Drug delivery formulation for controlling of initial burst and manufacturing method thereof

    公开(公告)号:US10307373B2

    公开(公告)日:2019-06-04

    申请号:US13022734

    申请日:2011-02-08

    Abstract: Provided is a drug delivery system for control of initial burst of a drug. More particularly, there are provided a drug delivery formulation including: a granule containing a biodegradable polymer and a drug; and a temperature-sensitive hydrogel, and a method for preparing the same. The presently disclosed drug delivery formulation can be prepared via a relatively simple process and allows a drug to be released slowly at a constant rate without initial burst and thus maintains a constant blood level of the drug for a long period of time. Consequently, it is capable of preventing the initial burst of the existing injection-type drug delivery formulations and slow-release granules and providing a desired release profile, including sustained release with time.

    METHOD FOR PREPARING TAXANE DERIVATIVES
    2.
    发明申请
    METHOD FOR PREPARING TAXANE DERIVATIVES 有权
    制备TAXANE衍生物的方法

    公开(公告)号:US20120035379A1

    公开(公告)日:2012-02-09

    申请号:US13262936

    申请日:2009-12-03

    CPC classification number: C07D305/14 Y02P20/55

    Abstract: Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.

    Abstract translation: 提供了一种紫杉烷衍生物的制备方法,其包括:使作为侧链的保护基的苯基异丝氨酸衍生物或其异构体的混合物与浆果赤霉素III衍生物或10-脱乙酰基浆果赤霉素III衍生物 得到异构体的混合物; 通过色谱分离异构体; 并进行选择性分离的异构体的立体化学结构的回归,其适用于以高产率大规模生产紫杉烷衍生物。

    Method for preparing taxane derivatives
    6.
    发明授权
    Method for preparing taxane derivatives 有权
    紫杉烷衍生物的制备方法

    公开(公告)号:US08633326B2

    公开(公告)日:2014-01-21

    申请号:US13262936

    申请日:2009-12-03

    CPC classification number: C07D305/14 Y02P20/55

    Abstract: Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.

    Abstract translation: 提供了一种紫杉烷衍生物的制备方法,其包括:使作为侧链的保护基的苯基异丝氨酸衍生物或其异构体的混合物与浆果赤霉素III衍生物或10-脱乙酰基浆果赤霉素III衍生物 得到异构体的混合物; 通过色谱分离异构体; 并进行选择性分离的异构体的立体化学结构的回归,其适用于以高产率大规模生产紫杉烷衍生物。

    TEMPERATURE-SENSITIVE POLYETHYLENE GLYCOL / POLYESTER BLOCK COPOLYMER IN WHICH BIOACTIVE FUNCTIONAL GROUP IS INTRODUCED INTO SIDE CHAIN THEREOF
    7.
    发明申请
    TEMPERATURE-SENSITIVE POLYETHYLENE GLYCOL / POLYESTER BLOCK COPOLYMER IN WHICH BIOACTIVE FUNCTIONAL GROUP IS INTRODUCED INTO SIDE CHAIN THEREOF 有权
    生物活性官能团的温度敏感性聚乙烯甘油酯/聚酯嵌段共聚物被引入到其中

    公开(公告)号:US20130331526A1

    公开(公告)日:2013-12-12

    申请号:US13983905

    申请日:2011-11-22

    Abstract: The present invention relates to preparation and application of a temperature-sensitive polyethylene glycol/polyester block copolymer having a bioactive functional group introduced into a side chain thereof. More specifically, it relates to a temperature-sensitive polyethylene glycol/polyester block copolymer including a lactide segment having a bioactive functional group introduced into a side chain thereof and a method for preparing same. The temperature-sensitive polyethylene glycol/polyester block copolymer according to the present invention having a bioactive functional group introduced into a side chain thereof can be widely used as a drug delivery system, a support for tissue engineering, an adhesion inhibitor, etc.

    Abstract translation: 本发明涉及引入其侧链的具有生物活性官能团的温度敏感性聚乙二醇/聚酯嵌段共聚物的制备和应用。 更具体地说,本发明涉及包含引入其侧链的生物活性官能团的丙交酯链段的温度敏感性聚乙二醇/聚酯嵌段共聚物及其制备方法。 具有引入其侧链的生物活性官能团的本发明的温度敏感性聚乙二醇/聚酯嵌段共聚物可广泛用作药物递送系统,组织工程用支持体,粘着抑制剂等。

    Method for purification of paclitaxel from paclitaxel-containing materials
    9.
    发明申请
    Method for purification of paclitaxel from paclitaxel-containing materials 有权
    从含紫杉醇的材料中纯化紫杉醇的方法

    公开(公告)号:US20050154218A1

    公开(公告)日:2005-07-14

    申请号:US11028487

    申请日:2004-12-30

    CPC classification number: C07D305/14

    Abstract: This invention relates to methods for purification of paclitaxel from a paclitaxel-containing material. The method comprises the following steps: (a) extracting a paclitaxel-containing material with an organic solvent to obtain an extract, and concentrating the extract; (b) adding the concentrate with an organic solvent which is not mixed with water to separate an organic solvent phase and then concentrating; (c) subjecting the concentrate to normal phase chromatography to obtain an eluate; (d) dissolving the eluate in an acetone or dichloromethane followed by adding pentane or hexane to form a precipitate; and (e) subjecting the precipitate to high performance liquid chromatography. According to the method of the present invention, paclitaxel of over 99.5% purity can be easily obtained from a Taxus genus plant with a high yield.

    Abstract translation: 本发明涉及从含紫杉醇的材料中纯化紫杉醇的方法。 该方法包括以下步骤:(a)用有机溶剂萃取含有紫杉醇的材料,得到提取物,浓缩提取物; (b)将浓缩物与不与水混合的有机溶剂加入以分离有机溶剂相,然后浓缩; (c)使浓缩物进行正相色谱以获得洗脱液; (d)将洗脱液溶解在丙酮或二氯甲烷中,然后加入戊烷或己烷以形成沉淀物; 和(e)使沉淀物进行高效液相色谱。 根据本发明的方法,可以容易地从具有高收率的紫杉属植物获得纯度超过99.5%的紫杉醇。

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