Improvement of photostability and dissolution profile of isradipine using inclusion complex

• Published in: Journal of pharmaceutical investigation 2013, 43(1), , pp.55-61
• Main Authors: Park, Jun-Bom, Lee, Gun-Hee, Kang, Ji-Won, Jeon, Ik-Sung, Kim, Jung-Mi, Kim, Ki-Beom, Kang, Chin-Yang
• Format: Article
• Language: English
• Subjects: Biomedical and Life Sciences; Biomedicine; Research Article; 약학
• ISSN: 2093-5552; 2093-6214
• DOI: 10.1007/s40005-013-0052-9

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.