Co-Crystals of Carvedilol: Preparation, Characterization and Evaluation

Thenge, Raju; Patel, Rakesh P.; Kayande, Nandu; Mahajan, Nilesh

doi:10.22159/ijap.2020v12i1.35640

Cited by 11 publications

(10 citation statements)

References 10 publications

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“…The phase transitions of pure CVD, physical mixture, and CVD solid dispersion were analyzed using the DSC method. Approximately 2 mg of the sample is heated over a temperature range of 25-180 °C at a rate of 10 °C /min under a nitrogen atmosphere (50 mL/min) [21][22].…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Solubility Enhancement of Carvedilol by Solid Dispersion Technique Using Sodium Alginate, Guar Gum, Xanthan Gum, and Locust Bean Gum as Polymers

et al. 2023

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Carvedilol (CVD) is a non-selective β-blocker. CVD is included in BCS class II. It has low water solubility. In this research, solid dispersion was used to increase the solubility and dissolution profile of CVD. In silico study using the ligand-ligand docking method. The preparation of solid dispersion using the kneading method with a weight ratio of 1:1, 1:2, 1:3, and 1:4, evaluation of solid dispersion includes solubility and dissolution. The best solid dispersion was characterized using FTIR, DSC, and PXRD. In silico study showed complexes CVD-SA, CVD-GG, CVD-XG and CVD-LBG have a hydrogen interaction. SA and XG were chosen as carriers in solid dispersion. CVD solid dispersion showed increased solubility in all samples, with the highest increase at 90.63 times at CVD: XG (1:4). The results of the dissolution profile obtained at 60 min are 64.95 ± 0.45% at pure CVD, 83.32 ± 1.19% at CVD:SA (1:4), and 72.56 ± 3.62% at CVD: XG (1:4). The FTIR spectrum indicates an interaction between CVD and SA. The thermogram indicated the amorphous drug, and the diffractogram showed a decrease in crystallinity. Solid dispersion is proven to increase the solubility and dissolution profile of CVD. Solid dispersion CVD: SA (1:4) showed the highest solubility and dissolution profile.

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Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Solubility Enhancement of Carvedilol by Solid Dispersion Technique Using Sodium Alginate, Guar Gum, Xanthan Gum, and Locust Bean Gum as Polymers

et al. 2023

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“…The samples for scanning electron microscopy were prepared by gently spreading the co-crystals on a double adhesive tape, which is stuck to an aluminum stub. The samples were then imaged using a 20 kV electron beam [41].…”

Section: Fourier Transform Infrared Spectroscopymentioning

confidence: 99%

Enhancement of Solubility and Dissolution Rate of Acetylsalicylic Acid via Co-Crystallization Technique: A Novel Asa-Valine Cocrystal

et al. 2021

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Objective: This study aims to synthesize acetylsalicylic acid (ASA) cocrystals using valine as a coformer via a co-crystallization technique to increase the solubility and dissolution rate of ASA. Methods: The ASA-valine cocrystal (1:1 molar ratio) was prepared using the solvent evaporation technique with ethanol: water (50:50). The cocrystal was characterized using Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), melting point to confirm the formation of cocrystal. The evaluation of cocrystal was done by drug content determination, solubility and dissolution studies. Results: The prepared cocrystal was successfully confirmed for the formation of a hydrogen bond. The melting point of prepared cocrystal was decreased compared to pure ASA and valine, which indicated the formation of a new crystalline form. The FT-IR studies showed the formation of a new hydrogen bond by shifting the-O-H,-C=O and-N-H functional groups. SEM studies ensured that the prepared cocrystals were in needle-like appearance. Finally, DSC and PXRD studies were also indicated the successful formation of ASA-valine cocrystal. The drug release of cocrystal was found to be 100% at 60th min. Where in the case of pure ASA and marketed product of ASA exhibited the dissolution rate of 59% and 69% at 60th min respectively. Conclusion: The co-crystallization technique can be adopted as the best strategy to increase the solubility and dissolution rate of BCS class 2 drugs. Therefore the prepared ASA-valine cocrystal can be a greater alternative to increase the solubility and dissolution rate compared with pure and marketed ASA.

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“…Angle of repose has been used to characterize the flow properties of a product, which is a characteristic related to interparticulate friction or resistance to movement between particles. This is the maximum angle possible between the surface of the pile of powder or granules and the horizontal plane where ϕ = angle of repose, h = height of heap, r = radius of base of heap circle.…”

Section: Experimental Sectionmentioning

confidence: 99%

Enhancing Stability and Formulation Capability of Fungicides by Cocrystallization through a Novel Multistep Slurry Conversion Process

Jin

Gong

et al. 2020

Crystal Growth & Design

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Solid agrochemicals with poor thermal stability pose a huge challenge to their production and application. Herein, two low-melting-point fungicides, pyraclostrobin (ZJ) and flusilazole (FZ), were designed to form cocrystals with the high melting point fungicide of thiophanate-methyl (TM), respectively. An infrequent multistep slurry conversion crystallization process was discovered and studied, which accelerated the formation of cocrystals, and the mechanism was revealed. Oiling-out of FZ and ZJ was the key process to multistep slurry conversion crystallization. The heterogeneous system possessed the advantage of high energy, which accelerated the synthesis of cocrystals. Furthermore, the variations of physicochemical properties containing thermal stability, tap density, formulation ability, and storage stability of both the parent fungicides and cocrystals were analyzed and compared. Packing coefficient and crystal structure analysis revealed the structure–property relationships of cocrystals. The single-crystal structure showed the strong N-H···N hydrogen bonds between the FZ and TM, and N-H···O and N-H···S interactions in the ZJ-TM cocrystal. Strong hydrogen bonds stabilize the structures of cocrystals, which enables ZJ-TM and FZ-TM to be made into a greener water suspension concentrate, instead of an emulsifiable concentrate with pollution.

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Co-Crystals of Carvedilol: Preparation, Characterization and Evaluation

Cited by 11 publications

References 10 publications

Solubility Enhancement of Carvedilol by Solid Dispersion Technique Using Sodium Alginate, Guar Gum, Xanthan Gum, and Locust Bean Gum as Polymers

Solubility Enhancement of Carvedilol by Solid Dispersion Technique Using Sodium Alginate, Guar Gum, Xanthan Gum, and Locust Bean Gum as Polymers

Enhancement of Solubility and Dissolution Rate of Acetylsalicylic Acid via Co-Crystallization Technique: A Novel Asa-Valine Cocrystal

Enhancing Stability and Formulation Capability of Fungicides by Cocrystallization through a Novel Multistep Slurry Conversion Process

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