Salt Engineering of Aripiprazole with Polycarboxylic Acids to Improve Physicochemical Properties

Afrooz, Hamideh; Mohamed, Eman M.; Ali, Sogra F. Barakh; Dharani, Sathish; Nutan, Mohammad T. H.; Khan, Mansoor A.; Rahman, Ziyaur

doi:10.1208/s12249-020-01875-x

Cited by 5 publications

(3 citation statements)

References 45 publications

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“…A ZRS-8G dissolution tester (Tianda Tianfa Technology Co., Ltd., Tianjin, China) was used to measure the in vitro dissolution of APZ-HCs based on a paddle method. Since APZ is weakly basic, the test was carried out in 500 mL of pH 1.2 HBS and pH 4.5 ABS at a rotation speed of 60 rpm, respectively. , APZ-HCs were suspended in water to a concentration of 5 mg/mL before the test. The suspensions (4 mL) were directly added to the dissolution medium.…”

Section: Methodsmentioning

confidence: 99%

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Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Man

Yang

et al. 2023

Mol. Pharmaceutics

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In vitro dissolution that predicts the in vivo performance of solid preparations is extremely important in formulation optimization. Fraction absorbed (F a ) has been used to screen in vitro dissolution protocols based on the idea of in vitro−in vivo correlation (IVIVC) but failed to increase the success rate due to the inaccuracy of the F a . The essence of IVIVC is the correlation between in vitro dissolution and in vivo dissolution. We tried to establish in vitro dissolution protocol via similarity with in vivo dissolution using aripiprazole (APZ) as a model drug. Hybrid APZ crystals (APZ-HCs) were prepared by physically embedding aggregation-caused quenching (ACQ) fluorophores inside the lattice to measure the in vivo dissolution. The process did not change the physicochemical properties and crystallinity of APZ. The fluorophore illuminated APZ crystals but was quenched upon dissolution of APZ-HCs in aqueous media, enabling monitoring intact APZ-HCs in real-time. The good correlation between fluorescent quenching and dissolution of APZ-HCs justified reliable quantification of intact APZ crystals. The residual percentage of fluorescence intensity in rats treated by APZ-HCs was recorded with time, which was converted to in vivo dissolution by the difference from 100%. The in vivo dissolution was validated with the F a . The in vitro dissolution profile of APZ was set up via a similarity factor larger than 50 in comparison with the in vivo dissolution. The study provides a novel idea and method to establish in vitro dissolution protocol.

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Section: Methodsmentioning

confidence: 99%

“…Since APZ is weakly basic, the test was carried out in 500 mL of pH 1.2 HBS and pH 4.5 ABS at a rotation speed of 60 rpm, respectively. 45,46 APZ-HCs were suspended in water to a concentration of 5 mg/mL before the test. The suspensions (4 mL) were directly added to the dissolution medium.…”

Section: Fluorescence Stability Of Apz-hcsmentioning

confidence: 99%

Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Man

Yang

et al. 2023

Mol. Pharmaceutics

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“…In this study, different ODFs were manufactured by 3D printing and solvent casting methods using the Biopharmaceutics Classification System (BCS) class II drug aripiprazole (ARP) that treats schizophrenia. In terms of drug and microenvironmental modifications, there was some research on changing salt forms and pH-dependent self-emulsifying formulations of the ARP [ 25 , 26 , 27 ]. Salts forms and lipid-based surfactants are not free from fluctuating bioavailability issues due to pH variability in the human body pH [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

Investigation of Patient-Centric 3D-Printed Orodispersible Films Containing Amorphous Aripiprazole

et al. 2022

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The objective of this study was to design and evaluate an orodispersible film (ODF) composed of aripiprazole (ARP), prepared using a conventional solvent casting technique, and to fuse a three-dimensional (3D) printing technique with a hot-melt extrusion (HME) filament. Klucel® LF (hydroxypropyl cellulose, HPC) and PE-05JPS® (polyvinyl alcohol, PVA) were used as backbone polymers for 3D printing and solvent casting. HPC-, PVA-, and ARP-loaded filaments were applied for 3D printing using HME. The physicochemical and mechanical properties of the 3D printing filaments and films were optimized based on the composition of the polymers and the processing parameters. The crystalline states of drug and drug-loaded formulations were investigated using differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). The dissolution and disintegration of the 3D-printed films were faster than those of solvent-cast films. HPC-3D printed film was fully disintegrated within 45 ± 3.5 s. The dissolution rate of HPC films reached 80% within 30 min at pH 1.2 and pH 4.0 USP buffer. There was a difference in the dissolution rate of about 5 to 10% compared to PVA films at the same sampling time. The root mean square of the roughness (Rq) values of each sample were evaluated using atomic force microscopy. The higher the Rq value, the rougher the surface, and the larger the surface area, the more salivary fluid penetrated the film, resulting in faster drug release and disintegration. Specifically, The HPC 3D-printed film showed the highest Rq value (102.868 nm) and average surface roughness (85.007 nm). The puncture strength of 3D-printed films had desirable strength with HPC (0.65 ± 0.27 N/mm2) and PVA (0.93 ± 0.15 N/mm2) to prevent deformation compared to those of marketed film products (over 0.34 N/mm2). In conclusion, combining polymer selection and 3D printing technology could innovatively design ODFs composed of ARP to solve the unmet medical needs of psychiatric patients.

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Drug and formulation development processes

Charoo,

Mohamed,

Eltigani

et al. 2024

From Current to Future Trends in Pharmaceutical Technology

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Salt Engineering of Aripiprazole with Polycarboxylic Acids to Improve Physicochemical Properties

Cited by 5 publications

References 45 publications

Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Establishment of In Vitro Dissolution Based on Similarity with In Vivo Dissolution: A Case Study on Aripiprazole

Investigation of Patient-Centric 3D-Printed Orodispersible Films Containing Amorphous Aripiprazole

Drug and formulation development processes

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