Enhanced oral bioavailability of novel mucoadhesive pellets containing valsartan prepared by a dry powder-coating technique
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Enhanced oral bioavailability of novel mucoadhesive pellets containing valsartan prepared by a dry powder-coating technique. / Cao, Qing-Ri; Liu, Yan; Xu, Wei-Juan; Lee, Beom-Jin; Yang, Mingshi; Cui, Jing-Hao.
In: International Journal of Pharmaceutics, Vol. 434, No. 1-2, 09.2012, p. 325-33.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Enhanced oral bioavailability of novel mucoadhesive pellets containing valsartan prepared by a dry powder-coating technique
AU - Cao, Qing-Ri
AU - Liu, Yan
AU - Xu, Wei-Juan
AU - Lee, Beom-Jin
AU - Yang, Mingshi
AU - Cui, Jing-Hao
N1 - Copyright © 2012 Elsevier B.V. All rights reserved.
PY - 2012/9
Y1 - 2012/9
N2 - The aim of this study was to develop novel mucoadhesive pellets containing valsartan (VAL) with enhanced oral bioavailability. Two types of VAL loaded core pellets were prepared by an extrusion/spheronization method, and further dry-coated with a mixture of hydroxypropylmethylcellulose (HPMC) and carbomer (CB) at different ratios. The effects of the pellet core composition, HPMC:CB ratio and coating level on the drug release from the coated pellets were investigated. The physicochemical properties of the core and coated pellets were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). In addition, the in vitro and in vivo mucoadhesion properties as well as the bioavailability of the coated pellets in rats were evaluated by using VAL suspension and core pellets as control preparations. The results of the release study demonstrated that the two types of core pellets, especially the pellets formulated with a solubilizer and a pH modulator gave considerably faster drug release than the VAL powder. However, the core and coated pellets exhibited similar release profiles indicating that the dry powder-coating did not retard the drug release. Strong molecular interactions were observed between the drug and the carriers in FT-IR analysis. The coated pellets displayed distinct mucoadhesive property in vitro and delayed gastrointestinal (GI) transit in vivo. Furthermore, the coated pellets exhibit significantly higher AUC(0-12h) and C(max), as compared to the core pellets and drug suspension. It was concluded that the mucoadhesive pellets could render poorly water soluble drugs like VAL with a rapid drug release, delayed GI transit and enhanced oral bioavailability.
AB - The aim of this study was to develop novel mucoadhesive pellets containing valsartan (VAL) with enhanced oral bioavailability. Two types of VAL loaded core pellets were prepared by an extrusion/spheronization method, and further dry-coated with a mixture of hydroxypropylmethylcellulose (HPMC) and carbomer (CB) at different ratios. The effects of the pellet core composition, HPMC:CB ratio and coating level on the drug release from the coated pellets were investigated. The physicochemical properties of the core and coated pellets were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). In addition, the in vitro and in vivo mucoadhesion properties as well as the bioavailability of the coated pellets in rats were evaluated by using VAL suspension and core pellets as control preparations. The results of the release study demonstrated that the two types of core pellets, especially the pellets formulated with a solubilizer and a pH modulator gave considerably faster drug release than the VAL powder. However, the core and coated pellets exhibited similar release profiles indicating that the dry powder-coating did not retard the drug release. Strong molecular interactions were observed between the drug and the carriers in FT-IR analysis. The coated pellets displayed distinct mucoadhesive property in vitro and delayed gastrointestinal (GI) transit in vivo. Furthermore, the coated pellets exhibit significantly higher AUC(0-12h) and C(max), as compared to the core pellets and drug suspension. It was concluded that the mucoadhesive pellets could render poorly water soluble drugs like VAL with a rapid drug release, delayed GI transit and enhanced oral bioavailability.
KW - Acrylic Resins
KW - Adhesiveness
KW - Administration, Oral
KW - Angiotensin II Type 1 Receptor Blockers
KW - Animals
KW - Area Under Curve
KW - Biological Availability
KW - Chemistry, Pharmaceutical
KW - Drug Compounding
KW - Drug Delivery Systems
KW - Excipients
KW - Gastrointestinal Transit
KW - Male
KW - Methylcellulose
KW - Powders
KW - Rats
KW - Rats, Sprague-Dawley
KW - Solubility
KW - Spectroscopy, Fourier Transform Infrared
KW - Tetrazoles
KW - Valine
U2 - 10.1016/j.ijpharm.2012.05.076
DO - 10.1016/j.ijpharm.2012.05.076
M3 - Journal article
C2 - 22688251
VL - 434
SP - 325
EP - 333
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1-2
ER -
ID: 44056742