Measurement of Drug Concentration in the Stomach After Intragastric Administration of Drug Solution to Healthy Volunteers: Analysis of Intragastric Fluid Dynamics and Drug Absorption

Yamashita, Shinji; Kataoka, Makoto; Higashino, Haruki; Sakuma, Shinji; Sakamoto, Takashi; Uchimaru, Hinako; Tsukikawa, Hiroshi; Shiramoto, Masanari; Uchiyama, Hiroo; Tachiki, Hidehisa; Irie, Shin

doi:10.1007/s11095-012-0931-1

Cited by 42 publications

(30 citation statements)

References 15 publications

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“…The difference in the drug release behavior may be attributed to the drug solubility at different pH conditions. SA is a weak acid and is less soluble at lower pHs and more soluble at higher pHs . MZ, on the other hand, has higher solubility at gastric pH environment than in the intestinal environment …”

Section: Resultsmentioning

confidence: 99%

Encapsulation of animal wax‐based organogels in alginate microparticles

Sagiri

Pal

Basak

2014

J of Applied Polymer Sci

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Encapsulation of organogels is a novel perspective in the field of controlled drug delivery. This study reports encapsulation of lanolin based organogels within alginate microparticles. The microparticles were prepared by emulsification/internal gelation method. Microscopic studies suggested spherical shape of the microparticles. Fourier transform infrared, X-ray diffraction and thermal studies confirmed the presence of organogels within the microparticles. Organogels containing microparticles showed improved drug (e.g., salicylic acid and metronidazole) entrapment efficiency. The release of the drugs from the microparticles was dependent on the pH of the dissolution medium. The release was diffusion mediated. The drug loaded microparticles showed antimicrobial activity against E. coli and B. subtilis. The preliminary study suggested that the encapsulation of the organogels may help prolonging the release of the drugs and hence may be tried as vehicles for controlled drug delivery. V C 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci.2014, 131, 40910.

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Section: Resultsmentioning

confidence: 99%

Encapsulation of animal wax‐based organogels in alginate microparticles

Sagiri

Pal

Basak

2014

J of Applied Polymer Sci

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“…70 In addition, the gastric emptying half time can be as short as 4 min in a fasted state. 71,72 Furthermore, the solubility of a drug in the small intestine was suggested to be sufficient to justify biowaiver. 73,74 Therefore, in the following discussion, the gastric emptying is assumed instant.…”

Section: Discussion Based On Facsmentioning

confidence: 99%

“…However, the gastric‐emptying rate largely depends on the phase of the migrating motor complexes, which are the waves of the GI walls that sweep through the stomach and the intestine in a regular cycle during a fasting state . In addition, the gastric emptying half time can be as short as 4 min in a fasted state . Furthermore, the solubility of a drug in the small intestine was suggested to be sufficient to justify biowaiver .…”

Section: Bioequivalencementioning

confidence: 99%

Rate- and Extent-Limiting Factors of Oral Drug Absorption: Theory and Applications

Sugano

Terada

2015

Journal of Pharmaceutical Sciences

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“…So far, no gastric perfusions studies have been performed to evaluate direct gastric P eff . However, gastric absorption has been approximated through indirect methods to be about 40% for salicylic acid (administered as a 150‐mL solution with a pH of 9.0–9.3) and 20% for diclofenac (administered as a 400‐mL standardized meal solution with a pH of 5.6) . Even for ethanol, a small molecule with high permeation rate, the gastric absorption after oral ingestion represents only approximately 10%–20% of the total absorption.…”

Section: Intestinal Perfusion Studies Performed In Humansmentioning

confidence: 99%

Direct In Vivo Human Intestinal Permeability (Peff) Determined with Different Clinical Perfusion and Intubation Methods

Dahlgren

Roos

Sjögren

et al. 2015

Journal of Pharmaceutical Sciences

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Regional in vivo human intestinal effective permeability (Peff ) is calculated by measuring the disappearance rate of substances during intestinal perfusion. Peff is the most relevant parameter in the prediction of rate and extent of drug absorption from all parts of the intestine. Today, human intestinal perfusions are not performed on a routine basis in drug development. Therefore, it would be beneficial to increase the accuracy of the in vitro and in silico tools used to evaluate the intestinal Peff of novel drugs. This review compiles historical Peff data from 273 individual measurements of 80 substances from 61 studies performed in all parts of the human intestinal tract. These substances include: drugs, monosaccharaides, amino acids, dipeptides, vitamins, steroids, bile acids, ions, fatty acids, and water. The review also discusses the determination and prediction of Peff using in vitro and in silico methods such as quantitative structure-activity relationship, Caco-2, Ussing chamber, animal intestinal perfusion, and physiologically based pharmacokinetic (PBPK) modeling. Finally, we briefly outline how to acquire accurate human intestinal Peff data by deconvolution of plasma concentration-time profiles following regional intestinal bolus dosing.

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Measurement of Drug Concentration in the Stomach After Intragastric Administration of Drug Solution to Healthy Volunteers: Analysis of Intragastric Fluid Dynamics and Drug Absorption

Abstract: This study provided valuable information on intragastric fluid dynamics and gastric drug absorption in humans to establish a better in vitro-in vivo correlation in oral drug absorption.

Cited by 42 publications

References 15 publications

Encapsulation of animal wax‐based organogels in alginate microparticles

Encapsulation of animal wax‐based organogels in alginate microparticles

Rate- and Extent-Limiting Factors of Oral Drug Absorption: Theory and Applications

Direct In Vivo Human Intestinal Permeability (Peff) Determined with Different Clinical Perfusion and Intubation Methods

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