Anticancer injection of rabdosia diterpene compound or its derivative and its preparing method

A technology of derivatives and diterpenoids, applied in the field of injection and preparation of Rubescens diterpenoids with anticancer effect or derivatives thereof, can solve the problems of low bioavailability, insufficient safety, poor stability and the like, and achieves The effect of improving solubility, good stability and improving compliance

Inactive Publication Date: 2006-11-08
常贵生 +2
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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 provide a kind of injection and the preparation method of containing oridonium diterpenoids or its derivatives with anticancer effect, and this injection also includes solubilizer β-cyclodextrin or its derivatives, overcomes existing It has the disadvantages of poor solubility, poor stability, low bioavailability and insufficient safety

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Oridonium diterpenoid injection preparation

[0030] The amount of raw material components (g): 0.5g of raw materials oridonin, oridonin B, oridonin C, oridonin, oridonin or oridonin, solubilizer β - Cyclodextrin 2-HP-β-CYD 10g, the remaining amount of water for injection to 50ml.

[0031] Preparation process: Weigh the raw material medicine of the prescribed amount, pulverize it and pass through an 80-mesh sieve, and set aside; in addition, fully dissolve the prescribed amount of 2HP-β-CYD with distilled water under continuous stirring, add the raw material drug to the above solution, and use distilled water The volume was adjusted to 50ml, the pH was adjusted to 4, magnetically stirred at 30°C and 50rpm / min for 5 hours, and left at room temperature to balance overnight. Filter the medicinal solution into a sterile container with a microporous filter membrane with a pore size of 0.2um, fill the medicinal solution into a pre-sterilized ampoule, seal and sterilize.

Embodiment 2

[0033] Oridonium diterpenoid injection preparation

[0034] Raw material ingredient dosage (g): 0.25g of raw material drug oridonin, oridonin B, oridonin C, oridonin, oridonin or oridonin, solubilizer hydroxy Propyl-β-cyclodextrin, hydroxyethyl-β-cyclodextrin, trimethyl-β-cyclodextrin or sulfoalkyl ether-β-cyclodextrin 6g, the balance of water for injection to 20ml.

[0035] Preparation process: Weigh the prescribed amount of raw material medicine, pulverize it and pass it through an 80-mesh sieve, and set aside; take another prescribed amount of solubilizer β-cyclodextrin, fully dissolve it with distilled water under continuous stirring, and add the treated raw material medicine The above solution was distilled to 20ml with distilled water, adjusted to pH 6, magnetically stirred at 40°C and 30rpm / min for 4 hours, left to stand at room temperature for 6 hours, filtered with a 0.2um nylon microporous membrane, and the filtrate was used as a mobile phase After diluting 4 times,...

Embodiment 3

[0037] Oridonium diterpenoid injection preparation

[0038] Raw material ingredient dosage (g): 0.3g of raw material drug oridonin, oridonin B, oridonin C, oridonin, oridonin or oridonin, solubilizer hydroxy Propyl-β-cyclodextrin, hydroxyethyl-β-cyclodextrin, trimethyl-β-cyclodextrin or sulfoalkyl ether-β-cyclodextrin 5g, the balance of water for injection to 20ml.

[0039] Preparation process: Weigh the prescribed amount of raw material medicine, pulverize it and pass through a 100-mesh sieve, and set aside; in addition, fully dissolve the prescribed amount of SEB-β-CYD with distilled water under continuous stirring, add the raw material drug to the above solution, and use distilled water The volume was adjusted to 20ml, the pH was adjusted to 3, magnetically stirred at 60°C and 50rpm / min for 4 hours, and allowed to stand at room temperature for 6 hours to balance. Filter the medicinal solution into a sterile container with a microporous filter membrane with a pore size of 0.2...

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PUM

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Abstract

The present invention provides a kind of anticancer injection containing rabdosia diterpene or its derivative and beta-cyclodextrin or its derivative. The insoluble rabdosia diterpene is first prepared into cyclodextrin inclusion to raise the dissolubility, and then prepared into injection or freeze dried powder for injection. The anticancer injection has high stability, high treating effect on liver cancer, esophageal cancer, gastric cancer and other malignant solid tumors and leukemia, and patient's compliance.

Description

technical field [0001] The invention relates to an injection containing a diterpene compound or a derivative thereof with anticancer effect and a preparation method thereof. The injection also includes a solubilizer β-cyclodextrin or a derivative thereof. Background technique [0002] Rabdosia rubescens (Rabdosia rubescens), also known as Binglingcao, is a plant of the genus Lamiaceae. It is mainly produced in Henan, Hebei, Shanxi, Sichuan and other places in my country. It has the effects of clearing away heat, reducing inflammation and relieving pain. Literature records can be used to treat acute and chronic tonsillitis, pharyngitis and other diseases. In 1991, the Ministry of Health of my country approved the use of the dried leaves and above-ground parts of Dongling grass as Chinese medicinal materials, which were included in the 1992 edition of the Ministry of Health Standards for Chinese Medicinal Materials. Since the 1970s, my country has started to study the chemica...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K9/08A61K36/53A61P35/00
Inventor 陈俊辉常贵生常菁
Owner 常贵生
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