(M1030-10-57) A Solution that Improves the Poor Soluble API Dissolution by Using Porous Calcium Silicate FLORITE^®

Purpose: The unique porous calcium silicate FLORITE^® has large internal cavities in particles and is already used in liquid absorbing and carrying. In this study, we investigated the availability of FLORITE^® to enhance dissolution improvement as new API carrier of solid dispersion technology for poor soluble APIs.

Methods: In this study, we selected powder formed FLORITE^® R and granule formed FLORITE^® PS-200 from our product line. For reference silicon dioxide was picked up as a comparison material. The intermediate with API and carrier materials was prepared on two methods: dry mixing (PM) and wet mixing (SD). The dissolution property of the intermediates was analyzed using a dissolution tester, NTR-8400A (TOYAMA SANGYO CO., LTD.) with water as the test solution.

Results: In the case of PM, Indomethacin crystals were observed as existing in separate with all materials by SEM pictures, the materials were observed individually without the crystals in case of SD. However, small Indomethacin crystals when examining the surface of materials. In the SD using silicon dioxide, Indomethacin was progressed amorphization in results of XRD analysis, but a part of Indomethacin was detected as different crystalline form from the original in the case of FLORITE^®s. From the results, intermediates made from wet mixing were considered as solid dispersion, FLORITE^®s made Indomethacin hybrid form of crystalline and amorphas but silicon dioxide basically did amorphas form. Indomethacin showed the lowest dissolution rate of less than 5% after 120 min. testing as well-known as poor soluble substance in water. In the case of SD using FLORITE^®s, the dissolution rate reached about 90% after 15 minutes. On the other hand, silicon dioxide slightly improved. In the case of PM using FLORITE^®s also showed an improvement in dissolution rate, although it was lower than SD.

Conclusion: It was suggested that FLORITE^® may further improve the dissolution properties of poor soluble APIs due to its solid dispersion preparation, when compared to the existing porous material, such as silicon dioxide.

Acknowledgements: There are no conflicts of interest to disclose.

Fig. 1 Results of XRD analysis in wet mixing with FLORITEs.

Fig. 2 Results of XRD analysis in wet mixing with silicon dioxide.

Fig. 3 Results of dissolution study with solid dispersion materials from wet mixing preparation.