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A kind of florfenicol instant microparticles and preparation method thereof

A technology of florfenicol and florfenicol, which is applied in the field of florfenicol instant soluble particles and its preparation, can solve problems such as unsatisfactory effects, and achieve oral bioavailability improvement, uniform distribution, and low requirements for preparation conditions Effect

Active Publication Date: 2021-09-03
SICHUAN AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the more methods used by people to reduce the particle size of drugs are crushing or recrystallization, but the effect is not ideal.

Method used

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  • A kind of florfenicol instant microparticles and preparation method thereof
  • A kind of florfenicol instant microparticles and preparation method thereof
  • A kind of florfenicol instant microparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The present embodiment provides a kind of florfenicol instant microparticles, comprising the following components: 1.16g of the original florfenicol, 5.25ml of composite emulsifier, 3.3mL of co-emulsifier, 0.1g of stabilizer, 117mL of liquid paraffin, Solvent 25mL.

[0023] The compound emulsifier is a mixture selected from span80 and Tween80, the volume ratio of span80 and Tween80 is 14:1, and the specific composition is span804.9mL and Tween800.35mL. The auxiliary emulsifier is selected from ethanol, the stabilizer is selected from poloxamer 188, and the solvent is selected from acetone.

[0024] The specific preparation method is as follows: take the prescribed amount of florfenicol and stabilizer, add acetone, and after fully dissolved by magnetic stirring, add emulsifier and liquid paraffin solution of co-emulsifier to obtain transparent O / O emulsion. Stir the emulsion continuously at a certain temperature to remove the organic solvent to obtain a microparticle su...

Embodiment 2

[0026] The mensuration of embodiment 2 microparticle drug loading and bag peak rate

[0027] Prepare instant microparticles according to Example 1, assuming that the quality of dropping into Florfenicol is m 1 , the mass of florfenicol instant soluble particles obtained is m 2 . When the drying of the instant microparticles is completed, respectively weigh 0.1 g of the instant microparticles prepared in three batches, dissolve and settle to 100 mL of water, measure the concentration of Florfenicol wherein C (g / L), according to the formula (1) Calculate its drug loading (L) and encapsulation efficiency (E) with formula (2) respectively.

[0028]

[0029]

[0030] Calculated according to the formula, the drug loading in the florfenicol instant microparticles is as high as 92.06%, and the encapsulation efficiency is 81.75%. It proves that the process of preparing florfenicol instant soluble particles is stable and reliable, the drug content is high, and most of the drugs...

Embodiment 3

[0031] Embodiment 3 Determination of Florfenicol Instant Dissolving Microparticle Dissolution Velocity and Saturation Solubility

[0032] Take excess florfenicol original drug and microparticles and place them in 500ml of distilled water (37±0.5°C), stir at 120rmp, and stir at 2, 5, 10, 20, 30, 45, 60, 90, 120, 180, 240min respectively. Take 5mL of the release medium, filter it with a microporous membrane, take the subsequent filtrate and measure its absorbance at 266nm to calculate the drug concentration. Take the concentration as the ordinate and time as the abscissa to draw a graph to obtain the drug dissolution curve.

[0033] Florfenicol is considered saturated when the solubility of Florfenicol no longer increases with time. At this point, take 5mL of the release medium, filter it with a microporous membrane, measure its absorbance at 266nm, and substitute it into the standard curve regression equation to calculate the solubility of florfenicol in the solution, which is...

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Abstract

The invention discloses a florfenicol instant granule and a preparation method thereof, comprising the following components: 1.16g of the original florfenicol, 5.25ml of a composite emulsifier, 3.3mL of a co-emulsifier, 0.1g of a stabilizer, and a liquid Paraffin 117mL, solvent 25mL. Take the prescribed amount of florfenicol and stabilizer, add solvent acetone, after fully dissolving, add paraffin wax solution containing emulsifier and co-emulsifier to obtain O / O emulsion. Stir the emulsion continuously at a certain temperature, and remove the organic solvent in the internal phase to obtain a suspension containing florfenicol microparticles. After centrifugal precipitation, discard the supernatant, wash with n-hexane, and dry to obtain Florfenicol instant particles. Compared with the original drug of florfenicol, the microparticles of the present invention have an increase of 40.57% in saturated solubility and a 43.72% increase in bioavailability, and the drug loading and encapsulation efficiency of the microparticles are as high as 92.06% and 81.75% respectively, which is better than that of fluorobenzene Other microparticulate formulations of Nicol.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a florfenicol instant granule and a preparation method thereof. Background technique [0002] In today's large-scale and rapid breeding, oral quick-acting drugs are more and more valued by animal drug companies because of their advantages of promoting drug absorption, saving drug costs, reducing animal pain and improving animal welfare. However, oral fast-acting drugs have high requirements on drug dissolution rate, and it is difficult for insoluble drugs to meet the fast-acting requirements. Florfenicol is a third-generation broad-spectrum chloramphenicol antibiotic for animals. Clinically, Florfenicol is mainly used for bacterial diseases of fish, infectious pleurisy of pigs caused by sensitive bacteria, respiratory diseases of cattle and colibacillosis of poultry, etc. However, its slow dissolution in water and low solubility lead to its slow ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/165A61P31/04
CPCA61K9/1641A61K31/165A61P31/04
Inventor 符华林刘梦娇陈诗奇豆海波刘泉金张伟舒刚袁志翔林居纯彭广能
Owner SICHUAN AGRI UNIV
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