Abstract: Provided is a composition for transdermal administration. The composition comprises a therapeutic agent having a net charge at skin pH and a topical penetration enhancer having a net charge at skin pH opposite the net charge of the therapeutic agent. In another aspect, a method is provided for increasing the transdermal absorption of a therapeutic agent. The method comprises forming a therapeutic composition at skin pH by combining a therapeutic agent having a net charge at skin pH with a topical penetration enhancer having a net charge at skin pH opposite the net charge of the therapeutic agent, the ratio of topical penetration enhancer to therapeutic agent being sufficient to increase absorption of therapeutic agent compared to absorption of therapeutic agent in the absence of topical penetration enhancer, and administering the therapeutic composition to a patient in need thereof.

Abstract: Design of new, safe and effective biodegradable agents, which can cover a wide range of drug molecules in the transdermal permeation and other membranes absorption of physiologically active agents are disclosed. Biodegradable agents includes compounds having a multiple hydrophilic moiety groups which are water loving groups with general chemical structures provide for contributing the penetration enhancement characteristics such as glycolic group and N-alkyl substituted amino acidic group and a lipophilic moiety and also in contributing the balanced lipophilicity of the compounds such as long chain alkyl group are disclosed. More particularly, compounds with R1, and R2, as the steric hindered but can significantly affect the hydrolytic and enzymatic degradation or stability of the biodegradable enhancers.

Abstract: Design of new, safe and effective biodegradable agents, which can cover a wide range of drug molecules in the transdermal permeation and other membranes absorption of physiologically active agents are disclosed. Biodegradable agents includes compounds having a multiple hydrophilic moiety groups which are water loving groups with general chemical structures provide for contributing the penetration enhancement characteristics such as glycolic group and N-alkyl substituted amino acidic group and a lipophilic moiety and also in contributing the balanced lipophilicity of the compounds such as long chain alkyl group are disclosed. More particularly, compounds with R1, and R2, as the steric hindered but can significantly affect the hydrolytic and enzymatic degradation or stability of the biodegradable enhancers.

Abstract: This invention provides monolithic matrix formulations for transdermal administration of molsidomine. The device includes a copolymer of 2-ethylhexyl acrylate, 2-hydroxyethylmethacrylate, and methacrylic acid. The invention also provides transdermal devices having a monolithic matrix made using such a formulation in combination with an active ingredient and a vehicle or vehicle formulation.

Abstract: This invention provides monolithic matrix formulations for transdermal administration of ketorolac tromethamine. The device includes a copolymer of 2-ethylhexyl acrylate, 2-hydroxyethylmethacrylate, and methacrylic acid. This invention also provides transdermal devices having a monolithic matrix made using such a formulation in combination with an active ingredient and a vehicle or vehicle formulation.

Abstract: A skin or buccal patch for providing nicotine replacement therapy which comprises a matrix type laminated composite in which the matrix is composed of a mixture of nicotine in a polymer wherein the amount of nicotine in the matrix, diffusion coefficient of nicotine in the matrix and the thickness of matrix are such that the release of nicotine is: (1) controlled by the patch; (2) rapid and at a relatively high flux over the prescribed wearing time of patch; and (3) such that a substantial proportion of the nicotine initially in the patch has been released at the end of the prescribed wearing time.

Abstract: Pharmaceutical formulations, transdermal drug delivery devices, and methods of drug delivery using the formulations and devices of the invention are disclosed which make it possible to enhance the rate of transdermal drug delivery of pharmaceutically active compounds and in particular molsidomine. The rate of drug delivery is increased by using absorption promoters which include monoalkyl phosphates and salts thereof alone or in combination with other absorption promoters such as polyhydroxyl esters, longchain fatty acids, polyhydroxyl alcohols and terpenes. Particular combinations of monoalkyl phosphates with one or more additional absorption promoters provides synergistic effects with respect to enhancing the rate of drug delivery of certain pharmaceutically active drugs such as molsidomine.

Abstract: Pharmaceutical formulations, transdermal drug delivery devices, and methods of drug delivery using the formulations and devices of the invention are disclosed which make it possible to enhance the rate of transdermal drug delivery of pharmaceutically active compounds and in particular molsidomine. The rate of drug delivery is increased by using absorption promoters which include monoalkyl phosphates and salts thereof alone or in combination with other absorption promoters such as polyhydroxyl esters, longchain fatty acids, polyhydroxyl alcohols and terpenes. Particular combinations of monoalkyl phosphates with one or more additional absorption promoters provides synergistic effects with respect to enhancing the rate of drug delivery of certain pharmaceutically active drugs such as molsidomine.

Abstract: Biodegradable absorption enhancers, especially useful in pharmaceutical formulations, are compounds having the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, benzyl or 4-hydroxybenzyl; n is a whole number from 4 to 18 inclusive; R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 -C.sub.7 alkyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted heterocycloalkyl radical having a total of 5 to 7 ring atoms, optionally including a hetero ring atom selected from oxygen, sulfur and nitrogen in addition to the indicated nitrogen atom, the substituents when present being one to three C.sub.1 -C.sub.7 alkyl radicals, which may be the same or different; and R.sub.3 and R.sub.4 are independently selected from hydrogen, methyl and ethyl.

Abstract: Biodegradable absorption enhancers, especially useful in pharmaceutical formulations, are compounds having the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, benzyl or 4-hydroxybenzyl; n is a whole number from 4 to 18 inclusive; R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 -C.sub.7 alkyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted heterocycloalkyl radical having a total of 5 to 7 ring atoms, optionally including a hetero ring atom selected from oxygen, sulfur and nitrogen in addition to the indicated nitrogen atom, the substituents when present being one to three C.sub.1 -C.sub.7 alkyl radicals, which may be the same or different; and R.sub.3 and R.sub.4 are independently selected from hydrogen, methyl and ethyl.

Abstract: A compound having the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are independently selected from hydrogen; hydroxy; fluorine; bromine; chlorine; C.sub.1 -C.sub.20 alkyl; C.sub.2 -C.sub.20 alkenyl; C.sub.2 -C.sub.20 alkynyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.2 -C.sub.20 (monohydroxy or polyhydroxy)alkyl; C.sub.1 -C.sub.20 (monohalo or polyhalo)alkyl; carboxy; C.sub.1 -C.sub.20 alkylcarboxy; C.sub.1 -C.sub.20 alkenylcarboxy; C.sub.1 -C.sub.20 carboxyalkyl; C.sub.1 -C.sub.20 alkanoyl; C.sub.1 -C.sub.20 alkanoyloxy; C.sub.1 -C.sub.20 alkoxycarbonyl; carbamoyl; carbamyl; C.sub.1 -C.sub.20 alkylcarbamyl; sulfo; C.sub.1 -C.sub.20 alkylsulfonyl; C.sub.1 -C.sub.20 alkylsulfinyl; C.sub.1 -C.sub.20 alkylsulfoxide; C.sub.1 -C.sub.20 alkylsulfone; thio; C.sub.1 -C.sub.20 alkylthio; amino; nitro; C.sub.1 -C.sub.20 alkylamino; C.sub.1 -C.sub.20 aminoalkyl; substituted or unsubstituted phenyl or benzyl, the substituents being selected from hydroxy, fluorine, bromine, chlorine, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.