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Improvement of photostability and dissolution profile of isradipine using inclusion complex

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Abstract

Inclusion complexes using β-cyclodextrin were manufactured by solvent evaporation method. Then, sustained release (SR) hydroxypropylmethylcellulose (HPMC) matrix tablets containing inclusion complex were prepared via direct compression. Isradipine was chosen as a model drug due to its low solubility, photo-instability and short elimination half-life. The physicochemical properties of the inclusion complexes were examined using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The solubility test and dissolution behaviours were also investigated. Based on the solubility experiments, a 1:2 molar ratio (isradipine:β-Cyclodextrin) was best and chosen to prepare inclusion complexes. In addition, the crystal structure of isradipine was converted to an amorphous structure, as confirmed by Fourier transform infrared spectroscopy (FT-IR) and DSC. The photostability of isradipine in the inclusion complex was more stable than pure isradipine after 4 days radiation. By using hypromellose as the hydrophilic sustained release material, the dissolution rate was retarded during 24 h. A combined method of inclusion complex and SR technology showed increased and sustained release profile above that of Dynacirc® SR Cap. 5 mg.

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Authors and Affiliations

  1. College of Pharmacy, Sahm Yook University, Seoul, Korea

    Jun-Bom Park, Gun-Hee Lee, Ji-Won Kang, Ik-Sung Jeon, Jung-Mi Kim, Ki-Beom Kim & Chin-Yang Kang

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  1. Jun-Bom Park
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  2. Gun-Hee Lee
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  3. Ji-Won Kang
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  4. Ik-Sung Jeon
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  5. Jung-Mi Kim
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  6. Ki-Beom Kim
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  7. Chin-Yang Kang
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Correspondence to Jun-Bom Park.

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Park, JB., Lee, GH., Kang, JW. et al. Improvement of photostability and dissolution profile of isradipine using inclusion complex. Journal of Pharmaceutical Investigation 43, 55–61 (2013). https://doi.org/10.1007/s40005-013-0052-9

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  • DOI: https://doi.org/10.1007/s40005-013-0052-9

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