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Slow released combination of anticancer drugs embedded in vivo

A technology of anticancer drugs and compositions, which is applied in the field of implanting anticancer drug compositions in vivo, which can solve the problems of difficult formation of effective drug concentration and dosage limitation, and achieve the effect of strengthening the anticancer effect

Inactive Publication Date: 2005-08-31
DASEN BIOLOGICAL PHARMA CO LTD
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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 are excessively expansive and hyperplastic, 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" 69 pages 76-82 (1998) (Kong Q et al., J Surg Oncol.1998 Oct; 69 (2 ):76-82), simply increasing the dosage is limited by systemic reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Put 90mg of PLGA (copolymer of glycolic acid and glycolic acid with a weight ratio of glycolic acid and glycolic acid of 25:75) with a molecular weight of 10000 into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg of docetaxel Match, shake again and vacuum dry to remove organic solvents. The dried solid composition is immediately shaped, and then ray sterilized after being dispensed to obtain an anticancer pharmaceutical composition containing 10% by weight of docetaxel. The drug release time of the anticancer drug composition in the in vitro physiological saline is 15-30 days, and the drug release time under the skin of the mouse is 30-45 days.

Embodiment 2

[0045] Example 2. As described in Example 1, the difference is that the active ingredient contained is one of the following:

[0046] 2'-hydroxypaclitaxel, 10-deacetylbaccatin III, 14β-hydroxy-10-deacetylbaccatin III, 9-dihydro-13-baccatin III, 13-(N-tri- Butoxycarbonyl-β-isobutylisoserine)-14-hydroxybaccatin-1,14-carbonate, new paclitaxel, strange new paclitaxel, 3'-(2-methyl-1-propenyl ) Paclitaxel, 3'-(2-methylpropyl)paclitaxel, 4a-paclitaxel, 4b-paclitaxel, 5a-paclitaxel, 10-deacetylpaclitaxel, 7-epi-paclitaxel, baccatin, baccatin III , Baccatin V, spruce yew, Canadian yew, berry yew, Chinese yew, sharp tooth yew, cultivated yew, Yunnan yew or Florida yew, the active ingredients are in the anticancer drug composition The weight percentage is 5-30%.

Embodiment 3

[0048] Put 90 mg of pharmaceutical excipient ethylene vinyl acetate copolymer (EVAc) into a container, add 100 ml of dichloromethane to dissolve and mix, add 10 mg of 7-epi-paclitaxel, shake again, and vacuum dry to remove organic solvents. The dried solid composition is immediately shaped, and then irradiated to sterilize the dried solid composition to obtain an anticancer pharmaceutical composition containing 10% by weight of 7-epi-paclitaxel. The drug release time of the anticancer drug composition in vitro in physiological saline is 14-24 days, and the drug release time under the skin of mice is 20-35 days.

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PUM

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Abstract

A slowly-releasing anticancer medicine able to be implantated in human body is composed of the anticancer Duoxitasai and / or its derivative and the biosoluble and biodegradable high-molecular polymer for slowly releasing said medicine to the cancer position.

Description

(1) Technical field [0001] The invention relates to an anti-cancer pharmaceutical composition, which is mainly a slow-release anti-cancer pharmaceutical composition implanted in the body, belonging to the technical field of medicines. (2) Background technology [0002] As a commonly used chemotherapeutic drug, docetaxel and its derivatives have been widely used in the treatment of a variety of malignant tumors, and have achieved relatively obvious effects. However, further studies have found that there are still many problems in the treatment of many malignant tumors, especially solid tumors. For solid tumors with excessive swelling and hyperplasia, the interstitial pressure, tissue elastic pressure, fluid pressure, and interstitial viscosity are higher than those of the surrounding normal tissues. 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 syste...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61P35/00
Inventor 孔庆忠
Owner DASEN BIOLOGICAL PHARMA CO LTD
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