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Preparation method of emulsifiable oily injection containing avermectins

A technology of abamectin and base abamectin, applied in the direction of medical preparations containing active ingredients, antibacterial drugs, pharmaceutical formulas, etc., can solve the problem that the immediate release effect is not as good as that of emulsion and microemulsion, and achieve optimal emulsification Performance and safety, good biocompatibility, and the effect of improving the effective utilization rate

Active Publication Date: 2017-09-19
中农华威制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Patent CN 103720652A discloses an oily injection containing abamectins prepared from poloxamer 407. The poloxamer 407 contained in the preparation has the property of gelling at body temperature. The preparation is injected into the body, The drug is double-wrapped by oil and gel and exists at the injection site. Its sustained release effect is worse than that of oil prepared by conventional methods, but its immediate release effect is far inferior to that of emulsion and microemulsion.

Method used

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  • Preparation method of emulsifiable oily injection containing avermectins
  • Preparation method of emulsifiable oily injection containing avermectins
  • Preparation method of emulsifiable oily injection containing avermectins

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、4

[0026] Composition, preparation and in vitro emulsification performance experiment of embodiment 1,4% abamectin injection

[0027] (1) Preparation composition: Based on the preparation of 100ml, the ingredients of preparations 1 to 10 and the comparative preparation are shown in the table below.

[0028] Preparation number

Abamectin (g)

P188(g)

HCO (g)

Soy Lecithin (g)

Preparation 1

4

5

0.3

0.4

Preparation 2

4

4

0.6

0.8

Preparation 3

4

3

0.9

0.4

Preparation 4

4

9

0.3

0.4

Preparation 5

4

8

0.6

0.8

Preparation 6

4

7

0.9

1.1

Preparation 7

4

12

0.6

0.8

Preparation 8

4

3

0.9

1.1

Preparation 9

4

3

-

-

Preparation 10

4

9

-

-

Comparative preparation 1

4

-

0.9

0.4

Comparative preparation 2

4

-

-

-

[0029] Note: All preparations in t...

Embodiment 2

[0041] Embodiment 2, preparation of different content ivermectin injections and in vitro emulsification performance experiment

[0042] (1) Preparation composition: Based on the preparation of 100ml, the ingredients of preparations 11 to 19 are shown in the table below.

[0043] Preparation number

Ivermectin (g)

P188(g)

HCO (g)

Soy Lecithin (g)

Benzyl Benzoate (ml)

Preparation 11

3

7

0.8

0.4

35

Preparation 12

4.5

5

0.8

0.4

50

Preparation 13

6

3

0.8

0.4

65

[0044] Preparation 14

3

7

0.8

-

35

Preparation 15

4.5

5

0.8

-

50

Preparation 16

6

3

0.8

-

65

Preparation 17

3

3

-

-

65

Preparation 18

4.5

5

-

-

65

Preparation 19

6

7

-

-

65

[0045] Note: All preparations in the table are added with antioxidants BHT0.02g, BHA0.01g, PG0.005g, and ethyl olea...

Embodiment 3

[0051] Embodiment 3, composition and preparation of doramectin injection

[0052] (1) Preparation composition: Based on the preparation of 100ml, the ingredients of preparations 20 to 25 are shown in the table below.

[0053]

[0054] Note: Antioxidant is BHT+BHA+PG=0.02+0.01+0.005=0.035

[0055] (2) Preparation method

[0056] aPut doramectin and P188 into a reflux bottle, add 4-6 times the amount of absolute ethanol equivalent to doramectin, dissolve in a water bath at 80-85°C under reflux, and then distill under reduced pressure to remove most of the solvent , cooled (5-10°C) to make it solidify, take out the solidified product, dry it to constant weight in a vacuum drying oven at 35-38°C, -0.09 to -0.1MPa, crush it, and pass through a 40-mesh sieve to obtain drug-loaded particles;

[0057] b Mix the drug-loaded particles, HCO, soybean lecithin, antioxidant and 2 / 3 of tea seed oil, and repeatedly shear them with a high-shear homogenizer until the particle size of the ...

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Abstract

Combining poloxamer 188 with an oily medium is used to prepare injections containing abamectin antiparasitic drugs. The preparation also contains an appropriate amount of hydrogenated castor oil, soybean lecithin, local analgesics and antioxidants. The main feature of the preparation is that the preparation is emulsified when it encounters water (or body fluid), and a mixed system of emulsion droplets and oil is formed at the injection site, and the preparation has both quick-release effect and long-term effect. This preparation is called an emulsifiable oily injection.

Description

technical field [0001] The invention belongs to the preparation technology of veterinary drug preparations, and in particular relates to the preparation of emulsifiable oily injections by combining abamectins, poloxamer 188, hydrogenated castor oil and oily medium. Background technique [0002] Abamectin drugs include abamectin, ivermectin, acetamidoabamectin, doramectin, mebemycin oxime, and moxidectin, which are mainly used for animal parasites in veterinary clinics. Insect Disease Control (Edited by Zhu Mozhong, Handbook of Veterinary Medicine, Chemical Industry Press, 1st edition in July 2002, pages 167-174). These antiparasitic drugs have been on the market for more than 30 years, and drug resistance has developed to varying degrees in places where they have been used for a long time at home and abroad, and drug resistance is still developing day by day. Therefore, from the perspective of effective control of drug-resistant parasites, the development of sustained-relea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/7048A61K31/365A61K47/44A61K47/10A61P31/04
Inventor 游锡火潘贞德王玉万戴晓曦任雅楠翁志飞沈力
Owner 中农华威制药股份有限公司
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