Favipiravir L-arginine frozen-dried preparation for injection

A technology of freeze-dried preparations and arginine salts, which is applied in the field of medicine, can solve problems such as difficult reconstitution, unsatisfactory satisfaction, and limited solubilization effect, and achieve uniform color, high unit loading dose, and good pharmaceutical characteristics Effect

Active Publication Date: 2020-06-02
REYOUNG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Patent CN103209967A reports a method for preparing a lyophilized preparation of piravir for injection, which is to prepare a lyophilized preparation by a conventional method after favipiravir and meglumine are generated into a lyophilized preparation of piravir. The compound has excellent resolubility, which overcomes the difficulty of reconstitution in sodium salt freeze-drying
However, due to the limited solubilization effect of the basic substance meglumine on favipiravir, according to its embodiment, the highest concentration of the prepared solution is no more than 75mg / ml (in terms of favipiravir), and each lyophilized The drug dose of the preparation does not exceed 600 mg
Obviously, for the clinical high-dose use demand, it cannot be well satisfied

Method used

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  • Favipiravir L-arginine frozen-dried preparation for injection
  • Favipiravir L-arginine frozen-dried preparation for injection
  • Favipiravir L-arginine frozen-dried preparation for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] 100 prescriptions

[0031]

[0032] Preparation

[0033] (1) Preparation of favipiravir L-arginine salt solution: take 80% of the recipe water for injection, heat to a temperature between 60 and 70 ° C, add L-arginine, stir to dissolve; then add method Pilavir, stir for 1-2 hours to obtain a clear solution, measure the pH between 7.2-7.6, then add 1M sodium hydroxide solution, adjust the pH to between 7.8-8.2, add water to the full amount, filter with a 0.22 μm membrane, the filtrate Filled in 20ml vials, each bottle contains 10ml.

[0034] (2) Freeze-drying: the above-mentioned favipiravir L-arginine salt solution is rapidly cooled (the cooling rate is greater than 20°C / h), so that the temperature of the sample is reduced to -35~-60°C and maintained for 1~4h; turn on the vacuum pump Vacuum, after the vacuum degree of the front box is lower than 200Pa, adjust the temperature of the partition to -15~-5℃, maintain the vacuum pressure at 25~150Pa, and keep it for 8~20...

Embodiment 2

[0036] 100 prescriptions

[0037]

[0038] Preparation

[0039] (1) Preparation of favipiravir L-arginine salt solution: take 80% of the recipe water for injection, heat to a temperature between 60 and 70 ° C, add L-arginine, stir to dissolve; then add method Pilavir, stir for 1-2 hours to obtain a clear solution, measure the pH between 7.2-7.6, then add 1M sodium hydroxide solution, adjust the pH to between 7.8-8.2, replenish water to the full amount, filter with a 0.22 μm membrane, and filter the filtrate. Filled in 20ml vials, each bottle contains 8ml.

[0040] (2) Freeze-drying: the above-mentioned favipiravir L-arginine salt solution was rapidly cooled (the cooling rate was greater than 20°C / h), so that the temperature of the sample was reduced to -35~-60°C and maintained for 1~3h; the vacuum pump was turned on Vacuum, after the vacuum degree of the front box is lower than 200Pa, adjust the temperature of the partition to -15~-5℃, maintain the vacuum pressure at 25~1...

Embodiment 3

[0042] 100 prescriptions

[0043]

[0044] Preparation

[0045] (1) Preparation of favipiravir L-arginine salt solution: take 80% of the recipe water for injection, heat to a temperature between 60 and 70 ° C, add L-arginine, stir to dissolve; then add method Pilavir, stir for 1-2 hours to obtain a clear solution, measure the pH between 7.2-7.6, then add 1M sodium hydroxide solution, adjust the pH to between 7.8-8.2, add water to the full amount, filter with a 0.22 μm membrane, the filtrate Filled in 20ml vials, each bottle contains 12ml.

[0046] (2) Freeze drying: the above-mentioned favipiravir L-arginine salt solution was rapidly cooled (the cooling rate was greater than 20°C / h), so that the temperature of the sample was reduced to -35~-60°C and maintained for 1~6h; turn on the vacuum pump Vacuum, after the vacuum degree of the front box is lower than 200Pa, adjust the temperature of the partition to -15~-5℃, maintain the vacuum pressure at 25~150Pa, and keep it for 10~...

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Abstract

The invention relates to a favipiravir L-arginine frozen-dried preparation for injection. The frozen-dried preparation comprises favipiravir and L-arginine, wherein the molar ratio of the favipiravirto the L-arginine is (1 to 1.1) to (1 to 1.3) ( weight ratio is (1 to 22) to (1 to 1.44) ). The invention further discloses a preparation method of the favipiravir L-arginine frozen-dried preparationfor injection, the obtained frozen-dried preparation can be guaranteed to have favorable redissolution properties, and based on high unit load dosage, the favipiravir L-arginine frozen-dried preparation for injection has favorable stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a freeze-dried preparation of favipiravir L-arginine salt for injection and a preparation method thereof. Background technique [0002] Favipiravir, chemical name 6-fluoro-3-hydroxypyrazine-2-carboxamide, is an RNA-dependent RNA polymerase inhibitor class broad-spectrum antiviral developed by Toyama Chemical Industry Co., Ltd. The drug, launched in Japan in July 2014, is used to treat new or recurrent influenza virus infections. [0003] Favipiravir is represented by the following structural formula: [0004] [0005] At present, the marketed dosage form of favipiravir is tablet, and the tablet specification is 200mg / tablet. The recommended dosage is: 1,600 mg once on the first day, twice a day, and 600 mg once a day on the 2nd to 5th, orally administered twice a day. The total dosing period was 5 days. Therefore, the dosage of the tablet is large, which causes great diffic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/18A61K31/4965A61P31/16
CPCA61K9/19A61K9/0019A61K47/183A61K31/4965A61P31/16
Inventor 王进京苗得足高峰李锋王振童元峰聂爱华
Owner REYOUNG PHARMA
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