The use of an in vitro dissolution and absorption system to evaluate oral absorption of two weak bases in pH-independent controlled-release formulations

Sugawara, Mitsuru; Kadomura, Shota; He, Xiaolong; Takekuma, Yoh; Kohri, Naonori; Miyazaki, Katsumi

doi:10.1016/j.ejps.2005.02.017

Cited by 62 publications

(35 citation statements)

References 25 publications

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“…Prediction of the extent and influence of intestinal precipitation of basic drugs after oral administration has previously been described in the literature (2)(3)(4)(5)(6)(7)(8). Dai et al have described 96-well plate experiments where precipitation has been measured over time in small volumes of various simulated gastrointestinal media, suitable for screening of different additives for prevention of precipitation (2).…”

Section: Introductionmentioning

confidence: 98%

Predicting Intestinal Precipitation—A Case Example for a Basic BCS Class II Drug

et al. 2010

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Section: Introductionmentioning

confidence: 98%

Predicting Intestinal Precipitation—A Case Example for a Basic BCS Class II Drug

et al. 2010

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“…The solubilitydissolution behavior of a drug is frequently the rate-limiting step to absorption of drugs from the gastrointestinal tract for orally administered drugs (Sugawara et al, 2005;Youn et al, 2006). Poor aqueous solubility has always been a very challenging obstacle as it is together with membrane permeability, an essential factor in the limitation of a drug's bioavailability following oral administration.…”

Section: Introductionmentioning

confidence: 99%

Preparation and comparative evaluation of liquisolid compacts and solid dispersions of Valsartan

2012

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The aim of the present study was to increase the solubility of a poorly water soluble BCS class II drug, valsartan. Liquisolid technology and solid dispersion by kneading method were techniques used to improve the solubility of the drug by using non-volatile solvents and some hydrophilic carriers. Liquisolid compacts were prepared by dissolving the drug in suitable non volatile solvents. The various non volatile solvents used were PG, PEG, and glycerine. The carrier coating materials play an important role in improving the solubility of the drug. The dissolution rate of the drug was increased by using propylene glycol as non-volatile solvent at 20:1 ratio of carrier to coating material. Solid dispersion by kneading method were another attempt to improve solubility the various carrier materials used were PVP K 30, PEG 6000 and mannitol, these carriers are used in various ratios to improve its solubility. The dissolution rate of drug using solid dispersion kneading method with mannitol was increased at 1:3 ratio. The DSC and FTIR studies revealed no drug excipients interactions, whereas XRD revealed the reduced crystalinity of drug, which showed enhanced solubility. From the results it was concluded that the liquisolid compacts enhanced the solubility of valsartan in comparison to traditional solid dispersion method.

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“…This issue is almost circumvented in later publications by employing several gastric acid models [52]. Nevertheless, the authors are able to mimic precipitation of weak bases in the "pH adjustment vessel," such as for albendazol [53]. Furthermore, the apparatus of Kobayashi et al [50] and He et al [51] shows a good linear relationship between the amount cumulatively permeated into the acceptor compartment and the fraction absorbed in humans, although clinical doses of the drugs are disregarded.…”

Section: Published Approaches For Combined Dissolution and Permeationmentioning

confidence: 99%

“…Finally, the authors concluded that this continuous dissolution/Caco-2 may be a tool to forecasting formulation effects on in vivo dissolution and in vivo permeation. [50][51][52][53]: Shortly after Ginski et al [48], Kobayashi and coworkers [50] published an open dissolution/permeation approach in 2001. A stirred glass vessel serves as a flow through dissolution device, from where the eluted solution is pumped into a second glass vessel for pH adjustment to a pH of 6.0.…”

Section: Published Approaches For Combined Dissolution and Permeationmentioning

confidence: 99%

Instrumented In Vitro Approaches to Assess Epithelial Permeability of Drugs from Pharmaceutical Formulations

Motz¹,

Bur²,

Schaefer³

et al.

Drug Absorption Studies

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The following chapter gives an overview of instrumented approaches to investigate the interactions of orally or pulmonary administered formulations with epithelial cell cultures in vitro. The first section is focused on the combined assessment of drug release/dissolution and subsequent absorption/permeation for solid oral dosage forms. Experimental approaches to mimic the complex physiologically surroundings in the gastrointestinal tract are presented as well as combinations of dissolution and permeation apparatus.The second part describes different experimental approaches to simultaneously assess deposition and subsequent absorption of pharmaceutical aerosol formulations, typically by adapting some existing impactor/impinger devices to accommodate pulmonary epithelial cell culture systems. Differences between longtime and low-dose aerosol deposition in environmental toxicology and short time bolus inhalation of pharmaceutical aerosols are elucidated.

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The use of an in vitro dissolution and absorption system to evaluate oral absorption of two weak bases in pH-independent controlled-release formulations

Cited by 62 publications

References 25 publications

Predicting Intestinal Precipitation—A Case Example for a Basic BCS Class II Drug

Predicting Intestinal Precipitation—A Case Example for a Basic BCS Class II Drug

Preparation and comparative evaluation of liquisolid compacts and solid dispersions of Valsartan

Instrumented In Vitro Approaches to Assess Epithelial Permeability of Drugs from Pharmaceutical Formulations

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