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

A technology for Rubescensica and diterpenoids, which is applied in the field of preparation of Rubesia officinalis diterpenoid compounds or derivatives thereof for injection with anticancer effect, can solve the problems of low bioavailability, insufficient safety, poor stability and the like, To achieve the effect of improving solubility, good stability and improving compliance

Inactive Publication Date: 2009-09-02
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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  • Anticancer injection of rabdosia diterpene compound or its derivative and its preparing method
  • Anticancer injection of rabdosia diterpene compound or its derivative and its preparing method

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Oridonium diterpenoid injection preparation

[0031] 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.

[0032] 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

[0034] Oridonium diterpenoid injection preparation

[0035] 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.

[0036] 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 adjusted 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

[0038] Oridonium diterpenoid injection preparation

[0039]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.

[0040] 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....

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Abstract

The invention provides an injection containing oridonium diterpenoids or derivatives thereof and β-cyclodextrin or derivatives thereof with anticancer effect. The diterpenoids of Rubescens japonicus are poorly soluble drugs, and making such compounds into cyclodextrin inclusion complexes can improve the solubility of such drugs, and then produce aqueous injections and frozen preparations of diterpenoids of Rubescens japonicus according to pharmaceutical preparations. Dry powder injection. The present invention can remarkably improve the solubility of this type of compound in water, making its solubility reach 8-16 mg / ml on average, and overcomes the shortcomings of traditional intravenous administration that patients cannot tolerate local stimulation and have to interrupt treatment; the stability of the drug of the present invention Good reproducibility of the process; the medicine of the present invention is used for the treatment of malignant solid tumors and leukemia including liver cancer, esophageal cancer, gastric cancer, bladder cancer, and colorectal cancer, and can better exert the therapeutic effect of this type of compound and improve patient 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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K36/53A61K9/08A61P35/00
Inventor 陈俊辉常贵生常菁
Owner 常贵生
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