Preparation and evaluation of ibuprofen beads by melt solidification technique

Paradkar, Anant; Maheshwari, Manish; Ketkar, Anant R; Chauhan, Bhaskar

doi:10.1016/s0378-5173(03)00081-4

Cited by 46 publications

(37 citation statements)

References 13 publications

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“…On the basis of this, MST was designed to obtain ibuprofen beads. 9 Because of its high melting point (114-117°C) flurbiprofen was never considered as a candidate for melt dispersion technique; however, in the present study flurbiprofen waxy beads were obtained by MST.…”

Section: Resultsmentioning

confidence: 91%

“…In melt dispersion technique, emulsification of melt is carried out at temperature above the melting point of the drug. But our recent report 9 on ibuprofen has shown that melt remains in liquid state up to a very low temperature and for a sufficient length of time, so that it can be emulsified below its melting point. On the basis of this, MST was designed to obtain ibuprofen beads.…”

Section: Resultsmentioning

confidence: 99%

“…7,8 Melt dispersion is generally carried out at temperature above melting point of drug. But recently, Paradkar et al 9 demonstrated that ibuprofen has low glass transition temperature (t g ) (<-30°C); hence, ibuprofen melt maintains liquid state for a sufficiently longer period of time, even at very low temperature. Therefore, in such cases melt emulsification can be carried out below the melting point of the drug.…”

Section: Introductionmentioning

confidence: 99%

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Preparation and characterization of flurbiprofen beads by melt solidification technique

et al. 2003

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KEYWORDS: flurbiprofen, melt solidification technique, factorial design, cetyl alcohol, response surface methodology, zero order kinetics A melt solidification technique has been developed to obtain sustained-release waxy beads of flurbiprofen. Low glass transition temperature (t g ) and shear-induced crystallization of flurbiprofen made it a suitable candidate for melt solidification technique. The process involved emulsification and solidification of flurbiprofen-cetyl alcohol melt at significantly low temperature (5°C). The effect of variables, namely, the amount of cetyl alcohol and the speed of agitation, was studied using 3 2 factorial design. The technique and the beads were evaluated on the basis of process and desired yield, surface topography, Fourier-transform infrared (FT-IR), differential scanning calorimetry (DSC), particle size distribution, crushing strength, and drug release. Average values for process and desired yields were 97% wt/wt and 26% wt/wt, respectively. No interaction was observed between drug and excipient. Multiple regression analysis was carried out, and response surfaces were obtained. A curvilinear relationship was observed between percentage of desired yield and the amount of cetyl alcohol. Linear decrease in crushing strength was observed with increase in the amount of cetyl alcohol. Drug released from the beads followed zero order kinetics. Burst release was shown to a greater extent in beads containing a lower amount of cetyl alcohol. Response surfaces of time required for certain percentage of drug (t D %) showed that after critical concentration of about 20% of cetyl alcohol (400 mg/batch), no significant release retardant effect was observed.

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Section: Resultsmentioning

confidence: 91%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Preparation and characterization of flurbiprofen beads by melt solidification technique

et al. 2003

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“…This melted drug obtained from the melt solidification technique was induced and transformed into crystals by agitation. 42,45 The investigation of a correlation of T g and crystallization temperature (T cr ) of BaNaB 9 O 15 glass indicated that a low T g promoted a low T cr . 46 This correlation indicated that a lower T g system required higher activation energy for crystallization than a higher T g system.…”

Section: Transformation Of Emulsion Droplet Into Particlementioning

confidence: 99%

“…The melting point for both powder and nanocrystals was 77°C as reported previously. 24,42 TGA thermograms of ibuprofen powder and ibuprofen nanocrystals showed only one step of …”

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Transformation of eutectic emulsion to nanosuspension fabricating with solvent evaporation and ultrasonication technique

Phaechamud

Tuntarawongsa

2016

IJN

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Eutectic solvent can solubilize high amount of some therapeutic compounds. Volatile eutectic solvent is interesting to be used as solvent in the preparation of nanosuspension with emulsion solvent evaporation technique. The mechanism of transformation from the eutectic emulsion to nanosuspension was investigated in this study. The 30% w/w ibuprofen eutectic solution was used as the internal phase, and the external phase is composed of Tween 80 as emulsifier. Ibuprofen nanosuspension was prepared by eutectic emulsion solvent evaporating method followed with ultrasonication. During evaporation process, the ibuprofen concentration in emulsion droplets was increased leading to a drug supersaturation but did not immediately recrystallize because of low glass transition temperature ( T g ) of ibuprofen. The contact angle of the internal phase on ibuprofen was apparently lower than that of the external phase at all times of evaporation, indicating that the ibuprofen crystals were preferentially wetted by the internal phase than the external phase. From calculated dewetting value ibuprofen crystallization occurred in the droplet. Crystallization of the drug was initiated with external mechanical force, and the particle size of the drug was larger due to Ostwald ripening. Cavitation force from ultrasonication minimized the ibuprofen crystals to the nanoscale. Particle size and zeta potential of formulated ibuprofen nanosuspension were 330.87±51.49 nm and −31.1±1.6 mV, respectively, and exhibited a fast dissolution. Therefore, the combination of eutectic emulsion solvent evaporation method with ultrasonication was favorable for fabricating an ibuprofen nanosuspension, and the transformation mechanism was attained successfully.

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Reduktion der Prozessschritte durch unmittelbare Selbstbeschichtung von Partikeln

Römbach

Ulrich

2007

Chemie Ingenieur Technik

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An dem binären Stoffsystem Ibuprofen und Cetylpalmitat soll die Anwendbarkeit der Idee der unmittelbaren Selbstbeschichtung überprüft werden. Da die unmittelbare Selbstbeschichtung sehr stark von den thermophysikalischen Eigenschaften des Stoffsystems abhängt, werden das Phasendiagramm, der Trenneffekt während der Kristallisation sowie die thermische Stabilität des Stoffsystems untersucht. Zur Bestimmung des Phasendiagramms wird die Differential Scanning Calorimetry angewandt. Die thermische Stabilität der Reinstoffe wird mithilfe der Thermogravimetrie und der Pulverröntgendiffraktometrie überprüft.

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Preparation and evaluation of ibuprofen beads by melt solidification technique

Cited by 46 publications

References 13 publications

Preparation and characterization of flurbiprofen beads by melt solidification technique

Preparation and characterization of flurbiprofen beads by melt solidification technique

Transformation of eutectic emulsion to nanosuspension fabricating with solvent evaporation and ultrasonication technique

Reduktion der Prozessschritte durch unmittelbare Selbstbeschichtung von Partikeln

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