Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2016 Spring;15(2):385-94.

In-Vitro Characterization and Oral Bioavailability of Organic Solvent-free Solid Dispersions Containing Telmisartan

Yue Cao  1 , Li-Li Shi  1 , Qing-Ri Cao  1 , Mingshi Yang  2 , Jing-Hao Cui  1
Affiliations

In-Vitro Characterization and Oral Bioavailability of Organic Solvent-free Solid Dispersions Containing Telmisartan

Yue Cao et al. Iran J Pharm Res. 2016 Spring.

Abstract

Poorly water-soluble drugs often suffer from limited or irreproducible clinical response due to their low solubility and dissolution rate. In this study, organic solvent-free solid dispersions (OSF-SDs) containing telmisartan (TEL) were prepared using polyvinylpyrrolidone K30 (PVP K30) and polyethylene glycol 6000 (PEG 6000) as hydrophilic polymers, sodium hydroxide (NaOH) as an alkalizer, and poloxamer 188 as a surfactant by a lyophilization method. In-vitro dissolution rate and physicochemical properties of the OSF-SDs were characterized using the USP I basket method, differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and fourier transform-infrared (FT-IR) spectroscopy. In addition, the oral bioavailability of OSF-SDs in rats was evaluated by using TEL bulk powder as a reference. The dissolution rates of the OSF-SDs were significantly enhanced as compared to TEL bulk powder. The results from DSC, XRD showed that TEL was molecularly dispersed in the OSF-SDs as an amorphous form. The FT-IR results suggested that intermolecular hydrogen bonding had formed between TEL and its carriers. The OSF-SDs exhibited significantly higher AUC0-24 h and Cmax, but similar Tmax as compared to the reference. This study demonstrated that OSF-SDs can be a promising method to enhance the dissolution rate and oral bioavailability of TEL.

Keywords: In-vitro characterization; Oral bioavailability; Organic Solvent-free; Solid dispersions; Telmisartan.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Scanning electron microscopy images of (A) OSF-SD2 (PVP K30 + Poloxamer 188) and (B) OSF-SD4 (PEG 6000 + Poloxmamer 188). Magnifications are shown for each sample 100×.
Figure 2
Figure 2
DSC thermograms of TEL (A), PVP K30 (B), PEG 6000 (C), NaOH (D), poloxamer 188 (E), OSF-SDs [OSF-SD1 (F), OSF-SD2 (G), OSF-SD3 (H), OSF-SD4 (I)] and their physical mixtures [PM1 (J), PM2 (K), PM3 (L), PM4 (M)].
Figure 3
Figure 3
XRD patterns of TEL (A), PVP K30 (B), PEG 6000 (C), NaOH (D), poloxamer 188 (E), OSF-SDs [OSF-SD1 (F), OSF-SD2 (G), OSF-SD3 (H), OSF-SD4 (I)] and their physical mixtures [PM1 (J), PM2 (K), PM3 (L), PM4 (M)].
Figure 4
Figure 4
FT-IR spectra of TEL (A), PVP K30 (B), PEG 6000 (C), NaOH (D), poloxamer 188 (E) and OSF-SDs [OSF-SD1 (F), OSF-SD2 (G), OSF-SD3 (H) and OSF-SD4 (I)].
Figure 5
Figure 5
Dissolution profiles of TEL bulk powder and OSF-SDs in pH6.8 buffer solution (mean ±SD, n=3).
Figure 6
Figure 6
Dissolution profiles of OSF SD4 in different pH media (mean ±SD, n=3).
Figure 7
Figure 7
Plasma concentration-time profiles of TEL following a single oral administration of its bulk powder and ODF-SD4 in rats (mean ±SD, n=6).
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

References

    1. Kumar AS, Ghosh S, Mehta GN. Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010;25:1–5. - PMC - PubMed
    1. Wienen W, Entzeroth M, van Meel JCA, Stangier J, Busch U, Ebner T, Schmid J, Lehmann H, Matzek K, Kempthorne-Rawson J, Gladigau V, Hauel NH. A review on telmisartan: A novel, long-acting angiotensin II-receptor antagonist. Cardiovasc Drug Rev. 2000;18:127–154.
    1. Castro SG, Bruni SS, Lanusse CE, Allemandi DA, Palma SD. Improved albendazole dissolution rate in pluronic 188 solid dispersions. AAPS PharmSciTech. 2010;11:1518–1524. - PMC - PubMed
    1. Tran PHL, Tran HTT, Lee BJ. Modulation of microenvironmental pH and crystallinity of ionizable TEL using alkalizers in solid dispersions for controlled release. J Control Rel. 2008;129:59–65. - PubMed
    1. Van den Mooter G, Augustijns P, Blaton N, Kinget R. Physico-chemical characterization of solid dispersions of temazepam with polyethylene glycol 6000 and PVP K30. Int J Pharm. 1998;164:67–80.

LinkOut - more resources