2002
DOI: 10.1002/jps.10083
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Testosterone 17β‐N,N‐Dimethylglycinate Hydrochloride: A Prodrug with a Potential for Nasal Delivery of Testosterone

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Cited by 21 publications
(9 citation statements)
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“…Furthermore, their nasal administration resulted in a rapid and complete absorption to the systemic circulation, where quick conversion to L-Dopa takes place. Similar results were obtained for testosterone which is also poorly water-soluble (127).…”
Section: Prodrugssupporting
confidence: 84%
“…Furthermore, their nasal administration resulted in a rapid and complete absorption to the systemic circulation, where quick conversion to L-Dopa takes place. Similar results were obtained for testosterone which is also poorly water-soluble (127).…”
Section: Prodrugssupporting
confidence: 84%
“…Thus, we first assessed the ability of four different sex steroid hormones to alter P. aeruginosa alginate production. The tested compounds varied in polarity and included the synthetic hormone ethinylestradiol (EE2) (logP, 4.15) ( 18 ) (least polar), testosterone (T) (logP, 3.30) ( 19 ), the pregnancy-related estrogen estriol (E3) (logP, 2.45) ( 20 ), and a water-soluble synthetic and hydrophilic derivative of testosterone, TSDG.HCl (logP, 2.40) ( 21 ) (most polar) ( Fig. 1A ).…”
Section: Resultsmentioning
confidence: 99%
“…One strategy often employed for improvement in oral bioavailability is masking a compound’s polar ionizable groups via a prodrug approach. The idea is that less polar prodrugs will have enhanced intestinal permeability, and upon absorption, they will be cleaved to the active drug via plasma or liver enzymes. Notably, prodrug strategies are common in drug development; about 10–12% of the approved worldwide drugs are prodrugs, and of these, most are primarily designed with an objective to enhance the permeability of the parent drug . Specifically, drugs containing carboxylates, phosphate, phosphonate, or phosphinate functional group encounter permeability challenges due to the anionic charge at nearly all physiological pH, making them highly polar and requiring their delivery as ester- or amide-based prodrugs. , This strategy has been successfully implemented for the approved prodrugs such as adefovir dipivoxil [bis-(pivaloyloxymethyl) ester of adefovir] and tenofovir disoproxil [bis-(isopropyloxycarbonyloxymethyl) ester of tenofovir], where a 4- and 7-fold enhancement in oral bioavailability was observed, respectively. …”
Section: Discussionmentioning
confidence: 99%