磷酸川芎嗪 pH 调控长时微孔渗透泵控释片的制备

作者：Shen Huifen; Zheng Aini; Yu Nuojun; Gao Chongkai^*

来源：Drug Evaluation Research, 2019, 42(7): 1342-1349.

DOI：10.7501/j.issn.1674-6376.2019.07.015

• microporous osmotic pump controlled release tablets
• orthogonal design
• tetramethylpyrazine phosphate
• zero-level release

Objective To prepare the microporous osmotic pump controlled release tablets of Tetramethylpyrazine Phosphate for 24 hours.Methods The drug release condition in vitro was investigated by the cumulative release in different times;and its optimal prescription was revisited;the optimal prescription was selected by single factor investigation and orthogonal design.Results The significant influence factors to the cumulative release within 16 hours were found out by the single factor investigation: pH regulator (sodium citrate, sodium tartrate) dosage, polyethylene glycol-400 (PEG-400), triethyl citrate (TEC) dosage, the coating weight. Three batches of samples were prepared by pilot and amplification test according to the two optimal prescriptions. The results of the cumulative release curve fitting in vitro were in line with the zero-level model, and the fitting degree was good (r = 0.995 0), the cumulative release rate was over 85% in 16 h. The inter batch similarity factor f2 was about 84—97 with good reproducibility about 24 h.Conclusion The preparation process of this prescription is simple and effective, and the preparation of tetramethylpyrazine phosphate microporous osmotic pump tablets had obvious zero-level release characteristics within 16 h, and can achieve long-term controlled release of drugs for 24 h. ? 2019 Authors.