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Nicergoline lyophilized preparation with excellent stability

A kind of technology of nicergoline and excipient, applied in the composition of new nicergoline freeze-dried preparation and its production field, can solve problems such as gap, absolute bioavailability less than 5%, complex process or composition, and avoid harm , Stability improvement, Stability improvement effect

Active Publication Date: 2019-07-19
湖北科莱维生物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is rapidly and almost completely absorbed after oral administration, its absolute bioavailability is less than 5% due to the first-pass effect and unstable factors
It can be seen that the stability and resolubility of nicergoline freeze-drying are a challenge faced by the preparation, but the above-mentioned patented technology also has certain deficiencies. Compared with the original formulation formulation, the process or ingredients are more complicated, organic solvents, Antioxidants, surfactants, etc. also introduce new safety risks. At the same time, there is a considerable gap in the stability of the above-mentioned existing formulations compared with the original formulations.

Method used

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  • Nicergoline lyophilized preparation with excellent stability
  • Nicergoline lyophilized preparation with excellent stability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] A kind of Nicergoline freeze-dried powder injection for injection, it is made up of following components: Nicergoline 2g, tartaric acid 0.5g, mannitol 20g, sodium chloride 0.5g. Dissolve tartaric acid, mannitol, and sodium chloride in about 800g of water for injection (20-25°C), stir until dissolved, add Nicergoline and continue stirring until it is completely dissolved, make up water for injection to 1000g, and check that the pH value should be 3.0 -5.0. After being filtered by a 0.22 micron microporous membrane, it is filled in a vial, half-tightened, and placed in a freeze dryer for freeze-drying in the following specific ways:

[0033] Pre-freezing: reduce the temperature of the shelf to -40°C in 2 hours and maintain it for 2 hours.

[0034] The first stage of drying: After pre-freezing, vacuumize, the vacuum degree is controlled at ≤10pa, the temperature of the partition is raised to -10°C in 1 hour, and maintained for 6 hours, and the temperature of the partition...

Embodiment 2

[0039] A kind of Nicergoline freeze-dried powder injection for injection, it is made up of following components: Nicergoline 2g, tartaric acid 0.5g, mannitol 20g, sodium chloride 2g. Dissolve tartaric acid, mannitol, and sodium chloride in about 400g of water for injection (25-30°C), stir until dissolved, add Nicergoline and continue stirring until it is completely dissolved, make up water for injection to 1000g, and check that the pH value should be 3.0 -5.0. After being filtered by a 0.22 micron microporous membrane, it is filled in a vial, half-tightened, and placed in a freeze dryer for freeze-drying in the following specific ways:

[0040] Pre-freezing: reduce the temperature of the shelf to -40°C in 1 hour and maintain it for 2 hours.

[0041] The first stage of drying: After pre-freezing, vacuumize, the vacuum degree is controlled at ≤10pa, the temperature of the partition is raised to -10°C in 1 hour, and maintained for 4 hours, and the temperature of the partition is...

Embodiment 3

[0046] A kind of Nicergoline freeze-dried powder for injection, it is made up of following components: Nicergoline 4g, tartaric acid 1g, mannitol 40g, sodium chloride 4g. Dissolve tartaric acid, mannitol, and sodium chloride in about 600g of water for injection (15-20°C), stir until dissolved, add Nicergoline and continue stirring until it is completely dissolved, make up water for injection to 1000g, and check that the Ph value should be 3.0 -5.0. After being filtered by a 0.22 micron microporous membrane, it is filled in a vial, half-tightened, and placed in a freeze dryer for freeze-drying in the following specific ways:

[0047]Pre-freezing: reduce the temperature of the shelf to -50°C in 2 hours and maintain it for 2 hours.

[0048] The first stage of drying: After pre-freezing, vacuumize, the vacuum degree is controlled at ≤10pa, the temperature of the partition is raised to -15°C in 1 hour, and maintained for 10 hours, and the temperature of the partition is raised to ...

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Abstract

The invention provides a nicergoline lyophilized preparation with excellent stability. The nicergoline lyophilized preparation is prepared by freeze-drying a nicergoline drug solution, and each 1000 gof the nicergoline drug solution comprises: 2-4 g of nicergoline, 0.5-1 g of tartaric acid, 0.2-9 g of sodium chloride, 20-40 g of an excipient, and an appropriate amount of water for injection, andthe pH value of the drug solution is 3.0-5.0. In the formula of the lyophilized preparation, mannitol is used to replacing lactose in an original development agent to be a lyophilized excipient, which can avoid the risks of allergies, pyrogens, and mad cow disease caused by lactose as an injection adjuvant, and overcomes the instability caused by the absence of lactose in the prior art. The mostnotable feature of the preparation is the combination of mannitol, sorbitol and the like with sodium chloride, and the nicergoline for injection still has excellent stability without using of nicergoline. The lyophilized product of the invention has rapid reconstitution and loose appearance, and is convenient for transportation and preservation and clinical use.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a new composition of a nicergoline freeze-dried preparation and a production method thereof. Background technique [0002] Nicergoline is a vasoactive drug developed in the 1960s. It is a semi-synthetic ergot alkaloid derivative. It has α-receptor blockade and vasodilation; it can strengthen the energy metabolism of brain cells and increase the utilization of oxygen and glucose; It can promote the conversion of neurotransmitter dopamine to increase nerve conduction, strengthen brain protein biosynthesis, and improve brain function. Clinically, it is mainly used for: improving low desire and emotional disorders caused by sequelae of cerebral infarction (sluggishness, inattention, memory loss, lack of ideas, depression, restlessness, etc.); acute and chronic peripheral circulation disorders (limb vascular occlusive disease) , Raynaud's syndrome, other symptoms of poor pe...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/12A61K47/02A61K47/26A61K31/48A61P25/28
CPCA61K9/0019A61K9/19A61K31/48A61K47/02A61K47/12A61K47/26A61P25/28
Inventor 白培锋张晓轩刘少华刘淑平周立明张树生张莉董进臣
Owner 湖北科莱维生物药业有限公司
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