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The Use of Cyclodextrins in Ophthalmic Formulations of Dipivefrin by Pekka Jarho; Kristiina Järvinen; Arto Urtti; Valentino J Stella; Tomi Järvinen is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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Dipivefrine (dipivalyl epinephrine, DPE) is a dipivalic acid ester prodrug of epinephrine. The present study evaluates the possible use of hydroxypropyl-i-cyclodextrin (HP-i-CD) or sulfobutyl ether i-cyclodextrin ((SBE) 7mi-CD) in ophthalmic formulations of DPE in order to increase the aqueous stability of DPE. The solubility of DPE was determined by phase-solubility method at pH 7.4 while the stability of DPE was investigated as a function of temperature (37-70°C) and CD concentrations at pH 5.0 and 7.4. The effect of HP-i-CD and (SBE) 7m -i-CD on the aqueous phase to organic phase transfer kinetics was studied with an aqueous buffer/n-octanol system, while the effect of (SBE) 7m -i-CD on (in vitro) corneal uptake of DPE was studied with isolated rabbit corneas in order to predict the ophthalmic bioavailability of DPE in the presence of CD. The negatively charged (SBE) 7m -i-CD formed significantly stronger inclusion complexes with the positively charged DPE (pK a = 9.01) and enhanced the aqueous stability of DPE significantly more compared to the neutral cyclodextrin HP-i-CD. At room temperature and at pH values of 5.0 and 7.4, 9.2 mM (SBE) 7m -i-CD increased the aqueous stabilit

Who reads The Use of Cyclodextrins in Ophthalmic Formulations of Dipivefrin?

Author

Pekka Jarho; Kristiina Järvinen; Arto Urtti; Valentino J Stella; Tomi Järvinen

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

1997

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)