Characterization of Carbamazepine–Gelucire 50/13 Microparticles Prepared by a Spray-congealing Process Using Ultrasounds

Passerini, Nadia; Perissutti, Beatrice; Moneghini, Mariarosa; Voinovich, Dario; Albertini, Beatrice; Cavallari, Cristina; Rodriguez, Lorenzo

doi:10.1002/jps.10085

Cited by 104 publications

(85 citation statements)

References 15 publications

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“…The reduction in drug crystallinity was also affirmed in other studies using olanzapine, felodipine, avobenzone and salbutamol sulphate (22)(23)(24)(25). However, there were also studies which showed that the spray congealing process had little impact on drug crystallinity of carbamazepine, praziquantel, glimepiride, verapamil or theophylline (15,16,(26)(27)(28). Various factors can affect the crystallinity of the drug such as the viscosity of the carrier used and the cooling rate of the spray congealing process.…”

Section: Crystallinity Of Mnz In Spray-congealed Microparticlesmentioning

confidence: 72%

Influence of Hydroxypropyl Methylcellulose on Metronidazole Crystallinity in Spray-Congealed Polyethylene Glycol Microparticles and Its Impact with Various Additives on Metronidazole Release

Heng

Chan

2015

AAPS PharmSciTech

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Abstract. The purpose of this study was to investigate the effect of a hydrophilic polymer, hydroxypropyl methylcellulose (HPMC), on the crystallinity and drug release of metronidazole (MNZ) in spraycongealed polyethylene glycol (PEG) microparticles and to further modify the drug release using other additives in the formulation. HPMC has been used in many pharmaceutical formulations and processes but to date, it has not been employed as an additive in spray congealing. Crystallinity of a drug is especially important to the development of pharmaceutical products as active pharmaceutical ingredients (APIs) are mostly crystalline in nature. A combination of X-ray diffractometry, differential scanning calorimetry, Raman spectroscopy and Fourier transform-infrared spectroscopy (FT-IR) spectroscopy was employed to investigate the degree of crystallinity and possible solid-state structure of MNZ in the microparticles. The microparticles with HPMC were generally spherical. Spray congealing decreased MNZ crystallinity, and the presence of HPMC reduced the drug crystallinity further. The reduction in MNZ crystallinity was dependent on the concentration of HPMC. Smaller HPMC particles also resulted in a greater percentage reduction in MNZ crystallinity. Appreciable modification to MNZ release could be obtained with HPMC. However, this was largely attributed to the role of HPMC in forming a diffusion barrier. Further modification of drug release from spray-congealed PEG-HPMC microparticles was achieved with the addition of 5% w/w dicalcium phosphate but not with magnesium stearate, methyl cellulose, polyvinylpyrrolidone, silicon dioxide and sodium oleate/citric acid. Dicalcium phosphate facilitated formation of the diffusion barrier.

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Section: Crystallinity Of Mnz In Spray-congealed Microparticlesmentioning

confidence: 72%

Influence of Hydroxypropyl Methylcellulose on Metronidazole Crystallinity in Spray-Congealed Polyethylene Glycol Microparticles and Its Impact with Various Additives on Metronidazole Release

Heng

Chan

2015

AAPS PharmSciTech

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“…To get evidence of possible chemical interaction of drug with the Gelucires, FTIR analysis was used (31,32). Figure 4 shows the IR spectra of MS, Gelucire 43/01, Gelucire 44/14, and the F9 formulation.…”

Section: Resultsmentioning

confidence: 99%

Formulation and Characterization of Floating Gelucire Matrices of Metoprolol Succinate

Siripuram¹,

Bandari²,

Jukanti³

et al. 2010

Dissolution Technol.

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The aim of the current investigation was to formulate floating sustained-release matrices of metoprolol succinate using Gelucire 43/01 and Gelucire 44/14 by a melt-solidification technique. The in vitro and in vivo characteristics of the prepared matrices were evaluated. The in vitro drug release studies performed in 0.1 N HCl revealed a proportional increase in drug release pattern with increased concentration of Gelucire 44/14.Drug release data were analyzed by various mathematical models, and the mean dissolution time, Dissolution Efficiency, and similarity factor (f 2 ) were determined in optimizing formulations. Differential scanning calorimetry and Fourier transform infrared spectroscopy showed no chemical interaction between drug and carriers studied. The in vitro floating characteristics of Gelucire matrices were greater than 12 h with good in vivo gastric retention. The results indicate that Gelucire 43/01 is an appropriate carrier for the development of sustained-release floating drug delivery systems and Gelucire 44/14, a highly hydrophilic and lipophilic balance (HLB) excipient, acts as release enhancer in the formulations studied.

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“…Fouad et al [16] showed that the increased dissolution rate of celecoxib in spray-dried mixtures of KL IR and other excipients was due to improving drug wettability. Also, the inherently higher dissolution rate of the soluble polymer introduces the less-soluble drug as finely divided particles into the dissolution medium [17]. Furthermore, Janssens et al [18] explained that a significant decrease of the drug particle size, possibly to the molecular level, in combination with an additional effect of the codissolving hydrophilic carrier on the drugs solubility, might decrease the time required for complete dissolution.…”

Section: In Vitro Dissolution Profiles Of Abz From Kl and Pvp Binary mentioning

confidence: 99%

Albendazole Microparticles Prepared by Spray Drying Technique: Improvement of Drug Dissolution

Ibrahim¹,

Shazly²,

El-Badry³

2015

Trop. J. Pharm Res

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Characterization of Carbamazepine–Gelucire 50/13 Microparticles Prepared by a Spray-congealing Process Using Ultrasounds

Cited by 104 publications

References 15 publications

Influence of Hydroxypropyl Methylcellulose on Metronidazole Crystallinity in Spray-Congealed Polyethylene Glycol Microparticles and Its Impact with Various Additives on Metronidazole Release

Influence of Hydroxypropyl Methylcellulose on Metronidazole Crystallinity in Spray-Congealed Polyethylene Glycol Microparticles and Its Impact with Various Additives on Metronidazole Release

Formulation and Characterization of Floating Gelucire Matrices of Metoprolol Succinate

Albendazole Microparticles Prepared by Spray Drying Technique: Improvement of Drug Dissolution

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