公开(公告)号：US20170258723A1

公开(公告)日：2017-09-14

申请号：US15601723

申请日：2017-05-22

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Haruka YOSHIDA ,  Toshiaki TANIGUCHI ,  Tadashi MUKAI

IPC分类号： A61K9/14 ,  A61J3/10 ,  A61K31/496 ,  A61J3/02

CPC分类号： A61K9/14 ,  A61J3/02 ,  A61J3/10 ,  A61K9/2059 ,  A61K31/496 ,  C07D215/227

摘要： [Object] An object of the present invention is to provide an oral solid preparation that can be produced in a simpler manner than conventional methods, that exhibits high bioavailability and high dissolubility even in persons having low stomach acid, and that can also ensure dissolubility after being allowed to stand for a certain period of time. Another object is to provide a simple method for producing the oral solid preparation.[Means for Achieving the Object] The present invention relates to an oral solid preparation comprising, as an active ingredient, a finely milled crystal obtained by milling an aripiprazole hydrate crystal, and a pharmaceutically acceptable carrier, the finely milled crystal having a mean particle size of 15 μm or less; and a method for producing an oral solid preparation comprising the steps of (1) milling an aripiprazole hydrate crystal into a finely milled crystal having a mean particle size of 15 μm or less, and (2) mixing the obtained finely milled crystal with a pharmaceutically acceptable carrier.

公开(公告)号：US09750710B2

公开(公告)日：2017-09-05

申请号：US15049313

申请日：2016-02-22

申请人： Emisphere Technologies, Inc.

发明人： Halina Levchik ,  Shingai Majuru ,  Brahma Singh ,  Jamila Harris

IPC分类号： A61K31/198 ,  A61K9/20 ,  A61K45/06 ,  A61J3/02 ,  C07C235/60

CPC分类号： A61K31/197 ,  A61J3/02 ,  A61K9/2095 ,  A61K31/198 ,  A61K45/06 ,  A61K2300/00 ,  C07C235/60

摘要： The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.

公开(公告)号：US09717795B2

公开(公告)日：2017-08-01

申请号：US14765983

申请日：2014-01-21

申请人： ZHEJIANG HISUN PHARMACEUTICAL CO., LTD

发明人： Chunrong Feng ,  Huanwei Zhang ,  Jianqiao Wang

IPC分类号： A61K31/40 ,  A61K41/00 ,  A61K9/19 ,  A61K31/409 ,  A61K9/00 ,  A61J3/02 ,  A61K9/14

CPC分类号： A61K41/0076 ,  A61J3/02 ,  A61K9/0019 ,  A61K9/143 ,  A61K9/145 ,  A61K9/19 ,  A61K31/409

摘要： Disclosed are a HPPH lyophilized powder injection for injection and the preparation method thereof. The HPPH lyophilized powder injection contains HPPH, auxiliary solvents, solubilizing agents, excipients, and pH adjusting agents. The HPPH lyophilized powder injection is loose and has good resolubility, low moisture, and good stability.

公开(公告)号：US09603794B2

公开(公告)日：2017-03-28

申请号：US14605610

申请日：2015-01-26

申请人： Mahmut Bilgic

发明人： Mahmut Bilgic

IPC分类号： A61K31/545 ,  A61K9/46 ,  A61J3/02 ,  A61K31/424 ,  A61K31/43

CPC分类号： A61K9/0007 ,  A61K31/424 ,  A61K31/43 ,  A61K31/545 ,  A61K2300/00

摘要： The present invention relates to a process for preparing effervescent dosage forms comprising at least one antibiotic of cephalosporin group. The present invention also relates to effervescent formulations and preparations comprising antibiotics of second generation cephalosporin.

公开(公告)号：US20170007502A1

公开(公告)日：2017-01-12

申请号：US15261462

申请日：2016-09-09

申请人： TSUMURA & CO.

发明人： Shoichi TESHIMA ,  Yoshikazu MORI ,  Keiichi NODA

IPC分类号： A61J3/02 ,  A61K45/06 ,  G06F19/00 ,  G01N30/86 ,  G01N30/74

CPC分类号： G01N30/74 ,  G01N30/8631 ,  G01N30/8686 ,  G01N30/88 ,  G01N2030/027 ,  G01N2030/8886 ,  G05B15/00 ,  G16C20/20

摘要： Provided are a method of and an apparatus for formulating a multicomponent drug capable of surely making a multicomponent drug meeting criteria for productization with high accuracy into a product. The method and apparatus obtain a chromatogram from an extract or a base of a multicomponent drug, evaluate whether the base meets the criteria for productization based on the obtained chromatogram with high accuracy, and subject the base determined in the high-accuracy evaluating as an accepted one meeting the criteria to dosage form processing, to produce a formulated drug having a given dosage-form. The high quality evaluation is realized by using fingerprint area segmentation feature values obtained from a fingerprint formed from a chromatogram and segmented into a plurality of areas.

摘要翻译： 本发明提供了一种配制多组分药物的方法和装置，该多组分药物能够将多组分药物高度精确地制成符合产品化标准的产品。 该方法和装置从多组分药物的提取物或碱中获得色谱图，基于获得的色谱图高精度评估基质是否满足产品化标准，并将在高精度评估中确定的碱基作为接受的 一种符合剂型加工的标准，以制备具有给定剂型的配制药物。 通过使用从由色谱图形成的指纹获得的指纹区域分割特征值并分割成多个区域来实现高质量评估。

公开(公告)号：US09452107B2

公开(公告)日：2016-09-27

申请号：US13829948

申请日：2013-03-14

申请人： Ecevit Bilgili ,  Rajesh Dave ,  Anagha Bhakay ,  Mohammad Azad

发明人： Ecevit Bilgili ,  Rajesh Dave ,  Anagha Bhakay ,  Mohammad Azad

IPC分类号： A61J3/00 ,  A61K9/14 ,  A61K9/51 ,  B82Y40/00 ,  A61J3/02

CPC分类号： A61K9/146 ,  A61J3/00 ,  A61J3/02 ,  A61K9/5138 ,  A61K9/5161 ,  A61K31/216 ,  A61K31/343 ,  B05D7/24 ,  B82Y40/00

摘要： The present disclosure provides improved systems and methods utilizing colloidal/ultrafine superdisintegrant-based composite particles for dispersion and/or dissolution of active pharmaceutical agents. In general, the present disclosure utilizes a surfactant-free or near surfactant-free formulation by incorporating a wet milled SDI as a dispersant in the formulation. As such, the present disclosure provides for the preparation of surfactant-free or substantially surfactant-free formulations (e.g., nano-composite micro-particle formulations) by incorporating a wet-milled superdisintegrant (SDI) as the dispersant in the formulations. The advantageous SDI particles (e.g., colloidal/ultrafine SDI particles) of the present disclosure can be used to break-up the aggregates (e.g., nanoparticle aggregates) of the active agents (e.g. poorly water-soluble drugs) in the formulations (e.g., micro-particle formulations) and enhance the recovery of the nanoparticles of active agents during aqueous re-dispersion and their dissolution rate in vitro and in vivo.

摘要翻译： 本公开提供了改进的利用胶体/超细超级基质复合颗粒用于活性药剂的分散和/或溶解的系统和方法。 通常，本公开内容通过在制剂中掺入湿法研磨的SDI作为分散剂来使用无表面活性剂的或接近表面活性剂的制剂。 因此，本公开内容通过在制剂中掺入湿磨超级崩解剂（SDI）作为分散剂来提供制备不含表面活性剂的或基本不含表面活性剂的制剂（例如纳米复合微粒子制剂）。 本公开的有利的SDI颗粒（例如，胶体/超细SDI颗粒）可用于分解制剂中活性剂（例如水不溶性药物）的聚集体（例如，纳米颗粒聚集体）（例如， 微粒子制剂），并且在水分散分散过程中增强活性剂纳米颗粒的回收率及其在体外和体内的溶解速率。

公开(公告)号：US20160271177A1

公开(公告)日：2016-09-22

申请号：US14661529

申请日：2015-03-18

申请人： Yogesh Narayan Bendale ,  Vineeta Yogesh Bendale

发明人： Yogesh Narayan Bendale ,  Vineeta Yogesh Bendale

IPC分类号： A61K33/36 ,  A61J3/02 ,  C01G28/00 ,  C22B30/04 ,  C22B7/00

CPC分类号： A61K33/36 ,  C01G28/005

摘要： The present invention is the process for bio synthesis of novel nano arsenic trioxide defined by its low toxicity, higher bio availability and nano particle size with the aid of buttermilk, goat urine, dolichos biflorous and other plant materials such as ginger, momordica charantia and musa paradisica. The invention is carried out in different steps involving purification of crude form of arsenic trioxide by boiling it with buttermilk, goat urine and extract of dolichos biflorous in subsequent steps, followed by the trituration of the bio purified arsenic trioxide with extracts of ginger and momordica charantia in subsequent steps and heating of the dry product obtained after trituration with musa paradisica resulting in the production of novel nano arsenic trioxide. The said novel product is effective in the treatment of various diseases including different types of cancer in animals, humans. The novel nano arsenic trioxide obtained through the present inventive process is less toxic with higher bio availability. Its applicability extends to treatment of plants, agriculture, nano technology and other fields where arsenic trioxide can be used.

摘要翻译： 本发明是通过其低毒性，较高的生物可利用性和纳米粒度的生物合成方法，借助于酪乳，山羊尿，双酚疽和其他植物材料如姜，苦瓜和麝香 paradisica。 本发明以涉及纯化粗三水氧化砷的步骤进行，其步骤包括用酪乳，山羊尿和双酚黑提取物，然后用生姜和苦瓜的提取物研磨生物纯化的三氧化二砷 在随后的步骤中，加热用玄参研磨后得到的干燥产物，产生新的纳米三氧化二砷。 所述新产品在动物，人类中治疗各种疾病，包括不同类型的癌症是有效的。 通过本发明方法获得的新型纳米三氧化砷在较高的生物利用度下毒性较小。 其适用范围扩展到植物，农业，纳米技术和其他可以使用三氧化二砷的领域的处理。

公开(公告)号：US20160193341A1

公开(公告)日：2016-07-07

申请号：US14844493

申请日：2015-09-03

申请人： Paladin Labs Inc. ,  Paladin Labs Europe Limited ,  Paladin Labs (Barbados) Inc.

发明人： Francois Ravenelle ,  Sandra Gori ,  David Lessard ,  Laibin Luo ,  Dorothee Le Garrec ,  Damon Smith

IPC分类号： A61K47/34 ,  A61K9/107 ,  A61K31/05 ,  B01F3/08 ,  A61J3/02 ,  A61K31/085 ,  A61K31/47 ,  A61K9/00 ,  A61K9/19

摘要： The instant invention relates to a solid product comprising a liquid biologically active agent which is intimately associated to a stabilizing agent; particularly a solid product that can be reconstituted to a clear, stable, stabilized nanodispersion or loaded micelles comprising a polymer as a stabilizing agent and a liquid, preferably water immiscible, biologically active agent. The instant invention is further directed toward a process for the production of the above solid product; particularly to micelles or nanodispersions produced by hydration of a cake or powder of the solid product, produced via an effective treatment of a stabilized solution comprising for example a polymer as a stabilizing agent, such as an amphiphilic block copolymer or a small molecular weight surfactant, loaded with a liquid biologically active agent, such as propofol, an optional additive, and a suitable solvent.

摘要翻译： 本发明涉及包含与稳定剂紧密结合的液体生物活性剂的固体产品; 特别是可以重构为透明，稳定，稳定的纳米分散体或负载胶束的固体产物，其包含作为稳定剂的聚合物和液体，优选与水不混溶的生物活性剂。 本发明进一步涉及生产上述固体产品的方法; 特别是通过有效处理包含例如作为稳定剂的聚合物如两亲性嵌段共聚物或小分子量表面活性剂的稳定溶液产生的固体产物的饼或粉末的水合产生的胶束或纳米分散体， 装载有液体生物活性剂，例如丙泊酚，任选的添加剂和合适的溶剂。

公开(公告)号：US20160045396A1

公开(公告)日：2016-02-18

申请号：US14860578

申请日：2015-09-21

申请人： Chang Lee ,  Tao Tom Du

发明人： Chang Lee ,  Tao Tom Du

IPC分类号： A61J3/02 ,  A61K9/16 ,  A61K9/00 ,  A61K31/573 ,  A61K31/58

CPC分类号： A61J3/02 ,  A61K9/0019 ,  A61K9/0075 ,  A61K31/56 ,  A61K31/57 ,  A61K31/573 ,  A61K31/58

摘要： The present invention relates to a pharmaceutical formulation powder that contains 17α-hydroxyprogesterone caproate (17-OHPC) powder and the method of producing the formulation produces particles that are suitable as an inhalant. The formulations, methods and kits of powdered 17-OHPC as taught herein may be used to reduce cytokine interleukin-17 (IL-17 or IL-17A) levels in both broncheoalveolar lavage fluid (BALF) and blood/serum and involve the inhibition of p38 mitogen activating protein kinase (MAPK) activity. The 17-OHPC powder formulation may be used in a method to treat IL-17 cytokine and/or p38 MAPK mediated auto-immune and auto-inflammatory diseases. Such diseases may include glucocorticoid (GC) insensitive related diseases or conditions. In alternate embodiment, the formulation may include the combined use of budesonide (BUD) and/or fluticasone with 17-OPHC.

摘要翻译： 本发明涉及含有17α-羟基孕酮己酸酯（17-OHPC）粉末的药物制剂粉末，并且制备该制剂的方法产生适合作为吸入剂的颗粒。 本文教导的粉末状17-OHPC的制剂，方法和试剂盒可用于减少支气管肺泡灌洗液（BALF）和血液/血清中的细胞因子白细胞介素-17（IL-17或IL-17A）水平，并且涉及抑制 p38丝裂原活化蛋白激酶（MAPK）活性。 17-OHPC粉末制剂可用于治疗IL-17细胞因子和/或p38MAPK介导的自身免疫和自身炎症性疾病的方法。 这些疾病可能包括糖皮质激素（GC）不敏感的相关疾病或病症。 在替代实施方案中，制剂可以包括布地奈德（BUD）和/或氟替卡松与17-OPHC的组合使用。

公开(公告)号：US09138381B2

公开(公告)日：2015-09-22

申请号：US14175635

申请日：2014-02-07

申请人： BASF SE

发明人： Andreas Kempter ,  Max Siebert ,  Heidrun Debus

IPC分类号： B01D1/18 ,  B01J2/04 ,  A61J3/02 ,  A61K9/14 ,  A61K31/192 ,  A61K31/415 ,  A61K31/58 ,  A61J3/00

CPC分类号： A61K9/1682 ,  A61J3/005 ,  A61J3/02 ,  A61K9/143 ,  A61K9/145 ,  A61K9/1611 ,  A61K9/1617 ,  A61K31/192 ,  A61K31/415 ,  A61K31/496 ,  A61K31/565 ,  A61K31/58 ,  B01D1/18 ,  B01J2/04

摘要： Process for producing composite materials by reactive spray-drying, where a liquid phase A, which comprises inorganic cations, and a liquid phase B, which comprises anions which, with the inorganic cations, form a salt that is insoluble in the mixture of the liquid phases are sprayed together using at least one multi-substance nozzle, and where at least one hydrophobic active ingredient is present in dissolved form in at least one liquid spraying phase, and where the salt formed from the cations of phase A and the anions of phase B has a solubility of less than 0.02 mol/l in the neutral aqueous medium.

摘要翻译： 通过反应性喷雾干燥制备复合材料的方法，其中包含无机阳离子的液相A和液相B，其包含阴离子，其与无机阳离子形成不溶于液体混合物的盐 使用至少一种多物质喷嘴将相分散在一起，并且其中至少一种疏水活性成分以溶解的形式存在于至少一个液体喷射相中，并且其中由相A的阳离子和相的阴离子形成的盐 B在中性水性介质中的溶解度小于0.02mol / l。