Design and characterization of aceclofenac and paracetamol spherical crystals and their tableting properties

Patra, Chinam Niranjan; Swain, Sanjit Kumar; Mahanty, Sauravo; Panigrahi, Kahnu Charan

doi:10.1016/j.powtec.2015.01.053

Cited by 23 publications

(14 citation statements)

References 22 publications

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“…The spherical crystallization technique has always been the focus of granulation because the drug spheres exhibit high performances in the post-treatment processes, such as filtration and tableting, over particles bearing other morphology . There are many literature studies focusing on the spherical crystallization techniques to enhance the drug dissolution rate, tableting properties, compactability properties, and physicochemical properties. − In classical spherical crystallization methods, good solvent, bridging liquid, and poor solvent should be utilized, whereas screening these appropriate solvents is very time-consuming and high-cost. − Besides, the use of the organic solvent in the traditional spherical crystallization can result in a problem of harmful organic solvent residual in the final products. For instance, in the wet spherical agglomeration method, a bridging liquid should be introduced to the system to induce the liquid–liquid phase separation (LLPS) phenomenon and thus create the bridging liquid droplets that are expected to collect the crystals suspended in the system, ,, while it is very difficult to separate the bridging liquid from the final products completely.…”

Section: Introductionmentioning

confidence: 99%

Design of Spherical Crystallization for Drugs Based on Thermal-Induced Liquid–Liquid Phase Separation: Case Studies of Water-Insoluble Drugs

Sun

Tang

et al. 2019

Ind. Eng. Chem. Res.

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Spherical crystallization of water-insoluble drugs was investigated based on thermal-induced liquid–liquid phase separation (TILLPS) without the use of organic solvent. The phase diagram of the drug in water was constructed first, consisting of solid–liquid and liquid–liquid equilibrium regions. Within the liquid–liquid phase region, droplets of the solute-rich phase were formed and dispersed under appropriate agitation in the solvent-rich phase. After being stabilized by a surfactant, the solute-rich droplets can be converted to monodisperse spherical particles by performing quench cooling crystallization where the drug is crystallized within the confinement of the droplets. Furthermore, the influences of the oil droplets on the size of the resulting crystals were investigated, demonstrating that a decrease of the oil droplet size, controlled by agitation speed, would result in the decline of the product size. l-Menthol and ibuprofen products with a spherical shape and a yield of more than 95% were prepared successfully using the above method, revealing the application prospect of TILLPS in the drug spherical crystallization and it gives important guidance for the preparation of spherical particles of water-insoluble drugs.

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Section: Introductionmentioning

confidence: 99%

Design of Spherical Crystallization for Drugs Based on Thermal-Induced Liquid–Liquid Phase Separation: Case Studies of Water-Insoluble Drugs

Sun

Tang

et al. 2019

Ind. Eng. Chem. Res.

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“…Simultaneously, the crystals are transformed into spherical aggregates. To date, these approaches have been widely used in the preparation of spherical organic drugs and have become an outstanding strategy for designing the desired products with improved physical and mechanical properties. − However, the formation mechanism of spherical crystals has not been fully understood, because the fast kinetics resulting from the antisolvent crystallization make the observation of the morphological evolution details difficult . Moreover, compared with organic drug molecules, only a few literature reports ,, have discussed the methods to prepare the spherical crystals of organic explosive molecules, especially for those molecules containing strong intra- and intermolecular hydrogen bonds, such as 2,4,6-trinitrobenzene-1,3,5-triamine (TATB), 3,5-dinitropyrazine-2,6-diamine-1-oxide (LLM-105), and 2,2-dinitroethylene-1,1-diamine (FOX-7).…”

Section: Introductionmentioning

confidence: 99%

A Novel Spherulitic Self-Assembly Strategy for Organic Explosives: Modifying the Hydrogen Bonds by Polymeric Additives in Emulsion Crystallization

Zhou

Zhang

et al. 2018

Crystal Growth & Design

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A novel strategy to prepare spherical crystals of 2,6-diamino-3,5-dinitropyrazine-1-oxide (LLM-105) has been developed by introducing polymeric additives into the antisolvent emulsion crystallization. The spherical crystals are induced by modifying the intermolecular hydrogen bonds network of LLM-105. The results show that the concentration of polyvinylpyrrolidone (PVP), which acts as a polymeric additive, is a crucial factor to get quite different morphologies of LLM-105 crystal products. X-like shaped crystals have been produced in the absence of PVP. In contrast, spherical crystals have been obtained in the presence of PVP. Importantly, LLM-105 spherulites with a mean particle size of 78.0 μm can be obtained by adding a proper amount of PVP, which has a narrow size distribution (CV = 31.2). In addition, time-resolved morphological evolution processes of X-like shaped and spherical crystals have been performed. Meanwhile, 1H NMR experiments also have been conducted to understand the intermolecular hydrogen bonds between LLM-105 molecules and the polymer. Inspired by the result of the above experiments, an LLM-105 spherulitic formation mechanism has been proposed. Furthermore, LLM-105 spherulites exhibit more excellent mechanical and safety properties. It is suggested that these spherulites have a great potentiality in the military application. Therefore, this polymer-induced spherical crystallization method is significantly important for the design and fabrication of organic small molecules with spherical shapes.

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“…9 Polymers are generally added to the aqueous phase. Drugs like acebutalol, 10 bucillamine, 11 celecoxib, 12 aceclofenac, 13 and albendazole 14 have been engineered using a similar strategy to overcome problems associated with solubility and compressibility.…”

Section: Introductionmentioning

confidence: 99%

Spherical Agglomeration of Platy Crystals: Curious Case of Etodolac

Jitkar

Thipparaboina

Chavan

et al. 2016

Crystal Growth & Design

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The present study reports an intriguing case study of agglomeration of platy crystals into spheroids. Etodolac a nonsteroidal anti-inflammatory drug is mainly used for rheumatoid arthritis, with emerging applications in management of prostate cancer and Alzheimer’s disease. It is a BCS class II drug with poor flow and compressibility issues. Recrystallization using various solvents resulted in platy crystals. Different polymers like hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), and polyvinylpyrrolidone (PVP), and copolymers poly(ethylene glycol) (PEG 400), poly(vinyl alcohol) (PVA), and Poloxamer were explored at various concentrations and in different combinations to provide systematic inputs for the development of spherical agglomerates with optimal sphericity, dissolution, yield, and mechanical properties suitable for direct compression. Effects of different process parameters on agglomeration were studied. Agglomerates obtained were characterized using SEM, DSC, and P-XRD and were evaluated for enhancements in flow, compressibility, and dissolution. All the agglomerates have shown improved flow properties and compressibility. Unlike plain drug, all spherical agglomerates have shown acceptable plastic behavior during compression studies resulting in tablets at low pressures. Agglomerates developed using a unique combination of HPMC, HPC, and PEG has shown 94% drug release in 15 min. The recrystallized spherical agglomerates can be used as readily compressible material for continuous manufacturing.

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Design and characterization of aceclofenac and paracetamol spherical crystals and their tableting properties

Cited by 23 publications

References 22 publications

Design of Spherical Crystallization for Drugs Based on Thermal-Induced Liquid–Liquid Phase Separation: Case Studies of Water-Insoluble Drugs

Design of Spherical Crystallization for Drugs Based on Thermal-Induced Liquid–Liquid Phase Separation: Case Studies of Water-Insoluble Drugs

A Novel Spherulitic Self-Assembly Strategy for Organic Explosives: Modifying the Hydrogen Bonds by Polymeric Additives in Emulsion Crystallization

Spherical Agglomeration of Platy Crystals: Curious Case of Etodolac

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