浏览全部资源
扫码关注微信
目的:基于“质量源于设计”(QbD)理念设计并优化茶碱亲水凝胶骨架缓释片(简称为“自制缓释片”)的处方工艺。方法:确定稀释剂类型、片径、黏合剂性质(即不同黏合剂种类的占比)、黏合剂用量作为关键工艺参数(CPPs),将自制缓释片与市售参比制剂溶出曲线的相似因子以及其在不同时间点的累积释放度作为关键质量属性(CQAs),采用L18(34)正交表进行设计和试验;对试验结果建立二次多项式回归模型,利用Modde 12.0软件通过最优模型进行计算并获得设计空间及其可接受范围(PAR),以确定自制缓释片的最优处方工艺,并对所得工艺进行验证试验和蒙特卡洛模拟验证。结果:获得吻合度、精确度、有效性、重现性均较好的最优模型,能较好地拟合CQAs和CPPs之间的关系;进一步计算获得设计空间及其PAR值[稀释剂最优值为乳糖;片径为9.07~9.33 mm,最优值为9.20 mm;羟丙基甲基纤维素(HPMC)K4M占HPMC总量的比例为0.50~0.83,最优值为0.80;HPMC总量为0.036 0~0.041 3g/片,最优值为0.038 7 g/片],并确定其优处方工艺为茶碱质量占比50%、HPMC K4M质量占比15.48%、HPMC K100M质量占比3.87%,其余部分使用乳糖作为稀释剂,制片后片径为9.20 mm。验证结果显示,所制备的茶碱缓释片与参比制剂具有相似的体外释放行为;模拟产生的95%以上的结果都在上、下限范围内。结论:基于QbD理念建立的茶碱缓释片处方工艺能够符合制剂设计要求,而且在PAR范围内调整CPPs所制备的产品能够符合CQAs的要求,表明QbD理念用于缓控释制剂处方工艺的设计和优化具有科学性和有效性。
OBJECTIVE: To design and optimize the formulation and technology of Theophylline hydrophilic gel matrix sustained-release tablets (self-made sustained-release tablets for short) based on the concept of “Quality by Design” (QbD). METHODS: Diluent type, tablet diameter, the property of adhesive (ratio of different adhesive types), the amount of adhesive were regarded as critical process parameters (CPPs). Similarity factor of dissolution curves of self-made Theophylline sustained-release tablets and reference preparation and its accumulative release rate at different time points were regarded as critical quality attributes (CQAs). L18(34) orthogonal tablet was adopted for design and trial, and secondary polynomial regression model was established. By using Modde 12.0 software, the design space and its acceptable range (PAR) were calculated through the optimal model. The optimal formulation and technology of Theophylline sustained-release tablets was determined, and validation test and Monte Carlo simulation verification were conducted. RESULTS: The optimal model with good coincidence, accuracy, validity and reproducibility was obtained, which could better fit the relationship between CQAs and CPPs. The design space and PAR value were obtained by further calculation (The optimum value of diluent was lactose; tablet diameter was 9.07-9.33 mm, and the optimal value was 9.20 mm; ratio of HPMC K4M to HPMC was 0.50-0.83, and the optimal value was 0.80; total amount of HPMC was 0.036 0-0.041 3 g per tablet, and the optimal value was 0.038 g per tablet). The optimal formulation and technology included that ratio of theophylline, HPMC K4M and HPMC K100M were 50%, 15.48% and 3.87%, respectively; the rest was filled with lactose and the diameter of the tablet was 9.20 mm. The results of validation confirmed that self-made Theophylline sustained-release tablets had similar in vitro release behavior compared with reference preparation. CONCLUSIONS: Based on the concept of QbD, the formulation and technology of Theophylline sustained-release tablets can meet the requirements of design, and the CPPs can be adjusted within the PAR range to meet the requirements of CQAs. This shows that the QbD concept is scientific and effective in the design and optimization of the formulation and technology of sustained and controlled release preparations.
茶碱亲水凝胶骨架缓释片质量源于设计关键质量属性关键工艺参数正交试验设计空间处方工艺优化
TheophyllineHydrophilic gel matrix sustained-release tabletsQuality by designCritical quality attributesCritical process parametersOrthogonal testDesign spaceFormulationTechnologyOptimization
0
浏览量
11
下载量
0
CSCD
关联资源
相关文章
相关作者
相关机构