Insulin rectal absorption

Hosny, E., et al. 1994. Effect of sodium salicylate on insulin rectal absorption in humans. Arzneimittelforschung 44 611. 

Hosny, E., El-Ahmady, O., El-Shattawy, H., Nabih, A. El-M., El-Damacy, H., Gamal-El-Deen, S., and El-Kabbany, N., 1994b, Effect of sodium salicylate on insulin rectal absorption in mmsLm,Arzneim.-Forsch./DrugRes. 44(I) 611-613. 

The sodium salt of the phenylglycine derivative (33) was investigated as an absorption promoter for the rectal absorption of beta-lactam antibiotics and insulin [80JAP(K)31040 81CPB1998, 81CPB2012], (Naphthothiazol-2-ylidene)malonates (1661 and 1662) were applied in silver halide photographic emulsions as sensitizer dyes [82JAP(K)54936]. 

Developments in the administration of insulin through the skin, the mouth, the nose, and the lung have been reviewed (183). Methods of absorption other than subcutaneous, such as nasal insulin, buccal insulin, rectal insulin, and insulin in enteric-coated capsules, are still experimental. A problem in nasal administration is still how to get a daily reproducible dose (184). The frequency of hypoglycemia is comparable to the frequency with subcutaneous insulin (185). Nasal irritation, sometimes with congestion, and dyspnea (186) can occur. Pulmonary insulin, delivered by aerosol inhalation, is another experimental method. No lung obstruction was reported, but the uptake varied considerably (187). 

Touitou, E., and M. Donbrow. 1983. Promoted rectal absorption of insulin Formulative parameters involved in the absorption from hydrophilic bases. Int J Pharm 15 13. 

Watanabe, Y., et al. 1992. Absorption enhancement of polypeptide drugs by cyclodextrins. I. Enhanced rectal absorption of insulin from hollow-type suppositories containing insulin and cyclodextrins in rabbits. Chem Pharm Bull 40 3042. 

Ichikawa, K., et al. 1980. Rectal absorption of insulin suppositories in rabbits. J Pharm Pharmacol 32 314. 

Kim, S., et al. 1983. Effect of enamine derivatives on the rectal absorption of insulin in dogs and rabbits. J Pharm Pharmacol 35 100. 

Nishihata, T., et al. 1981. Enhanced rectal absorption of insulin and heparin in rats in the presence of non-surfactant adjuvants. J Pharm Pharmacol 33 334. 

Due to a combination of poor membrane permeability and metabolism at the site of absorption, rectal bioavailability of peptide and proteins is low. As in other mucosal bioavailability testing, insulin is the most studied polypeptide with respect to rectal absorption. 

The possible use of mixed micelles (e.g., made of unsaturated fatty acids and monoglycerides) has been shown for the enhanced rectal absorption of several compounds, including a and p interferon and insulin. 

Nishihata, T. Rytting, J.H. Kamada, A. Higuchi, T. Routh, M. Caldwell, L. Enhancement of rectal absorption of insulin using sahcylates in dogs. J. Pharm. Pharmacol. 1983, 55, 148-151. 

Rectal absorption of drugs from aqueous or alcoholic solutions is generally much faster than from suppositories. Non-surfactant adjuvants, such as salicylates, increase rectal absorption of water-soluble drugs and also of high molecular weight compounds, such as insulin, heparin, and gastrin. 

Ichikawa, K., Ohata, I., Mitomi, M., Kawamura, S., Maeno, H., and Kawata, H., 1980, Rectal absorption of insulin suppositories in rabbits, / Pharm. Pharmacol. 32 314-318. 

Morimoto, K., Kamiya, E., Takeeda, T., Nakamoto, Y., and Morisaka, K., 1983, Enhancement of rectal absorption of insulin in polyacrylic acid aqueous gel bases containing long chain fatty acid in rats, M J. Pharm. 14 149-157. 

Nidiihata, T., Kim, S., Morishita, S., Kamada, A., Yata, N., and Higuchi, T., 1983b Adjuvant effects of glyceryl esters of acetoacetic acid on rectal absorption of insulin and insulin in rabbits, J. Pharm. Sci. 72 280-285. 

Recently, insulin absorption via the jejunum has been effected by administration of insulin-cetomacrogol solutions to diabetic rats [87]. Results presented in Table 7.5 are most likely to be due to a membrane effect rather than a surfactant-protecting effect on insulin degradation, as insulin administered h after cetomacrogol elicited a hypoglycaemic effect (see Section 7.4.2 below on rectal absorption). Sodium lauryl sulphate (0.75%) and sodium taurocholate (3.2 %) have been reported to cause an increase in the percentage of insulin absorbed from the ligated rat jejunal loop from 0.4% to 3.2% and 3.4%,... 

BJ Aungst, NJ Rogers, E Shefter. (1988). Comparison of nasal, rectal, buccal, sublingual, and intramuscular insulin efficacy and the effects of a bile salt absorption promoter. J Pharmacol Exp Therap 244 23-27. 

Aungst BJ, Rogers NJ (1988a) Site dependence of absorption-promoting actions of laureth-9, Na salicylate, Na2EDTA, and aprotinin on rectal, nasal, and buccal insulin delivery. Pharm Res 5 305-308... 

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