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Anticancer medicine slow-release preparation containing platinum compound and its synergist

A technology of anticancer drugs and compounds, applied in the direction of active ingredients of heavy metal compounds, non-active ingredients of polymer compounds, antitumor drugs, etc., which can solve problems such as treatment failure and increased tolerance

Inactive Publication Date: 2006-10-25
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0130] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into the container, add 100ml dichloromethane, dissolve and mix well, then add 10mg Cisplatin and 10 mg doxorubicin were shaken again to prepare microspheres for injection containing 10% cisplatin and 10% doxorubicin by spray drying. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0132] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0133] (a) 2-30% heptaplatin, lobaplatin, nedaplatin, oxaliplatin, denaplatin or enloplatin;

[0134] (b) 2-40% bleomycin, daunorubicin, clarithromycin, dactinomycin, amrubicin, arubicin, detorubicin, esorubicin, carrubicin, Rhodobi, Liu Rubi, Medobi, Naimo Rubi, Zorobi, Aroubi, Dorobi, Table Rubi, Idarbi, Pirabi , valrubicin, mitomycin C, actinomycin D, loxoxantrone, mitoxantrone, pyroxantrone, tiloxantrone, or clozocin; or

[0135] (c) 2-30% of cisplatin, carboplatin, omaplatin, dextro-omaplatin, heptaplatin, lobaplatin, nedaplatin, oxaliplatin, denaplatin or enloplatin with 2-40% blemplatin Daunomycin, daunomycin, clarithromycin, dactinomycin, amrubicin, arubicin, detorubicin, ethorubicin, carrubicin, rhodorubicin, rhrubicin , medorubicin, naimorubicin, zorubicin,...

Embodiment 3

[0137] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of carboplatin and 15 mg of 5-FU, re-shake, and vacuum dry to remove organic matter. solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% carboplatin and 15% 5-FU, and then suspending in physiological saline containing 1.5% carboxymethylcellulose sodium to prepare the corresponding suspension sustained-release injections. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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PUM

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Abstract

The present invention relates to an anticarcinogen slow-released injection containing platinum compound and its synergist. It is composed of microsphere and solvent, in which the microsphere includes anticancer effective component and slow-released auxiliary material, the solvent is general one or special solvent containing suspension adjuvant. The anticancer effective component includes platinum compound selected from heptylplatin, loplatin, neidaplatin, oxaliplatin, denaplatin or enloplatin and / or platinum compound synergist selected from antitumor antibiotic, antimetabolite medicine, taxane and / or plant alkaloid; the slow-released auxiliary material is selected from polylactic acid copolymer, ethylene-vinylacetate copolymer, difatty acid and sebacic acid polymer and poly (fumaric acid-sebacic acid) copolymer. The suspension adjuvant is selected from sodium cellulose glycollate, and its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C). The slow-released microsphere also can be made into slow-released implant preparation.

Description

(1) Technical field [0001] The invention relates to an anticancer drug sustained-release agent loaded with a platinum compound and a synergist thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release compound anticancer drug containing a platinum compound and / or its synergist, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As a commonly used chemotherapeutic drug, platinum compounds have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its unexpected neurotoxicity greatly limits the application of this drug. Blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the penetration of chemotherapy drugs around the tumor and in the tumor tissue and diffusion (see Netti et al. "The i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/282A61K31/555A61K45/00A61K47/26A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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