Co-crystallization for enhanced dissolution rate of bicalutamide: preparation and evaluation of rapidly disintegrating tablets

Essa, Ebtessam A.; Elbasuony, Aya R; Abdelaziz, Abdelaziz E.; Maghraby, Gamal M. El

doi:10.1080/03639045.2019.1571504

Cited by 16 publications

(19 citation statements)

References 20 publications

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“…These changes were also reported by other investigators who treated the sugar in a similar way. 7,8 Additionally, these modifications in the diffraction pattern coincide with the DSC data that showed increase in the Tm value for the processed sucralose that would suggest formation of new crystalline structure. The diffractogram of unprocessed mannitol showed its crystalline structure as noted from the recorded diffraction peaks (Figure 3b and Table 4).…”

Section: Powder X-ray Diffraction (Pxrd)supporting

confidence: 78%

“…The wetting time of the tablets was determined according to the established method. 7,16 This utilized Petri dish which was loaded with circular filter paper and 6 ml of distilled water. Allura red powder was carefully sprinkled over the tablet surface before mounting on wet filter paper.…”

Section: Evaluation Of Fast Disintegrating Tabletsmentioning

confidence: 99%

“…This diffractogram is similar to previously recorded for the same sugar. 7 Wet grinding of sucralose compromised the diffraction pattern compared to the unprocessed material with the reduction of the intensity and disappearance of some peaks. Additionally, new diffraction peaks at 2 theta values of 22.98, 25.86, 28.44, 34.77 and 36.24 ο was noted.…”

Section: Powder X-ray Diffraction (Pxrd)mentioning

confidence: 99%

“…Sucralose, which is used as an artificial sweetener, was able to enhance the dissolution rate of various hydrophobic drugs like nateglinide and bicalutamide after co-processing. 6,7 Xylitol was also employed to enhance the dissolution rate of felodipine. 8 Mannitol is another hydrophilic sugar showed promising efficacy in enhancing the dissolution rate of olanzapine and etoricoxib after solid dispersion formation and as cocrystal conformer for hydrochlorothiazide.…”

Section: Introductionmentioning

confidence: 99%

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Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing

et al. 2020

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Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability due to its low aqueous solubility. The objective of this work was to enhance the dissolution of cilostazol with the aim of formulating fast dissolving tablets for geriatrics and those of swallowing difficulties. Methods: Ethanol-assisted co-grinding of cilostazol with sugar-based excipients was adopted. Sucralose and mannitol were used for this purpose as hydrophilic excipient as well as taste improving agents. The obtained products were investigated regarding differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction, scanning electron microscope (SEM) and in vitro drug dissolution. Fast disintegrating tablets were prepared and evaluated. Results: Thermal behavior of the developed products reflected reduced crystallinity, it also suggested possible existence of new crystalline species with sucralose. Eutexia was also suggested for mannitol mixtures, that was supported by X-ray diffraction data. SEM indicated size reduction with the deposition of the drug as submicron particles over the excipient surface. Co-processing markedly improved cilostazol dissolution compared to unprocessed drug. The optimized formulations were successively formulated into fast disintegrating tablets. Conclusion: This investigation introduced the wet grinding strategy with sugar excipients as a platform for the formulation of easy to use tablets with optimum drug release.

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Section: Powder X-ray Diffraction (Pxrd)supporting

confidence: 78%

Section: Evaluation Of Fast Disintegrating Tabletsmentioning

confidence: 99%

Section: Powder X-ray Diffraction (Pxrd)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing

et al. 2020

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“…The change in melting behaviour signals the formation of a new solid form. 15 Melting point is affected by chemical structure, intermolecular interactions, molecular symmetry etc. Moreover, the change in meltingpoint as compared to starting components was taken as a basis for the identification of naproxen cocrystal.…”

Section: Resultsmentioning

confidence: 99%

Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals

Panzade¹,

Shendarkar²,

Kulkarni³

et al. 2020

Adv Pharm Bull

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Novel nimesulide multicomponent solid forms: screening, synthesis, thermoanalytical study and characterization

de Almeida,

Ferreira,

Porto

et al. 2024

J Therm Anal Calorim

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Nimesulide (NMS) is a widely used non-steroidal anti-inflammatory drug, however, presents low aqueous solubility. One way to overcome the solubility issue of drugs is altering their solid forms through some approaches like cocrystals, coamorphous, and eutectic mixtures. The purpose of this work was to prospect new multicomponent solid forms of NMS. A virtual-experimental cocrystal screening was carried out through COSMOquick software and mechanochemical experiments. Alternatively, dual-drug coamorphous systems were investigated by quench cooling and/or cryomilling processes. All solid samples were characterized using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and infrared spectroscopy (FTIR). The results confirmed the successful synthesis of a NMS-piperazine cocrystal (NMS-PPZ), two new eutectic mixtures NMS-gentisic acid (NMS-GSA) and NMS-isoniazid (NMS-INH), as well as novel drug-drug coamorphous systems. The eutectic compositions were determined by binary solid–liquid phase diagram construction and Tamman’s triangle plot. Nimesulide-omeprazole (NMS-OMP) coamorphous system was found to be stable for at least 120 days in dry conditions. The coamorphous system with bicalutamide (NMS-BICA) prepared by quench cooling process is more stable than that obtained by cryomilling. Finally, the dissolution rate study demonstrated that NMS multicomponent systems are dissolved relatively faster than pure drug.

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Co-crystallization for enhanced dissolution rate of bicalutamide: preparation and evaluation of rapidly disintegrating tablets

Cited by 16 publications

References 20 publications

Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing

Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing

Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals

Novel nimesulide multicomponent solid forms: screening, synthesis, thermoanalytical study and characterization

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