Abstract: A mixture of estradiol or other estrogen and an uncrosslinked, water-insoluble vinylpyrrolidone copolymer provides a matrix which gradually releases the medicament upon application to the skin of a patient in the form of an ointment, gel or film. The polymer provides for the slow and sustained release of the medicament upon topical application to the skin so that the concentration of drug in the blood plasma of the patient is maintained within the levels required for clinical efficacy.

Abstract: Compositions comprising a calcitonin gene related peptide and, as an absorption enhancer, a glycyrrhizinate.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH.sub.2).sub.

Abstract: A novel endermic medicament having a consistency of a gel is proposed which is formulated, as a gel base, with non-ionic water-soluble cellulose ether, e.g., methyl cellulose and hydroxypropyl methyl cellulose, modified with a modification agent containing, in the molecule, an alkyl group having 6 to 26 carbon atoms and a functional group having reactivity with the hydroxyl group in the cellulose ether, e.g., stearyl glycidyl ether, decyl glycidyl ether and cetyl epoxide. The endermic medicament formulated with the modified cellulose ether is stable by virtue of the very little interaction between the active ingredients and the gel base and also can exhibit high percutaneous absorptivity of the active ingredients through the human skin.

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: The invention relates to a monolith transdermal therapeutic system for the delivery of permeable drugs, especially formoterol, in the form of a matrix system comprising three layers: a) a backing layer which is impermeable to the components of the adhesive layer b),b) an adhesive layer capable of releasing the drug and consisting of a permeable polymeric material which is compatible with the skin and contains at least one drug which is capable of permeation across the skin, a combination of eucalyptol having a purity of at least 70% with an additional flux enhancer and further optional pharmaceutical excipients, andc) a protective release liner which can be peeled from the adhesive contact layer b).

Abstract: Improved bioavailability, particularly when the drug is administered orally, of the active ingredient 2-hydroxy-5-methyllaurophenoxime (HMLO) of a pharmaceutical preparation is achieved by improving the absorption of the active ingredient HMLO significantly by including bile acids in the preparation. As bile acids, it is possible to use, for example, desoxychloic acid or dehydrocholic acid or a mixture of the two in the form of their salts.

Abstract: A conditioning activator for a no-lye hair relaxer and a conditioning hair relaxer system includes a conditioning agent which is a water-soluble cationic compound. In a preferred embodiment the cationic conditioning agent is a cationic polymer. Also disclosed are methods for preparing phase-stable no-lye cream bases suitable for conditioning hair relaxer systems.

Abstract: Compositions of zwitterionic drugs for transdermal administration and methods of administering zwitterions transdermally are disclosed. The compositions comprise a zwitterionic drug in a salt form and a solvent therefor.

Abstract: A composition useful for administering therapeutically active compounds to improve the body absorption and/or retention thereof comprising a composition includes a therapeutically active compound having a molecular weight below about 5,000, having an acidic functional group and a pKa of .ltoreq.6 at pH 7.4 normally eliminated unmetabolized from the body via the renal tubular secretion pathway for organic anions, for example, Vitamin C, and at least one compound selected from the class consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible salts, aldono-lactones and aldono-lactides thereof.A method for establishing and maintaining body levels of a therapeutically active compound includes the step of administering a therapeutically effective dose of this composition.

Abstract: Absorption of Tissue Respiration Factor (TRF) into the gingival tissues is materially enhanced when it is formulated as a non-astringent hydrophilic pharmaceutical composition containing penetration promoting substances which are both hydrophilic and lipophilic. Additionally, a highly efficient means for effecting absorption of TRF into the gingival tissues is to utilize liposomes as carriers for the TRF in a non-astringent pharmaceutical composition.

Abstract: This invention is concerned with a composition of matter and method of applying same for use as hair grooming aid or preferably, to treat androgenetic alopecia comprising (a) an effective amount of a polysaccharide or mixtures thereof, polysaccharide derivatives or mixtures thereof, or any combination of the foregoing; and (b) a minor amount of a fatty acid ester of sorbitol and its anhydrides, or mixture of said fatty acid esters; and (c) a minor amount of a lower alkyl ester of p-hydroxy benzoic acid or mixture of said esters; and (d) water sufficient to create a composition of 100% by volume.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The composition contains diethylene glycol monoethyl or monomethyl ether in addition to an ester component such as propylene glycol monolaurate, methyl laurate or the like. The compositions are particularly useful in conjunction with the transdermal administration of steroid drugs such as progestogens and estrogens. Methods and drug delivery systems for using the enhancer compositions are provided as well.

Abstract: Method and compositions for enhancing the cutaneous penetration of topically or transdermally delivered pharmacologically active agent. The compositions include various urethane compounds as permeation enhancers, the urethane compounds formed from reaction of a monomeric organic diisocyanate with a hydroxy- or hydroxy/alkoxy-terminated linear alkylene or polyalkylene glycol or polyether.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: Topical pharmaceutical compositions containing a specific 6-amino-1,2-dihydro-1-hydroxy-2-iminopyrimidine component and a penetration-enhancing vehicle are disclosed. The vehicle comprises a binary combination of a C.sub.3 -C.sub.4 diol or C.sub.3 -C.sub.6 triol and isocetyl alcohol polar lipid compound. The vehicle provides marked transepidermal and percutaneous delivery of the iminopyrimidine compound. These compositions, when applied topically, act to stimulate the growth of mammalian hair on the body.

Abstract: Improved hexamethylmelamine containing parenteral emulsions are prepared in the absence of organic solvents and containing low levels of biocompatible emulsifiers using ultrahigh energy Microfluidizer.RTM. processing equipment. The emulsions have oil phase droplets with average diameters of less than about 0.4 microns with size distributions of less than about +/-50%.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: The novel compound, 3-hydroxy-N-methylpyrrolidone, is effective as a transdermal enhancer for the absorption of drugs through the skin of humans and animals. The 3-hydroxy-N-methylpyrrolidone is prepared from delta-butyrolactone which is converted to methyl 2,4-dibromobutyrate, this intermediate is reacted with methylamine to form N-methyl-2,4-dibromobutyramide, this intermediate is converted to 3-bromo-N-methyl-2-pyrrolidone by ring closure, and the 3-bromo-N-methyl-2-pyrrolidone is reacted with an alkaline earth metal carbonate or alkaline metal carbonate to form 3-hydroxy-N-methyl-2-pyrrolidone.

Abstract: The invention relates to a transdermal therapeutic system in the form of a multilayer plaster for the administration of active substances which are able to permeate, in the form of a matrix system containing at least three layers:(a) a covering layer which is impermeable for the constituents of the reservoir b);(b) a reservoir layer which is able to deliver active substance and which consists of optionally crosslinked block copolymer based on styrene, alkadienes and optionally alkenes mixed with adhesive polymers and is optionally provided with an additional adhesive membrane layer and contains at least one active substance capable of skin permeation, at least one agent promoting the skin permeability of active substances and optionally further pharmaceutical auxiliaries, and(c) a protective film which can be pulled off the reservoir layer.

Abstract: A method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I: ##STR1## wherein R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms, alkoxyalkyl, haloalkyl, specifically trifluoromethyl, alkoxy, amino, alkylamino and acylamino; R' and R" are hydrogen, alkyl, trifluoromethyl, alkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, carboxy, carbalkoxy, hydroxyalkyl or lower alkyl ester thereof; X is O or NR.sub.1 wherein R.sub.

Abstract: Transdermal flux enhancers such as oleic acid and 1-dodecylazacycloheptan-2-one are used in combination with iontophoresis in the topical administration of pharmaceutical agents.

Abstract: Penetration of various drugs through living membranes is improved by their use in transdermal compositions containing certain penetration-enhancing systems. A new delivery device is also described.

Abstract: The transdermal flux rates of 1,4-dihydropyridine derivatives, such as nilvapidine and its enantiomers may be increased by the use of a solvent vehicle which comprises dioctyl adipate, isopropyl myristate, benzyl alcohol, diisopropyl adipate, a mixture of 5 to 50% ethyl alcohol and 95-50% of diisopropyl adipate, or a mixture of any of the foregoing.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## Wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --Ch.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

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: The instant invention relates to a drug-delivery device for the controlled release of HMG-CoA reductase inhibitor salts, as the therapeutically active ingredient, into an environment of use which comprises:(A) a core composition comprising(1) a water insoluble, non-diffusible, charged resin entity, and(2) a diffusible, water soluble ionizable therapeutically active HMG-CoA reductase inhibitor salt carrying the same charge as said resin entity; and(B) an imperforate water insoluble wall surrounding said core composition and prepared from a semipermeable material substantially impermeable to core composition and permeable to the passage of an external fluid in the environment of use, with said wall having a means for release of the therapeutic agent through the water insoluble wall; or(C) a water insoluble wall surrounding said core composition and prepared from (1) a polymer material that is permeable to water but substantially impermeable to solute and (2) 0.

Abstract: A muscosal delivery system is provided for use in treating periodontal disease. The system is composed of a chemotherapeutic agent dissolved in a skin-penetration enhancer. The solution of chemotherapeutic agent and skin-penetration enhancer is placed into the periodontal pocket where the agent is transported into the surrounding gingival tissue by means of the penetration enhancer.

Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.

Abstract: A composition useful for administering therapeutically active compounds to improve the body absorption and/or retention thereof comprising a composition which includes a therapeutically active compound having a molecular weight below about 5,000 and having an acidic functional group, which is normally eliminated from the body via the renal tubular secretion pathway for organic anions, for example, Vitamin C, and at least one compound selected from the class consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible salts, aldono-lactones and aldono-lactides thereof.A method for establishing and maintaining body levels of a therapeutically active compound which includes the step of administering a therapeutically effective dose of this composition.

Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.

Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.

Abstract: Compositions and methods useful for the prevention or treatment of a human or animal disorder or for the regulation of the human or animal physiological condition are provided. The compositions used comprise, in admixture, a biologically-effective amount of a drug specific for the disorder or condition and a biocompatible, water-soluble, amphiphilic steroid, other than a natural bile salt, which is capable of increasing drug permeability of the human or animal body surface across which the drug is to be administered, in an amount effective to increase the permeability of the surface to the drug.

Abstract: A transdermal drug delivery system with a dual permeation enhancer is described. The transdermal system comprises a body that contains supplies of drug and a dual permeation enhancer comprising sucrose cocoate and methyl laurate, and has a basal surface that contacts an area of skin and transmits the drug and the dual permeation enhancer to the area for absorption thereby. A method for coadministering a drug and a dual permeation enhancer comprising sucrose cocoate and methyl laurate is also described.

Abstract: A percutaneous absorption accelerator and a percutaneous absorbent preparation containing the same and, more particularly, a percutaneous absorption accelerator containing either derivatives of specific glycerols or polyglycerols and alcohols as effective components and a percutaneous absorbent preparation containing the percutaneous absorption accelerators and pharmaceutically effective components.

Abstract: Cosmetic Base composition exhibiting therapeutic properties comprising an acyl fatty acid alpha-hydroxy carboxylic acid ester or alkali metal salt thereof, a sucrose fatty acid ester, and a solvent.

Abstract: A preparation for the once-daily, percutaneous administration of nicotine comprises nicotine uniformly distributed in a solid, semi-solid or mucilaginous medium which can be placed in intimate contact with the skin, the solid, semi-solid or mucilaginous medium is formed by adding a given amount of nicotine to a solution of a solidifying or gel-forming agent or mixture thereon in a suitable solvent or mixture of solvents and mixing or heating the mixture thereby obtained so as to form the solid, semi-solid or mucilaginous medium.The preparation can be used in a method of treating withdrawal symptoms associated with smoking cessation and for combating the psychological dependence that occurs through frequency smoking.

Abstract: Disclosed herein are compositions and methods for enhancing the transdermal delivery of physiologically active agents across mammalian skin or membranes and which comprise a percutaneous transfer enhancing amount of menthol and a drug.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or 2 hydrogen radicals; Y may represent --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; q is 2, 4, 6 or 8; wherein p.gtoreq.9; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl. These compositions are useful in topical or transdermal applications of the physiologically-active agent.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carboalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4

Abstract: The penetration of various drugs through living membranes, eg., skin, is improved by their use in topical compositions containing certain penetration-enhancer systems.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 10 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R.sup.1 and R.sup.2 is 5 or more.

Abstract: Medicinal compositions containing a water soluble absorption promoter having chelating activity, preferably in the presence of a salt at a concentration exhibiting higher osmotic pressure than isotonic sodium chloride solution, to promote absorption of the medicine through a gastrointestinal organ such as colon or rectum, and through the vagina.

Abstract: The present invention relates to 1-substituted derivatives of 4-methoxy-2,3,6-trimethylbenzene which are useful in cosmetic or pharmaceutical preparations for use in the treamtnet of dermatological complaints connected with a keratinisation disorder, dermatological complaints having an inflammatory and/or immuno-alleric component or ophthalmological complaints.

Abstract: This invention is a method of inducing a reservoir effect in skin and mucous membranes so as to enhance penetration and retention and reduce transdermal flux of topically applied therapeutic and cosmetic pharmacologically active agents. The invention also relates to topical treatment methods involving such reservior effect enhancers, and to pharmaceutical compositions containing them.

Abstract: Disclosed herein are compositions and methods for enhancing the transdermal delivery of physiologically active agents across mammalian skin or membranes and which comprise a percutaneous transfer enhancing amount of 1-carvone and a drug.

Abstract: Disclosed herein are compositions and methods for enhancing the transdermal delivery of physiologically active agents across mammalian skin or membranes and which comprise a percutaneous transfer enhancing amount of eugenol and a drug.

Abstract: This invention provides compositions comprising a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen. The invention also provides compositions comprising a physiologically-active agent and the hereinabove recited 1-substituted azacycloalkane compound in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: An azacycloalkane derivative useful for promoting the absorption of a medicine, an absorption promoting agent comprising at least one of the azacycloalkane derivatives as the effective ingredient for promoting the absorption and an external preparation containing the absorption promoting agent, the derivative being represented by the following formula ##STR1## wherein A is --CH.sub.2 -- or --S-- for example, B is sulfur or oxygen, R is --SR" in which R" is an alkyl group or alkylthioalkyl group for example, or --OR" in which R" is as defined above, an alkyl group or substituted amino group, R' is a hydrogen atom, alkyl group or alkyloxy group for example, m is an integer of 0-5 and n is an integer of 1-15.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comnprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X represents sulfur, oxygen or 2 hydrogen radicals; Y represents --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; wherein p.gtoreq.9; q is 2, 4, 6 or 8; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl.