Effect of mechanochemical grinding conditions on the formation of pharmaceutical cocrystals and co-amorphous solid forms of ketoconazole – Dicarboxylic acid

Mithu, Sadeque Hossain; Ross, Susan; Hurt, Andrew P.; Douroumis, Dennis

doi:10.1016/j.jddst.2021.102508

Cited by 17 publications

(8 citation statements)

References 51 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The cocrystal of DHOXA−OA was prepared by reaction crystallization in pure water medium, which is one of the commonly used solvent method for the successful preparation of pharmaceutical cocrystals. 44 Equimolar amounts of DHOXA and OA were added to water. The suspension was stirred for 24 h at room temperature.…”

Section: Synthesis Of Cocrystals 221 Synthesis Of Dhoxa−oamentioning

confidence: 99%

Strategy to Regulate the Stability and Reduction Rate of Oxaliplatin-Based Pt(IV) Complexes: Cocrystallization

Zhu,

Guo,

Yao

et al. 2023

Crystal Growth & Design

View full text Add to dashboard Cite

To overcome the clinical limitations of oxaliplatin (OXA), such as side effects and toxicity, increasing attention was paid to the use of OXA-based Pt(IV) complexes as oral administration prodrugs. In this study, we prepared trans-[Pt(R,R-DACH)(oxalate)(OH) 2 ] (DHOXA) as a model of OXA-based Pt(IV) complexes and synthesized six cocrystals of DHOXA to investigate their stability in pH 1.2 and 7.4 buffer and the reduction rate of producing OXA. Six cocrystals of DHOXA with oxalic acid, hydroquinone (HYD), benzoic acid, salicylic acid, 3,5-difluorobenzoic acid, and 3hydroxy-2-naphthoic acid were characterized by single-crystal X-ray diffraction, powder Xray diffraction, and thermal analysis. Further contrastive analysis of the dissolution behavior and reduction test of the six cocrystals of DHOXA showed that DHOXA-HYD dihydrate (DHOXA-HYD-DH) significantly improved the performances of the stability in hydrochloric acid (pH 1.2) and the reduction rate. Besides, the cytotoxicity studies showed that DHOXA-HYD-DH increased cytotoxicity to cancer cells and possessed higher safety. The study provides a new method to develop the OXA-based Pt(IV) complexes as prodrugs.

show abstract

Section: Synthesis Of Cocrystals 221 Synthesis Of Dhoxa−oamentioning

confidence: 99%

Strategy to Regulate the Stability and Reduction Rate of Oxaliplatin-Based Pt(IV) Complexes: Cocrystallization

Zhu,

Guo,

Yao

et al. 2023

Crystal Growth & Design

View full text Add to dashboard Cite

show abstract

“…Cocrystal preparation processes include solid-state grinding, solution-reaction crystallization, solvent evaporation, and slurry conversion, and have all been extensively reported to date. Numerous synthesis techniques have been utilized for the creation of pharmaceutical cocrystals [ 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 ]. In addition, pharmaceutical cocrystals are easier to produce than ECCs.…”

Section: New Energetic Cocrystalsmentioning

confidence: 99%

Recent Progress on Synthesis, Characterization, and Performance of Energetic Cocrystals: A Review

Sultan

Haq

et al. 2022

Molecules

View full text Add to dashboard Cite

In the niche area of energetic materials, a balance between energy and safety is extremely important. To address this “energy–safety contradiction”, energetic cocrystals have been introduced. The investigation of the synthesis methods, characteristics, and efficacy of energetic cocrystals is of the utmost importance for optimizing their design and development. This review covers (i) various synthesis methods for energetic cocrystals; (ii) discusses their characteristics such as structural properties, detonation performance, sensitivity analysis, thermal properties, and morphology mapping, along with other properties such as oxygen balance, solubility, and fluorescence; and (iii) performance with respect to energy contents (detonation velocity and pressure) and sensitivity. This is followed by concluding remarks together with future perspectives.

show abstract

“… 4 Using the amorphous form of poorly water-soluble drugs has become one of the most effective approaches to improve their solubility and dissolution rate and thus enhance drug bioavailability. 5 − 7 …”

Section: Introductionmentioning

confidence: 99%

“…It is a recognized fact that the majority of drug candidates in pharmaceutical development exhibit poor water solubility and are categorized as Class II or Class IV according to the Biopharmaceuticals Classification System (BCS). , Addressing this issue, the pharmaceutical industry has developed several strategies that include searching for appropriate solid forms such as polymorphs, salts, co-crystals, and amorphous phases . Using the amorphous form of poorly water-soluble drugs has become one of the most effective approaches to improve their solubility and dissolution rate and thus enhance drug bioavailability. − …”

Section: Introductionmentioning

confidence: 99%

Introduction to Pharmaceutical Co-amorphous Systems Using a Green Co-milling Technique

et al. 2023

View full text Add to dashboard Cite

The concept of co-amorphous systems is introduced in an integrated laboratory experiment, designed for advanced chemistry students, using solvent-free, environmentally friendly mechanochemistry. The dual-drug naproxen-cimetidine co-amorphous system (NPX-CIM) is investigated as an example of the emergent field of medicinal mechanochemistry. Students are trained in solid-state characterization techniques including X-ray powder diffraction, Fourier-transform infrared spectroscopy, and thermal analysis by differential scanning calorimetry. This lab experiment also provides an opportunity to discuss the relevance of different solid forms of pharmaceutics, emphasizing particular properties of disordered materials. This experiment can easily fit the curriculum of any Chemistry or Pharmacy master level degree in courses dealing with instrumental analysis, solid state chemistry, or green chemistry, for classes of 6 to 18 students, in a 5-h lab session. Suggestions to adapt it to the use of a single characterization technique are provided.

show abstract

Effect of mechanochemical grinding conditions on the formation of pharmaceutical cocrystals and co-amorphous solid forms of ketoconazole – Dicarboxylic acid

Cited by 17 publications

References 51 publications

Strategy to Regulate the Stability and Reduction Rate of Oxaliplatin-Based Pt(IV) Complexes: Cocrystallization

Strategy to Regulate the Stability and Reduction Rate of Oxaliplatin-Based Pt(IV) Complexes: Cocrystallization

Recent Progress on Synthesis, Characterization, and Performance of Energetic Cocrystals: A Review

Introduction to Pharmaceutical Co-amorphous Systems Using a Green Co-milling Technique

Contact Info

Product

Resources

About