Sustained-release injection containing nitrosourea drugs

A technology of sustained-release injection and nitrosourea, which is applied in the field of medicine and can solve problems such as treatment failure and enhanced tolerance

Inactive Publication Date: 2009-06-03
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 ce

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 carmustine, 20mg camptothecin, 10mg carmustine and 10mg camptothecin respectively, shake up again and prepare 20% carmustine, 20% camptothecin with spray drying method Injection microspheres of thecine, and 10% carmustine and 10% camptothecin. 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 60-70 days, and the release time in mouse subcutaneous is more than 65 days.

Embodiment 2

[0115] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the adjuvant used is p(BHET-EOP / TC) of 50:50, containing anticancer active ingredients and their weight percentages: 5-40% Combination of carmustine or nimustine with 1-20% camptothecin or hydroxycamptothecin.

Embodiment 3

[0117] 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 carmustine, 30mg camptothecin, 25mg carmustine and 5mg camptothecin, re-shake and prepare 30% carmustine, 30% camptothecin, 25% carmustine by spray drying method Injectable microspheres of statin and 5% camptothecin. 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 65-70 days, and the drug release time in mice subcutaneous is about 70 days.

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PUM

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Abstract

The invention provides a sustained-release injection containing nitrosourea drug (galamustine), which contains sustained-release microspheres and solvents. The sustained-release microspheres each comprise an anticancer-active component selected from nitrosourea drugs (such as nimustine and carmustine) and/or topoisomerase inhibitors, and a sustained-release agent. The solvents are common solvents or special solvents containing suspending agent. The viscosity of the suspending agent ranges from 100cp to 3000cp (at a temperature ranging from 20 DEG C to 30 DEG C). The suspending agent is selected from sodium carboxymethylcellulose and the like. The sustained-release agent is selected from p(LAEG-EOP) or p(DAPG-EOP) or other polyphosphate ester copolymers, or copolymer or blend of polyphosphate ester and PLA, polifeprosan, PLGA or poly(erucidic acid dipolymer-sebacic acid). The topoisomerase inhibitor is selected from camptothecin, hydroxycamptothecine, topotecan, lartotecan, irinotecan, etoposide or teniposide. The anticancer composition is also available in the dosage form of sustained-release implant, can retain the effective drug concentration for more than 60 days after intratumoral or local injection or implantation, can obviously reduce the systemic reaction to the drug, and can selectively enhance the curative effect of non-operative treatments such as radiotherapy and chemotherapy.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing nitrosourea drugs and topoase inhibitors and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a class of commonly used chemotherapeutic drugs, nitrosourea drugs 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 placement of camptothecin plus systemic camptothecin in the treatment of brain tumors in rats" "Journ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/7008A61K31/4745A61K47/34A61P35/00
Inventor 高化兰
Owner JINAN SHUAIHUA PHARMA TECH
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