Effect of Hydrophilization of Hydrophobic Drugs on Release Rate from Capsules

Lerk, Cf; Lagas, M.; Fell, John T.; Nauta, P.

doi:10.1002/jps.2600670716

Cited by 29 publications

(9 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Other research has shown that coating a hydrophobic powder with hydrophilic material increases dissolution rate. [23] In order to test wettability as a mechanism of increased dissolution, suspensions of neat micronized and comicronized CI-1040 were prepared in 1% HPMC and 0.5% Tween 80 in water. Dissolution in the suspension media prior to the actual test was insignificant since the solubility of CI-1040 in the suspension medium is extremely low.…”

Section: Resultsmentioning

confidence: 99%

Increased Dissolution Rate and Bioavailability Through Comicronization with Microcrystalline Cellulose

Spence

Bhattachar

Wesley

et al. 2005

Pharmaceutical Development and Technology

View full text Add to dashboard Cite

Micronization is a commonly used enabling technology to improve the bioavailability of compounds where absorption is dissolution rate limited. However, decreasing particle size often results in increased Van der Waals' interactions and electrostatic attraction between particles. This causes agglomeration of particles, thereby compromising the increase in surface area gained by micronization. Comicronization with excipients has been reported to offer significant advantages over neat micronization. The present work describes the comicronization of a model compound CI-1040 at a high drug load that shows an increase in the dissolution rate and bioavailability in male Wistar rats. Physicochemical characterization of the comicronized and neat micronized material is presented to help explain the in-vitro and in-vivo data.

show abstract

Section: Resultsmentioning

confidence: 99%

Increased Dissolution Rate and Bioavailability Through Comicronization with Microcrystalline Cellulose

Spence

Bhattachar

Wesley

et al. 2005

Pharmaceutical Development and Technology

View full text Add to dashboard Cite

show abstract

“…The main advantage of using water as granulating liquid is the enhancement of the hydrophilization of MN and hence enhancing its dissolution. It is previously demonstrated that the release of hydrophobic drugs can be improved by the hydrophilization process which was achieved by creation of hydrophilic surface on the drug (34). Also, the solubility of MN could be enhanced by water-soluble excipients as previously reported (35).…”

Section: In Vitro Dissolution Studymentioning

confidence: 79%

Miconazole Nitrate Oral Disintegrating Tablets: In Vivo Performance and Stability Study

et al. 2012

View full text Add to dashboard Cite

The interest in and need for formulating miconazole nitrate (MN), a broad-spectrum antifungal, as an oral disintegrating tablet for treatment of some forms of candidiasis have increased. Formulation of MN in this dosage form will be more advantageous, producing dual effect: local in the buccal cavity and systemic with rapid absorption. Four formulations were prepared utilizing the foam granulation technique. The prepared tablets were characterized by measuring the weight uniformity, thickness, tensile strength, friability, and drug content. In addition, tablet disintegration time, in vitro dissolution, and in vivo disintegration time were also evaluated. Stability testing for the prepared tablets under stress and accelerated conditions in two different packs were investigated. Each pack was incubated at two different elevated temperature and relative humidity (RH), namely 40 ± 2°C/75 ± 5% RH and 50 ± 2°C/75 ± 5% RH. The purpose of the study is to monitor any degradation reactions which will help to predict the shelf life of the product under the defined storage conditions. Finally, in vivo study was performed on the most stable formula to determine its pharmacokinetic parameters. The results revealed that all the prepared tablets showed acceptable tablet characteristics and were stable under the tested conditions. The most stable formula was that containing magnesium stearate as lubricant, hydrophobic Aerosil R972 as glidant, low urea content, mannitol/microcrystalline cellulose ratio 2:1, and 9% Plasdone XL100 as superdisintegrant. The in vivo results revealed that the tested formula showed rapid absorption compared to the physical blend (t (max) were 1 and 4 h, respectively), while the extent of absorption was almost the same.

show abstract

“…This angle measures the degree to which a drop spreads on a solid surface and thus describes the affinity of the materials. A large angle (>90°) indicates poor wetting and thus a hydrophobic surface if water is the liquid, whereas contact angles smaller than 90° indicate surface hydrophilicity 29. 30…”

Section: Resultsmentioning

confidence: 99%

Hydrophilized Silicone Matrix for the Preparation of Stable Carbonyl Reductase Immobilizates

2013

View full text Add to dashboard Cite

Industrial use of enzymes requires high activity, stability, and manageability under technical conditions. Therefore, most biocatalysts are immobilized before use, often by physical adsorption onto a solid carrier. However, a major limitation for the technical use of such immobilizates is the insufficient operational stability under process conditions resulting from enzyme leaching and carrier disintegration. Our group demonstrated recently that for lipase‐catalyzed esterifications these limitations can be largely overcome by the formation of silCoat biocatalysts, composite materials of carrier‐bound enzymes and silicone. Here, we report the successful transformation of this method to the immobilization of carbonyl reductase (CR), an enzyme representing oxidoreductases as a completely different class of biocatalysts. The silCoat biocatalysts cannot be transferred directly to CR because they require an overall hydrophilic surrounding, which opposes the hydrophobicity of silicone. Consequently, the hydrophilization of the material is necessary to achieve reasonable enzyme activity. This was realized by the rational modification of the precursors for silicone formation and applied to increase the leaching stability and mechanical strength of the carrier‐bound CR. The resulting HYsilCoat CR had a significantly longer half‐life than that obtained through the uncoated preparation; the mechanical stability of an alumina carrier was increased by a factor of 120. This enables the consideration of mechanically unstable but environmentally friendly and/or cheap material as an enzyme carrier for industrial use.

show abstract

Effect of Hydrophilization of Hydrophobic Drugs on Release Rate from Capsules

Cited by 29 publications

References 15 publications

Increased Dissolution Rate and Bioavailability Through Comicronization with Microcrystalline Cellulose

Increased Dissolution Rate and Bioavailability Through Comicronization with Microcrystalline Cellulose

Miconazole Nitrate Oral Disintegrating Tablets: In Vivo Performance and Stability Study

Hydrophilized Silicone Matrix for the Preparation of Stable Carbonyl Reductase Immobilizates

Contact Info

Product

Resources

About