ISSN:
1573-904X
Keywords:
inhalation aerosol
;
surfactant
;
micellar solubilization
;
formulation
;
solution
;
suspension
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Reverse micellization of nonionic surfactants in apolar media was applied to the formulation of solution phase, pressurized inhalation aerosols, employing soya lecithin (SPC) and water in chlorofluorocarbon (CFC) blends. The use of a 30/70 mixture of trichlorofluoromethane (Pll) and dichlorodifluoromethane (P12) resulted in the formation of stable, isotropic systems containing 0.5–2.0% (w/v) SPC and solubilized water; R (moles water/moles SPC), 0.9 to 4.28. In systems containing 〈30% Pll, phase separation became apparent, particularly at higher water and surfactant concentrations. Dramatic changes in solution viscosity were noted on increasing R values and were attributed to an increase in asymmetry of SPC micelles. Dynamic fractionation of the output from pressurized aerosols using a four-stage liquid impinger showed that the respira-ble fraction (as measured by the percentage of emitted droplets with aerodynamic diameters 〈5.5 µm) was highly dependent on SPC concentration and R. A significant correlation between RF and actuator score, based on orifice diameter and length, was also found and confirmed that the highest RF values were achieved with the systems of lowest SPC and water concentrations sprayed through an actuator with the smallest and shortest orifice dimensions. This novel mechanism for the formulation of hydrophilic drugs as solutions within CFC-based pressurized aerosols may offer advantages over the traditional suspension approach to pulmonary drug delivery
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1015813009024
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