Oral drug profiles

Wenlock, M.C., Austin, R.P., Barton, P., Davis, A.M., Leeson, P.D. (2003) A Comparison of Physicochemical Property Profiles of Development and Marketed Oral Drugs. Journal of Medicinal Chemistry, 46,1250-1256. 

Leeson, P. D., Davis, A. D. Time-related differences in the physical property profile of oral drugs. J. Med. Chem. 

Wenlock MG, Austin RP, Barton P, et al. (2003) A comparison of physio-chemical property profiles of development and marketed oral drugs. /. Med. Chem. 46 1250-1256. 

A combination of these approaches has utility for better characterizing the dissolution profile of low-dose solid oral drug products. 

Comparative pharmacokinetic profiles of nifedipine delivered from Procardia XL, an osmotic pressure-controlled drug delivery system, once-a-day versus that from Procardia, an immediate-release dosage form, taken on time 0, 8 and 16 in human volunteers. Modified from Y.W. Chien. Oral drug delivery and delivery systems. Y.W.Chien (ed.) (1992) Novel Drug Delivery Systems. Marcel Dekker, Inc. New York, pp. 139-196... 

Davis AM, Leeson PD. A comparison of physicochemical property profiles of development and marketed oral drugs. 

Comer J, Tam KY (2001) Lipophilicity Profiles Theory and Measurement. In Testa B, van de Waterbeemd H, Folk-ers G, Guy R (eds) Pharmacokinetic Optimization in Drug Research Biological, Physicochemical and Computational Strategies VHCA Zurich, 275-304 Dressman JB, Amidon GL, Reppas C et al. (1998) Dissolution testing as a prognostic tool for oral drug absorbtion. Pharm Res 15(1) 11-22... 

In most cases, oral drug delivery is the cheapest and most convenient method of dosing. Unfortunately, it is difficult to achieve a precise control of the plasma-concentration-time profile by this route due to marked intra- and intersubject variation in gastrointestinal transit even under the rigidly controlled conditions of the clinical trial. Daily patterns of food intake, activity, and posture are large contributors to this variation. Drugs that are only absorbed from specific areas of the gastrointestinal tract, i.e., have a narrow window of absorption, will be most affected by alterations in transit. The major determinants of this variation will be the amount of food and drink consumed. 

The control of physiological processes to achieve reliable plasma concentration-time profiles following oral drug administration is a key goal in therapy. At the investigational level, it would allow the scientist to use manageable numbers of volunteers in... 

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