Clozapine-carboxylic acid plasticized co-amorphous dispersions: Preparation, characterization and solution stability evaluation

Ali, Ahmed Mahmoud Abdelhaleem; Ali, Adel A.; Maghrabi, Ibrahim A.

doi:10.1515/acph-2015-0014

Cited by 45 publications

(23 citation statements)

References 24 publications

(24 reference statements)

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“…In contrast to polymeric ASDs, coamorphous systems are stoichiometric binary systems of two compatible drugs (Yamura et al, 1996(Yamura et al, & 2000Chieng et al, 2009;Alessø et al, 2009;Löbmann et al, 2011Löbmann et al, & 2012 or of a drug and a pharmaceutically acceptable small-molecule coformer (Lu and Zografi, 1998;Masuda et al, 2012;Hoppu et al, 2007Hoppu et al, & 2009. Coformers that have been successfully applied to stabilize an amorphous drug include saccharin (Gao et al, 2013), nicotinamide (Shayanfar, 2013), carboxylic acids (Lu and Zografi, 1998;Masuda et al, 2012;Hoppu et al, 2007Hoppu et al, & 2009Ali et al, 2015;Han et al, 2016;Hu et al, 2014) and sugars (Descamps et al, 2007). In particular, amino acids capable of forming charge-assisted hydrogen bonds have been widely studied (Löbmann et al, 2013;Jensen et al, 2014Jensen et al, , 2015Jensen et al, & 2016Laitinen et al, 2014;Lenz et al, 2015;Huang et al, 2016;Craye et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems

Gniado

MacFhionnghaile

McArdle

et al. 2018

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems

Gniado

MacFhionnghaile

McArdle

et al. 2018

International Journal of Pharmaceutics

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“…In addition to drug combinations with pharmacologically suitable drugs, co-amorphous systems of drugs and small molecule excipients seem to be a more common concept. Other small molecules, such as sugars, amino acids, nicotinamides, urea, carboxylic acids, and saccharin, have also been explored as co-amorphous excipients, which have significantly increased solubility, dissolution rate, and physical stability of amorphous drug forms [ 24 , 25 , 26 ]. Since a small molecule excipient is a molar stoichiometric unit, the required amount of a counter molecule used as a drug additive is generally smaller than that of a polymer in solid dispersion; thus, co-amorphous can provide a smaller volume and a relatively lower cost.…”

Section: Introductionmentioning

confidence: 99%

A Novel Desloratadine-Benzoic Acid Co-Amorphous Solid: Preparation, Characterization, and Stability Evaluation

et al. 2018

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Low physical stability is the limitation of the widespread use of amorphous drugs. The co-amorphous drug system is a new and emerging method for preparing a stable amorphous form. Co-amorphous is a single-phase amorphous multicomponent system consisting of two or more small molecules that are a combination of drugs or drugs and excipients. The co-amorphous system that uses benzoic acid (BA) as an excipient was studied to improve the physical stability, dissolution, and solubility of desloratadine (DES). In this study, the co-amorphous formation of DES and BA (DES–BA) was prepared by melt-quenching method and characterized by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and polarized light microscopy (PLM). Dissolution, solubility, and physical stability profiles of DES–BA were determined. The DES crystals were converted into DES–BA co-amorphous form to reveal the molecular interactions between DES and BA. Solid-state analysis proved that the co-amorphous DES–BA system (1:1) is amorphous and homogeneous. The DSC experiment showed that the glass transition temperature (Tg) of tested DES–BA co-amorphous had a higher single Tg compared to the amorphous DES. FTIR revealed strong interactions, especially salt formation. The dissolution rate and solubility of co-amorphous DES–BA (1:1) obtained were larger than the DES in crystalline form. The PXRD technique was used to assess physical stability for three months at 40 °C with 75% RH. The DES–BA co-amorphous system demonstrated better physical stability than a single form of amorphous DES. Co-amorphous DES–BA has demonstrated the potential for improving solid-state stability, as the formation of DES–BA co-amorphous salt increased solubility and dissolution when compared to pure crystalline DES. This study also demonstrated the possibility for developing a DES–BA co-amorphous system toward oral formulations to improve DES solubility and bioavailability.

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“…The coamorphous dispersions were prepared by a previously published coprecipitation method using fast solvent evaporation with some modifications [27]. Mixtures of QF and NIC based on their molar mass (441.5 and 122.12 g/mole) and electron donner/acceptor functional groups (Figure 1) were prepared as shown in Table 1.…”

Section: Methodsmentioning

confidence: 99%

Freeze Dried Quetiapine-Nicotinamide Binary Solid Dispersions: A New Strategy for Improving Physicochemical Properties and Ex Vivo Diffusion

Ali

Al-Remawi

2016

Journal of Pharmaceutics

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Improving the physicochemical properties and oral bioavailability of quetiapine fumarate (QF) enabling enhanced antipsychotic attributes are the main aims of this research. The freeze dried solid dispersion strategy was adopted using nicotinamide (NIC) as highly soluble coformer. The prepared dispersions were characterized using scanning electron microscopy (SEM) differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Static disc intrinsic dissolution rate and ex vivo diffusion through intestinal tissues were conducted and compared to pure quetiapine fumarate. The results demonstrated a highly soluble coamorphous system formed between quetiapine fumarate and nicotinamide at 1 : 3 molar ratio through H-bonding interactions. The results showed >14-fold increase in solubility of QF from the prepared dispersions. Increased intrinsic dissolution rate (from 0.28 to 0.603 mg cm−2 min−1) and faster flux rate through duodenum (from 0.027 to 0.041 mg cm−2 h−1) and jejunum (0.027 to 0.036 mg cm−2 h−1) were obtained. The prepared coamorphous dispersion proved to be effective in improving the drug solubility and dissolution rate and ex vivo diffusion. Therefore, binary coamorphous dispersions could be a promising solution to modify the physicochemical properties, raise oral bioavailability, and change the biopharmaceutics classification (BCS) of some active pharmaceutical ingredients.

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Clozapine-carboxylic acid plasticized co-amorphous dispersions: Preparation, characterization and solution stability evaluation

Cited by 45 publications

References 24 publications

The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems

The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems

A Novel Desloratadine-Benzoic Acid Co-Amorphous Solid: Preparation, Characterization, and Stability Evaluation

Freeze Dried Quetiapine-Nicotinamide Binary Solid Dispersions: A New Strategy for Improving Physicochemical Properties and Ex Vivo Diffusion

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