Tilmicosin micelle preparation and preparation method thereof

A technology of tilmicosin and micelles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of myocardial toxicity, unfavorable animal healthy growth, and difficulty in long-term placement , to achieve strong retention capacity, high encapsulation efficiency and drug loading rate, and not easy to oxidize

Inactive Publication Date: 2012-04-04
HENAN SOAR VETERINARY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Like most traditional preparations, tilmicosin drinking water, tablets, and ordinary injections are released according to first-order kinetics, and the drug concentration in the blood fluctuates greatly, often showing "peaks and valleys". The toxic concentration is at the bottom, and the effective blood concentration is maintained for a short time. It often requires repeated administration to achieve effective treatment, reduce side effects, and increase costs. In addition, repeated administration of some dosage forms is more irritating to animals, and the stress response is obvious. Not conducive to the healthy growth of animals
[0006] Safety issues of tilmicosin injection, such as subcutaneous injection of cows, 50mg per 1kg body weight can cause myocardial toxicity, 150mg can be fatal; intramuscular injection of pigs, 10m

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A tilmicosin micellar preparation, which is composed of: tilmicosin 3g, poloxamer 188 5g, PBS buffer 52g, glucose 3.0g and citric acid 0.7g.

[0021] The preparation method is as follows:

[0022] (1) Put poloxamer 188 in an eggplant-shaped bottle, add a dissolved amount of ethyl acetate to dissolve, and evaporate the organic solvent in a water bath at 45°C under reduced pressure to form a film.

[0023] (2) Dissolve tilmicosin and glucose with PBS buffer.

[0024] (3) Add (2) to (1), stir and hydrate for 2 hours, adjust the pH to 5 with citric acid, and then filter with a 0.45um filter membrane to obtain the product.

[0025] The encapsulation efficiency and drug loading of tilmicosin were determined to be 85.5% and 15%, respectively.

Embodiment 2

[0027] A tilmicosin micellar preparation, which is composed of: 3.5g tilmicosin, 12.5g poloxamer 118, 58g PBS buffer solution, 4g glucose and 1.0g citric acid.

[0028] The preparation method is as follows:

[0029] (1) Put Poloxamer 188 in an eggplant-shaped bottle, add a dissolved amount of absolute ethanol to dissolve, and evaporate the organic solvent in a water bath at 50°C under reduced pressure to form a film.

[0030] (2) Dissolve tilmicosin and glucose with PBS buffer.

[0031] (3) Add (2) to (1), stir and hydrate for 2.5 hours, adjust the pH to 6 with citric acid, and then filter through a 0.45 um membrane to obtain the product.

[0032] The encapsulation efficiency and drug loading of tilmicosin were determined to be 88% and 17%, respectively.

Embodiment 3

[0034] A tilmicosin micellar preparation, which is composed of: tilmicosin 5.0g, poloxamer 188 15.5g, PBS buffer 68g, glucose 8.0g, citric acid 1.1g.

[0035] The preparation method is as follows:

[0036] (1) Put Poloxamer 188 in an eggplant-shaped bottle, add a dissolved amount of acetonitrile to dissolve, and evaporate the organic solvent in a water bath at 55°C under reduced pressure to form a film.

[0037] (2) Dissolve tilmicosin and glucose with PBS buffer.

[0038] (3) Add (2) to (1), stir and hydrate for 3 hours, adjust the pH to 7 with citric acid, and then filter with a 0.45um filter membrane to obtain the product.

[0039] The encapsulation efficiency and drug loading of tilmicosin were determined to be 80% and 14%, respectively.

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Abstract

The invention belongs to the technical field of medicinal preparations and relates to a tilmicosin micelle preparation and a preparation method thereof. The tilmicosin micelle preparation comprises the following components in part by weight: 3 to 5 parts of tilmicosin, 5.0 to 15.5 parts of pharmaceutically acceptable carrier materials, 52 to 68 parts of poly(butylene succinate) (PBS ), 0 to 8 parts of additive and a pH modifier, wherein the pH value of the pH modifier is 5 to 7. In the tilmicosin micelle preparation, poloxamer 188 serves as the main micelle component. The poloxamer 188 is an asymmetric amphiphilic block copolymer and can automatically form the micelle in aqueous solution, wherein the hydrophobic block of the micelle gathers inwards and the hydrophilic block gathers outwards. Because the formed micelle is relatively smaller low in particle size, the micelle is higher in retention capability to an inflammatory part and stable onto heat and is not easy to oxidize. The entrapment rate and the drug loading capacity of the tilmicosin micelle preparation are high.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a tilmicosin micellar preparation and a preparation method thereof. Background technique [0002] Tilmicosin (Tilmicosin) is a kind of animal-specific macrolide antibiotic developed by Elanco in the 1980s, and was approved for marketing in my country in the 1990s. It is white or light yellow crystalline powder, easily soluble in methanol, acetonitrile, acetone, soluble in ethanol, almost insoluble in n-hexane. [0003] Tilmicosin has special antibacterial activity and pharmacological characteristics, and has inhibitory effects on Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, spirochetes, etc., especially against Actinomyces pleuropneumoniae, hemolytic Pasteurella Bacillus, Pasteurella multocida and Mycoplasma poultry have lighter antibacterial activity than tylosin; its pharmacokinetics have been studied in cows, dairy goats, sheep, pigs, ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/706A61K47/34A61P31/04
Inventor 贺培益柴保国高义
Owner HENAN SOAR VETERINARY PHARMA
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