“消痘灵”口崩片的处方优化及内外合治药效研究

Preparation and Internal and External Pharmacodynamic Study of Oral Disintegration Tablets of″Xiaodouling″

目的:筛选“消痘灵”口崩片的处方及制备工艺,并进行内外合治药效学及抑菌能力的考察。方法:以片剂外观、硬度、脆碎度、崩解时间作综合评价指标,选取药粉用量、崩解剂用量、微粉硅胶和硬脂酸镁用量比为考察因素,采用Box-Behnken响应面法优化口崩片的制备工艺,同时考察口崩片不同给药方法对小鼠皮脂腺斑组织的作用及不同致病菌抑菌能力的影响。结果:最优处方制备工艺为药粉量20%,崩解剂用量20%、微粉硅胶和硬脂酸镁用量为4∶1。以此处方制备口崩片的硬度为4~7 kg,崩解时间为50 s左右,脆碎度为0.98左右。小鼠皮脂腺斑组织苏木素-伊红(HE)染色结果表明,“消痘灵”口崩片内外合治组小鼠皮脂腺相较于阳性组和内治组萎缩更加明显,消痘效果更佳。抑菌结果显示,“消痘灵”口崩片水溶液对4种致病菌的最低抑菌浓度(MIC)依此次为25.0、50.0、12.5、25.0 mg·mL^(-1),最小杀菌浓度(MBC)分别为112.5、150.0、112.5、125.0 mg·mL^(-1)。结论:该口崩片处方工艺可行、操作简便,可使皮脂腺发生萎缩,在一定程度上控制皮脂分泌,且口崩片内外合治组效果更优,同时也对痤疮致病菌有明显的抑菌和杀菌效果。

Objective:To select the prescription and optimized preparation process of“Xiaoxieling”orally disintegrating tablets,and investigate the pharmacodynamics of internal and external treatment.Methods:The appearance,hardness,friability and disintegration time of the tablets were used as comprehensive evaluation indexes.The dosage of the powder,the dosage of disintegrant and the ratio of silica gel and magnesium stearate were taken as the investigation factors.The Box-Behnken response surface method was used to optimize the orally disintegrating tablets,and to investigate the effect of orally disintegrating tablets on sebaceous gland plaque tissue in mice and antibacterial ability of different pathogens.Results:The optimal prescription preparation process powder amount was 20%,the disintegrant dosage was 20%,and the micro powder silica gel and magnesium stearate dosage ratio was 4∶1.The hardness of the orally disintegrating tablet prepared by this prescription is 4-7 kg,the disintegration time is about 50 s,and the friability is about 0.98.The HE staining results of mouse sebaceous gland plaque showed that the sebaceous glands of the Internal and external combined governance group of″Xiaopiling″orally-dissolving tablets were significantly atrophied compared with the positive and internal groups.The bacteriostatic results showed that the minimal inhibitory concentration(MICs)of the″Xiaoxiaoling″orally disintegrating tablet solution on the four pathogenic bacteria were 25.0,50.0,12.5,25.0 mg·mL^(-1),and minimum bactericidal concentration(MBC)were:112.5,150.0,112.5,125.0 mg·mL^(-1).Conclusion:The prescription of the orally disintegrating tablet is feasible and easy to operate,the internal and external treatment group can cause the sebaceous gland to shrink and control sebum secretion to a certain extent and has obvious antibacterial and bactericidal effects on acne pathogens.