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    • 75. 发明公开
    • 인간 성장 호르몬의 안정화된 액상 제제용 조성물
    • 用于稳定的液体配制的组合物,其最小化人类生长激素(HGH)的去除,聚合物形成和氧化分解
    • KR1020050023875A
    • 2005-03-10
    • KR1020030061434
    • 2003-09-03
    • 한미사이언스 주식회사
    • 양근희정성엽김영민권세창이관순
    • A61K9/08
    • A61K9/08A61K38/27A61K47/10A61K47/26
    • PURPOSE: A composition for stabilized liquid formulation of human growth hormone is provided, which composition minimizes deamidation, polymer formation and oxidative dissociation of human growth hormone(hGH), so that the stability of the liquid formulation can be improved. CONSTITUTION: The composition for stabilized liquid formulation of human growth hormone comprises 1 to 10 mg/ml of human growth hormone(hGH), 5 to 100 mM of buffering agent, 0.001 to 20 mg/ml of polyethylene glycol(PEG) and 5 to 100 mg/ml of tonicity adjustment agent, wherein the human growth hormone is recombinant methionyl human growth hormone or recombinant natural human growth hormone; the buffering agent is sodium citrate; the tonicity adjustment agent comprises sodium chloride, mannitol and a mixture thereof; and the composition has pH 5.5 to 6.5.
    • 目的:提供用于人生长激素稳定液体制剂的组合物,该组合物使得人类生长激素(hGH)的脱酰胺化,聚合物形成和氧化解离最小化,从而可以提高液体制剂的稳定性。 组成:人生长激素稳定液体制剂的组合物包含1至10mg / ml人生长激素(hGH),5至100mM缓冲剂,0.001至20mg / ml聚乙二醇(PEG)和5至 100mg / ml张力调节剂,其中人生长激素是重组甲硫氨酰人生长激素或重组天然人生长激素; 缓冲剂是柠檬酸钠; 张力调节剂包括氯化钠,甘露醇及其混合物; 组合物的pH为5.5〜6.5。
    • 76. 发明公开
    • 고순도 1-안드로스텐 유도체의 제조 방법
    • 在高效制备高纯度1-安定剂衍生物的方法
    • KR1020050010320A
    • 2005-01-27
    • KR1020030049529
    • 2003-07-19
    • 한미사이언스 주식회사
    • 문영호김동준박철현이경익이재철이관순장영길
    • C07J43/00
    • C07J43/00
    • PURPOSE: A method for preparing highly pure 1-androstene derivatives is provided to produce 1-androstene derivatives, particularly finasteride easily in a high yield and a high purity. CONSTITUTION: The method for preparing the highly pure 1-anderostene derivatives represented by formula 1 comprises reacting 2-iodo-androstane derivatives represented by formula 12(wherein, R is -OH, -OR1 or -NHR2; R1 is a lower linear or branched alkyl of C1 to C5; R2 is a lower linear or branched alkyl of C1 to C5 or 2,5-bis(trifluoromethyl)phenyl) with an oxidant. The oxidant is selected from the group consisting of m-chloroperbenzoic acid, peracetic acid, trifluoro peracetic acid, permaleic acid, sodium bromide, sodium hypochloride, hydrogen peroxide, iodoso-methyl benzene and iodoso-benzene.
    • 目的:提供一种制备高纯度1-雄甾烯衍生物的方法,以高产率和高纯度方便地制备1-雄甾烯衍生物,特别是非那雄胺。 构成:制备由式1表示的高纯度1-降冰片烯衍生物的方法包括使由式12表示的2-碘 - 雄甾烷衍生物(其中,R是-OH,-OR1或-NHR2; R1是低级直链或支链的 C1至C5的烷基; R2是具有氧化剂的C1至C5或2,5-双(三氟甲基)苯基的低级直链或支链烷基)。 氧化剂选自间氯过苯甲酸,过乙酸,三氟过乙酸,多马来酸,溴化钠,次氯酸钠,过氧化氢,碘代甲基苯和碘代苯。
    • 77. 发明公开
    • 초임계 유체 공정을 이용한 무정형 세푸록심 악세틸 고체분산체의 제조 방법 및 이 방법으로 제조된 세푸록심악세틸 고체 분산체
    • 通过使用超临界耐溶剂工艺制备非晶质CEFUROXIME AXETIL固体分散体的方法和非晶态CEFUROXIME AXETIL固体分散体的制备方法
    • KR1020040072057A
    • 2004-08-18
    • KR1020030007980
    • 2003-02-08
    • 한미사이언스 주식회사
    • 황성주조국현우종수
    • C07D501/28
    • Y02P20/544
    • PURPOSE: A method for preparing non-crystalline cefuroxime axetil solid dispersion by using supercritical solvent-resistant process and non-crystalline cefuroxime axetil solid dispersion prepared thereby are provided, which non-crystalline cefuroxime axetil solid dispersion has high solubility, uniformed diameter of micrometer or less, increased specific surface area, and does not form gel when it contacts with aqueous solution, so that elution rate cannot be affected by the dissolving time. CONSTITUTION: The method for preparing non-crystalline cefuroxime axetil solid dispersion comprises the steps of: (1) dissolving cefuroxime axetil and pharmaceutically acceptable additives selected from hydrophilic polymer, surfactant and a combination thereof in organic solvent to prepare a mixed solution; (2) spraying the mixed solution into a reactor having supercritical carbon dioxide condition of 45 deg. C and 100 to 150 bar and introducing carbon dioxide into the reactor to form particles of cefuroxime axetil and additive mixture; and (3) introducing additional supercritical carbon dioxide into the reactor, wherein the hydrophilic polymer is selected from celluloses, polyethyleneglycol, povidone and a mixture thereof.
    • 目的:提供一种通过使用超临界溶剂耐受性方法制备非结晶性头孢呋辛酯固体分散体的方法和由此制备的非结晶头孢呋辛酯固体分散体,其非结晶头孢呋辛酯固体分散体具有高溶解度,均匀的直径的千分尺或 较少,比表面积增加,当与水溶液接触时不会形成凝胶,因此溶出速率不会受溶解时间的影响。 构成:非结晶头孢呋辛酯固体分散体的制备方法,包括以下步骤:(1)将头孢呋辛酯和选自亲水性聚合物,表面活性剂及其组合的药学上可接受的添加剂溶解在有机溶剂中以制备混合溶液; (2)将混合溶液喷雾到超临界二氧化碳条件为45度的反应器中。 C和100至150巴,并将二氧化碳引入反应器中以形成头孢呋辛酯和添加剂混合物的颗粒; 和(3)将另外的超临界二氧化碳引入反应器中,其中亲水性聚合物选自纤维素,聚乙二醇,聚维酮及其混合物。
    • 78. 发明公开
    • 안정한 무정형 암로디핀 캠실레이트, 이의 제조방법 및이를 포함하는 경구투여용 조성물
    • 稳定的无定形阿霉素蓖麻油酸酯,其制备方法及其口服制剂的组合物
    • KR1020040068877A
    • 2004-08-02
    • KR1020040005089
    • 2004-01-27
    • 한미사이언스 주식회사
    • 문영호김남두이경익이관순우종수장영길
    • C07D211/84
    • C07D211/90
    • PURPOSE: Stable amorphous amlodipine camsylate, a process for preparing the same and a composition for oral administration thereof are provided, which compound has high solubility and improved stability, so that it can be useful for treatment of cardiovascular disease. CONSTITUTION: The process for preparing the stable amorphous amlodipine camsylate comprises the steps of: dissolving amorphous amlodipine camsylate in organic solvent; and removing solvent from the amorphous amlodipine camsylate dissolved solution by using one method selected from spray drying, roller drying, solvent precipitation, freeze-drying and rapid solvent removement to recover amorphous amlodipine camsylate, wherein the organic solvent is selected from ketone, alcohol, nitrile, ether, ester, chlorinated solvent and a mixture thereof; the spray drying method uses gas selected from nitrogen, argon, carbon dioxide and oxygen. The oral administration composition for treating cardiovascular disease contains the stable amorphous amlodipine camsylate as an active constituent.
    • 目的:提供稳定的无定形氨氯地平樟脑磺酸盐,其制备方法和口服给药组合物,该化合物具有高溶解度和改善的稳定性,因此可用于治疗心血管疾病。 构成:制备稳定的无定形氨氯地平樟脑磺酸盐的方法包括以下步骤:将无定形氨氯地平樟脑磺酸盐溶解在有机溶剂中; 并通过使用选自喷雾干燥,辊式干燥,溶剂沉淀,冷冻干燥和快速溶剂去除的一种方法从无定形氨氯地平cams溶溶解溶剂中除去溶剂,以回收无定形氨氯地平樟脑磺酸盐,其中有机溶剂选自酮,醇,腈 ,醚,酯,氯化溶剂及其混合物; 喷雾干燥法使用选自氮气,氩气,二氧化碳和氧气的气体。 用于治疗心血管疾病的口服给药组合物含有稳定的无定形氨氯地平作为活性成分。
    • 79. 发明公开
    • 신규한 p-당단백질 저해제, 그의 제조방법 및 이를유효성분으로 하는 경구투여용 조성물
    • P-糖蛋白抑制剂,其制备方法和含有该组合物的口服组合物作为有效成分
    • KR1020040008377A
    • 2004-01-31
    • KR1020020042005
    • 2002-07-18
    • 한미사이언스 주식회사
    • 김희석함영진이광옥방극찬안영길김한경정금신이회철김기은김맹섭
    • C07D401/06
    • C07D401/06C07D215/20C07D401/12
    • PURPOSE: A p-glycoprotein inhibitor, a preparation method thereof and an oral composition containing the same as an effective component are provided, thereby increasing the oral adsorption rate of an anti-cancer agent having low bioavailability. CONSTITUTION: A compound as a p-glycoprotein inhibitor is represented by the formula 1, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently hydrogen, hydroxyl, C1-3 alkyl or alkoxy; R5 and R6 may form 4 to 8-membered ring together; l, m and n are independently an integer of 0 to 4; X is R11, OR12 or NR13R14; and R11, R12, R13 and R14 are independently optionally substituted phenyl, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, quinazoline, quinoxaline, pyrrole, pyrazol, imidazol, triazol, tetrazol, oxazole, thiazole, oxadiazole, thiadiazol, benzimidazol, benzthiazol, isoxazole, isothiazole, benzoxazole, pyridazine or triazine. A method for preparing the compound of the formula 1 comprises reacting a compound of the formula 2 with a compound of the formula 3, wherein E is a leaving group such as halogen, methanesulfonyloxy or toluenesulfonyloxy.
    • 目的:提供p型糖蛋白抑制剂及其制备方法和含有该组合物的有效成分的口服组合物,从而提高生物利用度低的抗癌剂的口服吸附率。 构成:作为p-糖蛋白抑制剂的化合物由式1表示,其中R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9和R 10独立地为氢,羟基,C 1-3烷基或烷氧基; R5和R6可以一起形成4至8元环; l,m和n分别为0〜4的整数。 X为R11,OR12或NR13R14; 吡唑,喹唑啉,喹喔啉,吡咯,吡唑,咪唑,三唑,四唑,恶唑,噻唑,恶二唑,噻二唑,苯并咪唑,苯并噻唑,苯并噻唑等。其中R 11,R 12,R 13和R 14独立地为任选取代的苯基,吡啶,嘧啶,吡嗪, 异恶唑,异噻唑,苯并恶唑,哒嗪或三嗪。 制备式1化合物的方法包括使式2化合物与式3化合物反应,其中E为离去基团如卤素,甲磺酰氧基或甲苯磺酰氧基。