Bivalirudin injection preparation and preparation method thereof

A technology for bivalirudin and injection preparations, which is applied in the field of medicine and can solve the problems of long time for bivalirudin to separate out and make liquid

Pending Publication Date: 2021-06-18
JIANGSU HANSOH PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of this, the present invention solves the problems of bivalirudin precipitation and long liquid preparation time during the liqu

Method used

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  • Bivalirudin injection preparation and preparation method thereof
  • Bivalirudin injection preparation and preparation method thereof
  • Bivalirudin injection preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] ① Measure 80% of the prescription amount (100ml’) of purified water into a beaker, and the water temperature is 30°C;

[0020] ②Add 2.5g of mannitol and magnetically stir until completely dissolved;

[0021] ③Add 5.0g (calculated as bivalirudin) of the crude drug, and magnetically stir until completely dissolved;

[0022] ④Use 15% (w / v) sodium hydroxide to adjust the pH of the solution, and control the addition rate of sodium hydroxide to 0.001875ml / min (time for adding sodium hydroxide) / ml (medicine solution) by a peristaltic pump 注1 ;

[0023] ⑤ Set the volume by weight (the density is 1.025g / ml), stir for 30 minutes after constant volume, and finally measure the pH of the liquid to 5-6. After constant volume, the drug solution was placed at ≤25°C to measure the stability of the drug solution within 12 hours.

[0024] Note 1: The amount of sodium hydroxide solution that per ml of liquid medicine is exposed to per minute.

Embodiment 2

[0026] ① Measure 80% of the prescription amount (100ml’) of purified water into a beaker, and the water temperature is 30°C;

[0027] ②Add 2.5g of mannitol and magnetically stir until completely dissolved;

[0028] ③Add 5.0g (calculated as bivalirudin) of the crude drug, and magnetically stir until completely dissolved;

[0029] 4. Regulate the pH of the solution with 5% (w / v) sodium hydroxide, and control the sodium hydroxide addition rate by a peristaltic pump to be 0.001875ml / min (the time of adding sodium hydroxide) / ml (medicine solution);

[0030] ⑤ Set the volume by weight (the density is 1.025g / ml), stir for 30 minutes after constant volume, and finally measure the pH of the liquid to 5-6. After constant volume, the drug solution was placed at ≤25°C to measure the stability of the drug solution within 12 hours.

Embodiment 3

[0032] ① Measure 80% of the prescription amount (100ml’) of purified water into a beaker, and the water temperature is 30°C;

[0033] ②Add 2.5g of mannitol and magnetically stir until completely dissolved;

[0034] ③Add 5.0g (calculated as bivalirudin) of the crude drug, and magnetically stir until completely dissolved;

[0035] 4. Regulate the pH of the solution with 5% (w / v) sodium hydroxide, and control the sodium hydroxide addition rate by a peristaltic pump to be 0.001875ml / min (the time of adding sodium hydroxide) / ml (medicine solution);

[0036] ⑤ Set the volume by weight (the density is 1.025g / ml), stir for 30 minutes after constant volume, and then measure the pH of the liquid.

[0037] After constant volume, the medicinal solution was placed at 30°C to measure the stability of the medicinal solution within 12 hours.

[0038] Conclusion: Through the comparison of Example 2 and Example 3, with the prolongation of time, the impurity C has a tendency to increase, but a...

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Abstract

The invention discloses a bivalirudin injection preparation and a preparation method thereof. The injection preparation comprises bivalirudin or a pharmaceutically acceptable salt thereof, an excipient, a pH regulator and a solvent, and the pH value of the injection preparation is 5.0-7.0. In the production process, by controlling the adding speed of sodium hydroxide and the preparation temperature of the liquid medicine, the stability of the liquid medicine can be guaranteed, meanwhile, the liquid medicine is rapidly mixed, the preparation time is shortened, energy consumption is reduced, and the production efficiency is improved. Meanwhile, according to the preparation process of the valirudin injection preparation, degradation of an impurity A and an impurity C is effectively reduced, and the safety of clinical use is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a bivalirudin injection preparation and a preparation method thereof. Background technique [0002] Bivalirudin is a specific reversible direct thrombin inhibitor derived from hirudin derivatives, which can directly inhibit the action of thrombin by specifically binding to the anion of the catalytic site of thrombin. Bivalirudin consists of 20 amino acids, the molecular weight is 2180.33, the molecular formula is C98H138N24O33, and the CAS number is 128270-60-0. Bivalirudin has the characteristics of poor stability, easy to be hydrolyzed by proteolytic enzymes in the gastrointestinal tract, short half-life, and poor passability of biological barriers. Bivalirudin for injection, the trade name of the original preparation is Developed by the American Medicine Company and approved for marketing in the United States (N020873) on December 15, 2000, it is used for patie...

Claims

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Application Information

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IPC IPC(8): A61K38/58A61K9/08A61K47/02A61K47/26A61P7/02
CPCA61K9/0019A61K9/08A61K38/58A61K47/02A61K47/26A61P7/02
Inventor 董礼于婷崔畅畅杨宝海余俊
Owner JIANGSU HANSOH PHARMA CO LTD
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