公开(公告)号：WO2003066691A1

公开(公告)日：2003-08-14

申请号：PCT/US2003/003216

申请日：2003-02-04

Applicant: ISP INVESTMENTS INC.

Inventor： MALAWER, Edward, G. ,  CULLEN, James, P. ,  WU, Chi-San ,  SENAK, Laurence ,  DREFKO, William, J.

IPC: C08F26/08

CPC classification number: C08F226/10

Abstract: What is described herein is a pharmaceutical excipient which is a proliferous copolymer of vinyl pyrrolidone and vinyl acetate, having advantageous dissolution and disintegration properties.

Abstract translation: 本文描述的是药物赋形剂，其是乙烯基吡咯烷酮和乙酸乙烯酯的增殖共聚物，具有有利的溶解和崩解性质。

公开(公告)号：WO1994018241A1

公开(公告)日：1994-08-18

申请号：PCT/US1994000806

申请日：1994-01-21

Applicant: ISP INVESTMENTS INC.

Inventor： ISP INVESTMENTS INC. ,  WU, Chi-San ,  CURRY, James, F. ,  CULLEN, James, P.

IPC: C08F04/04

CPC classification number: C08F26/10

Abstract: A free radical solution process for making PVP polymers having a molecular weight corresponding to a K-value of about 30-150, a narrow molecular weight distribution represented by a polydispersity of about 3 to 6, and a residual VP monomer level of less than 0.1 %, which comprises: (a) precharging a reaction mixture of vinylpyrrolidone monomer and water in a solids contents w/w VP/H2O of about 5-50 %, and a dual free radical initiator system which comprises both low and high decomposition temperature free radical initiators whose 10-hour half-life temperature decomposition constants differ from each other by more than 5 DEG C, the low and high temperature initiators being present, respectively, in an amount of about 0.05-0.5 %, and about 0.1-0.5 %, by weight of the VP monomer, (b) polymerizing said monomer in said reaction mixture at a temperature near or above the 10-hour decomposition temperature of said low temperature initiator, and (c) after substantially all of the VP monomer has been converted to PVP polymer, continuing the polymerization at the same temperature as in (b), or at a higher temperature near or above the decomposition temperature of the high 10-hour temperature initiator, to complete the polymerization and to reduce the residual VP monomer level to less than 0.1 %.

Abstract translation: 一种自由基溶液法，其制备具有对应于约30-150的K值的分子量的PVP聚合物，由多分散性约3-6组成的窄分子量分布和小于0.1的残留VP单体水平 ％，其包括：（a）将乙烯基吡咯烷酮单体和水的反应混合物以约5-50％的固体含量w / w VP / H 2 O预充电，以及双重自由基引发剂体系，其包含低和高分解温度 其10小时半衰期温度分解常数彼此相差大于5℃的自由基引发剂，低温和高温引发剂分别以约0.05-0.5％和约0.1-0.5％的量存在， ，（b）在所述低温引发剂的10分钟分解温度下接近或高于所述反应混合物中的所述单体聚合，和（c）在基本上所有的VP单体之后， 被转化为PVP聚合物，在与（b）相同的温度下继续聚合，或在高的10小时温度引发剂的分解温度附近或更高的温度下进行聚合，完成聚合并减少残留的VP单体 水平低于0.1％。