Itraconazole isomer oral liquid

A technology of itraconazole and oral solution, applied in the field of medicine, can solve the problems of increasing the absorption of lipophilic poisons, affecting health and the like

Active Publication Date: 2013-01-16
广州力鑫生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The oral safety of hydroxypropyl-β-cyclodextrin has been confirmed in animal and human experiments, but Jiri and Pitha [J Pharm Sci, 1996; 85(1):96] proposed that although hydroxypropyl-β-cyclodextrin Essence itself is not toxic, but it can affect health by increasing the absorption of lipophilic poisons and carcinogens in the gastrointestinal tract

Method used

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  • Itraconazole isomer oral liquid
  • Itraconazole isomer oral liquid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prepare 1000ml of 2S4R itraconazole concentration of 15% (w / v) oral solution, which contains the following ingredients:

[0033] 2S4R Itraconazole 150g, Hydroxypropyl-β-cyclodextrin 400g, Propylene Glycol 100ml, 70% Sorbitol 200ml, Hydrochloric Acid 3.8ml, Sodium Saccharin 0.6g, Hydroxypropylcellulose 0.5g, Cherry Flavor 1g , Add distilled water to 1000ml.

[0034]Its preparation method: first add 0.5g hydroxypropyl cellulose to 200ml distilled water, stir to dissolve; add 3.8ml concentrated hydrochloric acid to 100ml propylene glycol, slightly heat and stir, add 150g of 2S4R itraconazole and stir until homogeneous . Take another container, add 400g of hydroxypropyl-β-cyclodextrin into 400ml of distilled water and stir to dissolve, slowly add the above-mentioned 2S4R itraconazole propylene glycol acidic solution into the cyclodextrin solution under constant stirring to obtain 2S4R Add 200ml sorbitol solution, 0.6g sodium saccharin, 1g flavoring agent to the clathrate ...

Embodiment 2

[0037] Prepare 1000ml of 2S4R itraconazole concentration of 5% (w / v) oral solution, which contains the following ingredients:

[0038] 2S4R Itraconazole 50g, Hydroxypropyl-β-cyclodextrin 300g, Propylene Glycol 200ml, 70% Sorbitol 200ml, Hydrochloric Acid 3.8ml, Sodium Saccharin 0.6g, Hydroxypropylcellulose 0.1g, Caramel Flavor 1g, add distilled water to 1000ml.

[0039] Its preparation method: first add 0.1g hydroxypropyl cellulose to 200ml distilled water, stir to dissolve; add 3.8ml concentrated hydrochloric acid to 200ml propylene glycol, slightly heat and stir, add 50g of 2S4R itraconazole and stir until homogeneous . Take another container, add 300g of hydroxypropyl-β-cyclodextrin into 400ml of distilled water and stir to dissolve, then slowly add the above-mentioned 2S4R itraconazole propylene glycol acidic solution into the cyclodextrin solution under constant stirring to obtain 2S4R β-cyclodextrin Add 200ml sorbitol solution, 0.6g sodium saccharin, 1g flavoring agent...

Embodiment 3

[0042] Prepare 1000ml of 2S4R itraconazole concentration of 3% (w / v) oral solution, which contains the following ingredients:

[0043] 2S4R Itraconazole Isomer 30g, Hydroxypropyl-β-cyclodextrin 200g, Propylene Glycol 200ml, 70% Sorbitol 200ml, Hydrochloric Acid 3.8ml, Sodium Saccharin 0.6g, Hydroxypropylcellulose 1g, Cherry Flavor Dose 1g, add distilled water to 1000ml.

[0044] Its preparation method: firstly add 1g of hydroxypropyl cellulose to 300ml of distilled water, stir to dissolve; add 3.8ml of concentrated hydrochloric acid to 200ml of propylene glycol, slightly heat and stir, add 30g of 2S4R itraconazole and stir until homogeneous. Take another container, add 200g of hydroxypropyl-β-cyclodextrin into 200ml of distilled water and stir to dissolve, then slowly add the above-mentioned 2S4R itraconazole propylene glycol acidic solution into the cyclodextrin solution under constant stirring to obtain 2S4R β-cyclodextrin Add 200ml sorbitol solution, 0.6g sodium saccharin,...

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Abstract

The invention discloses itraconazole isomer oral liquid, which comprises itraconazole, cyclodextrin or derivative of cyclodextrin and other auxiliary materials, wherein itraconazole is 2S4R itraconazole. The solubility of the 2S4R itraconazole in an aqueous medium containing hydroxypropyl-beta-cyclodextrin is much higher than that of the racemic mixture of four isomers of itraconazole, namely under the condition of medicines at the same concentration, only a small amount of hydroxypropyl-beta-cyclodextrin is required as a solubilizer, so the consumption of hydroxypropyl-beta-cyclodextrin is reduced; thus, the clinic dose and administration period of the medicine are reduced, the clinic treatment effect is enhanced, and adverse reactions are reduced. In addition, because hydroxypropyl-beta-cyclodextrin is very expensive, the reduction of dose can reduce the production cost of the preparation. In the invention, the preparation which is prepared by using 2S4R itraconazole as the active ingredient requires much less hydroxypropyl-beta-cyclodextrin than the conventional itraconazole oral liquid and is suitable to be used as an angiogenesis inhibitor to treat various tumor diseases in clinic.

Description

Technical field: [0001] The invention belongs to the field of medicine, and in particular relates to an isomer oral solution of itraconazole, which uses itraconazole isomer-2S4R itraconazole as a drug for inhibiting angiogenesis. Background technique: [0002] Itraconazole or (±)-cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazole -1-yl-methyl)-1,3-dioxan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1 -Methylpropyl)-3H-1,2,4-triazol-3-one, the structure of which is shown in formula (I), is a kind of oral, parenteral and local broad-spectrum anti Fungal compound, trade name SPORANOX. Itraconazole is a 1:1:1:1 racemic mixture of four diastereomers (two enantiomeric pairs) with three chiral centers, corresponding to 2S4R2'S, 2S4R2'R, 2R4S2'S, 2R4S2'R itraconazole, the term "2S4R itraconazole" when used hereinafter shall be interpreted broadly and include either one of the 2S4R2'S, 2S4R2'R isomers or a mixture of both free base form and pharmaceutically...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/496A61K47/40A61P43/00
Inventor 傅和亮谢永立
Owner 广州力鑫生物科技有限公司
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