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Compound tilmicosin phosphate-ambroxol nanoemulsion preparation

A technology of tilmicosin phosphate and tilmicosin, which is applied in the fields of pharmaceutical formulations, emulsion delivery, and medical preparations containing active ingredients, etc. It can solve the problems of low bioavailability, short half-life in the body, and easy damage by gastric acid, etc. problem, to achieve high drug stability, simple preparation process, and good drug effect

Inactive Publication Date: 2015-11-04
HEBEI KEHENG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because tilmicosin is insoluble in water, its traditional preparation is tilmicosin phosphate, which is easily destroyed by gastric acid after oral administration, resulting in incomplete absorption, low bioavailability, and short half-life in vivo

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation of compound tilmicosin phosphate and ambroxol nanoemulsion

[0023] Prepare the recipe as follows:

[0024] Tilmicosin Phosphate 10.0g

[0025] Ambroxol 1.0g

[0026] Tween 80 25.58g

[0027] Absolute ethanol 13.31g

[0028] Ethyl acetate 5.29g

[0029] Distilled water 44.82g

[0030] The specific operation steps are:

[0031] Dissolve 10.0g of tilmicosin phosphate in 44.82g of distilled water first, then dissolve 1.0g of ambroxol in the aqueous solution of tilmicosin phosphate as mixture A, then mix 25.58g of Tween 80 and 13.31g of absolute ethanol Mix with 5.29g ethyl acetate to form mixture B; slowly add mixture A dropwise to mixture B at room temperature while stirring continuously until a uniform, transparent, uniform and stable system is formed, and the target product is obtained.

Embodiment 2

[0033] Preparation of compound tilmicosin phosphate and ambroxol nanoemulsion

[0034] Prepare the recipe as follows:

[0035] Tilmicosin Phosphate 5.0g

[0036] Ambroxol 1.0g

[0037] RH40 14.56g

[0038] Absolute ethanol 9.13g

[0039] Ethyl acetate 2.97g

[0040] Distilled water 67.34g

[0041] The specific operation steps are:

[0042] After first dissolving 5.0g tilmicosin phosphate in 67.34g distilled water, then 1.0g ambroxol was dissolved in the aqueous solution of tilmicosin phosphate as mixture A, then 14.56g RH40, 9.13g dehydrated alcohol and 2.97g Ethyl acetate was mixed uniformly to form mixture B; at room temperature, mixture A was slowly added dropwise to mixture B while stirring continuously until a uniform, transparent, uniform and stable system was formed, and the target product was obtained.

Embodiment 3

[0044] Preparation of Compound Tilmicosin Phosphate and Ambroxol Nanoemulsion

[0045] Prepare the recipe as follows:

[0046] Tilmicosin Phosphate 13g

[0047] Ambroxol 1.3g

[0048] Pingping plus 0 34.58g

[0049] Absolute ethanol 17.91g

[0050] Ethyl acetate 5.84g

[0051] Distilled water 27.37g

[0052] The specific operation steps are:

[0053] First dissolve 13g of tilmicosin phosphate in 27.37g of distilled water, then dissolve 1.3g of ambroxol in an aqueous solution of tilmicosin phosphate to form mixture A, then add 34.58g of Pingping 0, 17.91g of absolute ethanol and Mix 5.84g of ethyl acetate to form mixture B; slowly add mixture A to mixture B at room temperature while stirring continuously until a uniform, transparent, uniform and stable system is formed, and the target product is obtained.

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Abstract

The invention discloses a compound tilmicosin phosphate-ambroxol nanoemulsion preparation and a preparation method thereof. The nanoemulsion preparation is oil-in-water type, has a particle size of 1-100nm, and is prepared from tilmicosin phosphate, ambroxol, a surfactant, a co-surfactant, ethyl acetate and distilled water. The drug is a light yellow clarified liquid, and ahs the characteristics of simple preparation process, low production cost, obvious absorption effect and high stability, and can improve the bioavailability of drugs.

Description

technical field [0001] The invention belongs to the field of veterinary medicine, in particular to a compound tilmicosin phosphate and ambroxol nanoemulsion and a preparation method thereof. Background technique [0002] Tilmicosin is a special-purpose macrolide antibiotic for livestock and poultry, which has inhibitory effects on Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, spirochetes, etc., especially for Actinobacillus pleuropneumoniae, hemolytic Pasteurella and mycoplasma have the strongest effect. Because the main target organs of tilmicosin are the lungs and breasts, and the drug concentration is high, it is mainly used for respiratory tract infections in livestock and poultry and mastitis in dairy cows. Ambroxol is the active metabolite of bromhexine in the body. It can promote the secretion of pulmonary surfactant and airway fluid secretion, break the mucopolysaccharide protein fibers in sputum, promote the dissolution of mucus sputum, signi...

Claims

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Application Information

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IPC IPC(8): A61K31/706A61K9/107A61P31/04A61P11/14A61P11/06A61K31/137
Inventor 刘彦政袁向红王国威席顺新王洪亮李海峰王庆学李宏敏刘泽杰
Owner HEBEI KEHENG BIOTECH
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