Slow-released injection containing bendamustine and its synergist

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

Inactive Publication Date: 2006-10-18
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

[0109] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Bendamustine and 10 mg camptothecin were re-shaken and spray-dried to prepare microspheres for injection containing 10% bendamustine and 10% camptothecin. 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 15-25 days, and the drug release time in mice subcutaneous is about 30-40 days.

Embodiment 2

[0111] 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:

[0112] 2-40% bendamustine with 5-30% camptothecin, hydroxycamptothecin, letotecan, topotecan, irinotecan, etoposide, teniposide, amdex Combinations of Bixing, Erubicin, Rhodobiicin, Liurubicin, Zorubicin, Valrubicin or Idarubicin.

Embodiment 3

[0114] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of bendamustine and 15 mg of O6-benzylguanine, and re-shake After homogenization, the organic solvent was removed by vacuum drying. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 10% bendamustine and 10% O6-benzylguanine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose, 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 30-35 days.

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PUM

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Abstract

The slow released anticancer preparation consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is bendamustine and/or bendamustine synergist of topoisomerase inhibitor, guanine analogue, tetrazine compound and/or platinum compound; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, etc of viscosity of 100-3000 cp(at 20-30 deg.c). The slow released microballoon may be also prepared into slow released implantation preparation. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing bendamustine and / or its synergist and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As a commonly used chemotherapeutic drug, bendamustine has been widely used in the treatment of various malignant tumors, and its effect is relatively obvious. However, its unexpected neurotoxicity greatly limits the application of this drug. Blood vessels, connective tissue, matrix proteins, fibrinoproteins, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the diffusion of chemotherapy drugs around the tumor and in the tumor tissue. Infiltration and diffusion (see Netti et al. "The influence of the status of the extracellular matrix on the drug delivery in solid tumors" "Cancer Research" 60 pp. 2497-503 (2000) (Netti PA, Cancer Res.2000, 60 (9 ): 2497-503))....

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4184A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 孔庆霞
Owner JINAN SHUAIHUA PHARMA TECH
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