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Self-emulsifying solid preparation containing ivermectin drug

A solid preparation, ivermectin technology, applied in the field of preparation of self-emulsifying solid dispersion containing ivermectin drugs

Inactive Publication Date: 2017-05-24
北京科百大科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the surfactant is not selected properly, it will make the drug more susceptible to acid / base catalyzed degradation

Method used

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  • Self-emulsifying solid preparation containing ivermectin drug
  • Self-emulsifying solid preparation containing ivermectin drug
  • Self-emulsifying solid preparation containing ivermectin drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Screening of surfactants by acid-catalyzed degradation test of microemulsions containing different surfactants

[0041] (1) Microemulsion composition: The surfactants used in the preparation of microemulsions include the surfactants described in Table 5 and polyoxyethylene castor oil condensate, polyethylene glycol (40) palm kernel oil, polyethylene glycol (60) ) Corn oil, polyethylene glycol (60) corn oil glycerides, polyethylene glycol (60) almond oil, polyethylene glycol (50) castor oil, the effective component is ivermectin (0.6%), micro The oil phase in the emulsion is ethyl acetate, the co-emulsifier is 1,2-propylene glycol, and water is added to 100% of the volume of the microemulsion. (2) Acid-catalyzed degradation test method: Take 1ml of microemulsion, add 19ml of 0.1M hydrochloric acid solution, react at 36-37℃ for 1 hour, adjust the pH with alkali and filter, and detect MS H in the filtrate by HPLC 2 B 1 a and H 2 B 1 a, record the chromatogram, calc...

Embodiment 2

[0042] Example 2. Screening of surfactants through the acid catalytic degradation test of ivermectin

[0043] (1) The basic formula of the preparation (weight ratio): 0.6% ivermectin, 10% surfactant, 8% glyceryl monostearate, 0.8% 1,2-propanediol, between 40-100 mesh The corncob flour is added to 100%.

[0044] (2) Preparation method of the preparation: mix ivermectin, surfactant, glyceryl monostearate, 1,2-propanediol, stir and dissolve at 80-85°C, add corn cob powder, fully Stir and mix well and cool down to room temperature to get.

[0045] (3) Acid catalytic degradation test and test results

[0046] Take 1 gram of sample into a 25 ml test tube with stopper, add 18 ml of water, shake for 5 minutes, then add 2 ml of 1M hydrochloric acid solution, mix well, incubate at 36-37°C for 1 hour, draw 5 ml of reaction solution, add 10% About 0.24 ml of sodium hydroxide solution, mix well, add methanol to make the volume up to 10 ml, mix well, filter with 0.45um membrane, detect the filtra...

Embodiment 3

[0050] Example 3. Preparations containing HEL-40 and different oily media and their acid-catalyzed hydrolysis test

[0051] (1) The basic formulation (weight ratio) of the preparation: 0.6% ivermectin, HEL-4010%, 1,2-propanediol 1%, an appropriate amount of oily medium (see Table 6), and corncob powder to 100%. (2) Acid-catalyzed hydrolysis test: Take a sample of 1.00 g in a 25 ml test tube with a stopper, add 18 ml of water, shake for 5 minutes, then add 2 ml of 1M hydrochloric acid solution, mix well, incubate at 36-37°C for 2 hours, and absorb 5ml of reaction solution, add about 0.24ml of 10% sodium hydroxide solution, mix well, add methanol to make the volume to 10ml, mix well, filter with 0.45um membrane, and detect the filtrate by HPLC (inject 20ul), record the peak Area value, calculate MS H 2 B 1 a peak area value and H 2 B 1 a Ratio of peak area value (%). The test results are shown in Table 6.

[0052] Table 6. The effect of oily medium on the acid-catalyzed hydrolysis ...

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Abstract

The invention mainly aims at solving the technical problems to improve the water solubility of an ivermectin drug and overcome the defect that the ivermectin drug is easy to degrade under an acidic condition, so that the dissolubility of the drug in bodies is improved; meanwhile, the aim that the drug is not damaged or is less damaged in acidic gastric juice is realized; and secondly, during a storage period of a preparation, acid / alkali catalytic degradation and oxidization degradation problems of active components are solved, and fewer effective components in the drug are degraded. An especially preferable preparation is prepared from the ivermectin drug, a polyoxyethylene hydrogenated castor oil condensation compound with the HLB value more than 12, Arabic gum or / and polyvinylpyrrolidone, benzyl benzoate or azone, 1,2-propylene glycol, corncob meal or / and beef powder, chicken liver powder and pork liver powder. The ivermectin drug, the polyoxyethylene hydrogenated castor oil condensation compound, the Arabic gum or / and the polyvinylpyrrolidone, the benzyl benzoate or the azone and the1,2-propylene glycol exist in a preparation in a form of a self-emulsifying solid dispersion body drug releasing system.

Description

Technical field [0001] The invention belongs to the preparation technology of veterinary drug preparations, and specifically relates to a preparation technology of self-emulsifying solid dispersions containing ivermectin drugs. The preparations prepared by the technology have the characteristics of high dissolution rate and more resistance to acid / base catalytic degradation. Background technique [0002] Ivermectin drugs are highly effective and broad-spectrum antiparasitic drugs. They have a strong repellent effect on nematodes and ectoparasites that are parasitic in animals. They are widely used in the prevention and treatment of animal parasitic diseases. Commercially available veterinary products include injections, oral liquids, pouring agents, ointments, granules, sustained-release pellets, tablets, powders, premixes, etc. The premix is ​​mainly used for the prevention and control of parasitic diseases in pigs and horses. At the current stage, the products on the market in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/16A61K47/44A61K47/32A61K47/14A61K47/22A61K47/36A61K31/7048A61K31/365A61P33/00
CPCA61K9/145A61K9/146A61K9/1617A61K9/1635A61K9/1652A61K31/365A61K31/7048
Inventor 王玉万王金萍韩可可翁志飞任亚楠李莹李蕾沈力
Owner 北京科百大科技有限责任公司
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