Improved Dissolution of a Poorly Water-Soluble Drug from Solid Dispersions in Polyethylene Glyco1:Polysorbate 80 Mixtures

Serajuddin, Abu T.M.; Sheen, Pai‐Chang; Augustine, Matthew A.

doi:10.1002/jps.2600790524

Cited by 66 publications

(34 citation statements)

References 9 publications

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“…Sometimes the dissolution of poorly soluble drugs requires dissolution media that are different from those normally used for water-soluble drugs. One technique that is useful in the dissolution of such drugs is the incorporation of a small amount of surfactant in the dissolution medium (15,16). The use of surfactants in dissolution systems may be considered as physiologically meaningful because of the presence of natural surfactants such as bile salts and bile acids in the gastrointestinal tract (17).…”

Section: Dissolution Studiesmentioning

confidence: 99%

Development of a Discriminating Dissolution Method for Immediate-Release Soft Gelatin Capsules Containing a BCS Class II Compound

Damian¹,

Harati²,

Pathak³

et al. 2016

Dissolution Technol.

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The purpose of this study was to develop a robust dissolution procedure for liquid-filled, soft gelatin capsules (SGCs) that can distinguish small but real changes in drug product formulation. SGCs were manufactured using different ratios of fill formulations. The formulations were evaluated by performing dissolution testing on fresh capsules and capsules that were aged at different time points and conditions. USP Apparatus 1 (basket) and 2 (paddle) at rotating speeds of 50, 75, or 100 rpm were used to evaluate the release characteristics of the formulations. The model-independent method using difference factor (f1) and similarity factor (f2) was employed to compare dissolution profiles. Dissolution data showed that fill material characteristics played a major role in controlling the rate of dissolution of our drug products. The basket increased the discriminatory power of the dissolution process regardless of speed. We observed that the paddle rotation speed may impact discrimination power but not the ability of the method to discriminate. The basket was successful for the quality assessment and characterization of formulation changes of our drug products. Through understanding of drug product characteristics and evaluating parameters of dissolution testing, a methodology can be established to enable batch-to-batch evaluation.

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Section: Dissolution Studiesmentioning

confidence: 99%

Development of a Discriminating Dissolution Method for Immediate-Release Soft Gelatin Capsules Containing a BCS Class II Compound

Damian¹,

Harati²,

Pathak³

et al. 2016

Dissolution Technol.

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“…Direct filling of hard gelatin capsules with the liquid melt of solid dispersions avoids grinding-induced changes in the crystallinity of the drug. A surfactant must be mixed with the carrier to avoid formation of a drug-rich surface layer (e.g., poly-sorbate80 with PEG, phosphatidyl choline with PEG) 65,66 . The temperature of the molten solution should not exceed ~70-C because it might compromise the hard-gelatin capsule shell.…”

Section: Direct Capsule Fillingmentioning

confidence: 99%

Untitled

2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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“…One of the techniques that have been useful in dissolution of insoluble drugs is the incorporation of a small amount of surfactant in the dissolution medium. 36) The use of surfactant in the dissolution medium is physiologically meaningful, due to the presence of natural surfactants (like bile salts) in the gastrointestinal tract. The ability of surfactants to accelerate the in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or defocculation.…”

Section: )mentioning

confidence: 99%

Preparation, Characterization and in Vitro Dissolution Studies of Solid Systems of Valdecoxib with Chitosan

Kumar

Mishra

2006

CHEMICAL & PHARMACEUTICAL BULLETIN

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In the present study, the solubilizing and amorphizing properties of Valdecoxib (a poorly water soluble anti inflammatory drug) with low molecular weight chitosan (a polymer), have been investigated. Binary systems of varying drug/polymer ratios were prepared using different techniques (physical mixing, co-grinding, kneading) and were tested for dissolution. Drug carrier interactions were investigated in both the liquid and solid state, by phase solubility analysis, differential scanning calorimetry, powder X-ray diffractrometry, FT-IR spectroscopy and scanning electron microscopy. The solubility of the drug increased with increasing polymer concentration showing A N type phase solubility diagram. Differential scanning calorimetry, powder X-ray diffractrometry and scanning electron microscopic studies of binary systems suggested generation of amorphous form of drug (in kneading and co ground mixtures). IR spectroscopy revealed the presence of hydrogen bonding in kneading and co ground mixtures. Drug dissolution was improved with increasing the polymer concentration in the mixture (KneadedϾco groundϾphysical mixture), which was attributed to the amorphonization and/or decreased drug crystallinity, size and polymer wetting effect. Enhanced dissolution combined with its direct compression feasibility and anti ulcerogenic action results in low molecular weight chitosan for developing fast release oral solid dosage forms of valdecoxib.

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Improved Dissolution of a Poorly Water-Soluble Drug from Solid Dispersions in Polyethylene Glyco1:Polysorbate 80 Mixtures

Cited by 66 publications

References 9 publications

Development of a Discriminating Dissolution Method for Immediate-Release Soft Gelatin Capsules Containing a BCS Class II Compound

Development of a Discriminating Dissolution Method for Immediate-Release Soft Gelatin Capsules Containing a BCS Class II Compound

Untitled

Preparation, Characterization and in Vitro Dissolution Studies of Solid Systems of Valdecoxib with Chitosan

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