Abstract: The present invention relates to formulations and methods for pulmonary and nasal administration of raloxifene.

Abstract: The present invention is directed to a microsphere for the controlled release of a biologically active molecule which comprises a biologically active molecule and an ester of hyaluronic acid or mixtures of said esters of hyaluronic acids, and wherein said biologically active molecule is surrounded by or adhered to said ester of hyaluronic acid, and wherein said microsphere has a diameter of between 1 .mu.m to 100 .mu.m.

Abstract: A hyperhydrated form of citicoline and its formulations, which exhibits desirable characteristics, including crystal formation, moisture resistance, improved storage stability, and formulation versatility, is disclosed. Methods of preparing the citicoline hyperhydrate and its use in the manufacture of stable pharmaceutical dosage forms are also described.

Abstract: Powder batches of pharmaceutically-active particles and methods for making same. The pharmaceutically-active particles have a small particle size and a narrow particle size distribution and are particularly useful in devices such as medical inhalers. The present invention also provides an aerosol-based method for producing pharmaceutically-active particles wherein an aerosol is produced having a tightly controlled droplet size to produce pharmaceutically-active particles having a small particle size and narrow particle size distribution.

Abstract: The present invention provides DASC compositions, which upon introduction into aqueous solutions, form stable, non-gritty suspensions. The present invention also provides stable, non-gritty suspensions comprising the DASC compositions of the present invention admixed in aqueous solutions. In addition, the present invention provides processes for preparing the suspensions which comprise admixing the DASC compositions of the present invention with aqueous solutions. Finally, the present invention provides processes for preparing the DASC compositions of the present invention.

Abstract: A flowable personal care or cleaning composition, comprising a carrier and friable beads disbursed in the carrier, the beads containing an active ingredient and enclosing the active ingredient in a wall of bead material, the active ingredient amounting to approximately 0.5-5.0% by weight of the bead including its wall material and the active ingredient.

Abstract: A rapid release tablet involves as an active ingredient tolfenamic acid or its pharmaceutically acceptable salts having a mean particle size of <10 .mu.m, alginic acid or its pharmaceutically acceptable salts in an amount of 1.5-6.0% by weight, and a superdisintegrant in an amount of at least 6% by weight.

Abstract: This invention relates to sustained-release granular preparations obtained by wet-granulating an aqueous suspension, which comprises a medicinal ingredient, a fine particulate polymer having an average particle size not greater than 50 .mu.m and a plasticizer, into granules and treating said granules at a temperature not less than the lower one of a minimum film-forming temperature and glass transition temperature of a mixture of said polymer and said plasticizer. This invention is also concerned with a process for the production of the sustained-release granular preparations. According to the present invention, granular preparations having an excellent sustained-release property and a high safety to the human body can be easily produced in a simple manner.

Abstract: This invention relates to the controlled release of calcium sulfate as well as to the controlled release of an additive to a calcium sulfate matrix such as medicaments or pesticides. The controlled release is achieved by a pellet comprising calcium sulfate. The pellet is prepared by the process comprising mixing powder consisting essentially of alpha-calcium sulfate hemihydrate, a solution comprising water, and, optionally, an additive and a powder consisting essentially of beta-calcium sulfate hemihydrate to form a mixture, and forming said mixture into a pellet, wherein said alpha-calcium sulfate hemihydrate and beta-calcium sulfate hemihydrate powders have specified properties such as BET surface areas, densities, mean particle sizes, and purities. The dissolution rate of the calcium sulfate pellet is controlled by varying the weight ratio of the beta-calcium sulfate hemihydrate powder to the alpha-calcium sulfate hemihydrate powder from 0 to about 3.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: The invention is directed to a hard tablet that can be stored, packaged and processed in bulk. Yet the tablet dissolves rapidly in the mouth of the patient with a minimum of grit. The tablet is created from an active ingredient mixed into a matrix of a non-direct compression filler and a relatively high lubricant content.

Abstract: In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers.The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P.sub.2 O.sub.5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions.In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid.

Abstract: A synthetic particulate vector comprising a non-liquid hydrophilic nucleus and an outer layer at least partially consisting of amphiphilic compounds, which is combined with the nucleus by hydrophobic interactions and/or ionic bonds. A process for preparing a particulate vector by encapsulating an ionizable active principle, vectors obtained according to such a process, and pharmaceutical, cosmeticological and food compositions comprising such vectors are also disclosed.

Abstract: The invention deals with microspheres which are useful in pharmaceutical dosage forms. The microspheres contain active agents and solubilizing agents which have been processed via liquiflash techniques.

Abstract: The present invention relates to dust free, easily flowable and dosable granular compositions containing triazine, having a particle size distribution of between 40 and 400.mu. and an upper limit of particle size at 2000.mu., which can be effectively mixed with feed for administration to animals.

Abstract: An oral-delivery pharmaceutical composition for reducing the gastric irritation effect of an NSAID in the upper GI tract of a mammal. The composition includes (a) a mucosal protective amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants, (b) a dispersion-enhancing amount of another excipient and (c) a therapeutically-effective amount of an NSAID. Also disclosed is a process for preparing the composition and a method for reducing the gastric irritation effect of the NSAID by administering the composition. Also, disclosed is a composition particularly useful for preparing an aqueous suspension.

Abstract: Methods for preparing dry powders having hydrophobic and hydrophilic components comprise combining solutions or suspensions of the components and spray drying them simultaneously in a spray drier. Both the hydrophobic and hydrophilic component are dissolved in a solvent system selected to have adequate solubility for both components. The method provides dry powders having relatively uniform characteristics.

Abstract: The present invention provides a method of producing a composition, suitable for use in pharmaceutical or cosmetic compositions, comprising a micronised insoluble organic UV absorber, which method comprises grinding the insoluble organic UV absorber, in coarse particle form, in a grinding apparatus, in the presence of 0.1 to 30% by weight of an alkyl polyglucoside having the formula C.sub.n H.sub.2n+1 O(C.sub.6 H.sub.10 O.sub.5).sub.x H, in which n is an integer ranging from 8 to 16 and x is the mean polymerization level of the glucoside moiety (C.sub.6 H.sub.10 O.sub.5) and ranges from 1.4 to 1.6, or an ester thereof.

Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and either (b)(1) a carrier of (i) at least one amino acid and (ii) at least one diketopiperazine or (b)(2) at least one mono-N-substituted, di-N-substituted, or unsubstituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.

Abstract: An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (iii) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively hi

Abstract: An ultrafine particle powder for inhalation to be delivered mainly to a lower airway, containing specific cellulose lower alkyl ethers and a medicament, at least 80% of the powder having a particle size in the range of 0.5 to 10 .mu.m.

Abstract: A cosmetic composition containing a hollow spherically shaped aluminosilicate, which is superior in sebum absorption, moisture control, and feeling of use and which has a natural finish.

Abstract: The invention relates to a cosmetic and dermatological preparation for treating sensitive tissue, wounds and hair. The preparation contains (a1) magnetically hard particles such as barium or strontium hexaferrite single crystals, samariumcobalt particles (SmCo) and neodymium-iron-boron particles (Nd.sub.2 Fe.sub.14 B), each with a particle size in the range of 80 to 550 nm, and with a coercive field strength of the particles in the range of 1,000 to 20,000 Oerstedt; or (a2) particles according to (a1), encapsulated in aqueous liposomes or asymmetrical lamellar aggregates, where the aggregates consist of fluorocarbons and natural phospholipids with a phosphatidylcholine content of 30 to 99 wt %; and separately in addition to (a1) or (a2) or mixtures thereof, it also contains asymmetrical lamellar aggregates without encapsulated particles which are loaded with oxygen to the saturation limit. In addition, it also contains excipients and optionally other cosmetic or pharmacological active ingredients.

Abstract: A pharmaceutical composition containing at least one systemically and/or locally effective, topically applicable active substance, preferably selected from the group consisting of local anaesthetics, anti-allergic agents, dermatics, active substances for influenzal infections and colds, active substance for the treatment of neuropathies, chemotherapeutics, quinine, thalidomide, analgesics, non-steroid antirheumatics, opiate receptor agonists, opiate receptor antagonists, substances inhibiting the blood coagulation, substances inhibiting platelet aggregation, corticoids, histamine antagonists, anti-diabetics, regulatory peptides and the inhibitors thereof, prostaglandins and/or the esters thereof and/or antivirally effective substances is described.

Abstract: A pharmaceutical multiple unit particulate formulation in the form of coated cores which includes a pharmaceutically acceptable carrier selected from calcium carbonate, calcium silicate, calcium magnesium silicate, calcium phosphate, kaolin, sodium hydrogen carbonate, sodium sulfate, barium carbonate, barium sulfate, magnesium sulfate, magnesium carbonate, and activated carbon, and an active substance in a layer on the outer surface of the cores.

Abstract: Retinoic acid compositions intended for topical application are incorporated in novel formulations in which they are retained as impregnants inside the pores of porous solid particles or microspheres. The pores form a continuous network open to the exterior of the particles, permitting outward diffusion of the retinoic acid impregnant at a controlled rate depending on the pore size. The impregnated particles are prepared by impregnation of preformed particles with the retinoic acid.

Abstract: A pharmaceutical composition including a mixture of active compounds (A) a pharmaceutically active polypeptide, and (B) an enhancer compound which enhances the systemic absorption of the polypeptide in the lower respiratory tract of a patient, the mixture being in the form of a dry powder for inhalation in which at least 50% of the total mass of the active compounds consists of primary particles having a diameter less than or equal to about 10 microns, the primary particles optionally being formed into agglomerates.

Abstract: The use of complex coacervates of two or more biopolymer materials, preferably at least one of these being gelatin, as a fat-replacing ingredient. The complex coacervates may be used in foods and cosmetics and preferably are of substantially spherical or elliptical shape and have an average D.sub.3,2 particle size, of from 0.2 to 100 microns.

Abstract: Water soluble, powder form compositions suitable for completely and rapidly dissolving active ingredients which usually only dissolve in water in the presence of base salts, such as antibiotics of the betalactamide family, for example penicillins and their derivatives, cephalosporins and their derivatives, or other active ingredients such as sulphamides and quinolones, for oral absorption thereof and their applications. The water soluble powder form compositions contain, in combination and in powder form, at least one water soluble active ingredient, not in salt form, and with an exclusively alkaline pH, an excess of one or more strong base salts, and one or more buffers comprising one or more substances and capable of maintaining the pH of the medium at a level below the normal solubilization pH of said active ingredient. Aqueous solution compositions obtained from said powder form compositions are also described.

Abstract: Nanosols and process for preparing the same allow colloidally dispersed solutions of scarcely water-soluble active substances to be stabilized with gelatin or its derivatives, by partly or fully setting the iso-ionic point (IIP, equivalent to a neutral charge) between the gelatin and the surface charged active substance particles. In order to neutralize the charge of the system composed of active substance particles and gelatin, the surface charge of the particles is compensated by a corresponding opposite charge of the gelatin molecules. For that purpose, a determined charge in relation to the isoelectric point (IEP) and the pH value of the solution is set on the gelatin molecules. By stabilizing in this way the practically monodispersed state thus generated, the Ostwald maturation of the colloidal particles of scarcely soluble active substance is strongly reduced.

Abstract: A pesticidal composition comprising microcapsules, each microencapsulating an organophosphorus compound having a melting point of at least 15.degree. C., a proportion (A) of aromatic ring structure in microcapsule wall material being not more than 40% by weight, and a ratio of (A) to (average diameter/wall thickness) of the microcapsules being not less than 0, but not more than 0.8, causes less color change to applied area even if applied outdoors.

Abstract: The invention relates to microspheres which are suitable for biomedical uses which have a diameter in the range of 10 nm to 2 mm and which comprise a substantially spherical core particle of a non-water-soluble polymer and an outer surface layer consisting substantially of a water-soluble polymer. The water-soluble polymer is conjugated to polyethylene glycol and the non-water-soluble core particle is attached to the water-soluble polymer by the polyethylene glycol moiety. The microspheres are prepared by dissolving the non-water-soluble polymer in a suitable first solvent, dispersing the polymer solution in a solution of the PEG/water-soluble polymer conjugate and evaporating the first solvent to form microspheres in which the PEG anchors the water-soluble polymer to the core particle.

Abstract: Soft gelatin capsules consisting of capsule shell and capsule filling, where the capsule filling comprises one or more water-insoluble active ingredients) in the form of a powdered product.

Abstract: A cosmetic powder composition including a silica-sunscreen aggregate has a smooth light texture and provides ultra sheer coverage as well as enhanced sun protection to the skin.

Abstract: A delivery device for delivering an active substance to a patient at a predetermined time after administration comprises a male hydrogel plug engaged in the neck of a female body. An expandable excipient such as a hydrogel powder or a pharmaceutical disintegrant in powder, slug or tablet form is provided beneath the active substance. In contact with an aqueous medium, the excipient absorbs water and swells such as to rapidly expel the active substance and effectively deliver it from the device.

Abstract: A process for the manufacture of particles comprises mechanically working a mixture of a drug and a hydrophobic and/or hydrophilic fusible carrier in a high speed mixture so as to form agglomerates, breaking the agglomerates to give controlled release particles and optionally continuing the mechanical working with the optional addition of a low percentage of the carrier or diluent.

Abstract: Granules of starch or low protein rice flour are agglomerated to a larger size and a spherical shape by combining the granules with silicon dioxide and water to form a slurry, and drying the slurry by a spray dryer. The agglomerates have better flowability than the granules, and are readily used as direct compression fillers for tablets and capsules in drug or nutrient formulations. Tablets formed from these agglomerates have good hardness and friability, as well as favorable disintegration and dissolution characteristics. Chemically or physically modified starches can also be used, and starches other than rice starches can be included as well.

Abstract: The present invention relates to granules of water-soluble, hygroscopic products having a mean grain size in the range from 200 to 2000 .mu.m, the granule grains consisting of an agglomerate of fine product particles having a mean particle size in the range from 5 to 200 .mu.m, which are covered with a product layer.

Abstract: This invention provides a method for controlling soilborne fungal disease in cultivated field plants such as a peanut crop. Field crop soil is treated with a free-flowing granular fungicide composition which can be applied by aerial means with minimal settling on plant foliage. The granular fungicide composition comprises ammonium bicarbonate and a solid surfactant ingredient, and is effective against soilborne fungi such as a Sclerotinia, Rhizoctonia, Pythium, Fusarium, Phytophthora or Verticillium species.

Abstract: Benzoyl peroxide intended for topical application is incorporated in novel formulations in which it is retained as impregnants inside the pores of porous solid particles or microspheres. The pores form a continuous network open to the exterior of the particles, permitting outward diffusion of the benzoyl peroxide impregnant at a controlled rate depending on the pore size. The impregnated particles are prepared by impregnation of preformed particles with the benzoyl peroxide.

Abstract: A microcapsule contains a pharmaceutically effective amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof and a polymer binder and a method of preparing said microcapsule. The microcapsule is produced by dispersing in an aqueous phase a dispersion of the amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof in a solution of a polymer in an organic solvent to give an s/o/w type emulsion and subjecting the emulsion to in-water drying. The sustained-release microcapsule entraps 2-piperazinone-1-acetic acid compound or the salt thereof, as a drug, in high concentration, and in reducing the initial release of the drug, thereby reducing undesirable side effects of the drug.

Abstract: The present invention is a method of entrapping an additive within carbohydrate bodies. The additive is drawn into the internal structure as a fluid during transformation of the bodies from a substantially amorphous state to a crystalline state. The present invention is also a delivery system including a carbohydrate body having an internal free volume space defined by an at least partially crystalline structure at equilibrium conditions, and an additive loaded within the carbohydrate body.

Abstract: Ionic compositions comprise an active ingredient absorbed within a network of internal pores defined by a plurality of polymeric particles. The particles are preferably crosslinked polymeric beads having a diameter in the range from about 5 to 100 microns and a surface charge density from about 0.1 to 10 meq/qm hydrogen ion capacity. The active ingredients are released from the ionic polymer beads over time when orally administered, applied to a keratinic material, typically human skin or hair or otherwise delivered to a target environment. The use of a cationic charge promotes adhesion of the beads to the keratinic material.

Abstract: Methods and compositions for the treatment of the symptoms of a patient who has a pulmonary condition associated with an inhibition of surfactant secretion by type II alveolar cells are described. The method of treatment involves causing a patient to inhale an amount of a pH-raising buffer effective to raise the pH of the aqueous fluid in the microenvironment of the type II alveolar cell lumenal surface, thereby inducing an increase in the rate of surfactant secretion by type II alveolar cells.

Abstract: This invention relates to sustained-release granular preparations obtained by wet-granulating an aqueous suspension, which comprises a medicinal ingredient, a fine particulate polymer having an average particle size not greater than 50 .mu.m and a plasticizer, into granules and treating said granules at a temperature not less than the lower one of a minimum filmforming temperature and glass transition temperature of a mixture of said polymer and said plasticizer. This invention is also concerned with a process for the production of the sustained-release granular preparations. According to the present invention, granular preparations having an excellent sustained-release property and a high safety to the human body can be easily produced in a simple manner.

Abstract: A delaminated talc has a plurality of high aspect ratio, smooth surface particles. The aspect ratio of the particles is determined by dividing their extent along an upper surface thereof by their thickness. The upper surface is substantially parallel to the lamellar interface direction and the thickness is measured perpendicularly to the interface direction. The upper, lower and side surfaces of the particles are smooth, lacking acute angularity and staircase effect which give rise to increased coefficient of friction and light scattering. The talc is especially suitable in cosmetic and pharmacologic preparations due to its high degree of transparency, skin adhesiveness, lubricity and spreadability.

Abstract: A pharmaceutical composition comprising:i) substantially inert beads; wherein said beads are coated withii) an antifungal agent which is (-)-(2R-cis)-4-?4-?4-?4-??-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-tr iazol-1-ylmethyl)furan-3-yl!methoxy!phenyl!-1-piperazinyl!phenyl!-2,4-dihyd ro-2-?(S)-1-ethyl-2(S)-hydroxypropyl!-3H-1,2,4-triazol-3-one;iii) a binder to enables the antifungal compound to adhere to said beads.The composition enables the antifungal compound, which has very low water solubility, to have enhanced bioavailability in mammals, such as humans.

Abstract: A salt comprising the reaction product of nicotinic acid and an anion exchange resin having a degree of crosslinking with divinylbenzene of less than 4%. These salts are useful in reducing blood cholesterol levels.

Abstract: A pharmaceutical granular composition and method for taste masking bitter, or unpleasant tasting drugs comprising a drug core of a nonsteriodal anti-inflammatory drug, and as a taste masking agents, methacrylate ester copolymers. The method comprises coating the drug cores with separate layers of aqueous dispersions of the copolymers. Additionally, the coating composition may contain plasticizers and conventional excipients. The granules of the present invention can be used in the preparation of chewable tablets which have good palatability and bioavailability. Preferable copolymers are poly(ethylacrylate, methylmethacrylate) to which quaternary ammonium groups have been introduced to modify the permeability of the ester. The coating system of this invention releases the drug by diffusion and is influenced by drug solubility and media pH.

Abstract: The invention relates to a process for the treatment of dried aspartame characterized in that, in a first separation step, particles smaller than 50 .mu.m are removed, with the aid of a stream of air, from aspartame having a particle size distribution with which more than 5 wt. % of the aspartame has a particle size of less than 20 .mu.m and more than 10 wt. % of the aspartame has a particle size of more than 400 .mu.m, and that in a second separation step the product resulting from the first step is subjected to a screening step using a screen that separates at a value between 150 and 250 .mu.m, after which the fraction of the smaller particles thus obtained is recovered as a first product and the fraction of the larger particles is recovered as a second product or is optionally subjected to a further separation step using a screen that separates at a value between 400 and 1000 .mu.m, the fraction of smaller particles thus obtained being recovered as the second product.