Influence of sulfobutyl ether β-cyclodextrin (Captisol®) on the dissolution properties of a poorly soluble drug from extrudates prepared by hot-melt extrusion

Fukuda, Mamoru; Miller, Dave A.; Peppas, Nicholas A.; McGinity, James W.

doi:10.1016/j.ijpharm.2007.08.038

Cited by 68 publications

(40 citation statements)

References 29 publications

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“…A 2-3 mg sample of the pure drug and the polymer and their physical mixtures with varying drug concentrations (5,10,20,40,60, and 80%) were weighed using a Mettler Toledo™ Excellence Plus (model no. XP 204) analytical balance, sealed in aluminum crimped pans (Kit 0219-0062, PerkinElmer Instruments, Shelton, CT, USA), and heated from 40 to 245°C at a ramp rate of 20°C/min under nitrogen purge at a flow rate of 20 mL/min.…”

Section: Differential Scanning Calorimetry Analysismentioning

confidence: 99%

“…It was hypothesized that variability in the intimacy of mixing in different powder samples would be explained by investigating the extent of moisture absorption, which is directly proportional to the amount of hygroscopic surface area of the material being tested [20]. Thus, the extent of moisture absorption could be indicative of the intimate mixing of powders.…”

Section: Moisture Absorptionmentioning

confidence: 99%

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Influence of Process and Formulation Parameters on Dissolution and Stability Characteristics of Kollidon® VA 64 Hot-Melt Extrudates

et al. 2014

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Abstract. The objective of the present study was to investigate the effects of processing variables and formulation factors on the characteristics of hot-melt extrudates containing a copolymer (Kollidon® VA 64). Nifedipine was used as a model drug in all of the extrudates. Differential scanning calorimetry (DSC) was utilized on the physical mixtures and melts of varying drug-polymer concentrations to study their miscibility. The drug-polymer binary mixtures were studied for powder flow, drug release, and physical and chemical stabilities. The effects of moisture absorption on the content uniformity of the extrudates were also studied. Processing the materials at lower barrel temperatures (115-135°C) and higher screw speeds (50-100 rpm) exhibited higher post-processing drug content (~99-100%). DSC and X-ray diffraction studies confirmed that melt extrusion of drug-polymer mixtures led to the formation of solid dispersions. Interestingly, the extrusion process also enhanced the powder flow characteristics, which occurred irrespective of the drug load (up to 40% w/w). Moreover, the content uniformity of the extrudates, unlike the physical mixtures, was not sensitive to the amount of moisture absorbed. The extrusion conditions did not influence drug release from the extrudates; however, release was greatly affected by the drug loading. Additionally, the drug release from the physical mixture of nifedipineKollidon® VA 64 was significantly different when compared to the corresponding extrudates (f 2 =36.70). The extrudates exhibited both physical and chemical stabilities throughout the period of study. Overall, hot-melt extrusion technology in combination with Kollidon® VA 64 produced extrudates capable of higher drug loading, with enhanced flow characteristics, and excellent stability.

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Section: Differential Scanning Calorimetry Analysismentioning

confidence: 99%

Section: Moisture Absorptionmentioning

confidence: 99%

Influence of Process and Formulation Parameters on Dissolution and Stability Characteristics of Kollidon® VA 64 Hot-Melt Extrudates

et al. 2014

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“…However, until today, the potential of sulfobutyl ether 7 β-cyclodextrin (SBE 7 β-CD) in improving the dissolution rate and therapeutic efficacy of CBZ has not been established. SBE 7 β-CD is a highly water-soluble derivative of β-cyclodextrin that is commercially available as Captisol® (7,8). The water solubility of SBE 7 β-CD (∼70 g/100 ml at 25°C) is significantly higher than the parent β-cyclodextrin (1.85 g/100 ml at 25°C).…”

Section: Introductionmentioning

confidence: 99%

Sulfobutyl Ether7 β-Cyclodextrin (SBE7 β-CD) Carbamazepine Complex: Preparation, Characterization, Molecular Modeling, and Evaluation of In Vivo Anti-epileptic Activity

et al. 2011

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Abstract. The objective of the present investigation was to study the ability of sulfobutyl ether 7 -β-cyclodextrin to form an inclusion complex with carbamazepine, an anti-epileptic drug with poor water solubility. The formation of the complex was carried out using the industrially feasible spray-drying method. The inclusion complex and physical mixtures were characterized by various techniques such as differential scanning calorimetry (DSC), infrared (IR), nuclear magnetic resonance (NMR), X-ray diffraction (XRD), and molecular modeling. The DSC, IR, and NMR studies confirmed the formation of an inclusion complex between carbamazepine and sulfobutyl ether 7 β-cyclodextrin whereas XRD studies indicated an amorphous nature of the inclusion complex. Molecular modeling studies disclosed different modes of interaction between carbamazepine and sulfobutyl ether 7 β-cyclodextrin with good correlation with experimental observations. The inclusion complex exhibited significantly higher in vitro dissolution profile as compared with pure carbamazepine powder. The in vivo anti-epileptic activity of carbamazepine/sulfobutyl ether 7 β-cyclodextrin complex was evaluated in pentylenetetrazole-induced convulsions model. The carbamazepine/sulfobutyl ether 7 β-cyclodextrin complex showed significantly higher anti-epileptic activity (p <0.01) as compared with that of carbamazepine suspension on oral administration.

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“…3) In general, annealing increases the density within the polymer and decreases the rate of creep or stress relaxation at temperatures below the Tg. [4][5][6] These changes tend to improve the dimensional stability of the polymer, as well as remove any residual stresses, strains, or defects that may have occurred during processing. Annealing generally produces polymers which display higher moduli and tend to be more brittle than unannealed polymers.…”

mentioning

confidence: 99%

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Hasanzadeh

Ghaffari

Monajjemzadeh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the present study was to investigate the effect of thermal-treating on the release of ibuprofen from the granules prepared using aqueous dispersions of Eudragit. To accomplish this goal, different formulations were prepared using wet granulation method containing two different types of Eudragit aqueous dispersions, RS30D, RL30D and Avicel as filler. Tablets were prepared using direct compression method. The prepared tablets were thermally treated at 50 and 70°C for 24 h. The drug release from tablets was assessed before and after thermal-treating. The results of release study showed that, thermally-treating the tablets at the temperatures higher than glass transition temperature (Tg) of the polymer can decrease the drug release from matrices. For mechanistic evaluation of the effect of thermal-treating, powder X-ray diffraction (XPD), scanning electron microscopy (SEM), differential scanning calorimeter (DSC), Fourier transform infrared (FT-IR) and helium pycnometer have been employed. The SEM graphs showed that the tablets have smoother surface with less porosity after thermal-treating. FT-IR spectra showed no change in the spectrum of thermally-treated tablet compared to control. In DSC graphs, no crystalline change was seen in the heat-treated samples of ibuprofen tablets, but decreased and widened peak size were related to the probable formation of solid solution of ibuprofen in Eudragit matrix. The results of helium pycnometer showed a significant decrease in the total porosity of some heat-treated samples. This study revealed the importance of thermal treating on the drug release from sustained release tablets containing Eudragit polymer.

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Influence of sulfobutyl ether β-cyclodextrin (Captisol®) on the dissolution properties of a poorly soluble drug from extrudates prepared by hot-melt extrusion

Cited by 68 publications

References 29 publications

Influence of Process and Formulation Parameters on Dissolution and Stability Characteristics of Kollidon® VA 64 Hot-Melt Extrudates

Influence of Process and Formulation Parameters on Dissolution and Stability Characteristics of Kollidon® VA 64 Hot-Melt Extrudates

Sulfobutyl Ether7 β-Cyclodextrin (SBE7 β-CD) Carbamazepine Complex: Preparation, Characterization, Molecular Modeling, and Evaluation of In Vivo Anti-epileptic Activity

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

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