黄芩苷微囊片的制备

Preparation of baicalin microcapsule tablets

目的 制备黄芩苷微囊并对其处方工艺进行优化;将微囊压制成片剂使其具有缓释作用。方法 采用单凝聚法制备微囊,以包封率和载药量为评价指标,星点设计响应面试验优化微囊处方工艺;通过单因素试验,以硬度、外观和崩解时间为指标,确定乳糖和微晶纤维素用量,得到片剂的最优处方工艺。结果 微囊最优处方工艺为温度45℃,pH 3.9,转速550 r·min^(-1)制得的微囊分散性好,载药量为(22.80±0.33)%、包封率为(82.40±0.45)%;当黄芩苷微囊50 mg,乳糖855 mg和微晶纤维素345 mg,采用粉末直接压片法制得的片剂成型性好,崩解时限6 min,24 h释放达到87.2%。结论 该处方工艺简单,稳定可行,粉末直接压片法能够得到成型性好的片剂,具有一定的缓释作用。

Objective To prepare baicalin microcapsules and optimize the formulation process,to compress the microcapsules into tablets with a sustained release effect.Methods The microcapsules were prepared by single coacervation method,and the encapsulation efficiency and drug loading were used as evaluation indicators.The central composite design and response surface methodology was used to optimize the microcapsule formulation process.The single factor test,hardness,appearance and disintegration time were used as indicators to determine the lactose and the dosage of microcrystalline cellulose to obtain the optimal formulation technology for the tablets.Results The optimal formulation process for microcapsules temperature was 45℃,pH 3.9,and rotation speed at 550 r·min^(-1).The prepared microcapsules had good dispersibility,the drug loading was(22.80±0.33)%,the encapsulation efficiency was(82.40±0.45)%,the baicalin microcapsules was 50 mg,lactose was 855 mg and microcrystalline cellulose was 345 mg.The tablets obtained by the powder direct compression method had good formability.The disintegration time limit was 6 min,and the release reached 87.2%in 24 h.Conclusion The formulation process is simple,stable and feasible.The tablets with good formability can be obtained by direct powder compression method,which has a slow release effect.