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KMID : 0614020060210010054
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Journal of Pharmaceutical Sciences (C.N.U.)
2006 Volume.21 No. 1 p.54 ~ p.59
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Preparation and Evaluation of solid dispersion to enhance dissolution rate of biphenyl dimethyl dicarboxylate
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Lee Jung-Woo
Kim Jeong-Soo
Lee Gye-Won
Jee Ung-Kil
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Abstract
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Biphenyl dimethyl dicarboxylate(DDB) is synthetic compound derived from Schizandrin C, a component of Fructus Schizandrae. DDB is currently employed as an agent against virally induced hepatic injury and has been found to be effective in improving liver function and symptoms of patients with chronic viral hepatitis. But, DDB is practically water-insoluble and its dissolution rate is extremely low, resulting in very low bioavailability(20-30%). To improve the dissolution rate of DDB, solid dispersion particles of DDB were prepared with two different types of hydrophilic polymers such as Eudragit E100, hydroxypropylmethylcellulose(HPMC) by spray drying method. Properties of solid dispersions were characterized by DSC and PXRD. DDB tablets were prepared by compressing the powder mixtures composed of raw DDB, solid dispersions, lactose and Avicel PH102, magnesium stearate. At ratio above 1:3(w/w), DDB was amorphous state within DDB-Eudragit E100 solid dispersion. As the weight ratio of Eudragit E100 to DDB was increased, the dissolution rate of DDB-Eudragit E100 solid dispersion tablets was reached 69.37-98.29% after 30min. But, it rapidly decreased to 28.34-45.98% after 2hour due to precipitation of DDB. However, in case of 1:3:1 DDB-Eudragit E100-HPMC solid dispersion tablet containing HPMC, dissolution rate was reached 97.47% after 2hour without decrease of dissolution rate. From overall findings, DDB formulation containing Eudargit E100 and HPMC solid dispersion could be used to remarkably improve the dissolution rate in dosage form of tablets.
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KEYWORD
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DDB, Eudragit E100, HPMC, Solid dispersion
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