NAftifine Hydrochloride Cream (common name in English name: Naftifine Hydrochloride; chemical name: (E)-N-Cinna myl-N-methyl (1-naphthylmethyl) amine hydrochloride) is a kind of antifungal drug for propylamines, which Bactericidal against sensitive dermatophytes such as Trichophyton, Microsporum and Epidermophyton, and bacteriostatic against Candida and yeast. The drug’s mechanism of action may be to interfere with fungal sterol biosynthesis by inhibiting squalene monooxygenase, resulting in a decrease in the number of sterols in cells and the accumulation of squalene (an enzyme substrate), resulting in the production of fungal lipids Metabolic disorders play a role.
NAftifine Hydrochloride Cream Properties:
Melting point
172-175°C
storage temp.
Keep in dark place,Inert atmosphere,2-8°C
solubility
ethanol: soluble50mg/mL
Merck
14,6355
CAS DataBase Reference
65473-14-5(CAS DataBase Reference)
NAftifine Hydrochloride Cream Uses
NAftifine Hydrochloride Cream As antibiotics and antifungal drugs, it has broad antibacterial spectrum and strong effect; good curative effect and fast onset of action; high safety and tolerance. For the treatment of skin and its appendages [hair, finger (toe) nails] dermatophyte infections caused by Trichophyton, Microsporum and Epidermophyton, superficial candidiasis, onychomycosis, pityriasis versicolor, Indications include rubbing mycosis under the breast, between the fingers (toes), between the buttocks and the groin. This product has the characteristics of broad antifungal spectrum and low toxicity.
NAftifine Hydrochloride Cream of Action and Dosage of Naftifine Hydrochloride
The concentration of naftifine in the superficial skin layer within 24 hours of a single dose is sufficient to inhibit the growth of dermatophytes. Naftifine can be converted into at least three metabolites in vivo through benzene and naphthalene epoxidation and N-dealkylation. About 40% to 60% of the drug in the body is excreted in the urine in the form of prototype and metabolites, and the rest is excreted in the feces through bile. The half-life of naftifine for topical skin application is about 2 to 3 days.
The mechanism of action of NAftifine Hydrochloride Cream is to inhibit the fungal squalene epoxidase, interfere with the biosynthesis of ergosterol in the fungal cell wall, affect the lipid metabolism of the fungus, and cause the fungal cell damage or death to play a bactericidal and bacteriostatic effect. . It is suitable for skin fungal diseases caused by sensitive fungi such as tinea corporis, tinea pedis, tinea capitis, onychomycosis, tinea versicolor, superficial candidiasis and rubbing mycosis of skin folds. When 1% NAftifine Hydrochloride Cream ointment is applied externally to the skin of healthy people, about 3% to 6% of the dose is absorbed.
NAftifine Hydrochloride Cream can be used externally. For skin infection, it is generally applied once a day, and gently rubbed. It should be applied to the skin within 2.5cm of the surrounding area. For rubbing fungal diseases, gauze strips containing this product can be disposed of in the crease at night. Duration of treatment Chemicalbook: skin fungal infection is 2 to 4 weeks, which can be increased to 8 weeks in severe cases; 4 weeks for superficial candidiasis; 6 months for onychomycosis; 2 weeks for pityriasis versicolor. To prevent recurrence, continue treatment for about 2 weeks after all signs of infection have disappeared.
The Preparation Method of NAftifine Hydrochloride Cream
The prep work approach of NAftifine Hydrochloride Cream provided by the invention makes up the following steps that are performed in order: ( 1) N-methyl-1-naphthylmethylamine hydrochloride as resources and also the organic ether solvent as response solvent are mixed in proportion; (2) in above-mentioned mixed solution, add alkali metal carbonate and catalyst PEG-600, react 1-4h under the temperature of 30 ℃-100 ℃, by N-methyl-1-naphthylmethylamine hydrochloride Free as N-methyl-1-naphthylmethylamine; (3) in above-mentioned reaction solution, drip cinnamyl chloride, the time for adding is 1-10h, carry out condensation reaction, then continue to react 4-10h to react completely, make naftifine solution; ( 4) prior naftifine solution is filtered, then in the filtrate, drip the ethyl acetate saturated service of hydrogen chloride to acquire naftifine hydrochloride unrefined item; ( 5) prior naftifine hydrochloride crude item adopts ethyl acetate as well as methanol mixed solvent to perform recrystallization and can make explained naftifine hydrochloride. The organic ether solvent in the explained action (1) is ether, methyl tert-butyl ether, methyl isobutyl ether, isopropyl ether, anisole, tributyl methyl ether, tetrahydrofuran, dioxane. In the explained step (2 ), the alkali steel carbonate is among sodium carbonate as well as potassium carbonate, and also the usage is 1.5-3 matchings of N-methyl-1-naphthylmethylamine hydrochloride. In the defined action (2 ), the intake of PEG-600 is 0.05-0.5 matching of N-methyl-1-naphthylmethylamine hydrochloride. In the defined action (3 ), the usage of cinnamyl chloride is 1.0-2.0 matching of N-methyl-1-naphthylmethylamine hydrochloride. In the defined step (4 ), the usage of hydrogen chloride in the saturated ethyl acetate solution is 1-1.5 matchings of N-methyl-1-naphthylmethylamine hydrochloride. In the described action (5 ), the quantity ratio of ethyl acetate and also methanol is 1: 0.5-2.0. Above-mentioned reaction steps are as complies with:
The prep work technique of naftifine hydrochloride supplied by the invention has the adhering to advantages: 1. The raw material N-methyl-1-naphthylmethylamine hydrochloride is not purified by free, but reacts with alkali metal carbonate under the action of a catalyst, which is freed by alkalization, and directly participates in further condensation reaction, which simplifies the operation process; 2. The organic ether solvent replaces the toluene, acetonitrile, etc. reported in the literature as the reaction solvent. The test results show that the reaction is complete, the impurities are less, and the generated impurities are easily removed in the post-processing process, thus helping to obtain high-quality products ; 3. after the reaction finishes, the post-processing operation process is simple, and the organic solvent saturated solution of hydrogen chloride is directly added dropwise after the filtration to obtain the naftifine hydrochloride crude product with high yield and better quality; 4. Cleanse naftifine hydrochloride crude product by recrystallization technique to get naftifine hydrochloride item with high return as well as excellent quality, the recrystallization return can get to more than 80%, and the item material can reach more than 98% (HPLC normalized Law);. 5. The prep work approach has the advantages of easy operation procedure, high return, inexpensive, and also very easy industrialization.
The Specific Embodiment of NAftifine Hydrochloride Cream
In the 2L four-necked flask equipped with thermometer and mechanical stirring, add 1.2L methyl tert-butyl ether, add 74.2g (0.36mol) N-methylnaphthylmethylamine hydrochloride, 123.7g ( 0.90mol) anhydrous potassium carbonate and 60g (0.1mol) PEG-600, liquid temperature is heated to reflux, stirring reaction 1h, then begins to drip the cinnamyl chloride of 60g (0.39 mol), leaks in 4-6h After the enhancement was finished, the response was remained to be stirred for 8 h under reflux conditions, and also the response was complied with by TLC up until N-methyl-1-naphthylmethylamine went away, and also the response was finished. option (mass web content has to do with 8%) of 200ml hydrogen chloride under mixing, mix Eventually, up until a white strong was precipitated, the dropwise addition was completed for about 0.5 h.Then ice-water bath cooling, keeping liquid temperature less than 5 DEG C, stirring 1h, filtering, filter cake is washed with 50ml ethyl acetate, obtains white solid state naftifine hydrochloride crude product, wet weight is about 100g. Recrystallization with 200ml mixed solvent (ethyl acetate: methanol=1: 1 (V: V)), drying to obtain 86.2g of white powdery naftifine hydrochloride product, melting point: 180.1°C-180.3°C , yield: 74.0%, content is 98% (HPLC normalization method), this step can effectively remove impurities, and the recrystallization yield is high, thus the NAftifine Hydrochloride Cream product quality obtained is good.
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The production base is located in Zhangqiu chemical industry park and Tai’an high-tech chemical industry park. laboratory and workshop in strict accordance with the GMP standard and the product fit national ISO9001 and ISO2000 standards.
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