Del Rosso James Q, Pillai Radhakrishnan, Moore Robert
J Clin Aesthet Dermatol. 2010 Oct;3(10):26-8.
Clinicians have been reluctant to prescribe benzoyl peroxide concurrently with topical tretinoin due to a belief that the benzoyl peroxide may cause oxidation and degradation of the tretinoin molecule, thereby reducing its effectiveness. However, benzoyl peroxide-induced degradation of tretinoin may not necessarily apply to all topical tretinoin formulations.
To evaluate the potential for benzoyl peroxide-induced degradation of an optimized aqueous gel formulation of tretinoin (0.05%).
Tretinoin gel (0.05%) and benzoyl peroxide gel (6.26% premix concentration to produce 5% benzoyl peroxide in a fixed combination clindamycin product) were mixed together (1:1) at 32ºC and samples assayed after 1, 2, 3, 5, and 7 hours. Each sample was analyzed for tretinoin (expressed as % tretinoin remaining) and its degradation product content.
No loss of tretinoin was observed over the seven-hour time period. When tretinoin gel (0.05%) was combined with benzoyl peroxide, 100 percent of the initial tretinoin concentration remained after seven hours. There was no increase in the degradation products of tretinoin.
There was no benzoyl peroxide-induced degradation of tretinoin when the optimized formulation of tretinoin gel (0.05%) was admixed with benzoyl peroxide gel (6.26%). Although the direct clinical significance of these results is unknown, clinicians may feel comfortable using this particular combination concurrently without concerns about tretinoin oxidation and degradation.
临床医生一直不愿同时开具过氧化苯甲酰和外用维甲酸,因为他们认为过氧化苯甲酰可能会导致维甲酸分子氧化和降解,从而降低其疗效。然而,过氧化苯甲酰引起的维甲酸降解不一定适用于所有外用维甲酸制剂。
评估过氧化苯甲酰对优化的维甲酸水凝胶制剂(0.05%)的降解可能性。
将维甲酸凝胶(0.05%)和过氧化苯甲酰凝胶(预混浓度6.26%,在固定复方克林霉素产品中产生5%过氧化苯甲酰)在32℃下混合(1:1),并在1、2、3、5和7小时后对样品进行检测。分析每个样品中的维甲酸(以剩余维甲酸的百分比表示)及其降解产物含量。
在7小时的时间段内未观察到维甲酸损失。当维甲酸凝胶(0.05%)与过氧化苯甲酰混合时,7小时后初始维甲酸浓度的100%仍然存在。维甲酸的降解产物没有增加。
当将优化的维甲酸凝胶制剂(0.05%)与过氧化苯甲酰凝胶(6.26%)混合时,未发生过氧化苯甲酰诱导的维甲酸降解。尽管这些结果的直接临床意义尚不清楚,但临床医生在同时使用这种特定组合时可能会感到放心,而不必担心维甲酸的氧化和降解。