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
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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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