The Experts below are selected from a list of 456 Experts worldwide ranked by ideXlab platform

Shozo Muranishi - One of the best experts on this subject based on the ideXlab platform.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 2011
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-β-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-β-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-β-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-β-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

  • enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers their intestinal mucosal toxicity and absorption enhancing mechanism of n lauryl β d maltopyranoside
    Journal of Pharmacy and Pharmacology, 2010
    Co-Authors: Tomomi Uchiyama, Takuya Fujita, Shozo Muranishi, Tetsuo Sugiyama, Yingshu Quan, Atsushi Kotani, Naoki Okada, Akira Yamamoto
    Abstract:

    We have examined the in-vitro permeability characteristics of insulin in the presence of various absorption enhancers across rat intestinal membranes and have assessed the intestinal toxicity of the enhancers using an in-vitro Ussing chamber method. The absorption enhancing mechanism of n-lauryl-beta-D-maltopyranoside was studied also. The permeability of insulin across the intestinal membranes was low in the absence of absorption enhancers. However, the permeability was improved in the presence of enhancers such as Sodium Glycocholate and Sodium deoxycholate in the jejunum, and Sodium Glycocholate, Sodium deoxycholate, n-lauryl-beta-D-maltopyranoside, Sodium caprate and ethylenediaminetetraacetic acid (EDTA) in the colon. Overall, the absorption enhancing effects were greater on the colonic membrane than on the jejunal membrane. The intestinal membrane toxicity of these enhancers was characterized using the release of cytosolic lactate dehydrogenase from the colonic membrane. A marked increase in the release of lactate dehydrogenase was observed in the presence of Sodium deoxycholate and EDTA. The release of lactate dehydrogenase in the presence of these absorption enhancers was similar to that seen with Sodium dodecyl sulphate (SDS), used as a positive control, indicating high toxicity of these enhancers to the intestinal membrane. In contrast, Sodium Glycocholate and Sodium caprate caused minor releases of lactate dehydrogenase, similar to control levels, suggesting low toxicity. In addition, the amount of lactate dehydrogenase in the presence of n-lauryl-beta-D-maltopyranoside was much less than that seen with Sodium deoxycholate, EDTA and SDS. Therefore, Sodium Glycocholate, Sodium caprate and n-lauryl-beta-D-maltopyranoside are useful absorption enhancers due to their high absorption enhancing effects and low intestinal toxicity. To investigate the absorption enhancing mechanisms of n-lauryl-beta-D-maltopyranoside, the transepithelial electrical resistance (TEER), voltage clamp experiments and the circular dichroism spectra were studied. n-Lauryl-beta-D-maltopyranoside decreased the TEER values in a dose-dependent manner, suggesting that the enhancer may open the tight junctions of the epithelium, thereby increasing the permeability of insulin via a paracellular pathway. This speculation was supported by the findings that 20 mM n-lauryl-beta-D-maltopyranoside produced a greater increase in the paracellular flux rate than in the transcellular flux rate by the voltage clamp studies. Evaluating the circular dichroism spectra we found that insulin oligomers were not dissociated to monomers by the addition of n-lauryl-beta-D-maltopyranoside, but dissociation did occur with the addition of Sodium Glycocholate. Thus, the dissociation of insulin was not a major factor in the absorption enhancing effect of n-lauryl-beta-D-maltopyranoside. These findings provide basic information to select the optimal enhancer for the intestinal delivery of peptide and protein drugs including insulin.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 1996
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    : Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-beta-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-beta-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-beta-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-beta-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

Akira Yamamoto - One of the best experts on this subject based on the ideXlab platform.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 2011
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-β-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-β-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-β-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-β-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

  • enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers their intestinal mucosal toxicity and absorption enhancing mechanism of n lauryl β d maltopyranoside
    Journal of Pharmacy and Pharmacology, 2010
    Co-Authors: Tomomi Uchiyama, Takuya Fujita, Shozo Muranishi, Tetsuo Sugiyama, Yingshu Quan, Atsushi Kotani, Naoki Okada, Akira Yamamoto
    Abstract:

    We have examined the in-vitro permeability characteristics of insulin in the presence of various absorption enhancers across rat intestinal membranes and have assessed the intestinal toxicity of the enhancers using an in-vitro Ussing chamber method. The absorption enhancing mechanism of n-lauryl-beta-D-maltopyranoside was studied also. The permeability of insulin across the intestinal membranes was low in the absence of absorption enhancers. However, the permeability was improved in the presence of enhancers such as Sodium Glycocholate and Sodium deoxycholate in the jejunum, and Sodium Glycocholate, Sodium deoxycholate, n-lauryl-beta-D-maltopyranoside, Sodium caprate and ethylenediaminetetraacetic acid (EDTA) in the colon. Overall, the absorption enhancing effects were greater on the colonic membrane than on the jejunal membrane. The intestinal membrane toxicity of these enhancers was characterized using the release of cytosolic lactate dehydrogenase from the colonic membrane. A marked increase in the release of lactate dehydrogenase was observed in the presence of Sodium deoxycholate and EDTA. The release of lactate dehydrogenase in the presence of these absorption enhancers was similar to that seen with Sodium dodecyl sulphate (SDS), used as a positive control, indicating high toxicity of these enhancers to the intestinal membrane. In contrast, Sodium Glycocholate and Sodium caprate caused minor releases of lactate dehydrogenase, similar to control levels, suggesting low toxicity. In addition, the amount of lactate dehydrogenase in the presence of n-lauryl-beta-D-maltopyranoside was much less than that seen with Sodium deoxycholate, EDTA and SDS. Therefore, Sodium Glycocholate, Sodium caprate and n-lauryl-beta-D-maltopyranoside are useful absorption enhancers due to their high absorption enhancing effects and low intestinal toxicity. To investigate the absorption enhancing mechanisms of n-lauryl-beta-D-maltopyranoside, the transepithelial electrical resistance (TEER), voltage clamp experiments and the circular dichroism spectra were studied. n-Lauryl-beta-D-maltopyranoside decreased the TEER values in a dose-dependent manner, suggesting that the enhancer may open the tight junctions of the epithelium, thereby increasing the permeability of insulin via a paracellular pathway. This speculation was supported by the findings that 20 mM n-lauryl-beta-D-maltopyranoside produced a greater increase in the paracellular flux rate than in the transcellular flux rate by the voltage clamp studies. Evaluating the circular dichroism spectra we found that insulin oligomers were not dissociated to monomers by the addition of n-lauryl-beta-D-maltopyranoside, but dissociation did occur with the addition of Sodium Glycocholate. Thus, the dissociation of insulin was not a major factor in the absorption enhancing effect of n-lauryl-beta-D-maltopyranoside. These findings provide basic information to select the optimal enhancer for the intestinal delivery of peptide and protein drugs including insulin.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 1996
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    : Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-beta-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-beta-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-beta-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-beta-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

Tomomi Uchiyama - One of the best experts on this subject based on the ideXlab platform.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 2011
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-β-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-β-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-β-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-β-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

  • enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers their intestinal mucosal toxicity and absorption enhancing mechanism of n lauryl β d maltopyranoside
    Journal of Pharmacy and Pharmacology, 2010
    Co-Authors: Tomomi Uchiyama, Takuya Fujita, Shozo Muranishi, Tetsuo Sugiyama, Yingshu Quan, Atsushi Kotani, Naoki Okada, Akira Yamamoto
    Abstract:

    We have examined the in-vitro permeability characteristics of insulin in the presence of various absorption enhancers across rat intestinal membranes and have assessed the intestinal toxicity of the enhancers using an in-vitro Ussing chamber method. The absorption enhancing mechanism of n-lauryl-beta-D-maltopyranoside was studied also. The permeability of insulin across the intestinal membranes was low in the absence of absorption enhancers. However, the permeability was improved in the presence of enhancers such as Sodium Glycocholate and Sodium deoxycholate in the jejunum, and Sodium Glycocholate, Sodium deoxycholate, n-lauryl-beta-D-maltopyranoside, Sodium caprate and ethylenediaminetetraacetic acid (EDTA) in the colon. Overall, the absorption enhancing effects were greater on the colonic membrane than on the jejunal membrane. The intestinal membrane toxicity of these enhancers was characterized using the release of cytosolic lactate dehydrogenase from the colonic membrane. A marked increase in the release of lactate dehydrogenase was observed in the presence of Sodium deoxycholate and EDTA. The release of lactate dehydrogenase in the presence of these absorption enhancers was similar to that seen with Sodium dodecyl sulphate (SDS), used as a positive control, indicating high toxicity of these enhancers to the intestinal membrane. In contrast, Sodium Glycocholate and Sodium caprate caused minor releases of lactate dehydrogenase, similar to control levels, suggesting low toxicity. In addition, the amount of lactate dehydrogenase in the presence of n-lauryl-beta-D-maltopyranoside was much less than that seen with Sodium deoxycholate, EDTA and SDS. Therefore, Sodium Glycocholate, Sodium caprate and n-lauryl-beta-D-maltopyranoside are useful absorption enhancers due to their high absorption enhancing effects and low intestinal toxicity. To investigate the absorption enhancing mechanisms of n-lauryl-beta-D-maltopyranoside, the transepithelial electrical resistance (TEER), voltage clamp experiments and the circular dichroism spectra were studied. n-Lauryl-beta-D-maltopyranoside decreased the TEER values in a dose-dependent manner, suggesting that the enhancer may open the tight junctions of the epithelium, thereby increasing the permeability of insulin via a paracellular pathway. This speculation was supported by the findings that 20 mM n-lauryl-beta-D-maltopyranoside produced a greater increase in the paracellular flux rate than in the transcellular flux rate by the voltage clamp studies. Evaluating the circular dichroism spectra we found that insulin oligomers were not dissociated to monomers by the addition of n-lauryl-beta-D-maltopyranoside, but dissociation did occur with the addition of Sodium Glycocholate. Thus, the dissociation of insulin was not a major factor in the absorption enhancing effect of n-lauryl-beta-D-maltopyranoside. These findings provide basic information to select the optimal enhancer for the intestinal delivery of peptide and protein drugs including insulin.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 1996
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    : Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-beta-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-beta-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-beta-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-beta-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

Takuya Fujita - One of the best experts on this subject based on the ideXlab platform.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 2011
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-β-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-β-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-β-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-β-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

  • enhanced permeability of insulin across the rat intestinal membrane by various absorption enhancers their intestinal mucosal toxicity and absorption enhancing mechanism of n lauryl β d maltopyranoside
    Journal of Pharmacy and Pharmacology, 2010
    Co-Authors: Tomomi Uchiyama, Takuya Fujita, Shozo Muranishi, Tetsuo Sugiyama, Yingshu Quan, Atsushi Kotani, Naoki Okada, Akira Yamamoto
    Abstract:

    We have examined the in-vitro permeability characteristics of insulin in the presence of various absorption enhancers across rat intestinal membranes and have assessed the intestinal toxicity of the enhancers using an in-vitro Ussing chamber method. The absorption enhancing mechanism of n-lauryl-beta-D-maltopyranoside was studied also. The permeability of insulin across the intestinal membranes was low in the absence of absorption enhancers. However, the permeability was improved in the presence of enhancers such as Sodium Glycocholate and Sodium deoxycholate in the jejunum, and Sodium Glycocholate, Sodium deoxycholate, n-lauryl-beta-D-maltopyranoside, Sodium caprate and ethylenediaminetetraacetic acid (EDTA) in the colon. Overall, the absorption enhancing effects were greater on the colonic membrane than on the jejunal membrane. The intestinal membrane toxicity of these enhancers was characterized using the release of cytosolic lactate dehydrogenase from the colonic membrane. A marked increase in the release of lactate dehydrogenase was observed in the presence of Sodium deoxycholate and EDTA. The release of lactate dehydrogenase in the presence of these absorption enhancers was similar to that seen with Sodium dodecyl sulphate (SDS), used as a positive control, indicating high toxicity of these enhancers to the intestinal membrane. In contrast, Sodium Glycocholate and Sodium caprate caused minor releases of lactate dehydrogenase, similar to control levels, suggesting low toxicity. In addition, the amount of lactate dehydrogenase in the presence of n-lauryl-beta-D-maltopyranoside was much less than that seen with Sodium deoxycholate, EDTA and SDS. Therefore, Sodium Glycocholate, Sodium caprate and n-lauryl-beta-D-maltopyranoside are useful absorption enhancers due to their high absorption enhancing effects and low intestinal toxicity. To investigate the absorption enhancing mechanisms of n-lauryl-beta-D-maltopyranoside, the transepithelial electrical resistance (TEER), voltage clamp experiments and the circular dichroism spectra were studied. n-Lauryl-beta-D-maltopyranoside decreased the TEER values in a dose-dependent manner, suggesting that the enhancer may open the tight junctions of the epithelium, thereby increasing the permeability of insulin via a paracellular pathway. This speculation was supported by the findings that 20 mM n-lauryl-beta-D-maltopyranoside produced a greater increase in the paracellular flux rate than in the transcellular flux rate by the voltage clamp studies. Evaluating the circular dichroism spectra we found that insulin oligomers were not dissociated to monomers by the addition of n-lauryl-beta-D-maltopyranoside, but dissociation did occur with the addition of Sodium Glycocholate. Thus, the dissociation of insulin was not a major factor in the absorption enhancing effect of n-lauryl-beta-D-maltopyranoside. These findings provide basic information to select the optimal enhancer for the intestinal delivery of peptide and protein drugs including insulin.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 1996
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    : Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-beta-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-beta-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-beta-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-beta-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

Reiko Nishikawa - One of the best experts on this subject based on the ideXlab platform.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 2011
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-β-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-β-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-β-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-β-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.

  • effectiveness and toxicity screening of various absorption enhancers in the rat small intestine effects of absorption enhancers on the intestinal absorption of phenol red and the release of protein and phospholipids from the intestinal membrane
    Journal of Pharmacy and Pharmacology, 1996
    Co-Authors: Akira Yamamoto, Tomomi Uchiyama, Reiko Nishikawa, Takuya Fujita, Shozo Muranishi
    Abstract:

    : Sodium Glycocholate, Sodium taurocholate, Sodium deoxycholate, EDTA, Sodium salicylate, Sodium caprate, diethyl maleate, N-lauryl-beta-D-maltopyranoside, linoleic acid polyoxyethylated (60 mol) mixed micelles (all 20 mM) have been ranked in order of their effectiveness as enhancers of the absorption of drugs in the rat small intestine, by use of an in-situ loop model with phenol red as a model drug. Local toxicity in rats was examined by assessing protein and phospholipid release as biological markers. Of the absorption enhancers, Sodium deoxycholate, EDTA and N-lauryl-beta-D-maltopyranoside were the most effective; Sodium deoxycholate and EDTA, however, caused significant release of protein and phospholipids. N-lauryl-beta-D-maltopyranoside, on the other hand, did not damage the small intestinal membrane. Sodium taurocholate enhanced phenol red absorption from the small intestine and resulted in little or no protein and phospholipids release. Sodium salicylate, diethyl maleate and the mixed micelles had no absorption-promoting effects on phenol red. There was good correlation between the area under the plasma concentration-time curve for phenol red and the amounts of protein and phospholipid released in the presence of absorption enhancers. From these results it might be concluded that N-lauryl-beta-D-maltopyranoside and Sodium taurocholate are effective absorption enhancers which have low toxicity levels at a concentration of 20 mM.