Abstract: Sustained release oral drug dosage forms that comprise a tablet or capsule containing a plurality of particles of a solid-state drug dispersed in alkyl cellulose such as hydroxyethylcellulose or hydroxypropylcellulose. Once ingested the tablet or capsule disintegrates to disperse the particles into the stomach where they imbibe water to cause them to swell and also to become slippery, thus enhancing their retention in the stomach. Imbibed water from the gastric fluid dissolves the drug entrapped in the particles and the resulting solution diffuses from the dispersed particles, assuring that no solid drug, which with some drugs is more irritating, contacts the mucosal tissue. A number of embodiments of the dosage form utilizing different drugs are exemplified and the benefits are explained. Aspirin is one example.

Abstract: A pharmaceutical composition for transdermal delivery comprising an effective amount of an active ingredient selected from a benzodiazepine and a benzodiazepine antagonist; isopropanol; propylene glycol; oleic acid; and water. Additionally, the composition may contain diacetin, Cetiol B.RTM., caprylic acid, Silicon fluid, Miglyol.RTM. 840 or transcutol.

Abstract: A composition is disclosed containing nonesterified fatty acids having 14-18 carbon atoms, monoglycerides which are monoesters of glycerol and fatty acids having 14-18 carbon atoms, lysophosphatidylcholine in which the fatty acid moiety has 14-18 carbon atoms and bicarbonate. The compositions can optionally also contain bile salts. These compositions form submicron size colloidal particles and can act as vehicles for transporting orally administered drugs, sources of calories in the form of readily absorbable fats and as particles for topical application to the skin. A method of making these particles is also described.

Abstract: An aqueous cosmetic or dermo-pharmaceutical composition contains, in suspension in the continuous phase, hydrated spheroids of a hydrophilic lipidic substance. The hydrated spheroids have an average particle diameter ranging from 50 to 10,000 .mu.m. A process for the preparation of this composition is described.

Abstract: A method for treating inflammatory bowel disease in a patient by inhibiting the production of interleukin-8 in intestinal epithelial cells by administering to said patient an enema of an effective amount of tributyrin.

Abstract: A cosmetic composition contains saponin and/or diacyl phosphatide in addition to monoacyl phosphatide, which shows improved storage stability at high and low temperatures, organoleptic properties and appearance.

Abstract: A clear, gelled mineral oil based skin protectant especially adapted for irritated skin is provided. The product is clear so the underlying compromised skin can be seen, does not have the normal high drag of petrolatum based products and does not dry out. It contains a mineral oil gel blend which is a hydrocarbon mineral oil blended with di- and tri-block copolymers of hydrogenated butylene/ethylene/styrene copolymer and hydrogenated ethylene/propylene/styrene copolymer.

Abstract: A pharmaceutical composition for transdermal delivery comprising an effective amount of an active ingredient selected from a benzodiazepine and a benzodiazepine antagonist; ethanol; caprylic acid; and oleic acid. Additionally, the composition may contain silicon fluid, benzyl alcohol, transcutol or dimethyl sulfoxide.

Abstract: An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these monoglycerides, and B) at least one chemical substance selected from the following groups: i) local anesthetics of the amide type; ii) carbamide, iii) antibacterial substances in the form of steroid antibiotics, imidazole derivatives or nitroimidazole derivatives, and iv) diols with 3-6 carbon atoms, and C) optionally, a conventional physiologically acceptable carrier and/or physiologically acceptable additives. A process for the preparation of this composition by heating (A) to the transition temperature of the lipid, adding (B), and optionally (C), and cooling the mixture to form a solid lipid crystal composition. Use of the composition for the preparation of a dermatological preparation for combatting bacteria and fungi or as a preservative additive in a cosmetic product, a food product, or a medical product.

Abstract: A biocidal or agrochemical composition comprising particles or droplets of a substantially water-insoluble or sparingly-soluble biocidally-or agrochemically-active substance cosuspended, by an aqueous structured surfactant, with an aliphatic hydrocarbon or glyceride oil, wherein the weight ratio of said surfactant to said active substance is less than 20:1

Abstract: A method is disclosed for reducing the risk of infection by sexually transmitted viruses. This method involves spreading a lubricant fluid containing a selected zinc salt across the surfaces of the penis or vagina, before intercourse, in a manner that causes the lubricant to coat and remain in contact with the genital surfaces throughout intercourse. The zinc salt should be organic, water-soluble, non-irritating, physiologically acceptable, and have a high rate of dissociation, which allows it to release substantial quantities of divalent zinc ions. Suitable zinc salts include zinc acetate, zinc propionate, zinc butyrate, zinc formate, zinc gluconate, zinc glycerate, zinc glycolate, and zinc lactate. A preferred carrier fluid comprises a lubricant gel, which also contains water, a thickening agent (such as chemically treated cellulose) and a lubricating agent (such as glycerin).

Abstract: An aqueous cosmetic or dermo-pharmaceutical composition contains, in suspension in the continuous phase, hydrated spheroids of a hydrophilic lipidic substance. The hydrated spheroids have an average particle diameter ranging from 50 to 10,000 .mu.m. A process for the preparation of this composition is described.

Abstract: An extended-release galenical form of Diltiazem or a pharmaceutically acceptable salt thereof, which comprises beads containing said Diltiazem or a pharmaceutically acceptable salt thereof as an active ingredient and a wetting agent, said beads being coated with a microporous membrane comprising at least a water-soluble or water-dispersible polymer or copolymer and a pharmaceutically acceptable adjuvant.

Abstract: Cosmetic or dermatological composition in the form of a stable oil-in-water emulsion, characterized in that it contains:(a) from 5 to 40% by weight of an oily phase which may contain, in a proportion of less than 15% by weight, at least one vegetable oil which has more than 40% by weight of linoleic acid triglycerides,(b) from 0.5 to 5% by weight of an auto-emulsifiable composition containing from 60 to 90% by weight of at least one fatty alcohol having from 12 to 22 carbon atoms, from 10 to 40% by weight of an alkyl polyoside,(c) from 0.5 to 4% by weight of at least one co-emulsifying agent chosen from fatty alcohols having from 14 to 22 carbon atoms, fatty acids having from 14 to 22 carbon atoms, alkyl glyceryl ethers, the alkyl chain of which has from 14 to 22 carbon atoms, the compounds of formula: ##STR1## in which: R' and R", which may be identical or different, represent a cholesteryl, behenyl or 2-octyldodecyl radical, and the mixtures of the said co-emulsifying agents.

Abstract: Suppository formulations having long-term stability and containing readily bioavailable .DELTA..sup.9 -THC derivatives.

Abstract: Vitamin E acetate, C.sub.3 -linked triesters, glycerin, t-butanol, and transesterified oil/polyethylene glycol are effective dispersing agents for use with hydrofluoroalkanes. Effective amounts of the above are effective in suspending medicaments which are useful in inhalation aerosols, and especially meter-dose inhalers.

Abstract: A detergent composition comprising:(A) glycerol derivative having the following Formula (I) ##STR1## (B) a water-soluble polyhydric alcohol; and (C) at least one surfactant selected from the group consisting of an anionic surfactant, wherein component (A) and component (C) are in a ratio of from 2:1 to 1:100 by weight. When the detergent composition is used to clean skin, the skin remains moisturized after cleaning without stickiness or tackiness and without excess degreasing or dryness.

Abstract: A stable active substance emulsion of the oil-in-water type with a phospholipid as emulsifier is described, where the active substance dissolved in the lipid phase has one or more basic groups, is hydrophobic and oil-soluble, and has a pKa of at least 7.5, the aqueous phase is set at an acid pH, and the disperse phase gives a positive zeta potential of at least +15, but preferably +30, mV after dilution of the emulsion ready for administration to a fat content of 0.08% by weight.

Abstract: This invention relates to storage oil-in-water emulsions, hereinafter referred to as 0/w emulsions, containing alkyl glucosides and a partial glyceride with a monoglyceride content of 60-95% by weight and to emulsifier concentrates containing alkyl glucosides, a partial glyceride with a monoglyceride content of 60 to 95% by weight and a long-chain alcohol.

Abstract: A pharmaceutical composition and a dietary supplement comprising a single cell oil containing at least 20% docosahexaenoic acid (DHA) in triglyceride form are presented. The single cell oil is extracted from biomass produced by cultivating heterotrophic microalgae of the class Dinophyceae in an aerobic fermentor with a nutrient solution having a limited nitrogen source.

Abstract: The present invention is directed to liquid medicinal suspension compositions for the administration of doses of active pharmaceutical agents such as H.sub.2 -antagonists. H.sub.2 -antagonists are known for their adverse taste and/or malodor and the claimed suspension functions to mask the adverse taste and odor of such active ingredients. Also disclosed are liquid medicinal compositions comprising the claimed suspension composition and the H.sub.2 -antagonist active ingredients.

Abstract: A pharmaceutical composition is disclosed in the form of a nonirritating emulsion which includes at least one cyclosporin in admixture with a higher fatty acid glyceride and polysorbate 80. More particularly, the cyclosporin may be cyclosporin A and the higher fatty acid glyceride may be castor oil. Composition has been found to be of a high comfort level and low irritation potential suitable for delivery of medications to sensitive areas such as ocular tissues. In addition, the composition has stability for up to nine months without crystallization of cyclosporin.

Abstract: A novel organic dispersion comprises microfine titanium dioxide and a suitable branched chain organic without the use of any dispersing agent. The novel dispersion provide uniquely high SPF with low levels of dry weight titanium dioxide. Methods for preparing said dispersion and cosmetic sunscreen compositions comprising said dispersion are also included within the invention.

Abstract: Polyglycerol fatty acid ester mixtures of mono- di- and polyesters of polyglycerols having a degree of polymerization of 2 to 8 and at least one saturated and/or unsaturated fatty acid, the mixtures having an HLB of greater than 8 and containing 0 to less than 5 wt-% diglycerol fatty acid esters, 20 to 65 wt-% triglycerol fatty acid esters, 20 to 50 wt-% tetraglycerol fatty acid esters and 5 to 40 wt-% higher polyglycerol fatty acid esters, in which the fatty acid component consists of one or more fatty acids selected from the saturated and/or unsaturated, branched and/or unbranched C.sub.6 - to C.sub.14 -fatty acids containing less than 10 wt-% fatty acids having more than 14 carbon atoms; bath additive preparations containing such polyglycerol fatty acid ester mixtures; methods of using such polyglycerol fatty acid ester mixtures, and a process for preparing such mixtures.

Abstract: Novel fat-based, substantially water-free, insecticidal compositions are described which are particularly effective against insect pests such as cockroaches, ants, termites, flies, etc. The compositions may be used in various forms depending on the targeted pests. As an example, the composition in the form of a paste can be applied into cracks and crevices for control of such pests and have the advantage of superior durability and prolonged attractiveness.

Abstract: The orally administrable pharmaceutical compositions containing a slightly water-soluble drug, characterized by improved stability and improved absorption of the drug from digestive tract into blood. The use of the compositions of the present invention enables decrease of the dose amount of a slightly water-soluble drug, which eventually leads to alleviation of pains and side effects on the part of patients.

Abstract: An angiographic adjuvant comprising a fat emulsion containing a compound having prostaglandin E1 activities, and an angiographic method using the adjuvant.

Abstract: This invention provides a fungicide composition which is capable of in situ generation of ammonium bicarbonate when applied to plant foliage in the form of an aqueous dispersion. The constituents include (1) an ingredient such as urea which slow-releases ammonia under aqueous alkaline pH conditions; and (2) an alkali metal bicarbonate ingredient which imparts alkalinity to the aqueous dispersion, and provides bicarbonate ions for combination with the released ammonium ions. A spreader-sticker ingredient is included to maintain the ingredients in contact with plant foliage over an extended period after application.

Abstract: This invention provides a fungicide composition which is capable of in situ generation of ammonium bicarbonate when applied to plant foliage in the form of an aqueous dispersion. The constituents include (1) an ingredient such as urea which slow-releases ammonia under aqueous alkaline pH conditions; and (2) an alkali metal bicarbonate ingredient which imparts alkalinity to the aqueous dispersion, and provides bicarbonate ions for combination with the released ammonium ions. A spreader-sticker ingredient is included to maintain the ingredients in contact with plant foliage over an extended period after application.

Abstract: Mixtures of ethanol and monoglyceride are disclosed for enhancing the permeation of drugs through skin or mucosa. The monoglyceride is a monoglyceride or a mixture of monoglycerides of fatty acids with a total monoesters content of at least about 90%. Water is also included in the permeation-enhancing mixture.

Abstract: Pharmaceutically acceptable solutions of acidic, basic or amphoteric pharmaceutical agents are disclosed. These solutions are suitable for encapsulation in gelatin capsules for subsequent oral administration and include the pharmaceutical agent, an ion species and a solvent system.

Abstract: The invention relates to a controlled-release composition for a biologically active material, wherein said active material has been dissolved or dispersed in an L2-phase comprising(a) at least one monoglyceride of an unsaturated fatty acid having 16-22 carbon atoms or a vegetable or animal oil containing such a monoglyceride,(b) at least one triglyceride of at least one unsaturated fatty acid having 16-22 carbon atoms or a vegetable or animal oil containing such triglycerides and(c) at least one polar liquid selected from the group consisting of water, glycerol, ethylene glycol and propylene glycol. Such L2 phases are known per se but are novel in this context.The composition is prepared by forming the L2 phase and adding the biologically active material before, during or after the formation of the L2-phase. For sensitive substances such as proteins a mixture of the mono- and triglycerides is added dropwisely to a solution of said substance in the polar liquid.

Abstract: A gastric preparation developed in order to solve the technical problems of conventional preparations, which is prepared by the bilayer packing technique and comprises 5 to 60%, desirably 10 to 40% of a rapid release portion which can establish the therapeutic level of a drug shortly after the administration and 95 to 40%, desirably 90 to 60% of a sustained release portion which has a specific gravity or 1 or less and can maintain a satisfactory release rate.

Abstract: The present invention relates to new plant-protection suspo-emulsions. More specifically, the invention relates to a suspo-emulsion of a solid active substance, having a melting point greater than or equal to 45.degree. C. and which is substantially insoluble in water. The suspo-emulsion comprises at least one oil; a first surface-active system comprising at least sucroglycerides; the solid active substance; and either (A) a nonionic or anionic surface-active agent, or (B) a second surface-active system containing sucroglycerides and at least one compound selected from the group consisting of an alkoxylated triglyceride, an alkoxylated fatty acid, a sorbitan ester, and an alkoxylated sorbitan ester, and optionally a phospholipid.

Abstract: A composition for the sustained release of a biologically active therapeutic agent wherein the matrix of the sustained release composition is composed of an amorphous carbohydrate glass matrix comprising a suitable carbohydrate and an agent which retards the recrystallization of the carbohydrate and a biologically active therapeutic agent and a water-insoluble wax dispersed throughout the matrix. Biologically active therapeutic agents which can be incorporated into the carbohydrate glass matrix include prolactin, growth hormones, serum albumins, growth factors or any biologically active fragment or recombinant form thereof.

Abstract: An emulsified composition having an average particle size of 0.010 to 0.070 .mu.m contains at least the following components (A), (B) and (C):(A) a lipid-soluble drug and a lipid;(B) glycerol and water;(C) a phospholipid and/or a water-soluble nonionic surfactant having a molecular weight of 1000 or more, with (A)/(C) being 0.5 to 5 (weight ratio).

Abstract: The oral absorption of antibiotics given of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of Laureth-12 together with a second component salts of capric acid and caprylic acids. The antibiotic containing two component enhancer system includes Miglyol-812 for optimum absorption.

Abstract: A composition is disclosed containing non-esterified fatty acids having 14-18 carbon atoms, monoglycerides which are monoesters of glycerol and fatty acids having 14-18 carbon atoms, lysophosphatidylcholine in which the fatty acid moiety has 14-18 carbon atoms and bicarbonate. The compositions can optionally also contain bile salts. These compositions form submicron size colloidal particles and can act as vehicles for transporting orally administered drugs, sources of calories in the form of readily absorbable fats and as particles for topical application to the skin. A method of making these particles is also described.

Abstract: A cosmetic composition is provided having exceptional emulsion stability. The composition includes water, petroleum jelly, a sterol, a phosphatide and a C.sub.16 -C.sub.22 alkanoic triglyceride.

Abstract: A process for preparing a nonionic surfactant includes the steps of: cleaving at least one of the isopropylidene groups of an isopropylidene polyglycerol C.sub.6 -C.sub.22 -fatty acid or mono- or polyhydroxy fatty acid ester, by hydrolysis or ketal exchange, in the presence of acid, at a temperature in the range of about 20.degree. C. to about 100.degree. C., and at atmospheric, reduced or superatmospheric pressure, thereby regenerating hydroxyl groups on the polyglycerol; and recovering the resultant polyol ester nonionic surfactant. Such polyol ester surfactants are useful as emulsifiers, especially for preparing skin care or cosmetic formulations and paints and wood-preservation agents.

Abstract: A pharmaceutical solution which contains the compound of the general formula having the immusuppreseive activity is disclosed.

Abstract: A topical preparation for aiding in the care of minor skin irritations, such as chapping, reddening, tenderness, and the like, has as its constituents a mixture of glycerin, stearic acid, cocoa butter and boric acid blended together in a creamy base.

Abstract: The invention relates to emulsions intended for parenteral administration and contaning a hydrophobic phase emulsified in a an aqueous phase. In accordance with the invention, a substantial part of the hydrophobic phase contains one or more alkyl esters of pharmacologically acceptable fatty acids, and particularly their ethyl esters. The emulsions can be used for parenteral nutrient supply and as vehicles for pharmacologically active substances or agents and may also be used for both purposes in combination.

Abstract: A free flowing powder is prepared containing a water-soluble vitamin E compound and at least one fatty acid ester of glycerine. The powder is prepared by blending a low viscosity mixture of the vitamin E compound and fatty acid ester followed by spraying.

Abstract: An in vivo method is described for treating a subject for periodontal disease by placing a mixture of a glyceride composition and a therapeutic agent in the periodontal pocket of subject such that the therapeutic agent is released in a sustained manner. The glyceride composition is selected such that the mixture of the glyceride composition and the therapeutic agent is capable of forming a gel in the environment of the periodontal pocket. Also described is a sustained release delivery system comprising the mixture of the glyceride composition and therapeutic agent.

Abstract: This invention relates to a nonionic cold mix emulsion and preparation thereof. More particularly, the present invention relates to a cosmetic composition in the form of a cream preparation which comprises a discontinuous phase dispersed in a continuous phase. The continuous phase contains water, an emulsifier, and at least one oxidizing agent. The discontinuous phase contains salts of fatty acid esters of lactylic acid, saturated monoglycerides and propylene glycol monoesters. The emulsions are particularly suitable as components of oxidizing preparations for the bleaching of hair and for the dying of hair with oxidation hair dyes and hair bleaches.

Abstract: The use of monoacyl phosphoglycerides to enhance the penetration of topically applied ophthalmic drugs through the corneal epithelium is described.

Abstract: The controlled release of therapeutically active agents is achieved from a controlled release matrix of sodium alginate and a calcium salt. When the composition is to be administered rectally, the matrix is combined with a therapeutically active agent and a suitable suppository base. When the composition is to be administered orally, the matrix further includes a higher aliphatic alcohol.

Abstract: This invention relates to the use of zinc salts as anti-viral agents in sexual lubricants. A zinc salt which releases divalent zinc ions in an aqueous carrier fluid is provided in a sexual lubricant formulation which is spread on the genitals before sexual intercourse. The mixture is non-irritating, and the zinc ions serve as an anti-viral agent to reduce the risk of contracting genital herpes if a sexual partner is infected. These lubricants may also reduce the risk of infection by other sexually transmitted viral diseases, such as hepatitis, papilloma viruses, and AIDS. A preferred lubricant formulation comprises water, a thickening or suspending agent, a lubricating agent, and a suitable zinc salt. Salts which have been tested and shown to be non-irritating during sexual intercourse include zinc acetate, zinc propionate, and zinc gluconate. Other zinc salts have also been identified which are soluble in water and have low pK values, which indicates a high rate of zinc ion release.

Abstract: Fatty acid esters of polyglycerols, such as stearic acid penta(tetra)glyceryl ester, behenic acid hexa(tetra)glyceryl ester, lauric acid mono(deca)glyceryl ester, oleic acid di(tri)glyceryl ester, linolic acid di(hepta)glyceryl ester, palmitic acid deca(deca)glyceryl ester, etc. are employed as coating agents for coating solid preparations such as tablets, pills, granules, fine granules, etc. By coating with the coating agents, stable sustained release of active ingredients contained in the preparations is obtained, even after a long period of storage.