Bortezomib pharmaceutical composition and applications thereof

A technology of bortezomib and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of poor compliance of patients, and achieve the effects of long-lasting drug effect, precise blood drug concentration, and stable proteasome inhibition level for a long time

Inactive Publication Date: 2018-06-26
NINGBO NINGRONG BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Bortezomib with a short half-life often produces a higher steady-state plasma peak / trough ratio (>100) after multiple injections, that is, a large fluctuation in plasma concentration, although the drug has a reversible effect on the proteasome Inhibition, but still lead to many safety problems in the preparation, and there is the problem of poor compliance of patients with multiple injections, which limits the further improvement and exertion of its clinical efficacy

Method used

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  • Bortezomib pharmaceutical composition and applications thereof
  • Bortezomib pharmaceutical composition and applications thereof
  • Bortezomib pharmaceutical composition and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0046] The preparation method of the multivesicular liposome of the present invention adopts conventional methods in the art, such as adopting the double emulsion method, specifically, it needs to include the following 5 steps: (1) first dissolve the lipid component of the prescription amount in easy The volatilized organic solvent (usually the mixed solution of chloroform or chloroform and ether) forms an oil phase, and the bortezomib of the recipe quantity is dissolved in water to form a drug-containing aqueous solution (the first water phase), and then with a suitable oil-water volume ratio ( The volume ratio is 1:10-12:10, v / v) by mixing the aqueous solution containing the drug (the first water phase) with the organic phase of the lipid (oil phase), and ultrasonically or mechanically shearing at room temperature for a certain period of time to prepare Uniform water-in-oil (W / O) type colostrum; (2) absorb the formed W / O type colostrum, and inject the second aqueous phase buf...

Embodiment 1

[0079] The preparation of embodiment 1 bortezomib in situ gel preparation (reservoir type preparation)

[0080]

[0081] After dissolving and dispersing the PEGylated PLA with N-methylpyrrolidone, the drug bortezomib is dissolved to obtain the in situ gel injection.

Embodiment 2

[0087] Embodiment 2: Preparation of bortezomib microspheres

[0088]

[0089] Dissolve bortezomib and PLGA in dichloromethane, and inject it into BUCHI B-290 with a drying temperature of 65°C, a spray frequency of 120kHz, and a ventilation rate of 70L / min at an injection rate of 0.2ml / min at a rate of 0.5ml / min. Dry the electrostatic collection system to prepare microspheres with uniform particle size, and 80% of the microspheres have a particle size of 0.5-10um.

[0090] The release test of the bortezomib microsphere of test embodiment 2 embodiment 2

[0091] The bortezomib microspheres of Example 2 were placed in the release medium of physiological isotonic PBS solution (pH 7.4) and incubated at 37°C, under the condition of 100r / min, at a predetermined time point, 5ml of the dissolution medium was taken, and centrifuged at 10000rpm for 5min , Precisely measure 20 μl of the supernatant and inject the filtrate into the liquid chromatograph, record the chromatogram, and mak...

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Abstract

The invention discloses a bortezomib pharmaceutical composition and applications thereof, wherein the bortezomib pharmaceutical composition comprises, by weight, 0.1-200 parts of bortezomib, 0.1-500 parts of an auxiliary material for adjusting release rate, 0-10 parts of a small molecule adjusting agent, and 0-2000 parts of a pharmaceutically acceptable injectable solvent. According to the presentinvention, the bortezomib pharmaceutical composition has the controlled drug release behavior, and can maintain the effective blood concentration and the proteasome inhibition level in the body; through the long-acting injection of the bortezomib pharmaceutical composition, the in vivo blood concentration and the efficacy providing of bortezomib can be controlled, the treatment effect of the drugcan e improved, the acting time can be prolonged, and the toxic-side effect of the drug can be reduced; the in vivo proteasome inhibition pharmaceutical composition with characteristics of high efficiency, long acting and low toxic-side effect is provided; and the invention further discloses uses of the bortezomib pharmaceutical composition in treatment of refractory / recurrent multiple myeloma.

Description

technical field [0001] The present invention relates to the fields of pharmaceutical preparations and biology, in particular to a pharmaceutical composition of bortezomib and its use for treating multiple myeloma and other cancers. The pharmaceutical composition has a controllable release behavior and can maintain a stable In vivo plasma concentration and long-lasting proteasome inhibitory activity. Background technique [0002] Bortezomib has the molecular formula C 19 h 25 BN 4 o 4 , with a molecular weight of 384.237, and its chemical name is: [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinecarboxy)amino]propyl] Amino]butyl]boronic acid, which has the following chemical structure: [0003] [0004] The function of the nuclear factor-KB (NF-KB) of the cell is to promote the protein family to initiate or promote the signal transduction in the nucleus, but it is blocked in the cytoplasm by the specific inhibitor NF-KB inhibitor (IKB) in normal cells and inactive....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61P35/00A61K9/16A61K9/06A61K9/10A61K9/127
Inventor 不公告发明人
Owner NINGBO NINGRONG BIOPHARMA CO LTD
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