公开(公告)号：US06534092B2

公开(公告)日：2003-03-18

申请号：US10073864

申请日：2002-02-14

Applicant: Steven G. Wright ,  Michael E. Rickey ,  J. Michael Ramstack ,  Shawn L. Lyons ,  Joyce M. Hotz

Inventor： Steven G. Wright ,  Michael E. Rickey ,  J. Michael Ramstack ,  Shawn L. Lyons ,  Joyce M. Hotz

IPC: A61K914

CPC classification number: A61K31/519 ,  A61K9/1647 ,  A61K9/1694 ,  B01J13/02

Abstract: A method for preparing microparticles having a selected polymer molecular weight. The hold time and temperature of a solution containing a nucleophilic compound and a polymer having a starting molecular weight are controlled in order to control the molecular weight of the polymer in the finished microparticle product. In this manner a selected polymer molecular weight in the finished microparticle product can be achieved from a variety of starting material molecular weights.

公开(公告)号：US06471995B1

公开(公告)日：2002-10-29

申请号：US09671426

申请日：2000-09-27

Applicant: J. Michael Ramstack

Inventor： J. Michael Ramstack

IPC: A61K914

CPC classification number: A61K9/1647 ,  A61K9/1694 ,  B01J13/12 ,  Y10T428/2982

Abstract: Method and apparatus for preparing microparticles using liquid-liquid extraction. A first phase and a second phase are combined to form an emulsion. A portion of the second phase is separated from the emulsion (solvent rich), and the solvent is extracted from the separated second phase, which is then returned (solvent poor) to the emulsion. This process of separation of a solvent rich phase, extraction of solvent, and return of a solvent poor phase, is carried out until a selected level of solvent in the emulsion is achieved. Alternatively, the separated solvent rich phase is not returned to the emulsion, but replaced with another solution, such as an aqueous solution, that is free from solvent. The solvent is preferably extracted into an extraction liquid that functions as a “solvent sink” for the solvent.

Abstract translation: 使用液 - 液萃取制备微粒的方法和装置。 将第一相和第二相组合形成乳液。 将第二相的一部分与乳液分离（富溶剂），并从分离的第二相中提取溶剂，然后将其返回（溶剂不良）至乳液。 进行富溶相的分离，萃取溶剂和返回溶剂不良阶段的过程，直到达到乳液中所选择的溶剂含量。 或者，分离的富溶相不会返回到乳液中，而是用不含溶剂的另一溶液如水溶液代替。 优选将溶剂萃取到作为溶剂的“溶剂槽”的萃取液中。

公开(公告)号：US06403114B1

公开(公告)日：2002-06-11

申请号：US09920862

申请日：2001-08-03

Applicant: Michael E. Rickey ,  J. Michael Ramstack ,  Danny H. Lewis

Inventor： Michael E. Rickey ,  J. Michael Ramstack ,  Danny H. Lewis

IPC: A61F200

CPC classification number: B01J13/04 ,  A61K9/1647 ,  A61K9/1694 ,  A61K9/5089 ,  A61K31/519 ,  Y10T428/2985

Abstract: A method for preparing biodegradable, biocompatible microparticles. A first phase is prepared that includes a biodegradable, biocompatible polymer, an active agent, and a solvent. A second phase is prepared. The first and second phases are combined to form an emulsion in which the first phase is discontinuous and the second phase is continuous. The discontinuous first phase is separated from the continuous second phase. The residual level of solvent in the discontinuous first phase is reduced to less than about 2% by weight.

Abstract translation: 一种制备可生物降解的生物相容性微粒的方法。 制备包含可生物降解的生物相容性聚合物，活性剂和溶剂的第一相。 准备第二阶段 第一和第二相组合形成乳液，其中第一相是不连续的，第二相是连续的。 不连续的第一相与连续的第二相分离。 不连续第一相中溶剂的残留量减少到小于约2重量％。

公开(公告)号：US06379703B1

公开(公告)日：2002-04-30

申请号：US09722335

申请日：2000-11-28

Applicant: Shawn L. Lyons ,  J. Michael Ramstack ,  Steven G. Wright

Inventor： Shawn L. Lyons ,  J. Michael Ramstack ,  Steven G. Wright

IPC: A61K914

CPC classification number: A61K9/1647 ,  A61K9/1694 ,  B01J13/02 ,  Y10T428/2982

Abstract: An improved method for preparing microparticles that exhibit controlled release of an effective amount of an active agent over an extended period of time. More particularly, a method is provided for preparing microparticles having a selected release profile for release of active agent contained in the microparticles. By adjusting the degree of drying that is performed during the preparation of the microparticles, the release profile can be controlled. By performing no intermediate drying, an initial burst and a substantially linear release profile is achieved. By performing substantially complete intermediate drying, an initial lag phase and a substantially sigmoidal release profile is achieved.

Abstract translation: 一种用于制备在长时间内显示有效量的活性剂的受控释放的微粒的改进方法。 更具体地，提供了一种制备具有选择的释放曲线的微粒以释放微粒中所含的活性剂的方法。 通过调节在制备微粒期间进行的干燥程度，可以控制释放曲线。 通过不进行中间干燥，实现初始脉冲串和基本上线性的释放曲线。 通过进行基本上完全的中间干燥，实现了初始滞后期和基本上S形释放曲线。