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 journalArticle

39 Citations (Scopus)

Abstract

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
Volume441
Issue number1-2
DOIs
Publication statusPublished - 2013 Jan 30

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Solubility
Water
Pharmaceutical Preparations
Polymers
Povidone
telmisartan
Particle Size
Biological Availability
Gels
Weights and Measures

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Park, Junsung ; Cho, Wonkyung ; Cha, Kwang Ho ; Ahn, Junhyun ; Han, Kang ; Hwang, Sung Joo. / Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process. In: International Journal of Pharmaceutics. 2013 ; Vol. 441, No. 1-2. pp. 50-55.
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Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process. / Park, Junsung; Cho, Wonkyung; Cha, Kwang Ho; Ahn, Junhyun; Han, Kang; Hwang, Sung Joo.

In: International Journal of Pharmaceutics, Vol. 441, No. 1-2, 30.01.2013, p. 50-55.

Research output: Contribution to journalArticle

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