Abstract: The present invention relates to the use of certain vitamin D analogues in the preparation of a pharmaceutical preparation for the treatment of acne. The preparation contains a vitamin D analogue (calcipotriol) which has only moderate activity on the calcium metabolism when compared to 1,25-(OH).sub.2 D.sub.3, but has retained the ability to activate receptors for 1,25-(OH).sub.2 D.sub.3 not associated with calcium absorption or bone calcium mobilization.
Abstract: A series of cytotropic heterogeneous molecular lipids (CHML) and the method of preparation thereof are disclosed in the invention. CHML provided by this invention is in molecular type, it is an activated molecular carrier of functions with orientionally penetrating into membranes or walls of the cells. It possesses the active site for binding anti-carcinogenic drugs which is water soluble, lipid soluble or gas soluble and possesses the activated portion for binding structure of membrane of cancer cells also.CHML can synergetically injure the carcinoma cells and varius verus, at the same time it can enhance the immunity of the body. These are ascertained by the animal tests and in vitro tests.CHML in this invention can kill the sarcoma cell S-180 within 50 min. and the cells of human squamous cell carcinoma of esophagus within 40 min.The rate of DNA and RNA depolymerizations in cancer cells and mortality of cancer cells are attained to 100%. These are evidenced in the vitro test also.
Abstract: Compositions suitable for use in the preparation of dosage-form active vitamins D.sub.3 are disclosed. Each composition comprises an active vitamin D.sub.3 and a stabilizer selected from polyvinylacetal diethylaminoacetate and hydroxypropylcellulose. Also disclosed are processes for the preparation of stable dosage-form active vitamins D.sub.3. Each process comprises adding the above stabilizer to an active vitamin D.sub.3 and then adding a pharmaceutically-acceptable carrier to the resultant mixture.
Abstract: The compounds 1.alpha.,25(S), 26-trihydroxy-.DELTA..sup.22 -cholecalciferol; 1.alpha.,25(R), 26-trihydroxy-.DELTA..sup.22 -cholecalciferol; 1.alpha.,25(S),26-trihydroxyergocalciferol, 1.alpha.,25(R),26-trihydroxyergocalciferol and pharmaceutical compositions comprising the compounds as well as methods of making and using these compounds are disclosed.
Type:
Grant
Filed:
March 19, 1990
Date of Patent:
June 9, 1992
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico G. Baggiolini, Andrew D. Batcho, Gary A. Truitt, Milan R. Uskokovic, Peter M. Wovkulich
Abstract: A novel and effective treatment of psoriatic arthritis is provided using biologically active forms of vitamin D analogues and metabolites, and preferrably 1,25-dihydroxy vitamin D.sub.3. The administration of vitamin D analogues and metabolites may be made orally, topically, or parenterally. Substitive improvements in both the arthritic condition and skin lesions result after approximately two month's treatment when effective dosages are provided and maintained.
Abstract: A method of treating psoriasis in a patient which comprises administering to said patient an effective amount of a vitamin D compound which is capable of stimulating the differentiation of cultured tumor cells or normal rodent or human fibroblasts or keratinocytes in vitro.
Abstract: A method for parenteral administration of fat-soluble pharmaceuticals and vitamins using microemulsions is disclosed. The microemulsions are comprised of a naturally occurring amphipatic substance and a hydrophobic lipid along with the active ingredient, are size selected for 300-1000 .ANG. pseudomicelles, and permit safe intravenous injection of the active ingredient. Levels of the active ingredient in the various lipoprotein fractions of serum appear to mimic the natural distribution of the administered drug if taken orally.
Abstract: A method and composition for an improved treatment of human renal osteodystrophy, comprising the administration of 6-40 mcg/d (micrograms per day) of 24,25(OH).sub.2 D.sub.3 in combination with amounts of 1-alpha(OH)D.sub. 3 or 1,25(OH).sub.2 D.sub.3 or DHT.sub.2, which will maintain in the serum of patients the calcium concentration at 10-11 mg/dl (milligrams per deciliter) and the phosphate concentration at 5.5-6.0 mg/dl (milligrams per deciliter) and the numerical multiplication product of calcium x phosphate not more than 60-65.
Type:
Grant
Filed:
July 22, 1987
Date of Patent:
March 5, 1991
Assignee:
Teva Pharmaceutical Industries Ltd.
Inventors:
Mordecai Popovtzer, Ben Z. Weiner, Shmuel Edelstein, Zeev Mazor, David Ladkani, Benjamin Shalita, John A. Kanis
Abstract: Novel combination preparations containing 1.alpha.,25-dihydroxy vitamin D.sub.3 or 1.alpha.-hydroxy vitamin D.sub.3 and 1.alpha.,24,25(or 1.alpha.,25,26)-trihydroxy vitamin D.sub.3 are described. These preparations are useful in the treatment of various disorders which are characterized by disturbances of the calcium and phosphate metabolism such as osteoporosis and can also be used in animal nutrition.
Type:
Grant
Filed:
July 21, 1989
Date of Patent:
May 29, 1990
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Meier, Walter A. Rambeck, Harald Weiser, Hermann Zucker
Abstract: A unique, chemically-defined nutrient composition is disclosed which can enable stressed, catabolic, marathon athletes to achieve superior performance. The diet provides substantially all of the essential nutrients along with flavoring aids in simple, readily available form and comprises free amino acids, vitamins, minerals and trace elements, electrolytes, simple and complex carbohydrates, and flavoring aids. This diet benefits athletes because it provides for substantially all of the nutritional requirements, allows for reproducibility and user familiarity through precise chemical definition, supplies optimal nutritional requirements during training and competition through unique tailoring to the nutritional requirements of an individual athlete, requires minimal digestive energy, and encourages maximal absorption of nutrients. A specific mixture of amino acids, carbohydrates, and flavoring aids is used to achieve superior taste.
Abstract: The present invention relates to new carbazates of the general formula (I), ##STR1## wherein A is C.sub.3-10 alkyl, C.sub.3-10 alkenyl, C.sub.2-10 haloalkyl, trifluoromethyl, phenyl-C.sub.1-3 alkyl, phenyl-C.sub.2-3 -alkenyl, naphthyl-C.sub.1-3 alkyl; phenyl optionally substituted by one or more identical or different substituent(s) selected from C.sub.1-4 alkyl, halogen, C.sub.1-4 alkoxy and hydroxy; C.sub.3-7 cycloalkyl-C.sub.1-3 alkyl; optionally nitro-substituted furyl; diphenyl-hydroxy-methyl or indazolyl optionally substituted by one or more C.sub.1-4 alkoxy group(s) andR represents C.sub.1-4 alkyl,with the proviso that if R stands for ethyl, A is other than tertiary butyl, and acid addition salts thereof, a process for the preparation thereof and feed-additives comprising the same.The compounds of the general formula (I) may be used in animal husbandry due to their weight-gain increasing and fodder utilization improving effect.
Type:
Grant
Filed:
December 11, 1985
Date of Patent:
April 25, 1989
Assignee:
Egis Gyogyszergyar
Inventors:
Ildiko Ratz nee Simonek, Pal Benko, Edit Bernenyi nee Poldermann, Karoly Magyar
Abstract: Disclosed are aqueous multivitamin/trace elements formulations stabilized by a water soluble, organic acid that contains carbon-to-carbon unsaturation and water soluble salts thereof selected from the group consisting of maleic acid, fumaric acid, maleamic acid and acrylic acid.
Type:
Grant
Filed:
February 8, 1988
Date of Patent:
February 14, 1989
Assignee:
Rorer Pharmaceutical Corporation
Inventors:
Morris Kesselman, Abdur R. Purkaystha, James Cahill
Abstract: Disclosed are aqueous multivitamin/trace elements formulations stabilized by a water soluble, organic acid that contains carbon-to-carbon unsaturation and water soluble salts thereof selected from the group consisting of maleic acid, fumaric acid, maleamic acid and acrylic acid.
Type:
Grant
Filed:
May 27, 1986
Date of Patent:
April 26, 1988
Assignee:
USV Pharmaceutical Corporation
Inventors:
Morris Kesselman, Abdur R. Purkaystha, James Cahill
Abstract: Flavored, effervescent, water soluble compositions containing water-soluble and oil-soluble vitamins and amino acid chelated minerals in bioavailable form are contained in a composition consisting of 20-30% of a vitamin blend consisting of water-soluble and oil-soluble vitamins adsorbed on a lactose carrier containing a minor amount of propylene glycol, 5-25% of one or more amino acid chelated minerals selected from the group consisting of calcium, magnesium, iron, zinc, copper and manganese, 20-45% citric acid, 5-25% of one or more alkali or alkaline earth metal bicarbonates or carbonates, 1-5% flavoring agent, 0.5-2% of a sweetening agent and sufficient additional lactose carrier to provide the desired vitamin and mineral content per unit dosage which will normally vary between about 2 and 6 grams. When dissolved in water a flavored, lightly carbonated drink is provided which will contain in soluble bioavailable form between about 50 to 100% of the U.S.
Abstract: A method for treating or preventing metabolic bone disease characterized by loss of bone mass in mammals by administering 24-epi-1.alpha.,25-dihydroxy vitamin D.sub.2 alone or in combinations thereof with bone mobilization-inducing vitamin D derivatives to said mammals.
Abstract: Micellized aqueous formulations for fat soluble vitamins, essential nutrients, herb oils and pharmaceutical agents are obtained by a process wherein the fat soluble vitamin, essential nutrient or agent is first admixed with a suitable amount of polyethoxylated castor oil and a pharmaceutically acceptable polyol, such as glycerol to provide a non-aqueous phase. Thereafter, an aqueous phase containing mostly water and optionally a preservative, such as sodium benzoate, is slowly added to the agitated non-aqueous phase in such a manner that the temperature of the non-aqueous phase, including the aqueous phase added thereto, is maintained at an elevated temperature, preferably between approximately 60.degree. to 100.degree. C. After cooling, the final admixture is clear, homogeneous, having micelles of approximately 2 microns or smaller size.