Improved pharmaceutical properties of ritonavir through co-crystallization approach with liquid-assisted grinding method

Chaudhari, Khushbu; Savjani, Jignasa; Savjani, Ketan; Shah, Harsh

doi:10.1080/03639045.2022.2042553

Cited by 12 publications

(4 citation statements)

References 59 publications

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“…Surprisingly, due to its flexible molecular conformation and glass-forming tendency of the material, only a single cocrystal form of ritonavir co-crystallised with L-tyrosine have been reported. [11][12][13] More recently, Wang et al 14 have characterised and compared, in significant detail, the crystal chemistry for both forms I and II in terms of their molecular conformations, polarizabilities, hydrogen bonding networks, intermolecular packing structures and crystal morphologies cross-correlating these to a wider assessment of their crystallisability behaviour and respective surface properties.…”

Section: Introductionmentioning

confidence: 99%

A quaternary solid-form of ritonavir: an oxalate salt oxalic acid co-crystal acetone solvate

et al. 2023

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Section: Introductionmentioning

confidence: 99%

A quaternary solid-form of ritonavir: an oxalate salt oxalic acid co-crystal acetone solvate

et al. 2023

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“…Furthermore, the greater co-crystallization degree has been described for the indistinguishable arrangement at maximum temperatures and comparative dampness, nevertheless of the mechanical stimulation [20]. The formation of an isoniazid benzoic acid co-crystal via spontaneous co-crystallization was reported as well [24]. We found that a higher frequency of pre-grinding of uncontaminated components significantly improved the reaction rate [27].…”

Section: Contact Formationmentioning

confidence: 58%

“…Compared with solution-based approaches, solid milling is associated with higher performance because no product is lost due to its solubility in a solvent. Problems with dry milling can comprise impossibility to form a co-crystal, inadequate modifications to the co-crystal, and crystalline flaws with the presence of possible several amorphous compounds [24].…”

Section: Grindingmentioning

confidence: 99%

Chemistry and Modern Techniques of Characterization of Co-Crystals

Ali¹,

Кузнецов²,

Ibrahim³

et al. 2023

Drug Formulation Design

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Co-crystals are multicomponent molecular materials held together through non-covalent interactions that have recently attracted the attention of supramolecular scientists. They are the monophasic homogeneous materials where a naturally occurring pharmaceutical active ingredient (API) and a pharmaceutically acceptable co-crystal former are bonded together in a 1:1 via non-covalent forces such as H-bonds, π–π, and van der Waals forces. Co-crystallization is a promising research field, especially for the pharmaceutical industry, due to the enormous potential of improved solubility and bioavailability. Co-crystals are not the only multicomponent molecular materials, as there are many other forms of multicomponent molecular solids such as salts, hydrates, solvates, and eutectics. The formation of co-crystals can roughly be predicted by the value of ∆pKa, that is, if the ∆pKa is more than 3, then this monophasic homogeneous material usually falls in the category of salts, whereas if the ∆pKa is less than 2, then co-crystals are usually observed. A number of methods are available for the co-crystal formation, broadly classified into two classes established on state of formation, that is, solution-based and solid-based co-crystal formation. Similarly, a number of techniques are available for the characterization of co-crystals such as Fourier transforms-infrared spectroscopy, single-crystal and powder X-ray diffraction, etc. In this chapter, we will discuss the available methods for co-crystallization and its characterization.

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“…The DXI-CAF multicomponent crystal was prepared by liquid-assisted grinding method. 18,19 A mixture of 1.030 g (5 mmol) of DXI and 0.970 g (5 mmol) of CAF was placed into the mortar and five drops of ethanol were dropped. The mixture was milled for five minutes and allowed to dry.…”

Section: Preparation Of Dxi-caf Multicomponent Crystalmentioning

confidence: 99%

Multicomponent Crystal Formation of Dexibuprofen-Caffeine to Improve Solubility

2023

TJNPR

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It has been shown to increase the solubility of several APIs through the multicomponent crystal formation, including trimesic acid 11 , luteolin 12 , and paracetamol 13 , and dihydromyricetin. 14 The chemical structures of DXI and CAF as shown in Figure 1 have the opportunity to form multicomponent crystal due to the presence of groups of two components that are capable of acting as hydrogen bond donors/acceptors and proton donors/acceptors. The presence of a carboxylic acid group in DXI increases the chances of hydrogen bond formation with the N-imidazole group in CAF. 15 The weakly basic nature of CAF also increases the chances of proton transfer from DXI to form salts. The purpose of this research was to produce dexibuprofencaffeine (DXI-CAF) multicomponent crystal, to characterize, and to determine its effect on its solubility and dissolution rate. Materials and Methods MaterialsDexibuprofen was purchased from Beijing Mesochem Technology, CO., Ltd., China, whilst caffeine was obtained from Merck, Indonesia. Ethanol and materials for buffer solution were obtained from Merck, Indonesia. Crystal morphology observationCrystal morphological observations were carried out by placing approximately three mg each of DXI, CAF, and DXI-CAF equimolar mixture on a glass object. The samples were dripped with ethanol until they dissolved and were allowed to form crystals. The crystal morphology formed from each sample was observed with an Olympus BX-53 polarizing microscope. The microscope images were obtained by an Optilab Advance Plus camera attached to the microscope. Phase solubility testThe phase solubility of dexibuprofen (drug) in the caffeine (ligand) solution was carried out using the shaker method. 16,17 CAF solutions in water were prepared with various concentrations of 5,

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Improved pharmaceutical properties of ritonavir through co-crystallization approach with liquid-assisted grinding method

Cited by 12 publications

References 59 publications

A quaternary solid-form of ritonavir: an oxalate salt oxalic acid co-crystal acetone solvate

A quaternary solid-form of ritonavir: an oxalate salt oxalic acid co-crystal acetone solvate

Chemistry and Modern Techniques of Characterization of Co-Crystals

Multicomponent Crystal Formation of Dexibuprofen-Caffeine to Improve Solubility

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