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Florfenicol composition with high bioavailability and preparation method thereof

A technology of florfenicol and availability, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of low oral bioavailability, poor water solubility of florfenicol, etc. problems, to achieve the effect of improving oral bioavailability, improving solubility, and reasonable process design

Active Publication Date: 2016-04-13
CHINANIMAL NANJING VETERINARY DRUGS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Purpose of the invention: the purpose of the present invention is to solve the problem of poor water solubility of florfenicol and low oral bioavailability, and to provide a highly bioavailable florfenicol composition, which can not only improve florfenicol solubility, and can greatly improve its oral bioavailability; another object of the present invention is to provide a preparation method of the florfenicol composition with high bioavailability

Method used

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  • Florfenicol composition with high bioavailability and preparation method thereof
  • Florfenicol composition with high bioavailability and preparation method thereof
  • Florfenicol composition with high bioavailability and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0021] A highly bioavailable florfenicol composition is made from the following raw materials in parts by weight:

[0022]

[0023] The preparation method is:

[0024] (1) Add 1 part of florfenicol, 10 parts of β-cyclodextrin and 5 parts of sodium carboxymethylcellulose into 1 part of water, heat to 70-90°C, and stir magnetically for 30 minutes;

[0025] (2) The above-prepared solution is prepared into powder by spray drying to obtain a highly bioavailable Florfenicol composition.

Embodiment 2

[0026] Embodiment 2 A highly bioavailable Florfenicol composition, which is made from the following raw materials in parts by weight:

[0027]

[0028] The preparation method is:

[0029] (1) Add 1 part of florfenicol and 15 parts of β-cyclodextrin into 3 parts of water, heat to 70-90°C, and stir magnetically for 30 minutes;

[0030] (2) Prepare the above-prepared solution into powder by spray-drying, add 903 parts of povidone K90, and mix evenly to obtain the florfenicol composition with high bioavailability.

Embodiment 3

[0032]

[0033] Preparation:

[0034] (1) Add 1 part of florfenicol and 25 parts of β-cyclodextrin into 2 parts of water, heat to 70-90°C, and stir magnetically for 30 minutes;

[0035] (2) Prepare the solution prepared above into powder by freeze-drying, add 10 parts of Carbomer 971P, and mix evenly to obtain the Florfenicol composition with high bioavailability.

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PUM

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Abstract

The invention discloses a florfenicol composition with high bioavailability. The florfenicol composition is prepared from, by weight, 1-5 parts of florfenicol, 2-50 parts of beta-cyclodextrin and 5-10 parts of absorption promoter. The florfenicol composition has the advantages that the florfenicol composition with high bioavailability is obtained by screening through a large amount of experiments, the absorption promoter is added on the basis of florfenicol cyclodextrin inclusion complex, the defect that florfenicol is difficult to dissolve in water is overcome while the oral bioavailability of the florfenicol can be increased greatly. A preparation method of the florfenicol composition is reasonable in process design, high in operability and capable of achieving industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a highly bioavailable florfenicol composition and a preparation method thereof. Background technique [0002] Florfenicol, also known as fluprofen, fluthiamphenicol, Chinese name: [R--(R1.T)]-2,2-dichloro-N-{fluoromethyl)-2-hydroxy- 2-[4-(methylsulfonyl)phenyl]ethyl}acetamide is a new type of chloramphenicol broad-spectrum antibiotic developed by the American Schering-Plough Company in the 1970s. It has a broad antibacterial spectrum and can act on a variety of bacteria, mycoplasma, chlamydia, etc. However, florfenicol is almost insoluble in water, and its oral bioavailability is very low. In order to increase the solubility of Florfenicol, the current research is mostly focused on making Florfenicol into PEG solid dispersion, PVP solid dispersion and β-cyclodextrin inclusion complex. The application of these new technologies has improved the bioavailability to a cer...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/165A61K47/38A61K47/32A61K47/36A61K9/14A61K9/19
CPCA61K9/146A61K9/19A61K31/165A61K47/32A61K47/36A61K47/38
Inventor 马小平肖衍宇徐瑞华戴银娣胡娟
Owner CHINANIMAL NANJING VETERINARY DRUGS
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