Stabilized Amorphous State of Ibuprofen by Co‐Spray Drying With Mesoporous SBA‐15 to Enhance Dissolution Properties

Shen, Shoucang; Ng, Wai Kiong; Chia, Leonard; Dong, Youming; Tan, Reginald B. H.

doi:10.1002/jps.21967

Cited by 128 publications

(71 citation statements)

References 36 publications

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“…From this model, the sizes of the fenofibrate molecules were estimated to be in the range of 0.98-1. 27 13-17 times larger than that of the fenofibrate molecule. Therefore, the restricted pore size of Neusilin UFL2 inhibited the crystalline formation of fenofibrate.…”

Section: Crystallinity Evaluationmentioning

confidence: 90%

“…This tendency was also reported by Shen et al who studied the adsorption of ibuprofen onto submicron mesoporous SBA-15 particles. 27 They reported that the uniform silica pore walls separate the fine amorphous particles perfectly and prevent recrystallization and crystal growth, even under severe storage conditions. For comparison according to the adsorption method used, fenofibrate-loaded Neusilin UFL2 was also prepared by solvent evaporation and hot-melt adsorption at a fenofibrate to Neusilin UFL2 ratio of 40:60 (w/w).…”

Section: Crystallinity Evaluationmentioning

confidence: 99%

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Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

Ho¹,

Cho²,

Kim³

et al. 2012

IJN

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Background: The aim of this study was to enhance the bioavailability of fenofibrate, a poorly water-soluble drug, using a melt-adsorption method with supercritical CO 2 . Methods: Fenofibrate was loaded onto Neusilin ® UFL2 at different weight ratios of fenofibrate to Neusilin UFL2 by melt-adsorption using supercritical CO 2 . For comparison, fenofibrate-loaded Neusilin UFL2 was prepared by solvent evaporation and hot melt-adsorption methods. The fenofibrate formulations prepared were characterized by differential scanning calorimetry, powder x-ray diffractometry, specific surface area, pore size distribution, scanning electron microscopy, and energy-dispersive x-ray spectrometry. In vitro dissolution and in vivo bioavailability were also investigated. Results: Fenofibrate was distributed into the pores of Neusilin UFL2 and showed reduced crystal formation following adsorption. Supercritical CO 2 facilitated the introduction of fenofibrate into the pores of Neusilin UFL2. Compared with raw fenofibrate, fenofibrate from the prepared powders showed a significantly increased dissolution rate and better bioavailability. In particular, the area under the drug concentration-time curve and maximal serum concentration of the powders prepared using supercritical CO 2 were 4.62-fold and 4.52-fold greater than the corresponding values for raw fenofibrate. Conclusion: The results of this study highlight the usefulness of the melt-adsorption method using supercritical CO 2 for improving the bioavailability of fenofibrate.

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Section: Crystallinity Evaluationmentioning

confidence: 90%

Section: Crystallinity Evaluationmentioning

confidence: 99%

Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

Ho¹,

Cho²,

Kim³

et al. 2012

IJN

View full text Add to dashboard Cite

show abstract

“…In addition these conventional methods have intrinsic disadvantages such as the use of organic solvents that will require a subsequent solvent elimination process; impacting on time and cost factors (129). Therefore, supplementary approaches have been proposed to load drug into mesoporous carriers without affecting active stability such as supercritical fluids method (129,181), co-spray drying (182,183) and microwave irradiation (184). The supercritical fluid method (e.g.…”

Section: Drug Loading Methods For Mesoporous Materialsmentioning

confidence: 99%

“…This approach involves dispersing the carrier in a solution of the drug in a volatile solvent followed by spray drying of the dispersion. Compared to solvent based techniques, this method produces more stable amorphous state of the drug with considerably enhanced dissolution rate and oral bioavailability (182,183).…”

Section: Drug Loading Methods For Mesoporous Materialsmentioning

confidence: 99%

Porous Inorganic Drug Delivery Systems—a Review

et al. 2017

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Innovative methods and materials have been developed to overcome limitations associated with current drug delivery systems. Significant developments have led to the use of a variety of materials (as excipients) such as inorganic and metallic structures; marking a transition from conventional polymers. Inorganic materials, especially those possessing significant porosity, are emerging as good candidates for the delivery of a range of drugs (anti-biotics, anti-cancer and anti-inflammatories), providing several advantages in formulation and engineering (encapsulation of drug in amorphous form, controlled delivery and improved targeting). This review focuses on key selected developments in porous drug delivery systems. The review provides a short broad overview of porous polymeric materials for drug delivery before focusing on porous inorganic materials (e.g. Santa Barbara Amorphous (SBA) and Mobil Composition of Matter (MCM)) and their utilisation in drug dosage form development. Methods for their preparation and drug loading thereafter are detailed. Several examples of porous inorganic materials, drugs used and outcomes are discussed providing the reader with an understanding of advances in the field and realistic opportunities.

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“…Although Probucol rapidly crystallizes from saturated solutions of ethanol or acetone into one of two polymorphs [25], an amorphous form of the drug has been stabilized by mixing it with a hydrophilic polymer and spray drying [26]. Similarly, Ibuprofen readily crystallizes from an ethanol solution [27], however, a stabilized amorphous form of this drug has also been obtained by cospraying with mesoporous submicron particles to yield an enhanced dissolution rate [28]. Pure Ibuprofen, however, does form a supercooled liquid upon cooling from the melt and will not crystallize provided the temperature remains above À10 C since no nuclei form above this temperature [16].…”

Section: Fig 2 Insertmentioning

confidence: 99%

Amorphization of Molecular Liquids of Pharmaceutical Drugs by Acoustic Levitation

Benmore

Weber

2011

Phys. Rev. X

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It is demonstrated that acoustic levitation is able to produce amorphous forms from a variety of organic molecular compounds with different glass forming abilities. This can lead to enhanced solubility for pharmaceutical applications. High-energy x-ray experiments show that several viscous gels form from saturated pharmaceutical drug solutions after 10-20 min of levitation at room temperature, most of which can be frozen in solid form. Laser heating of ultrasonically levitated drugs can also result in the vitrification of molecular liquids, which is not attainable using conventional amorphization methods.

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Stabilized Amorphous State of Ibuprofen by Co‐Spray Drying With Mesoporous SBA‐15 to Enhance Dissolution Properties

Cited by 128 publications

References 36 publications

Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

Enhancement of the dissolution rate and bioavailability of fenofibrate by a melt-adsorption method using supercritical carbon dioxide

Porous Inorganic Drug Delivery Systems—a Review

Amorphization of Molecular Liquids of Pharmaceutical Drugs by Acoustic Levitation

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