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• W2050589670 abstract "□ The skin permeation of buprénorphine base and HCI salt through cadaver skin was investigated. The octanol-water partition coefficient and solubilities of both buprénorphine free base and HCI salt were determined at 32 °C. As expected, buprénorphine free base was more lipophilic than its HCI salt and was practically insoluble In aqueous buffer at pH 8.7. The drug solubility decreased exponentially as the pH of the solution increased, whereas the permeability coefficient Increased as the donor solution pH decreased. The skin flux of buprenorphlne-HCI was significantly higher than that of the free base from propylene glycol/laurlc acid vehicle mixtures. Buprénorphine base permeation through tape-stripped epidermis suggested that in addition to stratum corneum, viable epidermis presented a significant diffusion barrier because of the very low aqueous solubility of the free base observed. The mean steady-state skin fluxes of buprenorphlne-HCI were 20.3 and 29.7 /μg/cm2/h from propylene glycol:lauryl alcohol: ethanol (80:15:5) and propylene glycol:propylene glycol monolaurate: water (80:15:5) vehicle mixtures, respectively. The skin flux of buprenorphlne-HCI from various monolithic matrix patches was also evaluated. When capric acid, lauric acid, and lauryl alcohol were separately Incorporated into an adhesive matrix, the skin flux of buprenorphlne-HCI was enhanced by a factor of 2 to 3.5. Finally, based on the total body clearance and minimum effective concentration of buprénorphine, a transdermal delivery rate of 2.5 /μg/cm2/h from a 20-cm2 patch was estimated. The in vitro skin permeation data clearly suggest that transdermal delivery of buprénorphine Is feasible to achieve a desired systemic analgesic effect. □ The skin permeation of buprénorphine base and HCI salt through cadaver skin was investigated. The octanol-water partition coefficient and solubilities of both buprénorphine free base and HCI salt were determined at 32 °C. As expected, buprénorphine free base was more lipophilic than its HCI salt and was practically insoluble In aqueous buffer at pH 8.7. The drug solubility decreased exponentially as the pH of the solution increased, whereas the permeability coefficient Increased as the donor solution pH decreased. The skin flux of buprenorphlne-HCI was significantly higher than that of the free base from propylene glycol/laurlc acid vehicle mixtures. Buprénorphine base permeation through tape-stripped epidermis suggested that in addition to stratum corneum, viable epidermis presented a significant diffusion barrier because of the very low aqueous solubility of the free base observed. The mean steady-state skin fluxes of buprenorphlne-HCI were 20.3 and 29.7 /μg/cm2/h from propylene glycol:lauryl alcohol: ethanol (80:15:5) and propylene glycol:propylene glycol monolaurate: water (80:15:5) vehicle mixtures, respectively. The skin flux of buprenorphlne-HCI from various monolithic matrix patches was also evaluated. When capric acid, lauric acid, and lauryl alcohol were separately Incorporated into an adhesive matrix, the skin flux of buprenorphlne-HCI was enhanced by a factor of 2 to 3.5. Finally, based on the total body clearance and minimum effective concentration of buprénorphine, a transdermal delivery rate of 2.5 /μg/cm2/h from a 20-cm2 patch was estimated. The in vitro skin permeation data clearly suggest that transdermal delivery of buprénorphine Is feasible to achieve a desired systemic analgesic effect." @default.
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• W2050589670 date "1994-02-01" @default.
• W2050589670 modified "2023-10-03" @default.
• W2050589670 title "Transdermal Delivery of Buprenorphine through Cadaver Skin" @default.
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• W2050589670 doi "https://doi.org/10.1002/jps.2600830204" @default.
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