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

A technology of compound and diterpenoids, which is applied in the field of anticancer diterpenoids intravenous injection and its preparation, can solve the problems of poor solubility and low bioavailability of anticancer diterpenoids, and achieve enhanced anticancer efficacy , reduce the dosage, improve the effect of bioavailability

Inactive Publication Date: 2006-07-19
INST OF ZOOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] 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 application 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

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Experimental program
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Effect test

Embodiment 1

[0043] Embodiment 1, preparation anticancer diterpene compound intravenous injection

[0044] The diterpenoid compound shown in the formula I of anticancer effective amount is dissolved in the pharmaceutically acceptable compound solvent according to the following steps:

[0045] Described composite solvent comprises by weight percent:

[0046] Molecular inclusion carrier: Captisol (SBE-β-CD) 40wt%

[0047] Osmotic pressure regulator: NaCl 0.9wt%

[0048] Polar solvent: absolute ethanol 5wt%

[0049] Semi-polar solvent: propylene glycol 5wt%

[0050] Non-polar solvent: ethyl acetate 5wt%

[0051] Antioxidant: sodium sulfite 0.5wt%

[0052] Acidity (pH) adjuster: 8wt% NaHCO 3 Appropriate amount, adjust the pH of the mixture to 7.2

[0053] The balance is deionized triple distilled water

[0054] 1) first dissolving the diterpenoids and antioxidants shown in the formula I of anticancer effective amount in polar solvents, semipolar and nonpolar solvents to obtain a transp...

Embodiment 2

[0058] Example 2. In vivo anti-tumor experiment of diterpenoids on human nasopharyngeal carcinoma (CNE) xenograft tumor in nude mice

[0059]Test drug: the diterpenoid intravenous injection prepared in Example 1, wherein the diterpenoid was prepared and purified by the State Key Laboratory of Biofilm and Membrane Engineering, Institute of Zoology, Chinese Academy of Sciences, with a purity of more than 99%, and it is a white crystal , stable physical and chemical properties, prepared with nano-inclusion preparations.

[0060] Positive control: Cyclophosphamide (CTX), a product of Jiangsu Hengrui Pharmaceutical Co., Ltd., approved by the National Pharmaceutical Standard H32020857, prepared with normal saline.

[0061] Negative control: Molecular carrier inclusion agent (no drug, only the compound solvent of the aforementioned test drug), provided by the Institute of Zoology, Chinese Academy of Sciences

[0062] Cell model: human nasopharyngeal carcinoma cell (CNE), provided by...

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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 present invention relates to an anticancer diterpene compound intravenous injection, in particular to an anticancer diterpene compound intravenous injection that promotes differentiation and suppresses proliferation, and its preparation method and use Background technique [0002] In Chinese patent ZL98124416.5, a diterpenoid compound found in plants that have been artificially cultivated for many years is disclosed, as shown in formula I, but the solubility of this anticancer diterpenoid compound in water is only 1 / 100,000 , so in clinical application, it will affect its absorption in the body, making the bioavailability low. [0003] [0004] Formula I Contents of the invention [0005] 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 bi...

Claims

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Application Information

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