Abstract: Compositions and methods for prevention of adhesion formation, whereby an effective amount of quinacrine as active agent is administered for a period of time sufficient to permit tissue repair. The active agent is preferably administered in conjunction with a delivery vehicle (e.g., microcapsules, microspheres, lipid-based systems, viscous instillates and absorbable mechanical barriers) useful for maintaining local concentrations of the compound at an effective level.

Abstract: Stable, cold water-dispersible, liquid or pulverous compositions of fat-soluble substances which contain fish gelatin as the protective colloid and a method of making same are described.

Abstract: A process for the preparation of a dry adsorbable extract of at least one active ingredient, comprising the steps of: first, preparing an extract of the active ingredient in a solvent medium specific to the active ingredient; second coating granules of an absorbent carrier with the extract; third drying and calibrating to a predetermined size the coated granules; and finally absorbing the coated granules produced in step 3 in and on porous excipient nebulized microgranules, which have cavities and ducts which are partially filled by the coated granules, with a ratio of between 5 and 20 parts by weight of coated granules to 100 parts microgranules.

Abstract: There are disclosed herein a gelatin coating composition which comprises succinated gelatin as the main component and polyethylene glycol, and a hard gelatin capsule formed from said gelatin coating composition. The hard gelatin capsule has sufficient mechanical strength for filling operation. Moreover, it does not become insoluble due to reaction with a special drug having an aldehyde group filled therein. Therefore, it can be used for various drugs, especially macrolide antibiotics for which conventional hard gelatin capsules are inadequate.

Abstract: A controlled release formulation for use with a variety of drugs or hormones are formed in microspherical form. The drug or hormone, e.g. bovine somatropine, is suspended in a polymer matrix. The polymer matrix is formed from at least two highly water soluble biodegradable polymers, selected for example from starch, crosslinked starch, ficoll, polysucrose, polyvinyl alcohol, gelatine, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl-ethyl cellulose, hydroxypropyl-methyl cellulose, sodium carboxymethyl cellulose, cellulose acetate, sodium alginate, polymaleic anhydride esters, polyortho esters, polyethyleneimine, polyethylene glycol, methoxypolyethylene glycol, ethoxypolyethylene glycol, polyethylene oxide,poly(1,3 bis(p-carboxyphenoxy) propane-co-sebacic anhydride, N,N-diethylaminoacetate, block copolymers of polyoxyethylene and polyoxypropylene. The microspheres are coated with a (d,1 lactide-glycolide) copolymer.

Abstract: An oral dosage form of morphine is formulated by powder-layering an homogeneous mixture of morphine sulfate and hydrous lactose impalpable onto inert beads to obtain a multiparticulate product. A plurality of the powder-layered beads may be administered either in immediate release form or in an extended release form by coating with a hydrophobic material.

Abstract: The invention is directed to exactly dosable molded particles, for example granulates or pellets comprising hydrophilic macromolecules, active materials and additionally further pharmaceutically acceptable skeleton formers and additives wherein the active substance is provided to the matrix, dissolved, suspended or emulsified and a new process for the preparation of such molded particles wherein the process is particularly economically and ecologically unburdensome, as well as the use of such molded particles as pharmaceuticals in which the bioavailability, shelf life, and acceptability ar improved. Furthermore, by means of the molded particles of the present invention, mixtures, intermediates, and end products may be provided for the fields of pharmacy, cosmetics, diagnostics, and analysis and dietetics (health care).

Abstract: Plant extract containing pellets are formed by a dispersion of plant extract or extracts in a matrix, principally comprising a skeleton builder namely collagen, gelatin, fractionated gelatin, a collagen hydrolysate, gelatin derivative plant proteins, or plant protein hydrolysates. They are shelf stable and their pharmacological as well as cosmetic properties are substantially unchanged in comparison to the native extracts. They may be produced by a simple process in which a solution of the skeleton former is mixed with liquid plant extract or emulsified with solid extracts, dissolved or suspended, the dispersion of the skeleton former and the plant extract dropped into a very cold inert fluid, suitably liquid nitrogen, to form the pellets and the thus formed pellets dried.

Abstract: Aloe vera juice containing pellets are formed by a dispersion of aloe vera juice in a matrix, principally comprising a skeleton builder namely collagen, gelatin, fractionated gelatin, a collagen hydrolysate, gelatin derivative, plant proteins, or plant protein hydrolysates. They are shelf stable and their cosmetic as well as pharmacological properties are substantially unchanged in comparison to the native extracts. They may be produced by a simple process in which a solution of the skeleton former is mixed with aloe vera juice extract, the dispersion of the skeleton former and the aloe vera juice into a very cold inert fluid, suitably liquid nitrogen, to form the pellets and the thus formed pellets dried.

Abstract: The present invention is directed to dihydropyridine derivative containing pellets comprising a dispersion of the dihydropyridine derivatives in a matrix which is substantially formed of a skeleton builder such as gelatin, fractionated gelatin, a collagen hydrolysate and/or a gelatin derivative. The invention further directs to a process for the preparation of dihydropyridine derivative containing pellets as well as their use as acute dosage forms against heart/circulatory illnesses.

Abstract: The present invention relates to oral compositions in the form of microcapsules which reduce oral bacteria and provide long lasting breath protection.

Abstract: A pharmaceutical dosage form comprising gelatin encapsulating a pharmaceutical composition wherein said composition is at least about 6% (weight %) ethanol and lipid wherein said lipid comprises at least about 60% (weight %) and a method of protecting gelatin from deterioration is disclosed.

Abstract: A drug for preventing the absorption of food materials dissolved during digestion, a drug for preventing obesity, a drug for treating hyperlipemia, a drug for treating diabetes mellitus, and a drug for preventing constipation, wherein the flocculant and other auxiliary additives at request, are coated with the aquatic enteric material.

Abstract: A microgranular preparation having a core of biologically active material that is encapsulated by a water soluble film that is covered by an enteric coating of either an alkali soluble, acid insoluble polymer or a high molecular weight polymer whose structure is substituted with or contains windows of fatty acids or other material capable of being solubilized by intestinal juices. Useful for protecting pH sensitive and other biologically active materials from inactivation or contact with the stomach or rumen, and releasing the same in active form in the intestinal tract, particularly the duodenum.

Abstract: This invention discloses a composition comprised of nanoparticles having a surface modifier adsorbed on the surface thereof and a non-ionic cloud point modifier associated therewith, which cloud point modifier is present in an amount-sufficient to increase the cloud point of the surface modifier. A preferred surface modifier is a poloxamine such as Tetronic 908, and preferred non-ionic cloud point modifiers include polyethylene glycol, propylene glycol, ethanol, hydroxypropylcyclodextrin and/or glycerol. This invention further discloses a method of making nanoparticles having a surface modifier adsorbed on the surface and a non-ionic cloud point modifier associated therewith, comprised of contacting said nanoparticles with the cloud point modifier for a time and under conditions sufficient to increase the cloud point of the surface modifier.

Abstract: A seamless capsule comprising a content and a film for coating said content is disclosed. The content is a hydrophilic substance. A viscous liquid having a viscosity of not more than 1000 cp at 100.degree. C. which is scarcely miscible with water is present between the content and the film. There is also disclosed a process for producing a seamless capsule which comprises simultaneously extruding a film solution for the seamless capsule, a hydrophilic substance solution and a viscous liquid which is scarcely miscible with water into a cooling solution from a concentrically arranged multiple nozzle composed of at least three nozzles, an outermost nozzle, an innermost nozzle and at least one intermediate nozzle placed in the middle position between the above nozzles, respectively, the diameter of said nozzle gradually increasing in that order.

Abstract: Disclosed are a crosslinked gelatin microspheres containing CSF and a water soluble CSF-gelatin conjugate. Both the microspheres and the water soluble conjugate provide an improved CSF stability. They have a high potentiation on the antitumor activity of macrophages in respect of the CSF amount and the time required for macrophage activation and are effective in maintaining their activated state for a long period, compared with the native CSF. The mechanism of macrophage activation by the microspheres containing CSF is mediated via phagocytosis and different from that by native CSF, which is believed to activate macrophages via cell surface receptor. The species specificity of CSF may be abrogated when the CSF is internalized into macrophages through phagocytosis.

Abstract: The invention provides a method for the application of gelatin-resorcinol aldehyde glue to a surface, wherein a solution of gelatin-resorcinol is applied to the surface to obtain a gelatin-resorcinol coated surface. Subsequently, a solution of an aldehyde is aerosolized onto the gelatin-resorcinol coated surface. The mixture of gelatin-resorcinol and the aldehyde is then allowed to polymerize on the surface. The methods of the invention may be conveniently and efficiently used to apply gelatin-resorcinol aldehyde glue to high porosity vascular prostheses, either before or after implantation, to provide improved hemostasis.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier.A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: The present invention relates to oral compositions in the form of microcapsules which reduce oral bacteria and provide long lasting breath protection.

Abstract: The present invention provides collagen constructs and methods of making and using such constructs. The present invention also provides tissue equivalents having improved characteristics and methods of making and using such tissue equivalents. This invention also provides methods of producing highly concentrated solutions of collagen.

Abstract: A controlled release formulation of a calcium channel blocker for oral administration contains non-pareil seeds loaded with a calcium channel blocker, particularly diltiazem, nifedipine, or verapamil, and then microencapsulated in ethylcellulose by phase separation techniques. The resultant microcapsules provide an approximately zero order release rate, preferably over 12 to 16 hours. These microcapsules may be filled into gelatin capsules.

Abstract: A soft capsule composed of a plurality of cells coalesced to each other and filling substances encapsulated in the individual cells, the wall of at least one of the cells being formed of a material different from a material forming the wall of at least one of the other cells, and said capsule being seamless.

Abstract: A drug delivery composition comprising a plurality of microspheres and active drug associated with each microsphere, the drug being for systemic delivery and having a maximum molecular weight of 6000, and the composition being substantially free of an enhancer. The microspheres may be of starch, gelatin or albumin. Suitable drugs include peptides, such as insulin, and antigenic vaccine ingredients. The compositions are suitable for delivery across a mucosal surface such as the vagina, eye or nose.

Abstract: A simulated capsule-like medicament comprising a dual subcoating comprising an initial subcoating of a water soluble film forming polymer, e.g. povidone and a secondary subcoating of a mixture of two soluble film forming polymers, e.g. povidone and hydroxypropyl methylcellulose and a hydrophobic plasticizer, e.g. castor oil, which provides for a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; and a process of making such medicaments.

Abstract: A stable immunogen composition for oral administration which includes a dried spherical form comprised of an immunogen capable of immunizing human or animals and a gelatin having an average molecular weight of 80,000-120,000 and jelly strength of more than 150 (Bloom, g, 6.2/3%), and is enteric.

Abstract: A salt sensitive capsule has been developed which dissolves in the mouth and releases the encapsulated internal ingredient(s). The outer salt sensitive shell maintains its integrity when kept at a preselected aqueous salt concentration. When introduced into the mouth, the degree of salinity is lower and causes the shell to disassociate and release the internal component. The capsules may be associated with an adhesive system so that the capsules are topically applied to mouth tissue. The adhesive system is compatible with maintenance of the salt sensitive shell.

Abstract: A pharmacological agent-lipid solution preparation comprising a lipophilic pharmacological agent, a desalted charged lipid and an aqueous-miscible lipid solvent such that upon introduction into an aqueous medium a suspension of lipid aggregates associated with the pharmacological agent are formed, and methods of manufacture and use.

Abstract: A particulate carrier, including a hydrophilic, non-liquid core, a first layer or ring of lipid nature bonded to the core by covalent bonds and a second layer or outer shell of amphiphilic compounds bonded to the first lipid by hydrophobic interactions.

Abstract: Pharmaceutical tablets having increased slipperiness and swallowability are provided. The enhanced swallowability is imparted by an overcoat of a low bloom gelatin, which overcoat has a lower coefficient of friction than other known coatings.

Abstract: Microcapsules which are prepared using coacervation processes and/or which have a complex structure in which there is a large central core of encapsulated material, preferably perfume, and the walls contain small wall inclusion particles of either the core material or some other material that can be activated to disrupt the wall are disclosed. The microcapsules that are prepared by coacervation and contain perfume are especially desirable for inclusion in fabric softener compositions that have a pH of about 7 or less and which contain cationic fabric softener. The encapsulated perfume preferably does not contain large amounts of relatively water-soluble ingredients. Such ingredients are added separately to the fabric softener compositions. Ingredients that have high and low volatilities as compared to, e.g., the desired perfume, can either be added to, or removed from, the perfume to achieve the desired volatility.

Abstract: A cosmetic composition on an external treatment agent containing microcapsules, with an average particle size of 0.1 to 2000 .mu.m, enclosing a hydrophobic component, wherein the microcapsules are composed of a gelatin film swollen with water.

Abstract: A new delivery system for zinc compounds and the process for its preparation is disclosed, which has use in a variety of products including comestibles such as chewing gum compositions, confections, pharmaceuticals, food products such as vitamin preparations, dentifrice compositions and throat lozenges. More particularly, this invention relates to a process for preparing a zinc compound delivery system comprised of a zinc core material coated with a first hydrophilic coating comprising a hydrocolloid material and a second hydrophobic coating selected from the group consisting of fats, waxes and mixtures thereof. The delivery system provides enhanced masking of the bitter flavor characteristic of zinc compounds, as well as reduced grittiness with retained stability at the elevated temperatures of product formulation.

Abstract: This invention relates to microcapsules based on gelatin and anionic polysaccharides of low molecular weight which may contain solid or liquid matters, prepared by coacervation. The aqueous polysaccharide solutions which may be used present a low viscosity, the value of which is a function of the nature of the polysaccharide; for a concentration of 15 g/l, it is, at 75.degree. C., generally between 1 and 20 mPa.s. These polysaccharides are depolymerization products of natural products:alginates, carragheenans, pectins and pectates, carboxymethylcelluloses, carboxymethylguars and carboxymethyl starches. The microcapsules may be isolated and dried.

Abstract: According to this invention, the combination of a solid particulate water insoluble drug with a solid fish gelatin coating is produced by coacervation of the fish gelatin. The fish gelatin being soluble at ambient temperatures provides a basis for relatively low temperature coacervation impossible with other gelatins. Coacervation is brought about by the addition of conventional coacervation agents and the coacervating suspension containing gelatin and the agents is rendered insoluble by the addition of a suitable fixative such as glutaraldehyde.

Abstract: A process for producing microcapsules which comprises forming a wall of coacervates on microdroplets of an oily substance of water-insoluble solid particles through reaction between gelatin and an anionic polymer, allowing a ylidoid compound to act on the coacervates so that cross-linking occurs between the polymer molecules of gelatin to harden the microcapsules.

Abstract: The invention involves a method for making uniformly sized particles from solid compounds. First, a suitable solid compound is dissolved in a suitable solvent. Then, a precipitating liquid is infused, precipitating non-aggregated particles with substantially uniform mean diameter. The particles are then separated from the solvent. Depending on the solid compound and the desired particle size, the parameters of temperature, ratio of non-solvent to solvent, infusion rate, stir rate, and volume can be varied according to the invention. The precipitating liquid may be aqueous or non-aqueous, depending upon the relative solubility of the compound and the desired suspending vehicle.

Abstract: The present invention relates to gelatin composite for the use of capsules to fill medicine and the like, coating agents or binding agents of tablets, casing materials and so on. A gelatin composite of the invention is characterized by comprising gelatin and polypeptide as an essential component, wherein the polypeptide is in the range of 15-70% by weight, referring to the total weight of the polypeptide and gelatin, and the gelatin has a gelly strength of 250 bloom or greater. The gelatin composite prevents insolubilization of the gelatin due to the passage of time without any degradation of shape-retaining ability of the gelatin composite.

Abstract: The invention relates to pharmaceutical formulations comprising discrete units of zidovudine provided with a controlled release coating in which the said units are preferably in the form of spheroids.

Abstract: A liquid coacervate composition and a method of introducing heme, hemoproteins and/or heme-hemoprotein complexes into the body. The liquid composition, comprising an oxygen-carrying molecule containing iron and a two-phase aqueous coacervate system, can be administered orally or intraveneously. The liquid composition is utilized to augment the oxygen transport capability of the body, to treat for several of the anemias and/or to act as an oxygen-carrying plasma volume extender.

Abstract: A spray dried ibuprofen composition suitable for direct compression into tablets comprising a spray dried dispersion in water of ibuprofen, pregalatinized starch, a disintegrant and a wetting agent for the ibuprofen.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A method of manufacture and the product made thereby are set forth; in the preferred and illustrated embodiment, a core including an insect poison is encapsulated by shell material melting and hardening for encapsulation. The core is primarily soybean extract mixed with DURSBAN.RTM. insecticide, an example of a toxicant. The surrounding shell or encapsulation is formed by melt extrusion of shell material. The surrounding shell encloses the core material to form an impervious shell. The surrounding shell includes soy protein as an insect attractant mixed in gelatin or poly(vinyl alcohol). A gelling agent such as carrageenan and the attractant were added to the shell. The beads formed by the melt extrusion encapsulation has sufficient shell strength to enable mechanical handling for dispensing, are resistant to water, do not bleed from the inside to the outside, and yet can be penetrated by the insect.

Abstract: A granular composition containing 2-(4-isobutylphenyl)propionic acid (ibuprofen) as an active anti-inflammatory pharmaceutical ingredient as a major component, together with carboxymethylcellulose, a lubricant and water as minor components, is disclosed. Particles of ibuprofen and carboxymethylcellulose are both fluidized and coated with an aqueous disperson of a starch binder. After being dried to a moisture level of about 1-5% and blended with a lubricant and additional carboxymethylcellulose, the resulting granules can be directly molded into a pharmaceutically acceptable tablet having high hardness, short disintegration time and fast dissolution rate.

Abstract: A gel formation for oral administration having improved palatability comprising an effective hypocholesterolaemic amount of a uniform gelled dispersion of(a) between about 8 and about 20 percent by weight of a particulate, pharmaceutically acceptable, sparingly crosslinked non-digestible quaternary ammonium substituted polysytrene anion exchange resin having an average particle size below about 100 microns;(b) between about 4 and about 16 percent by weight of a pharmaceutically acceptable gelatin;(c) between about 0.015 and about 10 percent by weight of a natural or synthetic pharmaceutically acceptable sweetener;(d) between about 0.05 and about 2 percent by weight of a pharmaceutically acceptable organic acidulent;(e) between about 0.05 and about 5 percent by weight of one or more pharmaceutically acceptable flavoring or coloring agents or mixtures thereof; and(f) the remainder water.

Abstract: The invention involves a method for making uniformly sized particles from water-insoluble drugs or other organic compounds. First, a suitable solid organic compound is dissolved in an organic solvent, and the solution can be diluted with a non-solvent. Then, an aqueous precipitating liquid is infused, precipitating non-aggregated particles with substantially uniform mean diameter. The particles are then separated from the organic solvent. Depending on the organic compound and the desired particle size, the parameters of temperature, ratio of non-solvent to organic solvent, infusion rate, stir rate, and volume can be varied according to the invention.

Abstract: A controlled release pharmaceutical preparation containing a micronized gastrointestinal irritant drug, such as potassium chloride, in a non-toxic protective balm. An irritant/balm admixture may be formed into microparticles. Alternatively, an irritant/balm admixture, may be used as the core for microcapsules. The microparticles or microcapsules may themselves be filled into a capsule or tabletted.

Abstract: Controlled release drug delivery systems comprised of spherical microporous polymeric network of interconnecting channels containing pore incorporated drugs or other agents wherein the drugs or agents are confined within the pore channel are described. Also disclosed are processing parameters in connection with the novel method of the invention for obtaining drug delivery systems especially suited for parenteral as well as oral administration.

Abstract: There is disclosed an improved complex coacervation process for microencapsulation of core ingredients that are partially soluble in the microcapsule walls wherein the core ingredient is first mixed with a coacervation adjacent prior to forming a first colloidal emulsion of core ingredient, and, after combining the first emulsion with a second colloidal solution and cooling to cause gelation, a water-soluble wax derivative is added. No pH adjustment or dilution is necessary, and very high yields of non-agglomerated microcapsules are obtained, both in terms of quantity of microcapsules and content of core ingredient. When deet is the core ingredient there is obtained a long-lasting mosquito repellent.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.