19 results about "Hepatic first pass effect" patented technology

Disclosed in the present invention are a preparation method for a brain-targeting agomelatine nasal spray micelle and use thereof, which belong to the technical field of pharmaceutical formulations. According to the present invention, an injectable pharmaceutical excipient polyethylene glycol (15)-hydroxystearate (HS15) is taken as a carrier material, HS15 and agomelatine are dissolved in an organic solvent, and the resulting solution is subjected to rotary evaporation under reduced pressure to form a uniform film, which, upon hydration, forms an agomelatine micelle solution capable of being sprayed nasally for treating depression and insomnia. According to the present invention, the problem of low oral bioavailability of agomelatine due to poor solubility, serious first pass effect of hepar, difficulty in penetrating a blood-brain barrier, etc., is solved. The micelle structure constructed in the present invention is quickly delivered into the brain after nasal administration, and it is stable in cerebrospinal fluid and can achieve slow release of the drug, thereby improving the intracerebral bioavailability of the drug and achieving high brain targeting property and low systemic toxic and side effects. The micelle structure has good clinical application value and market prospects.

The invention belongs to the field of pharmaceutical preparations, and specifically relates to a triptolide preparation and a preparation method thereof, wherein nanocarbon is carboxyl modified, chitosan oligosaccharide is used to composite the modified nanocarbon to obtain a chitosan oligosaccharide nanocarbon composite, and then the chitosan oligosaccharide nanocarbon composite is used to load triptolide, and the preparation is obtained after alcohol body inclusion. The triptolide preparation of the invention can reduce digestive tract toxicity, avoid first-pass effect, and can slowly and continuously exert therapeutic effects through the skin, with high drug loading rate and high skin permeability.

The invention relates to the technical field of medicine production, and provides an enadostat fumarate crystal, a preparation method thereof and a hydrogel patch. According to the preparation method disclosed by the invention, the enadostat is prepared into the fumarate crystal, so that the solubility of the enadostat can be improved; the hydrogel type patch prepared from the enadostat fumarate crystal can reduce the drug dosage, avoid the first-pass effect, maintain the stable blood concentration and improve the patient compliance, and meanwhile, the hydrogel type patch also has good skin adhesiveness, the characteristic of being suitable for drug release and good physical and chemical stability; wide application prospects are realized.

The present application relates to a sublingual tablet of nicergoline and a preparation method thereof, the sublingual tablet of nicergoline comprising nicergoline and pharmaceutically acceptable excipients; the pharmaceutically acceptable excipients comprise organic acid, diluent, disintegrant and lubricant. In the sublingual tablet of nicergoline, the organic acid as a cosolvent and the combination with nicergoline can increase the cumulative dissolution rate and dissolution rate of nicergoline, and improve the bioavailability and pharmacodynamic persistence of nicergoline. At the same time, the sublingual tablet of nicergoline can avoid liver first-pass effect, and has the advantages of convenient use and no need of water for administration.

The invention provides an essential oil composition. The essential oil composition is prepared from the following raw materials in parts by weight: 0.5-1.5 parts of safflower essential oil, 0.5-1.5 parts of ligusticum wallichii essential oil and 0.5-1.5 parts of angelica sinensis essential oil. The invention also provides application of the essential oil composition in preparation of external medicines for preventing or / treating qi-blood disorder. According to the invention, a synergistic effect mechanism of medicine and massage is adopted, on one hand, pharmacological action is exerted through percutaneous absorption of active substances such as essential oil, and on the other hand, local blood circulation is remarkably promoted, muscle spasm is relieved and medicine permeation efficiency is enhanced by means of a massage technique, so that deep fusion of medicine effect and physical treatment effect is realized, and the traditional Chinese medicine composition takes effect quickly and lasts long; the essential oil raw materials are combined, so that the synergistic interaction effect is achieved; the first-pass effect and gastrointestinal tract adverse reaction can be effectively avoided, and the composition is high in safety and suitable for long-term use.

The invention relates to the technical field of medicine, in particular to an ethanesulfonic acid nintedanib sublingual tablet and a preparation method thereof.The ethanesulfonic acid nintedanib sublingual tablet contains ethanesulfonic acid nintedanib, a carrier material, a filling agent, a disintegrating agent, a flavoring agent and a lubricating agent, and the ethanesulfonic acid nintedanib sublingual tablet is prepared by setting the specific proportion of the raw materials and the auxiliary materials. Compared with an original research medicine, namely a nintedanib ethanesulfonate soft capsule, the problem that the bioavailability is low due to the liver first-pass effect is effectively solved, the medicine provided by the invention is good in taste, excellent in stability, rapid in disintegration and rapid in dissolution rate, and each detection item meets the quality standard. And meanwhile, the clinical use compliance of a patient is also improved.

The application discloses a kind of enlicarabine sublingual preparations and preparation method thereof, the enlicarabine sublingual preparation includes the following component raw materials preparation: enlicarabine 2.5~50 parts, dissolving agent 5~20 parts, penetration agent 0.5~25 parts, excipient 17.5~405 parts;Wherein, the dissolving agent is sodium taurocholate, and the penetration agent is 8-(2-hydroxybenzamide) sodium octanoate.This enlicarabine sublingual preparation can be directly absorbed by sublingual mucosa under tongue, and after administration, drug absorption and effect are fast, and it is not necessary to take water, and effectively avoid the first pass effect of oral enlicarabine, wherein when cooperating with dissolving agent sodium taurocholate and penetration agent 8-(2-hydroxybenzamide) sodium octanoate, the solubility of enlicarabine can be obviously increased, and the mucosa absorption effect of enlicarabine can be obviously improved, the bioavailability and curative effect can be greatly improved, and it has good clinical use value and social benefits.

The invention discloses an acupoint application for treating polycystic ovarian syndrome and a preparation and use method thereof. The acupoint application comprises a radix salviae miltiorrhizae acupoint application, a semen cuscutae-radix salviae miltiorrhizae acupoint application, a radix morindae officinalis-radix salviae miltiorrhizae acupoint application and a semen cuscutae-radix morindae officinalis acupoint application. The traditional Chinese medicine composition is prepared from salvia miltiorrhiza, semen cuscutae and salvia miltiorrhiza, morinda officinalis and salvia miltiorrhiza, and semen cuscutae and morinda officinalis. The invention further provides a preparation method of the acupoint application and an artificial cycle therapy using method. The acupoint application medicine cake has the advantages that the acupoint application medicine cake is mainly used for treating the polycystic ovarian syndrome, has the effects of tonifying the kidney, activating blood, removing stasis and promoting follicular maturation and ovulation, is convenient and safe to apply externally, can enhance the compliance of a patient, can be absorbed through peritoneal transdermal absorption, can avoid the first-pass effect of oral administration, is closer to a disease site in the administration position, and takes effect faster.

A progesterone self-emulsifying formulation, a preparation method therefor, and use thereof. The progesterone self-emulsifying formulation comprises the following preparation raw materials by mass fraction: 0.5%-20% of progesterone, 15%-50% of an oily solvent, 45%-80% of a surfactant, and 0-25% of a co-surfactant. Progesterone in the progesterone self-emulsifying formulation is in a completely dissolved state, which promotes the absorption of progesterone in the body, thereby improving the oral bioavailability of progesterone. In addition, by means of dispersing progesterone in a self-emulsifying system, under the action of an oil phase, progesterone enters the lymphatic circulation together with chylomicrons, thereby avoiding the liver first-pass effect, not only increasing the oral bioavailability of progesterone, but also reducing the plasma concentration of metabolites, and reducing the incidence of adverse reactions of oral progesterone.

The invention discloses an inhalation preparation for treating IPF diseases. The inhalation preparation is an aerosol inhalation liquid preparation, an inhalation aerosol, an inhalation powder aerosol or a soft aerosol. The inhalation preparation comprises an active drug, and the active drug is any one of apremilast, ibudilast, roflumilast, crisaborole and defamilast. A preparation process of an inhalation preparation is introduced into a traditional preparation, active ingredients of a traditional oral preparation are easily damaged in digestive tracts, the bioavailability is low, the liver first-pass effect is achieved, the effect is slow, and the inhalation preparation capable of remarkably improving IPF is prepared. Tests prove that the prepared inhalation preparation can effectively improve the bioavailability and improve the clinical use effect.

The invention provides the stable ramelteon solution nasal spray, the medicine is atomized and then absorbed by the nasal mucosa to enter body fluid circulation, the problem of low bioavailability caused by the first-pass effect of the liver during oral administration of ramelteon is solved, meanwhile, the ramelteon solution nasal spray takes effect faster and is obviously superior to an oral preparation, the osmotic pressure conforms to the acceptable range of a human body, and the ramelteon solution nasal spray is free of irritation and has a good application prospect. The medicine is safer and is suitable for long-term treatment of chronic diseases. The ramelteon solution nasal spray provided by the invention is simple in preparation process, suitable for industrial production and low in production cost.

An inhalation formulation for treating an IPF disease. The inhalation formulation is an aerosol inhalation liquid formulation, an inhalation aerosol, a dry powder inhaler or a soft mist inhaler. The inhalation formulation contains an active drug, and the active drug is any one of apremilast, ibudilast, roflumilast, crisaborole, and difamilast. A preparation process for the inhalation formulation is introduced into a conventional formulation. An active component in a conventional oral formulation is prone to being destroyed in the digestive tract, and has low bioavailability, a liver first pass effect, and a slow onset of action. An inhalation formulation capable of significantly alleviating IPF is prepared. Tests prove that the prepared inhalation formulation can effectively increase the bioavailability, and improve the clinical use effect.

The invention discloses an external biological preparation for reproductive maintenance and male function improvement and a preparation method thereof. The external biological preparation is mainly prepared from clerodendranthus spicatus extract, cistanche deserticola extract, herba epimedii extract, maca extract, fructus lycii extract, salvia officinalis oil and functional polypeptide. The composition further comprises arginine, oyster peptide, hippocampus peptide, a yam root extract, a coleus forskohlii root extract, a tea leaf extract, a cynomorium songaricum extract and a tribulus terrestris extract. The external biological preparation breaks through the limitations of a first pass effect, gastrointestinal tract dependence, low bioavailability and the like of a traditional oral product, realizes accurate intervention aiming at the sub-health problem of men, is beneficial to improving testosterone concentration and NO level, improving inflammation, activating cell energy to promote repair and regeneration, promoting sperm formation and enhancing body microcirculation, and has a good application prospect. Therefore, the aims of protecting the gonad axis and improving the male function are fulfilled.

Provided are a nicergoline sublingual tablet and a preparation method therefor. The nicergoline sublingual tablet comprises nicergoline and a pharmaceutically acceptable auxiliary material; the pharmaceutically acceptable auxiliary material comprises an organic acid, a diluent, a disintegrant and a lubricant. In the nicergoline sublingual tablet, the organic acid is used as a co-solvent, and the compounding of same with nicergoline can increase the cumulative dissolution rate and dissolution speed of nicergoline, thereby improving the bioavailability and efficacy durability of nicergoline. The nicergoline sublingual tablet can avoid the hepatic first-pass effect, and has the advantages of convenient use and no need to be taken with water.

The invention provides tadalafil supramolecular nanoparticles and a preparation method thereof, and relates to the technical field of medical treatment. The tadalafil supramolecular nanoparticle comprises a particle composed of a microfiber skeleton, in-situ molecular glue and a drug carrier component, the drug loading rate of the particle needs to be larger than 58%, the particle has a hexagonal pore channel arrangement structure, the microfiber skeleton is ginkgo leaf cell walls with the delignification rate of 40-60%, and the cell walls contain natural channels with the diameter of 20-100 nm. According to the technology, natural channels of ginkgo leaf cell walls are utilized to form ordered pore channels to improve the drug loading capacity, abietic acid-tartaric acid molecular glue realizes intestinal targeted release and avoids gastric acid damage and a first pass effect, sericin protein films enable particles to be rapidly disintegrated in an oral cavity and take effect conveniently, natural plant carriers are fully degraded and free of toxicity, and rolling forming ensures the mechanical strength of the particles; long-term storage is facilitated, and efficient, safe and convenient medication experience is brought to patients.

The invention discloses a composition for treating chronic prostatitis and a preparation method and application thereof. The composition is prepared from, by mass, 8-15 parts of cortex cinnamomi, 5-7 parts of radix et rhizoma rhei, 1-2 parts of borneol, 5-8 parts of fructus foeniculi, 2-5 parts of flos caryophylli and 5-7 parts of herba verbenae. The Shenque acupoint external application is adopted, the medicine can permeate into viscera meridians and collaterals through the Shenque acupoint to achieve the treatment effect, the medicine applied to the umbilical region is not metabolized by the liver, stimulation of the medicine to the digestive tract and damage of the first pass effect of the liver to effective components of the medicine are avoided, and the treatment effect can be better achieved. Clinical tests show that the total effective rate of the medicine reaches 86.5%, and the medicine can effectively treat chronic prostatitis.

The present invention discloses a matrine-based ionic liquid conotoxin polypeptide solution, a preparation method and application thereof, wherein the steps include: providing a conotoxin polypeptide mother liquor; adding matrine and an organic acid to water to obtain a matrine organic acid ion salt solution; mixing the matrine organic acid ion salt solution and the conotoxin polypeptide mother liquor to obtain a matrine-based ionic liquid conotoxin polypeptide solution. The prepared matrine-based ionic liquid conotoxin polypeptide solution has good stability and biocompatibility, and has a sustained-release and penetration-promoting effect, can be delivered through the skin, can avoid the degradation of polypeptide drugs in the acidic and enzymatic reaction conditions in the digestive system and the first-pass effect of the liver in clinical applications, and can reduce the influence of the skin barrier function when used externally.

The present application relates to a kind of sodium valproate nasal mucosa administration preparation and its preparation and application, belong to medical technical field.A kind of sodium valproate nasal mucosa administration preparation, the preparation includes gastrodin and as medicinal component sodium valproate.The weight ratio of sodium valproate and gastrodin is 1:0.0025~2.The administration preparation of the present application is a kind of sodium valproate nasal mucosa administration preparation, can be delivered to brain by bypassing blood-brain barrier through nasal administration, improve brain bioavailability, prolong the effective action time of drug in brain, avoid first pass effect, reduce the risk of peripheral toxic side effect.The present application uses gastrodin as absorption promoter, by optimizing the ratio of gastrodin and sodium valproate, can reach the effect of increasing the absorption of sodium valproate in whole body and brain, further improve its brain bioavailability, enhance its therapeutic potential.

The invention relates to the technical field of traditional Chinese medicines, in particular to spleen-enlivening and intestine-activating paste. The traditional Chinese medicine composition is prepared from 15g of dried ginger, 10g of cinnamon, 10g of clove, 10g of radix aucklandiae, 10g of bran-fried fructus aurantii, 10g of ginger-processed cortex magnoliae officinalis and 6g of scorpion, the original prescription proportion and medicine are unchanged, and the dosage can be changed according to clinical requirements. The negative constipation is researched and treated by the invention, the main symptoms of the type of constipation are difficult or dry and hard stool accompanied with the symptoms of labor-consuming defecation, pale complexion, clear and long urine, less complexion, dizziness, chill sensation of abdomen and the like, and patients have light red or light dark tongues, white or thin, white and greasy tongue coating, slow or weak pulse or tight pulse. The treatment method adopted by the invention is an acupoint application therapy integrating medical meridians, acupoints and medicines, the medicines are percutaneously absorbed at local acupoints, gastrointestinal stimulation and a liver first-pass effect are avoided, the effect of stimulating meridian qi transportation by the medicines and acupoint stimulation is stably exerted, and the device has the advantages of being simple, convenient and rapid to operate, noninvasive and painless, easy to accept by patients and the like.