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Anti-cancer medicine composition

A technology of anti-cancer drugs and compositions, which is applied in drug combinations, anti-tumor drugs, and pharmaceutical formulations, and can solve problems such as difficulty in forming effective drug concentrations

Inactive Publication Date: 2005-06-22
孔庆忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all 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 "Intratumoral placement of cisplatin plus systemic carmustine in the treatment of rat brain tumors" "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

[0193] The copolymer (PLGA) of lactic acid and glycolic acid that 90mg molecular weight is 10000 is put into container, after adding 100 milliliters of methylene chlorides to dissolve and mix well, add 10mg phosphoinositide 3-kinase inhibitors (7-O-alkyl- staurosporine), re-shake and vacuum-dry to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer drug composition containing 10% 7-O-alkyl-staurosporine. Put the drug-containing compound under the skin of mice, take it out regularly to measure the drug content, and calculate the cumulative release percentage (%) according to the remaining drug amount. It was found that 80-95% of the drug was released uniformly within 30 days.

Embodiment 2

[0195] The method of being processed into an anticancer pharmaceutical composition is the same as the examples, except that the phosphoinositide 3-kinase inhibitor in the first example is:

[0196] (a) 7-hydroxyl-staurosporine, β-methoxystaurosporine, alkylphosphocholine, hexadecylphosphorylcholine or octadecyl-(1,1-dimethyl-4 - piperidine) phosphate;

[0197] (b), phosphatidyl ether, 1-O-hexadecyl-2-O-methyl-radiocarbon-glyceryl-3-phosphocholine, 1-O-octadecyl-2-O-methyl- Carbo-glyceryl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-glyceryl-3-phosphocholine, or inositol polyphosphate; or

[0198] (c) Cyclosporin A, tetradecylphosphorylcholine, hexacylphosphoric acid (N-N-N-trimethyl) ethanolamine, octadecylphosphorylcholine or octadecyl-[2-(N -methylpiperidine)ethyl]-phosphate.

Embodiment 3

[0200] The steps of the method for processing the anticancer pharmaceutical composition are the same as in Example 1, but the pharmaceutical excipients used are one of the following a) to d):

[0201] a) Polylactic acid (PLA) with a molecular weight of 5000-15000, 10000-20000, 25000-35000 or 30000-50000;

[0202] b) Copolymers of polyglycolic acid and glycolic acid (PLGA) having a molecular weight of 5000-15000, 10000-20000, 25000-35000 or 30000-50000;

[0203] c) ethylene vinyl acetate copolymer (EVAc);

[0204] d) 10:90, 20:80, 30:70, 40:60, 50:50, or 60:40 p-carboxyphenylpropane (p-CPP):sebacic acid (SA) copolymer (polyphenylpropane ), are percentages by weight.

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PUM

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Abstract

The invention provides an anti-cancer medicine composition, which comprises anticancer active constituent and medicinal adjuvant, the anticancer active constituent employs phosphoinositide-3 and nitrosoureas, wherein the phosphoinositide-3 can effectively suppress the growth of the tumor cells, lower the survivability of tumor cells to Semustine anti-cancer drugs, and the medicinal adjuvant mainly employs biological compactable, degradable and absorbing, which can slowly release the phosphoinositide-3 kinase inhibitor onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. The anti-cancer medicinal composition also contain Nitrosoureas anti-cancer drugs, when locally dispensed on the tumor, the composition can lower down the whole body toxicity reaction of the anti-cancer medicament, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

Description

(1) Technical field [0001] The invention relates to an anticancer drug composition, which belongs to the technical field of drugs. (2) Background technology [0002] The treatment of solid tumors mainly includes surgery, radiotherapy and chemotherapy. Among the various chemotherapeutic drugs used, nitrosourea anticancer drugs have obvious effects and have been widely used in various malignant tumors. However, further research found that the DNA repair function in many tumor cells increased significantly after the treatment. The latter often leads to enhanced resistance of tumor cells to nitrosourea anticancer drugs, resulting in treatment failure. [0003] It has recently been found that inactivating or inhibiting intracellular DNA repair proteins can enhance the sensitivity of some tumor cells to chemotherapy, see Dolan et al. ""Cancer Research" 51 pp. 3367-3372 (1991) (Dolan et al., Cancer Res., 51, 3367-3372, 1991)). However, blood vessels, connective tissue, matrix p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61P35/00
Inventor 孔庆忠
Owner 孔庆忠
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