摘要:
Solid, water-insoluble lipospheres formed of a solid hydrophobic core having a layer of a phospholipid embedded on the surface of the core, containing biologically active agent in the core, in the phospholipid, adhered to the phospholipid, or a combination thereof, are disclosed for use in providing extended release of active agent, including drugs such as vaccines and anesthetics, insect control agents such as insecticides and repellents, and agricultural compounds such as fertilizers, fungicides, pesticides, and herbicides. Lipospheres can be prepared by a melt technique or a solvent technique, summarized as: (1) forming a liquid solution or suspension of the agent by either melting the agent, or dissolving or dispersing the agent in a liquid vehicle, to form a mixture of liquid agent that solidifies at room temperature or greater; (2) adding phospholipid and an aqueous solution to the liquid agent to form a suspension; (3) mixing the suspension at a temperature above the melting temperature until a homogeneous fine dispersion is obtained; and then (4) rapidly cooling the dispersion to below the melting temperature of the liquid mixture containing the agent. Agent can also be added to the phospholipid or mixed with the resulting lipospheres. The agent containing lipospheres have several advantages over other delivery systems, including emulsions, vesicles and liposomes, including stability, low cost of reagents, ease of manufacture, high dispersibility in an aqueous medium, a release rate for the entrapped substance that is controlled by the phospholipid coating and the carrier. Examples demonstrate the effective administration of anesthetics, antigens, and insect repellent (DEET).
摘要:
The cDNA sequence encoding porcine brain natriuretic peptide and related genes encoding canine and human peptides with natriuretic activity are disclosed. The gene is shown to make accessible the DNAs encoding analogous natriuretic peptides in other vertebrate species. The genes encoding these NPs can be used to effect modifications of the sequence to produce alternate forms of the NPs and to provide practical amounts of these proteins. The NPs of the invention can also be synthesized chemically.
摘要:
Complete coding sequences and amino acid sequences for both canine and human 32K alveolar surfactant proteins (ASP); clones for the 10K protein have also been obtained. Methods and vectors for obtaining these proteins in recombinant form. The availability of large amounts of these proteins through recombinant techniques permits the use of ASP in suitable pharmaceutical compositions in the treatment of respiratory deficiency syndromes.
摘要:
The present invention provides tools which are useful for the diagnosis of an animal's exposure to feline infectious peritonitis virus (FIPV) or susceptibility to FIPV. The diagnostic tools are composed of nucleic acid sequences which encode structural and nonstructural FIPV proteins and antibodies generated against FIPV proteins. The FIPV proteins may also be useful as subunit vaccines.
摘要:
The complete coding sequence and amino acid sequences for both canine and human 10K alveolar surfactant proteins (ASP) are disclosed; clones encoding variants of the SP-18 and SP-5 forms of human protein are disclosed. Methods and vectors for obtaining these proteins in recombinantform are also described. An improved method for purification of the 32K protein takes advantage of its carbohydrate affinity.Pharmaceutical compositions in the treatment of respiratory deficiency syndromes use the 10K proteins with or without the 32K form.
摘要:
Novel benzoic acid derivatives have formula (I) wherein: -X- represents C1 to C6 alkylene, C2 to C6 alkenylene or a divalent moiety having the structure -(CH2)m-Z- in which m is an integer from 0 to 3 and Z represents -O-, -S- or -NH-; -Y- represents a direct bond, C1 to C6 alkylene, C2 to C6 alkenylene or a divalent moiety having the structure -(CH2)m-Z-(CH2)n in which m and n are each, independently, an integer from 0 to 3 and -Z- represents -O-, -S- or -NH-; R represents a 5- or 6-membered carbocyclic or heterocyclic ring or a carbocyclic or heterocyclic fused ring system containing up to 10 members in the ring, which carbocyclic, heterocyclic or fused ring system may be saturated or unsaturated and may contain up to two substituents selected from lower alkyl, methoxy, halo and trifluoromethyl; and R?1 and R2¿ are each, independently, selected from hydrogen, lower alkyl, methoxy, halo and trifluoromethyl. The benzoic acid derivates are useful as anti-inflammatory agents.
摘要:
Le remplacement du L-Pro à la position 7 par D-Phe ou D-Tic et le remplacement de L-Phe à la position 8 par des éthers d'hydroxyproline et des thioéthers de bradykinine et d'autres analogues substitués de bradykinine transforme les agonistes de la bradykinine en antagonistes de la bradykinine. L'invention porte également sur d'autres modifications, en d'autres positions des antagonistes de bradykinine modifiés en position 7 et 8, qui renforcent la résistance aux enzymes, la puissance antagoniste et/ou la spécificité des nouveaux antagonistes de bradykinine. Les analogues obtenus sont utiles pour le traitement des états pathologiques chez les mammifères et chez l'être humain souffrant d'un excès de bradykinine ou de kinines voisines induit, par exemple, par une piqûre d'insecte.