公开(公告)号：US06890561B1

公开(公告)日：2005-05-10

申请号：US10069388

申请日：2000-08-15

申请人： Yoav Blatt ,  Oded Arad ,  Eugene Kimelman ,  David Cohen ,  Rika Pinto ,  Avner Rotman

发明人： Yoav Blatt ,  Oded Arad ,  Eugene Kimelman ,  David Cohen ,  Rika Pinto ,  Avner Rotman

IPC分类号： A61K9/16 ,  A61K9/26 ,  A61K9/50 ,  A61K9/52 ,  A61K9/54 ,  A61K31/352 ,  A61K9/14 ,  A61K9/20 ,  A61K9/22 ,  A61K9/48

CPC分类号： A61K9/1652 ,  A61K9/1635 ,  A61K9/5047 ,  A61K31/352

摘要： There is provided an orally-administrable formulation for the controlled release or stable storage of a granulated isoflavone-enriched fraction or mixture of such fractions, comprising at least one granulated isoflavone-enriched fraction and at least one carrier, diluent or excipient therefor. Preferably, the formulation is characterized in that the total in vitro dissolution time of said formulation required for release of 75% of the active ingredients available from the formulation is between about 4 and about 18 hours, as determined by the U.S.P. XXIII paddle method at a paddle speed of 75 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, at pH 6.8, and a temperature of 37° C. A process for the preparation of such a formulation is also provided.

摘要翻译： 提供了一种可口服给药的制剂，其用于控制​​释放或稳定地储存富含粒状异黄酮的级分或这些级分的混合物，其包含至少一种颗粒状异黄酮富集部分和至少一种载体，稀释剂或赋形剂。 优选地，所述制剂的特征在于，释放所述制剂中可获得的75％活性成分所需的所述制剂的总体外溶出时间为约4至约18小时，如U.S.P。 XXIII桨法以桨叶速度为75rpm，使用模拟肠液，没有通常在肠液中发现的消化酶，pH 6.8，温度为37℃。还提供了制备这种制剂的方法。

公开(公告)号：US6156347A

公开(公告)日：2000-12-05

申请号：US10165

申请日：1998-01-21

申请人： Yoav Blatt ,  Oded Friedman ,  Eugene Kimelman ,  Avner Rotman

发明人： Yoav Blatt ,  Oded Friedman ,  Eugene Kimelman ,  Avner Rotman

IPC分类号： A61K9/22 ,  A61K9/50 ,  A61K31/4402 ,  A61K31/555 ,  A61K33/24

CPC分类号： A61K31/555 ,  A61K31/4402 ,  A61K33/24 ,  A61K9/5078

摘要： The present invention relates to controlled/extended release oral dosage forms of chromium picolinate. Chromium picolinate is a common and effective biologically active form of chromium. As such, it has beneficial nutritional and therapeutic effects including improved insulin metabolism and lipid lowering activity.The controlled dosage form of the present invention can be provided in various ways, including matrix formulations such as matrix tablets or multiparticulate formulations like micro capsules or coated pellets put into hard gelatin capsules. This provides effective drug delivery for extended periods of time, at relatively stable, optimal plasma peak values, with minimal undesirable side effects.The invention provides effective controlled/extended release oral dosage formulations of chromium picolinate and processes for their preparation.

摘要翻译： 本发明涉及吡啶甲酸铬的受控/延长释放的口服剂型。 吡啶甲酸铬是一种常见且有效的生物活性形式的铬。 因此，它具有有益的营养和治疗效果，包括改善的胰岛素代谢和降脂活性。 本发明的受控剂型可以以各种方式提供，包括基质制剂如基质片剂或多颗粒制剂如微胶囊或放入硬明胶胶囊中的包衣丸剂。 这提供了在相对稳定的最佳血浆峰值下延长的时间段的有效药物递送，具有最小的不希望的副作用。 本发明提供了有效的控制/延长释放的吡啶甲酸铬的口服剂量制剂及其制备方法。

公开(公告)号：US06340478B1

公开(公告)日：2002-01-22

申请号：US09327752

申请日：1999-06-07

申请人： Yoav Blatt ,  Eugene Kimmelman ,  David Cohen ,  Avner Rotman

发明人： Yoav Blatt ,  Eugene Kimmelman ,  David Cohen ,  Avner Rotman

IPC分类号： A61K3578

CPC分类号： A61K9/5047 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2081

摘要： There is provided an orally-administrable formulation for the controlled release or stable storage of a granulated herb, comprising a granulated herb and at least one carrier, adjuvant or excipient therefor. Preferably, the formulation is characterized in that the total in vitro dissolution time of said formulation required for release of 75% of the active ingredients available from the formulation is between about 4 and about 18 hours, as determined by the U.S.P. XXIII paddle method at a paddle speed of 150 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.8, and a temperature of 37° C. A process for the preparation of such formulation is also provided.

摘要翻译： 提供了用于控制释放或稳定储存颗粒状药物的口服制剂，其包含颗粒状药草和至少一种载体，佐剂或赋形剂。 优选地，所述制剂的特征在于，释放所述制剂中可获得的75％活性成分所需的所述制剂的总体外溶出时间为约4至约18小时，如U.S.P。 XXIII桨法以150rpm的桨叶速度，使用模拟肠液，不含肠液中通常存在的消化酶，含有0.1％w / w十二烷基硫酸钠（SDS），pH 6.8，温度为37℃。 还提供了制备这种制剂的方法。

公开(公告)号：US06270803B1

公开(公告)日：2001-08-07

申请号：US09392754

申请日：1998-10-07

申请人： Yoav Blatt ,  David Cohen ,  Eugene Kimmelman ,  Oded Friedman ,  Avner Rotman

发明人： Yoav Blatt ,  David Cohen ,  Eugene Kimmelman ,  Oded Friedman ,  Avner Rotman

IPC分类号： A61K914

CPC分类号： A61K9/5073 ,  A61K9/2081 ,  A61K9/5042 ,  A61K9/5047 ,  A61K36/8962 ,  A61K2300/00

摘要： There are provided orally-administrable formulations for the controlled release of granulated garlic, comprising particles of granulated garlic coated with a film comprising a mixture of at least one water soluble polymer and at least one water insoluble polymer, said at least one water soluble polymer and at least one water insoluble polymer being present in a ratio that produces a substantially zero order linear release pattern of at least one active ingredient. Preferably, the formulations are characterized in that the total in vitro dissolution time of said formulations required for release of 75% of the Allicin available from said formulations based upon the total amount of alliin initially present in said formulations is between about 4 and about 12 hours, as determined by U.S.P. XXIII paddle method at a paddle speed of 150 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.8, and a temperature of 37° C. A process for preparing the formulations of the invention is also disclosed.

摘要翻译： 提供了用于受控释放造粒大蒜的口服给药制剂，其包括用包含至少一种水溶性聚合物和至少一种水不溶性聚合物的混合物的膜的粒状大蒜颗粒，所述至少一种水溶性聚合物和 至少一种水不溶性聚合物以一定比例存在，其产生至少一种活性成分的基本零级线性释放模式。 优选地，制剂的特征在于，基于最初存在于所述制剂中的蒜素的总量，从所述制剂释放75％的大蒜素所需的所述制剂的总体外溶出时间为约4至约12小时 ，由USP确定 XXIII桨法以150rpm的桨叶速度，使用模拟肠液，不含肠液中通常存在的消化酶，含有0.1％w / w十二烷基硫酸钠（SDS），pH 6.8，温度为37℃。 还公开了制备本发明制剂的方法。

公开(公告)号：US5098725A

公开(公告)日：1992-03-24

申请号：US501079

申请日：1990-03-29

申请人： Avner Rotman ,  Yoav Blatt

发明人： Avner Rotman ,  Yoav Blatt

IPC分类号： A21D2/00 ,  A21D2/02 ,  A23L1/00 ,  A23L1/22 ,  A23L1/236

CPC分类号： A21D2/00 ,  A21D2/02 ,  A23L27/32 ,  A23L27/72 ,  A23P10/35

摘要： Very small particles of flavoring materials which are labile when subjected to both heat and an aqueous medium are coated with a coating material containing hydrogenated castor oil and having a melting point of from about 80.degree. to about 100.degree. C. The coating layer remains stable during the first minutes of the baking process, when the concentration of water in the dough or batter is relatively high. After several minutes, when most of the water in the dough or batter has evaporated and the temperature increases to about 100.degree. C., the coating layer or layers melt away. Within a few minutes thereafter, the active ingredient is exposed within the product. Alternatively, a leavening agent may be used wihtin the capsule which will release a gas at the predetermined temperature and cause rupture of the microencapsulation.

公开(公告)号：US4710384A

公开(公告)日：1987-12-01

申请号：US889775

申请日：1986-07-28

申请人： Avner Rotman

发明人： Avner Rotman

IPC分类号： A61K9/22 ,  A61K9/20 ,  A61K9/46 ,  A61K9/52 ,  A61K9/50 ,  A61K9/26 ,  A61K9/28

CPC分类号： A61K9/2081 ,  A61K9/0007

摘要： A tablet for oral adminstration of a sustained-release medication is formed by compressing microcapsules of the active principle. The microcapsules are of a size range between about 5 and 300 microns and comprise particles of active principle coated with a thin, flexible layer of sustained release material. The sustained-release material contains about 15-30% by weight thereof of plasticizer and is coated in an amount corresponding to 10-25% of the weight of the active material. Excipients causing disintegration of the tablet after administration can be uniformly mixed with the microcapsules prior to compression.

公开(公告)号：US3963765A

公开(公告)日：1976-06-15

申请号：US487432

申请日：1974-07-11

申请人： Yehuda Mazur ,  Avner Rotman

发明人： Yehuda Mazur ,  Avner Rotman

IPC分类号： C07J9/00

CPC分类号： C07J9/00

摘要： Process for the production of hydroxylated derivatives of cholesterol and 7-dehydrocholesterol which comprises subjecting a saturated unsubstituted or substituted derivative of cholestane, dissolved in a suitable solvent, in the presence of peracetic acid, to irradiation with ultra-violet radiation of a wavelength below 350m.mu. , or heating in a suitable solvent, separating the reaction products, which if desired, are converted to other derivatives, and recovering the residue of the starting material. Novel derivatives are obtained and these are: 3.beta.-acetoxy,25-hydroxy,5.alpha.-cholestane; 3.beta.-acetoxy, 5.alpha.,25-dihydroxy cholestane; 3.beta.,5.alpha.,25-trihydroxy cholestane; 3-keto, 5.alpha.,25-dihydroxy cholestane; 3-keto,25-hydroxy-.DELTA..sup.4 -cholestane; 3.beta.,25-diacetoxy-5.alpha.-hydroxy-cholestane; 3.beta.-acetoxy, 25-trichloroacetoxy-5.alpha.-hydroxy-cholestane, 25-trichloroacetoxy-cholesterol and 25-acetoxy-cholesterol.

摘要翻译： 用于生产胆固醇和7-脱氢胆固醇的羟基化衍生物的方法，其包括在过乙酸存在下使溶解在合适溶剂中的饱和的未取代或取代的胆甾烷的衍生物经过饱和的溶解在合适溶剂中的衍生物照射波长低于350μm的紫外线辐射 或在合适的溶剂中加热，将反应产物分离，如果需要，将其转化为其它衍生物，并回收原料残余物。 得到新的衍生物，它们是：3β-乙酰氧基，25-羟基，5α-胆甾烷; 3β-乙酰氧基，5α，25-二羟基胆甾烷; 3β，5α，25-三羟基胆甾烷; 3-keto，5α，25-二羟基胆甾烷; 3-酮基，25-羟基-DTA4-胆甾烷; 3β，25-二乙酰氧基-5α-羟基 - 胆固醇; 3β-乙酰氧基，25-三氯乙酰氧基-5α-羟基 - 胆固醇，25-三氯乙酰氧基 - 胆固醇和25-乙酰氧基 - 胆固醇。

公开(公告)号：US4609740A

公开(公告)日：1986-09-02

申请号：US380472

申请日：1982-05-20

申请人： Avner Rotman

发明人： Avner Rotman

IPC分类号： C07D311/82

CPC分类号： C07D311/82

摘要： The invention relates to derivatives of fluorescein and to their production. The compounds are of value in determining the intracellular pH. Thus there may be obtained fluorescent living cells with a comparatively stable level of fluorescence. The novel fluorescein compounds can be used for other labelling purposes in biology and biochemistry.

摘要翻译： 本发明涉及荧光素的衍生物及其生产。 该化合物在确定细胞内pH值方面是有价值的。 因此，可以获得具有相对稳定的荧光水平的荧光活细胞。 新型荧光素化合物可用于生物学和生物化学中的其他标记目的。

公开(公告)号：US4749575A

公开(公告)日：1988-06-07

申请号：US823798

申请日：1986-01-29

申请人： Avner Rotman

发明人： Avner Rotman

IPC分类号： A23G1/00 ,  A23G1/42 ,  A61K9/00 ,  A61K9/20 ,  A61K9/22 ,  A61K9/52

CPC分类号： A23G1/426 ,  A61K9/0056 ,  A61K9/2081

摘要： Any orally administrable medicament is prepared into a dosage form which eliminates the unpleasant taste and mouth feel of the medicament and is easily and pleasantly ingested even by children, by microencapsulating the medicament into microcapsules of less than 300 microns diameter, and embedding the microcapsules into a soft, sweet, palatable matrix, such as chocolate.

摘要翻译： 将任何可口服给药的药剂制备成消除药物的令人不快的味道和口感的剂型，甚至通过将药物微囊化成小于300微米直径的微胶囊，并且将微胶囊包埋在 柔软，甜美，可口的基质，如巧克力。