초록 ▼

This invention relates to development of an iontotherapeutic device for regulated transdermal systemic administration of ionizable pharmaceutical compounds. It also provides an iontotherapeutic process for transdermal administration of ionized pharmaceuticals, particularly those which are otherwise

This invention relates to development of an iontotherapeutic device for regulated transdermal systemic administration of ionizable pharmaceutical compounds. It also provides an iontotherapeutic process for transdermal administration of ionized pharmaceuticals, particularly those which are otherwise transdermally absorbed to a small degree or not all, such as peptide pharmaceuticals, for example, insulins. The invention also relates to unit dose forms, for example, those in which an ionized pharmaceutical is dispersed in a hydrophilic polymer. The unit dose is adapted to be assembled as part of the pharmaceutical reservoir electrode, so that the ionized pharmaceutical will be delivered transdermally and then be absorbed systemically when the iontotherapeutic device is in operation.

대표청구항 ▼

A transdermal periodic iontotherapeutic process for administering a controlled and systemically effective amount of a pharmaceutically stable and transdermally absorbable peptide pharmaceutical, by (1) assembling a dosage unit containing a pharmaceutically acceptable aqueous solution of said peptide

A transdermal periodic iontotherapeutic process for administering a controlled and systemically effective amount of a pharmaceutically stable and transdermally absorbable peptide pharmaceutical, by (1) assembling a dosage unit containing a pharmaceutically acceptable aqueous solution of said peptide into a receptacle of a reservoir electrode of a transdermal periodic iontotherapeutic system, which electrode is a cathode or anode depending upon whether said peptide is anionic or cationic, said solution having a pH at least about 1.0 pH unit below or above the isoelectric point of said peptide; (2) placing the cathode and anode electrodes of said transdermal periodic iontotherapeutic system in electrical contact with the intact skin to be treated; and (3) applying to said electrodes an iontotherapeutically effective, periodic DC current of up to about 10 mA based on a reservoir electrode/skin-contacting area of about 5 cm, which DC periodic current is monitored and adjusted as required to maintain a constant current intensity within predetermined minimum and maximum levels, using (a) a periodic waveform in the square, triangular, sinusoidal, trapezoidal, or other acceptable geometric form, or combinations thereof, (b) a physiologically acceptable repetition frequency of at least about 10 Hz, and (c) an on/off ratio of from 1/50 to 10/1; said process providing a systemically effective absorption of said peptide pharmaceutical from said solution at a rate of at least 500 percent from that provided by passive diffusion transdermal absorption from said solution during an administration time of at least 2 hours.