Redefovir composition and application thereof

A technology for Remdesivir and a composition, applied in the field of pharmaceutical preparations, can solve the problems of high packaging requirements, contaminated drugs, and high equipment requirements, and achieve the effects of simple preparation process, overcoming poor solubility, and satisfying drug efficacy

Active Publication Date: 2021-10-19
METIS PHARM HZ INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The oral instant film has the advantages of quick effect and easy to carry, etc., but there are many auxiliary materials added in the preparation process of the oral instant film, and the air bubbles need to be removed under vacuum conditions, and because the film is thin, light and small, it is easy to absorb moisture , the packaging requirements are also high, not suitable for industrial production
[0007] CN111956630 discloses a liquid preparation of Remdesivir for nebulizers, the mass ratio of sulfobutyl-β-cyclodextrin to Remdesivir can reach below 15:1, although the amount of cyclodextrin is reduced, However, the treatment process requires the nebulizer to cooperate with manual pump pressure, high-pressure gas, and ultrasonic vibration to release the mist. The requirements for equipment are high, and there is a risk of drug contamination.
[0008] In summary, the prior art has not yet disclosed a low-toxic remdesivir preparation that can reduce the amount of cyclodextrin, is simple to operate, requires low process equipment, and is suitable for industrial production.

Method used

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  • Redefovir composition and application thereof
  • Redefovir composition and application thereof
  • Redefovir composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] (1) Preparation of sulfobutyl-β-cyclodextrin solution

[0031] Weigh 2.5g of sulfobutyl-β-cyclodextrin into a 50mL volumetric flask, add 40mL of purified water, shake to dissolve, add an appropriate amount of hydrochloric acid solution to adjust the pH of the system to 1.8, and add purified water to constant volume to prepare 5 % (w / v) of sulfobutyl-β-cyclodextrin solution.

[0032] (2) Remdesivir Saturation Solubility Experiment

[0033] After remdesivir passes through an 80-mesh sieve, weigh 10 mg of remdesivir into a 5mL centrifuge tube, and add 0.8mL of the 5% (w / v) sulfobutyl-β-cyclodextrin solution prepared in step (1) , add 0.2mL of purified water, shake and disperse, add 2M hydrochloric acid to adjust the pH to 1.8, vortex mix for 50min, then add 3M sodium hydroxide solution to adjust the pH to about 3.5, then vortex mix for 50min, the suspension is centrifuged to obtain sulfobutyl Based on the Redcivir composition with a β-cyclodextrin content of 4% (w / v), th...

Embodiment 2

[0035] (1) Preparation of solubilizer solution

[0036] Weigh appropriate amounts of 22 kinds of solubilizers into 5mL test tubes, add 2mL of water, and prepare solubilizer solutions with appropriate concentrations (as shown in Table 1).

[0037] (2) Dissolution experiment of remdesivir

[0038] After remdesivir passes through an 80-mesh sieve, weigh 10 mg of remdesivir into a 5mL centrifuge tube, add 0.8mL of hydrochloric acid solution with a pH of 1.8 and 0.2mL of a solubilizer aqueous solution, shake and disperse, and then add 2M hydrochloric acid solution to adjust The pH is 1.8, vortexed for 50 minutes, then added 3M sodium hydroxide solution to adjust the pH to 3.5, vortexed for 50 minutes, and the suspension was centrifuged to obtain the remdesivir solubilizer composition, and the content of remdesivir in it was detected , to obtain the solubility of remdesivir in different solubilizer solutions, and the results are shown in Table 1.

[0039] Table 1

[0040]

[0...

Embodiment 3

[0044] Pass remdesivir through an 80-mesh sieve, weigh 10 mg into a 5 mL centrifuge tube, add 0.8 mL of the sulfobutyl-β-cyclodextrin solution prepared in the same way as in step (1) of Example 1, and adjust the pH to 1.8. Vortex for 50 min, add 0.2 mL of different types of solubilizer solutions prepared according to the same method as in Example 2 step (1), adjust the pH to 1.8, vortex for 50 min, adjust the pH of the system to about 3.5 with 3M sodium hydroxide solution, and vortex After 50 minutes, the suspension was centrifuged to obtain a remdesivir composition containing sulfobutyl-β-cyclodextrin and a solubilizer, and the content of remdesivir in it was determined, and the results are shown in Table 2.

[0045] Table 2

[0046]

[0047]

[0048] The results showed that after remdesivir and sulfobutyl-β-cyclodextrin were fully mixed, adding solubilizers L-isoleucine, L-arginine, Span 20, propylene glycol, Span 80, polyethylene glycol Alcohol 200, polyethylene glyc...

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PUM

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Abstract

The invention provides a ridecevir composition, and a preparation method and application thereof. According to the composition, a solubilizer is used, so that the solubility of the ridecevir in cyclodextrin or cyclodextrin derivatives is greatly improved, and the content of the cyclodextrin or the cyclodextrin derivatives with renal toxicity in the ridecevir can be reduced to be 4% (w / v) or less. The ridecevir composition provided by the invention is simple in preparation process, low in equipment requirement, low in cost and suitable for industrial production.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to a composition of remdesivir and its preparation method and application. Background technique [0002] Remdesivir is a viral RNA-dependent RNA polymerase (rdrp) inhibitor developed by Gilead Science, which was approved to treat Ebola virus infection in the United States and Europe in 2015 and 2016, respectively. orphan drug qualification. In 2020, the FDA approved remdesivir for the treatment of hospitalized patients with new crowns, becoming the first officially approved new crown treatment drug in the United States. The structural formula of Remdesivir is as follows: [0003] [0004] Remdesivir has poor solubility and stability. The currently marketed remdesivir formulation is a lyophilized formulation. As described in the patent CN111093627 of Gilead Sciences, the lyophilizer increases the solubility of remdesivir by adding cyclodextrin derivatives and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/685A61K47/34A61K47/26A61K47/22A61K47/40A61P31/14
CPCA61K31/685A61K47/34A61K47/26A61K47/22A61K47/40A61P31/14
Inventor 赖青海王恺李海燕赖才达王文首
Owner METIS PHARM HZ INC
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