硫酸米诺地尔外用泡腾片的研制及其皮肤渗透性研究

Development of Topical Minoxidil Sulfate Effervescent Tablets and Investigation of Their Skin Permeation

关键词:  硫酸米诺地尔  外用泡腾片  处方工艺  质量评价  皮肤渗透性  

Key words:  minoxidil sulfate  topical effervescent tablets  formulation technology  quality evaluation  skin permeability  

摘要:

目的 研制一种新型硫酸米诺地尔外用泡腾片制剂（TMSET），并进行质量评价及皮肤渗透性研究。方法 采用粉末直接压片技术制备TMSET；在单因素试验的基础上采用正交试验优化TMSET处方工艺；通过外观性状、重量差异、崩解时限及含量测定对TMSET进行质量评价；采用Franz扩散池法对TMSET进行皮肤渗透性研究。结果 本研究成功制备了TMSET，其最优处方组成为：硫酸米诺地尔（MXS）66.67%、碳酸氢钠-酒石酸（2:1）15%、甘露醇16.33%、羟丙甲纤维素（HPMC）2%。制备得到的TMSET外观完整光洁，色泽均匀，重量差异小，崩解时限为52.89±4.37 s，每片平均含量为321.0±3.8 mg。皮肤渗透实验结果表明，TMSET的24 h单位面积累积渗透量为1306.13μg/cm2与米诺地尔酊剂相当，其角质层药物滞留量为60.10±24.33μg/cm2，较米诺地尔溶液剂提高了3.9倍。结论 本研究所研制的TMSET质量稳定，且具有良好的皮肤渗透性能，为脱发治疗提供了新的剂型选择。

Abstract:

OBJECTIVE Development and preparation of a novel topical minoxidil sulfate effervescent tablet (TMSET) formulation, with subsequent quality evaluation and dermal penetration study. METHODS The direct powder compression technique was employed for the preparation of TMSET.;the formulation process was optimized by orthogonal design based on single-factor testing;Quality evaluation of TMSET was conducted through assessment of appearance characteristics, weight variation, disintegration time limit, and drug assay; Dermal penetration studies were performed using the Franz diffusion cell method. RESULTS This study successfully prepared TMSET. The optimized formulation composition was: minoxidil sulfate (MXS) 66.67%, sodium bicarbonate-tartaric acid (2:1) 15%, mannitol 16.33%, and hydroxypropyl methylcellulose (HPMC) 2%. The resulting TMSET exhibited an intact and smooth-surfaced appearance with uniform coloration, minimal weight variation, a disintegration time of 52.89±4.37 s, and an average drug content of 321.0±3.8 mg per tablet. Skin permeation studies demonstrated that the 24 hour cumulative amount permeated per unit area for TMSET was 1306.13 μg/cm2, comparable to that of minoxidil tincture. Furthermore, the amount of drug retained in the stratum corneum was 60.10±24.33 μg/cm2, representing a 3.9 fold increase compared to minoxidil solution. CONCLUSION The TMSET developed in this study exhibits stable quality attributes and demonstrates favorable dermal permeation performance, providing a novel dosage form option for alopecia management.