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Valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and preparation method thereof

A self-emulsifying technology of warnemulin hydrochloride, which is applied in the direction of medical preparations, pharmaceutical formulas, and emulsion delivery of non-active ingredients, can solve the unavoidable problems of the palatability of warnemulin, overdose or deficiency of drugs, and Reduce the content of nimulin and other issues, to achieve the effect of reducing individual differences in administration, improving oral bioavailability, and reducing oral irritation

Active Publication Date: 2012-04-18
QILU ANIMAL HEALTH PROD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the dosage form of warnemulin is mainly premixed. This dosage form is not easy to control the dosage, resulting in overdose or deficiency of the drug, and it cannot avoid the problem of the palatability of warnemulin, which makes it difficult for animals to take it.
Chinese patent document CN101756899A (Application No. 200910254646.1) discloses a nano-emulsion of varnemulin, which effectively masks the bad smell of the drug, solves the problem of palatability, and also has certain targeting, which enhances the efficacy of the drug. Curative effect, but the warnemulin is not stable, the dosage form contains water, it is easy to decompose the warnemulin, the chemical stability is not good, and the content of the warnemulin will decrease after a period of time

Method used

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  • Valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and preparation method thereof
  • Valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and preparation method thereof
  • Valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] A veterinary self-emulsifying oral nanoemulsion preparation of warnemulin hydrochloride, the components are as follows:

[0025]

[0026] The preparation method of the above-mentioned warnimulin hydrochloride self-emulsifying oral nanoemulsion preparation for animals comprises the following steps:

[0027] (1) First mix and stir 13g oil, 35g surfactant and 95ml co-surfactant evenly, then add 1g antioxidant and 1g preservative, stir until completely dissolved to obtain a clear oily liquid;

[0028] (2) Add warnemulin hydrochloride to the clear oily liquid prepared in step (1), set the volume to 100ml with co-surfactant, and stir at 40-60°C until completely dissolved to obtain the veterinary hydrochloride Nimulin self-emulsifying oral nanoemulsion formulation.

[0029] Physical and chemical properties:

[0030] 1. Particle size determination:

[0031] Example 1 Determination of self-emulsifying ability: Take 50 μl of vonemulin hydrochloride self-emulsifying agent an...

Embodiment 2

[0051] A veterinary self-emulsifying oral nanoemulsion preparation of warnemulin hydrochloride, the components are as follows:

[0052]

[0053] The preparation method is the same as in Example 1.

[0054]6-month acceleration and 12-month long-term stability test conditions are as described in Example 1. After the test, the preparation still remains clear and transparent, without delamination and crystallization. After 6 months of acceleration, the content of warnemulin hydrochloride is 10.87 wt%, after the 12-month long-term stability test, the content of warnemulin hydrochloride was 10.98 wt%, and the results showed that the content of warnemulin hydrochloride did not significantly decrease, and the product had good stability. Take 50 μl of the varnemulin self-emulsifying nanoemulsion described in Example 2 and add it to a 100ml volumetric flask, dilute to the mark with distilled water, shake gently, and still form a clear microemulsion, which is measured by a particle si...

Embodiment 3

[0056] A veterinary self-emulsifying oral nanoemulsion preparation of warnemulin hydrochloride, the components are as follows:

[0057]

[0058]

[0059] The preparation method is the same as in Example 1.

[0060] 6-month accelerated and 12-month long-term stability test conditions are as described in Example 1. After the test, the preparation still remains clear and transparent without delamination and crystallization. wt%, after the 12-month long-term stability test, the content of warnemulin hydrochloride was 11.96 wt%, and the results showed that the content of warnemulin hydrochloride did not significantly decrease, and the product had good stability. Take 50 μl of the varnemulin self-emulsifying nanoemulsion described in Example 2 and add it to a 100ml volumetric flask, dilute to the mark with distilled water, shake gently, and still form a clear microemulsion, which is measured by a particle size analyzer. The distribution is between 10 and 100nm, and the averag...

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Abstract

The invention discloses valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use and a preparation method thereof. The valnemulin hydrochloride self-emulsified oral nano emulsion for veterinary use comprises the following components: valnemulin hydrochloride, oil, surfactant, preservative, antioxygen and auxiliary surfactant. After disintegrating in water and being stirred slightly or being taken orally and moving with intestine movement, the self-emulsified emulsion can spontaneously form emulsion with emulsion droplet size of 10 to 100 nanometers; the drawbacks of decomposition of valnemulin during long standing and content reduction of the valnemulin or valnemulin hydrochloride nano emulsion prepared in the prior art are overcome and the content stability of the product is increased; the palatability of the valnemulin product is improved; and the preparation process is simple, and the valnemulin hydrochloride self-emulsified oral nano emulsion is suitable to be produced in large scale by veterinary medicine enterprises.

Description

technical field [0001] The invention relates to a self-emulsifying oral nanoemulsion preparation of veterinary warnemulin hydrochloride and a preparation method thereof, belonging to the technical field of veterinary medicines. Background technique [0002] Vernimulin is a new generation of pleuromutilin semi-synthetic animal-specific antibiotics. It is unanimously recognized as the first choice drug for the treatment of animal mycoplasma disease, mainly used for the prevention and treatment of mycoplasma disease and Gram disease in pigs, cattle, sheep and poultry. positive bacterial infection. Its hydrochloride is commonly used clinically, and it is rapidly absorbed after oral administration, and its bioavailability is close to 100%. The mechanism of action is to inhibit bacterial protein synthesis at the ribosome level, and at high concentrations, it also inhibits RNA synthesis. [0003] Wonimulin tastes bitter, extremely irritating, insoluble and unstable in water, and ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/22A61K47/44A61K47/34A61P31/04
Inventor 李成应王海挺吴连勇田玉柱崔进
Owner QILU ANIMAL HEALTH PROD
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