摘要:
The invention relates to conjugates of lipids and basic, membrane disturbing peptides, particularly compounds of the formula(R--CONH).sub.n --R.sup.3 (I)and(R--S--S).sub.n --R.sup.3 (II)wherein R is the hydrocarbyl moiety of a straight-chain or branched-chain, saturated or unsaturated aliphatic carboxylic acid, or a phospholipid moiety having a free valence bond; R.sup.3 is a basic membrane disturbing peptide having a free valence bond at one or two carbon atom(s); and n is 1 or 2. These conjugates can be used as a vector for transfecting a cell with a polynucleotide or any other anionic macromolecule.
摘要:
Compounds of the formula R.sup.1 --NH--A I wherein R.sup.1 is an acyl moiety of a C.sub.12-40 aliphatic carboxylic acid, A is the residue of a oligopeptide devoid of one amino group, and --NH--A contains at least one positively charged amino acid, or derivatives thereof can be used for transferring anionic macromolecules into cells.
摘要:
The invention relates to compositions in the form of microemulsion preconcentrates that contain (a) a mixture that consists of a medium-chain triglyceride and an omega-9 fatty acid and/or an omega-6 fatty acid; and (b) a surface-active component that contains a polyoxethylene tenside. When contacted with water or with an aqueous medium these microemulsion preconcentrates form microemulsions. The microemulsions of the O/W type have an average particle size below 150 nm, preferably below 100 nm. The inventive microemulsion preconcentrates and microemulsions are suitable for use as vehicles for substances, namely active agents, that are hardly soluble in water, but soluble in components (a) and/or (b). In the aqueous phase, said microemulsions may contain water-soluble substances.
摘要翻译:本发明涉及微乳液预浓缩物形式的组合物,其含有(a)由中链甘油三酯和ω-9脂肪酸和/或ω-6脂肪酸组成的混合物; 和(b)含有聚氧乙烯表面活性剂的表面活性成分。 当与水或水介质接触时,这些微乳液预浓缩物形成微乳液。 O / W型的微乳液的平均粒度小于150nm,优选低于100nm。 本发明的微乳液预浓缩物和微乳液适用于难溶于水但可溶于组分(a)和/或(b)的物质即活性剂的载体。 在水相中,所述微乳液可含有水溶性物质。
摘要:
A nanodispersion comprises (a) a membrane-forming molecule, (b) a coemulsifier and (c) a lipophilic component, in pharmaceutical end formulations, the nanodispersion being obtainable by (α) mixing the components (a), (b) and (c) until a homogeneous clear liquid is obtained, and (β) adding the liquid obtained in step (α) to the water phase of the pharmaceutical end formulations, where steps (α) and (β) may be carried out without high energy mixing or homogenization. The nanodispersions prepared according to this invention are suitable as transport vehicles for pharmaceutical active agents.
摘要:
The present invention relates to a novel pharmaceutical formulation for the topical application of drugs, particularly non-steroidal anti-inflammatory drugs (NSAID's), comprising a therapeutically effective amount of a drug, sodium phosphate buffer, and, optionally, an alcoholic solvent. It has been found that by the addition of sodium phosphate buffer to such formulations, the permeation of the NSAID can be significantly improved.
摘要:
A controlled release pharmaceutical composition comprising a physiologically active agent dispersed in preformed porous polymeric microparticles is provided. The active agent concentration may be up to about 10% by weight to achieve controlled release. Each of the porous microparticles has a plurality of preformed pores into which active agent is loaded and from which the active agent is subsequently released to the environment of use. The compositions are capable of delivering physiologically effective amounts of active agent for at least about thirty days, which delivery may be reversibly controlled by exposure to ultrasound.
摘要:
Topical preparations containing a salt of a cholanic acid, a lipid, and optionally, one or more other pharmaceutically or cosmetically active substances, are disclosed. These preparations are used in pharmaceutical and/or cosmetic applications.