Drug absorption enhancement

Muranishi, S., Yamamoto, A., Mechanisms of absorption enhancement through gastrointestinal epithelium, in Drug Absorption Enhancement, de Boer, A. G. (ed.), Harwood Academic Publishers, 1994, 67-100. 

Optimization of Formulation Parameters and Drug Absorption Enhancement Strategies... 

Thanou M, Verhoef JC, Junginger HE (2001) Oral drug absorption enhancement by chitosan and its derivatives. Adv Drug Del Rev 52 117-126... 

Uekama, K., Hirayama, F., and Irie, T. 1994. Application of cyclodextrinsDtng Absorption Enhancement Drug Absorption Enhancement Concepts, Possibilities and Limitsti ite A. G. Boer. Switzerland Harwood Academic Publishers, 1994, pp. 411-456. 

Drug absorption enhancers have been intensively studied over the past three decades [190— 192] in order to increase the oral availability of poorly absorbed drugs (BSC classes II-IV) [193,194]. Much attention has been paid to the synthesis and evaluation of new absorption enhancer molecules. Excluding the preparation of polymer drug conjugates less awareness was focused on the delivery rate of the molecules tested that is, the concomitant input of the poorly soluble drug together with its enhancer, so that maximal area of the small intestine would be exploited for absorption. The differences between the dimensions of the GI tract in... 

Poorly Absorbed Drug Absorption Enhancer Reference... 

Van Hoogdalem, E.J., A.G. De Boer, and D.D. Breimer. 1989. Intestinal drug absorption enhancement an overview. Pharmacol Ther 44 407. 

De Boer, A.G., E.J. Van Hoogdalem, and D.D. Breimer. 1992. (D) Routes of delivery Case studies, (4) rate-controlled rectal peptide drug absorption enhancement. Adv Drug Deliv Rev 8 237. 

Although penetration enhancers promise superior therapeutic efficacy, this approach should be introduced for clinical use only after considering the balance of risks and benefits. Furthermore, information on the different mechanisms of drug penetration, ocular metabolism, side effects, and the influence of ocular diseases on the specific drug absorption-enhancement techniques is required before the use of any enhancer. 

Kagatani et al. [90] studied the effect of acylcamitines as drug absorption enhancers for the nasal delivery of azetirelin in a rat model. A buffered azetirelin sample solution was administered intranasally, as described previously [47], The nasal and oral absorptions of azetirelin were then compared. The Fabs after nasal absorption was found to be 17.1%, which was 21 times greater than the 0.8% after oral administration. As reported above, a pilot study of oral azetirelin showed a bioavailability of about 2%. A bioavailability of about 20% was seen in the case of nasally administered TRH in humans as well as rats. The authors predicted that since azetirelin is an analog of TRH, its pharmacokinetic properties after nasal delivery in humans could also be about 20% [90,91]. 

Hadgraft, J. and Walters, K. A. Skin penetration enhancement. In Drug Absorption Enhancement Concepts, Possibilities, Limitations and Trends, A. B. G. de Boer, Ed. Hardwood, 1994, pp. 177-198. 

Table 2 Some types of oral drug absorption enhancers Non-steroidal anti-inflammatory agents Surfactants Bile salts...

Table 4 Some common colonic drug absorption enhancers...

Drug Absorption Enhancement Concepts, Possibilities, Limitations and Trends de Boer, A.G., Ed. Harwood Academic Switzerland, 1994. 

Drug absorption enhanced if taken with food scored tablets may be crushed do not crush or break film-coated tablets. 

Anderberg EK and Artursson P. Cell Cultures to Assess Drug ABsorption Enhancement. In Drug absorption enhancement. Concepts, possibilities, limitations and trends. Ed A. (Bert) G. de Boer. 1994. Harwood Academic publishers. 

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