Tags

Type your tag names separated by a space and hit enter

In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier.
Drug Dev Ind Pharm. 2012 Nov; 38(11):1371-80.DD

Abstract

In order to improve the dissolution and absorption of the water insoluble drug repaglinide, a solid dispersion was developed by solvent method using polyvinylpyrrolidone K30 (PVP K30) as the hydrophilic carrier for the first time. Studies indicated that both solubility and the dissolution rate of repaglinide were significantly increased in the solid dispersion system compared with that of repaglinide raw material or physical mixtures. The repaglinide solid dispersions with PVP K30 solid state was characterized by polarizing microscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). DSC and XRD studies indicated that repaglinide existed in an amorphous form in the solid dispersion. FT-IR analysis demonstrated the presence of intermolecular hydrogen bonding between repaglinide and PVP K30 in the solid dispersion. In the in situ gastrointestinal perfusion experiment, solid dispersion was shown to remarkably enhance the absorption of repaglinide in stomach and all segments of intestine. In vivo pharmacokinetic study in rats showed that immediate and complete release of repaglinide from the solid dispersion resulted in rapid absorption that significantly increased the bioavailability and the maximum plasma concentration over repaglinide raw material. These results demonstrated PVP K30 was an appropriate carrier for solid dispersion of repaglinide, with increased dissolution and oral absorption.

Authors+Show Affiliations

School of Pharmacy, China Pharmaceutical University, Nanjing, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22296267

Citation

Yin, Li-Fang, et al. "In Vitro and in Vivo Studies On a Novel Solid Dispersion of Repaglinide Using Polyvinylpyrrolidone as the Carrier." Drug Development and Industrial Pharmacy, vol. 38, no. 11, 2012, pp. 1371-80.
Yin LF, Huang SJ, Zhu CL, et al. In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier. Drug Dev Ind Pharm. 2012;38(11):1371-80.
Yin, L. F., Huang, S. J., Zhu, C. L., Zhang, S. H., Zhang, Q., Chen, X. J., & Liu, Q. W. (2012). In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier. Drug Development and Industrial Pharmacy, 38(11), 1371-80.
Yin LF, et al. In Vitro and in Vivo Studies On a Novel Solid Dispersion of Repaglinide Using Polyvinylpyrrolidone as the Carrier. Drug Dev Ind Pharm. 2012;38(11):1371-80. PubMed PMID: 22296267.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier. AU - Yin,Li-Fang, AU - Huang,Shi-Jing, AU - Zhu,Chun-Li, AU - Zhang,Shu-Hui, AU - Zhang,Qiang, AU - Chen,Xi-Jing, AU - Liu,Qing-Wang, Y1 - 2012/02/02/ PY - 2012/2/3/entrez PY - 2012/2/3/pubmed PY - 2013/2/12/medline SP - 1371 EP - 80 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 38 IS - 11 N2 - In order to improve the dissolution and absorption of the water insoluble drug repaglinide, a solid dispersion was developed by solvent method using polyvinylpyrrolidone K30 (PVP K30) as the hydrophilic carrier for the first time. Studies indicated that both solubility and the dissolution rate of repaglinide were significantly increased in the solid dispersion system compared with that of repaglinide raw material or physical mixtures. The repaglinide solid dispersions with PVP K30 solid state was characterized by polarizing microscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). DSC and XRD studies indicated that repaglinide existed in an amorphous form in the solid dispersion. FT-IR analysis demonstrated the presence of intermolecular hydrogen bonding between repaglinide and PVP K30 in the solid dispersion. In the in situ gastrointestinal perfusion experiment, solid dispersion was shown to remarkably enhance the absorption of repaglinide in stomach and all segments of intestine. In vivo pharmacokinetic study in rats showed that immediate and complete release of repaglinide from the solid dispersion resulted in rapid absorption that significantly increased the bioavailability and the maximum plasma concentration over repaglinide raw material. These results demonstrated PVP K30 was an appropriate carrier for solid dispersion of repaglinide, with increased dissolution and oral absorption. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/22296267/In_vitro_and_in_vivo_studies_on_a_novel_solid_dispersion_of_repaglinide_using_polyvinylpyrrolidone_as_the_carrier_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2011.652635 DB - PRIME DP - Unbound Medicine ER -