20 results about "First pass effect" patented technology

The application discloses a folic acid composition, a folic acid patch and a preparation method thereof. The folic acid composition comprises folic acid, pressure-sensitive adhesive, a fatty compound and an alcohol compound; the fatty compound comprises a fatty acid and / or a fatty acid ester. The folic acid patch comprising the folic acid composition improves the bioavailability of folic acid, reduces the administration frequency, avoids the liver first-pass effect, has good folic acid penetration stability, and the folic acid content in the folic acid patch is basically unchanged after long-time placement.

The invention belongs to the technical field of transdermal patches, and relates to a transdermal patch for improving the bioavailability of estradiol and a preparation method of the transdermal patch. The transdermal patch is prepared from the following components in percentage by weight: 5 to 21 percent of estradiol, 8 to 15 percent of polymer matrix, 0.5 to 1.5 percent of butylated hydroxytoluene, 10 to 15 percent of hydrogenated rosin glyceride, 2 to 5 percent of penetration enhancer, 3 to 8 percent of plasticizer and 25 to 35 percent of solvent. According to the transdermal patch disclosed by the invention, continuous and stable release of a medicine is realized, the transdermal absorption rate of estradiol is improved, so that the bioavailability is improved, the treatment effect is further improved, and meanwhile, the transdermal patch disclosed by the invention can also avoid a first-pass effect of the liver and reduce side effects; the transdermal drug delivery system is convenient to use, and the compliance of a patient is improved.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to sublingual lozenges of progesterone and analogues thereof as well as a preparation method and application of the sublingual lozenges. Specifically, a novel sublingual administration dosage form which is more suitable for being absorbed by a human body is designed according to physicochemical properties of progesterone and analogues thereof. The sublingual lozenge is composed of a main drug, a filler, a disintegrating agent, a mucous membrane promoter, a flavoring agent, a lubricant and the like. The sublingual lozenge is quickly disintegrated under the action of saliva, is quickly absorbed through tongue mucosa, takes effect quickly, avoids the first-pass effect, improves the bioavailability, and is suitable for various clinical scenes needing quick and efficient progestational hormone support.

The present invention relates to a formulation of toothpaste for the treatment of various disorders or diseases in the human body by incorporating or adding appropriate active ingredients in therapeutic amount or pharmaceutically effective amount for a particular disorder or disease intended to be treated. In particular, the present invention relates to a toothpaste formulation comprising of one or more active ingredients, oral mucosal absorption enhancers, gelling agents, preservatives, and one or more inactive agents. The present invention provides a novel toothpaste formulation and the process of preparing the same. Oral cavity offers relatively consistent and friendly physiological conditions for drug delivery or drug absorption. Thus, absorption through oral buccal mucosa in the toothpaste under invention by-passes the undesirable first-pass effects in the liver ensuring rapid and better bioavailability and greater efficacy.

The invention discloses a traditional Chinese medicine compound beewax thermal therapy transdermal drug product as well as preparation and application thereof, and belongs to the technical field of external treatment of traditional Chinese medicines. The product is composed of 70%-90% of natural beeswax and 10%-30% of a traditional Chinese medicine compound, and the traditional Chinese medicine compound is selected from medicines for promoting blood circulation to remove blood stasis, dispelling wind and eliminating dampness and the like according to indications; the preparation method comprises the steps of traditional Chinese medicine pretreatment, beewax melting, medicine mixing and forming. During application, treatment is completed through medicinal wax heating, skin pretreatment, medicinal wax application, treatment maintenance and subsequent treatment. The physical effect of beeswax thermal therapy and the pharmacological effect of traditional Chinese medicine are synergistically combined, the continuous thermal effect of beeswax can promote blood circulation, improve the transdermal efficiency of the medicine and enhance the activity of the medicine, and the curative effect is remarkable; the natural beewax is good in biocompatibility, gastrointestinal tract stimulation and the first-pass effect of the liver are avoided through transdermal drug delivery, and the safety is high; the medicine is standardized in preparation, simple and convenient to operate, suitable for primary medicine and families, capable of treating various diseases such as painful diseases and soft tissue injury and high in clinical application value.

The invention relates to a cabazitaxel self-emulsifying oral preparation and a preparation method thereof. The cabazitaxel self-emulsifying oral preparation is prepared from the following raw materials: a cabazitaxel active matter, grease, a surfactant and a cosurfactant, the cabazitaxel active matter is cabazitaxel or pharmaceutically acceptable salt, ester and solvate of cabazitaxel. After the cabazitaxel self-emulsifying oral preparation developed by the invention is in contact with an aqueous medium, nano-emulsion with small particle size (below 450 nm) can be spontaneously formed, drugs can be quickly released, and the first-pass effect of the liver can be bypassed through lymphatic transport, so that relatively high oral bioavailability is realized; the invention provides a comprehensive technical scheme capable of simultaneously solving the three problems of dissolution, permeation and metabolism, and a brand-new feasible path is opened up for oral administration of the cabazitaxel active matter.

Provided in the present invention are kemeiflufen hydrochloride and a crystal form thereof, a preparation method, and an application. The kemeiflufen hydrochloride of the present invention is 3-(3-ethyl-1-methyl-1H-hexahydroazepin-3-yl),2-(2-fluoro-4-biphenyl)-phenyl propionate hydrochloride, and has good solubility and stability, has a rapid medicinal effect, avoids the liver first-pass effect, improves bioavailability, and achieves the effects of reducing toxicity and enhancing efficacy. The preparation method for the kemeiflufen hydrochloride of the present invention is simple, and the product yield is high.

The invention discloses a salbutamol sulfate oral solution and a preparation method thereof.According to the salbutamol sulfate oral solution, a physical barrier is formed through inclusion of hydroxypropyl-beta-cyclodextrin, and a stability synergistic mechanism is formed through the chelating chemical inhibition effect of EDTA-2Na, so that the oxidative degradation rate of salbutamol sulfate is obviously reduced; in addition, sucralose and peppermint essence are used as flavoring agents for taste, high-sweetness taste modification and cool taste modification are performed, and triple taste masking of HP-beta-CD inclusion, sucralose and peppermint essence is performed, so that the taste score is remarkably improved; by destroying intestinal epithelium tight connection through sodium cholate, the transmembrane transport efficiency is improved, the bioavailability is improved, the apparent permeability coefficient (Papp) is remarkably improved, the problem of low availability caused by the first-pass effect is solved, beagle is orally taken, the bioavailability is remarkably improved, and the application prospect is remarkable.

The invention relates to the technical field of pharmaceutical preparation science and technology, and discloses polygonum cuspidatum compound nano-cream as well as a preparation method and application thereof. The polygonum cuspidatum compound nano emulsifiable paste can synergistically exert the antibacterial, anti-inflammatory and anti-oxidation effects of PD, RV and SK, regulate and control key paths for acne attack in a targeted manner, improve the skin permeability of insoluble components and the retention volume of focus parts by virtue of the delivery advantage of glycyrrhizic acid nano-micelles, reduce the external irritation, and improve the curative effect of acne. The first-pass effect and the whole body toxic and side effects of oral administration are avoided, so that a novel preparation scheme with innovativeness and practicability is provided for safe and efficient treatment of acne.

The invention provides comeflufen hydrochloride as well as a crystal form, a preparation method and application thereof. The comeflufen hydrochloride disclosed by the invention is 3-(3-ethyl-1-methyl-1H-hexahydroazepine-3-yl) and 2-(2-fluoro-4-biphenyl)-phenyl propionate hydrochloride, has good solubility and stability, is quick in drug effect, and can avoid the first-pass effect of the liver, improve the bioavailability and achieve the effects of reducing toxicity and enhancing efficiency; the preparation method of the comeflufen hydrochloride is simple, and the product yield is high.

The application discloses a Mongolian medicine composition for treating chronic kidney disease and application thereof, and belongs to the technical field of biological medicine. The Mongolian medicine composition comprises the following components: 35-45 parts of rhubarb, 30-40 parts of Guangming salt, 15-25 parts of alkali flower, 20-30 parts of Punica granatum, 15-25 parts of Cyclocarya paliurus, 20-30 parts of Kaempferia, 10-20 parts of Inula helenium and 15-25 parts of Terminalia chebula. According to the theory of three roots and seven elements, the theory of viscera, the theory of metabolism of clear and turbid and the whole view, and in combination with the theory of "gut-kidney axis", the Mongolian medicine composition with remarkable curative effect on chronic kidney disease is developed. The enema administration is adopted, the drug directly acts on the intestinal mucosa, the liver first-pass effect is avoided, the drug utilization rate is improved, the administration scheme is optimized, the operation is simple and the safety is high. Moreover, all the components of the composition are natural Mongolian medicine components, the toxic and side effects are small, the patient compliance is good, a new treatment idea is provided for the clinical treatment of chronic kidney disease.

This invention discloses a sustained-release transdermal patch containing magnolia oleoresin, its preparation method, and its application, belonging to the field of traditional Chinese medicine external preparation technology. The patch consists of a gel layer containing magnolia oleoresin extract, a backing layer, and a protective film. Sodium polyacrylate, PVP K90, glycerin, and chitosan quaternary ammonium salt are used as the gel matrix, with the addition of high-purity magnolia oleoresin extract and a penetration enhancer. The preparation method includes ethanol extraction and macroporous resin purification of magnolia oleoresin from magnolia oleoresin, preparation of a blank matrix, preparation of the drug solution, drug loading and mixing, coating and molding, and drying and cutting. The process is stable and controllable. The transdermal patch prepared by this invention can achieve sustained transdermal drug release, bypassing the first-pass effect of the liver. It is convenient to use, has high compliance, and provides a safe and effective new formulation for the treatment of rhinitis.

The invention belongs to the technical field of pharmaceutical preparations, and discloses a nasal vinpocetine salt gel as well as a preparation method and application thereof. The vinpocetine salt type derivative in the nasal vinpocetine salt gel precursor composition provided by the invention is used as a key functional component, relatively high bioavailability and brain entry efficiency are shown, the central Abeta removal efficiency is enhanced, a nasal gel drug delivery system is formed by the chitosan / carboxymethyl cellulose and the derivative thereof, and the drug delivery effect is improved. The double functions of prolonging retention and efficiently entering the brain are achieved, and the problem that the first-pass effect of vinpocetine medicine is remarkable is solved through the system.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a lumepirone tosylate orally disintegrating composition and a preparation method thereof. The lumepirone tosylate orally disintegrating composition is obtained by taking lumepirone tosylate as an effective component and taking a methacrylic acid and methyl methacrylate (1: 2) copolymer or glyceryl monostearate and glyceryl distearate as a carrier to prepare drug-loaded nanoparticles and forming a highly porous loose structure which is rapidly disintegrated when meeting saliva through a freeze-drying process. The carrier effectively encapsulates the lumepirone tosylate through intermolecular force, bitter taste and numb taste of the medicine can be effectively shielded, meanwhile, the medicine is promoted to be rapidly dispersed in saliva and directly absorbed through oral mucosa by means of the small-size effect of nano-particles, the serious first-pass effect of the medicine absorbed through gastrointestinal tracts is avoided, and the bioavailability of the medicine is improved. The bioavailability of the medicine is obviously improved, the dosage of the medicine is reduced, and the medication compliance of a patient is improved.

The invention discloses lily polysaccharide dry powder particles for reducing blood sugar by inhalation administration as well as a preparation method and application of the lily polysaccharide dry powder particles. The lily polysaccharide dry powder is mainly particles which are formed by pelletizing lily polysaccharide and are suitable for inhalation. The preparation method mainly comprises the step of carrying out air jet pulverization or spray freeze drying on the lily polysaccharide to obtain the lily polysaccharide dry powder particles. The lily polysaccharide dry powder particles can be used for inhalation administration of hypoglycemic drugs or drugs for treating diabetes mellitus. Based on an air jet pulverization technology and a spray freeze drying technology, an environment capable of accurately regulating and controlling the particle size and distribution of the lily polysaccharide without the help of other carriers and auxiliary materials is provided, the lily polysaccharide is directly delivered to the lung, gastrointestinal tract damage and the first-pass effect of the liver can be effectively avoided, the administration dosage is reduced, and the onset time is shortened.

The invention provides a method for preparing an oral dissolving membrane for animals by using a micron-sized emulsified suspension homogeneous solution. The method comprises the following steps: preparing a membrane-forming material, an emulsifier and a water-insoluble substance into a suspension for later use in a solvent; adding other components, controlling the temperature, and uniformly mixing to prepare a suspension film-forming system; adding auxiliary materials; removing bubbles and injecting into a coating groove; flattening and coating treatment is carried out; and cutting after drying. The film is suitable for animals capable of being subjected to individualized operation, such as pets, breeding livestock and young livestock, natural alternative substances can be added into the film, the film can be accurately delivered, act on the oral cavity in a targeted mode and efficiently utilized, the first-pass effect is avoided through oral mucosa absorption, the bioavailability and the effect taking speed are improved, in the coating and film forming process, the utilization rate of power equipment is increased, and the cost is reduced. And the production cost is reduced. Individualized medication and traceable recording are achieved, cross contamination of group medication is avoided, and the feasibility, reliability and effectiveness of an anti-reducing and anti-replacing scheme are improved.

This invention belongs to the fields of pharmaceutical formulation and biomedicine, and relates to an anti-atherosclerotic hybrid exosome, its preparation method, and its application. A hybrid composed of M2 macrophage exosomes and liposomes is used as a carrier, with the carrier loaded with a ferroptosis inhibitor and atorvastatin. The drug loading and encapsulation efficiency of the ferroptosis inhibitor are 1.55–2.57% and 11.99–49.86%, respectively; the drug loading and encapsulation efficiency of atorvastatin are 1.48–12.66% and 46.4–77.31%, respectively. The hybrid exosome provided by this invention has inflammatory targeting ability and higher stability, and can avoid the first-pass effect of the liver and the clearance of the circulatory system through intravenous injection. Simultaneously, this hybrid exosome has effects such as inhibiting ferroptosis, promoting cholesterol efflux, promoting cell burial, anti-inflammation, and regulating the immune microenvironment, enabling multi-faceted treatment of atherosclerosis, thus achieving better therapeutic effects.

The invention discloses a ginsenoside-containing flash release agent as well as a preparation method and application thereof. The flash release agent is prepared from red ginseng, dwarf lilyturf tuber, Chinese magnoliavine fruit and specific auxiliary materials, and does not contain any sweetening agent or flavoring agent. The preparation method comprises the steps of superfine grinding, clathration and taste masking and direct tabletting. According to the invention, by optimizing the ratio of auxiliary materials and a tabletting process, the preparation is rapidly disintegrated within 3 seconds under the tongue, active ingredients are directly absorbed by sublingual mucous membrane, the first-pass effect is effectively avoided, and the preparation rapidly takes effect within 3 minutes; meanwhile, a sugar-free formula and a cyclodextrin inclusion technology are adopted, so that the beverage tastes good and is suitable for diabetics. The preparation method is simple and convenient in process and excellent in stability, and can be used for preparing medicines or health-care products for improving learning and memory, relieving fatigue or assisting sedation.

This invention provides a novel use of Atractylodes macrocephala essential oil for the prevention and treatment of hair loss and alopecia areata. The characteristic components of the Atractylodes macrocephala essential oil include: atractylenolide I, atractylenolide II, atractylenolide III, atractylone, β-elemene, hesperidin, and isohesperidin. The invention also provides a method for preparing essential oil compositions, pharmaceutical formulations, and uses for the prevention and treatment of hair loss and alopecia areata. This method reduces bitterness and the first-pass effect in the liver, resulting in more stable blood drug concentrations and improved patient compliance. Compared to existing methods, it has advantages such as better efficacy and no toxic side effects. Developing health products and pharmaceuticals for the prevention and treatment of hair loss and alopecia areata based on this method has great potential.

The invention provides an inhalation dry powder for improving sleep and a preparation method thereof, belongs to the technical field of pharmaceutical preparations, and particularly provides the inhalation dry powder for improving sleep, which comprises the following components in parts by mass: 0.5-50 parts of melatonin; 0.5 to 50 parts of a gamma-aminobutyric acid-first diluent mixture; and 0-99 parts of a second diluent. The inhalation dry powder for improving sleep provided by the invention can be administered in an inhalation manner through the cooperation of the small-particle-size melatonin and the small-particle-size gamma-aminobutyric acid, has no first-pass effect, and can effectively improve the blood concentration and the sleep time of a subject and reduce adverse reactions.