Preparation and Characterization of Stable Amorphous Glassy Solution of BCS II and IV Drugs.

Autor: Dharani S; Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, TX, 77843, USA., Sediri K; Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, TX, 77843, USA.; Laboratory of Applied Chemistry, ACTR Univ. Ain Temouchent DGRCT, BP 248, 46000, Ain Temouchent, Algeria., Cook P; Eastman Chemical Company, Kingsport, TN, 37662, USA., Arunagiri R; Eastman Chemical Company, Kingsport, TN, 37662, USA., Khan MA; Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, TX, 77843, USA., Rahman Z; Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, 310 Reynolds Medical Sciences Building, College Station, TX, 77843, USA. rahman@tamu.edu.
Jazyk: angličtina
Zdroj: AAPS PharmSciTech [AAPS PharmSciTech] 2021 Dec 23; Vol. 23 (1), pp. 35. Date of Electronic Publication: 2021 Dec 23.
DOI: 10.1208/s12249-021-02198-1
Abstrakt: 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 o C (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 o C/75% RH for a week. AGSs behave like a glassy solid at room temperature and liquified above 60 o C. 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.
(© 2021. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.)
Databáze: MEDLINE
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