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1. 发明专利

JP2011140527A Dosage formulation of ultrasound contrast agent 审中-公开
标题翻译：超声对比剂的剂量配方
公开(公告)号：JP2011140527A
公开(公告)日：2011-07-21
申请号：JP2011094529
申请日：2011-04-20
申请人： Acusphere Inc , アキュスフィア, インコーポレイテッド
发明人： WALOVITCH RICHARD , BERNSTEIN HOWARD , CHICKERING DONALD E III , STRAUB JULIE
IPC分类号： A61K49/00 , A61K9/10 , A61K9/14 , A61K47/06 , A61K47/24 , A61K47/26 , A61K47/34
摘要： PROBLEM TO BE SOLVED: To provide dosage formulations including microparticles which provide enhanced images of long duration, and to provide a kit for administering the dosage formulations including the microparticles for use in the ultrasound imaging technology.
SOLUTION: Clinical studies have been conducted and specific dosage formulations have been developed which provides significantly enhanced images of long duration by using polymeric microparticles. The polymeric microparticles have incorporated therein perfluorocarbon gases. The dosage formulation includes microparticles formed of a biocompatible polymer, preferably including a lipid incorporated therein, and containing a perfluorocarbon that is a gas at body temperature. The microparticles are provided to a patient in an amount effective to enhance ultrasound imaging in the cardiac ventricle for more than 5 minutes or in the myocardium for more than a minute, (in a dose ranging from 0.025 to 8.0 mg microparticles/kg body weight).
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供包括提供长时间增强图像的微粒的剂型，并提供用于施用包含用于超声成像技术的微粒的剂型。解决方案：已经进行了临床研究，并且开发了具体的剂型，其通过使用聚合物微粒提供了显着增强的持续时间的图像。聚合物微粒中已加入全氟化碳气体。剂量制剂包括由生物相容性聚合物形成的微粒，其优选包括掺入其中的脂质，并且含有在体温下作为气体的全氟化碳。将微粒以有效增强心室超声波成像超过5分钟或心肌超过一分钟（剂量范围为0.025至8.0mg微粒/ kg体重）的量提供给患者，。版权所有（C）2011，JPO＆INPIT

2. 发明申请

WO2007070843A3 PROCESSES FOR MAKING PARTICLE-BASED PHARMACEUTICAL FORMULATIONS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：制造基于粒子的药物制剂进行口腔管理的方法
公开(公告)号：WO2007070843A3
公开(公告)日：2007-10-25
申请号：PCT/US2006062073
申请日：2006-12-14
申请人： ACUSPHERE INC , ALTREUTER DAVID , BERNSTEIN HOWARD , BRITO LUIS A , BRITO SHAINA , CHICKERING DONALD E III , HUANG ERIC K , JAIN RAJEEV , NARASIMHAN SRIDHAR , STRAUB JULIE A
发明人： ALTREUTER DAVID , BERNSTEIN HOWARD , BRITO LUIS A , BRITO SHAINA , CHICKERING DONALD E III , HUANG ERIC K , JAIN RAJEEV , NARASIMHAN SRIDHAR , STRAUB JULIE A
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20
CPC分类号： A61K9/145 , A61K9/0056 , A61K9/0095 , A61K9/2072 , A61K9/2077 , A61K9/2095
摘要： A method is provided for making an oral dosage form of a pharmaceutical agent which includes the steps of (a) providing particles which include a pharmaceutical agent; (b) blending the particles with particles of a pre-processed excipient to form a primary blend, wherein the pre-processed excipient is prepared by (i) dissolving a bulking agent (e.g., a sugar) and at least one non-friable excipient (e.g., a waxy or liquid surfactant) in a solvent to form an excipient solution, and (ii) removing the solvent from the excipient solution to form the pre-processed excipient in dry powder form; (c) milling the primary blend to form a milled pharmaceutical formulation blend that includes microparticles or nanoparticles of the pharmaceutical agent; and (d) processing the milled pharmaceutical formulation blend into a solid oral dosage form or liquid suspension for oral administration. The process yields formulations having improved wettability or dispersibility.
摘要翻译：提供了制备药剂口服剂型的方法，其包括以下步骤：（a）提供包含药剂的颗粒; （b）将颗粒与预处理的赋形剂的颗粒混合以形成初级共混物，其中预处理的赋形剂通过以下步骤制备：（i）将填充剂（例如糖）和至少一种不易碎的赋形剂（例如，蜡状或液体表面活性剂）在溶剂中形成赋形剂溶液，和（ii）从赋形剂溶液中除去溶剂以形成干粉末形式的预处理赋形剂; （c）研磨初级共混物以形成研磨的药物配方混合物，其包括药剂的微粒或纳米颗粒; 和（d）将经研磨的药物制剂混合物加工成固体口服剂型或用于口服给药的液体悬浮液。该方法产生具有改善的润湿性或分散性的制剂。

3. 发明申请

WO0072827A9 POROUS DRUG MATRICES AND METHODS OF MANUFACTURE THEREOF 审中-公开
标题翻译：多糖药物及其制造方法
公开(公告)号：WO0072827A9
公开(公告)日：2002-01-31
申请号：PCT/US0014578
申请日：2000-05-25
申请人： ACUSPHERE INC
发明人： STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E III , KHATAK SARWAT , RANDALL GREG
IPC分类号： A61K9/14 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/16 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/12 , A61K47/26 , A61K47/34
CPC分类号： A61K9/1635 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solutions, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral admisnistration. Paclitaxel or docetaxel can be provided in a porous matrix form, which allows the drug to be formulated without solubilizing agents and administered as a bolus. rocessed using standard techniques into tablets or capsules for oral administration. Paclitaxel or docetaxel can be provided in a porous matrix form, which allows the drug to be formulated without solubilizing agents and administered as a bolus.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成乳液，悬浮液或第二溶液，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生药物的多孔基质。成孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服药物的片剂或胶囊。紫杉醇或多西紫杉醇可以以多孔基质形式提供，其允许药物配制而不含增溶剂并作为大剂量给药。使用标准技术加工成用于口服给药的片剂或胶囊。紫杉醇或多西紫杉醇可以以多孔基质形式提供，其允许药物配制而不含增溶剂并作为大剂量给药。

4. 发明专利

TWI246426B 供用作為顯像劑之微囊封的氟化氣體 MICROENCAPSULATED FLUORINATED GASES FOR USE AS IMAGING AGENTS 失效
简体标题：供用作为显像剂之微囊封的氟化气体 MICROENCAPSULATED FLUORINATED GASES FOR USE AS IMAGING AGENTS
公开(公告)号：TWI246426B
公开(公告)日：2006-01-01
申请号：TW086102918
申请日：1997-03-10
申请人：阿基斯菲爾有限公司 ACUSPHERE, INC.
发明人：哈瓦德.伯恩斯坦 HOWARD BENSTEIN , 茱莉A. 史塔博 JULIE A, STRAUB , 艾迪斯.玫茲歐伊喜 EDITH MATHIOWITZ , 亨利T. 布希 HENRY T. BRUSH , 理查E. 溫 RICHARD E. WING
IPC分类号： A61K
CPC分类号： A61B8/481 , A61K49/223
摘要：本發明，發現將氟化氣體(特別是諸如八氟丙烷之類的全氟化碳)加入合成之聚合性微粒子內，相較於具有空氣併入於其中之微粒子，可顯著地增強回聲作用。該等經微囊封之全氟化碳係以一適合於欲顯像而經鎖定之組織的直徑予以製備，以供，例如，靜脈投藥或口服投藥。在一實施例中，生物黏附性微粒子被形成以用於黏膜表面之增強的顯像。
简体摘要：本发明，发现将氟化气体(特别是诸如八氟丙烷之类的全氟化碳)加入合成之聚合性微粒子内，相较于具有空气并入于其中之微粒子，可显着地增强回声作用。该等经微囊封之全氟化碳系以一适合于欲显像而经锁定之组织的直径予以制备，以供，例如，静脉投药或口服投药。在一实施例中，生物黏附性微粒子被形成以用于黏膜表面之增强的显像。

5. 发明专利

TWI274589B 多孔狀藥物基質及其製造方法 POROUS DRUG MATRICES AND METHOD OF MANUFACTURE THEROF 失效
简体标题：多孔状药物基质及其制造方法 POROUS DRUG MATRICES AND METHOD OF MANUFACTURE THEROF
公开(公告)号：TWI274589B
公开(公告)日：2007-03-01
申请号：TW089110363
申请日：2000-05-29
申请人：阿基斯菲爾有限公司 ACUSPHERE, INC.
发明人：唐納德E. 奇可林 DONALD E. CHICKERING , 沙瓦特.哈塔克 SARWAT KHATTAK , 葛瑞格.藍道爾 GREG RANDALL , 霍華德.伯恩斯登 HOWARD BERNSTEIN , 茱莉葉.司特拉伯 JULIE STRAUB
IPC分类号： A61K
CPC分类号： A61K9/1635 , A61K9/1623 , A61K9/1688 , A61K9/1694
摘要：以較佳為微粒之一多孔狀基質的形式提供藥物，特別是低水溶性的藥物，該形式可增進藥物於含水介質中的溶解度。用以製造該藥物基質之一種較佳的方法包括(i)將一藥物溶解於一揮發性溶劑中以形成一藥物溶液，較佳該藥物的水溶性低；(ii)將至少一種造孔劑與該藥物溶液結合，以形成一乳化液、懸服液或第二溶液；及(iii)自該乳化液、懸服液或第二溶液中除去揮發性溶劑與造孔劑，以製得該藥物的多孔狀基質。該造孔劑可為一種與該藥物溶劑不互溶之揮發性液體，或為一種揮發性固態化合物，較佳為一種揮發性鹽類。在一個較佳的具體例中，係使用噴霧乾燥作用以除去該溶劑與造孔劑。相較於該藥物之非多孔狀基質，所產生的多孔狀基質在投藥至一病人之後，具有較快的溶解速率。在一個較佳的具體例中，以一含水介質將多孔狀藥物基質的微粒重新組成，及以非經腸的方式投藥，或以標準的技術製成口服用的錠劑或膠囊。能於一多孔狀基質的形式中提供派克里泰索(paclitaxel)或多賽泰索(docetaxel)，使得在不需要增溶劑之下得以配方製造該藥物，及能以大丸方式投藥。
简体摘要：以较佳为微粒之一多孔状基质的形式提供药物，特别是低水溶性的药物，该形式可增进药物于含水介质中的溶解度。用以制造该药物基质之一种较佳的方法包括(i)将一药物溶解于一挥发性溶剂中以形成一药物溶液，较佳该药物的水溶性低；(ii)将至少一种造孔剂与该药物溶液结合，以形成一乳化液、悬服液或第二溶液；及(iii)自该乳化液、悬服液或第二溶液中除去挥发性溶剂与造孔剂，以制得该药物的多孔状基质。该造孔剂可为一种与该药物溶剂不互溶之挥发性液体，或为一种挥发性固态化合物，较佳为一种挥发性盐类。在一个较佳的具体例中，系使用喷雾干燥作用以除去该溶剂与造孔剂。相较于该药物之非多孔状基质，所产生的多孔状基质在投药至一病人之后，具有较快的溶解速率。在一个较佳的具体例中，以一含水介质将多孔状药物基质的微粒重新组成，及以非经肠的方式投药，或以标准的技术制成口服用的锭剂或胶囊。能于一多孔状基质的形式中提供派克里泰索(paclitaxel)或多赛泰索(docetaxel)，使得在不需要增溶剂之下得以配方制造该药物，及能以大丸方式投药。

6. 发明申请

WO2007070852A3 PROCESSES FOR MAKING PARTICLE-BASED PHARMACEUTICAL FORMULATIONS FOR PARENTERAL ADMINISTRATION 审中-公开
标题翻译：用于制备基于颗粒的药物制剂用于肠胃外给药的过程
公开(公告)号：WO2007070852A3
公开(公告)日：2007-11-01
申请号：PCT/US2006062094
申请日：2006-12-14
申请人： ACUSPHERE INC , ALTREUTER DAVID , BERNSTEIN HOWARD , BRITO LUIS , BRITO SHAINA , CARNEIRO OLINDA C , CHICKERING DONALD E , HUANG ERIC K , JAIN RAJEEV , NARASIMHAN SRIDHAR , PANDIT NAMRATA , STRAUB JULIE A
发明人： ALTREUTER DAVID , BERNSTEIN HOWARD , BRITO LUIS , BRITO SHAINA , CARNEIRO OLINDA C , CHICKERING DONALD E , HUANG ERIC K , JAIN RAJEEV , NARASIMHAN SRIDHAR , PANDIT NAMRATA , STRAUB JULIE A
IPC分类号： A61K9/14
CPC分类号： A61K9/0019 , A61K9/145 , A61K9/146 , A61K9/19
摘要： A method is provided for making a parenteral dosage form of a pharmaceutical agent which Includes (a) providing particles of a pharmaceutical agent; (b) blending the particles with particles of at least one bulking agent to form a first powder blend, which does not include a surfactant; (c) milling the first powder blend to form a milled blend which comprises microparticles or nanopartides of the pharmaceutical agent; and (d) reconstituting the milled blend with a liquid vehicle, which includes at least one surfactant, for parenteral administration. A method also is provided which includes (a) providing particles of a pharmaceutical agent; (b) blending these particles with particles of an excipient to form a first blend; and (c) milling the first blend to form a milled blend that includes microparticles or tianopartÊcles, which exhibits a greater dispersibility, wettability, and suspcndability as compared to the particles of step (a) or the first blend.
摘要翻译：提供了用于制备药剂的肠胃外剂型的方法，其包括（a）提供药剂颗粒; （b）将所述颗粒与至少一种填充剂的颗粒共混以形成不包含表面活性剂的第一粉末混合物; （c）研磨第一粉末混合物以形成包含药剂的微粒或纳米粒子的研磨混合物; 和（d）用含有至少一种表面活性剂的液体载体重新配制经碾磨的混合物用于肠胃外给药。还提供了一种方法，其包括（a）提供药剂颗粒; （b）将这些颗粒与赋形剂颗粒混合以形成第一混合物; 和（c）研磨第一种共混物以形成包含微粒或天鹅绒的研磨混合物，与步骤（a）或第一种混合物的颗粒相比，该混合物显示出更大的分散性，润湿性和可悬浮性。

7. 发明申请

WO2007070851A2 PROCESSES FOR MAKING PARTICLE-BASED PHARMACEUTICAL FORMULATIONS FOR PULMONARY OR NASAL ADMINISTRATION 审中-公开
标题翻译：制备基于粒子的药物制剂用于肺癌或鼻咽管理的方法
公开(公告)号：WO2007070851A2
公开(公告)日：2007-06-21
申请号：PCT/US2006/062093
申请日：2006-12-14
申请人： ACUSPHERE, INC. , BERNSTEIN, Howard , BRITO, Shaina , CHICKERING, Donald, E. , HUANG, Eric, K. , JAIN, Rajeev , STRAUB, Julie, A.
发明人： BERNSTEIN, Howard , BRITO, Shaina , CHICKERING, Donald, E. , HUANG, Eric, K. , JAIN, Rajeev , STRAUB, Julie, A.
IPC分类号： A61K9/00 , A61K9/14
CPC分类号： A61K9/0075 , A61K9/0043 , A61K9/0073 , A61K9/143 , A61K9/145
摘要： Dry powder pharmaceutical formulations for pulmonary or nasal administration are made to provide an improved respired dose. These formulations may be blends of milled blends and may include a phospholipid, alone or Ên combination with other excipient materials. In one case, the process includes the steps of (a) providing particles which comprise a pharmaceutical agent; (b) blending the particles with particles of at least one first excipient to form a first powder blend; (c) railling the first powder blend to form a milled blend which comprises microparticies or nanoparticles of the pharmaceutical agent; and (d) blending the milled blend with particles of a second excipient to form a blended dry powder blend pharmaceutical formulation suitable for pulmonary or nasal administration.
摘要翻译：制备用于肺或鼻给药的干粉药物制剂以提供改善的呼吸剂量。这些制剂可以是研磨的共混物的混合物，并且可以包括单独的磷脂或与其它赋形剂材料组合的磷脂。在一种情况下，该方法包括以下步骤：（a）提供包含药剂的颗粒; （b）将颗粒与至少一种第一赋形剂的颗粒混合以形成第一粉末混合物; （c）冲击第一粉末混合物以形成包含药剂的微粒或纳米颗粒的研磨混合物; 和（d）将研磨的共混物与第二赋形剂的颗粒混合以形成适于肺或鼻施用的混合的干粉混合药物制剂。

8. 发明申请

WO2004060547A1 METHODS AND APPARATUS FOR MAKING PARTICLES USING SPRAY DRYER AND IN-LINE JET MILL 审中-公开
标题翻译：使用喷雾干燥机和在线喷射机制造颗粒的方法和装置
公开(公告)号：WO2004060547A1
公开(公告)日：2004-07-22
申请号：PCT/US2003/037108
申请日：2003-11-20
申请人： ACUSPHERE, INC.
发明人： CHICKERING, Donald, E., III , NARASIMHAN, Sridhar , ALTREUTER, David , KOPESKY, Paul , KEEGAN, Mark , STRAUB, Julie, A. , BERNSTEIN, Howard
IPC分类号： B01J2/04
CPC分类号： F26B17/102 , A61K9/1647 , A61K9/1688 , B01D1/18 , B01J2/04 , F26B3/12
摘要： Methods and apparatus are provided for making particles comprising: (a) spraying an emulsion, solution, or suspension, which comprises a solvent and a bulk material (e.g., a pharmaceutical agent), through an atomizer (14) and into a primary drying chamber (12), having a drying gas flowing therethrough, to form droplets comprising the solvent and bulk material dispersed in the drying gas; (b) evaporating, in the primary drying chamber (12), at least a portion of the solvent into the drying gas to solidify the droplets and form particles dispersed in drying gas; and (c) flowing the particles and at least a portion of the drying gas through a jet mill (24) to deagglomerate or grind the particles. By coupling spray drying with "in-line" jet milling, a single step process is created from two separate unit operations, and an additional collection step is advantageously eliminated. The one-step, in-line process has further advantages in time and cost of processing.
摘要翻译：提供了用于制备颗粒的方法和装置，包括：（a）通过雾化器（14）将包含溶剂和散装材料（例如药剂）的乳液，溶液或悬浮液喷雾到初级干燥室（12），其具有流过其中的干燥气体，以形成包含分散在干燥气体中的溶剂和散装材料的液滴; （b）在主干燥室（12）中将至少一部分溶剂蒸发到干燥气体中以固化液滴并形成分散在干燥气体中的颗粒; 和（c）使颗粒和至少一部分干燥气体流过喷射磨机（24）以使颗粒解聚或研磨。通过将喷雾干燥与“直列式”喷射式研磨相结合，由两个单独的单元操作产生单步骤，有利地消除了另外的收集步骤。一步一步的在线过程在处理时间和成本方面具有进一步的优势。

9. 发明申请

WO9732609A3 MICROENCAPSULATED FLUORINATED GASES FOR USE AS IMAGING AGENTS 审中-公开
标题翻译：用作成像剂的微型氟化气体
公开(公告)号：WO9732609A3
公开(公告)日：1998-01-29
申请号：PCT/US9703117
申请日：1997-02-27
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , STRAUB JULIE ANN , MATHIOWITZ EDITH , BRUSH HENRY T , WING RICHARD E
IPC分类号： A61K47/06 , A61B8/00 , A61K49/00 , A61K49/22
CPC分类号： A61B8/481 , A61K49/223
摘要： It has been discovered that the incorporation of fluorinated gases, especially a perfluorocarbon such as octafluoropropane, into synthetic polymeric microparticles, significantly enhances echogenicity as compared with microparticles having air incorporated therein. The microencapsulated perfluorocarbon is manufactured with a diameter suitable for the targeted tissue to be imaged, for example, for intravenous or oral administration. In one embodiment, bioadhesive microparticles are formed for enhanced imaging of mucosal surfaces.
摘要翻译：通过在微粒中掺入氟化气体而不是空气来增强超声成像中合成聚合物微粒的回波性的方法是新的。还要求保护的是用于超声成像的组合物，其包含掺入氟化气体以增强成像的合成生物相容性聚合物微粒和药学上可接受的载体。还要求的是制备由具有增强的回声反应性的生物相容性聚合物形成的微粒的方法，包括将生物相容性聚合物的溶液掺入挥发性盐中，然后除去聚合物溶剂和挥发性盐以形成多孔微粒。

10. 发明申请

WO2008060934A2 FORMULATIONS OF TETRAHYDROPYRIDINE ANTIPLATELET AGENTS FOR PARENTERAL OR ORAL ADMINISTRATION 审中-公开
标题翻译：用于肠胃外或口服给药的四氢吡啶抗血小板药物的制剂
公开(公告)号：WO2008060934A2
公开(公告)日：2008-05-22
申请号：PCT/US2007/084040
申请日：2007-11-08
申请人： ACUSPHERE, INC. , BERNSTEIN, Howard , CARNEIRO, Olinda , JAIN, Rajeev A. , PANDIT, Namrata , RANE, Shveta , STRAUB, Julie Ann
发明人： BERNSTEIN, Howard , CARNEIRO, Olinda , JAIN, Rajeev A. , PANDIT, Namrata , RANE, Shveta , STRAUB, Julie Ann
IPC分类号： A61K9/00 , A61K9/107 , A61K9/16 , A61K31/4365
CPC分类号： A61K31/4365 , A61K9/0019 , A61K9/1075 , A61K9/1617 , A61K9/19
摘要： A pharmaceutical composition for the oral or parenteral administration of a compound of Formula (I) comprising an oil in water emulsion, wherein the oil phase comprises the free base of or a pharmaceutically acceptable salt thereof of a compound of Formula (I), and one or more surfactants which are soluble in the oil phase and/or the aqueous phase. The emulsion optionally contains one or more excipients that are soluble in the oil phase and/or the aqueous phase, such as pH modifying agents such as buffers, osmolality/tonicity modifying agents, emulsifying agents, water-soluble polymers, and preservatives. The compound of Formula (I) can be formulated as a solid material and stored until needed. Kits for forming the emulsion are provided. Prior to administration, the solid material can be reconstituted in an aqueous medium to form the emulsion.
摘要翻译：一种用于口服或肠胃外给药式（I）化合物的药物组合物，其包含水包油乳剂，其中所述油相包含化合物的游离碱或其药学上可接受的盐（I）的化合物和一种或多种可溶于油相和/或水相的表面活性剂。乳剂任选含有一种或多种可溶于油相和/或水相的赋形剂，例如pH调节剂如缓冲剂，渗透压/张力调节剂，乳化剂，水溶性聚合物和防腐剂。式（I）化合物可以配制成固体材料并储存直至需要。提供用于形成乳液的试剂盒。在给药之前，固体材料可以在水性介质中重构以形成乳液。

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