公开(公告)号：KR100358076B1

公开(公告)日：2002-10-25

申请号：KR1019990033693

申请日：1999-08-16

Applicant: 한국화학연구원

Inventor： 구정 ,  조선행 ,  정제교 ,  강길선 ,  이해방

IPC: A61K31/35

Abstract: 본발명은생체이용율을증진시킨경구용이프리플라본제제에관한것으로서, 더욱상세하게는골다공증치료제로사용하는이프리플라본원제제를수용성고분자및 부형제에고체분산시킴과동시에상기약제의결정크기를 10 ㎚∼ 20 ㎛로아주작게분산시킴으로써, 수용성고분자에상기이프리플라본이포접되어종래보다적은약물의투여량과적은횟수로복용하여도소화위장관내의체액에대한용해도와유효혈중농도를증가시키므로약물의과다투여로인한사용상의불편함과위장에대한부담을감소시킬수 있는생체이용율을증진시킨경구용이프리플라본제제에관한것이다.

公开(公告)号：KR1020020014570A

公开(公告)日：2002-02-25

申请号：KR1020000047918

申请日：2000-08-18

Applicant: 한국화학연구원

Inventor： 이해방 ,  강길선 ,  정제교 ,  구정 ,  조선행

IPC: C07D311/76

CPC classification number: A61K9/146 ,  A61K9/145 ,  A61K31/352 ,  A61K47/28

Abstract: PURPOSE: Provided is a process for preparing amorphous ipriflavone having increases bioavailability. When ipriflavone containing amorphous ipriflavone as an active ingredient is formulated and administered orally, its blood concentration easily reaches the effective level with less dose than conventional preparations. CONSTITUTION: The amorphous ipriflavone is manufactured by solid dispersing the mixture of the water soluble polymer solution with the solution containing ipriflavone and absorption enhancer in the water soluble polymer solution by fluidized bed spray drying machine or solid dispersing the mixture of ipriflavone with alginic acid and polyethylene glycol by melting the mixture at 90deg.C. The above water soluble polymer is one or more polymer mixtures selected from polyvinylpyrrolidone, polyvinylalcohol, polyethylene glycol, gum-arabic, dextran, dextrin, gelatin, methyl cellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, carboxymethyl cellulose, pluronic acid, poloxamer and polysorbate. The above absorption enhancer is one or mixtures of more than two selected from citric acid, alginic acid, ascorbic acid, bile acid, lithocolic acid, cholic acid, deoxycholic 5β-cholanic acid, trihydroxycholane, cholesterol, cholesteryl oleate, cholesteryl palmitate, choleseryl acetate, cholesteryl stearate, salicylic acid, mannitol, xylitol, dextrose, glucose, sucrose, galactose, sorbitol, lactose, fructose, maltose, pentaerythritol, and pentaerythritol tetraacetate.

Abstract translation: 目的：提供增加生物利用度的非晶异黄酮的制备方法。 当配制含有异黄酮异黄酮作为活性成分的异唑酮时，口服给药，其血药浓度容易达到有效水平，剂量比常规制剂低。 构成：通过流化床喷雾干燥机将水溶性聚合物溶液的混合物与含有异黄酮和吸收促进剂的溶液固体分散在水溶性聚合物溶液中或将异黄酮与藻酸和聚乙烯的混合物固体分散在一起制备无定形异黄酮 乙二醇通过将混合物熔化在90℃。 上述水溶性聚合物是选自聚乙烯吡咯烷酮，聚乙烯醇，聚乙二醇，阿拉伯树胶，葡聚糖，糊精，明胶，甲基纤维素，乙基纤维素，羟乙基纤维素，羟丙基纤维素，羧甲基纤维素，普朗尼克酸，泊洛沙姆和 聚山梨酯。 上述吸收增强剂是选自柠檬酸，藻酸，抗坏血酸，胆汁酸，石油酸，胆酸，脱氧胆酸5β-胆酸，三羟基胆甾醇，胆固醇，胆固醇油酸酯，胆固醇基棕榈酸酯，胆固醇酯乙酸酯 ，硬脂酸胆固醇酯，水杨酸，甘露糖醇，木糖醇，葡萄糖，葡萄糖，蔗糖，半乳糖，山梨醇，乳糖，果糖，麦芽糖，季戊四醇和季戊四醇四乙酸酯。

公开(公告)号：KR1020010017936A

公开(公告)日：2001-03-05

申请号：KR1019990033693

申请日：1999-08-16

Applicant: 한국화학연구원

Inventor： 구정 ,  조선행 ,  정제교 ,  강길선 ,  이해방

IPC: A61K31/35

CPC classification number: A61K31/352 ,  A61K47/58

Abstract: PURPOSE: A bio-availibility-improved ipriflavone preparation for oral is provided, which increases solubility to body fluid and effective blood concentration in the gastrointestines by smaller quantity of drug and less administration frequency than existing ipriflavone preparation, so decreases inconvenience of use, and increases bio-availibility. CONSTITUTION: A process for the preparation of bio-availibility-improved ipriflavone preparation for oral comprises: dissolving ipriflavone raw preparation in acetone; meanwhile, dissolving polyvinylpyrolidone in a mixed solution of acetone/ethanol(1:1, v/v) evenly; adding the prepared ipriflavone solution and polyvinylpyrolidone solution in a spray-dryer, and spraying to ipriflavone to be dispersed in polyvinylpyrolidone(ipriflavone:polyvinylpyrolidone=50:50 in weight part); drying by ventilation to get ipriflavone preparation of 10μm size(influx air temperature is 50deg.C, jet air pressure is 30psi, rate of spray solution is 12ml/min).

Abstract translation: 目的：提供一种生物可用性改善的异胡酮酮口服制剂，其通过较少量的药物和较少的给药频率比现有的异黄酮制剂增加对体液的溶解度和有效的血液浓度，从而减少使用的不便，并增加 生物可否订购。 构成：用于口服制备生物可利用性改良的异黄酮制剂的方法包括：将异黄酮原料制备于丙酮中; 同时将聚乙烯吡咯烷酮溶解在丙酮/乙醇（1：1，v / v）的混合溶液中; 将制备的异黄酮溶液和聚乙烯吡咯烷酮溶液加入喷雾干燥器中，喷雾至异黄酮分散在聚乙烯吡咯烷酮（异丙酮：聚乙烯吡咯烷酮= 50:50重量份）中; 通风通风干燥，得到异黄酮制剂10μm（流入气温50℃，喷气压30psi，喷雾速率为12ml / min）。