Abstract: Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety.

Abstract: The invention relates to ultrasonic contrast agents consisting of microparticles which consist of amyloses and synthetic biodegradable polymers and a gas and/or a fluid with a boiling point below 60° C., process for the preparation thereof and their use as diagnostic and therapeutic agents.

Abstract: A magnetically controllable, or guided, carrier composition and methods of use and production are disclosed, the composition for carrying biologically active substances to a treatment zone in a body under control of a magnetic field. The composition comprises composite, volume-compounded paclitaxel-adsorbed particles of 0.2 to 5.0 &mgr;m in size, and preferably between 0.5 and 5.0 &mgr;m, containing 1.0 to 95.0% by mass of carbon, and preferably from about 20% to about 60%. The particles are produced by mechanical milling of a mixture of iron and carbon powders. The obtained particles are placed in a solution of a biologically active substance to adsorb the substance onto the particles. The composition is generally administered in suspension. Magnetic carrier particles having therapeutic quantities of adsorbed paclitaxel, doxorubicin, Tc99, and antisense-C Myc oligonucleotide, an hematoporphyrin derivative, 6-mercaptopurine, Amphotericin B, and Camptothecin have been produced using this invention.

Abstract: A biological material is prepared for use in ophthalmology by steps of providing animal pericardium, subjecting the animal pericardium to multiple steps of freezing and thawing in a salt solution and incubating the animal pericardium in a solution of ammonia and ethyl alcohol. The multiple steps of freezing and thawing are conducted in a mixture of about 0.9% sodium chloride solution and distilled water in about 1:1 proportions of sodium chloride solution to distilled water. The incubating step is conducted in a mixture of 1% ammonia solution and 1% ethyl alcohol solution in about 1:1 proportions of ammonia solution to ethyl alcohol solution over a period of 48 to 72 hours.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: The invention relates to a multiparticulate pharmaceutical form with delayed and pulsed release, enabling to obtain the onset of the availability of the active ingredient within 4 to 8 hours after the ingestion of the pharmaceutical form, and then a progressive release of the totality of the active ingredient within the 8 to 20 following hours, characterized by the fact that it is free of organic acid and that it is in the form of medicinal spheroids consisting of a neutral spherical core comprising a first coating based on a mixture of at least one hydrosoluble polymer and of at least one non hydrosoluble polymer throughout which are uniformly distributed the constitutive particles of an active ingredient, the whole comprising a second coating based on at least two pH independent polymers presenting rates of permeability different from one another with respect to the gastric and intestinal mediums, optionally at least one pH dependent polymer, at least one plasticizer and at least one inert carrier uniformly

Abstract: The invention is concerned with a flowable dry particle consisting of at least one oleophilic substance as the active ingredient present in a matrix of at least one carrier material and a coating. The coating consists of calcium silicate or of a mixture of calcium silicate with one or more mixture components, with the mixture components being microcrystalline cellulose, magnesium silicate, magnesium oxide, stearic acid, calcium stearate, magnesium stearate, silicon dioxide, kaolin and/or hydrogenated vegetable oil.

Abstract: Disclosed is a method of dry blend compression of potent drugs with low solubility, such as steroidal medicaments using directly compressible agglomerated excipients that are not a conventional or spray dried polyalcohol or lactose. The agglomerated excipients include mannitol, maltodextrin or corn syrup solids, which hold the medicament(s) in the crevices of the agglomerates. Also disclosed are the critical ratios of the agglomerated excipients to steroidal agent, specifically estradiol, that is distributed uniformly throughout the dry blend and then compressed into tablets.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: This disclosure is directed to preparation of individual taste-masked, high bioavailability, high payload, microcapsules by microencapsulation of water-insoluble NSAID drug materials in the substantial absence of microcapsule agglomerates. These taste-masked microcapsules contain a high payload, e.g., about 83+wt. % of said NSAID drug material having high bioavailability and can then be formulated into chewable tablets and liquid aqueous suspensions for medicinal use. Both cellulose acetate phthalate and gelatin are the microencapsulating polymer wall material.

Abstract: The invention relates to a lyophilized emulsion composition which contains an active substance and which can be redispersed with water to give the original emulsion, and to a process for the preparation thereof.The redispersed emulsion is suitable for parenteral use.

Abstract: An NSAID in the form of a compound with an essential fatty acid or essential fatty acid alcohol, particularly an NSAID as listed in categories 1 to 9 herein. Further, a method of preparation of a medicament for the treatment including prophylatic treatment of rheumatoid arthritis, osteoarthritis and related disorders; dysmenorrhoea; dementias, including Alzheimer's disease; or any other inflammatory or other conditions specified herein, wherein the said NSAID is used.

Abstract: Paperboard packaging material is disclosed for use in the manufacture of cartons for products which give off significant odors or aromas. The packaging material is treated to absorb odors generated by the products packaged in the packaging material. For this purpose, the paperboard packaging material is coated on one surface with an odor sorbing coating composition comprising activated carbon dispersed in an aqueous binder system. The odor sorbing coating covers substantially all interior surfaces of cartons formed from the packaging material to provide an effective concentration of activated carbon sufficient to render the contents substantially odor-free.

Abstract: The present invention contemplates nasal compositions effective for relieving mammalian sinus headache associated with inflamed or congested turbinates, or both, accompanied by localized pain perceived on the septum, containing an anaesthetically effective amount of a non-addictive, rapidly absorbable anaesthetic component such anaesthetic being the sole active ingredient in the composition or being combined with a decongestant of the sympathomimetic amine class.

Abstract: A particulate composition comprises particles having a substantially anhydrous core comprising an active ingredient. Generally the core comprises a matrix polymer with the active ingredient distributed throughout this. Generally there is an outer protection shell of polymer, generally formed by coacervation. The invention is a value for the production of powders, dispersions in non-aqueous liquids (for instance when the active ingredient is a detergent enzyme) and dispersions in water (for instance when the active ingredient is an agrochemical.

Abstract: A highly absorbable pharmaceutical composition containing, as the active ingredient, methyl 3-phenyl-2(E)-propenyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylate in an amorphous state and a pH-dependent type copolymer of methacrylic acid or its derivatives which composition has been prepared by dissolving the two components together in an organic solvent and thereafter removing the solvent.

Abstract: A pharmaceutical dosage form is prepared from a multiplicity of coated potassium chloride crystals coated with two distinct layers, the first of ethylcellulose and the second of a hydrophilic coating polymer, preferably hydroxypropylcellulose, resulting in microcapsules. These microcapsules are capable of being compressed into tablets of suitable hardness and friability with minimum quantities of excipients. The resultant controlled release tablets are useful for treatment of potassium deficiencies in humans.

Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine (or analogs) microparticles. In the preferred embodiment the microparticle is stable at low pH and disintegrates at physiological pH, and is particularly useful for oral drug delivery. In the most preferred embodiment the microparticles are formed in the presence of the drug to be delivered, for example, insulin or heparin. The diketopiperazine synthetic intermediates are preferably formed by cyclodimerization to form diketopiperazine derivatives at elevated conditions under dehydrating conditions, then precipitated with drug to be incorporated into microparticles.

Abstract: A finely divided solid pharmaceutical dosage form for oral administration dissolved or suspended in a pharmaceutically acceptable liquid is described which pharmaceutical dosage form consists of a pharmaceutical coating on a sugar core.

Abstract: Disclosed are sustained release dosage forms of liothyronine, in combination with normal or sustained release of thyroxine in a molar ratio of about 1 to 50:1, especially 5 to 20:1, useful in thyroid hormone replacement therapy. Surprisingly, it is found that by incorporating liothyronine and optionally thyroxine into a prolonged action dosage form in the described ratios, that the side effects associated with thyroid hormone replacement therapy are greatly reduced or eliminated. The preparation can be a dosage form containing salts of both thyroxine and liothyronine which release in a sustained manner. The preparations will typically contain 5 to 25 .mu.g of liothryronine. Also disclosed are processes of manufacturing the pharmaceutical preparations. The compositions are useful in treating disease states such as hypothyroidism, hyperthyroidism (in combination with thyrostatic drugs), so-called "TSH" suppressive therapy, and depression.