Acetyl amino abamectin sustained-release microsphere and preparation method as well as sustained-release microsphere injection

A technology of acetamido abamectin and slow-release microspheres, which can be applied in pharmaceutical formulations, medical preparations containing active ingredients, and devices for making medicines into special physical or taking forms, etc. It can improve the bioavailability, reduce the cost of medication, and reduce the number of times of administration.

Inactive Publication Date: 2012-04-25
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing microsphere preparation method mainly adopts the emulsified solvent evaporation method, the parti

Method used

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  • Acetyl amino abamectin sustained-release microsphere and preparation method as well as sustained-release microsphere injection
  • Acetyl amino abamectin sustained-release microsphere and preparation method as well as sustained-release microsphere injection
  • Acetyl amino abamectin sustained-release microsphere and preparation method as well as sustained-release microsphere injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: The acetamidoabamectin sustained-release microspheres were prepared by the following method.

[0025] 1. Dissolve 250mg of acetaminobamectin and 1g of PLGA (50 / 50 DLG 4E Mw=57000) in 10ml of dichloromethane to fully dissolve to form an oil phase.

[0026] 2. Prepare 0.5L aqueous solution of polyvinyl alcohol with a concentration of 1wt% (the degree of alcoholysis is 88%, the degree of polymerization is 1725, and the weight average molecular weight is 30,000), so as to ensure that the polyvinyl alcohol is completely dissolved in water to form an aqueous phase; The injection pump injects the oil phase into the vortex-shaped PVA water phase dispersion medium at a constant speed through a conical nozzle with an inner diameter of 0.12 mm. During the injection process, the oil phase stream at the outlet of the nozzle obtains a constant shear force, forming an oil-in-water emulsion. Stir at room temperature for 6 hours to solidify the microspheres.

[0027] 3. T...

Embodiment 2

[0030] Embodiment 2: The acetamidoabamectin sustained-release microspheres were prepared by the following method.

[0031] 1. Dissolve 250mg of acetaminobamectin and 1g of PLGA (50 / 50 DLG 9E Mw=155000) in 20ml of dichloromethane to fully dissolve to form an oil phase.

[0032] 2. Prepare 0.7L of polyvinyl alcohol (PVA) aqueous solution with a concentration of 1wt% (alcoholysis degree of 90%, polymerization degree of 1750, weight average molecular weight of 50,000) to make the water phase; use a syringe pump to pass the oil phase through 0.12 A conical nozzle with an inner diameter of mm is injected into the vortex-shaped PVA water-phase dispersion medium at a constant speed. During the injection process, the shear force obtained by the fine flow of the oil phase at the outlet of the nozzle is constant, forming an oil-in-water emulsion. Stir at room temperature for 18 hours to make the microspheres solidify.

[0033]3. The solidified microspheres were centrifuged and washed th...

Embodiment 3

[0036] Example 3: The acetamidoabamectin sustained-release microspheres were prepared by the following method.

[0037] 1. Dissolve 467mg of acetamidobamectin and 1g of PLGA (65 / 35 DLG 5E IV=0.5) in 15ml of dichloromethane to fully dissolve to form an oil phase.

[0038] 2. Prepare 1.0L of polyvinyl alcohol (PVA) aqueous solution with a concentration of 3wt% (alcoholysis degree of 87%, polymerization degree of 1700, weight average molecular weight of 20,000) to make the water phase; use a syringe pump to pass the oil phase through 0.20 The conical nozzle with an inner diameter of mm injects the vortex-shaped PVA water phase dispersion medium at a constant speed. During the injection process, the oil phase stream at the outlet of the nozzle obtains a constant shear force to form an oil-in-water emulsion. Stir at room temperature for 12 hours to make the micro The ball solidifies.

[0039] 3. The solidified microspheres were centrifuged and washed three times with water, collec...

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Abstract

The invention discloses an acetyl amino abamectin sustained-release microsphere and a preparation method as well as sustained-release microsphere injection. In the acetyl amino abamectin sustained-release microsphere, PLGA (polylactic-co-glycolic acid) is taken as a host material. The acetyl amino abamectin/PLGA microsphere is a long-acting constant-speed release preparation, and the medicine is controlled to release at zeroth order rate without burst release. By controlling the particle size of the microsphere, the PLGA molecular weight and copolymer proportioning, the microspheres at different medicine releasing time are obtained, and the microsphere releases the medicine for at least 50 days. Compared with the existing acetyl amino abamectin preparation formulation, the sustained-release microsphere injection has the advantages that the medicine quantity and the medicine utilization cost are remarkably reduced, the bioavailability is improved over 60%; and compared with the normal injection, the sustained-release microsphere injection has the advantages that the dosing times are reduced, and the intensification cultivation of animal husbandry is facilitated.

Description

technical field [0001] The invention belongs to the technical field of veterinary drug preparations, in particular to an acetamidoabamectin sustained-release microsphere, a preparation method thereof and a sustained-release microsphere injection. Background technique [0002] Acetaminobamectin is a macrolide antibiotic developed by Merck Company of the United States in 1996. It mainly acts on the nervous system of parasites, promotes the release of γ-aminobutyric acid, opens chloride ion channels, and prevents the excitation to muscles Transmission, eventually causing parasite paralysis to death, has a strong killing effect on most nematodes and arthropods. At present, the broad-spectrum antiparasitic drug widely used in the market is ivermectin, which has a high milk / blood partition coefficient (1.1). When it is applied to lactating dairy cows, it needs to waste 35 days of milk; it needs 28 days of milk to be used in beef cattle. drug holiday. However, acetaminobamectin h...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/7048A61K47/34A61P33/00A61P33/10A61J3/00
Inventor 尚青郑婷
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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