Evaluation of intestinal pressure-controlled colon delivery capsule containing caffeine as a model drug in human volunteers

Muraoka, Motoki; Hu, Zhaopeng; Shimokawa, Tatsuharu; Sekino, Syu-ichi; Kurogoshi, Ri-e; Kuboi, Yoshiko; Yoshikawa, Yukako; Takada, Kanji

doi:10.1016/s0168-3659(97)00201-0

Cited by 101 publications

(39 citation statements)

References 28 publications

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“…Caffeine Lee et al, 1996bMuraoka et al, 1998 on a protocol to establish a prospective relationship between plasma and saliva levels. On the basis of the application of an improved assay for 5-FU, the authors concluded that saliva PK was not predictive of plasma PK and therefore concluded that the utility of saliva was limited in establishing the risk of developing toxicity using the Mayo-regimen for 5-FU treatment.…”

Section: Selectivity Issues Specific To Salivamentioning

confidence: 99%

“…Caffeine) Muraoka et al (1998) have used salivary matrix to evaluate and define the PK parameters of a new delivery system, the pressurecontrolled colon delivery capsule (PCDC), using caffeine as the model drug. The appearance of caffeine in saliva (T i ) was targeted for the various PCDC relative to that of a plain gelatin capsule.…”

Section: Development Of Innovative Pk/pd Models For Patchmentioning

confidence: 99%

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Measurement of xenobiotics in saliva: is saliva an attractive alternative matrix? Case studies and analytical perspectives

Mullangi

Agrawal

Srinivas³

2008

Biomedical Chromatography

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The use of saliva for measuring xenobiotic concentrations has been practiced for a number of years. While the use of saliva has been generally reserved for the analysis of diagnostic and forensic/toxicology samples, attempts have been made to further enhance the value of saliva as an alternate matrix to those of plasma and serum. It is understood that saliva represents a handy tool for therapeutic drug monitoring (TDM) as it offers certain distinctive advantages. This scope of this review encompasses the following: (a) a comprehensive view of saliva as an alternate matrix for either plasma or serum to understand the pharmacokinetic/pharmacodynamic (PK/PD) characteristics; (b) an account of the factors contributing to the observed variability in salivary monitoring; (c) a tabular compilation of diverse case studies of xenobitoics belonging to different therapeutic classes with emphasis on assay methodology and applicable analytical/biopharmaceutical/pharmacokinetic findings; (d) relevant thoughts on assay procedures as they relate to salivary monitoring; and (e) some representative case studies highlighting the new thinking on the use of saliva outside of traditional TDM. Overall, based on the review, saliva represents a valuable TDM tool for a number of xenobiotics. While parent compound and phase I metabolite(s) for many xenobiotics have been generally quantifiable in saliva, phase II metabolites have not generally been detected in saliva. Therefore saliva samples could also be used to answer some specific PK/PD questions during the drug development process, if applicable. However, the development and validation of the assay in saliva needs to be carried out carefully with particular focus on proper sample collection, processing and storage to ensure the stability of the xenobiotics and with the same rigor as applied to plasma, serum and urine matrices.

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Section: Selectivity Issues Specific To Salivamentioning

confidence: 99%

Section: Development Of Innovative Pk/pd Models For Patchmentioning

confidence: 99%

Measurement of xenobiotics in saliva: is saliva an attractive alternative matrix? Case studies and analytical perspectives

Mullangi

Agrawal

Srinivas³

2008

Biomedical Chromatography

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“…They can be categorized as: (a) Prodrug approach (Riley & Turnberg, 1990;McLeod et al, 1994); (b) Pressure-based systems (Muraoka et al, 1998;Jeong et al, 2001); (c) The temporal control of delivery (Steed et al, 1997;Del Curto et al, 2009); (d) pH-based systems (Klein et al, 2005;Basak & Adhikari, 2009;Sareen et al, 2014), and (e) Enzyme-based systems (Xi et al, 2005;Varshosaz et al, 2006;Kshirsagar et al, 2011;Ramasamy et al, 2013;Rai et al, 2014). Polysaccharides which undergo hydrolysis of their glycosidic bonds by the microflora of the colon appear to be the most promising because of their attractive properties, such as wide availability, low cost of production, low toxicity and biodegradability (Chourasia & Jain, 2004).…”

Section: Introductionmentioning

confidence: 99%

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

et al. 2015

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The colon is a promising target for drug delivery owing to its long transit time of up to 78 h, which is likely to increase the time available for drug absorption. Progesterone has a short elimination half-life and undergoes extensive first-pass metabolism, which results in very low oral bioavailability ($25%). To overcome these shortcomings, we developed an oral multiparticulate system for the colonic delivery of progesterone. Zn-pectinate/chitosan microparticles were prepared by ionotropic gelation and characterized for their size, shape, weight, drug entrapment efficiency, mucoadhesion and swelling behavior. The effect of crosslinking pH, cross-linking time and chitosan concentration on progesterone release were also studied. Spherical microparticles having a diameter of 580-720 mm were obtained. Drug entrapment efficiency of $75-100% was obtained depending on the microparticle composition. Microparticle mucoadhesive properties were dependent on the pectin concentration, as well as the cross-linking pH. Progesterone release in simulated gastric fluids was minimal (3-9%), followed by burst release at pH 6.8 and a sustained phase at pH 7.4. The in vivo study revealed that the microparticles significantly increased progesterone residence time in the plasma and increased its relative bioavailability to $168%, compared to the drug alone. This study confirms the potential of Zn-pectinate/chitosan microparticles as a colon-specific drug delivery system able to enhance the oral bioavailability of progesterone or similar drugs.

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“…In contrast, the transit time in small intestine for the preparation is surprisingly constant at 3±1 h and appears to be independent of the types of the preparations and whether subjects are fed or not (Halsas et al, 2001;Muraoka, Shimokawa, 1998). Based on these understandings, we designed the enteric timedependent colon-specific drug delivery system to achieve a considerable drug release after the preparation's arrival into the colon.…”

Section: Discussionmentioning

confidence: 99%

A suppository-base-matrix tablet for time-dependent colon-specific delivery system

Zou

Wang

Zhang

et al. 2014

Braz. J. Pharm. Sci.

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Our research has focused on the main design features and release performances of time-dependent colon-specific (TDCS) delivery tablets, which relies on the relative constancy that is observed in the small intestinal transit time of dosage forms. But inflammatory bowel disease(IBD)can affect the transit time, and usually results in watery stool. Compared to the TDCS and wax-matrix TDCS tablet, a promising time-dependent colon-specific delivery system was investigated. In our study, a suppositorybase-matrix coated tablet was evaluated. Water soluble suppository-base helps the expansion of tablet, facilitates uniform film dissolution and achives high osmotic pressure. Combining the expansion of carboxymethyl starch sodium (CMS-Na) and the moisture absorption of NaCl, the coated TDCS tablet obtained a burst and targeted drug delivery system. A very good correlation between in vitro drug release and in vivo outcome was observed. This TDCS coated tablet provides a promising strategy to control drug release to the desired lower gastrointestinal region.Uniterms: Inflammatory bowel disease. Lonicera japonica Thunb/extract. Suppository/colon-specific delivery system. Drugs/colon-specific delivery system. Tablets/colon-specific delivery system. Nossa pesquisa focou-se nas principais características de planejamento e de desempenho de liberação cólon-específica tempo-dependente (TDCS) de comprimidos, que leva em conta a constância relativa observada no tempo de trânsito intestinal das formas de dosagem. A doença inflamatória do intestino (IBD) pode afetar o tempo de trânsito e, geralmente, resulta em fezes aquosas. Comparando ao TDCS e a comprimidos TDCS com matriz-cerosa, investigou-se sistema promissor de liberação cólon-específica tempo-dependente. Em nosso estudo, avaliou-se comprimido revestido com matriz base de supositório. A base de supositório solúvel em água auxilia a expansão do comprimido, facilita a dissolução uniforme do filme e atinge alta pressão osmótica. Associando a expansão do carboximetil amido sódico (CMS-Na) à absorção de umidade do NaCl, o comprimido revestido TDCS originou sistema de liberação direcionado e de erupção. Observou-se correlação muito boa entre a liberação in vitro e a in vivo do fármaco. Este comprimido revestido TDCS representa estratégia promissora para o controle da liberação do fármaco na região gastrintestinal mais baixa.Unitermos: Doença inflamatória do intestino. Lonicera japonica Thunb./extrato. Supositório/liberação cólon-específica. Fármaco/liberação cólon-específica. Comprimidos/revestidos/liberação cólon específica.

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Evaluation of intestinal pressure-controlled colon delivery capsule containing caffeine as a model drug in human volunteers

Cited by 101 publications

References 28 publications

Measurement of xenobiotics in saliva: is saliva an attractive alternative matrix? Case studies and analytical perspectives

Measurement of xenobiotics in saliva: is saliva an attractive alternative matrix? Case studies and analytical perspectives

Development and in vitro/in vivo evaluation of Zn-pectinate microparticles reinforced with chitosan for the colonic delivery of progesterone

A suppository-base-matrix tablet for time-dependent colon-specific delivery system

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