期刊
AAPS PHARMSCITECH
卷 23, 期 1, 页码 -出版社
SPRINGER
DOI: 10.1208/s12249-021-02198-1
关键词
Amorphous glassy solution; Sucrose acetate isobutyrate; Stability; Powder X-ray diffraction; Crystalline; Amorphous
资金
- Eastman Chemical Company, Kingsport, TN
This study focused on developing amorphous glassy solutions (AGSs) of BCS Class II and IV drugs using sucrose acetate isobutyrate (SAIB) and analyzing their properties through NIR, NIR-H, and XRPD. The results showed that these solutions behaved like glassy solids at room temperature and liquified at higher temperatures, demonstrating stability and high solubility.
The focus of the present investigation was to develop amorphous glassy solutions (AGSs) of BCS Class II and IV drugs using sucrose acetate isobutyrate (SAIB). The drugs studied were rifaximin (RFX), dasatinib (DST), aripiprazole (APZ), dolutegravir (DLT), cyclosporine (CYS), itraconazole (ITZ), tacrolimus (TAC), sirolimus (SRL), aprepitant (APT), and carbamazepine (CBZ). AGSs were prepared by dissolving known quantity of the drug in the SAIB at 120 (TAC and APZ), 140 (CYS) or 150 C-o (RFX, DST, DLT, ITZ, SRL, APT, and CBZ). They were characterized visually and by NIR, NIR hyperspectroscopy (NIR-H), and XRPD. Stability were determined by exposing open vials to 40 C-o/75% RH for a week. AGSs behave like a glassy solid at room temperature and liquified above 60 C-o. The solubility of APT, DLT, SRL, APZ, RFX, CBZ, TAC and CYS in SAIB was 0.4 +/- 0.0, 1.7 +/- 0.4, 1.9 +/- 0.0, 21.6 +/- 2.6, 36.4 +/- 0.9, 76.5 +/- 4.0, 115.1 +/- 2.3, and 239.0 +/- 12.6 mg/g, respectively. NIR, NIR-H, and XRPD data indicated the amorphous nature of the AGSs. Furthermore, AGSs were stable against devitrification on exposure to high temperature and humidity. In summary, SAIB can be employed to develop stable AGSs of poorly soluble drugs to increase dissolution, and oral bioavailability with the addition of hydrophilic excipients.
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