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Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes.
Int J Pharm. 2012 Jan 17; 422(1-2):202-10.IJ

Abstract

With the aim of developing a novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes, various valsartan-loaded solid dispersions were prepared with water, hydroxypropyl methylcellulose (HPMC) and sodium lauryl sulphate (SLS). Effects of the weight ratios of SLS/HPMC and carrier/drug on both the aqueous solubility of valsartan and the drug-release profiles of solid dispersions were investigated. The physicochemical properties of solid dispersions were characterized using scanning electron microscope (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The bioavailability of the solid dispersions in rats was evaluated compared to valsartan powder and a commercial product (Diovan). Unlike the conventional solid dispersion system, the valsartan-loaded solid dispersion had a relatively rough surface and did not change the crystalline form of the drug. It was suggested that the solid dispersions were formed by attaching hydrophilic carriers to the surface of the drug, thus changing from a hydrophobic to a hydrophilic form without changing the crystalline form. The drug-loaded solid dispersion composed of valsartan/HPMC/SLS at a weight ratio of 3/1.5/0.75 improved the drug solubility by about 43-fold. It gave a higher AUC, C(max) and shorter T(max) compared to valsartan powder and the commercial product. The solid dispersion improved the bioavailability of the drug in rats by about 2.2 and 1.7-fold in comparison with valsartan powder and the commercial product, respectively. Thus, the valsartan-loaded solid dispersion would be useful for delivering poorly water-soluble valsartan with enhanced bioavailability and no crystalline changes.

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Authors+Show Affiliations

Yan YD
College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Kyungsan, Kyungbuk 712-749, South Korea.
Sung JH
No affiliation info available
Kim KK
No affiliation info available
Kim DW
No affiliation info available
Kim JO
No affiliation info available
Lee BJ
No affiliation info available
Yong CS
No affiliation info available
Choi HG
No affiliation info available

MeSH

Angiotensin II Type 1 Receptor BlockersAnimalsBiological AvailabilityCalorimetry, Differential ScanningChemistry, PharmaceuticalCrystallizationCrystallography, X-RayDrug CarriersDrug CompoundingHydrophobic and Hydrophilic InteractionsHypromellose DerivativesMaleMethylcelluloseMicroscopy, Electron, ScanningPowdersRatsRats, Sprague-DawleySodium Dodecyl SulfateSolubilitySurface PropertiesTechnology, PharmaceuticalTetrazolesValineValsartanWater

Pub Type(s)

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

Language

eng

PubMed ID

22085435

Citation

Yan, Yi-Dong, et al. "Novel Valsartan-loaded Solid Dispersion With Enhanced Bioavailability and No Crystalline Changes." International Journal of Pharmaceutics, vol. 422, no. 1-2, 2012, pp. 202-10.
Yan YD, Sung JH, Kim KK, et al. Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes. Int J Pharm. 2012;422(1-2):202-10.
Yan, Y. D., Sung, J. H., Kim, K. K., Kim, D. W., Kim, J. O., Lee, B. J., Yong, C. S., & Choi, H. G. (2012). Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes. International Journal of Pharmaceutics, 422(1-2), 202-10. https://doi.org/10.1016/j.ijpharm.2011.10.053
Yan YD, et al. Novel Valsartan-loaded Solid Dispersion With Enhanced Bioavailability and No Crystalline Changes. Int J Pharm. 2012 Jan 17;422(1-2):202-10. PubMed PMID: 22085435.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes. AU - Yan,Yi-Dong, AU - Sung,Jun Ho, AU - Kim,Kun Kook, AU - Kim,Dong Wuk, AU - Kim,Jong Oh, AU - Lee,Beom-Jin, AU - Yong,Chul Soon, AU - Choi,Han-Gon, Y1 - 2011/11/06/ PY - 2011/09/23/received PY - 2011/10/11/revised PY - 2011/10/28/accepted PY - 2011/11/17/entrez PY - 2011/11/17/pubmed PY - 2012/4/28/medline SP - 202 EP - 10 JF - International journal of pharmaceutics JO - Int J Pharm VL - 422 IS - 1-2 N2 - With the aim of developing a novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes, various valsartan-loaded solid dispersions were prepared with water, hydroxypropyl methylcellulose (HPMC) and sodium lauryl sulphate (SLS). Effects of the weight ratios of SLS/HPMC and carrier/drug on both the aqueous solubility of valsartan and the drug-release profiles of solid dispersions were investigated. The physicochemical properties of solid dispersions were characterized using scanning electron microscope (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The bioavailability of the solid dispersions in rats was evaluated compared to valsartan powder and a commercial product (Diovan). Unlike the conventional solid dispersion system, the valsartan-loaded solid dispersion had a relatively rough surface and did not change the crystalline form of the drug. It was suggested that the solid dispersions were formed by attaching hydrophilic carriers to the surface of the drug, thus changing from a hydrophobic to a hydrophilic form without changing the crystalline form. The drug-loaded solid dispersion composed of valsartan/HPMC/SLS at a weight ratio of 3/1.5/0.75 improved the drug solubility by about 43-fold. It gave a higher AUC, C(max) and shorter T(max) compared to valsartan powder and the commercial product. The solid dispersion improved the bioavailability of the drug in rats by about 2.2 and 1.7-fold in comparison with valsartan powder and the commercial product, respectively. Thus, the valsartan-loaded solid dispersion would be useful for delivering poorly water-soluble valsartan with enhanced bioavailability and no crystalline changes. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/22085435/Novel_valsartan_loaded_solid_dispersion_with_enhanced_bioavailability_and_no_crystalline_changes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(11)01032-5 DB - PRIME DP - Unbound Medicine ER -