Manipulation of Pharmaceutical Polymorphic Transformation Process Using Excipients

作者: Beiqian Tian , Zhiyong Ding , Shuyi Zong , Jinyue Yang , Na Wang

DOI: 10.2174/1381612826666200213122302

关键词:

摘要: BACKGROUND In the pharmaceutical field, it is vital to ensure a consistent product containing single solid-state form of active ingredient (API) in drug product. However, some APIs are suffering from risk transformation their target forms during processing, formulation and storage. METHODS The purpose this review summarize relevant category excipients demonstrate availability importance using as key strategy manipulate polymorphic transformation. RESULTS excipient effects on solvent-mediated phase transformations, transitions amorphous crystallization significant. Common including amino acids derivatives, surfactants, various polymers different manipulation were summarized discussed. CONCLUSION Appropriate use plays role manipulating process corresponding APIs, with promising application guaranteeing stability effectiveness dosage forms.

参考文章(109)
Sonja Joseph, Michael Rappolt, Martin Schoenitz, Vera Huzhalska, Wolfgang Augustin, Stephan Scholl, Heike Bunjes, Stability of the Metastable α-Polymorph in Solid Triglyceride Drug-Carrier Nanoparticles. Langmuir. ,vol. 31, pp. 6663- 6674 ,(2015) , 10.1021/ACS.LANGMUIR.5B00874
Stephen R. Byrn, Solid state chemistry of drugs ,(1982)
Paul J Sheskey, Marian E Quinn, Raymond C Rowe, Handbook of Pharmaceutical Excipients ,(1994)
Joel Bernstein, Polymorphism in Molecular Crystals ,(2020)
Ross S. Forgan, Ronald A. Smaldone, Jeremiah J. Gassensmith, Hiroyasu Furukawa, David B. Cordes, Qiaowei Li, Christopher E. Wilmer, Youssry Y. Botros, Randall Q. Snurr, Alexandra M. Z. Slawin, J. Fraser Stoddart, Nanoporous Carbohydrate Metal–Organic Frameworks Journal of the American Chemical Society. ,vol. 134, pp. 406- 417 ,(2012) , 10.1021/JA208224F
A.V. Volod’ko, V.N. Davydova, E. Chusovitin, I.V. Sorokina, M.P. Dolgikh, T.G. Tolstikova, S.A. Balagan, N.G. Galkin, I.M. Yermak, Soluble chitosan-carrageenan polyelectrolyte complexes and their gastroprotective activity. Carbohydrate Polymers. ,vol. 101, pp. 1087- 1093 ,(2014) , 10.1016/J.CARBPOL.2013.10.049
Shan-Yang Lin, Cheng-Hung Hsu, Wen-Ting Ke, Solid-state transformation of different gabapentin polymorphs upon milling and co-milling International Journal of Pharmaceutics. ,vol. 396, pp. 83- 90 ,(2010) , 10.1016/J.IJPHARM.2010.06.014
Kristīne Krūkle-Bērziņa, Andris Actiņš, The effect of excipients on the stability and phase transition rate of xylazine hydrochloride and zopiclone. Journal of Pharmaceutical and Biomedical Analysis. ,vol. 107, pp. 168- 174 ,(2015) , 10.1016/J.JPBA.2014.12.031
Andrea G. Schmidt, Siegfried Wartewig, Katharina M. Picker, Potential of carrageenans to protect drugs from polymorphic transformation. European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 56, pp. 101- 110 ,(2003) , 10.1016/S0939-6411(03)00037-7
Fang Tian, Dorothy J. Saville, Keith C. Gordon, Clare J. Strachan, J. Axel Zeitler, Niklas Sandler, Thomas Rades, The influence of various excipients on the conversion kinetics of carbamazepine polymorphs in aqueous suspension. Journal of Pharmacy and Pharmacology. ,vol. 59, pp. 193- 201 ,(2010) , 10.1211/JPP.59.2.0006