Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique

Jung, Jae‐Young; Yoo, Sun Dong; Lee, Sang‐Heon; Kim, Kye Hyun; Yoon, Doo-Sun; Lee, Kyuhyun

doi:10.1016/s0378-5173(99)00191-x

Cited by 197 publications

(93 citation statements)

References 15 publications

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“…An increase in the concentration of poloxamer 188 in the physical mixture samples increased the saturation solubility of MLX. This phenomenon could be attributed to an improvement of the MLX wettability because of high water solubility of poloxamer 188 (Jung et al, 1999). As shown in Table I, MLX SDs that contain MLX and poloxamer 188 (SD1, SD2 and SD3) show a significant increase in saturation solubility compared to the pure MLX and physical mixtures with the same ratios (p value<0.05).…”

Section: Saturation Solubility Of MLX Sds and Physical Mixturesmentioning

confidence: 73%

“…The interaction could decrease the number of available polar groups that could interact with water during the water sorption and dissolution phenomena. Moreover, the formation of the gel formed by crospovidone around the solid dispersions could increase the viscosity in the donor phase and decrease the saturation solubility of MLX (Jung et al, 1999;Punčochová et al, 2014).…”

Section: Saturation Solubility Of MLX Sds and Physical Mixturesmentioning

confidence: 99%

“…In SD1 and SD2, the saturation solubility of MLX increased after the amount of poloxamer 188 was raised. This was because of the high water solubility of poloxamer 188 (Jung et al, 1999). The preparation of the dosage form of solid dispersions (SDs) is a critical aspect that should be considered by scientists.…”

Section: Saturation Solubility Of MLX Sds and Physical Mixturesmentioning

confidence: 99%

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Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Shoormeij

Taheri

Homayouni

2018

Braz. J. Pharm. Sci.

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Meloxicam (MLX) is a non-steroidal, anti-inflammatory drug that is prescribed in the treatment of rheumatoid arthritis and osteoarthritis. MLX is practically insoluble in water and exhibits a slow onset of action. In this study, MLX solid dispersions (MLX SDs) were prepared to improve the water solubility of this poorly water-soluble drug. Then orally disintegrating tablets (ODT) of MLX were developed using MLX SD to decrease the onset of action of this drug. MLX, poloxamer 188, and crospovidone of different ratios were melted in molten poloxamer 188 as a hydrophilic carrier. The optimum SD with the highest saturation solubility in water (13.09±0.34 microgram/mL) consisting of MLX: poloxamer 188: crospovidone in the ratio of 1:2:0 was used for the preparation of MLX ODTs. MLX ODTs were prepared by the direct compression method and optimized by the 2 3 factorial design. The effect of the superdisintegrant concentration, the mannitol-avicel ratio, and the level of compression force on the disintegration time, hardness, and percent of dissolved MLX from MLX ODTs after 30 min was evaluated. DSC and XRD analysis approved an amorphous form of MLX in SDs. The optimized ODT formulation containing 10% of superdisintegrant, and mannitol and avicel in the ratio of 4:1 respectively was compressed using a high level of compression force. The optimized ODT showed hardness (34.37±2.1 N) and friability (1.26±0.04%). This formulation showed a rapid disintegration in 12.66±2.5 seconds, which 82.66±5.1% of the MLX released within 30 min. MLX ODTs, prepared from MLX SD, could be introduced as a suitable dosage form of MLX with improved solubility and the onset of action.

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Section: Saturation Solubility Of MLX Sds and Physical Mixturesmentioning

confidence: 73%

Section: Saturation Solubility Of MLX Sds and Physical Mixturesmentioning

confidence: 99%

Section: Saturation Solubility Of MLX Sds and Physical Mixturesmentioning

confidence: 99%

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Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Shoormeij

Taheri

Homayouni

2018

Braz. J. Pharm. Sci.

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“…Numerous studies have reported arginine to enhance the dissolution of various drugs such as meloxicam (11), indomethacin (12), and lornoxicam (13). Exhaustive research has been carried out on dissolution enhancement of drugs using water-insoluble polymers such as crospovidone (14,15) and enteric polymers such as hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, Eudragit® L100 and S100 (16), and Eudragit® E (17,18). As a rule, inclusion of water-soluble carriers results in a fast release of the drug from the matrix, and a poorly soluble or insoluble carrier leads to a slower release of the drug from the matrix (19,20).…”

Section: Introductionmentioning

confidence: 99%

Solid-State Characterization and Dissolution Properties of Meloxicam–Moringa Coagulant–PVP Ternary Solid Dispersions

et al. 2013

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Abstract. The effect of ternary solid dispersions of poor water-soluble NSAID meloxicam with moringa coagulant (obtained by salt extraction of moringa seeds) and polyvinylpyrrolidone on the in vitro dissolution properties has been investigated. Binary (meloxicam-moringa and meloxicam-polyvinylpyrrolidone (PVP)) and ternary (meloxicam-moringa-PVP) systems were prepared by physical kneading and ball milling and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry. The in vitro dissolution behavior of meloxicam from the different products was evaluated by means of United States Pharmacopeia type II dissolution apparatus. The results of solid-state studies indicated the presence of strong interactions between meloxicam, moringa, and PVP which were of totally amorphous nature. All ternary combinations were significantly more effective than the corresponding binary systems in improving the dissolution rate of meloxicam. The best performance in this respect was given by the ternary combination employing meloxicam-moringa-PVP ratio of [1:(3:1)] prepared by ball milling, with about six times increase in percent dissolution rate, whereas meloxicam-moringa (1:3) and meloxicam-PVP (1:4) prepared by ball milling improved dissolution of meloxicam by almost 3-and 2.5-folds, respectively. The achieved excellent dissolution enhancement of meloxicam in the ternary systems was attributed to the combined effects of impartation of hydrophilic characteristic by PVP, as well as to the synergistic interaction between moringa and PVP.

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“…ITR is a well-known broad-spectrum antifungal agent (Glasmacher and Prentice, 2006) belonging to BCS II (Wu and Benet, 2005), the solid dispersions of which have been published with Eudragit E matrix by several authors (Janssens et al, 2010;Jung et al, 1999;Six et al, 2003). In these works, the miscibility limit and phase separation of amorphous and crystalline ITR were investigated in melt extruded polymer systems in comparison with film casting and SD.…”

Section: Drying (Sd) and Electrospinning (Es)mentioning

confidence: 99%

Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions

Sóti

Bocz

Pataki

et al. 2015

International Journal of Pharmaceutics

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Three solvent based methods: spray drying (SD), electrospinning (ES) and air-assisted electrospinning (electroblowing; EB) were used to prepare solid dispersions of itraconazole and Eudragit E. Samples with the same API/polymer ratios were prepared in order to make the three technologies comparable. The structure and morphology of solid dispersions were identified by scanning electron microscopy and solid phase analytical methods such as, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Raman chemical mapping. Moreover, the residual organic solvents of the solid products were determined by static headspace-gas chromatography/mass spectroscopy measurements and the wettability of samples was characterized by contact angle measurement. The pharmaceutical performance of the three dispersion type, evaluated by dissolution tests, proved to be very similar. According to XRPD and DSC analyses, made after the production, all the solid dispersions were free of any API crystal clusters but about 10 wt% drug crystallinity was observed after three months of storage in the case of the SD samples in contrast to the samples produced by ES and EB in which the polymer matrix preserved the API in amorphous state.

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Enhanced solubility and dissolution rate of itraconazole by a solid dispersion technique

Cited by 197 publications

References 15 publications

Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion

Solid-State Characterization and Dissolution Properties of Meloxicam–Moringa Coagulant–PVP Ternary Solid Dispersions

Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions

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