TH53243A - The use of nanoscale dispersants in final-stage pharmaceutical formulations. - Google Patents

Abstract

DC60 (24/06/42) Detailed description: This invention describes the use of a nano-dispersion consisting of (a) membrane-forming molecules, (b) co-emulsifier, and (c) lipid-loving components in a pharmaceutical final formulation. The nano-dispersion is obtained by (alpha) mixing components (a), (b), and (c) until a homogeneous, transparent liquid is obtained, and (beta) adding the liquid obtained in step (alpha) to the aqueous phase of the pharmaceutical final formulation. Steps (alpha) and (beta) are performed without any additional energy input. The nano-dispersion used as described in this invention is suitable for use as a carrier for pharmaceutical active ingredients. Detailed description: This invention describes the use of a nano-dispersion consisting of (a) membrane-forming molecules, (b) co-emulsifier, and (c) lipid-loving components in a pharmaceutical final formulation. In pharmaceutical formulations, the nano-disperse is obtained by (alpha) mixing components (a), (b), and (c) until a homogeneous, transparent liquid is obtained, and (beta) adding the liquid obtained in step (alpha) to the aqueous phase of the final pharmaceutical formulation. Steps (alpha) and (beta) are performed without any additional energy input. The nano-disperse used as described in this invention is suitable for use as a transport medium for pharmaceutical active ingredients.

Claims (28)

1. In pharmaceutical final formulations, the nano-dispersion, consisting of (a) membrane-forming molecules, (b) co-emulsifiers, and (c) lipid-loving components, is obtained by (alpha) mixing components (a), (b), and (c) until a homogeneous, clear liquid (called the nano-dispersion prephase) is obtained, and (beta) adding the liquid obtained in step (alpha) to the aqueous phase of the pharmaceutical final formulation. Steps (alpha) and (beta) are performed without any additional energy input. 2. The use as defined in Claim 1, which is characterized by the alpha step being performed in an anhydrous medium. 3. Use as defined in Claim 1 or Claim 2, which is characterized by the beta procedure being performed without homogenization. 4. Uses as defined in any of the claims in claims 1 through 3, which are characterized by particles in the nanoscale dispersion having an average diameter of less than 50 nanometers. 5. Uses as defined in any one of the claims of Claims 1 through 4, which are characterized by the nanoscale dispersion of (a) a substance suitable for double membrane formation as a membrane-forming molecule, (b) a substance proposed to be of the O/W type as a co-emulsifier, and (c) a lipid-loving active substance as a lipid-loving component. 6. Use as defined in any of the claims of Claims 1 through 5, which is characterized by a nanoscale dispersion of phospholipids, hydrolyzed or partially hydrolyzed phospholipids, lysophospholipids, ceramides or mixtures of these as components (a) 7. Use as defined in claim 6, which is characterized by the presence of component (a) in the nano-dispersion at concentrations of 0.1 to 30 percent by weight relative to the total weight of components (a), (b), and (c). 8. Use as defined in any one of the claims in claims 1 through 7, which is characterized by a nanoscale dispersion consisting of saturated and unsaturated polyoxyethylene C3-C18 alkyl sulfate emulsifiers, alkali metal salts, and ammonium salts. or amine salts of fatty acids C8-C20, C8-C20 alkane sulfonates, fatty alcohol phosphorates, salts of colic acid, invert (quaternary) soaps, partial fatty acid esters of sorbitan, sugar esters, of fatty acids, partial glycerides of fatty acids, alkylmaltosides, alkylglucosides, C8-C18 betaine or C8-C24 alkylamino-C1-C4-alkylene betaine, proteins, polyglycerol esters of fatty acids, propylene glycol esters of fatty acids, and fatty acid lactates or mixtures of these as components (b) 9. The use as defined in claim 8, which is characterized by a nanoscale dispersion containing at least one polyoxyethylene emulsifier as a component (b). 10. The uses as defined in claim 9, which is characterized by the presence of nanoscale dispersions consisting of ethoxylated sorbitan fatty acid esters, ethoxylated fatty alcohols, ethoxylated fatty acids, ethoxylated vitamin E derivatives, ethoxylated lanolin and its derivatives, ethoxylated fatty acid partial glycerides, ethoxylated alkylphenols, sulfuric acid semiesters, and fatty alcohols. Ethoxy decomposed compounds and their salts, ethoxy decomposed fattyamines and fattyamides, ethoxy decomposed carbohydrates, block polymers of ethylene oxide and propylene oxide as components (b) 11. Use as defined in any of the claims of claims 1 through 10, which is characterized by the presence of component (b) in a nanoscale dispersion as defined in this invention at a concentration of 1 to 50 percent by weight relative to the total weight of components (a), (b), and (c). 12. Use as defined in any of the claims of Claims 1 through 11, which is characterized by a nanoscale dispersion of diglycerides or triglycerides of natural, synthetic or semi-synthetic type, mineral oil, silicone oil, wax, fatty alcohol, gerbate alcohol or esters of this substance, pharmaceutical active substance of an oil-loving functional group or a mixture of these substances as an ingredient (c) 13. Use as defined in any of the claims of claims 1 through 12, which is characterized by the presence of element (c) in the nanoscale dispersion defined in this invention at concentrations of 0.1 to 80 percent by weight relative to the total weight of elements (a), (b), and (c). 14. Use as defined in any one of the claims of claims 1 through 13, which is characterized by a nanoscale dispersion containing C2-C3 alcohol as a component (d). 15. Use as defined in any one of the claims in Claims 1 through 14, which is characterized by the final formulation of the pharmaceutical compound as a finished drug in liquid, semi-solid, or solid form. 16. A final pharmaceutical formulation in liquid form, such as an injectable suspension, intravenous solution, drip, aerosol, emulsion, liquid, suspension, oral solution, gargle, or inhalant, containing nano-dispersive substances as defined in Claim 1. 17. A final pharmaceutical formulation that is semi-solid in the form of an ointment, cream (o/w emulsion), fatty cream (o/w emulsion), gel, liquid, foam, paste, suspension, ointment, or plaster, containing nano-dispersive substances as defined in Claim 1. 18. Final pharmaceutical formulations in solid form, such as tablets, coated tablets, ampoules, granules, fine tablets, aqueous release tablets, aqueous release tablets, lozenges, chewable tablets, suppositories, implants, freeze-dried tablets, adsorbed tablets, or powders containing nano-dispersions as defined in Patent 1. 19. Pharmaceutical delivery systems, either matrix-controlled or membrane-based, orostomy tubes, transdermal delivery systems, or injectable microcapsules containing nano-dispersible substances, as defined in Claim 1. 20. The final pharmaceutical formulation as defined in Claim 16, Claim 17, or Claim 19, which contains nano-sized dispersions in an aqueous phase. 21. A final pharmaceutical formulation as defined in Claim 16, Claim 17, Claim 19, or Claim 20, which contains nanoscale dispersions in an aqueous phase at concentrations of 0.01 to 100 percent by weight. 22. A final pharmaceutical formulation as defined in claims 16 or 19, containing nano-sized dispersions directly within it. 23. A final pharmaceutical formulation as defined in claim 18, containing a pre-phase of the nanoscale dispersion directly within it. 24. The final pharmaceutical formulation, as defined in claim 18, contains a nano-dispersed substance in its dehydrated form. 25. The use of the final pharmaceutical formulation as specified in any one of the claims 16 through 23 for the treatment of diseases of the system, endocrine system, cardiovascular system, respiratory system, gastrointestinal system, renal and urinary tract, musculoskeletal system, immune system, skin and mucous membranes, including for the treatment of infectious diseases, tumors and vitamin and mineral deficiencies. 26. The prephase of a nanoscale dispersion is obtained from a mixture of (a) membrane-forming molecules, (b) co-emulsifier, and (c) lipid-loving components until a homogeneous clear liquid is obtained; mixing is performed in an anhydrous medium. 27. The pre-phase of the nanoscale dispersion, as defined in Claim 26, characterized by its mixing, is achieved without any additional energy input. 28. A nanoscale dispersion consisting of (d) membrane-forming molecules, (e) co-emulsifier, and (f) lipid-loving components is obtained by (alpha) mixing components (a), (b), and (c) until a homogeneous transparent liquid (beta) is obtained. The addition of the liquid in step (alpha) to the aqueous phase, steps (alpha) and (beta) are performed without additional energy input.