Preparation and characterization of co-amorphous Ritonavir–Indomethacin systems by solvent evaporation technique: Improved dissolution behavior and physical stability without evidence of intermolecular interactions

Dengale, Swapnil J.; Ranjan, Om Prakash; Hussen, Syed Sajjad; Krishna, Bandarupalli; Musmade, Prashant B; Shenoy, Gautham G.; Bhat, Krishnamurthy

doi:10.1016/j.ejps.2014.05.015

Cited by 128 publications

(67 citation statements)

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“…The XRD results (Figure 4) also confirm the interactions and formation of single homogenous phase by the appearance of the amorphous halo characteristic of single co-amorphous dispersions (Löbmann et al, 2013;Dengale et al, 2014).…”

Section: Discussionsupporting

confidence: 53%

In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids

et al. 2016

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Improvement of water solubility, dissolution rate, oral bioavailability, and reduction of first pass metabolism of OL (OL), were the aims of this research. Co-amorphization of OL carboxylic acid dispersions at various molar ratios was carried out using rapid solvent evaporation. Characterization of the dispersions was performed using differential scanning calorimetry (DSC), Fourier transform infrared spectrometry (FTIR), X-ray diffractometry (XRD), and scanning electron microscopy (SEM). Dispersions with highest equilibrium solubility were formulated as fast dissolving oral films. Modeling and optimization of film formation were undertaken using artificial neural networks (ANNs). The results indicated co-amorphization of OL-ascorbic acid through H-bonding. The co-amorphous dispersions at 1:2 molar ratio showed more than 600-fold increase in solubility of OL. The model optimized fast dissolving film prepared from the dispersion was physically and chemically stable, demonstrated short disintegration time (8.5 s), fast dissolution (97% in 10 min) and optimum tensile strength (4.9 N/cm 2 ). The results of in vivo data indicated high bioavailability (144 ng h/mL) and maximum plasma concentration (14.2 ng/mL) compared with the marketed references. Therefore, the optimized co-amorphous OL-ascorbic acid fast dissolving film could be a valuable solution for enhancing the physicochemical and pharmacokinetic properties of OL.

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Section: Discussionsupporting

confidence: 53%

In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids

et al. 2016

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“…There is an increased interest in the binary glassy materials containing two small molecules, due to the disadvantages of solid dispersion technology which includes system tackiness, phase separation, reduced glass transition temperature due to hygroscopicity [9][10][11][12][13][14][15][16]. It uses small molecules as a stabilizing agent instead of using polymers, which is devoid of problems faced by solid dispersion technology.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous improvement of solubility and permeability by fabricating binary glassy materials of Talinolol with Naringin: Solid state characterization, in-vivo in-situ evaluation

Teja

Musmade

Khade

et al. 2015

European Journal of Pharmaceutical Sciences

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“…The solvent was evaporated under reduced at room temperature by using petridish and the resulting residue dried under vacuum for 3 h. The mixture was stored overnight in a desiccator. The hardened mixture was powdered in a mortar, sieved through a 100-mesh screen, and stored in a screw-cap vial at room temperature until further use 16 .…”

Section: Preparation Of Gliclazide Solid Dispersions (Sds)mentioning

confidence: 99%

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2018

IJPSR

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In order to effectively manage the diabetic mellitus type-II hyperglycemic surge, bilayered tablets comprising of gliclazide in immediate release layer (IRL) and metformin in sustained release layer (SRL) have been designed and fabricated for years. Gliclazide suffers from reduced aqueous solubility of 0.19 mg/mL which remained a crucial problem for the biological effect as a result of reduced dissolution and bioavailability. Therefore, in this research an effort was done to improve the aqueous solubility of gliclazide in a bilayer tablet by forming solid dispersions which will provide prompt release to completely manage the postprandial effectually. In this study, a bilayer tablet of gliclazide solid dispersion in IRL and metformin in SRL were fabricated by direct compression method, with an intention that the IRL of the formulation will release the gliclazide at its earliest to combat the postprandial hyperglycemic level followed by a control of steady state plasma glucose by sustained release metformin. The compatibility studies, pre-compression studies, post-compression studies, disintegration studies, dissolution studies, and kinetic release studies were performed. The formulation B3 was found to be highly optimized and demonstrated the highest cumulative drug release where the metformin followed the either zero-order or first-order and the gliclazide followed anomalous diffusion. Therefore, the designed formulation will offer a better therapeutic regimen and provide patient friendly postprandial hypoglycemic management, where an immediate control and maintenance dose are required.

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Preparation and characterization of co-amorphous Ritonavir–Indomethacin systems by solvent evaporation technique: Improved dissolution behavior and physical stability without evidence of intermolecular interactions

Cited by 128 publications

References 20 publications

In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids

In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids

Simultaneous improvement of solubility and permeability by fabricating binary glassy materials of Talinolol with Naringin: Solid state characterization, in-vivo in-situ evaluation

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