Tablet Formulation of a Polymeric Solid Dispersion Containing Amorphous Alkalinized Telmisartan
- Authors
- Chae, J.S.; Chae, B.R.; Shin, D.J.; Goo, Y.T.; Lee, E.S.; Yoon, H.Y.; Kim, C.H.; Choi, Y.W.
- Issue Date
- Oct-2018
- Publisher
- Springer New York LLC
- Keywords
- telmisartan; alkalizer; amorphous form; solid dispersion; dissolution
- Citation
- AAPS PharmSciTech, v.19, no.7, pp 2990 - 2999
- Pages
- 10
- Journal Title
- AAPS PharmSciTech
- Volume
- 19
- Number
- 7
- Start Page
- 2990
- End Page
- 2999
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/3425
- DOI
- 10.1208/s12249-018-1124-y
- ISSN
- 1530-9932
1522-1059
- Abstract
- To overcome the poor dissolution of telmisartan (TMS) at weak acidic pH, amorphous alkalinized TMS (AAT) was prepared by introducing sodium hydroxide as a selective alkalizer. AAT-containing polymeric solid dispersions were prepared by a solvent evaporation method; these solid dispersions were AAT-PEG, AAT-PVP, AAT-POL, and AAT-SOL for the polymers of PEG 6000, PVP K30, Poloxamer 407, and Soluplus, respectively. The characteristics of the different formulations were observed by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. To compare the supersaturation behavior, a dissolution test was performed at 37 ± 0.5 °C either in 900 ml (plain condition) or 500 ml (limited condition) of pH 6.8-simulated intestinal fluid used as a medium. AAT-SOL exhibited enhanced dissolution, indicating the probability of extended supersaturation in the limited condition. AAT-SOL was further formulated into a tablet by introducing other excipients, Vivapur 105 and Croscarmellose, as a binder and superdisintegrant, respectively, using a direct compression method. The selected AAT-SOL tablet was superior to Micardis (the reference product) in the aspect of supersaturation maintenance during dissolution in the limited condition, suggesting that it is a promising candidate for practical development that can replace the commercial product in the future. © 2018, American Association of Pharmaceutical Scientists.
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