Improved dissolution and micromeritic properties of naproxen from spherical agglomerates: preparation, in vitro and in vivo characterization

Saritha, Damineni; Bose, P. Subhash Chandra; Madhuri, G. Sandhya; Nagaraju, R.

doi:10.1590/s1984-82502012000400010

Cited by 9 publications

(5 citation statements)

References 8 publications

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“…The spherical aggregates are formed by cluster of small particles that are characterized by both low density and contact area. This result in higher specific surface is associated to greater porosity [ 19 ]. Consequently, spherical phosphates are more suitable for their electrochemical performance because of the Li ion diffusion [ 20 ].…”

Section: Resultsmentioning

confidence: 99%

Statistical optimization of amorphous iron phosphate: inorganic sol–gel synthesis-sodium potential insertion

et al. 2021

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Iron phosphate, Fe2 (HPO4)3*4H2O, is synthesized at ambient temperature, using the inorganic sol–gel method coupled to the microwave route. The experimental conditions for the gelling of Fe (III)-H3PO4 system are previously defined. Potentiometric Time Titration (PTT) and Potentiometric Mass Titration (PMT) investigate the acid–base surface chemistry of obtained phosphate. Variations of surface charge with the contact time, Q a function of T, are examined for time contact varying in the range 0–72 h. The mass suspensions used for this purpose are 0.75, 1.25 and 2.5 g L−1. The point of zero charge (PZC) and isoelectric point (IEP) are defined using the derivative method examining the variations $$\frac{{{\text{dpH}}}}{{{\text{d}}t}} = f\left( {{\text{pH}}} \right)$$ dpH d t = f pH , at lower contact time. A shift is observed for PZC and IEP towards low values that are found to be 2.2 ± 0.2 and 1.8 ± 0.1, respectively. In acidic conditions, the surface charge behavior of synthesized phosphate is dominated by $$\overline{{ > {\text{POH}}}}$$ > POH ¯ group which pKa = 2.45 ± 0.15. Q against T titration method is performed for synthesized Fe2 (HPO4)3*4H2O in NaCl electrolytes. The maximal surface charge (Q) is achieved at the low solid suspension. Hence, for m = 0.75 g L−1, Q value of 50 coulombs is carried at μ = 0.1 and pH around 12, while charge value around 22 coulombs is reached in the pH range: 3–10. The effect of activation time, Q and pH on sodium insertion in iron phosphate, were fully evaluated. To determine the optimal conditions of the studied process, mathematical models are used develop response surfaces in order to characterize the most significant sodium interactions according to the variation of the pH, Q, the contact time and the contents of the synthesized material.

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Section: Resultsmentioning

confidence: 99%

Statistical optimization of amorphous iron phosphate: inorganic sol–gel synthesis-sodium potential insertion

et al. 2021

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“…Asterisks mark coincident peaks with literature data. [41][42][43][44] Table 1. Dissolution parameters of the untreated and laser-generated particles.…”

Section: Resultsmentioning

confidence: 99%

Efficient Synthesis of Submicrometer‐Sized Active Pharmaceuticals by Laser Fragmentation in a Liquid‐Jet Passage Reactor with Minimum Degradation

Friedenauer,

Buck,

Eberwein

et al. 2023

Part & Part Syst Charact

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One challenge in the development of new drug formulations is overcoming their low solubility in relevant aqueous media. Reducing the particle size of drug powders to a few hundred nanometers is a well‐known method that leads to an increase in solubility due to an elevated total surface area. However, state‐of‐the‐art comminution techniques like cryo‐milling suffer from degradation and contamination of the drugs, particularly when sub‐micrometer diameters are aspired that require long processing times. In this work, picosecond‐pulsed laser fragmentation in liquids (LFL) of dispersed drug particles in a liquid‐jet passage reactor is used as a wear‐free comminution technique using the hydrophobic oral model drugs naproxen, prednisolone, ketoconazole, and megestrol acetate. Particle size and morphology of the drug particles are characterized using scanning electron microscopy (SEM) and changes in particle size distributions upon irradiation are quantified using an analytical centrifuge. The findings highlight the superior fragmentation efficiency of the liquid‐jet passage reactor setup, with a 100 times higher fraction of submicrometer particles (SMP) of the drugs compared to the batch control, which enhances solubility and goes along with minimal chemical degradation (<1%), determined by attenuated total reflection‐Fourier transform infrared spectroscopy (ATR‐FTIR), high‐performance liquid chromatography (HPLC), and X‐ray diffraction (XRD). Moreover, the underlying predominantly photo‐mechanically induced laser fragmentation mechanisms of organic microparticles (MP) are discussed.

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“…The NPX/pHEMA spectra exhibits a shift in the broad absorption band of the hydroxyl group vibrations from 3472 to 3463 cm −1 and a shift of the sharp absorption band attributed to the carbonyl group (C=O) vibration of pHEMA from 1727.62 cm −1 to 1724.32 cm −1 . It is well known that the position of the vibration peak of the carbonyl group suggests that most of the carboxylic acid groups are associated with the intermolecular hydrogen bonds formed between the HEMA derived moieties and the acid groups [ 39 , 40 , 41 ]. In addition, the wide absorption band in the spectral region 3200–3600 cm −1 corresponding to the vibrations of the OH group also confirms that hydrogen bonds form in the structure of poly(2-hydroxyethyl methacrylate-co-acrylic acid).…”

Section: Resultsmentioning

confidence: 99%

Naproxen-Loaded Poly(2-hydroxyalkyl methacrylates): Preparation and Drug Release Dynamics

et al. 2022

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Poly(2-hydroxyethylmethacrylate)/Naproxen (NPX/pHEMA) and poly (2-hydroxypropyl methacrylate)/Naproxen (NPX/pHPMA) composites with different NPX content were prepared in situ by free radical photopolymerization route. The resulted hybrid materials were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning Electron microscopy (SEM), and X-ray diffraction (XRD). These composites have been studied as drug carrier systems, in which a comparison of the in vitro release dynamic of NPX between the two drug carrier systems has been conducted. Different factors affecting the performance of the release dynamic of this drug, such as the amount of Naproxen incorporated in the drug carrier system, the pH of the medium and the degree of swelling, have been investigated. The results of the swelling study of pHEMA and pHPMA in different media pHs revealed that the diffusion of water molecules through both polymer samples obeys the Fickian model. The “in vitro” study of the release dynamic of Naproxen from NPX/pHEMA and NPX/pHPMA drug carrier systems revealed that the higher percentage of NPX released was obtained from each polymer carrier in neutral pH medium, and the diffusion of NPX trough these polymer matrices also obeys the Fickian model. It was also found that the less the mass percent of NPX in the composites, the better its release will be. The comparison between the two drug carrier systems revealed that the pHEMA leads to the best performance in the release dynamic of NPX. Regarding Naproxen solubility in water, the results deducted from the “in vitro” study of NPX/pHEMA10 and NPX/pHPMA10 drug carrier systems revealed a very significant improvement in the solubility of NPX in media pH1 (2.33 times, 1.43 times) and 7 (3.32 times, 2.60 times), respectively, compared to those obtained by direct dissolution of Naproxen powder.

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Improved dissolution and micromeritic properties of naproxen from spherical agglomerates: preparation, in vitro and in vivo characterization

Cited by 9 publications

References 8 publications

Statistical optimization of amorphous iron phosphate: inorganic sol–gel synthesis-sodium potential insertion

Statistical optimization of amorphous iron phosphate: inorganic sol–gel synthesis-sodium potential insertion

Efficient Synthesis of Submicrometer‐Sized Active Pharmaceuticals by Laser Fragmentation in a Liquid‐Jet Passage Reactor with Minimum Degradation

Naproxen-Loaded Poly(2-hydroxyalkyl methacrylates): Preparation and Drug Release Dynamics

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