Melanotan-II (MT-II) is a cyclic heptapeptide analogue of α-MSH (α-melanocyte stimulating hormone) which tans the skin rapidly and is currently being evaluated for the prevention of sunlight-induced skin cancers. In these preformulation studies, the degradation of MT-II followed apparent first-order kinetics. The degradation rate increased as the temperature or phosphate buffer concentration were increased. The pH-rate profile of MT-II degradation showed that MT-II was most stable at approximately pH 5. The degradation of MT-II was not affected by ionic strength. The pKa1 and pKa2 were estimated to be 6.53 and 11.74, respectively. The partition coefficient was studied at various pH values. The Δ log PC at pH 7.35 was 1.05 which indicated that MT-II could pass the intestinal membrane relatively easily. The preformulation data presented here can be used to help develop an appropriate dosage form for MT-II.
| Identifer | oai:union.ndltd.org:arizona.edu/oai:arizona.openrepository.com:10150/291574 |
| Date | January 1992 |
| Creators | Lan, En-Ling, 1964- |
| Contributors | Blanchard, James |
| Publisher | The University of Arizona. |
| Source Sets | University of Arizona |
| Language | en_US |
| Detected Language | English |
| Type | text, Thesis-Reproduction (electronic) |
| Rights | Copyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author. |
Page generated in 0.0021 seconds