Animal medicine inclusion compound, preparation method and application thereof

A technology of inclusion compounds and veterinary drugs, applied to veterinary drug inclusion compounds and preparation thereof, and the application field of veterinary drug inclusion compounds in the preparation of veterinary drugs, can solve the problem of failure to disclose inclusion compounds on solubility and stability, limited convenience and Economical, poor animal palatability, etc., to achieve the effects of improving hygroscopicity, reducing toxic and side effects, and facilitating application

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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In addition, the color of some raw materials such as enrofloxacin, norfloxacin, sarafloxacin, and acetylmequin will gradually become darker when exposed to light and heat, and some such as norfloxacin, ciprofloxacin lactate, Sarafloxacin, apramycin sulfate, etc. are hygroscopic and will absorb moisture in the air, which will lead to changes in their composition during storage, thereby affecting the quality of the drug
In addition, some drugs such as enrofloxacin, doxycycline hydrochloride, tylosin tartrate, etc. have bad taste, resulting in poor palatability to animals, thus limiting the convenience and economy of their use
[0004] In patent 200610049243.X, microcolloids are used to cover up bad odors, and the taste is masked by preparing microcolloids of gelatin-ethyl p-hydroxybenzoate ethanol-formaldehyde solution. This production method is more complicated, and the cost of sterilization is high. Due to the use of a large amount of organic solvents in the process, it is easy to cause solvent residues in the finished product, which will cause certain toxic and side effects on animals.
Moreover, this patent also fails to disclose the technical solutions on solubility and stability of clathrates

Method used

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  • Animal medicine inclusion compound, preparation method and application thereof
  • Animal medicine inclusion compound, preparation method and application thereof
  • Animal medicine inclusion compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation and Properties of Enrofloxacin Inclusion Compound

[0032] 1. Preparation of enrofloxacin inclusion complex

[0033] Weigh 14.40g (0.04mol) of enrofloxacin and 61.64g (0.04mol) of hydroxypropyl-β-cyclodextrin, place hydroxypropyl-β-cyclodextrin in a beaker, add 100ml of distilled water, and Prepare a saturated solution of hydroxypropyl-β-cyclodextrin on a water bath at ℃; take another enrofloxacin, add it to saturated hydroxypropyl-β-cyclodextrin, stir on a water bath at 70℃ for 30 minutes, and place it in a freeze dryer immediately Pre-freeze at -40°C for 12 hours, freeze-dry at -30°C, pass through a 100-mesh sieve to obtain enrofloxacin inclusion compound.

[0034] 2. Determination of dissolution rate of enrofloxacin inclusion compound

[0035] 1) Determination of Enrofloxacin Content

[0036] Chromatographic conditions: Octadecylsilane bonded silica gel is used as filler; column temperature is 40°C; detection wavelength is 278nm; theoretical ...

Embodiment 2

[0057] Example 2 Preparation of Sarafloxacin Hydrochloride Inclusion Compound and 1% W / V Sarafloxacin Hydrochloride Solution

[0058] 1. Sarafloxacin hydrochloride inclusion compound

[0059] Weigh 16.91 g (0.04 mol) of sarafloxacin hydrochloride and 61.64 g (0.04 mol) of hydroxypropyl-β-cyclodextrin, and prepare according to the method described in Example 1.

[0060] The solubility of sarafloxacin hydrochloride inclusion compound is measured with reference to the method of Example 1. The solubility of sarafloxacin hydrochloride inclusion compound is 1.41 mg / ml, and the solubility of sarafloxacin hydrochloride raw material is 0.067 mg / ml, that is, sarafloxacin hydrochloride inclusion compound The solubility is 21.0 times that of sarafloxacin hydrochloride raw material.

[0061] According to the technical guidelines for the stability research of veterinary chemical drugs, high-temperature test research was carried out on the inclusion compound of sarafloxacin hydrochloride. T...

Embodiment 3

[0070] Example 3 Ciprofloxacin Lactate Inclusion Compound and Stability Determination

[0071] Ciprofloxacin lactate has hygroscopicity, and the clathrate technology is used to clathrate ciprofloxacin lactate, which can prevent ciprofloxacin lactate from attracting moisture during storage.

[0072] 1. Preparation of inclusion compound of ciprofloxacin lactate: Weigh 16.92g (0.04mol) of ciprofloxacin lactate and 58.60g (0.04mol) of 2,6-dimethyl-β-cyclodextrin, according to Example 1 prepared by method.

[0073] 2. Stability test of ciprofloxacin lactate inclusion compound

[0074] Carry out high-humidity test research on the ciprofloxacin lactate inclusion compound according to the technical guidelines for the stability research of veterinary chemical drugs. Place it under the condition of humidity 90%±5% for 10 days, take samples on the 5th and 10th days, and compare with the properties, moisture absorption weight gain, and content detection results on the 0th day; the raw m...

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Abstract

The invention discloses application of an inclusion technology in preparing animal medicines, and an animal medicine inclusion compound. The animal medicine inclusion compound can increase the dissolution velocity and the solubility of indissolvable medicines, improve the stability of the medicines which are changeable in the presence of lights or moistures and the like, and facilitate the storage of medicines. The invention also provides a method for preparing the animal medicine inclusion compound, and the method is simple in operation, can reduce the use of organic solvent, lower the cost, reduce the poisonous side effects of the medicines, and can be applied to the preparation of animal medicines.

Description

technical field [0001] The invention relates to the application of a veterinary drug inclusion compound in the preparation of veterinary drugs, more specifically relates to a veterinary drug inclusion compound and a preparation method thereof, belonging to the field of veterinary drugs. Background technique [0002] The solubility of drugs is one of the important factors affecting the bioavailability of drugs. Insoluble drugs are difficult to be absorbed by animals due to their low solubility in water, resulting in poor bioavailability. With the widespread application of combinatorial chemistry, gene screening, high-throughput screening and other technologies in drug development, a large number of active drug candidates have been found, but many drugs have the defect of poor water solubility, which limits their clinical application. It is estimated that about 65 billion US dollars of drugs are produced globally every year due to poor bioavailability, which causes a serious i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/61
Inventor 张许科刘兴金张晓会
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