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Posaconazole hydrogel patch and preparing method thereof

A posaconazole hydrogel patch, posaconazole technology, applied in antifungal agents, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve the problems of monotonous dosage forms, difficult transportation, and difficult storage , to achieve the effect of preventing infection and preventing external infection

Inactive Publication Date: 2019-05-14
ZHENGZHOU TAIFENG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dosage form is relatively monotonous, and the oral suspension is packaged in glass, which is fragile and difficult to transport, and is greatly affected by temperature. It is easy to freeze at low temperature and difficult to store

Method used

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  • Posaconazole hydrogel patch and preparing method thereof
  • Posaconazole hydrogel patch and preparing method thereof
  • Posaconazole hydrogel patch and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Posaconazole gel patch

[0038] Posaconazole 10.0g

[0039] Carbomer-940 20.0g

[0040] Concentrated hydrochloric acid 2.0ml

[0041] Absolute ethanol 50ml

[0042] PEG-400 100.0g

[0043] Hydroxypropyl-β-cyclodextrin 300.0g

[0044] Glycerin 50.0g

[0045] Methylparaben 0.5g

[0046] Ethylparaben 0.5g

[0047] Appropriate amount of triethanolamine

[0048] 1) The preparation method is: slowly disperse the prescribed amount of carbomer into an appropriate amount of distilled water, swell, and leave overnight

[0049] 2) Add an appropriate amount of absolute ethanol and concentrated hydrochloric acid to the prescribed amount of posaconazole, and fully dissolve it. Take the prescribed amount of hydroxypropyl-β-cyclodextrin, add an appropriate amount of distilled water, dissolve it in a hot water bath, slowly add it to the medicinal solution, stir, and inclusion complex at 35°C for 24 hours to obtain a posaconazole inclusion complex solution.

[0050] 3...

Embodiment 2

[0053] Example 2 Posaconazole gel patch

[0054] Posaconazole 15.0g

[0055] Carbomer-940 25.0g

[0056] Concentrated hydrochloric acid 2.3ml

[0057] Absolute ethanol 60ml

[0058] PEG-400 150.0g

[0059] Hydroxypropyl-β-cyclodextrin 360.0g

[0060] Glycerin 55.0g

[0061] Methylparaben 0.55g

[0062] Appropriate amount of triethanolamine

[0063] 1) Slowly disperse the prescribed amount of carbomer into an appropriate amount of distilled water, swell, overnight

[0064] 2) Add an appropriate amount of absolute ethanol and concentrated hydrochloric acid to the prescribed amount of posaconazole, and fully dissolve it. Take the prescribed amount of hydroxypropyl-β-cyclodextrin, add an appropriate amount of distilled water, dissolve it in a hot water bath, slowly add it to the medicinal solution, stir, and inclusion complex at 35°C for 24 hours to obtain a posaconazole inclusion complex solution.

[0065] 3) Slowly add glycerin, PEG-400, methylparaben and ethylparaben int...

Embodiment 3

[0068] Example 3 Posaconazole gel patch

[0069] Posaconazole 15.0g

[0070] Carbomer-940 25.0g

[0071] Concentrated hydrochloric acid 2.3ml

[0072] Absolute ethanol 60ml

[0073] PEG-400 150.0g

[0074] Sulfobutyl-β-cyclodextrin 360.0g

[0075] Glycerin 55.0g

[0076] Methylparaben 0.55g

[0077] Ethylparaben 0.55g

[0078] Appropriate amount of triethanolamine

[0079] 1) Slowly disperse the prescribed amount of carbomer into an appropriate amount of distilled water, swell, overnight

[0080] 2) Add an appropriate amount of absolute ethanol and concentrated hydrochloric acid to the prescribed amount of posaconazole, and fully dissolve it. Take the prescribed amount of sulfobutyl-β-cyclodextrin, add an appropriate amount of distilled water, dissolve it in a hot water bath, slowly add it to the medicinal solution, stir, and inclusion complex at 35°C for 24 hours to obtain a posaconazole inclusion complex solution.

[0081] 3) Slowly add glycerin, PEG-400, methylpar...

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Abstract

The invention relates to a posaconazole hydrogel patch and a preparing method thereof. The patch is prepared from posaconazole, a hydrogel matrix, a humectant, a solubilizer, a preservative and a pH regulator according to the weight percentage. When the posaconazole hydrogel patch is prepared from a hydrophilic polymer material high in biocompatibility, the problem of the poor dissolubility of theposaconazole is solved; by means of the skin local dosage approach, the local medicine concentration of a medication part is increased, the adverse reaction of a medicine is reduced, the long-term medication compliance is increased, and a better medication option is provided for a patient.

Description

technical field [0001] The invention belongs to the field of posaconazole preparations, and in particular relates to a posaconazole hydrogel patch and a preparation method thereof. Background technique [0002] Invasive fungal infection is a common infectious disease, and its incidence has been increasing year by year in recent decades. Due to the poor prognosis and high mortality rate of fungal infection, there is an increasing clinical demand for new antifungal drugs. Posaconazole is a new type of triazole antifungal drug, which overcomes the problems of narrow antibacterial spectrum, low drug resistance and low bioavailability of the first and second generation drugs. The drug was developed and marketed by Schering-Plough Company of the United States, and its trade name is Noxafil. Posaconazole, a new chemical molecular entity, is the first antimicrobial drug approved by the FDA for the prevention of lesions caused by invasive Aspergillus species. It inhibits fungal ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/496A61K47/32A61P31/10
Inventor 沙薇牛莉峰李婷
Owner ZHENGZHOU TAIFENG PHARMA CO LTD
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