Dissolution Behavior of Probucol from Solid Dispersion Systems of Probucol-Polyvinylpyrrolidone.

Yagi, Naomi; Terashima, Yuhji; Kenmotsu, Harumi; Sekikawa, Hitoshi

doi:10.1248/cpb.44.241

Cited by 60 publications

(44 citation statements)

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“…The dissolution medium was 900 mL of 0.1 N HCl. Samples were withdrawn from the dissolution vessels at selected time intervals (5,10,15,20,30,45,60,90,120, and 150 min), and piroxicam was quantified at 328.8 nm with a UV spectrophotometer (Shimadzu, Japan). Each sample was replaced with fresh dissolution medium.…”

Section: Dissolution Studiesmentioning

confidence: 99%

“…The drug and stabilizing agent concentration, homogenization speed, and stabilizer type had a significant effect (p < 0.05) on DE 150 of gliclazide microcrystals prepared by the solvent-change method (30). A linear model was fitted to the effect of drug concentration and homogenization speed on DE 150 .…”

Section: Dissolution Studiesmentioning

confidence: 99%

“…Accordingly, DE 150 decreased linearly with increasing drug concentration at all homogenization speeds. Mixing the drug powder with polymers resulted in increased wettability and dissolution surface area and reduced interfacial tension between the dissolution medium and the hydrophobic drug surface (30).…”

Section: Dissolution Studiesmentioning

confidence: 99%

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Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques

Varshosaz¹,

Khajavinia²,

Ghasemlu³

et al. 2013

Dissolution Technol.

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Piroxicam is a nonsteroidal anti-inflammatory drug that is practically insoluble in water. The oral absorption rate of piroxicam is dependent on its dissolution rate in the GI tract. The aim of this study was to enhance the dissolution of piroxicam by a microcrystallization technique. The preparation of microcrystals of piroxicam was done by two methods, solvent change and pH shift. In the solvent-change method, the drug was dissolved in acetone, and the stabilizer was dissolved in water. The aqueous phase was added to acetone under homogenization in an ice bath for 1 min. In the pH-shift method, the drug and stabilizer were both dissolved in 0.1 N NaOH (pH 12) using homogenization. The pH was adjusted to 3 using 0.1 N hydrochloric acid. Dissolution testing was carried out in a hydrochloric acid medium using the rotating basket method. Particle size and morphology, FTIR, DSC, XRD, and surface area of the microcrystals were studied. The effects of drug and stabilizer concentration and homogenization rate on particle size and dissolution efficiency were studied statistically using a D-optimal design. The dissolution efficiency in both methods was increased about 3-to 4-fold. The particle size in both methods was decreased in comparison with untreated drug. Maximum dissolution and minimum particle size were obtained by the solvent-change method. According to the results, both microcrystallization methods are effective in the modification of the crystalline the habit of piroxicam.

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Section: Dissolution Studiesmentioning

confidence: 99%

Section: Dissolution Studiesmentioning

confidence: 99%

See 1 more Smart Citation

Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques

Varshosaz¹,

Khajavinia²,

Ghasemlu³

et al. 2013

Dissolution Technol.

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“…12 The use of hydrophilic polymers as carriers for the dissolution enhancement of poorly water-soluble drug is increasing. 13,14 Various hydrophilic carriers such as polyethylene, 15 polyvinylpyrrolidone 16 and sugars 17 have been investigated for improvement of dissolution characteristics and bioavailability of poorly water soluble drugs. Polyvinylpyrrolidone (PVP) has been used for the preparation of solid dispersion of loratadine using rotary evaporation and spray-drying solvent evaporation techniques.…”

Section: -10mentioning

confidence: 99%

Enhancement of Dissolution Profile of Poorly Water Soluble Loratadine by Solid Dispersion Technique

Uddin

Chowdhury

Hasan

et al. 2017

Dhaka Univ. J. Pharm. Sci

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This study was carried out to improve the dissolution properties of loratadine by solid dispersion technique. A series of solid dispersions of loratadine in PVP K-30 (1:1, 1:3 and 1:5) were prepared by kneading technique. The prepared solid dispersions were characterized by various physicochemical properties (fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy) and the dissolution characteristics were compared with loratadine and the physical mixtures of loratadine. It was revealed from the physicochemical analyses that there was a good compatibility between drug and carrier. On the other hand, the drug release from the prepared binary solid dispersions was significantly enhanced in comparison to both drug alone and the physical mixtures. Finally solid dispersion of loratadine: PVP K-30 prepared as 1:5 ratio was found to be described by non-Fickian release mechanism and was selected as the best formulation in this study.

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“…1) Probucol can not be injected intravenously due to the poor water solubility (5 ng/ml at 25°C). 1,2) The bioavailability of probucol is very poor (up to 6%) through oral administration.…”

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confidence: 99%

In Vivo Assessment of Oral Administration of Probucol Nanoparticles in Rats

Shudo

Pongpeerapat

Wanawongthai

et al. 2008

Biological & Pharmaceutical Bulletin

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Pharmacokinetic profiles of probucol were evaluated after oral administration of the various nanosuspensions in rats. Probucol nanoparticles were prepared by co-grinding with various molecular weights of polyvinylpyrrolidone (PVP K12, PVP K17 and PVP K30) and sodium dodecyl sulfate (SDS). The average particle sizes of probucol after dispersing the ternary ground mixtures (GMs), probucol/PVP K12/SDS, probucol/PVP K17/SDS and probucol/PVP K30/SDS into water were 28, 75 and 89 nm respectively. The ternary GM suspensions with PVP K17/SDS and PVP K30/SDS were stable at 25°C. However the particle size of probucol from the ternary GM with PVP K12/SDS gradually increased. Pharmacokinetic profiles of probucol indicated that variation in particle surface condition covered with PVP and SDS in addition to the particle size affected the improvement of in vivo absorption of probucol. The ternary GM with PVP K12/SDS exhibited a superior improvement of probucol absorption compared to the GMs with PVP K17/SDS and PVP K30/SDS. The binary GM with PVP or SDS and physical mixtures with PVP and/or SDS did not show significant differences in the area under the plasma concentration-time curve compared to the unprocessed probucol. In conclusion, preparation of probucol nanoparticles by co-grinding with PVP K12 and SDS could be a promising method for bioavailability enhancement.

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Dissolution Behavior of Probucol from Solid Dispersion Systems of Probucol-Polyvinylpyrrolidone.

Cited by 60 publications

References 0 publications

Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques

Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques

Enhancement of Dissolution Profile of Poorly Water Soluble Loratadine by Solid Dispersion Technique

In Vivo Assessment of Oral Administration of Probucol Nanoparticles in Rats

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