Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses

A compound and diterpenoid technology, applied in the field of anticancer diterpenoid intravenous injection and preparation thereof, can solve the problems of low bioavailability, poor solubility of anticancer diterpenoid, etc. Enhanced anti-cancer efficacy and improved stability

Inactive Publication Date: 2008-02-13
INST OF ZOOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to overcome the defects of poor solubility in water and low bioavailability of anticancer diterpenoids in the living body, thereby providing an anticancer diterpenoid with good water solubility, non-toxicity and high bioavailability. Terpenoid compound intravenous injection, preparation method and use thereof

Method used

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  • Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses
  • Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses
  • Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1. Preparation of intravenous injection of anticancer diterpenoids

[0042] The anti-cancer effective amount of the diterpenoid compound represented by formula I is dissolved in a pharmaceutically acceptable composite solvent according to the following steps:

[0043] The composite solvent is calculated by weight percentage, including:

[0044] Molecular inclusion carrier: Captisol (SBE-7-β-CD) 40wt%

[0045] Osmotic pressure regulator: NaCl 0.9wt%

[0046] Polar solvent: absolute ethanol 5wt%

[0047] Semi-polar solvent: propylene glycol 5wt%

[0048] Non-polar solvent: ethyl acetate 5wt%

[0049] Antioxidant: sodium sulfite 0.5wt%

[0050] PH adjuster: 8wt% NaHCO 3 Proper amount, adjust the pH of the mixed solution. 7.2

[0051] The balance is deionized three-distilled water

[0052] 1) First dissolve the diterpenoids and antioxidants of formula I in an effective amount of anticancer in polar solvents, semi-polar and non-polar solvents to obtain a transparent solu...

Embodiment 2

[0056] Example 2. In vivo anti-tumor experiment of diterpenoids on human nasopharyngeal carcinoma (CNE) xenograft tumors in nude mice

[0057] Test drug: the diterpenoid intravenous injection prepared in Example 1, wherein the diterpenoid compound was prepared and purified by the State Key Laboratory of Biomembrane and Membrane Engineering, Institute of Zoology, Chinese Academy of Sciences, with a purity of more than 99%, and it was white crystal , The physical and chemical properties are stable, and it is formulated with nano-inclusion preparations.

[0058] Positive control: Cyclophosphamide (CTX), a product of Jiangsu Hengrui Pharmaceutical Co., Ltd., Chinese Medicine Zhunzi H32020857, prepared with normal saline.

[0059] Negative control: molecular carrier inclusion agent (no drug, only a compound solvent for the aforementioned test drug), provided by the Institute of Zoology, Chinese Academy of Sciences

[0060] Cell model: human nasopharyngeal carcinoma cell (CNE), provided ...

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Abstract

The invention relates to an Anticancer diterpene analog compound intravenous injection formulation, and its preparation method and uses, wherein the injection comprises medicinal composite dissolvent and anticancer effective dose of diterpenoids of formula I, the composite dissolvent includes molecule inclusion carrier Captisol or Ecapsin. The diterpenoids are used as guest molecules to be coated into the Captisol or Ecapsin carriers as the host molecules. The coated diterpenoids have increased dissolvability in water.

Description

Technical field [0001] The invention relates to an intravenous injection of anticancer diterpenoids, in particular to an intravenous injection of anticancer diterpenoids that promotes differentiation and inhibits proliferation, and a preparation method and application thereof Background technique [0002] Chinese patent ZL98124416.5 discloses a diterpenoid compound found in artificially cultivated plants for many years, as shown in formula I, but the solubility of this anti-cancer diterpenoid compound in water is only one hundred thousandths. , So in clinical application, it will affect its absorption in the body, making the bioavailability low. [0003] Summary of the invention [0004] The purpose of the present invention is to overcome the poor solubility of anti-cancer diterpenoids in water and low bioavailability in organisms, thereby providing an anti-cancer two with good water solubility, non-toxicity and high bioavailability. Terpenoid intravenous injection, its prepar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/34A61K9/08A61P35/00
Inventor 王敬泽
Owner INST OF ZOOLOGY CHINESE ACAD OF SCI
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