Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium

Lee, Junhee; Ku, Jeong; Park, Jung Soo; Park, Jong Hak; Ahn, Sik-Il; Mo, J; Kim, Yun-Tae; Rhee, John-M.; Lee, Hai-Bang; Khang, Gilson

doi:10.4333/kps.2008.38.2.111

Journal of Korean Pharmaceutical Sciences

2008

DOI: 10.4333/kps.2008.38.2.111

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Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium

Junhee Lee¹,

Jeong Ku²,

Jung Soo Park³

et al.

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2011

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Cited by 2 publications

References 15 publications

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Molecular Effect of PVP on The Release Property of Carvedilol Solid Dispersion

Oh¹,

Shim²,

Eunyong³

et al. 2011

Journal of Pharmaceutical Investigation

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This study aimed to confirm the effect of molecular weight (MW) in solid dispersion of carvedilol with polyvinylpyrrolidone (PVP) of various MW. Solid dispersion of carvedilol with PVP was prepared by spray-drying method. Scanning electron microscopy (SEM) was used to analyze the surface of solid dispersion samples. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were used to analyze the crystalline of solid dispersion. Fourier transform infrared spectroscopy (FT-IR) was used to analyze the change of chemical structure characteristic of solid dispersion. DSC and XRD show that drug crystalline was changed. FT-IR revealed that chemical structure of solid dispersion comparing the chemical structure of drug was changed. The dissolution studies of solid dispersion presented at simulated gastric juice (pH 1.2). The dissolution rate of solid dispersion was dramatically enhanced than pure drug and the MW of PVP has an effect on the release property of carvedilol in solid dispersion. In conclusion, the present study has confirmed the effect of MW of PVP on release property of solid dispersion formulation of carvedilol with PVP.

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Molecular Effect of PVP on The Release Property of Carvedilol Solid Dispersion

Oh¹,

Shim²,

Eunyong³

et al. 2011

Journal of Pharmaceutical Investigation

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Preparation and Characterization of Simvastatin Solid Dispersion using Aqueous Solvent

Kim¹,

Park²,

Choi³

et al. 2011

Journal of Pharmaceutical Investigation

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Simvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in the biosynthesis of cholesterol. Simvastatin has good permeability, but it also has low solubility (BCS class II), which reduces its bioavailability. To overcome this problem, a solid dispersion is formed using a spray-dryer with polymeric material carrier to potentially enhance the dissolution rate and extend drug absorption. As carriers for solid dispersion, Gelucire ® 44/14 and Gelucire ® 50/13 are semisolid excipients that greatly improve the bioavailability of poorly-soluble drugs. To avoid any toxic effects of an organic solvent, we used aqueous medium to melt Tween ® 80 and distilled water. The structural behaviors of the raw materials and the solid dispersion were analyzed by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). The DSC and PXRD data indicated that the crystalline structure of simvastatin was transformed to an amorphous structure through solid dispersion. Then, solid dispersion-based tablets containing 20 mg simvastatin were prepared with excipients. Dissolution tests were performed in distilled water and artificial intestinal fluid using the USP paddle II method. Compared with that of the commercial tablet (Zocor ® 20 mg), the release of simvastatin from solid dispersion based-tablet was more efficient. Although the stability study is not complete, this solid dispersion system is expected to deliver poorly water-soluble drugs with enhanced bioavailability and less toxicity.

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Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium

Cited by 2 publications

References 15 publications

Molecular Effect of PVP on The Release Property of Carvedilol Solid Dispersion

Molecular Effect of PVP on The Release Property of Carvedilol Solid Dispersion

Preparation and Characterization of Simvastatin Solid Dispersion using Aqueous Solvent

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