Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process

Junsung Park, Wonkyung Cho, Kwang Ho Cha, Junhyun Ahn, Kang Han, Sung Joo Hwang

Research output: Contribution to journalArticlepeer-review

57 Citations (Scopus)


Telmisartan is a biopharmaceutical classification system (BCS) class II drug that has extremely low water solubility but is freely soluble in highly alkalized solutions. Few organic solvents can dissolve telmisartan. This solubility problem is the main obstacle achieving the desired bioavailability. Because of its unique characteristics, the supercritical anti-solvent (SAS) process was used to BCS class II drug in a variety of ways including micronization, amorphization and solid dispersion. Solid dispersions were prepared using hydroxypropylmethylcellulose/polyvinylpyrrolidone (HPMC/PVP) at 1:0.5, 1:1, and 1:2 weight ratios of drug to polymer, and pure telmisartan was also treated using the SAS process. Processed samples were characterized for morphology, particle size, crystallinity, solubility, dissolution rate and polymorphic stability. After the SAS process, all samples were converted to the amorphous form and were confirmed to be hundreds nm in size. Solubility and dissolution rate were increased compared to the raw material. Solubility tended to increase with increases in the amount of polymer used. However, unlike the solubility results, the dissolution rate decreased with increases in polymer concentration due to gel layer formation of the polymer. Processed pure telmisartan showed the best drug release even though it had lower solubility compared to other solid dispersions; however, because there were no stabilizers in processed pure telmisartan, it recrystallized after 1 month under severe conditions, while the other solid dispersion samples remained amorphous form. We conclude that after controlling the formulation of solid dispersion, the SAS process could be a promising approach for improving the solubility and dissolution rate of telmisartan.

Original languageEnglish
Pages (from-to)50-55
Number of pages6
JournalInternational Journal of Pharmaceutics
Issue number1-2
Publication statusPublished - 2013 Jan 30

Bibliographical note

Funding Information:
This work was supported by the Yonsei University Research Fund of 2011.

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science


Dive into the research topics of 'Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process'. Together they form a unique fingerprint.

Cite this