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Itraconazole oral solution and preparation method thereof

A technology for oral administration and oral solution of itraconazole, which is applied in the directions of pharmaceutical formulations, non-active components of polymer compounds, antifungal agents, etc., can solve the problems of salty taste of oral solution, low bioavailability of capsules, strong side effects and the like, To achieve the effect of improving medication compliance, good taste and stable quality

Inactive Publication Date: 2012-09-19
NANJING TEFENG PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Itraconazole is a triazole antifungal drug, and its dosage forms include oral solution, injection, and capsule, and the bioavailability of capsules in oral preparations is low
At present, there are limited manufacturers of itraconazole in the domestic market, and its dosage forms are mainly capsules and injections. There is no manufacturer of oral solutions. Traconazole oral solution, its formula is: itraconazole 1.5g / 150ml, hydroxypropyl-β-cyclodextrin 40%, application of orange essence, its oral solution tastes salty and astringent, poor mouthfeel, hydroxypropyl-β-cyclodextrin The amount of β-cyclodextrin is large, it has strong side effects, and the cost is high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Itraconazole 1.5kg

[0033] Hydroxypropyl-β-cyclodextrin 45kg

[0034] 1,2-Propanediol 30L

[0035] Sorbitol 9kg

[0036] Sodium saccharin 30g

[0037] Red fruit essence 0.1Kg

[0038] Prepared as 150L oral solution.

[0039] The preparation method of aforementioned itraconazole oral solution comprises the following steps:

[0040] Stir the aqueous solution of hydroxypropyl-β-cyclodextrin and 1,2-propanediol in a water bath at 40°C evenly, add itraconazole while stirring, add hydrochloric acid (1mol / L) dropwise until itraconazole is completely dissolved, continue Mechanically stir in a water bath for about 1.5 hours, add sorbitol, sodium saccharin and an appropriate amount of red fruit essence, mix well, adjust the pH to 1.50 with sodium hydroxide and hydrochloric acid after cooling down, and set the volume to 150L. At this time, a transparent and clear solution is obtained. Bottle 150ml, sterilized, this is the itraconazole oral solution product of the present in...

Embodiment 2

[0042] Itraconazole 1.0kg

[0043] Hydroxypropyl-β-cyclodextrin 30kg

[0044] 1,2-Propanediol 40L

[0045] Sorbitol 10kg

[0046] Sodium saccharin 35g

[0047] Red fruit essence 0.07Kg

[0048] Prepared as 150L oral solution

[0049] The specific operation steps are as in Example 1, the temperature of the water bath is 50° C., and the pH is adjusted to 1.80.

Embodiment 3

[0051] Itraconazole 1.5kg

[0052] Hydroxypropyl-β-cyclodextrin 60kg

[0053] 1,2-Propanediol 50L

[0054] Sorbitol 10kg

[0055] Sodium saccharin 25g

[0056] Red fruit essence 0.11Kg

[0057] Prepared as 150L oral solution

[0058] The specific operation steps are as in Example 1, wherein the temperature of the water bath is 60° C., and the pH is 2.00.

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PUM

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Abstract

The invention relates to an oral solution of an antifungal medicine, and a preparation method for the oral solution. An itraconazole oral solution consists of slightly soluble bulk pharmaceutical itraconazole, hydroxypropyl-beta-cyclodextrin, preservative and additive. 150 milliliters of the itraconazole oral solution contains 1.0 to 2.0g of itraconazole, 30.0 to 60.0g of hydroxypropyl-beta-cyclodextrin, 30 to 60ml of 1,2-propylene glycol, preservative sorbierite, saccharin sodium and essence additive. The problem of low dissolubility of the itraconazole is solved; a product has the advantages of simple process, low cost, small side effect, convenience in taking, high bioavailability and the like and has an obvious effect on fungus infection; and an oral solution preparation has an obvious curative effect on monilial infection in oral cavity / esophagus.

Description

technical field [0001] The invention relates to an oral preparation for treating fungal infection, in particular to a poorly water-soluble oral solution for anti-fungal infection and its preparation. Background technique [0002] Itraconazole is (±)-cis-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-tri Azol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-( 1-Methylpropyl]-3H-1,2,4-triazol-3-one, is a broad-spectrum antifungal compound for oral, parenteral and topical use in the treatment of systemic fungal infections including mycosis, cryptococcal meningitis, histoplasmosis, gynecologic vulvovaginal candidiasis, dermatological / ophthalmic tinea versicolor, dermatophytosis, fungal keratitis and oral candidiasis with dermatophytes and / or or yeast-induced onychomycosis, disclosed in US-4,267,179. Itraconazole is a weakly basic drug with a pKa value of 3.7, which is only dissociated at low pH values ​​(such as in gastric acid), so gastric ac...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/496A61K47/40A61P31/10
Inventor 陶亮钱晓敏李华锋温天文孙柏旺刘实李述斌罗俊赵千肖建民云琦徐智勇朱怀柏夏秋月邢华训
Owner NANJING TEFENG PHARMA
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