Pharmaceutical co‐crystal: An alternative strategy for enhanced physicochemical properties and drug synergy

Ngilirabanga, Jean Baptiste; Samsodien, Halima

doi:10.1002/nano.202000201

Cited by 36 publications

(29 citation statements)

References 104 publications

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“…Utilizing a laboratory RAM resonant acoustic blender operating at 80−100G and 60 Hz, a series of carbamazepine co-crystals have been efficaciously formed. The co-crystal product has been separated at a wide array of gauges from the lab, 100 mg, 1.5 g, and 22 g, and the equipment seems to hold itself up to scale [37].…”

Section: Acoustic Resonant Mixingmentioning

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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Section: Acoustic Resonant Mixingmentioning

confidence: 99%

Chemistry and Modern Techniques of Characterization of Co-Crystals

Ali¹,

Кузнецов²,

Ibrahim³

et al. 2023

Drug Formulation Design

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show abstract

“…This co crystallization process to improve the physicochemical properties of the drugs. The salt formation during co crystallization are found in micronization and amorphization [16]. Segments connect through non-covalent collaborations, for example, hydrogen holding, particle associations, van der Waals communications, and PARcooperation's [17].…”

Section: Propertiesmentioning

confidence: 99%

A Comprehensive Mini Review on Co-Crystallization Process

Das

Amin

Sarma

et al. 2021

JPRI

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Co‑crystal chemistry has recently attracted supramolecular scientists. Co-crystals are comprising of hydrogen bonding assembly between different molecules. Many issues related to the performance characteristics of an active pharmaceutical ingredient (API) can be resolved using the co-crystallization approach. A proper understanding of the crystal structure of an API is required for the successful formation of co-crystals with the selected co‑former. Co-crystal chemistry has recently attracted scientists from the super molecules. Co crystals consist of the assembly of hydrogen bonds between various molecules. Many problems related to the performance characteristics of an active pharmaceutical ingredient (API) can be solved using the method of co-crystallization. Co-Crystals offer an alternate pathway where any API, paying little mind to be acidic, essential, or ionizable gatherings, might be co-gem. This aspect also helps to complement existing methods by reintroducing molecules with limited pharmaceutical profiles based on their non-ionizable functional groups.

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“…It is only applicable to APIs with ionizable moieties [ 9 ]. Cocrystal formation has been introduced as a promising alternative to commonly used solid form control strategies [ 10 , 11 , 12 ]. It can afford a broad platform for optimizing API properties based on the pharmaceutical development requirements.…”

Section: Introductionmentioning

confidence: 99%

Formation of Ciprofloxacin–Isonicotinic Acid Cocrystal Using Mechanochemical Synthesis Routes—An Investigation into Critical Process Parameters

et al. 2022

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The mechanochemical synthesis of cocrystals has been introduced as a promising approach of formulating poorly water-soluble active pharmaceutical ingredients (APIs). In this study, hot-melt extrusion (HME) as a continuous process and grinding and ball milling as batch processes were employed to explore the feasibility of cocrystallization. Ciprofloxacin (CIP) and isonicotinic acid (INCA) were selected as the model API and coformer. CIP–INCA cocrystal was produced in all techniques. It was revealed that higher cocrystal content could be achieved at longer durations of grinding and ball milling. However, milling for more than 10 min led to increased co-amorphous content instead of cocrystal. A design of experiment (DoE) approach was used for deciphering the complex correlation of screw configuration, screw speed, and temperature as HME process parameters and their respective effect on final relative cocrystal yield. Statistical analysis showed that screw configuration, temperature, and their interaction were the most critical factors affecting cocrystallization. Interestingly, screw speed had minimal impact on the relative cocrystallization yield. Cocrystallization led to increased dissolution rate of CIP in phosphate buffer up to 2.5-fold. Overall, this study shed a light on the potential of mechanochemical synthesis techniques with special focus on HME as a continuous process for producing cocrystals.

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Pharmaceutical co‐crystal: An alternative strategy for enhanced physicochemical properties and drug synergy

Cited by 36 publications

References 104 publications

Chemistry and Modern Techniques of Characterization of Co-Crystals

Chemistry and Modern Techniques of Characterization of Co-Crystals

A Comprehensive Mini Review on Co-Crystallization Process

Formation of Ciprofloxacin–Isonicotinic Acid Cocrystal Using Mechanochemical Synthesis Routes—An Investigation into Critical Process Parameters

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