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公开(公告)号：US4339463A
公开(公告)日：1982-07-13
申请号：US169395
申请日：1980-07-16
申请人： Yasushi Takagishi , Yoshio Doi , Noboru Hoshi
发明人： Yasushi Takagishi , Yoshio Doi , Noboru Hoshi
CPC分类号： A61K9/4858 , A61K9/4816 , A61K9/485
摘要： The invention provides a novel means for overcoming the problem of undue and irregular delay in the exhibition of the effect of medicine when a patient is administrated with an enterosoluble hard-capsulated medicament. The unexpected discovery that the key parameter ruling the smooth transfer of an enterosoluble capsule from the stomach to the intestinal canals is the overall specific gravity of the capsule has led to the establishment of the invention which proposes an enterosoluble hard-capsulated medicament having an overall specific gravity of at least 1.05 or, preferably, at least 1.10.
摘要翻译： 本发明提供了一种新颖的手段，克服了当患者服用肠溶性硬封闭药物时，展示药物效果的不当和不规律延误的问题。 意外的发现是，将肠溶胶囊从胃平滑转移到肠道的关键参数是胶囊的总比重导致本发明的建立，其提出了具有总体特异性的肠溶性硬封闭药物 重力至少为1.05，优选为至少1.10。
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2.发明授权Long acting preparation of cefalexin for effective treatments of bacterial infection sensitive to cefalexin 失效长效制剂头孢氨苄用于有效治疗对头孢氨苄敏感的细菌感染
公开(公告)号：US4250166A
公开(公告)日：1981-02-10
申请号：US801402
申请日：1977-05-27
IPC分类号： A61K9/50 , A61K31/545 , A61K31/78 , A61K31/54
CPC分类号： A61K9/5084 , A61K31/545
摘要： A cefalexin preparation coated with a coating layer the solubility of which layer is pH-dependent and dissolves in the upper intestine is preferably administered concurrently with a normal (plain, quick-releasing) cefalexin. The coated preparation is preferably coated, in the particle form and when administered orally, exists in the particle form in the stomach. Preferably, the coating layer is made from a coating material having a dissolution pH of from 5.5 to 6.5, and the ratio in terms of potency of the coated cefalexin to the normal cefalexin is between 15:85 and 60:40. The coated cefalexin and the normal cefalexin can be formulated in a pharmaceutical preparation preferably in a unit-dosage form, e.g., capsules, tablets or particles or in strip-packages.
摘要翻译： 涂覆有涂层的头孢氨苄制剂优选与普通（平滑，快速释放）头孢氨苄同时施用哪一层的溶解度依赖于pH并溶解于上肠。 涂覆的制剂优选以颗粒形式包衣，并且当口服给药时，以颗粒形式存在于胃中。 优选地，涂层由溶解pH为5.5至6.5的涂层材料制成，并且涂覆的头孢氨苄与正常头孢氨苄的效力之比在15:85至60:40之间。 涂覆的头孢氨苄和正常的头孢氨苄可以配制成药物制剂，优选为单位剂型，例如胶囊，片剂或颗粒或带状包装。
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公开(公告)号：US4892738A
公开(公告)日：1990-01-09
申请号：US185354
申请日：1988-04-18
CPC分类号： A61K9/5026 , A61K9/1617 , A61K9/5084
摘要： A favorable sustained-releasing property is given to granular preparations by incorporating therein at least one C.sub.16 -C.sub.18 saturated fatty acid and/or metal salts thereof at a rate of 10-50% of the total weight of the dosage form. The disclosed dosage form releases the active ingredient both in a low pH region of the stomach and in a high pH region of the intestine at an appropriate rate.
摘要翻译： 通过以至少一种C16-C18饱和脂肪酸和/或其金属盐的剂量形式的总重量的10-50％的比例掺入颗粒状制剂来获得有利的持续释放性质。 所公开的剂型在适当的速率下在胃的低pH区域和肠的高pH区域中释放活性成分。
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4.发明授权Suppository containing sulfamethoxazole/trimethoprim complex and process for preparing the same 失效含有磺胺甲恶唑/甲氧苄啶复合物的栓剂及其制备方法
公开(公告)号：US4461765A
公开(公告)日：1984-07-24
申请号：US288795
申请日：1981-07-31
申请人： Yasushi Takagishi , Kiichiro Ohsuga , Sadao Ohama
发明人： Yasushi Takagishi , Kiichiro Ohsuga , Sadao Ohama
IPC分类号： A61K31/505 , A61K9/02 , A61K31/63 , A61K31/635 , A61P31/04 , A61K31/625
CPC分类号： A61K9/02 , A61K31/635 , Y10S424/15
摘要： Suppository containing a one-to-one complex of sulfamethoxazole and trimethoprim dispersed in a pharmaceutically acceptable carrier is disclosed. It may contain a supplemental amount of sulfamethoxazole in addition to the sulfamethoxazole component in the complex and is superior to conventional preparations of a simple mixture in its manufacturing process as well as its pharmacokinetical property.
摘要翻译： 公开了含有分散在药学上可接受的载体中的磺胺甲恶唑和甲氧苄啶的一对一复合物的栓剂。 除了复合物中的磺胺甲恶唑组分外，还可含有补充量的磺胺甲恶唑，并且在制造过程中优于常规制剂，简单混合物及其药物动力学性质。
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公开(公告)号：US4405597A
公开(公告)日：1983-09-20
申请号：US292040
申请日：1981-08-11
CPC分类号： A61K9/4816 , A61K9/025
摘要： The invention provides a novel means for the administration of a therapeutically effective ingredient in the form of a rectally applicable medicament capsule, in which the otherwise unavoidable extreme variation in the absorbability of the effective ingredient among the individuals rectally treated with the capsules is minimized. It has been unexpectedly found that, when the effective ingredient is contained in the capsule in the form of a liquid medicine, the osmotic pressure of the liquid content plays a very essential role in the absorption of the effective ingredient through the rectum and the variation in the absorbability of the effective ingredient among the individuals can be minimized when the osmotic pressure of the liquid content is substantially higher than the osmotic pressure of the rectal fluid with which the capsules are contacted.
摘要翻译： 本发明提供了一种用于施用直肠可用药物胶囊形式的治疗有效成分的新方法，其中用胶囊直肠治疗的个体之间有效成分的吸收性的其他不可避免的极端变化最小化。 已经意外地发现，当液体药物形式的胶囊中含有有效成分时，液体含量的渗透压在通过直肠的有效成分的吸收中发挥非常重要的作用， 当液体含量的渗透压显着高于胶囊与其接触的直肠液的渗透压时，个体之间有效成分的吸收能力可被最小化。
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公开(公告)号：US5290569A
公开(公告)日：1994-03-01
申请号：US895466
申请日：1992-06-08
申请人： Noboru Nagafuzi , Takayuki Tsukada , Kazuhiro Shima , Yasushi Takagishi , Yusuke Suzuki , Yoshitaka Tomoda , Takashi Hayashi
发明人： Noboru Nagafuzi , Takayuki Tsukada , Kazuhiro Shima , Yasushi Takagishi , Yusuke Suzuki , Yoshitaka Tomoda , Takashi Hayashi
CPC分类号： B82Y5/00 , A61K47/48969 , A61K9/1641 , A61K9/5073
摘要： A process for preparing a coated composition comprising a pharmaceutically active substance stable to heat, which comprises centrifugally granualting a mixture comprising said active substance and a first thermomelting material as a binder under heating without using any solvent and coating the resultant granules with a second thermomelting material as a coating material under heating, the melting point of the second thermomelting material being lower than that of the first thermomelting material.
摘要翻译： 一种制备包含对热稳定的药物活性物质的包衣组合物的方法，其包括在不使用任何溶剂的情况下将加入包含所述活性物质和第一热熔融材料的混合物作为粘合剂进行离心成型，并用第二热熔胶材料 作为加热时的涂料，第二热塑性材料的熔点低于第一热塑性材料的熔点。
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公开(公告)号：US4402692A
公开(公告)日：1983-09-06
申请号：US269706
申请日：1981-06-02
申请人： Yasushi Takagishi , Yoshio Doi , Kanji Aita , Noboru Hoshi
发明人： Yasushi Takagishi , Yoshio Doi , Kanji Aita , Noboru Hoshi
CPC分类号： A61K9/025 , A61K9/4816 , Y10S514/962
摘要： The invention provides a novel and efficient means for the administration of a therapeutically effective ingredient by rectal application in the form of a medicament capsule encapsulating the effective ingredient. The medicament capsule according to the invention is formed of a hard capsule shell made of a mixed ester of a cellulose ether, e.g. alkyl-, hydroxyalkyl- and hydroxyalkyl alkylcelluloses, esterified with aliphatic monacyl groups and acidic succinyl groups. When the capsule is inserted into the rectum, the capsule shell is disintegrated and the rectally absorbable effective ingredient is readily and smoothly released into the rectum and absorbed to exhibit therapeutical effects as efficiently as with conventional suppositories.
摘要翻译： 本发明提供了一种用于通过直肠施用以包封有效成分的药物胶囊的形式施用治疗有效成分的新型和有效的方法。 根据本发明的药物胶囊由纤维素醚混合酯制成的硬胶囊壳形成。 烷基，羟基烷基和羟烷基烷基纤维素，用脂族单酰基和酸性琥珀酰基酯化。 当胶囊插入直肠时，胶囊壳崩解，直肠可吸收的有效成分容易平稳地释放到直肠中并被吸收以显示与常规栓剂一样有效的治疗效果。
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公开(公告)号：US4397835A
公开(公告)日：1983-08-09
申请号：US372791
申请日：1982-04-28
申请人： Yasushi Takagishi , Yoshio Doi , Noboru Hoshi
发明人： Yasushi Takagishi , Yoshio Doi , Noboru Hoshi
IPC分类号： A61K9/48
CPC分类号： A61K9/4858 , A61K9/4816 , A61K9/485
摘要： The invention provides a novel means for overcoming the problem of undue and irregular delay in the exhibition of the effect of medicine when a patient is administrated with an enterosoluble hard-capsulated medicament. The unexpected discovery that the key parameter ruling the smooth transfer of an enterosoluble capsule from the stomach to the intestinal canals is the overall specific gravity of the capsule has led to the establishment of the invention which proposes an enterosoluble hard-capsulated medicament having an overall specific gravity of at least 1.05 or, preferably, at least 1.10.
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