Improvement of Large Intestinal Absorption of Insulin by Chemical Modification with Palmitic Acid in Rats

Hashizume, Minoru; Douen, Takayuki; Murakami, Masahirô; Yamamoto, Akira; Takada, Kanji; Muranishi, Shozo

doi:10.1111/j.2042-7158.1992.tb05463.x

Cited by 74 publications

(24 citation statements)

References 12 publications

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“…Significant improvements of oral insulin absorption were already attained by masking the hydrophilic surface of its molecule. Moreover, chemical modification of the molecule by optimizing the fatty acid chain length with palmitic acid achieved an enhanced oral absorption of insulin [56][57][58].…”

Section: Future Research Pathsmentioning

confidence: 99%

Oral Antidiabetic Therapy in Patients with Heart Disease

Fisman

Tenenbaum

Motro

et al. 2004

Herz

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Five types of oral antihyperglycemic drugs are currently approved for the treatment of diabetes: biguanides, sulfonylureas, meglitinides, glitazones, and alpha-glucosidase inhibitors. The cardiovascular effects of the most commonly used antidiabetic drugs in these groups are briefly reported, in an attempt to improve knowledge and awareness regarding their influences and potential risks when treating patients with coronary artery disease (CAD). Regarding biguanides, gastrointestinal disturbances such as diarrhea are frequent, and the intestinal absorption of group B vitamins and especially folate is impaired during chronic therapy. This deficiency may lead to increased plasma homocysteine levels which, in turn, accelerate the progression of vascular disease due to adverse effects on platelets, clotting factors, and endothelium. The existence of a graded association between homocysteine levels and overall mortality in patients with CAD is well established. In addition, metformin may lead to lethal lactic acidosis, especially in patients with clinical conditions that predispose to this complication, such as heart failure or recent myocardial infarction. Sulfonylureas avoid ischemic preconditioning. During myocardial ischemia, they may prevent the opening of the ATP-dependent potassium channels, impeding the necessary hyperpolarization that protects the cell by blocking calcium influx. Meglitinides may exert similar effects, due to their analogous mechanism of action. During treatment with glitazones, edema has been reported in 5% of patients, and these drugs are contraindicated in diabetics with NYHA class III or IV cardiac status. The long-term effects of alpha-glucosidase inhibitors on morbidity and mortality rates and on diabetic micro- and macrovascular complications are yet unknown. The combined sulfonylurea/metformin therapy reveals additive effects on mortality. It is concluded that(1) four of the five oral antidiabetic drug groups present proven or potential cardiac hazards;(2) these hazards are not mere "side effects", but are deeply rooted in the drugs' mechanism of action;(3) current data indicate that the combined glibenclamide/metformin therapy seems to present special risk and should be avoided in the long-term management of type 2 diabetics with proven CAD; and(4) customized antihyperglycemic pharmacological approaches should be investigated for optimal treatment of diabetic patients with heart disease.

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Section: Future Research Pathsmentioning

confidence: 99%

Oral Antidiabetic Therapy in Patients with Heart Disease

Fisman

Tenenbaum

Motro

et al. 2004

Herz

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“…R123 absorption was analyzed first using an in situ closed-loop procedure and then using a bioavailability study, these studies were similar to previous studies [13][14][15][16] with following modifications. For the in situ closed-loop method, the intestine was exposed through a midline abdominal incision and a 20 cm jejunum loop was prepared by cannulation with silicone tubing (i.d.…”

Section: Absorption Experimentsmentioning

confidence: 99%

Determination of Rhodamine 123 in rat plasma utilizing liquid chromatography–tandem mass spectrometry

Sun

Yao

Yan

et al. 2011

Journal of Chromatography B

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“…Fatty acid addition to peptides can enhance bioavailability and membrane permeability of peptides that are poorly absorbed [10]. Whittaker et al…”

Section: Lipopeptidesmentioning

confidence: 99%

Peptide delivery systems

Ali

Manolios

2001

Lett Pept Sci

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SummaryEfficient delivery of peptide drugs to the desired site is very important. There are a number of barriers that may limit using peptides as potential drugs, some of these obstacles include poor biomembrane permeability, enzymatic degradation and low pH. To improve peptide drug efficiency a selective drug delivery system is required. Here we review some of the delivery systems available for peptides and we will also briefly discuss peptides that have been used as delivery systems.

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Improvement of Large Intestinal Absorption of Insulin by Chemical Modification with Palmitic Acid in Rats

Cited by 74 publications

References 12 publications

Oral Antidiabetic Therapy in Patients with Heart Disease

Oral Antidiabetic Therapy in Patients with Heart Disease

Determination of Rhodamine 123 in rat plasma utilizing liquid chromatography–tandem mass spectrometry

Peptide delivery systems

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