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Itraconazole injection for dogs and preparation method thereof

An itraconazole and injection technology, applied in the field of veterinary medicines, can solve the problems of high price, restricted promotion and use, etc., and achieve the effects of high drug concentration, good therapeutic effect and good stability

Inactive Publication Date: 2010-11-24
NORTHEAST AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the price is more expensive, which limits its promotion and use

Method used

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  • Itraconazole injection for dogs and preparation method thereof
  • Itraconazole injection for dogs and preparation method thereof
  • Itraconazole injection for dogs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Weigh 1g of itraconazole and 25g of hydroxypropyl-β-cyclodextrin, and put them into Erlenmeyer flasks A and B respectively. Then add 5 mL of propylene glycol to bottle A, and slowly add 12 mol·L -1 Concentrated hydrochloric acid 370μL until itraconazole is completely dissolved; hydroxypropyl-β-cyclodextrin in B is dissolved in 30mL double distilled water. Then, under the condition of magnetic stirring, the itraconazole solution in A was slowly added dropwise to B, and the dropping time was 15 minutes. For inclusion, the inclusion time is 30h. After the inclusion is completed, the concentration of the inclusion solution is 0.8mol L -1 NaOH solution to adjust the pH to 5.5. Filter it with a 0.45 μm microporous membrane, and sterilize it by flowing steam at 100°C after bottling, that is, itraconazole injection for dogs.

[0017] In the injection prepared in this example, the inclusion rate of itraconazole can reach 80%. The prepared injection is clear and yellow. The...

Embodiment 2

[0019] Weigh 1g of itraconazole and 20g of hydroxypropyl-β-cyclodextrin, and put them into Erlenmeyer flasks A and B respectively. Then add 5mL of propylene glycol to bottle A, and then slowly add the concentration of 12mol L -1 Concentrated hydrochloric acid 370μL until itraconazole is completely dissolved; hydroxypropyl-β-cyclodextrin in B is dissolved in 24mL double distilled water. Then, under the condition of magnetic stirring, the itraconazole solution in A was slowly added dropwise to B, and the dropping time was 15 minutes. For inclusion, the inclusion time is 36h. After the inclusion is completed, the concentration of the inclusion solution is 0.8mol L -1 NaOH solution to adjust the pH to 5.5. Filter it with a 0.45 μm microporous membrane, and sterilize it by flowing steam at 100°C after bottling to obtain itraconazole injection for dogs.

[0020] The average particle size and encapsulation efficiency of the liposomes prepared in this example were 73%. The prepar...

Embodiment 3

[0022] Weigh 1g of itraconazole and 30g of hydroxypropyl-β-cyclodextrin, and put them into Erlenmeyer flasks A and B respectively. Then add 5mL of propylene glycol to bottle A, and then slowly add the concentration of 12mol L -1 Concentrated hydrochloric acid 370μL until itraconazole is completely dissolved; hydroxypropyl-β-cyclodextrin in B is dissolved in 36mL double distilled water. Then, under the condition of magnetic stirring, the itraconazole solution in A was slowly added dropwise to B, and the dropping time was 15 minutes. For inclusion, the inclusion time is 24h. After the inclusion is completed, the concentration of the inclusion solution is 0.8mol L -1 NaOH solution to adjust the pH to 5.5. Filter it with a 0.45 μm microporous membrane, and sterilize it by flowing steam at 100°C after bottling to obtain itraconazole injection for dogs.

[0023] The inclusion rate of itraconazole in the injection prepared in this example was 86%. The prepared injection solution...

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Abstract

The invention relates to itraconazole injection for dogs and a preparation method thereof and belongs to an animal medicament. The injection consists of itraconazole, hydroxypropyl-beta-cyclodextrin, propylene glycol, 12 mol.L<-1> of concentrated hydrochloric acid and double distilled water. The preparation method comprises the following steps of: preparing itraconazole inclusion liquid by using hydroxypropyl-beta-cyclodextrin inclusion technology; adding sodium hydroxide solution into the inclusion liquid; adjusting the pH value; filtering the mixture; and circulating vapor for sterilization to obtain the itraconazole injection for the dogs. The injection finished product prepared by the method is yellow and transparent liquid and has the characteristics of high stability, sustained-release property and long-term effectiveness; the inclusion rate of the itraconazole can reach 80 percent; pharmacokinetic characteristic and pharmacodynamics are superior to those of the conventional formulations.

Description

technical field [0001] The invention belongs to the field of veterinary drugs, and mainly relates to a new dosage form of a dog drug for treating canine fungal skin diseases and a preparation method thereof. Background technique [0002] Hydroxypropyl-β-cyclodextrin is a cylindrical compound formed by connecting six glucose molecules through α-1.4 glycosidic bonds. On the outside, the glycosidic bond oxygen atom is located in the middle of the cylinder and inside the cylinder, the two ends and the outside of the hydroxypropyl-β-cyclodextrin are hydrophilic, while the outside of the cylinder is hydrophobic, some size The drug molecules with appropriate shape are included in the ring structure to form ultramicrocapsule inclusion complexes. It has many advantages, such as increasing the solubility of drugs; increasing the stability of drugs; improving the link and improvement of local irritation; improving bioavailability; slow and controlled release of drugs, etc. With the d...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/496A61K47/40A61P31/10A61P17/00
Inventor 刘云陈亮陈曦
Owner NORTHEAST AGRICULTURAL UNIVERSITY
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