Dabigatran etexilate pharmaceutical composition for injection, preparation method and uses thereof

A technology of dabigatran etexilate and composition, applied in the field of injection dabigatran etexilate pharmaceutical composition and its preparation, can solve the problems of low bioavailability, difficult process, life-threatening, etc. Simplicity, increased exposure, and low production costs

Pending Publication Date: 2018-12-18
SHANGHAI MEIYUE BIOTECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The hard capsule is not only very difficult in technology, but also has very low bioavailability (3-7%) in the human body.
Oral bioavailability may be increased by up to 75% when the granules are taken directly from the hydroxypropyl methylcellulose (HPMC) capsule shell compared to the reference capsule, resulting in bleeding and even life-threatening

Method used

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  • Dabigatran etexilate pharmaceutical composition for injection, preparation method and uses thereof
  • Dabigatran etexilate pharmaceutical composition for injection, preparation method and uses thereof
  • Dabigatran etexilate pharmaceutical composition for injection, preparation method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 prepares dabigatran etexilate pharmaceutical composition for injection 1

[0033] 1) Prescription: based on 1000 bottles (specification: 40mg / bottle)

[0034] Active substance dabigatran etexilate I-2 40g

[0035] Macrogol Stearate 15 150mL

[0036] PBS buffer 850mL

[0037] 2) Preparation method:

[0038] Weigh the active substance dabigatran etexilate I-2 and polyethylene glycol stearate 15 of the prescription amount, add an appropriate amount of PBS buffer solution, after stirring and dissolving, continue to add to the prescription amount, after stirring evenly, add a solution amount of 0.1 % (w / v) medicinal activated carbon, after stirring and adsorbing for 30 minutes, decarbonize with a Φ0.45μm microporous membrane, and then use a Φ0.22μm microporous membrane to filter and sterilize.

[0039] Then put the above filter-sterilized product into the labconco FreeZone freeze dryer for freeze-drying. Finally, after subpackaging, plugging, capping, and f...

Embodiment 2

[0040] Embodiment 2 prepares dabigatran etexilate pharmaceutical composition for injection 2

[0041] 1) Prescription: based on 1000 bottles (specification: 40mg / bottle)

[0042] Active substance dabigatran etexilate I-2 40g

[0043] Olive oil 1000mL

[0044] 2) Preparation:

[0045] The active substance dabigatran etexilate I-2 of prescription quantity is taken, add olive oil appropriate, after stirring and dissolving, continue to add to prescription quantity, after stirring, add the medicinal gac of solution quantity 0.1% (w / v), After stirring and adsorbing for 30 minutes, decarbonize by filtration with a Φ0.45 μm microporous membrane, and then filter and sterilize with a Φ0.22 μm microporous membrane. Finally, after sub-packaging, plugging, capping, and full inspection, the pharmaceutical composition 2 of dabigatran etexilate for injection of the present invention is obtained.

Embodiment 3

[0046] Embodiment 3 prepares dabigatran etexilate pharmaceutical composition for injection 3

[0047] 1) Prescription: based on 1000 bottles (specification: 40mg / bottle)

[0048] Active substance dabigatran etexilate I-2 40g

[0049] Polyethylene glycol PEG-400 1000mL

[0050] 2) Preparation:

[0051] Take the active substance dabigatran etexilate I-2 of the prescription amount, add polyethylene glycol PEG-400 in an appropriate amount, after stirring and dissolving, continue to add to the prescription amount, after stirring evenly, add solution amount 0.1% (w / v) After stirring and adsorbing for 30 minutes, decarbonize with a Φ0.45μm microporous membrane, and then use a Φ0.22μm microporous membrane to filter and sterilize. Finally, after sub-packaging, plugging, capping, and full inspection, the pharmaceutical composition 3 of dabigatran etexilate for injection of the present invention is obtained.

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Abstract

The present invention relates to a dabigatran etexilate pharmaceutical composition for injection, a preparation method and uses thereof, wherein the dabigatran etexilate pharmaceutical composition comprises: (1) an active substance dabigatran etexilate represented by a formula I-2, (2) a pharmaceutically acceptable solvent, and optionally (3) other pharmaceutically acceptable excipients. Accordingto the present invention, the test results show that various indexes of the dabigatran etexilate pharmaceutical composition meet the relevant drug regulations, and the safety, the resolubility and the long-term stability are good; the pharmacokinetic test results show that the dabigatran etexilate pharmaceutical composition can maintain the proper blood drug level and the proper treatment duration time in the body after administration, and the pH value is neutral so as to greatly reduce the stimulating effect on gastrointestinal tract; and the preparation method has characteristics of simplepreparation process, convenience, feasibility, good repeatability and low production cost, and is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a sustained-release preparation of marketed drugs, in particular to a pharmaceutical composition of dabigatran etexilate for injection, a preparation method and application thereof. Background technique [0002] Cardiovascular disease is currently one of the leading causes of human death, and one of its main aspects is thrombosis, which is caused by a series of complex reactions that cause blood coagulation. Blood coagulation is a protective mechanism of the organism by which it quickly and reliably "seals" defects in the vessel wall, thus avoiding or minimizing blood loss, maintaining normal hemostasis, that is, the balance of bleeding and coagulation, is regulated by a complex mechanism. Unregulated activation of the coagulation system or lack of inhibition of the activation process can lead to various diseases and complications, such as venous thrombosis, deep vein thrombosis, pulmonary embolism, atherosclerosis, acute coro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4439A61P7/02A61P9/10A61P11/00
CPCA61K47/10A61K47/14A61K47/26A61K47/44A61K9/0019A61K31/4439
Inventor 冯焱胡治隆王小林李世强余尚海陈永凯张轶涵王朝东
Owner SHANGHAI MEIYUE BIOTECH DEV
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