The Changing Face of the Rate Concept in Biopharmaceutical Sciences: From Classical to Fractal and Finally to Fractional

Dokoumetzidis, Aristides; Macheras, Panos

doi:10.1007/s11095-011-0370-4

Cited by 42 publications

(26 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…According to Ostwald-Freundlich equation and Noyes-Whitney equation [31,32], it was generally thought that the huge surface area and saturation solubility resulting from particle radius in nanometer range leaded to the increased and accelerated dissolution velocity. This would be conductive to formation of high concentration gradient and then enhanced antibacterial activity on the wound surface.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of genipin-crosslinked chitosan hydrogels as a potential carrier for silver sulfadiazine nanocrystals

Gao

Gan²,

Meng³

et al. 2016

Colloids and Surfaces B: Biointerfaces

View full text Add to dashboard Cite

Section: Discussionmentioning

confidence: 99%

Evaluation of genipin-crosslinked chitosan hydrogels as a potential carrier for silver sulfadiazine nanocrystals

Gao

Gan²,

Meng³

et al. 2016

Colloids and Surfaces B: Biointerfaces

View full text Add to dashboard Cite

“…Moreover, particular emphasis was placed on the random effects of drug dissolution as well as the role of heterogeneity in the deterministic models of drug dissolution 57. These concepts were further developed by the introduction of fractional kinetics to model nonclassical drug dissolution, release, and absorption 58–60…”

Section: Scientific Aspects Of Oral Drug Absorptionmentioning

confidence: 99%

Antituberculosis Therapy–Induced Acute Liver Failure: Magnitude, Profile, Prognosis, and Predictors of Outcome

et al. 2010

View full text Add to dashboard Cite

Antituberculosis therapy (ATT)–associated acute liver failure (ATT-ALF) is the commonest drug-induced ALF in South Asia. Prospective studies on ATT-ALF are lacking. The current study prospectively evaluated the magnitude, clinical course, outcome, and prognostic factors in ATT-ALF. From January 1986 to January 2009, 1223 consecutive ALF patients were evaluated: ATT alone was the cause in 70 (5.7%) patients. Another 15 (1.2%) had ATT and simultaneous hepatitis virus infection. In 44 (62.8%) patients, ATT was prescribed empirically without definitive evidence of tuberculosis. ATT-ALF patients were younger (32.87 [±15.8] years), and 49 (70%) of them were women. Most had hyperacute presentation; the median icterus encephalopathy interval was 4.5 (0-30) days. The median duration of ATT before ALF was 30 (7-350) days. At presentation, advanced encephalopathy and cerebral edema were present in 51 (76%) and 29 (41.4%) patients, respectively. Gastrointestinal bleed, seizures, infection, and acute renal failure were documented in seven (10%), five (7.1%), 26 (37.1%), and seven (10%) patients, respectively. Compared with hepatitis E virus (HEV) and non-A non-E–induced ALF, ATT-ALF patients had nearly similar presentations except for older age and less elevation of liver enzymes. The mortality rate among patients with ATT-ALF was high (67.1%, n = 47), and only 23 (32.9%) patients recovered with medical treatment. In multivariate analysis, three factors independently predicted mortality: serum bilirubin (≥10.8 mg/dL), prothrombin time (PT) prolongation (≥26 seconds), and grade III/IV encephalopathy at presentation. Conclusion: ATT-ALF constituted 5.7% of ALF at our center and had a high mortality rate. Because the mortality rate is so high, determining which factors are predictors is less important. A high proportion of patients had consumed ATT empirically, which could have been prevented. Hepatology 2010

show abstract

“…It was Lansky and Weis40 who raised a question on this issue for the first time in 1999, and soon after dose was incorporated explicitly into the fundamental relationships used routinely in dissolution 39. 41 The Noyes–Whitney equation (Equation 1) was modified taking into account the dose and the volume of the dissolution medium;39, 41 thus Equation 1 was expressed in terms of the fraction of dose dissolved, Φ : …”

Section: The Evolution Of Gi Drug Absorption Analysismentioning

confidence: 99%

“…When the entire dose is not dissolved ( q >1), the Mean Dissolution Time for saturation is MDT s = k −1 37. To model correctly these two cases, a branched version of the Noyes–Whitney equation has been considered 41. Expressing the equation as fraction of dose dissolved, Φ , the branched Noyes‐Whitney equation has the form …”

Section: The Evolution Of Gi Drug Absorption Analysismentioning

confidence: 99%

“…where q is the dimensionless dose/solubility ratio equal to Dose/( C s V ), C s is the saturation solubility and T is the time where the entire quantity of the initial dose has been dissolved; V is the volume of the dissolution medium. The branched version of the dissolution model allows, in principle, the estimation of solubility even when the data do not reach saturation 41…”

Section: The Evolution Of Gi Drug Absorption Analysismentioning

confidence: 99%

See 1 more Smart Citation

Computational‐Regulatory Developments in the Prediction of Oral Drug Absorption

Valsami

Macheras

2011

Molecular Informatics

View full text Add to dashboard Cite

Early prediction of human intestinal absorption is important in selection of potential orally administered drugs. Various computational models for prediction of the fraction of dose absorbed, Fa, have been developed. In 1989, a sigmoidal relationship between Fa and drug absorption potential was shown. Since then various physicochemical descriptors of molecules (lipophilicity, polar surface area, hydrogen bond descriptors) have been found to correlate with human intestinal absorption and various attempts in estimating Fa have been reported. Most studies rely on the presupposition that Fa is mainly dependent on drug's solubility, which drives the dissolution rate in the gastrointestinal (GI) fluids, and the rate of passive drug transport across the intestinal membrane. In the same vein, the biopharmaceutics classification system (BCS) and the relevant FDA guideline classify drugs in four categories according to their aqueous solubility and permeability. However, the biopharmaceutics drug disposition classification system (BDDCS) revealed the poor predictability of permeability estimates for Fa and the major role of transporters for GI uptake of drugs. The role of solubility in the reaction limited model of dissolution and the ubiquitous presence of supersaturated solubility-dissolution phenomena in the GI lumen, call for a more physiologically relevant consideration of GI absorption.

show abstract

The Changing Face of the Rate Concept in Biopharmaceutical Sciences: From Classical to Fractal and Finally to Fractional

Cited by 42 publications

References 23 publications

Evaluation of genipin-crosslinked chitosan hydrogels as a potential carrier for silver sulfadiazine nanocrystals

Evaluation of genipin-crosslinked chitosan hydrogels as a potential carrier for silver sulfadiazine nanocrystals

Antituberculosis Therapy–Induced Acute Liver Failure: Magnitude, Profile, Prognosis, and Predictors of Outcome

Computational‐Regulatory Developments in the Prediction of Oral Drug Absorption

Contact Info

Product

Resources

About