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Sustained-released injection including antimetabolite medicine and alkylate agent

A slow-release injection, anti-metabolism technology, applied in the field of medicine, can solve problems such as treatment failure and enhanced 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

[0107] 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 fluorouracil, 20mg carmustine, 10mg fluorouracil and 10mg carmustine respectively, re-shake and use spray drying method to prepare 20% fluorouracil, 20% carmustine, and 10% carmustine Microspheres for Injection of Fluorouracil and 10% Carmustine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 50-60 days, and the release time in mice subcutaneously is more than 50 days.

Embodiment 2

[0109] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that the p(BHET-EOP / TC) that used adjuvant is 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0110] (1) 2-30% carmustine or nimustine;

[0111] (2) 5-40% fluorouracil, tegafur or capecitabine; or

[0112] (3) Combination of 5-40% fluorouracil, tegafur or capecitabine and 1-20% carmustine.

Embodiment 3

[0114]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 fluorouracil, 30mg of nimustine, 25mg of fluorouracil and 5mg of nimustine, re-shake and use spray drying method to prepare 30% fluorouracil, 30% nimustine, 25% fluorouracil and 5% 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 drug release time of the sustained release injection in physiological saline in vitro is 55-60 days, and the drug release time in mice subcutaneous is about 60 days.

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Abstract

The invention relates to a slow release injection which contains antimetabolite and / or alkyl agent, formed by slow release micro ball and solvent. The slow release micro ball comprises the anti-cancer effective components 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 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 50 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 slow-release injection containing anti-metabolite drugs and / or alkylating agents and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, anti-metabolite drugs have been widely used in the treatment of various malignant tumors, and the effect is more 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 Oncology"...

Claims

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Application Information

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IPC IPC(8): A61K31/7068A61K9/10A61K45/00A61K47/30A61K47/38A61K47/10A61K9/00A61P35/00A61K31/505
Inventor 孔庆霞
Owner JINAN SHUAIHUA PHARMA TECH
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