Rational selection of formulation components to improve dissolution of Dipyridamole

• Published in: Journal of drug delivery science and technology 2020-02, Vol.55, p.101467, Article 101467
• Main Authors: Maghsoodi, Maryam, Nokhodchi, Ali, Babi, Hadi Izadi
• Format: Article
• Language: English
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2019.101467

The aim of the current study was firstly to identify polymers which effectively inhibit precipitation of Dipyridamole (DP), a poorly water-soluble basic drug, in neutral solution. Secondly, to test the viability of formulation approaches where a component is used to enhance the dissolution of DP at a neutral solution, while another component is added to inhibit its precipitation. The effectiveness of some Eudragit polymers in inhibition of DP precipitation was evaluated. Solid dispersion technology using enteric polymer, Eudragit L 100-55 (Eu L100-55), or pH-modifier technology employing an appropriate acidifier, Tartaric acid (Tar), were used to enhance the dissolution of DP in neutral solution, while an effective polymer, was added to inhibit the DP precipitation. FT-IR, differential scanning calorimetry and dissolution testing were used to characterize the formulations. The results indicated that Eudragit E (Eu E) inhibited DP precipitation the most, probably owing to interaction with DP, as verified by FT-IR. Dissolution results revealed that addition of Eu E to Eu L100-55-based formulations led to an inconsiderable improvement in dissolution rate of DP. But, the inclusion of Eu E into Tar-based formulations exhibited not only stability to precipitation but also higher maximum achievable concentration level of DP, demonstrating more efficiency in offering dissolution benefits in comparison to the predicted dissolution performances which only account for additive influences. Results demonstrated that the choice of suitable components with the capacity to act complementary to each other, is vital to the success of the strategy formulation of this work. [Display omitted]