Abstract:
:Melanotan-II (1) is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH) which tans the skin and is currently being evaluated for the prevention of sunlight-induced skin cancers. The dissociation constants of 1 were determined using potentiometric titration and ultraviolet spectrophotometry. The pKa1 (histidine) and pKa2 (arginine) were estimated to be 6.54 and 11.72, respectively. The apparent partition coefficient (PC) was measured at three pH values using both n-octanol and isooctane as the nonpolar phase. The PC(octanol) and delta log PC at pH 7.35 were 2.82 and 1.05, respectively. These data, together with the observance of a bioavailability of 4.6% in the rat, indicate that 1 may be a suitable candidate for oral delivery. The data presented here are useful in developing an appropriate dosage form for 1.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Lan EL,Ugwu SO,Blanchard J,Fang X,Hruby VJ,Sharma Sdoi
10.1002/jps.2600830805subject
Has Abstractpub_date
1994-08-01 00:00:00pages
1081-4issue
8eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49547-4journal_volume
83pub_type
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