874results about How to "Reduced bioavailability" patented technology

This invention relates to a method of reducing an irritating or adverse side effect associated with the topical use of an active ophthalmic drug comprising incorporating an effective amount of a cyclodextrin or cyclodextrin derivative into a formulation to complex the active drug such that the concentration of the free active drug is reduced below a tolerable threshold, and incorporating an effective amount of a viscosity increasing agent in said formulation such that the bioavailability of said drug is high enough to be therapeutically effective, wherein the cyclodextrin or cyclodextrin derivative is not required to solubilize the active drug. Another aspect of this invention relates to topical ophthalmic formulations comprising an active drug, a cyclodextrin or cyclodextrin derivative, and a viscosity-enhancing agent, in effective amounts as stated above.

An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.

A spherical particle of the present invention contains a sugar alcohol and a crystalline cellulose and/or powdered cellulose, wherein the mass ratio between the sugar alcohol and the crystalline cellulose and/or powdered cellulose is within a range from 50:50 to 90:10, the particle size is within a range from 75 to 250 μm, the sphericity is not less than 0.8, and the bulk density is not less than 0.6 g/ml. Further, a method for producing the spherical particle of the present invention includes a granulation step of rolling a sugar alcohol having an average particle size of not more than 40 μm and a crystalline cellulose and/or powdered cellulose having an average particle size of not more than 50 μm while spraying a liquid thereon.

The present invention is directed to oral, therapeutically effective extended release pharmaceutical compositions of 3-hydroxy-N-methylmorphinan, including delayed onset, extended release dosage forms and the use thereof.

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Preparation and in vitro and in vivo characterization of novel forms of active pharmaceutical ingredients, suitable for pharmaceutical compositions in drug delivery systems for humans.

Compounds comprising nitric oxide derivatives of stilbenes, polyphenols and flavonoids and methods of their use are provided for treating patients suffering from any of hypercholesterolemia, vascular oxidative stress and endothelial dysfunction.

A pharmaceutically acceptable base addition salt of an organoboronic acid of formula (XXX):

wherein: P is hydrogen or an amino-group protecting moiety; R is hydrogen or alkyl; A is 0, 1 or 2;

• • R¹, R² and R³ are independently hydrogen, alkyl, cycloalkyl, aryl or —CH₂—R⁵;
  • R⁵, in each instance, is one of aryl, aralkyl, alkaryl, cycloalkyl, heterocyclyl, heteroaryl, or —W—R⁶, where W is a chalcogen and R⁶ is alkyl; and
  • where the ring portion of any of said aryl, aralkyl, alkaryl, cycloalkyl, heterocyclyl, or heteroaryl in R¹, R², R³ or R⁵ can be optionally substituted.

Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Disclosed are devices for urine voiding postponement, and methods for treating conditions such as central diabetes insipidus, enuresis, nocturia, urinary frequency or incontinence. The devices deliver a desmopressin flux through the skin of a patient in a low dose amount just necessary to achieve a desired anti-diuretic effect without undesirable side effects such as hyponatremia. The devices are designed to permit a state of normal urinary production to return quickly after the desmopressin flux is terminated.

The present invention relates to novel estrogen-related steroidal quinols and their use as drugs for estrogen replacement therapy. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues, bone, in the cardiovascular system, and in the CNS (central nervous system) with only a slight estrogenic action or no estrogenic action in the uterus. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example, estrogen replacement therapy, prevention and treatment of osteoporosis).

A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution/dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0.

The invention disclose a method for intercepting and fixing the persistent organic contaminants of soil through bio-carbon which includes the following steps: 1) a biomass material is carbonized for 0.5 to 6 hours under the temperature of 250 to 550 DEG C and the condition of oxygen limitation and passes through the screen of 10 to 200 meshes, thus preparing the bio-carbon; 2) the prepared bio-carbon is added into the soil polluted by the persistent organic matters according to the ratio of 1 to 200tons/hektare and the soil within 0 to 30cm of a surface layer is ploughed for leading the soil to be fully mixed with the bio-carbon; 3) after being aged, the bio-carbon fiercely absorbs the persistent organic matters, thereby greatly reducing the biological effectiveness thereof and being capable of producing safe farm products in the oil polluted by the organic mattes. The bio-carbon adopted by the treatment method has the advantages of easy obtaining, low cost, environmental friendlessness, non-secondary pollution, simple preparation technique, good treatment effect and long time effectiveness; simultaneously the bio-carbon contains a plurality of carbon and other nutrition elements, thus being capable of providing abundant carbon sources and nutrition for the growing of soil crops and having the effect for enriching the soil.

The invention concerns the repairing dose to repair the soil polluted by heavy metal, which belongs to the technique field of repairing soil polluted by heavy metal. The repairing dose mainly includes: Na unit soil, haibao stone, stick stone, coal powder and microorganism germ root. Every composition' rate by weight is: Na unit soil15--40%, haipao stone 10--50%, stick stone 10--30%, coal powder 5--30%, microorganism germ root 0--40%. The repairing dose in the invention has the advantages of low cost of material, simple working equipment, good effect and no second pollution.

The present invention relates to novel amino acid salts of fumaric acid monoalkylesters. The salts are suitable for use as active substances in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders.

Compositions and methods are provided that comprise improved means to achieve and maintain a targeted level of copper status in persons in order to treat and prevent copper associated diseases.

The present invention belongs to the technical field of soil heavy metal remediation, specifically discloses a method for preparing the iron-based biochar material, the iron-based biochar material prepared there from and a method for controlling the heavy metal pollution in soil using the iron-based biochar material. For the iron-based biochar material of the present invention, by using a method of high-temperature carbonization, a biomass is used as a raw material and an iron-containing compound is add in the process of preparing biochar, wherein iron is incorporated in a specific ratio, to form the iron-based biochar material with a special structure and function. The material has a simple preparation process, low cost and a short production period; the prepared iron-based biochar material has an unique effect on the arsenic-cadmium combined pollution soil remediation, can effectively reduce the bioavailability of arsenic and cadmium in the soil, significantly reduces the arsenic and cadmium contents in the agricultural products planted in the arsenic-cadmium combined pollution soil, and has no toxic and side effects on the crops, is safe to apply and can be applied to the control of arsenic-cadmium combined pollution soil in a large scale.

The invention relates to a reductive degradable stabilizer for heavy metal and/or organic matter polluted soil as well as a preparation method and use of the stabilizer. The reductive degradable stabilizer can be used for quickly and efficiently stabilizing the heavy metals and the organic matters in the polluted soil by virtue of a synergistic effect of a plurality of active ingredients, and can also be used for further lowering the content of the organic matters, so that the purpose of lowering leaching toxicity of pollutants and health risk is realized; therefore, the reductive degradable stabilizer is a novel and efficient stabilizer which has the advantages of being wide in treatment substrate, capable of reducing the total amount of the organic matters, good in stabilizing effect, convenient to operate and the like, and has a wide range of application in the governance fields including polluted soil, bottom mud, sludge and the like.