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Drug composition of bortezomib and preparation method thereof

A technology of bortezomib and its composition, which is applied in the field of medicine, can solve the problems of poor resolubility of freeze-dried powder injections, and achieve the effects of accelerating dissolution, excellent stability, and ensuring physiological effects

Inactive Publication Date: 2014-11-05
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The object of the present invention is to provide a pharmaceutical composition of bortezomib, which can quickly dissolve bortezomib, thereby rapidly reacting with polyalcohol excipients such as mannitol to form a more stable borate ester, However, when the pharmaceutical composition is prepared into a freeze-dried powder injection, there is no need to add additional antioxidants, which can well solve the stability problem of the bortezomib freeze-dried powder injection itself and the problem of poor resolubility.

Method used

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  • Drug composition of bortezomib and preparation method thereof
  • Drug composition of bortezomib and preparation method thereof
  • Drug composition of bortezomib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Preparation Example 1, Bortezomib freeze-dried powder injection

[0047] Prescription:

[0048]

[0049]

[0050] Preparation:

[0051] 1) Weigh 3.5g bortezomib, 1.75g ​​tert-butanol, 35g mannitol and 3.5g sodium chloride according to the above prescription;

[0052] 2) Add the prescribed amount of bortezomib into the liquid preparation tank, then add the prescribed amount of tert-butanol, seal the container to obtain a suspension, heat the suspension to 45°C for 5 minutes to completely dissolve the drug, and obtain a solution;

[0053] 3) Add 80% of water for injection to the solution in step 2), stir, then add the prescribed amount of mannitol and sodium chloride, stir the resulting mixture to dissolve completely, cool to room temperature; then add 20% of the prescribed amount of water for injection, stir to fully uniform;

[0054] 4) The prepared solution is sterilized by secondary terminal filtration through a 0.22 μm microporous membrane to obtain a filt...

Embodiment 2

[0059] Formulation example 2, bortezomib freeze-dried powder injection

[0060] Prescription:

[0061]

[0062] Preparation:

[0063] 1) Weigh 3.5g bortezomib, 1.75g ​​tert-butanol, 17.55g mannitol and 17.5g sodium chloride according to the above prescription;

[0064] 2) Add the prescribed amount of bortezomib to the liquid preparation tank, then add the prescribed amount of tert-butanol, seal the container to obtain a suspension, heat the suspension to 40°C for 3 minutes to completely dissolve the drug, and obtain a solution;

[0065] Step 3) and step 4) are the same as the preparation example 1;

[0066] The low-temperature freeze-drying described in step 5) includes the following three stages:

[0067] Pre-freezing stage: lower the temperature of the shelf to -50°C, put the product in quickly, and keep the temperature for 3 hours after the temperature of the product reaches -37°C, and keep the vacuum in the box at 8Pa;

[0068] Primary drying stage: keep the vacuu...

Embodiment 3

[0070] Preparation Example 3, Bortezomib freeze-dried powder injection

[0071] Prescription:

[0072]

[0073] Preparation:

[0074] 1) Weigh 3.5g bortezomib, 1.75g ​​tert-butanol, 70g mannitol and 10.5g sodium chloride according to the above prescription;

[0075] 2) Add the prescribed amount of bortezomib into the liquid preparation tank, then add the prescribed amount of tert-butanol, seal the container to obtain a suspension, heat the suspension to 48°C for 8 minutes to completely dissolve the drug, and obtain a solution;

[0076] Step 3) and step 4) are the same as the preparation example 1;

[0077] The low-temperature freeze-drying described in step 5) includes the following three stages:

[0078] Pre-freezing stage: lower the temperature of the shelf to -50°C, put the product in quickly, and keep the temperature for 5 hours after the temperature of the product reaches -33°C, and keep the vacuum in the box at 12Pa;

[0079] Primary drying stage: keep the vacuu...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a drug composition of bortezomib and a preparation method thereof. The drug composition disclosed by the invention contains bortezomib, tert butyl alcohol, sodium chloride and an excipient in the mass ratio of 1:0.5:(1-5):(5-20). The drug composition adopts freeze-dried powder injection or water injection, preferably the freeze-dried powder injection. The drug composition contains tert butyl alcohol and sodium chloride besides the conventional excipient; through adding tert butyl alcohol, bortezomib can be rapidly dissolved and rapidly reacted with polyalcohol excipients such as mannitol to form more stable borate, so that the stability problem of the bortezomib freeze-dried powder injection per se is solved; and through adding the drug active constituent i.e. sodium chloride, the normal physiological and biochemical activities and functions in vivo are fully guaranteed.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition of bortezomib and a preparation method thereof. Background technique [0002] Bortezomib (PS-341), trade name Velcade, is a new type of anti-tumor drug developed by Millennium Pharmaceutical Company of the United States. The drug leads to the death of tumor cells by blocking the degradation of various proteins that regulate apoptosis and signal transduction in cells. A large number of studies have found that bortezomib has strong anti-tumor activity against a variety of tumors, especially multiple myeloma, mantle cell lymphoma, other B-cell lymphomas, and Hodgkin's lymphoma in hematological tumors. [0003] Yi Wenyuan and others pointed out in "Research Progress of Proteasome Inhibitors Reversing Multidrug Resistance of Tumors" ("Foreign Medicine and Pharmacy Volume", April 2007, Volume 34, Issue 2) that boronic acid peptides include bor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/05A61K33/14A61K31/69A61K9/19A61K47/10A61P35/00
Inventor 钟正明陈颖江王小树马鹰军
Owner HAINAN JINRUI PHARMA CO LTD
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