Microcrystalline cellulose as an effective crystal growth inhibitor for the ternary Ibrutinib formulation

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

“…In other words, it is unclear if the behavior of those five drugs in CAMS with respect to co-formability, physical stability, and dissolution behavior can be directly translated to other drugs. ents to form strong molecular interactions with basic drugs (for example in [25,[31][32][33][34][35][36][37][38][39][40][41][42][43]). The organic acids used as co-formers differ in their number of carboxylic acid groups, which was hypothesized to lead to salt formation with a basic drug at different molar ratios.…”

“…Considerations of bioactivity, structural characteristics of drug and co-former, and physicochemical properties of co-formers on the one hand and consideration of combination therapy on the other hand accounted for 18.1% and 6.8%, respectively. However, a systematic co-former screening was only performed in 21.8% of the reported studies [29,36,41,[50][51][52][53][54][55][56][57]. Therefore, systematic, predictive, and computational screening methods for co-former selections are still largely unexplored (see also a review: [27]).…”

Ternary Solid Dispersion Strategy for Solubility Enhancement of Poorly Soluble Drugs by Co-Milling Technique

“…However, in the ternary co-grinding system, no crystallization was observed and this was attributed to higher acid-base interaction between Indomethacin and SiO 2 -Mg (OH) 2 interface that promotes the formation of bridging bonds (Si-O-C or Mg-O-C) which inhibited the molecular mobility of amorphous drug. Mura et al (2003), have shown that aqueous dissolution of Naproxen (a poorly water-soluble anti-inflammatory drug) can be considerably enhanced by combination with hydroxypropylβ-cyclodextrin and some aminoacids (Arginine) [14]. Such ternary system exhibited higher stability constant and drug solubility (at pH ≈ 7and T = 25°C) than binary system (Naproxen/Arginine).…”

“…Such ternary system exhibited higher stability constant and drug solubility (at pH ≈ 7and T = 25°C) than binary system (Naproxen/Arginine). The synergetic effect in Naproxen solubility (a 13.4-fold increase compared to pure drug) can be attributed to the establishment of electrostatic interactions between Arginine and the carboxylic group of Naproxen, as well as hydrogen bond formation between Arginine and the hydroxyl groups of HPβCD [14].…”

“…In some cases, the stabilization and solubilization efficiency of binary solid dispersion is weak by exhibiting limited bioavailability enhancement [12] and required a large amount of carriers. In order to further enhance drug dissolution rate, several researchers have introduced third compound in drug formulations, this led to simultaneous enhancement of drug solubility and physical stability [13][14][15][16][17][18][19]. In this chapter, the challenges and strategies in developing robust ternary solid dispersion of high stability and performance are briefly discussed.…”