A Systematic Approach to Design and Prepare Solid Dispersions of Poorly Water-Soluble Drug

Abstract

The objective of the present study was to define a systematic approach to design and prepare solid dispersions of poorly water-soluble drug. The systematic approach can be defined in four phases. In the first phase, glass forming ability is assessed, and in the second phase, probable excipients are screened. The screened excipients are evaluated (third phase) for glass transition temperatures (Tg) and miscibility studies according to Florey-Huggins interaction parameter. The predicted excipients are used to prepare the solid dispersion and evaluated for Tg and any interactions using Fourier transfer infrared studies (fourth phase), and the findings are correlated with phase three predictions. For this investigation, cilostazol (CIL) was selected as model drug, which was classified as a poor glass former. As per the physical chemical properties of CIL, ten excipients, both polymeric and non-polymeric, were selected and screened. Out of these, povidone, copovidone, hypromellose and Eudragit EPO were found theoretically miscible with CIL. After going through phase 2 to phase 4, only povidone, copovidone and hypromellose were confirmed as polymer of choice for preparing the solid dispersion of CIL with a prediction of better physical solid-state stability on the basis of good miscibility between drug and carrier.

Wetting Kinetics: an Alternative Approach Towards Understanding the Enhanced Dissolution Rate for Amorphous Solid Dispersion of a Poorly Soluble Drug

“…As per these evaluations, it was concluded that the sample of CIL received was crystalline, polymorphic form A (30,31,34). The purity for CIL was 99.3%.…”

Effervescence Assisted Fusion Technique to Enhance the Solubility of Drugs

“…Quickly water soluble carrier dissolved rapidly and exposes the drug particles with increased surface area and augments the rate of dissolution. Selection of a carrier is an important step for preparing solid dispersion since the physical stability of the dispersion depends on the miscibility of drug with carrier matrix (5).…”

Physicochemical properties of tadalafil solid dispersions – Impact of polymer on the apparent solubility and dissolution rate of tadalafil

“…In our previous study the amorphous 95 form of Td was obtained using several commercially available 96 amorphization techniques [25]. As a result of its relatively high 97 glass transition point (T g ), which is 147°C, Td can be considered 98 as a good glass former in conjunction with its melting point (T m ) 99 at 302°C, with the T g /T m ratio equal to 0.73 [22]. However, Td on 100 its own showed poor physical stability upon contact with water 101 and crystallized immediately, resulting in a quick return to ther-102 modynamic solubility.…”