Microparticle size control and glimepiride microencapsulation using spray congealing technology

Ilić, Ilija; Dreu, Rok; Burjak, Matejka; Homar, Miha; Kerč, Janez; Srčič, Stanko

doi:10.1016/j.ijpharm.2009.05.011

Cited by 88 publications

(84 citation statements)

References 28 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%

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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%

“…Savolainen et al have found that the drug crystallinity of spray-congealed products plays a more significant role in drug release than the matrix lipophilicity (14). However, some studies have reported that the spray congealing process does not affect the crystallinity of the drug (15,16).…”

Section: Introductionmentioning

confidence: 99%

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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“…However, the drawback for the use of GM as oral dosage forms is attributable to its low aqueous solubility (1.6 µg/mL) and slow dissolution rate, which lead to low oral bioavailability. 6,7 Hence many studies have tried to enhance its solubility, and several reports including those where nanocrystals, 8 cosolvency, 9 spray congealing, 10 solid self-nanoemulsify,…”

Section: Introductionmentioning

confidence: 99%

Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique

Li¹,

Pan²,

Cui³

et al. 2016

IJN

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The objective of this work was to prepare an oil/water glimepiride (GM) microemulsion (ME) for oral administration to improve its solubility and enhance its bioavailability. Based on a solubility study, pseudoternary phase diagrams, and Box–Behnken design, the oil/water GMME formulation was optimized and prepared. GMME was characterized by dynamic laser light scattering, zeta potential, transmission electron microscopy, and viscosity. The in vitro drug release, storage stability, pharmacodynamics, and pharmacokinetics of GMME were investigated. The optimized GMME was composed of Capryol 90 (oil), Cremophor RH40 (surfactant), and Transcutol (cosurfactant), and increased GM solubility up to 544.6±4.91 µg/mL. The GMME was spherical in shape. The particle size and its polydispersity index were 38.9±17.46 nm and 0.266±0.057, respectively. Meanwhile, the GMME was physicochemically stable at 4°C for at least 3 months. The short-term efficacy in diabetic mice provided the proof that blood glucose had a consistent and significant reduction at a dose of 375 µg/kg whether via IP injection or IG administration of GMME. Compared with the glimepiride suspensions or glimepiride-meglumine complex solution, the pharmacokinetics of GMME in Wistar rats via IG administration exhibited higher plasma drug concentration, larger area under the curve, and more enhanced oral bioavailability. There was a good correlation of GMME between the in vitro release values and the in vivo oral absorption. ME could be an effective oral drug delivery system to improve bioavailability of GM.

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“…Poor dissolution and unsatisfied bioavailability of this drug are the results of this poor aqueous solubility (Frick et al, 1998). Previous reports on this drug revealed that dissolution rate is increased through formation of inclusion complex with cyclodextrin (Ammar et al, 2006) or preparation of solid dispersions using either water soluble carriers (Boregowda et al, 2011;Rajpurohit et al, 2011), insoluble carriers (Kiran et al, 2009;Reven et al, 2010;Vidyadhara et al, 2011) or preparation of spray congealed microparticles (Ilić et al, 2009). However, for improving its bioavailability only a few attempts have been made.…”

Section: Introductionmentioning

confidence: 99%

Dissolution enhancement of glimepiride dispersion using glyceryl monostearate and ?-cyclodextrin as carrier

Rafshanjani

Rahman

Parvin³

et al. 2015

Int Curr Pharm J

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Glimepiride is an antidiabetic drug of sulfonylurea group and indicated for the treatment of type 2 diabetes mellitus. The present study was conducted to enhance the dissolution rate of glimepiride solid lipid nano particle dispersions using hot homogenization method and glimepiride solid dispersion by precipitation method. Solid lipid nanoparticles have been used as suitable carriers for delivery of drug with poor solubility. In this investigation glyceryl monostearate and stearic acid were used as solid lipid, Lutrol F-68 as surfactant, Tween 80 as stabilizer and the used polymer were urea crystal and ?-cyclodextrin. Three formulations were prepared in different ratios for two methods and were designated as GMLN1 to GMLN3 in case of hot homogenization method and GMP1 to GMP3 for precipitation method. The evaluation of all the dispersions were done by in vitro dissolution studies using US Pharmacopeia type II apparatus (paddle method) in 900ml distilled water at 50 rpm to a temperature of 37°C ± 0.5°C for 45 minutes. In situ and externally sink method revealed the release pattern of drug was found to follow zero order, first order and Korsmeyer-Peppas equations. Improved dissolution profile was observed in all the solid lipid nano particle dispersions as compared to pure drug as well as market preparation. Thus, glyceryl monostearate and ?-cyclodextrin can be successfully used as carrier for improvement of dissolution and bioavailability of glimepiride.Rafshanjani et al., International Current Pharmaceutical Journal, September 2015, 4(10): 436-441

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Microparticle size control and glimepiride microencapsulation using spray congealing technology

Cited by 88 publications

References 28 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

Improved oral bioavailability of poorly water-soluble glimepiride by utilizing microemulsion technique

Dissolution enhancement of glimepiride dispersion using glyceryl monostearate and ?-cyclodextrin as carrier

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