Charge-assisted intermolecular hydrogen bond formed in coamorphous system is important to relieve the pH-dependent solubility behavior of lurasidone hydrochloride

Abstract

In comparison to amorphous LH, coamorphous LH-REP without evidence of intermolecular hydrogen bond, exhibited greatly improved solubility with pH-dependent behavior, significantly enhanced dissolution rate and physical stability.

A novel drug–drug coamorphous system without molecular interactions: improve the physicochemical properties of tadalafil and repaglinide

“…The endothermic peaks at 303.2 C and 132.2 C were attributed to the melting peak of the recrystallized tadalal and repaglinide, which agreed with their reported values. 19,50 Similarly, only a single value of T g at 73.1 C was observed for coamorphous system (Fig. 3A(f)), together with its PXRD halo (Fig.…”

“…7b). 62 In comparison to crystalline form, the 13 C NMR spectra of amorphous tadalal and repaglinide showed slight changes in chemical shis with signicantly broadening lines and resonances merging due to the conformational distribution aer amorphization (Fig. 7d and e).…”

“…Supersaturated dissolution testing (six replicates) was conducted using a small-volume dissolution apparatus (RC-806 dissolution tester, TDTF Technology Co., Ltd, China) by a paddle method. 19 In brief, the dissolution studies were performed in 150 mL dissolution medium (water, 0.2 M PBS 6.8, respectively) with a rotation speed of 100 rpm at 37 C. Aer adding the tested powders (crystalline tadalal, crystalline repaglinide, physical mixture or coamorphous system) into the dissolution medium, 3 mL samples were withdrawn and ltered at predetermined time points (5,10,15,30,60,120,180,240,360, and 480 min) and the same amount of fresh medium was added immediately. The concentrations of tadalal and repaglinide were determined by the above HPLC/UV method aer appropriate dilution.…”

“…3A(a and b)), respectively, which were consistent with previously reported values. 19,51 The physical mixture showed only one single melting point at 131.5 C (Fig. 3A(c)) when the heating rate was 10 C min À1 .…”

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

“…Whilst this review will focus on the physical stability of CAMS, the chemical stability can be of interest, especially when using ball milling, which has been shown to be able to induce degradation. The reader is referred to several studies, which have investigated the chemical stability (either after preparation or after storage) [ 18 , 20 , 21 , 33 , 34 , 47 , 87 , 98 , 102 , 120 , 121 , 122 , 123 , 124 , 125 , 126 ].…”