Stabilization of a Supersaturated Solution of Mefenamic Acid from a Solid Dispersion with EUDRAGIT® EPO

Kojima, Takanori; Higashi, Kenjirou; Suzuki, Toyofumi; Tomono, Kazuo; Moribe, Kunikazu; Yamamoto, Keiji

doi:10.1007/s11095-011-0655-7

Cited by 124 publications

(146 citation statements)

References 45 publications

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“…Hydrophilic polymers could induce and maintain a supersaturated drug solution by inhibiting nucleation and crystal growth through steric stabilization, and/or specific interactions with the drug, such as hydrogen bonding, hydrophobic interactions, and complex formation. 17,22 PVP, PEG, and HPMC have been found to be effective drug precipitation inhibitors in various formulations, including lipid-based formulations. [23][24][25][26] Meanwhile, amphiphilic polymers have been widely used not only to prevent drug precipitation but also to act as surfactants for solubilization via micelle formation.…”

mentioning

confidence: 99%

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Yeom¹,

Chae²,

Son³

et al. 2017

IJN

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A novel, supersaturable self-microemulsifying drug delivery system (S-SMEDDS) was successfully formulated to enhance the dissolution and oral absorption of valsartan (VST), a poorly water-soluble drug, while reducing the total quantity for administration. Poloxamer 407 is a selectable, supersaturating agent for VST-containing SMEDDS composed of 10% Capmul ® MCM, 45% Tween ® 20, and 45% Transcutol ® P. The amounts of SMEDDS and Poloxamer 407 were chosen as formulation variables for a 3-level factorial design. Further optimization was established by weighting different levels of importance on response variables for dissolution and total quantity, resulting in an optimal S-SMEDDS in large quantity (S-SMEDDS_LQ; 352 mg in total) and S-SMEDDS in reduced quantity (S-SMEDDS_RQ; 144.6 mg in total). Good agreement was observed between predicted and experimental values for response variables. Consequently, compared with VST powder or suspension and SMEDDS, both S-SMEDDS_LQ and S-SMEDDS_RQ showed excellent in vitro dissolution and in vivo oral bioavailability in rats. The magnitude of dissolution and absorption-enhancing capacities using quantity-based comparisons was in the order S-SMEDDS_RQ > S-SMEDDS_LQ > SMEDDS > VST powder or suspension. Thus, we concluded that, in terms of developing an effective SMEDDS preparation with minimal total quantity, S-SMEDDS_RQ is a promising candidate.

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mentioning

confidence: 99%

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Yeom¹,

Chae²,

Son³

et al. 2017

IJN

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“…[4][5][6][7] In many cases, a supersaturated drug solution generated by amorphous solid dispersion is thermodynamically unstable and energetically tends to return to equilibrium via precipitation. 8) To maintain supersaturation, precipitation must be inhibited, in many cases by a polymeric precipitation inhibitor. 9) Several commercially available polymeric precipitation inhibitors have been explored in this context, including polyvinyl pyrrolidone (PVP), polyethylene glycol (PEG), and hydroxypropyl methyl cellulose (HPMC).…”

mentioning

confidence: 99%

Preparation and Evaluation of Solid Dispersion of Atorvastatin Calcium with Soluplus® by Spray Drying Technique

Baek

Cho

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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The aim of the present study was to investigate the effect of Soluplus ® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus ® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus ® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus ® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.

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“…10) During drug precipitation, polymers may adsorb onto the surface of small embryo particles and inhibit crystal growth by blocking the active surface and providing steric stabilization. 11) In addition, hydrogen bonding between the drug and polymers may compliment hydrophobic interactions between these species, helping to maintain supersaturation.…”

Section: Resultsmentioning

confidence: 99%

“…10) However, further study on the formation and stabilization mechanism of the Eudragit E solid dispersion is needed.…”

Section: Resultsmentioning

confidence: 99%

Improved Supersaturation and Oral Absorption of Dutasteride by Amorphous Solid Dispersions

Beak

Kim

2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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In this study, amorphous solid dispersions containing dutasteride and various excipients, manufactured by spray-drying processes, were characterized to determine the effects on their ability to form supersaturated solutions and to identify the effects of supersaturation on increasing the bioavailability of dutasteride. The excipients included Eudragit E, hydroxypropyl-β-cyclodextrin (HP-β-CD), hydroxypropyl cellulose (HPC), hydroxypropylmethyl cellulose (HPMC), and polyvinylpyrrolidone (PVP K30). A solid dispersion with Eudragit E displayed a high maximum supersaturation with extended supersaturation, compared with a water-soluble polymer. The maximum concentration and the degree of supersaturation increased in the following order: PVP K30

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Stabilization of a Supersaturated Solution of Mefenamic Acid from a Solid Dispersion with EUDRAGIT® EPO

Abstract: The formation and high stability of the supersaturated solution were attributable to the specifically formed intermolecular interactions between MFA and EPO.

Cited by 124 publications

References 45 publications

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

Preparation and Evaluation of Solid Dispersion of Atorvastatin Calcium with Soluplus® by Spray Drying Technique

Improved Supersaturation and Oral Absorption of Dutasteride by Amorphous Solid Dispersions

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