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Preparation method of tinib drug alhumin nano preparation used for injection

A technology of albumin nanometer and albumin nanoparticle, which is applied in the directions of drug combination, pharmaceutical formula, medical preparation containing active ingredients, etc., can solve the problems of large amount of phospholipid, difficult industrialization of preparation process, poor stability, etc., and achieves reduction of dosage. , the effect of increasing stability and application security, and expanding the range of choices

Inactive Publication Date: 2016-06-01
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is aimed at the low drug loading of nanoparticles (only 2-5%), poor stability, large amount of phospholipids (up to 50-75%) in the prior art, which is easy to cause toxic and side effects, and the preparation process is difficult to industrialize etc. Shortcomings and deficiencies, provide a kind of preparation method of albumin nano-preparation of tinib medicine for injection, this preparation method can greatly improve the drug content of described preparation (drug loading can reach up to 20%), strengthen the nanoparticle Stability (the nanosuspension can be stable for 15 days at room temperature) and safety (reduce the amount of phospholipid or adjust the type of solubilizer), this method is suitable for industrial production of albumin nanoparticles

Method used

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  • Preparation method of tinib drug alhumin nano preparation used for injection
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  • Preparation method of tinib drug alhumin nano preparation used for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: The parameter of high-pressure homogenization is for the influence of preparation albumin nanoparticle particle size

[0043] Weigh a certain amount of icotinib and polyoxyethylene castor oil and dissolve it in a mixed solvent of chloroform and ethanol as the oil phase, add it to the aqueous solution of human serum albumin, and control the volume ratio of the oil phase and the water phase to 1 :20~1:80, the mass ratio of icotinib to albumin is 1:5~1:10. Utilize high-shear dispersing emulsifier to emulsify (rotating speed: 5000r / min, shearing time: 10min) to form colostrum, quickly transfer to high-pressure homogenizer, homogenize according to the conditions in Table 1, and the obtained nanoemulsion is removed by thin film evaporation Organic solvent, that is, albumin nanoparticle suspension loaded with icotinib.

[0044] It can be seen from Table 1 that when the high-pressure homogenization pressure is increased from 5000psi to 15000psi, the particle size...

Embodiment 2

[0047] Example 2: Comparison of the amount of phospholipids required for the preparation of nanoparticles by the method of the present invention and the method of patent 2012101304132

[0048] Dissolve sorafenib and hydrogenated soybean lecithin in different proportions in dichloromethane as the oil phase, add human serum albumin aqueous solution with a pH of 4 to 7, and control the volume ratio of the oil / water phase to 1:50 to 1:100 , the mass ratio of sorafenib to albumin is 1:5-1:12. Sorafenib-loaded albumin nanoparticles were prepared by the method of the present invention and the method of patent 2012101304132 respectively, and the particle size was measured. The results are shown in Table 2.

[0049] The impact of the amount of hydrogenated soybean lecithin on the particle size of nanoparticles in the prescription of table 2

[0050]

[0051]

[0052] It can be seen that when the amount of hydrogenated soybean lecithin is used as a solubilizer, the particle size ...

Embodiment 3

[0053] Example 3: Comparison of the stability of nanoparticles prepared by the method of the present invention and the method of patent 2012101304132

[0054] The albumin nanoparticles loaded with icotinib in Example 1 were prepared by the method of the present invention and the method of patent 2012101304132 respectively. Place the two suspensions of icotinib albumin nanoparticles at room temperature, observe their appearance and measure the particle size at 0, 3, 6, 9, 12, and 15 days respectively (attached figure 1 ). As a result, the icotinib-loaded albumin nanoparticle suspension prepared by the method of patent 2012101304132 showed obvious drug precipitation on the 3rd to 6th day, and the particle size reached the μm level. However, the nanoparticle suspension prepared by the method of the present invention has better stability, no obvious suspension layering or precipitation was observed within 15 days, and the particle diameter of the nanoparticle slightly increased t...

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Abstract

The invention belongs to the field of medicinal preparation, and relates to a preparation method of a tinib drug alhumin nano preparation used for injection. According to the preparation method, a tinib drug is dissolved in an oil phase; a mixture is prepared from the oil phase and a human serum albumin water phase; the mixture is delivered into a high pressure homogenizer for high shearing so as to obtain a nano preparation; organic solvents are removed via thin film evaporation; and a finished product is obtained via freeze drying. A solubilizer, an oil stabilizing agent, and a pH adjusting agent are added so as to ensure the stability of the nano particles, relatively small particle size, and narrow particle size distribution. Reproducibility of the preparation method is excellent; content of the tinib drug in the nano particles can be increased; corresponding sets of apparatus from laboratory scale to large-scale production scale of the adopted technologies are available; and industrial production application prospect is promising.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a method for preparing an albumin nano-preparation of tinib drugs for injection. The method prepares insoluble tinib drugs into soluble albumin nano-particle preparations for injection, and the method has good reproducibility , can greatly increase the drug loading capacity of nanoparticles, enhance their stability and safety, and are suitable for industrial production. Background technique [0002] The prior art discloses that tinib drugs are a class of molecular targeted drugs developed in recent years and successfully applied clinically. These drugs are mainly used for non-small cell lung cancer, breast cancer, pancreatic cancer, kidney cancer, melanoma, chronic The treatment of cancers such as myeloid leukemia mainly inhibits tumor growth by specifically targeting and inhibiting the activity of tyrosine kinase, and its anti-tumor effect is good. Among them, imatinib ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/42A61K45/00A61K31/506A61K31/5377A61P35/00A61P35/02
Inventor 张奇志万旭庞晓莹高会乐蒋新国
Owner FUDAN UNIV
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