiviral drug; (b) 0.05 to 20 weight percent of a Chinese medicine enhancer; and (c) a pharmaceutical acceptable vehicles. The antiviral drug is selected from the group consisting of ACV(Acyclovir), Carbovir, DDA(2',3'-Dideoxyadnosine), HPMPA(1-(3-Hydroxy-2-phosphonylmethoxylpropyl)-adenosine), DHPG(Ganciclovir), Desciclovir, IDC (5-Iodo-2'-deoxy-cytidine), Vidarabine(Ara-A), DDI(2',3'-Dideoxyinosine), Cordycepin, Cytarabine, Deoxyguanosine, d4T(2',3'-Didehydro-3'-deoxythymidine), FIAC(2'-Fluoro-5-iodoaracytosine), AZT(ZDV, Zidovudine), Ara-T(1-.beta.-D-Ara-binofuranosylthymine), Deoxythymidine, Ribavirin, EDU(5-Ethyl-2'-deoxy-uridine), Enviroxime, Amantadine, Arildone, HPMPC(9-(3-Hydroxy-2-phosphonyl-methoxyl-propyl)cytidine), Riboxamide, Rimantidine, Tromantadine, Foscamet sodium, Moroxydine, F3T(5-Trifluoro-methyl-2'-deoxy-uridine), BVDU (Bromovinyldeoxyuridine). Preferably, the Chinese medicine enhancer is oleanolic acid, and the pharmaceutical acceptable vehicles is polyethylene glycols.
摘要翻译： 一种用于在真皮或表皮中提供抗病毒作用的透皮制剂，其中包含（a）0.01至30重量％的抗病毒药物; （b）0.05〜20重量％的中药增强剂; 和（c）药物可接受的车辆。 抗病毒药物选自ACV（阿昔洛韦），卡博维尔，DDA（2'，3'-二脱氧腺苷），HPMPA（1-（3-羟基-2-膦酰基甲氧基丙基） - 腺苷），DHPG（更昔洛韦）， 去甲昔洛韦，IDC（5-碘-2'-脱氧胞苷），阿达拉滨（Ara-A），DDI（2'，3'-二脱氧肌苷），虫草素，阿糖胞苷，脱氧鸟苷，d4T（2'，3'-二脱氢 - 3'-脱氧胸苷），FIAC（2'-氟-5-碘代胞嘧啶），AZT（ZDV，齐多夫定），Ara-T（1-β-D-Ara-二呋喃糖基胸腺嘧啶），脱氧胸苷，利巴韦林，EDU（5-乙基 - （9-（3-羟基-2-膦酰基 - 甲氧基 - 丙基）胞苷），内酰胺，R啶啶，特仑他丁，Foscamet钠，Moroxydine，F3T（5-三氟 甲基-2'-脱氧尿苷），BVDU（溴乙酰基脱氧尿苷）。 优选地，中药增强剂是齐墩果酸，药学上可接受的载体是聚乙二醇。
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公开(公告)号：US07169763B2
公开(公告)日：2007-01-30
申请号：US10080043
申请日：2002-02-22
IPC分类号： A61K31/7004
CPC分类号： A61K45/06 , A61K31/01 , A61K31/11 , A61K31/353 , A61K31/7048 , A61K2300/00
摘要： The present invention provides cytochrome P450 3A (CYP3A) inhibitors and enhancers. Examples of the CYP3A inhibitors include free bases or pharmacologically acceptable salts of at least one of the following compounds: α-naphthoflavone, β-naphthoflavone, apigenin, baicalein, β-myrcene, catechin, 3-phenylpropyl acetate, formononetin, gallic acid, hesperetin, hesperidin, isoquercitrin, lauryl alcohol, luteolin, luteolin-7-glycoside, narigin, nordihydroguaiaretic acid, quercitrin, swertiamarin, terpineol, and trans-cinnamaldehyde. Examples of the CYP3A enhancers include free bases or pharmacologically acceptable salts of at least one of the following compounds: apigenin, formononetin, and luteolin-7-glycoside. The CYP3A inhibitors can be used, alone or co-administered with a drug, to improve the drug bioavailability. The CYP3A inhibitors can also be used as chemopreventors to prevent biotransformation of procarcinogenic compounds into carcinogens via CYP3A activity or for treatment of intestinal or hepatic cancer by inhibit the CYP3A activity. The CYP3A enhancers can be used to improve the enzymatic activity of CYP3A so as to improve the biotransformation and degradation of active drugs or the sustrates of CYP3A from the body. The CYP3A inhibitors and enhancers of the present invention are natural substances extracted from herbs and non-toxic.
摘要翻译： 本发明提供细胞色素P450 3A（CYP3A）抑制剂和增强剂。 CYP3A抑制剂的实例包括以下化合物中的至少一种的游离碱或药理学上可接受的盐：α-萘黄酮，β-萘醌，芹菜素，黄芩素，β-月桂烯，儿茶素，乙酸3-苯基丙酯，草铵膦，没食子酸，橙皮素 ，橙皮苷，异槲皮苷，月桂醇，木犀草素，木犀草素-7-糖苷，奈格林，去甲二氢愈创木酚酸，槲皮素，藜芦醇，萜品醇和反式肉桂醛。 CYP3A增强剂的实例包括至少一种以下化合物的游离碱或药理学上可接受的盐：芹菜素，角叉菜胶和木犀草素-7-糖苷。 CYP3A抑制剂可单独使用或与药物共同施用以改善药物生物利用度。 CYP3A抑制剂也可用作化学预防剂，以通过CYP3A活性或通过抑制CYP3A活性来预防致癌物质转化为致癌物质。 CYP3A增强子可用于改善CYP3A的酶活性，从而改善活体药物或体外CYP3A的生物转化和降解。 本发明的CYP3A抑制剂和增强剂是从草药中提取的天然物质和无毒的。
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公开(公告)号：US06703398B2
公开(公告)日：2004-03-09
申请号：US09991948
申请日：2001-11-26
IPC分类号： A61K31485
CPC分类号： A61K31/485
摘要： The present invention provides orally administered pharmaceutical compositions which contains an effective amount of free base or pharmaceutcially acceptable salts of nalbuphine and/or nalbuphine ester, an oily substance, and a solubility-assisting agent. The oily substance is preferably sesame oil. The solubility-assisting agent is preferably benzyl benzoate. The pharmaceutical composition is useful as an analgesic. The compositions achieves a much higher bioavailability rate and yields much longer lasting effects on nalbuphine than other nalbuphine products currently in the market.
摘要翻译： 本发明提供口服给药的药物组合物，其含有有效量的游离碱或药物可接受的纳布啡和/或纳布丁酯的盐，油性物质和溶解性辅助剂。 油状物优选为芝麻油。 溶解性助剂优选苯甲酸苄酯。 药物组合物可用作止痛剂。 与目前市场上其他纳布啡组合物相比，组合物达到高得多的生物利用度并且对纳布啡组产生更长时间的持久作用。
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公开(公告)号：US06544954B1
公开(公告)日：2003-04-08
申请号：US10076650
申请日：2002-02-19
IPC分类号： A61K3170
CPC分类号： A61K9/0019 , A61K31/7004 , A61K47/02 , A61K47/12 , A61K47/22 , Y10S514/893
摘要： The present invention provides stable galactose injection solutions, which contain 1 to 50% by weight of galactose, 0.01 to 1 M of a buffer solution, and 0.01 to 5% of an antioxidant. The preferred buffer solution is citrate buffer. The preferred anti-oxidant is sodium bisulfite. The galactose injection solution of the present invention has a pH between 4.0 and 9.0 and is stable at 80° C. for at least 2 weeks.
摘要翻译： 本发明提供了稳定的半乳糖注射溶液，其含有1至50重量％的半乳糖，0.01至1M缓冲溶液和0.01至5％的抗氧化剂。 优选的缓冲溶液是柠檬酸盐缓冲液。 优选的抗氧化剂是亚硫酸氢钠。 本发明的半乳糖注射溶液具有4.0至9.0之间的pH，并且在80℃下稳定至少2周。
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公开(公告)号：US20130184227A1
公开(公告)日：2013-07-18
申请号：US12628194
申请日：2009-11-30
IPC分类号： A61K31/12 , A61K31/352
CPC分类号： A61K31/12 , A61K31/015 , A61K31/192 , A61K31/352 , A61K31/353 , A61K31/47 , A61K31/70 , A61K31/704 , A61K31/7048
摘要： This invention is to provide multiple specific inhibitors of cytochrome P450 isozyme CYP2C9. These inhibitors can be derived from any combinations with the following compounds including: Tamarixetin, Formononetin, isoliquritigenin, Phloretin, luteolin, Quercitrin, quercetin, myricetin, Wongonin, Puerarin, Genistein, Nordihydroguaiaretic acid, Narigenin, Capillarisin, Chrysin, Fisefin, eriodictyol, 6-Gingerol, Isorhamneti, isoquercitrin, Morin, (+)-Taxifolin, isovitexin, 3-Phenylpropyl Acetate, Oleanolic acid, ursolic acid, β-Myrcene, cinnamic acid, Luteolin-7-Glucoside, Liquiritin, (+) Limonene, Homoorientin, Swertiamarin, Embelin, Daidzein, Poncirin, (−)-Epicatechin, ergosterol. These natural products can be used to enhance the bioavailability of therapeutic agents (drugs).
摘要翻译： 本发明提供细胞色素P450同功酶CYP2C9的多种特异性抑制剂。 这些抑制剂可以衍生自与以下化合物的任何组合，包括：Tamarixetin，Formononetin，sepiquritigenin，Phloretin，木犀草素，槲皮素，槲皮素，杨梅素，Wongonin，葛根素，染料木黄酮，Nordihydroguaiaretic acid，Narigenin，Capillarisin，Chrysin，Fisefin，eriodictyol，6 姜黄素，异黄酮，异槲皮素，莫林，（+） - 紫杉醇，异鸟苷酸，乙酸3-苯基丙酯，油酸，熊果酸，β-月桂烯，肉桂酸，木犀草素7-葡萄糖苷，甘草苷，（+）柠檬烯， Swertiamarin，Embelin，Daidzein，Poncirin，（ - ） - 表儿茶素，麦角甾醇。 这些天然产物可用于提高治疗剂（药物）的生物利用度。
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6.发明授权公开(公告)号：US06225321B1
公开(公告)日：2001-05-01
申请号：US08869917
申请日：1997-06-05
申请人： Oliver Yoa-Pu Hu , Shung-Tai Ho , Fangchen Lee
发明人： Oliver Yoa-Pu Hu , Shung-Tai Ho , Fangchen Lee
IPC分类号： C07D48902
CPC分类号： C07D498/04
摘要： The nalbuphine polyester derivative is related to a novel long acting agent. The nalbuphine polyester derivative is R—[CO-NAL]n wherein n is an integer from 2-4 and, in which the R is selected from a saturated or nonsaturated, substituted or unsubstituted, aliphatic or aromatic group having 1 to 40 carbon atoms. The process for producing the derivative includes esterifying nalbuphine with a saturated or unsaturated fatty acid or a halogen compound of the fatty acid with an acid anhydride. A pharmaceutical composition contains the derivative and a pharmaceutically acceptable carrier, which can be administered to an animal or person for treating pain.
摘要翻译： 纳布啡聚酯衍生物与新型长效剂有关。 纳布啡聚酯衍生物是R- [CO-NAL] n，其中n是2-4的整数，其中R选自饱和或非饱和的取代或未取代的具有1至40个碳原子的脂族或芳族基团 。 制备衍生物的方法包括用饱和或不饱和脂肪酸或脂肪酸的卤素化合物与酸酐酯化纳布啡。 药物组合物含有可以给予动物或人治疗疼痛的衍生物和药学上可接受的载体。
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公开(公告)号：US6022558A
公开(公告)日：2000-02-08
申请号：US886400
申请日：1997-07-01
申请人： Oliver Yoa-Pu Hu , Chieh Fu Chen
发明人： Oliver Yoa-Pu Hu , Chieh Fu Chen
IPC分类号： A61K31/5415 , A61K47/08 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/22 , A61K47/26 , A61F13/00
CPC分类号： A61K47/10 , A61K31/5415 , A61K47/08 , A61K47/12 , A61K47/14 , A61K47/22 , A61K47/26 , A61K9/0014 , Y10S514/944 , Y10S514/946 , Y10S514/947 , Y10S514/969
摘要： The present invention is related to a trandermal preparation of oxicams. In preparation, it is comprised of 0.1% to 50% of an oxicam, 0.1% to 70% of pure compositions from Chinese herbal enhancers as enhancers, as well as other necessary excipients for transdermal delivery of an active ingredient. This transdermal preparation is intended to be used for anti-inflammatory cases, but with few gastrointestinal side effects. Based on results from testing this preparation on nude mice skin, rabbit skin, and human leg skin, it was found that skin penetration of the transdermal preparation containing 20% terpineol oil was 157.6 times higher than that of the control group.
摘要翻译： 本发明涉及牛磺酸的皮肤制剂。 在制备时，它由0.1％至50％的奥卡胺，0.1％至70％的中草药增强剂作为增强剂的纯组合物以及用于透皮递送活性成分的其它必需赋形剂组成。 这种透皮制剂旨在用于抗炎症病例，但具有很少的胃肠道副作用。 根据对裸鼠皮肤，兔皮肤和人体皮肤的这种制剂的测试结果，发现含有20％萜品醇油的透皮制剂的皮肤渗透是对照组的157.6倍。
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8.发明授权公开(公告)号：US06680067B2
公开(公告)日：2004-01-20
申请号：US09991608
申请日：2001-11-26
IPC分类号： A61F202
CPC分类号： A61K9/0019 , A61K31/485 , A61K36/185 , A61K36/48 , A61K47/44 , A61K2300/00
摘要： A controlled-release pharmaceutical preparation containing an oil suspension which comprises an analgesic and an injectable oil. The analgesic is either a nalbuphine free base or a pharmaceutical salt of nalbuphine such as nalbuphine HCl. The injectable oil is preferably sesame oil. The oil suspension contains microparticles in the size range of 1 to 100 &mgr;m, preferably less than 50 &mgr;m, which is produced by treating the analgesic and injectable oil in an ultra high energy mixing equipment. The controlled-release preparation permits nalbuphine free base or nalbuphine HCl to have a longer duration of action in relieving pain, and allows the administration of lower doses. A process for preparing the injectable oil suspension is also disclosed.
摘要翻译： 含有油悬浮液的控释药物制剂，其包含止痛剂和可注射油。 止痛剂是纳布啡碱游离碱或纳布啡的药物盐，例如盐酸萘胺。 注射油优选为芝麻油。 油悬浮液含有通过在超高能量混合设备中处理镇痛和可注射油产生的尺寸范围为1至100μm，优选小于50μm的微粒。 控制释放制剂允许纳布啡游离碱或纳布啡盐在缓解疼痛中具有更长的作用时间，并允许施用较低剂量。 还公开了一种制备可注射油悬浮液的方法。
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公开(公告)号：US6004969A
公开(公告)日：1999-12-21
申请号：US948234
申请日：1997-10-09
申请人： Oliver Yoa-Pu Hu
发明人： Oliver Yoa-Pu Hu
CPC分类号： A61K9/0014 , A61K31/485 , A61K47/06 , A61K47/10 , A61K47/12 , A61K47/38 , Y10S514/947
摘要： Buprenorphine is a potent analgesic agent, it has been shown to be as effective as morphine. The main clinical application of buprenorphine is to relief postoperative pains or for patients in the terminal phase of cancer. The chance of becoming addiction and abuse is low, therefore it is pretty safe for clinical use. The half life of buprenorphine is short, since its hepatic extraction (extraction ratio is 0.7 to 0.9) and metabolism are high. For these reasons, oral administration of buprenorphine becomes impractical due to the need of giving drug frequiently. The present invention is related to enhancers used in transdermal preparations of narcotic analgesic agents. This invention employs pure components of Chinese herbs in a fixed ratio as transdermal penetration enhancers. Compositions of these transdermal preparations usually include 0.1 to 50% of narcotic analgesic agent, 0.1 to 70% of pure components from Chinese herb as transdermal penetration enhancers, and other necessary excipients for transdermal delivery. Studies for the present invention in nude mice revealed that a transdermal preparation containing 10% of terpineol can delivery 15 mg of buprenorphine through 10 cm.sup.2 skin area in 48 hours, which satisfied the need of practical use.
摘要翻译： 丁丙诺啡是一种有效的止痛剂，已被证明与吗啡一样有效。 丁丙诺啡的主要临床应用是缓解术后疼痛或癌症终末期患者。 成瘾和虐待的机会很低，因此临床使用相当安全。 丁丙诺啡的半衰期短，因其肝提取（提取率为0.7〜0.9），代谢高。 由于这些原因，由于需要频繁给药，因此丁丙诺啡的口服给药变得不切实际。 本发明涉及用于麻醉止痛剂的透皮制剂中的增强剂。 本发明采用固定比例的中草药纯组分作为透皮渗透促进剂。 这些透皮制剂的组合物通常包括0.1至50％的麻醉止痛剂，0.1至70％的中草药纯组分作为透皮渗透促进剂，以及用于透皮递送的其它必需赋形剂。 本发明在裸鼠中的研究显示，含有10％萜品醇的透皮制剂可在48小时内通过10cm 2皮肤区域递送15mg丁丙诺啡，这满足实际使用的需要。
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10.发明授权
公开(公告)号：US5807115A
公开(公告)日：1998-09-15
申请号：US594595
申请日：1996-01-31
申请人： Oliver Yoa-Pu Hu
发明人： Oliver Yoa-Pu Hu
摘要： An automated dissolution apparatus and method that simulates the physiological condition of gastrointestinal tract has been developed. The invention is capable of continuously adjusting the pH and enzyme content of dissolution medium with consideration of the transit time of a pharmaceutical dosage form. The apparatus includes a pH meter with recorder, a dissolution tester, a UV spectrophotometer, a dissolution data recorder with processor, a personal computer and a printer. The present invention can adjust the pH and enzyme content of a dissolution medium based on the literature information of human gastrointestinal conditions and transit times of various pharmaceutical dosage forms. Use of the present invention not only can change the pH and enzyme content of dissolution medium continueously, but also can differentiate the change of drug release and effects of pH and enzyme content on the drug release rate of pharmaceutical formulations.
摘要翻译： 已经开发了一种模拟胃肠道生理状态的自动溶解仪和方法。 考虑到药物剂型的转运时间，本发明能够连续地调节溶解介质的pH和酶含量。 该装置包括具有记录器的pH计，溶解测试仪，UV分光光度计，具有处理器的溶出数据记录器，个人计算机和打印机。 本发明可以根据人类胃肠道条件和各种药物剂型的运输时间的文献信息来调节溶出介质的pH和酶含量。 本发明的用途不仅可以连续改变溶出介质的pH和酶含量，而且可以区分药物释放的变化以及pH和酶含量对药物制剂的药物释放速率的影响。
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