Insight into the Mechanisms of Cocrystallization of Pharmaceuticals in Supercritical Solvents

Padrela, Luís; Rodrigues, Miguel A.; Tiago, João; Velaga, Sitaram P.; Matos, Henrique A.; Azevedo, Edmundo Gomes de

doi:10.1021/acs.cgd.5b00200

Cited by 45 publications

(48 citation statements)

References 28 publications

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“…To determine changes in chemical structure and molecular interactions that occur in the cocrystal lattice. The cocrystal sample was formed by KBr crystal pellets and measured using an IR spectrophotometer at a wavenumber of 4000-400 cm-1, [65].…”

Section: Ftir-spectrophotometerymentioning

confidence: 99%

Systematic Review: Cocrystal as Efforts to Improve Physicochemical and Bioavailability Properties of Oral Solid Dosage Form

et al. 2021

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Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability.

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Section: Ftir-spectrophotometerymentioning

confidence: 99%

Systematic Review: Cocrystal as Efforts to Improve Physicochemical and Bioavailability Properties of Oral Solid Dosage Form

et al. 2021

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“…These modifications include (a) rapid expansion of the supercritical solution into a liquid solvent (RESOLV) [26][27][28][29] that contains polymers, surfactants, etc. ; (b) rapid expansion of the supercritical solution with an added solid co-solvent (RESS-SC) [30][31][32]; and (c) crystallization from supercritical solutions (CSS) [33,34]. Detailed discussion of these techniques is beyond the scope of this review.…”

Section: Rapid Expansion Of Supercritical Solutions (Ress) and Relatementioning

confidence: 99%

Using Supercritical Fluid Technology as a Green Alternative During the Preparation of Drug Delivery Systems

Chakravarty¹,

Famili²,

Nagapudi³

et al. 2019

Pharmaceutics

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Micro- and nano-carrier formulations have been developed as drug delivery systems for active pharmaceutical ingredients (APIs) that suffer from poor physico-chemical, pharmacokinetic, and pharmacodynamic properties. Encapsulating the APIs in such systems can help improve their stability by protecting them from harsh conditions such as light, oxygen, temperature, pH, enzymes, and others. Consequently, the API’s dissolution rate and bioavailability are tremendously improved. Conventional techniques used in the production of these drug carrier formulations have several drawbacks, including thermal and chemical stability of the APIs, excessive use of organic solvents, high residual solvent levels, difficult particle size control and distributions, drug loading-related challenges, and time and energy consumption. This review illustrates how supercritical fluid (SCF) technologies can be superior in controlling the morphology of API particles and in the production of drug carriers due to SCF’s non-toxic, inert, economical, and environmentally friendly properties. The SCF’s advantages, benefits, and various preparation methods are discussed. Drug carrier formulations discussed in this review include microparticles, nanoparticles, polymeric membranes, aerogels, microporous foams, solid lipid nanoparticles, and liposomes.

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“…Over the last years, the perception of cocrystal pharmaceutical engineering has gained great visibility [ 7 ]. A variety of cocrystal formation techniques are used in the pharmaceutical field, such as slow evaporation [ 8 ], solution crystallization [ 9 ], the anti-solvent method [ 10 ], mechanochemistry [ 11 ], melt crystallization [ 12 ], Sonic Slurry™ [ 13 ], solvo-thermal synthesis [ 14 ], the hot-melt extrusion method [ 15 ], the spray drying technique [ 16 ], supercritical solvent cocrystallization [ 17 ], and the reaction crystallization method (RCM) [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Obtaining Cocrystals by Reaction Crystallization Method: Pharmaceutical Applications

et al. 2021

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Cocrystals have gained attention in the pharmaceutical industry due to their ability to improve solubility, stability, in vitro dissolution rate, and bioavailability of poorly soluble drugs. Conceptually, cocrystals are multicomponent solids that contain two or more neutral molecules in stoichiometric amounts within the same crystal lattice. There are several techniques for obtaining cocrystals described in the literature; however, the focus of this article is the Reaction Crystallization Method (RCM). This method is based on the generation of a supersaturated solution with respect to the cocrystal, while this same solution is saturated or unsaturated with respect to the components of the cocrystal individually. The advantages of the RCM compared with other cocrystallization techniques include the ability to form cocrystals without crystallization of individual components, applicability to the development of in situ techniques for the screening of high quality cocrystals, possibility of large-scale production, and lower cost in both time and materials. An increasing number of scientific studies have demonstrated the use of RCM to synthesize cocrystals, mainly for drugs belonging to class II of the Biopharmaceutics Classification System. The promising results obtained by RCM have demonstrated the applicability of the method for obtaining pharmaceutical cocrystals that improve the biopharmaceutical characteristics of drugs.

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Insight into the Mechanisms of Cocrystallization of Pharmaceuticals in Supercritical Solvents

Cited by 45 publications

References 28 publications

Systematic Review: Cocrystal as Efforts to Improve Physicochemical and Bioavailability Properties of Oral Solid Dosage Form

Systematic Review: Cocrystal as Efforts to Improve Physicochemical and Bioavailability Properties of Oral Solid Dosage Form

Using Supercritical Fluid Technology as a Green Alternative During the Preparation of Drug Delivery Systems

Obtaining Cocrystals by Reaction Crystallization Method: Pharmaceutical Applications

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