Relationship of dissolution rate in anionic polymeric solutions to viscosity

Chang, Shu-Hwa; Parrott, Eugene L.

doi:10.3109/03639049109043820

Cited by 9 publications

(6 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Previous studies examining drug dissolution and disintegration under viscous conditions showed reduced dissolution and disintegration rates , e.g. a reduction in the intrinsic dissolution rate by reduced diffusivity of benzoic acid in solutions of uncharged polymers according to the Stokes‐Einstein equation .…”

Section: Introductionmentioning

confidence: 98%

Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity

Radwan

Amidon

Langguth

2012

Biopharm & Drug Disp

104

View full text Add to dashboard Cite

A negative food effect, i.e. a decrease in bioavailability upon the co-administration of compounds together with food, has been attributed particularly with high solubility/low permeability compounds (BCS class III). Different mechanisms have been proposed including intestinal dilution leading to a lower concentration gradient across the intestinal wall as well as binding of the active pharmaceutical ingredient to food components in the intestine and thereby decreasing the fraction of the dose available for absorption. These mechanisms refer primarily to the compound and not to the dosage form. An increase in viscosity of the dissolution fluid will in particular affect the absorption of BCS type III compounds with preferential absorption in the upper small intestine if the API release is delayed from the dosage form. The present study demonstrated that the increase in viscosity of the dissolution medium, following ingestion of a solid meal, may drastically reduce disintegration and dissolution. For that purpose the viscosity of the standard FDA meal was determined and simulated by solutions of HPMC in buffer. As model formulations, three commercially available tablets containing trospium chloride, a BCS class III m-cholinoreceptor antagonist was used. Trospium chloride drug products have been described to undergo a negative food effect of more than 80% following ingestion with food. The tablets showed prolonged disintegration times and reduced dissolution rates in viscous media, which could be attributed to changes in the liquid penetration rates. The effect was particularly significant for film-coated tablets relative to uncoated dosage forms. The results show the necessity of considering media viscosity when designing in vitro models of drug release for BCS type III drug formulations.

show abstract

Section: Introductionmentioning

confidence: 98%

Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity

Radwan

Amidon

Langguth

2012

Biopharm & Drug Disp

104

View full text Add to dashboard Cite

show abstract

“…Nevertheless, it has been described that water addition results in less viscosity 39 , which could impact in some desirable properties, including good material transfer. This property is an essential requirement for mixing operations and in drug release processes to give optimum bioavailability characteristics of the therapeutic drug 40 , 41 .…”

Section: Resultsmentioning

confidence: 99%

A Natural Deep Eutectic Solvent Formulated to Stabilize β-Lactam Antibiotics

Olivares

Martínez

Rivas

et al. 2018

Sci Rep

View full text Add to dashboard Cite

β-lactam antibiotics, such as penicillin share a very unstable chemical structure. In water-based solutions, such as those used for clinical applications, the β-lactam ring is readily opened due to a nucleophilic or electrophilic attack, leading to the loss of antimicrobial activity. Since the achievement and maintenance of optimum therapeutic levels of β-lactam antibiotics is critical for the resolution of many infectious clinical situations, and to avoid antibiotic resistance generation, the design of new non-aqueous dosage forms is urgent. Recently, natural deep eutectic solvents (NADES) have emerged as alternative non-toxic and non-aqueous solvents for different biomedical applications. In this work, we formulated and characterized a NADES composed by betaine and urea (BU). Using this solvent, we evaluated the stability of clavulanic acid (CLV) and imipenem (IMP) and characterized their antimicrobial activities calculating the minimal inhibitory concentration. Characterization of BU solvent by infrared spectroscopy (IR) and nuclear magnetic resonance spectroscopy (NMR) indicated that the obtained solvent has a microstructure mainly based on hydrogen bonding interactions and water addition strongly affects its dynamic. The stability of β-lactam antibiotic IMP and CLV using this solvent was increased by 7 fold and 2.5 fold respectively compared to water when analysed seven days after being dissolved. Microbiological assays showed that antibacterial activity at day seven was significantly decreased for both CLV and IMP when dissolved in water, while no change in their antibacterial properties was observed when antibiotics were dissolved in BU. The increased stability of IMP and CLV in BU may be related to the inert behaviour of the solvent and the higher dynamic restriction that helps antibiotics to maintain a more stable conformation. These data suggest the potential use of BU as a solvent to prevent degradation of β-lactam antibiotics.

show abstract

“…1) as representative of the viscoelastic properties to establish correlations for both type of systems. Power law functions were used16:…”

Section: Resultsmentioning

confidence: 99%

Acyclovir Delivery Matrices Based on Poly(Ethylene Glycol)/Chitosan Semi-Interpenetrating Networks

Dı́ez-Sales

Dolz

Hernández

et al. 2007

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Relationship of dissolution rate in anionic polymeric solutions to viscosity

Cited by 9 publications

References 19 publications

Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity

Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity

A Natural Deep Eutectic Solvent Formulated to Stabilize β-Lactam Antibiotics

Acyclovir Delivery Matrices Based on Poly(Ethylene Glycol)/Chitosan Semi-Interpenetrating Networks

Contact Info

Product

Resources

About