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https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3074025/
Although the Rule of Five was originally derived based primarily using data on oral drugs, the excellent correlation of the Rule with non-oral drugs can be attributed at least in part to similarity of the epithelial barriers and biological fluids present in both oral and non-oral routes and the fact that many drugs administered by non-oral routes were originally developed for oral delivery but were later switched to a non-oral route.Author: Young Bin Choy, Mark R. Prausnitz
https://www.ncbi.nlm.nih.gov/pubmed/20967491
The Rule of Five does appear to apply well to ophthalmic delivery. We conclude that although current non-oral drugs mostly have physicochemical properties within the Rule of Five thresholds, the Rule of Five should not be used to predict non-oral drug candidates, especially for inhalation and transdermal routes.Author: Young Bin Choy, Mark R. Prausnitz
https://www.researchgate.net/publication/47521170_The_Rule_of_Five_for_Non-Oral_Routes_of_Drug_Delivery_Ophthalmic_Inhalation_and_Transdermal
The Rule of Five for Non-Oral Routes of Drug Delivery: Ophthalmic, Inhalation and Transdermal
https://www.sciencedirect.com/science/article/pii/S0169409X16300370
Molecular inflation, attrition and the rule of five ... M.R. PrausnitzThe rule of five for non-oral routes of drug delivery: ophthalmic, inhalation and transdermal. Pharm. Res., 28 (2011), pp. 943-948 ... (2012), pp. 191-200. Google Scholar ☆ This review is part of the Advanced Drug Delivery Reviews theme issue on “Understanding the ...Author: Paul D. Leeson
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4910824/
Jun 01, 2016 · However, orally administered compounds, even those that are substrates for transporters, rarely break Rule of 5. This is in marked contrast to Ro5 violations of two or more for all of the non-oral drugs, independent of BDDCS class, as noted in Table 2. This is logical, since many of these drugs are formulated for non-oral delivery because of difficulties of membrane permeability …Author: Leslie Z. Benet, Chelsea M. Hosey, Oleg Ursu, Tudor I. Oprea
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5629190/
Oct 05, 2017 · An often cited rule is the Rule of 5 proposed by Lipinski et al. which states that non-oral delivery of drugs can only be accomplished if the drug has a molecular weight below 500 Da, has less than five H-bond donors, has less than ten H-bond acceptors, and has an octanol-water partition coefficient (also known as log P, which is a measure of lipophilicity) below five .Author: Martin Anthony Christopher Manoukian, Christopher William Migdal, Amode Ravindra Tembhekar, Jerad Al...
https://www.sciencedirect.com/topics/pharmacology-toxicology-and-pharmaceutical-science/lipinskis-rule-of-five
One way to screen out compounds with probable absorption problems is known as Lipinski's ‘rule of five.’ 4 The rule states that poor absorption or permeation of a drug is more probable when the chemical structure fulfils two or more of the following criteria: 1. Molecular weight (MW) is greater than 500. 2. The calculated log P value is above five.
https://en.wikipedia.org/wiki/Lipinski%27s_Rule_of_Five
Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would make it a likely orally active drug in humans.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4025648/
Mar 08, 2012 · This solubility allows for formulations with a concentration up to 100 mg/mL (10%), which are isotonic with human tears at approximately 300 mOsmol/L. 25 To maintain the ophthalmic solution at physiological pH values in animal and human studies, the highest dosing strength used was up to 50 mg/mL (5…Author: Min Zhong, Thomas R. Gadek, Minna Bui, Wang Shen, John Burnier, Kenneth J. Barr, Emily J. Hanan, Joh...
https://www.sciencedirect.com/science/article/pii/S1740674904000551
Citations in CAS SciFinder to the rule-of-five (RO5) publication will exceed 1000 by year-end 2004. Trends in the RO5 literature explosion that can be discerned are the further definitions of drug-like.Author: Christopher A. Lipinski
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