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Method for preparing florfenicol microcrystal

A florfenicol and microcrystal technology, which is applied in the field of florfenicol preparation, can solve the problems of slow dissolution rate, small dissolution rate, unreliable safety, etc., and achieves increasing solubility, accelerating dissolution, and improving bioavailability. Effect

Inactive Publication Date: 2014-12-17
SICHUAN AGRI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

And injection is difficult to be applied on a large scale in large-scale farms due to inconvenient application.
Moreover, most of the injections are prepared with organic solvents such as dimethylformamide and propylene glycol, which are likely to cause local irritation and toxicity, and are unreliable in safety.
[0004] In view of the above reasons, solving the problem of poor solubility of florfenicol in water has always been a hot spot in the field of veterinary medicine.
Currently, there are two types of methods for improving the water solubility of Florfenicol reported: one is physical methods, including β-cyclodextrin inclusion complexes, hydroxypropyl-β-cyclodextrin inclusion complexes, and preparation of solid dispersions. But this kind of method is generally poor in solubilizing effect, and dissolution rate is slow, and dissolution rate is little, and process is complicated, needs a large amount of special auxiliary materials, is difficult to meet the demand of preparation and clinical use; It becomes an inactive prodrug, and after entering the animal body, it is metabolized into florfenicol to play a role. It is characterized in that its water solubility is much greater than that of physical methods, but due to structural changes, it will change the pharmacokinetic characteristics of the drug and produce some unpredictable effects

Method used

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  • Method for preparing florfenicol microcrystal
  • Method for preparing florfenicol microcrystal
  • Method for preparing florfenicol microcrystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A method for preparing florfenicol microcrystals, the method is as follows: the former powder of florfenicol is dissolved in methanol to prepare a methanol solution of florfenicol, and the stabilizer is dissolved in water to form a stabilizer-containing The aqueous solution, wherein, the methanol solution concentration of Florfenicol is 40mg / ml, and the concentration of the aqueous solution containing stabilizer is 4mg / ml, and stabilizer adopts hydroxypropyl methylcellulose, and the volume ratio of methanol and water is 1: 2. Slowly add the methanol solution of florfenicol to the aqueous solution containing stabilizer under the condition of stirring and ice bath at 4°C. The stirring time is 15min. Florfenicol slowly precipitates out to form a suspension. The suspension is suction filtered and dried to obtain the florfenicol microcrystalline powder.

[0042] The solubility of the florfenicol microcrystals prepared by the method in water can reach 3960 μg / ml.

Embodiment 2

[0043] Example 2 Effect of Different Stabilizers on the Dissolution of Florfenicol Microcrystals

[0044] Florfenicol microcrystal preparation method is the same as embodiment 1, but changes the kind of stabilizer, investigates stabilizer respectively with hydroxypropyl methylcellulose, polyvinylpyrrolidone, Tween-80, poloxamer 188, polyvinylpyrrolidone Ethylene glycol 4000, a mixture of poloxamer 188 and Tween-80 (poloxamer 188-tween 80), a mixture of poloxamer 188 and hydroxypropyl methylcellulose (poloxamer 188 - hydroxypropyl methylcellulose), the mixture of hydroxypropyl methylcellulose and Tween-80 (hydroxypropylmethylcellulose-Tween 80) on the formation of florfenicol microcrystals (above The mass ratio of both substances in the mixture is 1:1).

[0045] During the formation of florfenicol microcrystals, the stabilizer, on the one hand, prevents the aggregation of drug molecules to avoid the formation of coarse drug particles, and on the other hand, enables the formed ...

Embodiment 3

[0046] Embodiment 3 The influence of the concentration of florfenicol in methanol on the dissolution of microcrystals

[0047] The preparation method of Florfenicol microcrystals is the same as in Example 1, but the concentration of the methanol solution of Florfenicol is changed, and the methanol concentration of Florfenicol is investigated to be 30mg / ml, 50mg / ml, 80mg / ml, 100mg / ml respectively. The effect of ml on microcrystal formation. from figure 2 From the results in Table 1, it can be seen that with the increase of the concentration of the methanol solution of Florfenicol, the solubility of the microcrystals decreases. This is because the concentration is too high to speed up the nucleation rate, which in turn leads to the instantaneous solid particle density in the system is too high to cause aggregation. In addition, in the liquid phase-particle system, there is interaction between particles. When the distance between two particles is reduced to a critical distance...

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Abstract

The invention discloses a method for preparing florfenicol microcrystal, and belongs to the technical field of florfenicol preparation methods. According to the method, the florfenicol microcrystal is prepared by using an anti-solvent sediment method, thereby increasing the solubility of the florfenicol microcrystal in water and accelerating the florfenicol microcrystal to be dissolved. The method comprises the following steps of: dissolving the florfenicol into methanol, dropping a florfenicol methanol solution into a water solution with a stabilizer under the stirring ice-bath condition, and through selecting appropriate process condition, precipitating out the florfenicol so as to obtain the florfenicol microcrystal with good solubility property. According to the method, the chemical structure of the florfenicol is not changed, no other cosolvents are used, and the florfenicol as the raw powder can be made into a variety of dosage forms. The particle size of the florfenicol microcrystal prepared by using the method is greatly reduced, the crystal structure is greatly damaged, the solubility of the florfenicol in water is increased to 3960 mu g / ml from 1350 mu g / ml, and the result shows that the solubility property of the florfenicol is remarkably enhanced because of the florfenicol microcrystal, so that the florfenicol can be further popularized and applied.

Description

technical field [0001] The invention belongs to the technical field of preparation methods of florfenicol, in particular to a method for preparing florfenicol microcrystals. Background technique [0002] Florfenicol is a synthetic thiamphenicol derivative. It is a broad-spectrum chloramphenicol antibiotic for animals. It can be used for bacterial diseases and mycoplasma diseases in cattle, pigs, poultry, etc., as well as aquatic products. It has a remarkable curative effect on animal diseases and is the first choice for treating various infections caused by typhoid bacillus, paratyphoid bacillus and salmonella. Compared with similar chloramphenicol and thiamphenicol, florfenicol has the characteristics of broad antibacterial spectrum, good absorption, wide distribution in the body, safety and high efficiency, and has no potential aplastic anemia, teratogenicity, carcinogenicity and Mutagenicity, especially chloramphenicol is prohibited from being used in food animals due to...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C317/32C07C315/06
Inventor 符华林何燕飞唐进波张伟熊俊芳肖欣戈曹航
Owner SICHUAN AGRI UNIV