目的:通过滑石粉与阿司匹林的相容性考察,探索滑石粉中酸中可溶物对制剂质量的影响情况并初步探讨了影响机制。方法:通过阿司匹林与含有不同量酸中可溶物的滑石粉之间的相容性试验,考察滑石粉酸中可溶物含量与阿司匹林降解程度之间的相关性,并对酸中可溶物中对阿司匹林降解的影响因素进行考察。结果:滑石粉酸中可溶物在一定程度上加速了阿司匹林的降解。结论:滑石粉中的强碱弱酸盐或金属氧化物如碳酸钙、碳酸镁和氧化镁等酸中可溶物的水解,导致样品微环境的pH增加,影响对pH敏感活性药物成分的稳定性。
Objective: To study the compatibility of Talc and aspirin,to explore the influence of acid soluble substance of Talc on the quality of the preparation, and the influencing mechanism. Methods: Through the compatibility test between aspirin and Talc containing acid-soluble substances in a series of concentration gradient, the correlation between the content of soluble substances in the acid of talc and the content of impurities degraded by aspirin, and the influencing factors of aspirin degradation in acid soluble substances were investigated. Results: Acid-soluble substances in Talc accelerated the degradation of aspirin in a certain extent. Conclusion: Hydrolysis of strong base and weak acid salts or metal oxides such as calcium carbonate, magnesium carbonate and magnesium oxide in talc powder leads to pH increase in the sample microenvironment and affects the stability of pH sensitive active pharmaceutical ingredient.
[1] 曹筱琛,贾飞,陶巧凤.药物与辅料相容性研究进展[J].中国现代应用药学,2013,30(2):223
CAO XC, JIA F, TAO QF.Progress in the study of drug-excipient compatibility in dosage forms[J].Chin J Mod Appl Pharm, 2013, 30(2):223
[2] 胡欣,金鹏飞.仿制药和专利药临床疗效差异的技术思考[J].中国新药杂志,2012,21(6):601
HU X, JIN PF.Technical discussion on the curative effect differences between generic drugs and proprietary drugs[J].Chin J New Drugs, 2012, 21(6):601
[3] 涂家生.药用辅料标准的制定及其意义[J].中国食品药品监管,2018(9):31
TU JS. Formulation and significance of standards for pharmaceutical excipients [J].China Food Drug Admi Mag, 2018(9):31
[4] 王念明. 滑石新型饮片的药学研究及其用于炮制辅料的适宜性研究[D].成都:成都中医药大学,2014
WANG NM. Study on Talc New Slices of Pharmacy and Its Suitability Used for Processing Adjuvants[D].Chengdu:Chengdu University of Traditional Chinese Medicine, 2014
[5] 李楠,谭裕君,王念明,等.滑石粉炒鱼鳔胶炮制工艺优选[J].中国药业,2017,26(13):5
LI N, TAN YJ, WANG NM, et al. Optimization of processing technology of stir-frying swim bladders with talcum powder[J].China Pharm, 2017, 26(13):5
[6] 谢彦兵,李海兵,肖红兵,等.复方鲜竹沥液制备工艺改进[J].解放军药学学报,2012,28(1):36
XIE YB, LI HB, XIAO HB, et al.Improvement of the technique for preparing an oral liquid of Xianzhuli compounds[J].Pharm J Chin PLA, 2012, 28(1): 36
[7] 吴赟. 阿托伐他汀钙氨氯地平双层片处方和工艺研究[D].天津:天津大学,2014
WU Y. Research on Preparation Technology of Compound Amlodipine Besylate and Atorvastatin Calcium Double-layer Tablets[D].Tianjing:Tianjin University, 2014
[8] 马英杰,逄秀娟,王思玲,等.辅料对尼莫地平固体分散体粉体学性质的影响[J].沈阳药科大学学报,2009,26(4):254
MA YJ, PANG XJ, WANG SL, et al. Effects of excipients on powder technology properties of nimodipine dispersion powders[J].J Shenyang Pharm Univ, 2009, 26(4): 254
[9] 李海兵,谢彦兵,徐晶,等.藿香正气口服液制备工艺改进[J].国际药学研究杂志,2014,41(4):490
LI HB, XIE YB, XU J, et al. Improvement of the technique to prepare oral liquid of Huoxiangzhengqi[J].J Int Pharm Res, 2014, 41(4): 490
[10] 申瑞芳. 抗粘剂滑石粉对Eudragit® NE 30D功能性控释膜的影响研究[D].郑州:河南大学,2015
SHEN RF. Influence of Talc as Anti-tacking Agents on Eudragit® NE30D Coatings[D].Zhengzhou:Henan University, 2015
[11] 中华人民共和国药典2020年版.四部[S].2020:779
ChP 2020. Vol Ⅳ[S].2020:779
[12] 中华人民共和国药典2020年版.一部[S].2020:364
ChP 2020. VolⅠ[S].2020:364
[13] USP 42-NF 37[S].2019: 2770
[14] EP 9.0[S].2016:3011
[15] BP 2019[S].2019:II-236
[16] 周林杰,王立军,陈夫山. 滑石粉的性质及其在造纸中的作用[J].西南造纸, 2005(6): 32
ZHOU LJ, WANG LJ, CHEN FS. Properties of talc and its role in papermaking [J].Southwest Pulp Paper, 2005(6): 32
[17] 中华人民共和国药典2020年版.二部[S].2020:666
ChP 2020. VolⅡ[S].2020:666
[18] [H]GPH 4-1化学药物制剂研究基本技术指导原则.[S].2005
[H]GPH 4-1 Guidelines for Research of Chemical Pharmaceutical Preparations[S].2005
[19] 高晓霞,王奖,徐爱菊,等.Ni- Co-Al混合氧化物的制备及其丙烷氧化脱氢催化性能[J].分子催化,2019,33(6):531
GAO XX, WANG J, XU AJ, et al. Preparation of Ni-Co-Al mixed oxides and their catalytic performance for oxidative dehydrogenation of propane[J].J Mol Catal, 2019, 33(6):531
[20] 罗力莎. 改性硅酸盐矿石催化臭氧氧化去除水中抗生素类污染物的研究[D].长春:吉林大学,2019
LUO LS. Study on Catalytic Ozonation of Modified Silicate Ore To Remove Antibiotic Pollutants in Water[D].Changchun:Jilin University, 2019
[21] 农以宁,吴群英.ICP-MS法测定药用滑石粉酸溶物杂质成分[J].桂林工学院学报,2005,25(2):221
NONG YN, WU QY. Impurity determination in acid-solution of medical talc powder by ICP-MS[J].J Guilin Univ Technol,2005, 25(2):221
[22] 赵雯. 阿司匹林复方双层片的质量标准、相容性、制备工艺和稳定性研究[D].贵阳:贵州大学,2017
ZHAO W. The Study of a Quality Standard, Compatibility, Preparation and Stability of Aspirin Compoound Double Layer Tablets[D].Guiyang:Guizhou University, 2017
[23] Sarab Boslaugh. 统计学及其应用[M].第二版.北京:机械工业出版社,2016:290
Sarab Boslaugh.Statistics in a Nutsbell[M].2nd Ed. Beijing: China Machine Press, 2016:290
[24] 汪芳.纵览阿司匹林发展历史[J].中国全科医学,2016,19(26):3129
WANG F. Overview on the history of asprin [J].Chin Gen Pract, 2016, 19(26):3129
[25] RAYMOND CR, PAUL JS, MARIAN Q. Handbook of Pharmaceutical Excipients [M].6th Ed. London: Pharmaceutical Press and American Pharmacists Association, 2009
