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AAPS PharmSciTech

, Volume 19, Issue 7, pp 2990–2999 | Cite as

Tablet Formulation of a Polymeric Solid Dispersion Containing Amorphous Alkalinized Telmisartan

  • Jun Soo Chae
  • Bo Ram Chae
  • Dong Jun Shin
  • Yoon Tae Goo
  • Eun Seok Lee
  • Ho Yub Yoon
  • Chang Hyun Kim
  • Young Wook Choi
Research Article
  • 94 Downloads

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.

KEY WORDS

telmisartan alkalizer amorphous form solid dispersion dissolution 

Notes

Funding Information

This research was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2016R1A2B4011449). This work also supported in part by the Korea Health Industry Development Institute (KHIDI) funded by the Ministry of Health and Welfare, Republic of Korea (HI17C0710), and the Advanced Technology Center program (10051950) funded by the Ministry of Trade, Industry and Energy (MI, Korea).

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Jun Soo Chae
    • 1
  • Bo Ram Chae
    • 1
  • Dong Jun Shin
    • 1
  • Yoon Tae Goo
    • 1
  • Eun Seok Lee
    • 1
  • Ho Yub Yoon
    • 1
  • Chang Hyun Kim
    • 1
  • Young Wook Choi
    • 1
  1. 1.College of PharmacyChung-Ang UniversitySeoulRepublic of Korea

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