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Taxine kind anti-cancer slow release injection

A technology for sustained-release injections and anti-cancer drugs, applied in the field of medicine, can solve the problems of reduced immunity, limited dosage of administration, large trauma, etc., and achieves the effect of enhanced effect

Inactive Publication Date: 2007-03-07
孔庆忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that there are still many problems in the treatment of various malignant tumors, especially solid tumors.
Solid tumors have excessive expansive hyperplasia, and the interstitial pressure, tissue elastic pressure, fluid pressure, and interstitial viscosity are all higher than those of the surrounding normal tissue. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of brain tumors in rats" "Journal of Surgical Oncology" 1998 69 pages 76-82 (Kong Q et al., J Surg Oncol.1998Oct; 69(2): 76 -82), simply increasing the dosage is limited by systemic reactions
Drug implantation may solve the problem of drug concentration to some extent. However, the operation of drug implantation is more complicated and traumatic. In addition to easily causing various complications such as bleeding, infection, and decreased immunity, it can also cause or accelerate tumor spread and metastasis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Put 80 mg of pharmaceutical excipient ethylene vinyl acetate copolymer (EVAc) into a container, add 100 ml of dichloromethane to dissolve and mix well, add 20 mg of docetaxel, re-shake, and vacuum dry to remove the organic solvent. The dried solid composition is melted to prepare sustained-release pellets containing 20% ​​by weight of docetaxel, which are subpackaged and then sterilized by radiation to prepare the sustained-release docetaxel for injection. The docetaxel sustained-release preparation for injection is suspended in a special vehicle (water for injection containing 1.5% sodium carboxymethylcellulose) to prepare a corresponding suspension-type sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 14-24 days, and the drug release time in mice subcutaneous is 20-35 days.

Embodiment 2

[0036] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the contained anticancer active ingredients are: 30% by weight of paclitaxel, docetaxel, 2'-hydroxy paclitaxel, 10-deacetyl Baccatin III, 14β-hydroxy-10-deacetylbaccatin III, 9-dihydro-13-baccatin III, 13-(N-tri-butoxycarbonyl-β-isobutylisofilament Amino alcohol)-14-hydroxybaccatin-1,14-carbonate, neotaxol, novel taxol, 3'-(2-methyl-1-propenyl)paclitaxel, 3'-(2-methyl propyl) paclitaxel, 4a-paclitaxel, 4b-paclitaxel, 5a-paclitaxel, 10-desacetylpaclitaxel or 7-epi-paclitaxel.

Embodiment 3

[0038] Put 80 mg of PLGA (copolymer of glycolic acid and glycolic acid with a ratio of 75:25) with a molecular weight of 20,000 into a container, add 100 ml of dichloromethane to dissolve and mix well, then add 20 mg of paclitaxel, re-shake and remove by vacuum drying Organic solvents. The dried solid composition is melted to prepare slow-release pellets containing 20% ​​by weight of paclitaxel, the slow-release pellets are mixed with 1.5 mg of sodium carboxymethylcellulose and 15 mg of mannitol, and sterilized by radiation after sub-packaging Afterwards, paclitaxel sustained-release preparation for injection is made. The Paclitaxel Sustained-release Formulation for Injection is suspended in physiological saline (ordinary vehicle). Prepare the corresponding suspension type sustained release injection. The drug release time of the slow-release injection in physiological saline in vitro is 14-24 days, and the drug release time in mice subcutaneous is 20-35 days.

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Abstract

The invention relates to a slow-release injection of taxine anti-cancer drug, which comprises anti-cancer drug, slow-release finding, suspension and / or solvent. Wherein, said anti-cancer drug is taxine, 2'-hydroxy Paclitaxel, etc; the slow-release finding is polymer of hydroxyl, glycollic acid and glycolic acid, one of acetic acid ethyenyl ester polymer and polyphony; the suspension is polyphenyl (sodium), and mannite; the solvent is distilled water, injection water, absolute ethyl alcohol, etc. The invention can be injected to reduce the toxicity effect of drug, and improve the density locally to strengthen the treatment effect of chemotherapy and radiation therapy.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing taxine anticancer drugs, which belongs to the technical field of medicines. (2) Background technology [0002] As commonly used chemotherapeutic drugs, taxane anticancer drugs have been widely used in the treatment of various malignant tumors, and have achieved relatively obvious effects. However, further studies have found that there are still many problems in the treatment of various malignant tumors, especially solid tumors. Solid tumors have excessive expansive hyperplasia, and the interstitial pressure, tissue elastic pressure, fluid pressure, and interstitial viscosity are all higher than those of the surrounding normal tissue. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of brain tumors in rats" "Journal of Surgi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K45/00A61K9/00A61P35/00
Inventor 孔庆忠孙娟苏红清张婕
Owner 孔庆忠
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