Abstract: New polysaccharide esters are disclosed, and more precisely esters of acidic polysaccharides chosen from the group formed by carboxymethylcellulose, carboxymethyl starch and carboxymethylchitin. These new esters and some esters of the type already known are useful as medicaments, for the manufacture of pharmaceutical and cosmetic preparations, in the field of biodegradable plastic materials and, therefore, for the manufacture of medical, surgical and sanitary articles, as well as numerous other industrial sectors in the place of acidic polysaccharides now in common use.

Abstract: A tamper-resistant, caplet like medicament that masks the taste of poor tasting drugs and possesses an improved lubricity for easier swallowing is produced by shrinking a gelatin-based capsule about a caplet-shaped tablet of the medicament at specific temperatures, pressure and relative humidity.

Abstract: The present invention provides an improved compositions and methods for regulating the immune response, for ameliorating effects of stress, and for avoiding untoward effects of chemotherapy or exposure to irradiation by administration of androstenediol (AED) and androstenetriol (AET). The improved means of regulating immune response can be utilized in treating infectious diseases and immune diseases such as diabetes and chronic fatigue syndrome, both diseases now considered to be immune response related syndromes.

Abstract: The present invention provides a resin molding composition for preventing gnawing damage by the animal, a microcapsule filled with a capsaicine compound, and a process for producing the capsaicine compound and the microcapsule.

Abstract: A method for encapsulating a biological substance is biocompatible microcapsules is disclosed, said method comprising:a) maintaining a coating-forming liquid film sheet comprising a solution of a soluble organic polymer in an organic solvent,b) causing droplets comprising biological substance is an aqueous medium to pass through said sheet to form microcapsules comprising cores of said droplets coated by said liquid film, andc) permitting said microcapsules to pass through said sheet so that a portion of said polymer precipitates in the presence of water in said droplets while evaporating a portion of said solvent to form a continuous permeable polymer coating of sufficient structural that said microcapsules are self-supporting.

Abstract: A hard capsule for pharmaceutical drugs comprises a water-soluble cellulose derivative as a capsule base, a gelatinizing agent and an auxiliary for gelation. The hard capsule is prepared by preparing an aqueous solution of a capsule base containing a water-soluble cellulose derivative, a gelatinizing agent and an auxiliary for gelation, immersing a capsule molding pin in the aqueous solution of the capsule base, subsequently drawing out the molding pin from the aqueous solution of the capsule base, subjecting the aqueous solution of the capsule base attached to the outer surface of the molding pin to gelate at room temperature, and forming a capsule film on the outer surface of the molding pin.

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: This invention provides a method and compositions for increasing the permeability of epithelial cells to a chloride ion in a subject comprising administering a permeability enhancing amount of a composition comprising a nontoxic, nonionic surfactant having (1) a critical micelle concentration of less than about 10 mM and a hydrophile-lipophile balance number of from about 10 to 20 and (2) a suitable hydrophobic organic group joined by a linkage to a suitable hydrophilic polyol.

Abstract: A pharmaceutical composition comprising a shaped enteric material having distributed therethrough preferably substantially uniformly, pharmaceutical loaded particles, said particles having a size no greater than about 10 microns in any dimension and being alkali insoluble and the method of delivering pharmaceuticals to Peyer's glands.

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: Pharmaceutical forms of pimobendan for oral administration comprising citric acid, whereby a constant, satisfactory resorption is ensured even when there are major pH fluctuations in the gastrointestinal tract.

Abstract: The present invention relates to a polymer composition comprised of gellan, carrageenan and mannan gums and a process for producing flexible films for encapsulation comprising the gellan, carrageenan and mannan gum composition. The mannan gums include the galactomannans and the glucomannans. Advantageously, soft capsules of the above composition are produced using the novel process. The composition comprises a blend of a gellan gum: (carrageenan/mannan gum) wherein the gellan gum concentration ranges from about 0.1 to 50 weight percent and the ratio of carrageenan/locust bean gum ranges from 3:1 to 1:3. Additional reagents are added to this gum blend to form a film-forming polymer composition useful in the production of gelatin-free capsules or microcapsules.

Abstract: Pharmaceutical compositions suitable for administration by inhalation and containing pentamidine, or pharmaceutically acceptable salt thereof, in powder form. Such compositions include pressurized aerosol compositions and nonpressurized power compositions. Also described is finely divided powdered pentamidine with a mass median diameter in the range 0.01 to 10 microns and a method for the prevention or treatment of pneumo-cystis carinii pneumonia which comprises administration by inhalation to a patient having or susceptible to that condition of a therapeutically effective quantity of pentamidine, or a pharmaceutically acceptable salt thereof, in powder form.

Abstract: Oral pharmaceutical compositions containing high content anthocyanosides, preferably higher than 80% w/w, suspended in fractionated coconut oil have higher bioavailability than water solutions or suspensions in other lipophilic carriers.

Abstract: When a powdered extract of Kampo medicine is encapsulated as such in hard capsules, the pharmaceutical effects of the Kampo medicine cannot be fully achieved, since the dissolution of the content of the hard capsules requires a long period of time. Therefore, the present invention aims at providing Kampo medicine hard capsules having good dissolution properties.The present invention provides a process for producing Kampo medicine hard capsules which comprises compacting Kampo medicine extract powder, mixing magnesium stearate with the compacted Kampo medicine extract powder and filing the mixture into gelatin hard capsules.It is preferable that the weight ratio of the magnesium stearate to the Kampo medicine powdered extract ranges from 0.5/100 to 3/100. Furthermore, it is preferable that said Kampo medicine is selected from Oren-gedoku-to, Sho-saiko-to, Ninjin-to, San'o-shashin-to, Mao-bushi-saishin-to, Anchu-san, Keishi-bukuryo-gan, Byakko-ka-ninjin-to, Shakuyaku-kanzo-to and Sairei-to.

Abstract: A polyprenyl compound having formula (1) is stabilized by a tocopherol, an organic acid, a neutral amino acid or a basic amino acid: ##STR1## in which n is an integer of 1 to 3.

Abstract: Sustained and enhanced antipyretic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage sustainedly enhancing, antipyretically effective amount of the free acid S(+) flurbiprofen enantiomer, said enantiomer being substantially free of its R(-) flurbiprofen antipode.

Abstract: The subject invention relates to compositions in dosage form comprising a solid dispersion which is a solidified melt mixture consisting essentially of the following components:(a) from about 15% to about 75% of tebufelone;(b) from about 25% to about 65% of a poloxamer surfactant having a melting point of about 40.degree. C. or greater, the poloxamer surfactant consisting essentially of a block copolymer having three polymer blocks, a middle block of poly(oxypropylene) with a molecular weight of from about 1450 daltons to about 6000 daltons, and end blocks of poly(oxyethylene), the end blocks being from about 50% to about 90% of the copolymer; and(c) from 0% to about 60% of other components, wherein the other components are miscible with a melt mixture of components (a) and (b).

Abstract: A cosmetic product is provided that stores a cosmetic composition in a capsule having a spheroidal body with hollow chamber forming a major portion of the capsule, a tab forming a minor portion of the capsule, and a neck section connecting the tab with the spheroidal body. At least two wings are positioned along opposite sides of the spheroidal body perpendicularly extending outward therefrom. Upon twisting, the neck can be broken to allow release of cosmetic composition from within the chamber.

Abstract: Sugar or sugar/starch beads coated with a first coating of a drug, for example 1,2-dihydro-6-(lower alkyl)-2-oxo-5-(4-pyridinyl)-nicotinonitrile (milrinone), hydroxypropyl methylcellulose or hydroxypropyl cellulose and a plasticizer selected from triacetin, diacetylated monoglycerides, glycerin, propylene glycol, polyethylene glycol, diethyl phthalate and triethyl citrate or a mixture of two or more thereof and a second coating of high-viscosity ethylcellulose, low-viscosity ethylcellulose, hydroxypropyl cellulose, polyvinyl acetate phthalate and a plasticizer selected from diacetylated monoglycerides and triacetin or a mixture thereof and optionally coated with additional first coating and capsules filled therewith and method of preparation thereof are disclosed.

Abstract: This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.

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: Pharmaceutical compositions suitable for administration by inhalation and containing pentamidine, or pharmaceutically acceptable salt thereof, in powder form. Such compositions include pressurized aerosol compositions and non-pressurized powder compositions. Also described is finely divided powdered pentamidine with a mass median diameter in the range 0.01 to 10 microns and a method for the prevention or treatment of pneumacystics carinii pneumonia which comprises administration by inhalation to a patient having or susceptible to that condition of a therapeutically effective quantity of pentamidine, or a pharmaceutically acceptable salt thereof, in powder form.

Abstract: A process for producing alginate capsules comprises slowly introducing an aqueous alginate solution into crosslinking solution of a polyvalent metal salt. The aqueous alginate solution has mannuronic units (M) and guluronic units (G) in a molar ratio between 0.4 and 1.9 and preferably an amount of (G) blocks greater than 50%. Preferably, the alginate is a sodium alginate having a viscosity, in a 0.5% solution in water at 25.degree. C., lower than 20 mPa.s measured with a TV Contraves viscosimeter having a No. 1 measurement body in the presence of a calcium chelate. The alginate concentration is between 0.2 and 2 weight percent. The polyvalent metal salt concentration in solution is from 3.4.times.10.sup.-3 to 6.8.times.10.sup.-2 M. The alginate capsules are employed in cosmetic compositions.

Abstract: The invention relates to cosmetic and pharmaceutical compositions containing the derivatives of benzylidenecamphor of formula: ##STR1## where R.sub.1 denotes H, OH, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.8 alkoxy, R.sub.3 denotes OH, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.8 alkoxy, or else when R.sub.1 denotes H or OH, R.sub.3 can represent C.sub.1 -C.sub.8 alkyl, R.sub.2 and R.sub.4 denote H or OH, at least one of the radicals R.sub.2 and R.sub.4 representing OH.The compounds (I) are wide-band sunscreens and antioxidants, and are utilized in the treatment of cutaneous inflammations and allergies.

Abstract: A pharmaceutical composition comprising a solution of a tenin inhibitor of the formula: ##STR1## wherein R.sub.1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-methyl-4-homopiperazinyl;R.sub.2 is benzyl, p-methoxybenzyl, 2-phenylethyl, 1-naphthylmethyl or 2-naphthylmethyl;R.sub.3 is 4-thiazolyl, 2-amino-4-thiazolyl, 2-thiazolyl, 5-thiazolyl, 1-pyrazolyl, 3-pyrazolyl, 1-imidazolyl, n-propyl, isopropyl, CH.sub.3 S-- or CH.sub.3 SCH.sub.2 --;R.sub.4 is loweralkyl or cyclopropyl;R.sub.5 is hydrogen or loweralkyl; andX is CH.sub.2 or NH; or a pharmaceutically acceptable salt, ester or prodrug thereof in a pharmaceutically acceptable solvent, said solution being encapsulated in a soft elastic gelatin capsule.

Abstract: A method for preventing the sickling of sickle cells in a patient having sickle cell disease, the method which comprises administering to the patient a therapeutically effective amount of a compound having the formula: ##STR1## wherein X.sup.- is selected from the group consisting of iodide, chloride, bromide, hydroxyl, nitrite, phosphate and acetate.

Abstract: A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000 centipoises in 2% solution at 20.degree. C. and excipients.

Abstract: 8,10-Dideazatetrahydrofolic acid derivatives of the formula: ##STR1## where R.sub.1 and R.sub.2 are selected from hydrogen and alkyl having from one to about eight carbon atoms and the carboxylates and acid addition salts thereof, showing strong inhibition of L1210 murine leukemia cells in culture, modest inhibition of glycinamide ribotide transformylase and aminoimidazole carboxamide ribotide transferase, and insignificant inhibition of dihydrofolate reductase and thymidylate synthase enzymes.

Abstract: A process for producing alginate capsules comprises slowly introducing an aqueous alginate solution into crosslinking solution of a polyvalent metal salt. The aqueous alginate solution has mannuronic units (M) and guluronic units (G) in a molar ratio between 0.4 and 1.9 and preferably an amount of (G) blocks greater than 50%. Preferably, the alginate is a sodium alginate having a viscosity, in a 0.5% solution in water at 25.degree. C. lower than 20 mPa.s measured with a TV Contraves viscosimeter having a No. 1 measurement body in the presence of a calcium chelate. The alginate concentration is between 0.2 and 2 weight percent. The polyvalent metal salt concentration in solution is from 3.4.times.10.sup.-3 to 6.8.times.10.sup.-2 M.The alginate capsules are employed in cosmetic compositions.

Abstract: An extended release pharmaceutical formulation adapted to approach zero order release of drug over a 12 to at least 24 hour period, comprised of a mixture of 0 to aobut 50% of an immediate release particle containing a drug, inert substrate and binder, coated with talc and up to 100% of an extended release particle comprising the immediate release particle coated with a dissolution modifying system containing plasticizers and a film forming agent.

Abstract: Pressing having sustained release of active compound for the oral or parenteral administration of medicaments, which contains at least one solid pharmaceutical active compound, polylactic acid and a homo- or copolymer of D(-)-3-hydroxybutyric acid and processes for its production.

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: New polysaccharide esters are disclosed, and more precisely esters of acidic polysaccharides chosen from the group formed by carboxymethylcellulose, carboxymethyl starch and carboxymethylchitin. These new esters and some esters of the type already known are useful as medicaments, for the manufacture of pharmaceutical and cosmetic preparations, in the field of biodegradable plastic materials and, therefore, for the manufacture of medical, surgical and sanitary articles, as well as numerous other industrial sectors in the place of acidic polysaccharides now in common use.

Abstract: A method for preventing the sickling of sickle cells in a patient having sickle cell disease, the method which comprises administering to the patient a therapeutically effective amount of a compound having the formula: ##STR1## wherein X.sup.- is selected from the group consisting of iodide, chloride, bromide, hydroxyl, nitrite, phosphate and acetate.

Abstract: A cosmetic product is disclosed in the form of a gelatin walled capsule encompassing a cosmetic composition that includes a carrier which is a silicone polymer and an antioxidant. The antioxidant operates to inhibit degradation of the gelatin wall to prevent malodors from being generated. Retinoic acid derivatives such as retinyl palmitate are especially effective as antioxidants.

Abstract: Capsules containing a hygroscopic or deliquescent component are stabilized by a) forming a mixture of the hydrogscopic or deliquescent compound with a sufficient quantity of water to achieve an equilibrium, b) adding a thickening agent and c) heating the solution or suspension; and introducing the heated composition so formed into the capsule. Preferably an equilibrium-protecting agent, such as glycerin, is also added.

Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted divinylazobenzene are useful as pharmaceutical compositions for the delivery of medicaments. The polymers are degraded by the enzymes of the upper gastrointestinal tract or are transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine. In particular, the polymers contain divinylazobenzene compounds of the formulae ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, (except that R.sub.1 and R.sub.2 are not both H), Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is alkyl of up to 18 carbon atoms and Ar is mono- or bicyclic aryl of up to 15 carbon atoms.

Abstract: This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.

Abstract: The use of frangible microcapsules in cleansing creams and cold creams and other cosmetic products improves their cleansing, cleaning, and removal properties without damage to the skin.

Abstract: The instant invention relates to guar flour formulations, to be ingested, wherein the formulations contain natural guar flour having a particle size diameter or 50 .mu.m to 1500 .mu.m and neither containing nor having been treated with any additive which substantially affects its form or consistency or which substantially delays or reduces the swelling ability of the flour.

Abstract: The present invention relates to a multiple-unit-dose comprising L-dopa as pharmaceutically active compound, whereby the composition provides a release of L-dopa in accordance with a test in accordance with U.S. Pharmacopeia Standards in an artificial gastric juice having a pH of at most 1.2 of at most 20% by weight during 1 hr, and in a phosphate buffer according to the same standard a release of at least 35% by weight during 1 hr, and at least 80% by weight during 3 hrs.

Abstract: Onset-hastened and enhanced antipyretic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage onset-hastening/enhancing antipyretically effective amount of the S(+) ibuprofen enantiomer, said enantiomer being substantially free of its R(-) ibuprofen antipode.

Abstract: Onset-hastened and enhanced antipyretic response is elicited in a human mammal in need of such treatment, i.e., a human mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage onset-hastening/enhancing antipyretically effective amount of the S(+) ketoprofen enantiomer, said enantiomer being substantially free of its R(-) ketoprofen antipode.

Abstract: A solid dosage form having a fill composition encased in a shell composition; the fill composition comprising(a) 5-60 mg of nifedipine;(b) a 5-7 membered cyclic pharmaceutically acceptable ingestible carbonate of the formula ##STR1## where A is an alpha,omega-C.sub.2 -C.sub.4 alkylene which is unsubstituted or substituted by at least one C.sub.1 -C.sub.4 alkyl; and(c) a pharmaceutically acceptable ingestible surfactant having a total of d ring members and being of the formula ##STR2## wherein B is a C.sub.1-4 -alpha,omega-alkylene;n is an integer from 0 up to d-1;m is an integer from 0 up to (d-n-1);each R is independently H or a C.sub.1-4 alkyl which is unsubstituted or substituted by at least one R';each R' is independently a hydroxy which is free, etherified by R.sup.2, or esterified by R.sup.3 ;each R.sup.2 is a C.sub.2-4 straight or branched oxyalkylene or a poly (C.sub.2-4 straight or branched oxyalkylene), the terminal oxygen of which is bound to hydrogen or R.sup.3 ; and each R.sup.

Abstract: A soft capsular preparation comprising a polyethylene glycol solution of sodium picosulfate. The soft capsular preparation is stable over a prolonged storage time and is convenient to carry around. In addition, an exact dosage of the medicine can be administered.

Abstract: The invention relates to a completely novel type of micro-capsules, viz. such capsules where an encapsulated hydrophobic or lipophilic substance is surrounded by polar solid crystals of polar lipids which expose their hydrophilic face outwards and their hydrophobic face turned inwards towards the hydrophobic or lipophilic substance. These micro-capsules can be utilized to encapsulate for instance tacky substances or substances to be protected against oxidation or influence from light. Moreover, an especially interesting use according to the invention is the use of said micro-capsules in an ointment base, where the active ingredient is well protected within said capsules up to the use but which at the application on the skin directly comes into contact with the skin surface as a consequence of the crystalline structure of the shell.

Abstract: Sustained and enhanced analgesic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering pain, by administering thereto a unit dosage sustainedly enhancing, analgesically effective amount of the free acid S(+) flurbiprofen enantiomer, said enantiomer being substantially free of its R(-) flurbiprofen antipode.

Abstract: A solution of etoposide in dimethylisosorbide is disclosed. The solution is useful for filling gelatin capsules and may also be formulated into parenteral dosage forms.

Abstract: An orally administrable and stable solution containing as an active ingredient Methoxasalen (8-methoxyfuro-[3',-2':6,7]-coumarin) of the formula ##STR1## useful in the photochemotherapy of psoriasis, to a process for the preparation thereof and to a process for the use thereof.