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
. 2018 Nov;13(6):546-554.
doi: 10.1016/j.ajps.2018.08.010. Epub 2018 Oct 12.

Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique

Wenxiang Dong  1 , Xitong Su  1 , Meng Xu  1 , Mingming Hu  1 , Yinghua Sun  1 , Peng Zhang  1
Affiliations

Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique

Wenxiang Dong et al. Asian J Pharm Sci. 2018 Nov.

Abstract

Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. Moreover, all these studies suggested the conversion of crystalline atorvastatin calcium. In addition, the drug solubility studies as well as dissolution rates compared with bulk drug and market tablets Lipitor were also examined. Furthermore, the study investigated the pharmacokinetics after oral administration of Lipitor and solid dispersion. And the AUC0-8 h and Cmax increased after taking ATC-P188 solid dispersion orally compared with that of Lipitor. All these could be demonstrated that ATC-P188 solid dispersions would be prospective means for enhancing higher oral bioavailability of ATC.

Keywords: Atorvastatin calcium; Dissolution rate; Oral bioavailability; Poloxamer 188; Solid dispersion.

PubMed Disclaimer

Conflict of interest statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

Figures

Image, graphical abstract
Graphical abstract
Fig. 1.
Fig. 1
Dissolution profiles of different weight ratios (1:1, 1:3, 1:5, 1:8) of drug: P188. Each value represents the mean ± SD (n = 3).
Fig. 2.
Fig. 2
Dissolution profiles of different medium pH 1.0 (A), pH 4.5 (B), water (C) and pH 6.8 (D) of bulk drug, solid dispersion and Lipitor. Each value represents the mean ± SD (n = 3).
Fig. 3.
Fig. 3
Solubility of bulk drug, physical mixture-bulk drug: P188 = 1:5 and solid dispersion in dissolution medium.
Fig. 4.
Fig. 4
FTIR spectrum of physical mixture-bulk drug: P188 = 1:5, solid dispersion, P188, ATC.
Fig. 5.
Fig. 5
Powder X-ray diffraction patterns of physical mixture-bulk drug: P188 = 1:5, solid dispersion, P188, ATC.
Fig. 6.
Fig. 6
Differential scanning calorimetry of physical mixture-bulk drug: P188 = 1:5 (A), solid dispersion, P188, ATC.
Fig. 7.
Fig. 7
SEM images of P188 (A), solid dispersion (B), ATC (C) and physical mixture-bulk drug: P188 = 1:5 (D).
Fig. 8.
Fig. 8
Mean plasma concentration − time curves of ATC in rats after oral administration of Lipitor and solid dispersion at a dose of 25 mg/kg AC (mean ± SD, n = 5).
See this image and copyright information in PMC

References

    1. Desager JP, Horsmans Y. Clinical pharmacokinetics of 3-hydroxy-3-methylglutaryl-coenzyme: a reductase inhibitors. Clin Pharmacokinet. 1993;31(5):348–371. - PubMed
    1. Jahangiri A, Jalali MB, Garjani A. Evaluation of physicochemical properties and in vivo efficiency of atorvastatin calcium/ezetimibe solid dispersions. Eur J Pharm Sci. 2016;82(72):21–30. - PubMed
    1. Yin YM, Cui FE, Kim JS. Preparation, characterization and in vitro intestinal absorption of a dry emulsion formulation containing atorvastatin calcium. Drug Deliv. 2009;16(1):30–36. - PubMed
    1. Shete G, Puri V, Kumar L, Bansal AK. Solid state characterization of commercial crystalline and amorphous atorvastatin calcium samples. AAPS PharmSciTech. 2010;11(2):598–609. - PMC - PubMed
    1. Palanisamy M, James A, Khanam J. Atorvastatin ecyclodextrin systems: Physiochemical and biopharmaceutical evaluation. J Drug Deliv Sci Technol. 2016;31:41–52.