Title:
COMBRETASTATIN DERIVATIVE LYOPHILIZED POWDER INJECTION AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2020/103175
Kind Code:
A1
Abstract:
Disclosed are a combretastatin derivative lyophilized powder injection and a preparation method therefor. The lyophilized powder injection is constituted by a combretastatin derivative phospholipid complex, a stabilizer, and a lyophilized protective agent. The preparation method comprises: the preparation of the combretastatin derivative phospholipid complex; pressurized homogenization; and freeze drying. The lyophilized powder injection is dissolved in a 5% glucose or 0.9% saline injection for use, and is applicable in intravenous injection, intravenous infusion, or direct oral administration to treat non-small-cell lung cancer, liver cancer, and colon cancer. The lyophilized powder injection prepared per the present invention has a high drug-to-lipid ratio and low toxic side effects, improves the hydrophilicity and lipophilicity of a combretastatin derivative, provides a certain degree of sustained-release effect and passive targeting, increases oral bioavailability, reduces the dosage for intravenous administration, enhances attenuation, and has great resolubility; moreover, the preparation method has a simple process and is easy for industrial production.
Inventors:
ZHOU JIANPING (CN)
DING YANG (CN)
YUAN ZHOU (CN)
DING YANG (CN)
YUAN ZHOU (CN)
Application Number:
PCT/CN2018/118108
Publication Date:
May 28, 2020
Filing Date:
November 29, 2018
Export Citation:
Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
A61K9/19; A61K31/09; A61K47/24; A61P35/00
Foreign References:
| CN106580945A | 2017-04-26 | |||
| CN105288648A | 2016-02-03 | |||
| US20090202621A1 | 2009-08-13 |
Other References:
MA, JUANJUAN ET AL.: "Nanoformulations of Vascular Inhibitors: Combretastatin A4 and Combretastatin A4 Phosphate", JOURNAL OF INTERNATIONAL PHARMACEUTICAL RESEARCH, vol. 43, no. 5, 31 October 2016 (2016-10-31)
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM ( ORDINARY PARTNERSHIP ) (CN)
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