Crystallization by Antisolvent Addition and Cooling

Giulietti, Marco; Bernardo, André

doi:10.5772/50328

Cited by 18 publications

(17 citation statements)

References 25 publications

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“…Ezetimibe is containing two hydrogen bond donors and three hydrogen bond acceptors. 12 Two molecules of ezetimibe -maleic acid are connected by strong N-H…O hydrogen bonds forming a hydrogen bond dimer in a cyclic motif, 13 which indicates potential for co-crystal formation based on molecular hydrogen bonding. Maleic acid being strong hydrogen bond acceptor and receptor was selected as the co-former to prepare co-crystals.…”

Section: Sem Resultsmentioning

confidence: 99%

Nano Co-crystal Engineering Technique to Enhance the Solubility of Ezetimibe

Bhandari¹,

Kanswami²,

Lakshmi³

2020

JYP

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Background: Co-crystals have been highly promising for tailoring physicochemical properties of Active pharmaceutical ingredient (API) by coupling with co-former. Objectives: The objective of the present work was to prepare and characterize novel nano co-crystals of Ezetimibe by different methods in various ratios of co-formers and to optimize the formulation based on the enhancement in solubility and dissolution rate. Methods: Ezetimibe nano co-crystals were prepared employing oxalic acid, succinic acid and maleic acid as co-formers by solvent evaporation method and anti-solvent method. Results: Instrumental analysis of co-crystals (DSC, IR, SEM and XRD) was performed to characterize the novel nano co-crystals. Dissolution studies and chemical stability were assessed and compared with pure Ezetimibe. The formulation with maleic acid as a co-former in the molar ratio of Ezetimibe and maleic acid (0.4:0.4) was found to be efficient than oxalic acid and succinic acid. The co-crystal dissolution profile in distilled water containing 0.5% SLS showed 18.8 folds increase in the dissolution efficiency and was found to be 95.2% within 45 min. Conclusion: The results demonstrate feasibility of co-crystallization method using maleic acid as co-former to enhance the solubility of poorly soluble drug Ezetimibe.

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Section: Sem Resultsmentioning

confidence: 99%

Nano Co-crystal Engineering Technique to Enhance the Solubility of Ezetimibe

Bhandari¹,

Kanswami²,

Lakshmi³

2020

JYP

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“…The co-crystals prepared by antisolvent addition method demonstrated higher solubility than that of FNO and other cocrystals ( fig. 1 ) because addition of an antisolvent which reduces the solute solubility in the resultant system, or changing the solute by chemical reaction producing another substance with much lower solubility[ 9 ].…”

Section: Resultsmentioning

confidence: 99%

Formulation and solid state characterization of nicotinamide-based co-crystals of fenofibrate

Shewale¹,

Shete²,

Doijad³

et al. 2015

Indian J Pharm Sci

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The present investigation deals with formulation of nicotinamide-based co-crystals of fenofibrate by different methods and solid-state characterization of the prepared co-crystals. Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods. The prepared molecular complexes were characterized by powder X-ray diffractometry, differential scanning calorimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy and in vitro dissolution study. Considerable improvement in the dissolution rate of fenofibrate from optimized co-crystal formulation was due to an increased solubility that is attributed to the super saturation from the fine co-crystals is faster because of large specific surface area of small particles and prevention of phase transformation to pure fenofibrate. In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate. Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.

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“…Namun hal tersebut juga dipengaruhi oleh kandungan impuritis yang terkandung di dalam ekstrak tersebut [11]. [12].…”

Section: Gambar 1 Struktur Kimia Dari Likopen [5]unclassified

“…Hal ini dapat diakibatkan karena jumlah pelarut yang terlalu banyak dan tidak efisien menyebabkan impuritis yang ikut terlarut serta menyebabkan perubahan komponen dari bahan yang diekstrak. Dimana, impuritis merupakan salah satu faktor penghambat proses kristalisasi dengan penambahan antisolvent [12]. Adapun sejumlah impuritis yang berpengaruh terhadap kemurnian likopen ini adalah residu pelarut yang terikut bersama likopen serta sejumlah logam dan arsenik yang menurunkan nilai rendemen ekstrak likopen tersebut.…”

Section: Gambar 2 Grafik Perbandingan Umpan Dan Pelarut ( V / V ) Teunclassified

KRISTALISASI LIKOPEN DARI BUAH TOMAT (Lycopersicon esculentum) MENGGUNAKAN ANTISOLVENT

2015

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Studies on the utilization of lycopene had been conducted to determine the effect of comparison feed and solvent (F/S) and the addition of methanol for extraction of lycopene from tomatoes using mixture solvent of hexane:ethyl acetate (1:1) followed by crystallization antisolvent. In this research, ripe tomatoes juice was used with volume 150 ml. Lycopene extract was obtained through extraction method at temperature of 70 °C and the stirring speed 7 rpm. The other method was by the addition of methanol as antisolvent for crystallization. As for changing variable in this study were a comparison of feed and solvent (F/S) 1:2; 1:2.5; 1:3; 1:3.5; 1:4 and 1:4,5, and the volume of methanol as antisolvent were 50 ml, 100 ml, 150 ml and 200 ml. The results of this research about influence of feed and solvent to lycopene yield extracted obtained at the optimum condition 1:4 with a volume of 200 ml antisolvent. Whereas the influence about addition of methanol as antisolvent as an agent of precipitation and maximum condition occurs on volume of 200 ml. Wavelength analysis of C=C linkage with Fourier Transform Infrared (FT-IR) detected at wavenumber 1519,91 cm-1, CH2 linkage detected at wavenumber 1446,61 cm-1, R-CH=CH-R linkage detected at wavenumber 979,84 cm-1. While, C-C and C-CH linkage detected at wavenumber 1138 and 1373,32 cm-1.

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Crystallization by Antisolvent Addition and Cooling

Cited by 18 publications

References 25 publications

Nano Co-crystal Engineering Technique to Enhance the Solubility of Ezetimibe

Nano Co-crystal Engineering Technique to Enhance the Solubility of Ezetimibe

Formulation and solid state characterization of nicotinamide-based co-crystals of fenofibrate

KRISTALISASI LIKOPEN DARI BUAH TOMAT (Lycopersicon esculentum) MENGGUNAKAN ANTISOLVENT

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