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1. 发明授权

US4056340A Prilling apparatus 失效
标题翻译：造粒机
公开(公告)号：US4056340A
公开(公告)日：1977-11-01
申请号：US701892
申请日：1976-07-01
申请人： Samuel H. Yalkowsky
发明人： Samuel H. Yalkowsky
IPC分类号： A61J3/06 , B22D23/08
CPC分类号： A61J3/06
摘要： A process and apparatus for prilling pharmaceuticals and the like. A mixture supply device provides a melted mixture of a pharmaceutical and a vehicle at a preselected pressure and at a temperature less than the decomposition temperature of the pharmaceutical, such vehicle being solid at normal room temperature. One or more guns receive the melted mixture. A pulse generator provides a train of pulses of preselected frequency and width which through a transducer causes a valve in each gun to periodically open at a frequency and for a duration controlled by the pulse frequency and width. Each gun has a nozzle supplying melted material upon opening of the corresponding valve and from which is ejected a series of spaced droplets of melt mixture at the pulse frequency, which droplets are of size controlled by the pulse width. Means below the nozzle define a gravity drop path for the droplets and contain a fluid for congealing the droplets as they fall along such path to form same into substantially spherical prills.
摘要翻译：用于制备药物等的方法和装置。混合物供应装置在预选压力和低于药物分解温度的温度下提供药物和载体的熔融混合物，这种载体在正常室温下为固体。一个或多个枪接收熔化的混合物。脉冲发生器提供预定频率和宽度的脉冲序列，其通过换能器使每个枪中的阀周期性地以频率和持续时间来打开，持续时间由脉冲频率和宽度控制。每个喷枪具有在打开相应阀门时提供熔化材料的喷嘴，并且以脉冲频率喷射一系列间隔开的熔融混合物液滴，液滴的尺寸由脉冲宽度控制。在喷嘴下面的装置限定了用于液滴的重力下落路径，并且当液滴沿着这样的路径落下时，容纳用于凝结液滴的流体，以形成为基本上为球形的颗粒。

2. 发明授权

US4301175A E-Type prostaglandin compositions 失效
标题翻译： E型前列腺素组合物
公开(公告)号：US4301175A
公开(公告)日：1981-11-17
申请号：US220599
申请日：1980-12-29
申请人： Samuel H. Yalkowsky
发明人： Samuel H. Yalkowsky
IPC分类号： A61K9/08 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , A61K31/215 , A61K31/19
CPC分类号： A61K31/557
摘要： PGE-type compounds are stabilized in a composition comprising a mixture of triacetin and ethanol. This composition surprisingly and unexpectedly retains virtually all of the stability of triacetin compounds and additionally provides the superior water miscibility of ethanol.
摘要翻译： PGE型化合物在包含三醋精和乙醇的混合物的组合物中稳定。这种组合物出人意料地意外地保留了三醋精化合物的几乎所有的稳定性，并且另外提供了乙醇的优异的水混溶性。

3. 发明授权

US07022712B2 Solubilization of weak bases 失效
公开(公告)号：US07022712B2
公开(公告)日：2006-04-04
申请号：US10402347
申请日：2003-03-26
申请人： Samuel H. Yalkowsky
发明人： Samuel H. Yalkowsky
IPC分类号： A61K31/4745 , A61K31/4196
CPC分类号： A61K9/0095 , A61K9/0019 , A61K31/4184 , A61K31/437 , A61K47/12
摘要： A pharmaceutical composition for administration to mammals comprising: a weak base compound having a compound pKa below about 7; an acidic buffer with a buffer pKa below 7; and optional pharmaceutically acceptable additives, wherein the composition has a pH below about 4 is provided. Preferred pharmaceutically active compounds are imidazole derivatives, pyridine derivatives, and aniline derivatives. The pharmaceutical compositions have greater water solubility than the weak base.

4. 发明授权

US4489026A Process for preparing solid unit dosage forms of ultra-low dose drugs 失效
标题翻译：制备超低剂量药物固体单位剂型的方法
公开(公告)号：US4489026A
公开(公告)日：1984-12-18
申请号：US415294
申请日：1982-09-07
申请人： Samuel H. Yalkowsky
发明人： Samuel H. Yalkowsky
IPC分类号： A61K9/16 , A61K9/00
CPC分类号： A61K9/16
摘要： A process for the preparation of solid unit dosage forms is disclosed wherein a fine spray of a dilute solution of a pharmaceutically active material is gradually finely sprayed over an extended time period onto fine excipient particles undergoing agitation. Extremely small amounts of the pharmaceutically active material are deposited on the excipient particles, allowing the resulting powder to be formed into solid unit dosage forms, such as tablets, containing 100 mcg or less of the active ingredient per unit, with high content uniformity among the solid unit dosage forms.
摘要翻译：公开了一种用于制备固体单位剂型的方法，其中将药物活性物质的稀释溶液的细微喷雾在延长的时间段内逐渐细微喷雾到经历搅拌的精细赋形剂颗粒上。将非常少量的药物活性物质沉积在赋形剂颗粒上，使所得粉末形成固体单位剂型，例如片剂，每单位含有100mcg或更少的活性成分，其中固体单位剂型。

5. 发明授权

US3966962A Triacetin solutions of PGE-type compounds 失效
标题翻译： PGE型化合物的三醋精溶液
公开(公告)号：US3966962A
公开(公告)日：1976-06-29
申请号：US562535
申请日：1975-03-27
申请人： Samuel H. Yalkowsky
发明人： Samuel H. Yalkowsky
IPC分类号： A61K9/08 , A61K9/48 , A61K31/557 , A61K31/5575 , A61K47/14 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , A61K31/215 , A61K31/19
CPC分类号： A61K31/557 , A61K47/14
摘要： A stable dosage form of PGE-type compounds is obtained by dissolving these compounds in triacetin.
摘要翻译：通过将这些化合物溶解在三醋精中获得稳定剂型的PGE型化合物。

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