Topical fluorouracil vesicle gel and preparation method thereof

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 ...

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 myelosuppression and hemorrhagic enteritis, and eliminates non-linearity in the body, with large individual differences.

And need continuous intravenous medication, poor patient compliance, thus limiting the application of 5-Fu

The 2010 edition of the Chinese Pharmacopoeia contains 5-Fu cream, but its drug release rate is fast, and it is less stored in the skin, so it is difficult to maintain the effective concentration, resulting in high frequency of medication

However, the drug cannot accumulate in the skin

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