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Sustained-released injection including platinum compound and the alkylate agent

A sustained-release injection and compound technology, applied in the field of medicine, can solve problems such as treatment failure and increased tolerance

Inactive Publication Date: 2007-09-26
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

[0105] Put 80, 80 and 80 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 80: 20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 20mg cisplatin, 20mg carmustine, 10mg cisplatin and 10mg carmustine respectively, shake up again and prepare 20% cisplatin, 20% carmustine, And 10% cisplatin and 10% carmustine microspheres for injection. 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 sustained release injection in the physiological saline in vitro is 60-65 days, and the drug release time in the mouse subcutaneous is more than 60 days.

Embodiment 2

[0107] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that used auxiliary material is the p(BHET-EOP / TC) of 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0108] (1) 2-30% carmustine or nimustine;

[0109] (2) 5-40% cisplatin, nedaplatin, or carboplatin; or

[0110] (3) Combination of 5-40% cisplatin, nedaplatin or carboplatin and 1-20% carmustine or nimustine.

Embodiment 3

[0112] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg of cisplatin, 30mg of nimustine, 25mg of cisplatin and 5mg of nimustine, shake up again and use the spray drying method to prepare Nimustine microspheres for injection. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The release time of the slow-release injection in physiological saline in vitro is 65-70 days, and the release time in mice subcutaneously is about 65 days.

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PUM

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Abstract

The invention relates to an anti-cancer compound as a slow release injection which contains platinum compound and / or alkyl agent, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components and slow release findings, selected from platinum compound of kpeitabing, peimeiquse, caplatinum, or jxitabing and / or alkyl agent, the solvent is a common solvent or a special solvent with suspending agent, while the viscosity of suspending agent is 100cp-3000cp (at 20-30Deg. C), selected from carboxymethyl cellulose, the anti-cancer effective component is phosphoinositide 3-kinase restrainer and / or the phosphoinositide 3-kinase restrainer booster selected from self-anti-cancer antibiotics and / or tetrazine drug, the slow release finding is selected from phosphate polyester as p (LAEG-EOP) or p (DAPG-EOP), or the polyester or mixture of phosphate, PLA, polyphenyl, PLGA, poly (erucic acid dimmer-sebacic acid) or poly (fumaric acid-sebacic acid), and the alkyl agent is selected from ranimustine or the like. The anti-cancer compound can be made as slow release plant agent, to inject cancer or around cancer to hold the effective drug density for more than 60 days, while it can significantly reduce the general reaction of drug and selectively strengthen the effect of non-surgery treatments as chemotherapy or the like.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing a platinum compound and / or an alkylating agent and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, platinum compounds have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs. [0003] 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 carmustine plus systemic carmustine treatment of rat brain tumors" "Journal of Surgical O...

Claims

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Application Information

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IPC IPC(8): A61K31/282A61K31/505A61K9/10A61K45/00A61K47/30A61K47/38A61K47/10A61K47/36A61K47/34A61K47/42A61K9/00A61P35/00A61K47/26A61K47/32
Inventor 高化兰
Owner JINAN SHUAIHUA PHARMA TECH
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