Imatinib mesylate liposome preparation and preparation method thereof

A technology of imatinib mesylate and liposome preparations, which is applied in the field of imatinib mesylate preparations, can solve the problems of non-selectivity of tumor cells and harm to normal cells, and achieve enhanced anti-tumor Efficacy, preparation stability, and good reproducibility

Inactive Publication Date: 2017-05-31
QINGDAO HUANGHAI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although ordinary capsules and ordinary film-coated tablets are easy to prepare, because they are not selective for tumor cells, they will inevitably have harmful effects on normal cells after being absorbed into the blood. Therefore, it is very important to develop suitable dosage forms to reduce their toxic and side effects. necessary

Method used

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  • Imatinib mesylate liposome preparation and preparation method thereof
  • Imatinib mesylate liposome preparation and preparation method thereof
  • Imatinib mesylate liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043]

[0044] Prepare blank liposomes: Dissolve the prescribed amount of HSPC, CH, and PEG-DSPE (PEG molecular weight is 2000) in 10 mL of absolute ethanol at 55°C; inject into hydration medium preheated to the same temperature, and incubate for 10 minutes to obtain liposomes The primary plastid product: After the initial product was mixed with 200W ultrasonic for 2min, 400W ultrasonically dispersed for 4min (working for 1s, intermittent for 1s), and then passed through 0.8, 0.45, 0.22μm microporous membranes in turn to obtain blank liposomes .

[0045] Prepare drug liposome: get a certain amount of blank liposome, add appropriate amount of sodium phosphate-phosphate buffer (concentration is 100mmol L -1 ) to adjust the pH to 7.0, and inject the drug-lipid ratio of 1:10 (w / w) with imatinib mesylate solution. The measured encapsulation efficiency is 98.6%, and the particle size is 124nm.

[0046] At the same time, on the basis of the injections obtained above, the corres...

Embodiment 2

[0049]

[0050] The preparation process of the liposome initial product is the same as "Example 1", the liposome initial product is processed with micro jet (12000psi handles 2 cycles, 14000psi handles 2 cycles), then passes through 0.8, 0.45, 0.22, 0.10 successively , 0.05 μm microporous membrane to obtain blank liposomes. The blank liposome was loaded with drug according to the drug-lipid ratio and drug-loading conditions of "Example 1", and the liposome encapsulation efficiency was determined to be 95.2%, and the particle size was 116nm.

[0051] After adding trehalose in imatinib mesylate liposomes as a lyoprotectant (the ratio of trehalose to phospholipid dry weight is 4), freeze-dry according to conventional techniques to obtain imatinib mesylate Liposome formulations were lyophilized. When reconstituted, water for injection is added to the lyophilized liposome for reconstitution to obtain the imatinib mesylate liposome preparation. The encapsulation efficiency after...

Embodiment 3

[0053] Liposome membrane material is composed of HSPC, CH and mPEG 2000 -DSPE composed of HSPC and mPEG 2000 -The mass ratio of DSPE is 3:1, and the mass ratio of CH to HSPC is 1:0.5, 1:1, 1:1.5, 1:3, 1:5, 1:10, respectively, and the lipids without adding CH are prepared body. According to the method described in "Example 1", imatinib mesylate liposomes were prepared, and the encapsulation efficiency and particle size of the obtained liposomes are shown in Table 1.

[0054] Table 1 Effect of cholesterol content on liposome particle size and encapsulation efficiency

[0055]

[0056] As can be seen from Table 1, the cholesterol content in the prescription has a greater impact on the encapsulation efficiency and particle size of imatinib mesylate liposomes. When the prescription does not contain CH, the encapsulation efficiency of imatinib mesylate liposome is less than 10.0%; as the cholesterol content increases, the encapsulation efficiency increases gradually, when the ...

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Abstract

The invention relates to an imatinib mesylate preparation, in particular to an imatinib mesylate liposome preparation. Imatinib mesylate liposome comprises blank liposome and imatinib mesylate liposome original medicines, the blank liposome comprises phospholipid, cholesterol, hydrophilic polymer lipid derivatives, citric acid-sodium citrate solution and alkaline substances, the mass ratio of imatinib mesylate to the phospholipid ranges from 1:8 to 1:30, the mass ratio of the cholesterol to the phospholipid ranges from 1:1 to 1:8, and the mole ratio of the hydrophilic polymer lipid derivatives to the phospholipid ranges from 1:30 to 1:10. A preparation process includes the steps of blank liposome preparation, liposome grading, medicine loading and the like. The imatinib mesylate liposome preparation is high in liposome embedding ratio, uniform in particle size, low in cost and good in process repeatability.

Description

technical field [0001] The invention relates to a preparation of imatinib mesylate, in particular to a liposome preparation of imatinib mesylate. Background technique [0002] Imatinib mesylate belongs to the aniline-quinoline compound, which was developed by Novartis and is the world's first marketed tumorigenesis-related signal transduction inhibitor. It is clinically used for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia (Ph+CML ) in the chronic phase, accelerated phase or blast phase, for the treatment of adult patients with unresectable and / or metastatic malignant gastrointestinal stromal tumors (GIST). [0003] Imatinib mesylate is a selective tyrosine kinase inhibitor. Its specific mechanism of action is: imatinib can inhibit Bcr-Abl tyrosine kinase at the cellular level both in vivo and in vitro, and can selectively inhibit chronic myeloid myelopathy in Bcr-Abl positive cell line cells and Philadelphia chromosome positive (Ph+). Prolife...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/506A61K47/28A61K47/24A61K47/22A61P35/02A61P35/00
CPCA61K9/127A61K31/506A61K47/22A61K47/24A61K47/28
Inventor 牟琳琳李普成尤恒田大丰
Owner QINGDAO HUANGHAI PHARM CO LTD
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