Permeability enhancement, effect

Other fatty acids as absorption enhancers have been reported. Ogiso et al. [112] demonstrated that lauric acid (C12) produced the largest increase in permeation rate, penetration coefficient, and partition coefficient of propranolol. Onuki et al. [113] reported that docosa-hexaenoic acid (DHA) has a strong insulin permeability enhancement effect and little toxicity, compared to oleic acid and eicosapentaenoic acid (EPA) using a water-in-oil-in-water (W/O/W) multiple emulsion with no or little mucosal damage. 

In addition to their usefulness in the enhancement of oral bioavailability of lipophilic drugs, microemulsion formulations have found considerable application as potential delivery systems for peptides whose delivery is often limited by poor GI permeability. W/O microemulsions provide a convenient means of delivery of both permeability-enhancing lipids and water-soluble peptides. The GI permeability-enhancing effects of lipids and their use in the delivery of highly water-soluble compounds are reviewed elsewhere [18, 56, 59],... 

Wu S-Y, Robinson JR (1999) Transcellular lipophilic complex-enhanced intestinal absorption of human growth hormone. Pharm Res 16 1266-1272 Yamashita S, Saitoh H, Nakanishi K, Masada M, Nadai T, Kimura T (1987) Effects of diclofenac sodium and disodium ethylenediaminetetraacetate on electrical parameters of the mucosal membrane and their relation to the permeability enhancing effects in the rat jejunum. J Pharm Pharmacol 39 621-626... 

Davidsen, J., Mouritsen, O.G., and Jorgensen, K., Synergistic permeability enhancing effect of lysophospholipids and fatty acids on lipid membranes, Biochim. Biophys. Acta, 1564, 256, 2002. 

Such a composition reduces friction, permeates drilling mud wall cake, destroys binding wall cake, and reduces differential pressure. Unfortunately, many of such compositions are toxic to marine life. Synthetic PAOs are nontoxic and effective in marine environments when used as lubricants, retum-of-permeabiUty enhancers, or spotting fluid additives for water-based drilling muds. A continuing need exists for other nontoxic additives for water-based drilling muds, which serve as lubricants, retum-of-permeability enhancers, and spotting fluids. 

Where an unusual excipient is chosen, or where an established excipient is chosen for a dosage form that results in its administration by a novel route of administration, then additional data will need to form part of the application. In effect, a novel excipient will need to be supported by data similar to those required for a new drug, with full supporting data including composition, function, and safety. Novel excipients include the components of the matrix in prolonged release products, new propellants, and new permeability enhancers. The exception to this need for extensive supporting data would be for a material already approved for food use and administered by the oral route or a material already approved for cosmetic use with a topical route of administration. In all cases the quality of the excipients has to be described adequately and shown to be satisfactory (which will depend on its role). 

Yamamoto A, Tanaka H, Okumura S, Shinsako K, Ito M, Yamashita M, Okada N, Fujita T, Muranishi S (2001) Evaluation of insulin permeability and effects of absorption enhancers on its permeability by an in vivo epithelial system using Xenopus pulmonary membrane. Biol Pharm Bull 385-389... 

The use of surfactants as intestinal absorption promoters is the most investigated approach. Furthermore, this chapter will review the enhancing effect of surfactants with various structures on the permeability of GI membrane to macromolecules. 

Murakami, T., et al. 2000. Enhancing effect of 5 a-cyprinol sulfate on mucosal membrane permeability to sodium ampicillin in rats. Eur J Pharm Biopharm 49 111. 

Ahsan, F., et al. 2003. Effects of permeability enhancers, tetradecylmaltoside and dimethyl-beta-cyclodextrin, on insulin movement across human bronchial epithelial cells (16HBE14o ). Eur J Pharm Sci 20 27. 

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