Topical fluorouracil vesicle gel and preparation method thereof

A technology of fluorouracil vesicle gel and vesicle gel, which is applied in the field of fluorouracil vesicle gel and its preparation, which can solve the problems of eliminating nonlinearity, large individual differences, drug retention and accumulation, and large toxic and side effects , achieve high efficiency and low toxicity to treat related skin diseases, improve drug transdermal rate and efficiency, and improve bioavailability

Active Publication Date: 2010-12-22
SUZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because only a small amount of 5-Fu can be converted into active 5-Fu deoxynucleotides and 5-Fu nucleotides in the body, most drugs are converted into dihydrofluorouracil by dihydropyrimidine dehydrogenase in the liver, while Loss of activity, so its half-life in vivo is short and bioavailability is low
In addition, its poor fat solubility makes it difficult to enter tissues and cells, which is another reason for low bioavailability
The drug has high toxic and side effects, can cause myelosuppre

Method used

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  • Topical fluorouracil vesicle gel and preparation method thereof
  • Topical fluorouracil vesicle gel and preparation method thereof
  • Topical fluorouracil vesicle gel and preparation method thereof

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Embodiment 1

[0020] 1. Preparation of drug-loaded vesicles

[0021] A. Weigh the prescribed amount of Span85, Span40, and cholesterol into a vial, add absolute ethanol, heat in a water bath at 60°C and stir magnetically (1000r / min) to dissolve completely until clarified, then add 5-Fu that has passed through an 80-mesh sieve powder, continue to stir evenly, and sonicate in a water bath at 60°C for 3 minutes to obtain an organic phase. While stirring, use a glass rod to drain and add 2.5ml of 60°C pH7.29 PBS solution to the organic phase, continue to stir for 12 minutes to evaporate ethanol, pump for 2 minutes under reduced pressure with a water pump, take a water bath for 1 minute, and then pump for 2 minutes, then stir at room temperature for 5 minutes , forming a white milky vesicle suspension. Using the same method, but without adding 5-Fu, a blank vesicle suspension without 5-Fu can be prepared.

[0022] B. Take cholesterol (25mg) and an appropriate amount of Span40 in a vial, add ...

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Abstract

The invention relates to a fluorouracil vesicle gel which is prepared by using fluorouracil, PlronicF68, Span and other surfactants, cholesterols and the like to prepare vesicle suspension in the self-assembly way, and further using carbomer and other excipients to prepare the vesicle gel, and the fluorouracil vesicle gel can be topically applied o the skin for treating various viral warts, keratosis, skin cancer, psoriasis, keloid, melanoma and other diseases. The prepared vesicle has complete shape and relatively uniform particle size distribution, and the encapsulation rate is 23.48%-51.14%. The vesicle gel has good uniformity and stable nature, and excised skin test results of rats and mice prove that the vesicle gel can significantly increase the retention of a drug in the skin and have the sustained release property, indicating that the fluorouracil vesicle gel has high utilization rate of the drug in the topical part of medication and significant sustained release effect of a drug storage library, and is conductive to reducing the systemic toxicity and side effects and improving the efficacy.

Description

technical field [0001] The invention relates to a fluorouracil vesicle gel and a preparation method thereof, which can be used as topical skin medicine to treat various diseases such as viral warts, keratosis, skin cancer, psoriasis (psoriasis), keloids and melanoma. Background technique [0002] In 1957, the successful clinical application of the pyrimidine anti-metabolite tumor chemotherapeutic drug --- 5-fluorouracil (5-Fu for short) synthesized by Duschinsky et al. 5-Fu has inhibitory effects on a variety of animal tumors, and has no cross-resistance with other commonly used anti-tumor drugs. When other antitumor drugs are used in combination, the antitumor effect of 5-Fu is definite. [0003] 5-Fu, also known as: 5-fluorouracil, bisfuridine, is a molecular formula of C 4 h 3 FN 2 o 2 , white crystal or powder with molecular weight of 130.08, chemical structure similar to uracil, odorless, slightly soluble in cold water, relatively soluble in boiling water, soluble ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/50A61K31/513A61P35/00A61P31/12A61P17/12A61P17/00A61P17/06A61P17/02
Inventor 邓安平杨红刘茂男陈华黎
Owner SUZHOU UNIV
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