23 results about "In vivo absorption" patented technology

The present invention relates to a liposome composition for oral administration, the composition comprising a GLP-1 analog. The liposome according to the present invention has both excellent encapsulation efficiency and encapsulation content of the GLP-1 analog drug, and the prepared liposome composition resists digestive enzymes in the gastrointestinal tract and does not easily degrade when administered orally, thus having excellent stability, and has a high absorption rate in the body, and thus exhibits excellent pharmacological effects.

The present invention discloses a heart-protective complex composition for improving the absorption rate of Coenzyme Q10 and a preparation method thereof, relating to the technical field of medicine and functional foods. The core active ingredients comprise Coenzyme Q10, Vitamin E, and black pepper extract within a specific mass ratio range. Pharmaceutically acceptable carriers and antioxidant synergists may also be combined to prepare various oral dosage forms. By constructing a ternary active component system with a specific ratio, the present invention achieves temporal synergy between absorption promotion and antioxidant regeneration in vivo, thereby solving the technical problems of low oral bioavailability and insufficient myocardial targeted accumulation of existing Coenzyme Q10 preparations. It significantly enhances the conversion efficiency of Coenzyme Q10 into the active form available to myocardial cells, and can be widely used in the preparation of drugs or functional foods for preventing or treating heart diseases.

This invention discloses a apigenin-betaine compound and its preparation method. The compound uses apigenin (Api) as its core, with -O-(CH2) at the 7', 4', and / or 5-position hydroxyl groups. n -N + (CH3)2-CH2COO ‑ Fragment substitution (n=2~12, x=1~3) forms an internal salt-type zwitterionic structure. In preparation, apigenin is first reacted with bromool Br(CH2). n A mitsunobu reaction was performed on OH under triphenylphosphine / dialkyl azodicarbonate conditions to obtain mono / polysubstituted bromoalkoxylated apigenin; subsequently, nucleophilic substitution with N,N-dimethylglycine under alkaline conditions yielded the target product. This structure, possessing both a tunable alkyl chain and a betaine cation / anion pair, significantly enhances the solubility and hydration capacity of apigenin in aqueous / alcoholic media, strengthens its affinity and stability for biomembranes, thereby improving in vivo absorption and distribution and potentially maintaining its antioxidant and anti-inflammatory activities. The method is mild, with a wide solvent and temperature range, suitable for scale-up and formulation applications.

The invention discloses a tadalafil oral soluble film and a preparation method thereof. The oral soluble film comprises the following components in parts by weight on a dry basis; the pharmaceutical composition comprises 20-35 parts of a deep eutectic drug carrier, 50-65 parts of a film-forming matrix, 1-3 parts of a polymer anti-devitrification agent, 3-5 parts of a disintegration accelerator, 4-8 parts of a plasticizer and 3-6 parts of a flavoring agent. An amphiphilic natural deep eutectic solvent technology is adopted, choline chloride, dicarboxylic acid and a hydrophobic donor are used for constructing a ternary system according to a specific molar ratio, the hydrophobic donor remarkably improves the solubility of tadalafil through hydrophobic interaction, a strong hydrogen bond of the deep eutectic solvent inhibits drug crystallization, and a high-speed shearing micro-domain dispersion technology is combined, so that the solubility of tadalafil is remarkably improved. The high-efficiency solubilization of insoluble drugs, excellent anti-crystallization stability, rapid disintegration performance and good taste are realized, mucous membrane irritation of a traditional surfactant is avoided, and in-vivo absorption and patient compliance are expected to be improved.

The application discloses a kind of composite protein gels and preparation method thereof, its preparation method includes the following steps: with the blood collection tube with anticoagulant is collected blood;The above-mentioned blood is centrifuged at 300-700g centrifugal acceleration at room temperature 10-20min;After centrifugation, blood is transferred to biological safety cabinet, and the upper plasma layer is extracted, and then it is placed in-80 ℃ ultra-low temperature refrigerator and rapidly frozen, and the freezing time is 24-72h;Then, the frozen plasma is taken out, and freeze-drying treatment is carried out under the condition that the temperature is-55-65 ℃ and the pressure is 50-100Pa, and the freeze-dried plasma is prepared;Calcium chloride injection is added to the freeze-dried plasma at a volume ratio of 1:0.5-2, then reacted in a water bath at 60-90 ℃ for 5-15min, and removed to prepare.The protein gel can effectively solve the problem of easy skin stiffening, collapse, high in vivo absorption rate and poor filler stability caused by hyaluronic acid and autologous fat.

GLP-1R agonist pharmaceutical compositions and uses thereof are disclosed. The pharmaceutical compositions include the compound represented by formula I or a pharmaceutically acceptable salt thereof, as an active ingredient. The pharmaceutical compositions include an acid-fast compound, and can release the active ingredient in the pharmaceutical composition slowly, thereby reducing in vivo absorption side effects following GLP-1R administration.

This invention relates to a pharmaceutical formulation, a coated pharmaceutical formulation, a method of preparation, and its application. The pharmaceutical formulation comprises a compound of formula I or a solvate thereof or a pharmaceutically acceptable salt thereof or a solvate thereof, a filler, a disintegrant, and a lubricant; based on the total mass of the pharmaceutical formulation, the mass percentage of the compound of formula I is 1%-50%, the mass percentage of the filler is 60%-90%, the mass percentage of the disintegrant is 1%-10%, and the mass percentage of the lubricant is 1%-10%. This formulation is used to prepare a medicament for the treatment and / or prevention of diseases related to GLP-1R. This invention achieves a better form of administration by mixing the active ingredient with excipients and undergoing formulation processing, resulting in a formulation with excellent in vivo absorption.

According to the trazodone hydrochloride sustained release tablet and the preparation method thereof, high-viscosity hydroxypropyl methylcellulose and low-viscosity hydroxypropyl methylcellulose are combined to serve as a sustained release material, the sustained release tablet can play a synergistic role to form a double-skeleton structure, so that medicine is stably released at a constant speed within 12-24 hours, and the sustained release effect is good. The sustained-release tablet can accurately regulate and control the drug release speed and reduce the fluctuation of blood concentration, so that the drug taking frequency is reduced to once a day, the risk of adverse reactions such as dizziness and drowsiness is reduced, the curative effect, compliance and safety of a patient are improved, and meanwhile, the sustained-release tablet is consistent in release behavior in different pH media, good in in-vivo absorption predictability and suitable for clinical application. Related substances grow slowly, the tablet stability is good, and the preparation method is simple, low in cost and suitable for industrial production.

Disclosed are a GLP-1R agonist pharmaceutical composition and a use thereof. The pharmaceutical composition comprises a compound represented by formula I, or a pharmaceutically acceptable salt thereof, as an active ingredient. The pharmaceutical composition contains an acid-resistant compound, and can slowly release active ingredients in the pharmaceutical composition, so as to reduce side effects of in vivo absorption after GLP-1R administration.

The invention provides an enteric-coated tablet for treating neuritis and a preparation method of the enteric-coated tablet. The enteric-coated tablet is prepared from the following components in percentage by weight: 0.01%-1% of mecobalamin, 60%-80% of butanedisulfonic acid adenosyl methionine, 10%-30% of a diluent, 4%-9% of an adhesive, 1%-5% of a disintegrating agent, 0.1%-1% of a lubricant and 8%-16% of an enteric-coated material. The enteric-coated tablet disclosed by the invention is simple in production process, universal in production equipment and low in cost, mainly overcomes the defect of large in-vivo absorption difference, and has a remarkable curative effect on treating neuritis.

This invention relates to the pharmaceutical field, specifically to a YBM compound, its preparation method, and its applications. The invention provides a YBM compound or its pharmaceutically acceptable salts and metabolites, wherein the YBM compound has the structure of Formula 1. Formula 1. Using SAR405 as the core skeleton, this invention aims to enhance its absorption in vivo or reduce its clearance rate by modifying and replacing its ring structure and substituents on the ring, ultimately providing a novel compound with a different skeleton structure and modifying groups. This compound can serve as a host-targeted antiviral drug that blocks viral replication by inhibiting virus-host interactions, exhibiting in vivo antiviral capabilities that SAR405 lacks. Therefore, it has applications in the preparation of VPS34 autophagy inhibitors, anti-SARS-CoV-2 drugs, and drugs for treating pneumonia caused by SARS-CoV-2.

The present application provides a kind of micro tablet, it includes the compound shown in formula I, filler and optionally pharmaceutically acceptable adjuvant, wherein, the diameter of the micro tablet is 1 ~ 3mm, the ratio of diameter and thickness is 0.6 ~ 1.2, the tablet weight is 2.5 ~ 10mg, and includes 1 ~ 5mg compound shown in formula I.The present application also provides the preparation method and pharmaceutical use of the micro tablet.The micro tablet of the present application can realize small dose direct precision dosing, easy to use;It is easy to swallow, can effectively improve the problem of poor palatability of cholic acid drugs, improve medication compliance;It can realize the effect of consistent dissolution characteristics of different doses, ensure the stability of treatment effect under different doses;It can reduce the use of adjuvant, avoid the safety problem of children medication;High stability, conducive to storage and transportation, improve the safety of use;High bioavailability, can more effectively realize in vivo absorption and utilization;Effectively solve the content uniformity problem, reduce the difficulty of process, more suitable for industrial production.

The present invention relates to a pharmaceutical formulation, a coated pharmaceutical formulation, a method for preparing same, and use thereof. The pharmaceutical formulation comprises a compound of formula I, or a solvate thereof, a pharmaceutically acceptable salt thereof, or a solvate of the pharmaceutically acceptable salt thereof, a filler, a disintegrant, and a lubricant. On the basis of the total mass of the pharmaceutical formulation, the mass percentage of the compound of formula I is 1% to 50%, the mass percentage of the filler is 60% to 90%, the mass percentage of the disintegrant is 1% to 10%, and the mass percentage of the lubricant is 1% to 10%. The formulation is used for preparing a medicament for treating and / or preventing GLP-1R-related diseases. The present invention achieves a better administration form by mixing the active ingredient with excipients and formulating, and provides the formulation with excellent in vivo absorption.

This invention relates to the pharmaceutical field, specifically to a YDT compound, its preparation method, and its applications. The invention provides a YDT compound or its pharmaceutically acceptable salt or metabolite, wherein the YDT compound has the structure of Formula 1. Formula 1. Using SAR405 as the core skeleton, this invention aims to enhance its absorption in vivo or reduce its clearance rate by modifying and replacing its ring structure and substituents on the ring, ultimately providing a novel compound with a different skeleton structure and modifying groups. This compound can serve as a host-targeted antiviral drug that blocks viral replication by inhibiting virus-host interactions, and exhibits in vivo antiviral capabilities that SAR405 lacks. Therefore, it has applications in the preparation of VPS34 autophagy inhibitors, anti-SARS-CoV-2 drugs, and drugs for treating pneumonia caused by SARS-CoV-2.

The invention discloses a gamma-PGA synthetase gene cluster pgsBCA '. The gamma-PGA synthetase gene cluster pgsBCA' is formed by sequentially connecting genes pgsB, pgsC and pgsA 'in series, the genes pgsB and pgsC are derived from a gamma-PGA synthetase gene cluster BA-pgsBCA of the bacillus altitudinis; the gene pgsA'is derived from a gamma-PGA synthetase gene cluster BM-pgsB 'C' A 'of bacillus megatherium. Bacillus amyloliquefaciens CF of which a genome knockout polyglutamate synthetase gene cluster is used as a host, and a recombinant polyglutamate synthetase gene cluster pgsBCA'is subjected to free expression through plasmids, so that a gene engineering strain capable of synthesizing gamma-L-PGA is obtained. When the strain is used for producing gamma-L-PGA in a 5L fermentation tank through amplification fermentation, the maximum yield can reach 10.5 g / L. Besides, the gamma-poly-L-glutamic acid is free of cytotoxicity and low in immunogenicity, so that the gamma-poly-L-glutamic acid has a wide application prospect in the fields of preparation of wound dressings, in-vivo absorption materials and the like. The invention provides a new material basis and technical support for application and development of polyglutamic acid in the fields of medicine and related biomedicine.

Disclosed are a gastroretentive double-layer sustained-release tablet, a preparation method therefor, and use thereof. An active ingredient of the gastroretentive double-layer sustained-release tablet is 3-[4-[4-(lH-benzotriazol-1-yl)butyl]piperazin-1-yl]benzisothiazole hydrochloride. Said tablet consists of two drug release layers comprising an immediate-release layer and a sustained-release layer. The immediate-release layer comprises the active ingredient, a filler I, and a disintegrant, and the sustained-release layer comprises the active ingredient, a filler II, a swelling material, a release blocker, a swelling enhancer, and a stabilizer. Said tablet can prolong the in vivo absorption window of the drug, maintain the plasma concentration, and prolong the in vivo half-life of the active ingredient.

The application discloses a gastric retention double-layer sustained-release tablet and a preparation method and application thereof, and belongs to the field of pharmaceutical preparations.The active ingredient of the gastric retention double-layer sustained-release tablet is 3-[4-[4-(1H-benzotriazole-1-yl)butyl]piperazin-1-yl]benzisothiazole hydrochloride, which is composed of two release layers, namely a quick-release layer and a sustained-release layer.The quick-release layer contains the active ingredient, a filler I and a disintegrant; and the sustained-release layer contains the active ingredient, a filler II, an expanding material, a release retardant, an expansion promoter and a stabilizer.The gastric retention double-layer sustained-release tablet can quickly release the drug in the quick-release layer to reach an effective blood drug concentration, and can prolong the retention time of the tablet in the stomach after the sustained-release layer expands, thereby prolonging the absorption window of the drug in the body to maintain the blood drug concentration and significantly prolong the in-vivo half-life of the active ingredient, and the drug administration frequency can be reduced and the patient compliance can be improved.The preparation process is simple, suitable for industrial production, and has a wide development prospect.

The present invention belongs to the field of pharmaceutical preparations, and relates to an oral preparation, which comprises (a) a compound of formula (1) or a pharmaceutically acceptable salt, isomer, solvate, hydrate or crystal thereof; and (b) an adsorbent. The invention also relates to a preparation method of the oral preparation and application of the oral preparation in medicines for preventing and / or treating hepatitis C. The oral preparation disclosed by the invention can be completely dissolved out, is well absorbed in vivo, has few impurities and is good in stability.

The invention discloses an apigenin betaine compound and a preparation method thereof. According to the compound, apigenin (Api) is taken as a parent nucleus, hydroxyl groups at the 7 position, the 4'position and / or the 5 position of the apigenin (Api) are substituted by-O-(CH2) n-N + (CH3) 2-CH2COO-fragments (n is equal to 2-12, and x is equal to 1-3), so that an inner salt type zwitterionic structure is formed. The preparation method comprises the following steps: firstly, carrying out Mitsunobu reaction on apigenin and brominated alcohol Br (CH2) nOH under the condition of triphenylphosphine / dialkyl azodicarboxylate to obtain mono / polysubstituted bromine-containing alkoxy apigenin; and then carrying out nucleophilic substitution with N, N-dimethylglycine under an alkaline condition to obtain a target product. The structure has an adjustable alkyl chain and a betaine cation / anion pair, the solubility and hydration capacity of apigenin in a water / alcohol medium are remarkably improved, and the affinity and stability of apigenin to a biological membrane are enhanced, so that in-vivo absorption and distribution are improved, and the activities of oxidation resistance, inflammation resistance and the like of apigenin are expected to be maintained. The method is mild in condition, wide in solvent and temperature range and suitable for amplification and preparation application.

Oral cannabinoid formulations, including an aqueous-based oral dronabinol solution, that are stable at room or refrigerated temperatures and may possess improved in vivo absorption profiles with faster onset and lower inter-subject variability.

The present invention relates to a health functional food having excellent functions of improving in vivo calcium absorption rate and improving vascular health. The health functional food comprises seaweed powder, milk calcium, magnesium oxide, microcrystalline cellulose, hydroxypropylmethylcellulose, vitamin D, organic maltodextrin, cross-linked sodium carboxymethylcellulose, magnesium stearate, and glycerin fatty acid esters.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a deferiprone composition and a preparation method thereof. The deferiprone composition provided by the invention is prepared from the following components in parts by weight: 50 to 70 parts of deferiprone, 0.1 to 2 parts of polyoxyethylene stearate, 0.1 to 2 parts of colloidal silicon dioxide, 25 to 40 parts of filling agent and 0.1 to 2 parts of lubricating agent. The deferiprone composition provided by the invention contains polyoxyethylene stearate, polyoxyethylene stearate and deferiprone are fully combined in a dry granulation mode, and deferiprone tablets or deferiprone capsules are obtained by tabletting, coating or filling into capsule shells, so that the preparation process is simple, the dissolution rate of the preparation is better improved, and the deferiprone composition is suitable for clinical application. The in-vivo absorption of the postprandial medicine during oral administration is facilitated. Meanwhile, the problems of sticking during tabletting and wall sticking during capsule filling are avoided, and the qualified weight difference of the preparation is ensured.