Slow release injection containing anti-metabolism medicament and alkylating agent

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

Inactive Publication Date: 2007-08-08
JINAN KANGQUAN 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

[0113] 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, shake again 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

[0115] 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:

[0116] (1) 2-30% carmustine or nimustine;

[0117] (2) 5-40% fluorouracil, tegafur or capecitabine; or

[0118] (3) Combination of 5-40% fluorouracil, tegafur or capecitabine and 1-20% carmustine.

Embodiment 3

[0120]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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PUM

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Abstract

Disclosed is a slow release injection containing antimetabolites and/or alkylating agents, which comprises slow release microspheres and dissolvent, the slow release microspheres include antimetabolites selected from Tegafur, Capecittabine, Pemetrexed, Carmofur or Gemcitabine, and/or alkylating agent anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, poly(dodecanedioic acid-tetradecanedioic acid) or poly(fumaric acid-sebacylic acid). The alkylating agent is selected from Carmustine, Nimustine, Fotemustine, Lomustine or bendamustine. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 50 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 张红军邹会凤俞建江张婕
Owner JINAN KANGQUAN PHARMA TECH
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