Facile formation of co-amorphous atenolol and hydrochlorothiazide mixtures via cryogenic-milling: Enhanced physical stability, dissolution and pharmacokinetic profile

Moinuddin, Sakib M.; Ruan, Sida; Huang, Yu-Ting; Gao, Qin; Shi, Qin; Cai, Baochang; Cai, Ting

doi:10.1016/j.ijpharm.2017.09.020

Cited by 65 publications

(58 citation statements)

References 48 publications

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“…18) These results suggest that the binary SCL system could enhance stability compared with the SCL of single compound similar to glassy co-amorphous systems. 11,12,19) Therefore KET-ETH (2 : 1) SCL was selected and evaluated as a suitable formulation from the viewpoint of physical stability.…”

Section: Crystal Form Of Scls After Recrystallization Induced By Stimmentioning

confidence: 99%

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A Novel Binary Supercooled Liquid Formulation for Transdermal Drug Delivery

Hirakawa

Ueda

Wakabayashi

et al. 2020

Biological & Pharmaceutical Bulletin

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The aim of this study was to prepare binary supercooled liquid (SCL) by intermolecular interaction and apply this formulation to transdermal drug delivery. Ketoprofen (KET) and ethenzamide (ETH) were selected as binary SCL component. Thermal analysis of physical mixtures of KET and ETH showed decreases in melting points and glass transition below room temperature, thereby indicating formation of KET-ETH SCL. Intermolecular interactions between KET and ETH in the SCL were evaluated from Fourier transform (FT)-IR spectra. KET-ETH SCL maintained SCL state at 25°C with silica gel over 31 d and at 40°C/89% relative humidity (RH) over 7 d. KET SCL and KET-ETH SCL showed similar permeability of KET for hairless mice skin, which was twofold higher than that of KET aqueous suspension. Our findings suggest that the SCL state could enhance the skin permeation of drugs and the binary SCL formed by intermolecular interaction could also improve the stability of the SCL. The binary SCL system could become a new drug form for transdermal drug delivery.

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Section: Crystal Form Of Scls After Recrystallization Induced By Stimmentioning

confidence: 99%

“…9,10) Several researchers have shown that a co-amorphous system improved stability of the amorphous state compared with that of single compound. 11,12) Hence SCL based on the co-amorphous approach, which stabilizes the thermodynamically unstable state by intermolecular interactions, should also improve the stability of the SCL state.…”

Section: Introductionmentioning

confidence: 99%

A Novel Binary Supercooled Liquid Formulation for Transdermal Drug Delivery

Hirakawa

Ueda

Wakabayashi

et al. 2020

Biological & Pharmaceutical Bulletin

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“…High curcumin concentration administered as co-amorphous with artemisin was found in the plasma of male rats compared to administration alone, although it was not clear whether the increase was due to amorphization of curcumin or to co-amorphization [ 20 ]. Additionally, studies in mice showed great improvement in the bioavailability of hydrochlorothiazide co-amorphous mixture with atenolol following the order of enhancement: co-amorphous dispersion > natural mixture > amorphous drug > crystalline drug as demonstrated in Figure 6 [ 38 ].…”

Section: Co-amorphous Dispersionsmentioning

confidence: 99%

“…Moinuddin et al [ 38 ] studied the system of atenolol (ATE) with hydrochlorothiazide (HCT). The co-amorphous ATE-HCT sample with 1:1 molar ratio showed excellent physical stability, which could be attributed to the formation of strong molecular interactions between ATE and HCT as evidenced by FT-IR spectra.…”

Section: Solid State Characterizationmentioning

confidence: 99%

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Co-Amorphous Solid Dispersions for Solubility and Absorption Improvement of Drugs: Composition, Preparation, Characterization and Formulations for Oral Delivery

2018

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The amorphous solid state offers an improved apparent solubility and dissolution rate. However, due to thermodynamic instability and recrystallization tendencies during processing, storage and dissolution, their potential application is limited. For this reason, the production of amorphous drugs with adequate stability remains a major challenge and formulation strategies based on solid molecular dispersions are being exploited. Co-amorphous systems are a new formulation approach where the amorphous drug is stabilized through strong intermolecular interactions by a low molecular co-former. This review covers several topics applicable to co-amorphous drug delivery systems. In particular, it describes recent advances in the co-amorphous composition, preparation and solid-state characterization, as well as improvements of dissolution performance and absorption are detailed. Examples of drug-drug, drug-carboxylic acid and drug-amino acid co-amorphous dispersions interacting via hydrogen bonding, π−π interactions and ionic forces, are presented together with corresponding final dosage forms.

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