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: 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: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: A capsule and method for delivery for an active ingredient in the oral cavity that has a pH sensitive encapsulant shell and is associated with an adhesive. The pH sensitive shell dissolves at a pH in the oral cavity while the adhesive allows dissolution at the selected tissue.

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: A controlled-release organic nitrate formulation for once-per-day oral administration is provided by spheres having a core which includes an organic nitrate, and a membrane surrounding the core composed of a pharmaceutically acceptable, film forming polymer. The film forming polymer is effective to permit release of the organic nitrate from the spheres, over a daily dosing period, at a rate that achieves a therapeutically effective level of the organic nitrate, while effecting a drug holiday towards a latter portion of the daily dosing period so as not to induce tolerance.

Abstract: The invention related generally to the preparation of colloidal metal(O) particles having a crosslinked aminodextran coating with pendent amine groups attached thereto. The aminodextran acts as both a reductant for reducing metal ions to metal(O) particles and as the protective agent which coats the metal(O) particles thus formed. After stabilizing the aminodextran coating by use of a crosslinking agent, the coated particles can be used to covalently bind proteins. The resulting protein containing colloidal particles can be used as markers in optical and electron microscopy, in immunological and biological assays, and possibly as therapeutic agents.

Abstract: Orally administrable pharmaceutical preparation containing an active ingredient to be released in the lower part of the gastrointestinal tract, i.e. in the large intestine, and especially colon, consisting of a core containing a therapeutically active substance and coated with three protection layers at different solubility. The manufacturing and the use of these preparations are also described.

Abstract: There is disclosed a process for preparing compositions comprising microcapsules by phase separation microencapsulation wherein the hardening agent employed is a volatile silicone fluid and with the compositions prepared thereby. The use of the volatile silicone fluid as a hardening agent permits the production of microcapsules substantially free of any alkane hardening agent, eliminating potential combustability problems of the prior art processes and toxicity problems of the prior art compositions.

Abstract: A controlled-release organic nitrate formulation for once-per-day oral administration is provided by spheres having a core which includes an organic nitrate, and a membrane surrounding the core composed of a pharmaceutically acceptable, film forming polymer. The film forming polymer is effective to permit release of the organic nitrate from the spheres, over a daily dosing period, at a rate that achieves a therapeutically effective level of the organic nitrate, while effecting a drug holiday towards a latter portion of the daily dosing period so as not to induce tolerance.

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: This application describes the preparation and in vivo testing of surface coatings and matrix materials, which when applied to or caused to comprise the carriers for drugs and diagnostic agents, and administered in a fashion that allows efficient vascular access, causes the carriers to recognize determinants present or normal or focally diseased endothelium, and induces the following in vivo effects: 1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; 2) sequestration of the carrier and protecting entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; 3) acceleration of the carrier's transport across or through the vascular endothelium and/or subendothelial structures into the tissue compartment (interstitium); and 4) improvement of the efficiency with which the drug (or diagnostic) carrier migrates across the endothelium, or epi-endothelial or subendothe

Abstract: A pharmaceutical composition useful for treating hypercholesterolemia comprising a bile acid sequestrant resin such as cholestyramine and cholestipol maintained in a semipermeable water-insoluble material; wherein said semipermeable material enables bile acids from the digest tract to contact and bind to said resin while preventing substances having a higher molecular weight than bile acids from contacting said resin material. A method for treating hypercholesterolemia using the inventive composition is also disclosed.

Abstract: The present invention concerns novel immunogens. These immunogens comprise novel compounds which consist of an antigen or antigenic determinant couple dot an amphiphilic adjuvant molecule and optionally also free amphiphilic adjuvant molecules. An advantageous features of these novel immunogens is the presence of both an excellent immunogen activity as well as a pronounced adjuvant activity in a single complex.

Abstract: An ion exchange resin composition which is readily dispersible in water is provided. This resin composition comprises a granulated ion exchange resin, a pharmacologically active ingredient bound thereto with a sugar or sugar alcohol, and a sufficient amount of water, alcohol or aqueous alcohol to facilitate granulation. The invention further comprises a method for the preparation of such ion exchange resin composition.

Abstract: A method for treating azaribine-responsive diseases in patient's who exhibit severe pyridoxal phosphate depletion following the oral administration of azaribine comprises first encapsulating azaribine in a film-forming substance which is selectively soluble in the digestive juice of the intestines. The encapsulated azaribine is then orally administered to the patient in an amount effective for the treatment of the disease, preferably in an amount to provide from about 1.5 to about 15 grams of azaribine per square meter of patient body surface area per day.

Abstract: There is disclosed a process for preparing compositions comprising microcapsules by phase separation microencapsulation wherein the hardening agent employed is a volatile silicone fluid and with the compositions prepared thereby. The use of the volatile silicone fluid as a hardening agent permits the production of microcapsules substantially free of any alkane hardening agent, eliminating potential combustability problems of the prior art processes and toxicity problems of the prior art compositions.

Abstract: Drug delivery compositions yeild new and unexpected degrees of stabilization, solubilization and delivery of incorporated medicaments, drugs, or other physiologically-active compounds. The compositions enable administration of drugs and other medically useful compounds via a variety of routes. More particularly, a drug delivery system or composition including one or more monomeric or polymerized surface active agents allows for rapid dissolution and smooth liberation of any desired incorporated drug or combinations, and the method of preparing the drug composition. In one embodiment, the physiologically-active compound is encapsulated by a coacervate-derived film, and the finished product is suitable for transmucosal administration. Other formulations of this invention may be administered via inhalation, oral, parenteral and by transdermal and transmucosal routes.

Abstract: Healing of injured avascular tissue is promoted by applying angiogenic factor in proximity to the injured tissue.

Abstract: Healing of injured avascular tissue is promoted by applying angiogenic factor in proximity to the injured tissue.

Abstract: This application describes the preparation and in vivo testing of surface coatings and matrix materials, which when applied to or caused to comprise the carriers for drugs and diagnostic agents, and administered in a fashion that allows efficient vascular access, causes the carriers to recognize determinants present or normal or focally diseased endothelium, and induces the following in vivo effects: (1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; (2) sequestration of the carrier and protecting entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; (3) acceleration of the carrier's transport across or through the vascular endothelium and/or subendothelial structures into the tissue compartment (interstitium); and (4) improvement of the efficiency with which the drug (or diagnostic) carrier migrates across the endothelium, or epi-endothelial or subend

Abstract: A sustained absorption propranolol-containing pellet for oral administration comprises a core of propranolol or a pharmaceutically acceptable salt thereof and an organic acid embedded in a polymeric material in a multi-layer arrangement and an outer membrane which permits release of the propranolol at a controlled rate in an aqueous medium. The pellet has a dissolution rate in vitro in an aqueous medium, which when measured in a basket assembly according to U.S. Pharmacopoeia XX at 37.degree. C. and 75 r.p.m., is not more than 15% of the total propranol after 2 hours of measurement in a buffer solution at pH 7.5. Not more than 30% of the total propranolol is released after a total of 4 hours of measurement and not more than 63% of the total propranolol is released after a total of 6 hours.

Abstract: Compositions for the controlled and prolonged release of macromolecular compounds comprise a porous matrix of chitosan having dispersed therein the macromolecular compound. Examples of macromolecules used in the composition are pharmacologically active ones such as peptide hormones, e.g. growth hormone.

Abstract: An antigen delivery system utilizing a biodegradable polymer with good mechanical properties in combination with a material stimulating the immune system. The material having adjuvant activity may be polymer degradation products or an adjuvant which is contained within or bound to the polymer. In one embodiment, the polymer is formed from tyrosine dipeptides. Poly(CTTH-iminocarbonate) is a preferred tyrosine dipeptide polymer for constructing implantable delivery systems for antigenic material. The polymer is not an adjuvant in itself but degrades into products which stimulate the immune system. The tyrosine dipeptide can also be used as a conventional adjuvant.

Abstract: A composition adapted to administer a pharmocologically effective amount of a pharmaceutical agent when ingested orally comprising (a) a pharmaceutical agent; (b) a lipid coating materials; and (c) an enteric coating materials optionally comprising water soluble coating materials; emulsifying and solubilizing agents; binding agents; stabilizing and enzyme inhibiting agents surfactants and antimicrobial agents. The composition can also include a low density lipoprotein composition and lipolytic enzymes.

Abstract: Pharmaceutical compositions containing an iron complex of 3-hydroxy-4-pyrone or of a 3-hydroxy-4-pyrone in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by an aliphatic hydrocarbon group of 1 to 6 carbon atoms, are of value for the treatment of iron deficiency anaemia.

Abstract: A medication and method for treating heartworms in dogs, which medication includes a time release capsule or tablet dosage structure which is characterized either by discrete elements (capsule) or an outer layer or layers (tablet) of vasoconstricting and bronchial dilating medications and an inner, time-released layer or pellets of diethylcarbamazine. The vasoconstrictors and bronchial dilators are designed to counteract life-threatening vasodilation and bronchial constriction resulting from the release of acetylcholine by the dog when the heartworms are attacked by the diethylcarbamazine. The solid dosage structure can be constructed by layering such vasoconstrictors and bronchial dilators as prednisone, ephedrine, digoxin and dextroamphetamine sulfate in separate layers or combining these ingredients in a single layer separated from the diethylcarbamazine by a time-release substance such as gelatin.

Abstract: A controlled-release pharmaceutical unit dosage form is provided comprising a gelatin capsule enclosing a solid matrix formed by the cation-assisted gellation of a liquid fill incorporating vegatable gum and a pharmaceutically-active compound, as well as methods for the preparation thereof.

Abstract: The present invention provides for an oral drug delivery system based on a two phase liquid coacervate system prepared from water and one or more surfactants selected from anionic, cationic, amphoteric, and non-toxic surfactants, polysaccharides, synthetic polymers and polysorbates and their derivatives, and in which a pharmaceutical component is incorporated. The delivery system may be prepared in the form of a microemulsion as well as other forms including encapuslated microparticles. The claimed oral composition is useful to delivery oral dosage forms of drugs, their salts and derivatives thereof; biologicals, enzymes, and other pharmocologically active compositions. A method to prepare the oral drug delivery system is also disclosed.

Abstract: Capsules are formed herein a liquified core while avoiding capsule core gelation by adding drops of a solution of either an anionic polymer composition or a cationic polymer composition to a solution of an ionic polymer of opposite charge. The drops contain an active ingredient such as a cell or microorganism capable of producing a biologically active product or can contain a biological or chemical composition. The interface of the ionic polymers form a permeable membrane surrounding the liquid drops.

Abstract: Capsules are formed herein a liquified core while avoiding capsule core gelation by adding drops of a solution of either an anionic polymer composition or a cationic polymer composition to a solution of an ionic polymer of opposite charge. The drops contain an active ingredient such as a cell or microorganism capable of producing a biologically active product or can contain a biological or chemical composition. The interface of the ionic polymers form a permeable membrane surrounding the liquid drops.

Abstract: This disclosure recognizes the fact that the technology of making vesicles from lecithin and lecithin-like molecules, although well known and highly developed, is associated with problems of instability. It is known that vesicles coalesce, rupture and spill their contents long before the vesicle is used for its intended purpose.It has been discovered and disclosed herein that the deterioration of the vesicle delivery system is due in part to the rupture of the bipolar lipid vesicle membrane by the contents of the core volume or by an external agent. For example, the more detergent-like the properties of the pharmacological agent within the vesicle core volume, the more pronounced will be the attack on the vesicle wall interior. These events in turn will lead to vesicle membrane rupture.

Abstract: A new sustained-release, microencapsulated pharmaceutical composition is disclosed, suitable for oral administration which contains an effective amount of an orally-administered pharmaceutical in granular form wherein the granules are coated by a layer of homogeneous, native collagen to encapsulate the granules. Also disclosed is a method for administering the sustained-release compositions and a process for covering the granulated pharmaceutical with the layer of homogeneous, native collagen.

Abstract: A controlled-release pharmaceutical unit dosage form is provided comprising a gelatin capsule enclosing a solid matrix formed by the cation-assisted gellation of a liquid fill incorporating a vegetable gum and a pharmaceutically-active compound, as well as methods for the preparation thereof.

Abstract: The present invention relates to a multiple soft capsule in which a soft capsule is contained in another soft capsule and the production thereof. The multiple soft capsule is useful for various industrial fields such as medicine, foods, table luxuries and the like. Especially, the multiple capsule is useful in medical field, for instance, in combining two or more components which cannot be enclosed together in a single capsule or in the dissolution control in vivo of the medicines by properly selecting the kind of the film-forming substance for the outer and inner soft capsules.