公开(公告)号：KR1020000000265A

公开(公告)日：2000-01-15

申请号：KR1019990043354

申请日：1999-10-08

Applicant: 한국과학기술연구원

Inventor： 정서영 ,  권익찬 ,  박주애

IPC: A61K9/16

CPC classification number: A61K9/167 ,  Y02A50/471

Abstract: PURPOSE: A microsphere is provided to enhance the absorption efficiency in the small intestines on oral medication by modifying its surface using the Cholera Toxin B(CTB). CONSTITUTION: A microsphere is formed by: combining the CTB(Cholera Toxin B) to a microsphere containing more than one kinds of physiological activating substances in its inside or on its surface through a polyethylene glycol linker(PEG) having 3000-4000 of molecular weight.

Abstract translation: 目的：通过使用霍乱毒素B（CTB）改变其表面，提供微球以增强口服药物中小肠的吸收效率。 构成：通过以下方法形成微球：通过具有3000-4000分子量的聚乙二醇接头（PEG）将CTB（霍乱毒素B）与其内部或其表面上含有多于一种生理活化物质的微球结合 。

公开(公告)号：KR1020020005563A

公开(公告)日：2002-01-17

申请号：KR1020017001096

申请日：1999-08-19

Applicant: 한국과학기술연구원

Inventor： 정서영 ,  권익찬 ,  박주애

IPC: A61K9/50

CPC classification number: A61K47/36 ,  A61K9/1652 ,  A61K39/092

Abstract: PURPOSE: Provided are vaccine compositions for oral administration consisting of a protein antigen encapsulated in biodegradable alginate microspheres by the diffusion-controlled interfacial gelation technique which produces microspheres having less than 5μm of diameter, and to preparation process thereof. CONSTITUTION: The process for preparing the vaccine composition comprises the steps of: i) mixing aliquot of a protein antigen or a protein antigen including immune adjuvant with an alginate aqueous solution; ii) homogenizing by adding a mixture of the alginate and a protein antigen of step i) to n-octanol containing an emulsifier; iii) spraying n-octanol solution containing CaCl2 into the emulsion while stirring the whole emulsion slowly; iv) adding additional CaCl2 solution to saturate the emulsion, and curing microspheres; v) dehydrating microspheres by addition of dehydrating solvent; vi) collecting the microspheres on membrane filters and washing with alcohol, and then drying in vacuo.

Abstract translation: 目的：提供用于口服给药的疫苗组合物，其通过扩散控制的界面凝胶化技术包封在可生物降解的藻酸盐微球中的蛋白质抗原，其产生具有小于5μm直径的微球体及其制备方法。 构成：制备疫苗组合物的方法包括以下步骤：i）将蛋白质抗原或包含免疫佐剂的蛋白质抗原的等分试样与藻酸盐水溶液混合; ii）通过将步骤i）的藻酸盐和蛋白质抗原的混合物加入含有乳化剂的正辛醇进行均化; iii）将缓慢地搅拌整个乳液的含有CaCl 2的正辛醇溶液喷雾到乳液中; iv）加入另外的CaCl 2溶液使乳液饱和并固化微球; v）通过加入脱水溶剂脱水微球; vi）在膜过滤器上收集微球并用醇洗涤，然后真空干燥。

公开(公告)号：KR1020010003853A

公开(公告)日：2001-01-15

申请号：KR1019990024336

申请日：1999-06-25

Applicant: 한국과학기술연구원

Inventor： 정서영 ,  권익찬 ,  박주애

IPC: A61K9/52 ,  A61K47/36

CPC classification number: A61K47/36 ,  A61K9/1652 ,  A61K39/092

Abstract: PURPOSE: An arginate-microsphere used for oral vaccine is provided, which delivers antigens effectively through a pathway by Peyer's patch and a by-pathway of lymphatic gland with its small size; shows higher immunity property; improves level of serum and mucous membrane when administrated with cholera toxin or cholera toxin B unit; so can be used as an effective oral vaccine. CONSTITUTION: A process for the preparation of arginate-microsphere used for oral vaccine comprises: adding a solution containing antigen protein(or antigen protein and immuno-adjuvant) to arginate solution; adding n-octanol solution containing an emulsifier to the antigen protein(or antigen protein and immuno-adjuvant)-arginate mixed solution, and homogenizing; adding calcium chloride-contained n-octanol using a sprayer while stirring the emulsion slowly; adding calcium chloride solution to saturate the emulsion, and gelating microspheres; dehydrating the microspheres by adding dehydration solvent; filtering the microspheres, washing with alcohol, and drying in vacuum state.

Abstract translation: 目的：提供用于口服疫苗的精氨酸 - 微球，通过派耶氏贴片和小尺寸的淋巴管旁路有效传递抗原; 显示较高的免疫力; 当施用霍乱毒素或霍乱毒素B单位时，提高血清和粘膜水平; 所以可以用作有效的口服疫苗。 构成：用于制备用于口服疫苗的精氨酸 - 微球的方法包括：向精氨酸溶液中加入含有抗原蛋白（或抗原蛋白和免疫佐剂）的溶液; 向抗原蛋白（或抗原蛋白和免疫佐剂）中加入含有乳化剂的正辛醇溶液 - 调节混合溶液，均化; 使用喷雾器在缓慢搅拌乳状液的同时加入含氯化钙的正辛醇; 加入氯化钙溶液使乳液饱和，凝胶化微球; 加入脱水溶剂使微球脱水; 过滤微球，用乙醇洗涤，并在真空状态下干燥。

公开(公告)号：KR100345466B1

公开(公告)日：2002-07-26

申请号：KR1019990043354

申请日：1999-10-08

Applicant: 한국과학기술연구원

Inventor： 정서영 ,  권익찬 ,  박주애

IPC: A61K9/16

CPC classification number: A61K9/167 ,  Y02A50/471

Abstract: 본발명은콜레라독소 B 소단위체 (Cholera toxin B subunit, CTB)가표면에수식된마이크로스피어 (microsphere)에관한것으로, 구체적으로본 발명에서는마이크로스피어에 PEG 링커 (polyethylene glycol linker)를접합하거나접합하지않은형태에 CTB를다시접합함으로써 CTB-마이크로스피어또는 CTB-PEG-마이크로스피어를제조하고이와같이제조된마이크로스피어가마우스소장에서흡수효율이탁월함을확인한다. 따라서, 본발명의 CTB가접합된마이크로스피어는항원등 생리활성물질의경구투여용제형으로서유용하다.