Doramectin sustained-release microcapsule injection

A technology of doramectin and injection, which is applied in the field of antiparasitic pharmaceutical preparations, and can solve problems such as short half-life, impact on the healthy growth of livestock, and stimulation response of livestock and poultry

Active Publication Date: 2020-11-27
江西省科达动物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of doramectin itself, the current common dosage form is oily injection, and the drug release in livestock and poultry often has a "peak and valley" phenomenon, which is easy to cause livestock and poultry poisoning, and has a short half-life, poor stability, and requires a large number of repeated administration , increased labor costs, and the repeated administration of some dosage forms brought obvious irritating reactions to livestock and poultry, which affected the healthy growth of livestock

Method used

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  • Doramectin sustained-release microcapsule injection
  • Doramectin sustained-release microcapsule injection
  • Doramectin sustained-release microcapsule injection

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0031] 1. Preparation of silica airgel particles:

[0032] (a) Add tetraethyl orthosilicate to deionized water, slowly add ethanol until the mixed solution becomes clear;

[0033] (b) Adding dilute hydrochloric acid under stirring to adjust the pH to 3.0-4.0, standing still at room temperature for 12-24 hours, adding a pore-enlarging agent to prepare an aqueous phase system;

[0034] (c) Use n-hexane as the oil phase, mix the emulsification system and stir evenly to make an oil phase system, add the water phase system of step (b) into the oil phase system under stirring, add ammonia water under stirring to adjust the pH to 7.0 ~8.0 and continue to stir for 15 minutes, let it stand until the wet gel is formed, add the protective solution and put it in a closed container for aging;

[0035] (d) add n-hexane to soak in the wet gel after aging, perform solvent exchange, and replace n-hexane several times;

[0036] (e) removing solvent to obtain silica airgel powder;

[0037] (f...

Embodiment 1

[0060] (1) Dissolve poly-L-lactic acid and poly-D-lactic acid with a molecular weight of 1-10W in chloroform to obtain 10g / L poly-L-lactic acid solution and 10g / L poly-D-lactic acid solution, and then add excess doramectin, stirred and filtered to obtain poly L-lactic acid solution and poly D-lactic acid solution containing saturated doramectin.

[0061] (2) Add the drug-loaded particles 16 into a centrifuge tube, add poly-L-lactic acid solution and shake to disperse the particles, shake at 40°C for 1 hour, and wash with chloroform centrifuge for 3 times, the centrifugation parameters are 1000r / min, 1min;

[0062] (3) Add poly-D-lactic acid solution into the centrifuge tube and oscillate to disperse the particles, oscillate at 40°C for 1 hour, wash with chloroform for 3 times, and the centrifugation parameter is 1000r / min, 1min;

[0063] (4) Freeze-dry to constant weight to obtain polylactic acid-wrapped silicon dioxide airgel-doramectin microcapsule particles.

[0064] Compa...

Embodiment 2

[0066] (1) Dissolve poly-L-lactic acid and poly-D-lactic acid with a molecular weight of 1-10W in chloroform to obtain 10g / L poly-L-lactic acid solution and 10g / L poly-D-lactic acid solution, and then add excess doramectin, stirred and filtered to obtain poly L-lactic acid solution and poly D-lactic acid solution containing saturated doramectin.

[0067] (2) Add the drug-loaded particles 17 into a centrifuge tube, add poly-L-lactic acid solution and oscillate to disperse the particles, oscillate at 40°C for 1 hour, and centrifuge and wash 3 times with chloroform, the centrifugation parameter is 1000r / min, 1min;

[0068] (3) Add poly-D-lactic acid solution into the centrifuge tube and oscillate to disperse the particles, oscillate at 40°C for 1 hour, wash with chloroform for 3 times, and the centrifugation parameter is 1000r / min, 1min;

[0069] (4) Freeze-dry to constant weight to obtain polylactic acid-wrapped silicon dioxide airgel-doramectin microcapsule particles.

[0070]...

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Abstract

The invention belongs to the field of antiparasitic pharmaceutical preparations, and particularly relates to a doramectin sustained-release microcapsule injection. The doramectin sustained-release microcapsule injection comprises doramectin microcapsule particles, a wetting agent, a suspending agent, a deflocculating agent and water for injection, wherein the doramectin microcapsule particles takedoramectin-loaded silicon dioxide aerogel particles as a capsule core and polylactic acid as a capsule membrane. The prepared polylactic acid-coated silicon dioxide aerogel-doramectin microcapsule particles have a sustained-release effect, are stable to light and are prepared into an injection, and the injection can achieve a long-acting effect after being administered in animal testing.

Description

technical field [0001] The invention belongs to the field of antiparasitic drug preparations, and in particular relates to a doramectin sustained-release microcapsule injection. Background technique [0002] Animal parasitic diseases are common diseases in my country's animal husbandry, with various types and wide distribution, causing great harm to animal husbandry. Doramectin is a kind of abamectin antiparasitic drug which is fermented by the new strain of Streptomyces avermitilis with the precursor of cyclohexyl amino acid. It is the third generation of abamectin Derivatives are considered to be one of the best antiparasitic drugs in the abamectin family. Doramectin has high fat solubility and is easily soluble in organic solvents, such as methanol, ethanol, acetone, propylene glycol, dimethyl sulfoxide, ethyl acetate, isopropyl acetate, etc., and has low solubility in water. sensitive. Due to the poor water solubility of doramectin itself, the current common dosage fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/52A61K47/04A61K47/34A61K31/7048A61P33/00
CPCA61K9/0019A61K9/08A61K9/5031A61K9/5089A61K9/5073A61K47/02A61K31/7048A61P33/00Y02A50/30
Inventor 嵇根龙
Owner 江西省科达动物药业有限公司
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