359results about How to "Promote oral absorption" patented technology

The present invention relates to an orally administrable composition containing nanoparticles with the particle size of 500 nm or less, comprising 0.1˜30 weight % of a complex of a water-soluble drug and a counter-ion substance in which the charged water-soluble drug is bonded with the counter-ion substance, 0.5˜80 weight % of a lipid, 0.5˜80 weight % of a polymer, and 1˜80 weight % of an emulsifier, wherein the weight ratio of said lipid and said polymer is in the range of 1:0.05˜3, and a preparation method thereof. The composition of the present invention has high gastrointestinal absorption rate upon oral administration, and has high drug entrapping rate in the nanoparticle, and is also stable against lipases.

There are provided a fused pyrimidine compound having antagonistic activity against luteinizing hormone releasing hormone, and a medicine containing the compound. A luteinizing hormone releasing hormone antagonist containing a compound represented by the formula: wherein R1a is a hydrocarbon group which may be substituted or a hydrogen atom, ring Aa is a 6-membered aromatic ring which may be further substituted, ring Ba is a homocyclic or heterocyclic ring which may be further substituted, Wa is an oxygen atom or a sulfur atom, Xa1 and Xa2, which may be identical or different, are each a hydrogen atom, a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted, or Xa1 and Xa2 together may form an oxygen atom, a sulfur atom or NR3a (wherein R3a is a hydrocarbon group which may be substituted or a hydrogen atom), and Ya is C1-6 alkylene which may be substituted or a bond, or a salt or prodrug thereof.

The present invention provides a compound represented by the formula:wherein R1 is a C1-4alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4alkyl and (4′) a C1-4alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4alkoxy-C1-4alkyl, (3′) a mono-C1-4alkyl-carbamoyl-C1-4alkyl, (4′) a C1-4alkoxy and (5′) a mono-C1-4alkylcarbamoyl-C1-4alkoxy, or the like; R3 is a C1-4alkyl; R4 is a C1-4alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor / binding cite and a medicament comprising the same as an active ingredient:wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups:wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of:represents an aromatic heterocyclic ring.

The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+ / H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.

It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and / or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.

The present invention provides a particulate composition wherein an oil component containing reduced coenzyme Q10 is polydispersed forming a domain in a matrix containing a water-soluble excipient, which simultaneously shows high oxidative stability and high oral absorbability, a production method thereof, and a stabilizing method thereof. It also provides a food, food with nutrient function claims, food for specified health uses, dietary supplement, nutritional product, animal drug, drink, feed, pet food, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like, which contain the composition.

A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects.

The invention discloses a cyclohexane amine compound and application of the cyclohexane amine compound as anti-schizophrenia medicine. The cyclohexane amine compound has high affinity to a dopamine D3 receptor and a 5-HT1A, and representative compounds have a high selectivity of D3 / D2 receptors. According to in vivo tests, the representative compounds such as I-1 compound can remarkably improve relative symptoms of apomorphine model mice and MK-801 model mice. The cyclohexane amine compound has the advantages of being good in anti-schizophrenia effect, low in acute toxicity and good in safety, and having development value of serving as novel high-efficiency and low-toxicity medicine for anti-neurological disorder diseases. The cyclohexane amine compound is a compound with a structural general formula (I) or stereomer, free alkali, aquo-complex or salt.

The present invention provides a method of increasing the absorbability of oxidized coenzyme Q10 by preparing the oxidized coenzyme Q10 as a composition in the presence of a lysolecithin and an oil and fat. The composition of the present invention comprising oxidized coenzyme Q10, a lysolecithin and an oil and fat, wherein the weight ratio of the lysolecithin to the oxidized coenzyme Q10 is not less than 0.7, shows superior absorption of oxidized coenzyme Q10 and can be utilized for food, food with nutrient function, food for specified health uses, nutritional supplement, nutritional product, animal drug, beverage, feed, pet food, cosmetics, pharmaceutical product, therapeutic drug, preventive drug and the like.

Belonging to the field of pharmaceutical chemical engineering, the invention in particular relates to a variety of scutellarin aglycone crystal forms and a preparation method thereof. The invention also relates to application of the scutellarin aglycone crystal forms in preparation of drugs preventing and / or treating cardiovascular and cerebrovascular diseases, rheumatism arthritis, stroke sequelae and the like. The scutellarin aglycone crystal forms provided by the invention have good stability, and can overcome the poor oral absorption and low bioavailability problems of scutellarin.

A self-emulsifying product of coix seed oil in the orally taken forms, such as softgel, liquid capsule, solid capsule, particle, etc, is proportionally prepared from coix seed, emulsifier, disperser, emulsifying aid, and solid adsorbent. It can be emulsified by itself in gastrointestinal tract for higher biologic utilization rate and higher curative effect. Its preparing process is also disclosed.

The invention relates to a pH sensitivity solid drug composite used for oral preparations and a preparation method thereof. Drug release of the solid drug composite in a gastrointestinal tract has the pH sensitivity, and the solid drug composite can enhance the absorption of drugs in the gastrointestinal tract or improve other performances of the drugs.

The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same.The present invention relates to a compound represented by the formula (I) or salt(s) or solvate(s) thereof. (In the formula, is an optionally substituted divalent residue of benzene, pyridine, cyclohexane or naphthalene or is a vinylene group whereAr is an optionally substituted aryl group;X is —NH—, oxygen atom or sulfur atom;Y is —NR1—, oxygen atom, sulfur atom, sulfoxide or sulfone;Z is a single bond or —NR2—;R1 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group;R2 is hydrogen atom, optionally substituted lower alkyl group, optionally substituted aryl group or optionally substituted silyl lower alkyl group;l is an integer of from 0 to 15;m is an integer of 2 or 3; andn is an integer of from 0 to 3).The compound of the present invention is useful as a pharmaceutical composition, particuarly as an inhibitor of acyl coenzyme A cholesterol acyltransferase (ACAT).

The invention belongs to the field of biomedicine, particularly to a novel chitosan derivative simulating the structure of cell-penetrating peptide and preparation method and application thereof. The invention has the beneficial effects that the invention provides a chitosan derivative which simulates the structure of cell-penetrating peptide, is relatively simple in structure and easy to synthesize and is provided with or promotes physiological active substances to penetrate the cells, the mucosa, the digestive tract, the skin, the hemato encephalic barrier and other physiological barriers of various organisms.

The invention discloses a nitrogenous benzheterocycle derivate and application thereof to treating nervous and mental diseases. Pharmacology experiments show that the derivate has better anti-schizophrenia action and lower toxicity. The derivate is free alkali or salt having the following structure general formula.

The present invention uses puerarin as main medicine, phospholipid as absorption-promoting agent, polysorbate 80 as solubilization agent, and the weight ratio of puerarin and phospholipid is 1-20:1-4, and the weight ratio of puerarin and polysorbate 80 is 1-20:1-15, and adopts a certain preparation method to obtain the invented puerarin oral preparation which can be made into granules, tablet, capsule and soft capsule, etc. Said invention also provides its preparation method, including preparation of puerarin and phospholipid composite and its preparation. Said invention preparation is stable in quality, has no toxicity and irritation to body, and its biological utilization rate can be obviously raised.

The invention belongs to the technical field of chemical synthetic medicines and particularly relates to water soluble salts of an organic acid of 5-(2-fluorophenyl)-N-methyl-1-(3-pyridyl sulfonyl)-1H-pyrrole-3-methylamine and an injection thereof for treating gastric acid related diseases and a preparation method thereof. The invention discloses the salts of the organic acid of 5-(2-fluorophenyl)-N-methyl-1-(3-pyridyl sulfonyl)-1H-pyrrole-3-methylamine shown as the following general formula in the specification, wherein n is 1 or 1 / 2 and HA is an organic acid. According to the salts of the organic acid, which are disclosed by the invention, the solubility of the salts in water or an artificial gastric and intestinal juice is far greater than TAK438, and the solubility of pyroglutamate and lactate in water is greater than 1g / mL.

A self-emulsified ganoderma spore oil in the form of soft capsule, liquid soft capsule, capsule, particle, etc is prepared from ganoderma spore oil, carrier, emulsifier, emulsifying assistant and / or adsorbent. Its preparing process is also disclosed.

Compositions for protection against SVFS induced by niacin, a carcinoid, mesenteric traction, serotonin, post-menopause, alcohol, monosodium glutamate, mastocytosis, atopic dermatitis, food-allergy or food intolerance, and mast cell activation syndrome, or against individual symptoms of SVFS, superficial vasodilation, feeling of warmth, itching (pruritus) and hives, comprising a flavonoid compound of the structure 2-phenyl-4H-1-benzopyran or 2-phenyl-4-keto-1-benzopyran or glycosides thereof, or chalconoid compounds, with appropriate substitutions of their hydroxyl groups to render them water soluble or in combination with a pshospholipid or cyclodextrin to render them to have higher oral absorption, administered alone or together with an anti-superficial vasodilation dose of one or more of, olive kernel oil, a serotonin inhibitor, a prostaglandin inhibitor, willow bark extract. A composition for treating cardiovascular disease with niacin, but without eliciting the SVFS effects of niacin, has also been invented.

The present invention discloses a method for treating or preventing a bone disorder in a mammal in need thereof comprising orally administering to said mammal a pharmaceutically effective amount of a pharmaceutical composition of at least one bisphosphonate, or a pharmaceutically acceptable salt or esters thereof, and at least one aminoalky methacrylate copolymer, according to a dosing schedule having a dosing interval selected from once-weekly dosing, twice-monthly dosing, once-monthly, once-quarterly and once-annually dosing. The present invention further discloses a method for treating or preventing a bone disorder in a mammal in need thereof comprising continuously orally administering a unit dosage per-day to said mammal in a short time for a long time therapy.

The present invention relates to the compound represented by formula (I):(wherein, all the symbols has the same meanings as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof.Since the compound of the present invention has an anti stress action, it is useful for preventive and / or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.

The invention relates to an oligosaccharide metallic compound. The compound is characterized in that sugar residues of the compound consist of alpha-1, 4-L-guluronic acid; the weight average molecular weight of the compound is less than or equal to 12kD; and a molecular general formula of the compound is (C6H7O6)nCrm, wherein n is equal to 1 to 54, m is equal to 1 to 27 and the mass percentage of trivalent chromium is 0.1 to 12 percent. The preparation of the compound comprises the following steps: slowly adding chromic salt and dilute alkaline aqueous solutions in oligoguluronic acid aqueous solution under the conditions that pH is equal to 5 to 10 and temperature is between 40 and 80 DEG C; after stopping adding dilute alkaline and chromic salt aqueous solutions, carrying out heat-insulation reaction for 1 to 3h; carrying out filtration and precipitating the filtrate by ethanol with the volume 3 to 5 times that of the filtrate; carrying out static, precipitation and centrifugation; and collecting and washing the precipitate by using anhydrous ethanol to obtain the compound after drying. The oligosaccharide metallic compound has the advantages that because the raw materials are derived from marine natural products, the compound has abundant resources, easy industrialization, high safety, unique structure and ideal oral absorption and particularly integrates the advantages of marine oligosaccharide and trivalent chromium; and the compound not only has the functions of preventing insulin resistance and adjusting sugar and fat metabolism disturbance, but also has broad market and application prospects particularly in the prevention and treatment of diabetes II.

The invention relates to the field of pharmaceutical preparations, in particular to a hydroxy safflor yellow A soft capsule preparation with high bioavailability, the invention is characterized in that the invention consists of hydroxy safflor yellow A, oily matrix and surfactant, and the invention also discloses the preparation method.

2-Amino-6-arylthiopurine phosphonate shows no toxicity (inhibition of bone marrow cell growth, mutagenicity, etc.) but a high antiviral activity, has an oral absorbability and a high safety and can be produced in a short process. Thus, use of this compound makes it possible to provide an excellent antiviral agent which can be efficiently produced.

The invention relates to preparation and application of oral insulin nanoparticles. The oral insulin nanoparticles mainly comprises a carrier of N-amino acid chitosan and medicinal insulin, are used for treating diabetes and have a better effect of reducing blood sugar.

The invention provides a controlled release dosing medicine core composition and an osmotic pump preparation comprising the medicine core composition. The medicine core composition comprises, by weight, 100 parts of an amphiphilic polymer carrier Soluplus, 5-200 parts of medicines, 0-50 parts of a surface active agent, 0-200 parts of a framework material having the controlled release effect, 100-200 parts of an osmotic pressure accelerant having the controlled release effect and 0-20 parts of other auxiliary materials acceptable in pharmacy; the low-solubility medicines are medicines with the in-water solubility smaller than or equal to 1 mg / mL and comprise indissolvable or insoluble medicines with the solubility smaller than or equal to 0.1 mg / mL in water and medicines with the solubility larger than 0.1 mg / mL and very slightly soluble medicines smaller than or equal to 1 mg / mL; the surface active agent is an anion surface active agent; and the other auxiliary materials acceptable in pharmacy comprises one or more kinds of a bonding agent, a coloring agent and a lubricating agent.

Provided is a pharmaceutical composition having improved oral absorption of a bisphosphonate drug, comprising at least one active substance selected from bisphosphonate drugs having non-permeability to a lipid biomembrane due to ionization and high water-solubility in vivo and having bioavailability of less than 10%, and at least one selected from biocompatible water-soluble chitosan, as essential ingredients.

The invention provides a use of low-molecular weight oligomannuronate in preparation of a drug or a health care product for preventing or treating Parkinson's disease. According to the invention, marine acidic polysaccharose as a raw material is prepared into a water-soluble low-molecular weight mannuronic acid compound. An experiment proves that the low-molecular weight mannuronic acid can be used for preventing and treating or improving Parkinson's disease, has obvious pharmacological effects and no toxic or side effects on nerve cells and can be taken for a long time. The low-molecular weight mannuronic acid is a marine natural product, has the advantages of rich resources, easy industrialization, high safety, unique structure and good oral absorption, and has a wide market application prospect in prevention and treatment of Parkinson's disease.

There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.A compound represented by the following formula (I):wherein R1 represents a hydrogen atom or a C1-8 alkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, or a benzyloxy group which may be substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group which may be substituted; R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and A1 represents a nitrogen atom or C—R3d (wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group),or a salt thereof, or a VLA-4 inhibitory drug comprising the compound or the salt as an active ingredient.