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Objective: To optimize the preparation technique for bifonazole suppositories and evaluate the quality.Methods: The appearance, hardness and melting time of suppositories were used as the evaluation indices to optimize the process conditions, such as suppository matrix, drug particle size, injection molding temperature and stirring conditions, etc.The content of bifonazole was determined by HPLC.Results: The best formula was as follows: the matrix was multiplicated monofatty glyceride-36, bifonazole was sieved by 100 mesh sieve and the best molding temperature was 45 ℃.The quality of the prepared suppositories with the above conditions was controllable in the appearance, melting time limit, hardness and content determination, etc.Conclusion: The formula of bifonazole suppositories is reasonable, the preparation process is feasible, and the quality control methods are reliable.
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OBJECTIVE:To evaluate the quality of Bifonazole Gel from different manufacturers. METHODS:HPLC was per-formed on the column of Diamonsil C18 with mobile phase of methanol- water- tetrahydrofuran(75∶24∶1,V/V/V)at a flow rate of 1.0 ml/min,detection wavelength was 254 nm,column temperature was 23 ℃,and the injection volume was 10 μl. RESULTS:The linear range of bifonazole was 50-600 μg/ml (r=0.999 9);RSDs of precision,stability and reproducibility tests were lower than 1%;recovery was 97.71%-101.68%(RSD=1.16%,n=9). The contents of Bifonazole gel samples from 3 manufacturers were more than 10 mg/g,with little difference. CONCLUSIONS:The method is simple and accurate with good separation and re-producibility,and suitable for the content determination of Bifonazole gel. The investigated contents of products from different man-ufactures conform to relevant standards.
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OBJECTIVE:To establish a method for the determination of related substances in bifonazole raw material. METH-ODS:HPLC method was performed on the column of Kromasil C18 with mobile phase of methanol-0.02 mol/L phosphoric acid(ad-justed pH to 7.5 with triethylamine)(70:30,V/V)at a flow rate of 1.0 ml/min,detection wavelength was 258 nm,volume injection was 20 μl,and the column temperature was 40 ℃. RESULTS:The linear range was 0.05-0.25 μg/ml for bifonazole(r=0.9996), 0.05-0.25 μg/ml for impurity A(bifonol)(r=0.9997)and 0.05-0.25 μg/ml for impurity B(4-C isomer)(r=0.9995);the detec-tion limits were 8.2 ng/ml,7.5 ng/ml and 8.4 ng/ml,and the quantification limits were 27.1 ng/ml,24.7 ng/ml and 27.8 ng/ml,re-spectively;RSDs of precision and reproducibility tests were lower than 1%;recovery of impurity B was 95.13%-101.29%(RSD=1.89%,n=9);both impurity A and impurity B were were detected in the 3 batches of samples. CONCLUSIONS:The method is accurate,sensitive and reproducible,and can be used for the determination of the related substances in bifonazole raw material.
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OBJECTIVE: To prepare bifonazole hollow effervescent suppository and establish its quality standard. METHODS: Bifonazole hollow effervescent suppository was prepared by hot-melting method, 38-type semisynthetic glyceride as the base material, NaHCO3 and citric acid as the effervescent agent, bifonazole as main ingredient. UV spectrophotometry was used for the content determination of bifonazole. RESULTS: The weight of prepared suppository was about 2.3 g and mean size of maximal foaming capacity were all above 8 mL. The linear range of bifonazole were 1.015～10.15 ?g?mL-1(r=0.999 9) with an average recovery of 99.74% (RSD=1.28%). CONCLUSION: The established preparation is simple, practical and up to the standard. The content determination method is precise and accurate.
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Objective To investigate the efficacy and safety of butenafine hydrochloride 1% aerosol in the treatment of tinea pedis,tinea cruris or tinea corporis.Methods A randomized,double-blind,multi-center clinical trial was conducted.Efficacy was assessed in terms of mycological cure,total clinical sign and symptom scores,and clinical response,at baseline,mid-term,end of study,and 2 weeks after treatment.Results One hundred and seventeen patients with tinea cruris or tinea corporis were randomly allocated to individual groups treated with either butenafine 1% aerosol (n = 58,male 53,female 5,age 29.45 ? 11.80,course of disease 3.0 ? 5.0 months) or bifonazole 1% aerosol (n = 59,male 49,female 10,age 34.12 ? 12.98,course of disease 3.0 ? 11.0 months).One hundred and nineteen patients with tinea pedis were also allocated to two groups treated with either butenafine (n = 59,male 59,age 22.97 ? 3.97,course of disease 24.0 ? 36.0 months) or bifonazole (n = 60,male 60,age 23.77 ? 4.12,course of disease 36.0 ? 48.0 months).The cure rates and total response rates were 25.86% vs.40.68%,and 86.21% vs.91.53%,in the study group and the control group,respectively,at the end of study,and 58.62% vs.74.58%,and 96.55% vs.96.61% in 2 weeks following-up,for the patients with tinea cruris or tinea corporis.Also,the cure rates and total response rates were 23.73% vs.25.00%,81.36% vs.78.33%,in the study group and the control group,respectively,at the end of study,and 37.29% vs.41.57% and 81.36% vs.90.00% in 2 weeks following-up,for the patients with tinea pedis.Local adverse reactions were recorded in 13 of butenafine group,and 20 of bifonazole group.The differences of above data between two groups were not statistically significant.Conclusion Butenafine hydrochloride 1% aerosol is effective and well tolerated for the treatment of tinea pedis,tinea cruris or tinea corporis.
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Objective To investigate the effects of compound bifonazole solution for the treatment of superficial mycosis.Methods The study groups were treated with compound bifonazole solution and the control group with clotrimazole solution in a double-blind controlled clinical trial.The solutions were applied to skin lesions once a day.The course of treatment was two weeks for tinea corporis and tinea cruris and four weeks for tinea manus and tinea pedis.The patients were followed up weekly for two weeks after cessation of treatment and evaluated with regard to erythema,papule,blister,scale,keratinization and pruritus.Mycologic examinations were performed before,during and right after treatment and two weeks after treatment.Results A total of434patients participated into the study.The clinical cure rates of study group were82.25%in tinea corporis and tinea cruris,and68.75%tinea manus and tinea pedis,with a total response rates of95.85%and92.5%in tinea corporis and tinea cruris,and92.5%in tinea manus and tinea pedis,respectively.The clinical cure rates of control group were58.6%in tinea corporis and tinea cruris,and44.7%in tinea manus and tinea pedis,with a total response rates of83.0%and87.2%in tinea corporis and tinea cruris,and in tinea manus and tinea pedis,respectively.The MICs to350clinical isolates of pathogenic fungi were1.6~2.5mg/L for compound bifonazole solution,and3.125~25mg/L for clotrimazole solution.Conclusions Compound bifonazole solution is a high-effective,broad-spectrum anti-fungal agent.It is keratolytic,well permeable and safe for relatively long term application.
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In this experiment,topical application of 1% Bifonazole cream or ethanol solution on guinea-pig trichopkytosis model, 0.3g or 0.3ml once a day for two weeks, showed the satisfying effoet.But topical application of 0.5%,0.1% Bifonazole cream or ethanol solution was less effective.The remaining time of Bifonazole on the skin was about 72 hours.During interval, it would protect the guinea-pigs from mycotic infection
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Bifonazole is a new imidazolyl derivative, with broad spectrum anlimycotic activity. In our experiment, 100 strains of common dermatophytes in clinical practice were used to evaluate the MIC of Bifonazole. All the species tested, were sensitive to this agent, and the MIC values of 79% of strains were under 4g/ml. The MIC value was influenced by inoculum size, the larger the inoculum size, the larger the MIC value. It was found that the efficacy of Bifonazole is comparable to Mico-nazole