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1. 发明专利

JP2007332101A Enteric granule and method for producing the same 有权
标题翻译：有效颗粒及其制造方法
公开(公告)号：JP2007332101A
公开(公告)日：2007-12-27
申请号：JP2006167814
申请日：2006-06-16
申请人： Shin Etsu Chem Co Ltd , Toa Eiyo Ltd , トーアエイヨー株式会社 , 信越化学工業株式会社
发明人： TANJI CHIKANORI , MATSUI TADASHI , YUASA SHIYUUICHIROU , NISHIYAMA YUICHI , ITO YUICHI , FUKUI IKUO
IPC分类号： A61K47/38 , A61K9/16 , A61K47/14
CPC分类号： A61K9/1688 , A61K9/1652 , A61K9/5026 , A61K9/5042 , A61K9/5073
摘要： PROBLEM TO BE SOLVED: To provide enteric granules in which elution to water is suppressed in a low coating amount and to provide a method for producing the enteric granules. SOLUTION: The enteric granules comprise raw granules or granules containing the raw granules and one or more layers for applying the raw granules, a first enteric layer for applying the raw granules or granules and a second enteric layer thereon, and the first enteric layer and the second enteric layer each contains hydroxypropylmethyl cellulose acetate succinate (HPMCAS) which are different in dissolution pH and the dissolution pH of HPMCAS of the second enteric layer is lower than the dissolution pH of HPMCAS of the first enteric layer. The method for producing the enteric granules comprises a step for forming the first enteric layer by coating raw granules or granules containing one or more layers for applying the raw granules with an enteric coating agent containing HPMCAS and a step for forming the second enteric layer on the first enteric layer by using an enteric coating agent containing HPMCAS having dissolution pH which is lower than that of the above HPMCAS. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供以低涂布量抑制洗脱水的肠溶颗粒，并提供生产肠溶颗粒的方法。解决方案：肠溶颗粒包含含有原料颗粒的原料颗粒或颗粒和用于施加原料颗粒的一层或多层，用于施加原料颗粒或颗粒的第一肠溶层和其上的第二肠溶层，以及第一肠层和第二肠溶层各自含有溶解pH不同的羟丙基甲基纤维素乙酸琥珀酸酯（HPMCAS）和第二肠溶层的HPMCAS的溶解pH低于第一肠溶层的HPMCAS的溶解pH。肠溶颗粒的制造方法包括以下步骤：通过将包含一层或多层的原料颗粒或颗粒用含有HPMCAS的肠溶包衣剂涂敷原料颗粒并在其上形成第二肠溶层的步骤来形成第一肠溶层通过使用含有低于上述HPMCAS溶出度的pH值的HPMCAS的肠溶包衣剂来进行第一肠溶层。版权所有（C）2008，JPO＆INPIT

2. 发明专利

JP2007332102A Enteric granule and method for producing the same 有权
标题翻译：有效颗粒及其制造方法
公开(公告)号：JP2007332102A
公开(公告)日：2007-12-27
申请号：JP2006167815
申请日：2006-06-16
申请人： Toa Eiyo Ltd , トーアエイヨー株式会社
发明人： TANJI CHIKANORI , MATSUI TADASHI , YUASA SHIYUUICHIROU
IPC分类号： A61K31/7076 , A61K9/62 , A61K47/14 , A61K47/38 , A61P1/04 , A61P1/08 , A61P1/14 , A61P9/04 , A61P9/08 , A61P9/10 , A61P17/00 , A61P25/00 , A61P27/02
摘要： PROBLEM TO BE SOLVED: To provide enteric granules in which elution to water is suppressed in a low coating amount, in the enteric granules containing adenosine triphosphate or its pharmaceutically permissible salt as a pharmaceutically effective component, and to provide a method for producing the enteric granules.
SOLUTION: The enteric granules comprise raw granules carrying adenosine triphosphate or its pharmaceutically permissible salt as a pharmaceutical effective component or granules containing the raw granules and one or more layers for applying the raw granules, a first enteric layer for applying the raw granules or the granules and a second enteric layer thereon, and the first enteric layer and the second enteric layer each contains hydroxypropylmethyl cellulose acetate succinate (HPMCAS) which are different in dissolution pH and the dissolution pH of HPMCAS of the second enteric layer is lower than the dissolution pH of HPMCAS of the first enteric layer. The method for producing the enteric granules is also provided.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：为了提供以低涂布量抑制洗脱水的肠溶颗粒，在含有三磷酸腺苷或其药学上允许的盐作为药学上有效成分的肠溶颗粒中，提供一种生产方法肠溶颗粒。解决方案：肠溶颗粒包含携带三磷酸腺苷或其药学上可允许的盐作为药物有效成分或含有原料颗粒的颗粒的原料颗粒和用于施加原料颗粒的一层或多层，用于施加原料颗粒的第一肠溶层或颗粒和第二肠溶层，第一肠溶层和第二肠溶层各自含有溶解pH不同的羟丙基甲基纤维素乙酸琥珀酸酯（HPMCAS）和第二肠溶层的HPMCAS的溶解pH低于第一肠溶层的HPMCAS的溶出pH。还提供了生产肠溶颗粒的方法。版权所有（C）2008，JPO＆INPIT

3. 发明专利

JP2007186499A Bisoprolol-containing adhesive preparation 有权
标题翻译：含双酚A的粘合剂制剂
公开(公告)号：JP2007186499A
公开(公告)日：2007-07-26
申请号：JP2006328922
申请日：2006-12-06
申请人： Nitto Denko Corp , Toa Eiyo Ltd , トーアエイヨー株式会社 , 日東電工株式会社
发明人： IWAO YOSHIHIRO , OKUBO KATSUYUKI , OKADA KATSUHIRO , MINAMI KUNIHIRO , YUASA SHIYUUICHIROU
IPC分类号： A61K47/10 , A61K9/70 , A61K31/138 , A61K47/32 , A61P25/02
CPC分类号： A61K9/7053 , A61K31/138 , A61K47/10 , A61K47/32
摘要： PROBLEM TO BE SOLVED: To provide an adhesive preparation for percutaneously administering free base of bisoprolol into a living body, which uses a polyisobutylene-based adhesive as an adhesive, inhibits the bleeding of the free base of bisoprolol, and has sufficient adhesive characteristics.
SOLUTION: This bisoprolol-containing adhesive preparation 10 is characterized by laminating an adhesive layer 2 to one side of a support 1. This adhesive layer 2 comprises a 12 to 28C branched monohydric alcohol, the free base of bisoprolol, and a polyisobutylene-based adhesive. Thereby, the compatibility of the polyisobutylene-based adhesive with the free base of the bisoprolol can specifically be enhanced. Consequently, the amount of the free base of the bisoprolol can be increased, and the bleeding of the free base of the bisoprolol from the adhesive layer can be prevented. Sufficiently adhesive characteristics on practical aspects can be obtained.
COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：为了提供一种用于将使用聚异丁烯类粘合剂作为粘合剂的比索洛尔的游离碱经皮给药的生物体的粘合剂，抑制比索洛尔的游离碱的渗出，并且具有足够的粘合剂特点。解决方案：该含比索洛列的粘合剂制剂10的特征在于将粘合剂层2层压到载体1的一侧。该粘合剂层2包含12至28℃的支链一元醇，比索洛韦的游离碱和聚异丁烯的粘合剂。由此，能够提高聚异丁烯类粘合剂与比索洛尔的游离碱的相容性。因此，可以增加比索洛尔的游离碱的量，并且可以防止比索洛尔的游离碱从粘合剂层渗出。可以获得实用方面的足够的粘合特性。版权所有（C）2007，JPO＆INPIT

4. 发明专利

JP2007099759A Adhesive preparation containing bisoprolol 有权
标题翻译：包含双酚的胶体制剂
公开(公告)号：JP2007099759A
公开(公告)日：2007-04-19
申请号：JP2006235270
申请日：2006-08-31
申请人： Nitto Denko Corp , Toa Eiyo Ltd , トーアエイヨー株式会社 , 日東電工株式会社
发明人： IWAO YOSHIHIRO , OKUBO KATSUYUKI , OKADA KATSUHIRO , MINAMI KUNIHIRO , YUASA SHIYUUICHIROU
IPC分类号： A61K31/138 , A61K9/70 , A61K47/10 , A61K47/14 , A61K47/32 , A61P9/06 , A61P9/10 , A61P9/12 , A61P43/00
CPC分类号： A61K31/138 , A61K9/7053
摘要： PROBLEM TO BE SOLVED: To provide an adhesive preparation which has a low irritation to the skin surface, excellent in stability of bisoprolol in the preparation and further capable of continuously administrating a pharmacologically effective amount of bisoprolol to the living body. SOLUTION: The adhesive preparation 10 has a support 1 and an adhesive layer 2 which is layered on one surface of the support 1. The adhesive layer 2 is characterized by containing bisoprolol, polyisobutylene, a tackifier and an organic liquid component which is compatible with polyisobutylene and the tackifier. By this, the adhesive preparation having good skin adhesiveness, low skin irritation and reduced pain or adhesive residue at the time of removal from the skin surface can be provided. Further, the adhesive preparation in which the stability of bisoprolol in the adhesive preparation is excellent and the pharmacologically effective amount of bisoprolol can be continuously administrated to the living body through the skin surface is provided. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供一种对皮肤表面具有低刺激性的粘合剂，比索洛尔在制剂中的稳定性优异，并且还能够将有效量的比索洛尔连续施用于生物体。粘合剂制剂10具有层叠在载体1的一个表面上的载体1和粘合剂层2.粘合剂层2的特征在于含有比索洛尔，聚异丁烯，增粘剂和有机液体组分，其为与聚异丁烯和增粘剂相容。由此，可以提供从皮肤表面去除时具有良好的皮肤粘合性，低皮肤刺激性和减轻的疼痛或粘合剂残留的粘合剂。此外，提供粘合剂制备中比索洛尔的稳定性优异且比索洛尔的药理学有效量可以通过皮肤表面连续施用于生物体的粘合剂。版权所有（C）2007，JPO＆INPIT

5. 发明专利

JPH04364127A MEDICINAL PREPARATION CONTAINING CYCLOHEPTENOPYRIDINE DERIVATIVE OR ITS SALT AND ITS PREPARATION 失效
公开(公告)号：JPH04364127A
公开(公告)日：1992-12-16
申请号：JP16346891
申请日：1991-06-10
申请人： TOA EIYO LTD
发明人： YUASA SHIYUUICHIROU , NISHINOMIYA YOZO
IPC分类号： A61K31/44 , A61K47/02 , A61K47/18 , A61K47/26 , A61P1/04
摘要： PURPOSE:To improve the stability of a solid preparation containing a cycloheptenopyridine derivative useful as an antiulcer agent or its salt as an active component. CONSTITUTION:The objective solid medicinal preparation having remarkably improved stability and useful as an antiulcer agent is produced by compounding (A) a compound of formula (R is H or lower alkyl; R is H, lower alkoxy or substituted lower alkoxy; R is H or halogen) or its salt with (B) an amine exhibiting liquid state at normal temperature or soluble in an alcoholic solvent, preferably mono- to triethanolamine, ethylenediamine or diisopropanolamine, (C) a basic inorganic salt, preferably having a pH of >=9 in the form of 0.1(W/V)% aqueous solution or suspension, especially MgO, Mg(OH)2 or CaCO3 and (D) a non-reducing sugar, preferably maltitol, mannitol or lactitol. Preferably, the amount of the component B is 0.0001-1 pt.wt. per 1 pt.wt. of the component A and that of the component C and D is 5-50wt.% each based on the total preparation.

6. 发明专利

JP2002154960A STABLE VASODILATOR AND METHOD FOR PRODUCING THE SAME 失效
公开(公告)号：JP2002154960A
公开(公告)日：2002-05-28
申请号：JP2000353473
申请日：2000-11-20
申请人： TOA EIYO LTD
发明人： YUASA SHIYUUICHIROU , SEGAWA ISATAKE
IPC分类号： A61K9/20 , A61K31/47 , A61K47/26 , A61K47/38 , A61P9/08
摘要： PROBLEM TO BE SOLVED: To provide a vasodilator in the form of tablets suppressed in whisker generation, maintaining sufficient tablet hardness during compression and preservation and enabling the isosorbitol-5-mononitrate as the active ingredient to be run out relatively quickly. SOLUTION: This stable vasodilator in the form of tablets comprises isosorbitol-5-mononitrate as the active ingredient and anhydrous lactose as the vehicle.

7. 发明专利

JP2002326927A QUICK-RELEASING TABLET CONTAINING METFORMIN HYDROCHLORIDE 失效
公开(公告)号：JP2002326927A
公开(公告)日：2002-11-15
申请号：JP2001136873
申请日：2001-05-08
申请人： TOA EIYO LTD
发明人： MATSUI TADASHI , YUASA SHIYUUICHIROU
IPC分类号： A61K9/20 , A61K31/155 , A61K47/38 , A61P3/10
摘要： PROBLEM TO BE SOLVED: To provide quick-releasing tablets of metformin hydrochloride, capable of improving dosing feeling, because the tablets can be prepared in small size, being medically remarkably useful and exhibiting effects such as excellent productivity and storage stability. SOLUTION: The quick-releasing tablets are characterized by comprising (A) metformin hydrochloride and (B) hydroxypropyl cellulose in which viscosity of 2 mass % aqueous solution at 20 deg.C is 2.0-10.0 mPas.

8. 发明专利

JPH05112452A MEDICAL COMPOSITION CONTAINING CYCLOHEPTENOPYRIDINE DERIVATIVE OR ITS SALT 失效
公开(公告)号：JPH05112452A
公开(公告)日：1993-05-07
申请号：JP14273491
申请日：1991-05-20
申请人： TOA EIYO LTD
发明人： YUASA SHIYUUICHIROU , NISHINOMIYA YOZO
IPC分类号： A61K9/14 , A61K31/435 , A61K47/18 , A61P1/04 , C07D401/12
摘要： PURPOSE:To obtain a stabilized medical composition by blending a cycloheptenopyridine derivative with an amine showing a liquid state or soluble in an alcoholic solvent respectively at the ordinary temperature. CONSTITUTION:A compound of the formula (R is H or lower alkyl; R is H, lower alkoxy or substituted lower alkoxy; R is H or halogen) or its salt, e.g. sodium 9-(benzimidazol-2-yl)sulfinyl-4-methoxy-2,3-cycloheptenopyridinium is blended with an amine showing a liquid state or soluble in an alcoholic solvent respectively at the ordinary temperature, e.g. monoethanolamine. The amount of the amine blended is 0.0001-1 pts.wt. based on 1 pts.wt. compound of the formula. Preparation into a tablet, a granule, a powder, an injection, etc., is possible by suitably blending an additive and using the conventional method. The compound of the formula is useful as an antiulcer agent and excellent in gastric inhibitory effect.

9. 发明专利

JP2001354560A SUSTAINED RELEASE TABLET COMPRISING ISOSORBIDE-5- MONONITRATE AS ACTIVE INGREDIENT AND METHOD FOR PRODUCING THE SAME 失效
公开(公告)号：JP2001354560A
公开(公告)日：2001-12-25
申请号：JP2000171201
申请日：2000-06-07
申请人： TOA EIYO LTD
发明人： YUASA SHIYUUICHIROU , MATSUI TADASHI , NAGAI MASAHIKO
IPC分类号： A61K9/22 , A61K31/34 , A61K47/04 , A61K47/38 , A61P9/10
摘要： PROBLEM TO BE SOLVED: To obtain a sustained release tablet comprising isosorbide-5- mononitrate as an active ingredient, capable of maintaining a change in concentration in plasma by administration daily at a time and excellent in preservation stability and compression moldability. SOLUTION: This sustained release tablet comprising isosorbide-5-mononitrate is obtained by carrying out direct compression molding of a mixed powder containing the isosorbide-5-mononitrate as an active ingredient, hydroxypropyl methyl cellulose as a sustainedly releasing agent and a synthetic hydrotalcite as an excipient.

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