Reliability of the Hansen solubility parameters as co-crystal formation prediction tool

Salem, Ala’; Nagy, Sándor; Pál, Szilárd; Széchenyi, Aleksandar

doi:10.1016/j.ijpharm.2019.01.007

Cited by 63 publications

(37 citation statements)

References 31 publications

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“…For the theoretical miscibility assessment, if the solubility parameter difference ( Δδ ) is less than 7.0 MPa 1/2 , the components are considered to have good miscibility. If Δδ is less than 2.0 MPa 1/2 , the components may possess excellent miscibility and easily form a solid solution, while Δδ greater than 10 MPa 1/2 indicates immiscibility between them [ 30 , 42 ]. Theoretical predicted δ using the Fedors and Hoftyzer–Van Krevelen methods are given in Supplementary Materials Table S1 .…”

Section: Resultsmentioning

confidence: 99%

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Han

et al. 2021

Pharmaceutics

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Different from previously reported co-amorphous systems, a co-amorphous curcumin-magnolol (CUR-MAG CM) system, as compared with its crystalline counterparts, exhibited decreased dissolution due to its aggregation during dissolution. The main purpose of the present study is to deaggregate CUR-MAG CM to optimize drug dissolution and explore the deaggregation mechanism involved. Herein, a small amount of polymer (HPMC, HPC, and PVP K30) was co-formulated at 5% (w/w) with CUR-MAG CM as ternary co-amorphous systems. The polymer addition changed the surface properties of CUR-MAG CM including improved water wettability enhanced surface free energy, and hence exerted a deaggregating effect. As a result, the ternary co-amorphous systems showed faster and higher dissolution as compared with crystalline CUR/MAG and CUR-MAG CM. In addition, the nucleation and crystal growth of dissolved CUR and MAG molecules were significantly inhibited by the added polymer, maintaining a supersaturated concentration for a long time. Furthermore, polymer addition increased the Tg of CUR-MAG CM, potentially involving molecular interactions and inhibiting molecular mobility, resulting in enhanced physical stability under 25 °C/60% RH and 40 °C/75% RH conditions. Therefore, this study provides a promising strategy to optimize the dissolution and physical stability of co-amorphous systems by deaggregation and crystallization inhibition via adding small amounts of polymers.

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Section: Resultsmentioning

confidence: 99%

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Han

et al. 2021

Pharmaceutics

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“…This in vitro dissolution study indicates the significant contribution of multicomponent crystal engineering in solubility enhancement and drug release of LMG [Figure 5]. [28] Comparative in vitro dissolution study of tablet formulation of LMG and LMG-AA eutectics reveal the advantage of eutectics formation in solubility, drug release, and dissolution. LMG-AA eutectic tablet showed near about double drug release as compare to pure LMG tablet.…”

Section: Comparative In Vitro Dissolution Analysis Of Lmg and Lmg Eutectics Tabletsmentioning

confidence: 84%

Untitled

Kulkarni¹

2021

AJP

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Objective: Lamotrigine (LMG) is the Biopharmaceutical Classification System Class-II drug with hurdle in drug release and dissolution efficiency due to poor water solubility. The present investigation was aimed to improve the solubility and dissolution of LMG by crystal engineering by formation of cocrystals but which accidently turn toward eutectics formation. Methods: LMG was subjected to neat grinding with different Cocrystal Formers (CCF) to develop multicomponent crystalline system. The prepared multicomponent system was analyzed by Differential Scanning Calorimetry, Raman spectroscopy, and Powder X-ray Diffraction reveals the formation of multicomponent system. Improved dissolution was interpreted by comparative drug release study of tablet formulation of unprocessed drug and eutectics. Results: There was unplanned formation of eutectics of LMG-Ascorbic acid (LMG-AA) that was observed with improved drug solubility. LMG-AA eutectics showed enhanced solubility (651.61 ± 1.02 µg/ml) in comparison with pure drug (161.46 ± 0.86 µg/ml) and all remaining multicomponent systems formed with other CCF's. The LMG-AA eutectics showed comparatively better drug release than pure LMG tablet. LMG eutectics also showed significant improvement in flow properties and compressibility as compared to pure drug. Conclusion: Multicomponent LMG-AA eutectics although formed in unplanned way they effectively enhances the solubility of LMG serving the main purpose of the research work. It can be utilized efficiently for drug delivery due to its improved dissolution and better drug release.

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“…However, the selection of coforms has still largely relied on trial and error, which is time consuming and labor-intensive. Recently, a variety of computer-assisted approaches have emerging as attractive tools to accelerate the screening process of cocrystals 214 , 215 , 216 , 217 , 218 . For example, the artificial neural network models are developed to predict cocrystal formation by analyzing a network of coformers extracted from the Cambridge Structural Database (CSD) 218 .…”

Section: Concluding Remarks and Future Perspectivesmentioning

confidence: 99%

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

Guo

Sun

Chen

et al. 2021

Acta Pharmaceutica Sinica B

151

106

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Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.

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Reliability of the Hansen solubility parameters as co-crystal formation prediction tool

Cited by 63 publications

References 31 publications

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Untitled

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

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