12 results about "Hepatic first pass effect" patented technology

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.

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 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.