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Slow-released injection containing methotrexate and its synergist

A technology for sustained-release injection and methotrexate, which is applied in the field of sustained-release injection and its preparation, sustained-release injection and sustained-release implant, and can solve the problems of many complications, easy generation of drug resistance, poor sensitivity of anticancer drug methotrexate, etc.

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

However, solid sustained-release implants (Chinese Patent No. ZL96115937.5; ZL97107077.6) and existing sustained-release microspheres for the treatment of brain tumors (ZL00809160.9) or U.S. Patent (US5,651,986) all have inadequacies. Easy operation, poor curative effect, many complications, etc.
In addition, many solid tumors are less sensitive to anticancer drugs, including methotrexate, and are prone to drug resistance during treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0119] 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 Methotrexate and 7-hydroxyl-staurosporine, re-shake and spray-dry to prepare microspheres for injection containing 10% methotrexate and 10% 7-hydroxyl-staurosporine. 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 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0121] 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:

[0122] 2-40% of 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkylphosphocholine, hexadecylphosphocholine, Octadecyl-(1,1-dimethyl-4-piperidine) phosphate, 1-O-hexadecyl-2-O-methyl-radio-propanetriyl-3-phosphocholine, 1 -O-octadecyl-2-O-methyl-sn-propanetriyl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-propanetriyl-3- Phosphocholine, inositol polyphosphate, cyclosporin A, tetradecylphosphorylcholine, hexacylphospho(N-N-N-trimethyl)hexanolamine, octadecylphosphorylcholine or octadecylphosphorylcholine Base-[2-(N-methylpiperidinium)ethyl]-phosphate; or

[0123] 2-40% methotrexate with 2-40% 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkylphosphocholine, Hexadecylphosphorylcholine, octadecyl-(1,1-dimethyl-4...

Embodiment 3

[0125] 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 methotrexate and 15 mg of 7-ethyl-10-hydroxycamptothecin, and re- Shake well and dry under vacuum to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 10% methotrexate and 10% 7-ethyl-10-hydroxycamptothecin, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose , to 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 20-30 days.

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Abstract

The slow released anticancer injection containing methotrexate and its synergist 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 methotrexate synergist or the composition of methotrexate and its synergist; the methotrexate synergist is selected from phosphorinositide 3-kinase (PI3K) inhibitor, pyrimidine analogue and DNA repair enzyme inhibitor; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, etc. 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 sustained-release injection of methotrexate and its synergist and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a sustained-release preparation of anticancer drugs containing methotrexate synergist or methotrexate and its synergist, mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] As a commonly used chemotherapeutic drug, methotrexate 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. I...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/5025A61K45/00A61K47/26A61K47/32A61K47/34A61K47/38A61P35/00
Inventor 孔庆霞
Owner JINAN SHUAIHUA PHARMA TECH
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