Ivermectin controlled-release capsule and preparation method and application thereof

A slow-release technology for ivermectin, which is applied in the field of preparation of animal drugs, can solve the problems of only oral bioavailability, low blood drug concentration, and poor treatment effect on ectoparasites, so as to improve the drug protection rate and enhance Therapeutic, particle uniform effect

Inactive Publication Date: 2018-03-09
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The problem to be solved by the present invention is to degrade the existing ivermectin preparations under acidic environment conditions, resulting in oral bioavailability of only 40% to 80%, resulting in animal body surface blood drug concentration lower than therapeutic blood drug concentration, for Insufficient technology for poor efficacy of ectoparasite treatment

Method used

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  • Ivermectin controlled-release capsule and preparation method and application thereof
  • Ivermectin controlled-release capsule and preparation method and application thereof
  • Ivermectin controlled-release capsule and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Follow the steps below to prepare ivermectin sustained-release microcapsules:

[0047] S1. Weigh 0.2% ivermectin, 38.8% hydroxypropyl-β-cyclodextrin, 60% PVAP (polyethylene phthalate) according to the proportion, heat and melt hydroxypropyl-β-cyclodextrin at 90°C , mixed evenly to obtain a mixture;

[0048] S2. The ivermectin raw material is dissolved in ethanol and added to the mixture described in step S1, and stirred evenly to obtain the mixture;

[0049] S3. Add PVAP (polyethylene phthalate) to the mixture described in step S2, and stir evenly at 40°C to obtain a mixture;

[0050] S4. Cool the mixture described in step S3 to 65-80°C, and carry out fluidized bed spray granulation, the temperature of fluidized air is 20°C, and the linear velocity is 55 m / s;

[0051] S5. Cool the powder described in step S4, sieve through a 40-mesh sieve, and collect to obtain 0.2% ivermectin sustained-release microcapsules with a particle size of about 400 μm.

Embodiment 2

[0053] Follow the steps below to prepare ivermectin sustained-release microcapsules:

[0054] S1. According to the proportion, weigh 0.4% ivermectin, 44.6% HPMC (hydroxypropyl methylcellulose), 55% acrylic resin No. II, heat and melt HPMC (hydroxypropylmethylcellulose) at 95°C, and mix evenly to obtain a mixture ;

[0055] S2. The ivermectin raw material is dissolved in ethanol and added to the mixture described in step S1, and stirred evenly to obtain the mixture;

[0056] S3. Add acrylic resin No. II to the mixture described in step S2, and stir evenly at 50° C. to obtain a mixture;

[0057] S4. Cool the mixture described in step S3 to 65-80°C, and carry out fluidized bed spray granulation, the temperature of fluidized air is 18°C, and the linear velocity is 135 m / s;

[0058] S5. Cool the powder described in step S4, sieve through a 40-mesh sieve, and collect to obtain 0.4% ivermectin sustained-release microcapsules with a particle size of about 80 μm.

Embodiment 3

[0060] Follow the steps below to prepare ivermectin sustained-release microcapsules:

[0061] S1. Weigh 0.6% ivermectin, 45.4% bile salt / phospholipid mixed micelles, 54% HPMCAS (hydroxypropyl methylcellulose acetate succinate) according to the proportion, heat and melt the bile salt / phospholipid mixed micelles at 100°C , mixed evenly to obtain a mixture;

[0062] S2. The ivermectin raw material is dissolved in ethanol and added to the mixture described in step S1, and stirred evenly to obtain the mixture;

[0063] S3. Add HPMCAS (hydroxypropylmethylcellulose acetate succinate) to the mixture described in step S2, and stir evenly at 50°C to obtain a mixture;

[0064] S4. Cool the mixture described in step S3 to 65-80°C, and carry out fluidized bed spray granulation, the temperature of fluidized air is 25°C, and the linear velocity is 100 m / s;

[0065] S5. Cool the powder described in step S4, sieve through a 40-mesh sieve, and collect to obtain 0.6% ivermectin sustained-relea...

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Abstract

The invention discloses an ivermectin controlled-release capsule and a preparation method and application thereof. The ivermectin controlled-release capsule comprises, by mass, 0.1-1% of ivermectin raw material, 20-60% of water-soluble carrier and 30-70% of enteric-soluble wrapping material, the water-soluble carrier is one or multiple of hydroxypropyl-beta-cyclodextrin, methyl-beta-cyclodextrin,HPMC, PVP, PEG, poloxamer 188, mannitol, D-alpha-tocopherol PEG 1000 succinate, cholate/phospholipid mixed micelle, polyethylenediamine dendritic polymer, phospholipid or cholesterol, and the enteric-soluble wrapping material is one or multiple of hydroxypropyl methyl cellulose phthalic acid, acrylic resin II, acrylic III, cellulose acetate phthalate, polyethylene diacetate phthalate or hydroxypropyl methyl cellulose acetate succinate. The ivermectin controlled-release capsule has the advantage of outstanding acid resistance, enables drug to reach intestinal tracts to be disintegrated and released, remarkably improves bioavailability and has remarkable treatment effect.

Description

technical field [0001] The invention belongs to the technical field of preparation of animal medicines, and in particular relates to a vermectin sustained-release microcapsule and its preparation method and application. Background technique [0002] Animal parasitic diseases are an important part of livestock infectious diseases that cannot be ignored, and there are many types of pathogenic parasites. Common internal parasites include roundworms, flagellates, strongyloids, trichinella, nodularia, coccidia, tapeworms, trematodes Etc. External parasites include ticks, fleas, flies, ticks, lice, etc. It seriously affects the output of meat, milk and eggs, the quality of fur, seriously restricts the healthy development of animal husbandry, and some zoonotic parasitic diseases also directly endanger human health, causing huge economic losses to the animal husbandry industry and causing serious public health problem. [0003] Ivermectin (IVM) was discovered by Berge in 1979. The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/7048A61K47/40A61K47/32A61K47/10A61K47/38A61K47/34A61P33/10A61P33/00A61K31/4184
CPCA61K31/7048A61K9/5026A61K9/5031A61K9/5036A61K9/5042A61K31/4184A61K2300/00
Inventor 黄显会张申魏开赟
Owner SOUTH CHINA AGRI UNIV
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