176 results about "Enhanced bioavailability" patented technology

The invention discloses an application of Lactobacillus brevis 146 (Lactobacillus brevis 146) in improving the bioavailability of GABA (gamma-aminobutyric acid) (gamma-aminobutyric acid). According to the present invention, the specific Lactobacillus brevis 146 is adopted, such that the component of GABA is enriched, the GABA is more diversified, and the GABA, the dead bacteria component of the postbiotics, and the other metabolic components such as the active components such as polysaccharide are provided, such that the bioavailability of the GABA is improved; therefore, the lactobacillus brevis 146 and the GABA can be combined for use, and the lactobacillus brevis 146 can be used for preparing the medicine for treating the nervous system and intestinal diseases, and can be used for preparing food and health care products.

Pharmaceutical compositions are provided, which comprise cabozantinib or pharmaceutically acceptable salts thereof, and at least one pharmaceutically acceptable excipient, wherein the inventive compositions exhibit enhanced bioavailability compared to the currently marketed or commercially available formulations. The present invention also provides manufacturing processes thereof and use of the said inventive compositions for the prevention, treatment or prophylaxis of disorders in human patients in need thereof. The present invention relates to oral pharmaceutical compositions of cabozantinib, methods for their administration, processes for their production, and use of these compositions for treatment of diseases treatable by cabozantinib.

Solid lipid nanoparticles (SLNs) for delivery of bioactive compounds are disclosed. The SLNs comprise a lipid matrix and surfactant layer encapsulating at least one bioactive compound selected from vitamins, minerals, enzymes, algae-derived bioactives, proteins, peptides, amino acids, antioxidants, small synthetic molecules, plant-derived volatile compounds, or botanical extracts. The SLNs exhibit submicron particle size, low polydispersity, and sufficient surface charge to ensure colloidal stability and efficient delivery. In one embodiment, algae-based bioactives, such as phycocyanin or fucoxanthin, are encapsulated using only natural and sustainable lipids and surfactants to improve bioavailability and support environmentally friendly formulations. The SLNs may be formulated for oral, topical, transdermal, injectable, ophthalmic, mucosal, textile, veterinary, or agricultural administration. Applications include human and animal health, functional foods, skincare, nutrient supplementation, and crop treatment. The disclosed SLNs offer a biocompatible and scalable delivery system that protects sensitive compounds, enables sustained release, and enhances absorption across diverse industries.

Crystalline polymorphic lutein and cocrystal forms of lutein are disclosed. The new forms have enhanced bioavailability and stability, and may be used, for example, for topically delivering lutein to the eye for inhibiting or preventing cataracts, macular degeneration, and photooxidative damage to retinal pigment epithelium.

Pharmaceutical compositions are provided, which comprise cabozantinib or pharmaceutically acceptable salts thereof, and at least one pharmaceutically acceptable excipient, wherein the inventive compositions exhibit enhanced bioavailability compared to the currently marketed or commercially available formulations. The present invention also provides manufacturing processes thereof and use of the said inventive compositions for the prevention, treatment or prophylaxis of disorders in human patients in need thereof. The present invention relates to oral pharmaceutical compositions of cabozantinib, methods for their administration, processes for their production, and use of these compositions for treatment of diseases treatable by cabozantinib.

Provided herein, are compositions comprising GalNAc moieties that may be conjugated to an oligonucleotide. The oligonucleotide may be a small interfering RNA or an antisense oligonucleotide. Also provided herein are methods of treatment that include administering the composition to a subject.

The invention discloses a topiromilast osmotic pump tablet and a preparation method thereof. The topiromilast osmotic pump tablet comprises a tablet core composed of a drug layer and a pushing layer, a semipermeable membrane coating outside the tablet core, and a single drug release small hole and an isolation coating on the surface of a controlled release tablet on one side of the drug layer. Compared with topiromilast tablets on the market at present, the topiromilast osmotic pump controlled release tablet prepared by the invention can realize continuous and stable constant-speed release of drugs. After a patient takes the medicine, the medicine in the medicine release layer cannot be released immediately, and the tablet can rhythmically release the medicine, maintain the steady-state blood concentration, delay the peak time and prolong the half-life period of the medicine within more than ten subsequent hours under the action of the pushing layer, so that the bioavailability is improved, and the slow release effect of more than 12 hours is achieved. Due to the adoption of a double-layer osmotic pump controlled release technology, compared with a single-layer tablet, the double-layer osmotic pump controlled release tablet has the advantages of stronger controllability, more complete release and higher availability.

The present disclosure relates to a methimazole pulvis or powder and a preparation method therefor. By means of combining a solid dispersion technique with a micronization modification and secondary crushing process, a drug powder with a high dispersity is prepared, so that the specific surface area of the drug is increased, the dissolution rate of the drug is increased, the absorption rate is increased, and the bioavailability is improved. Other sweetening agents are also added to a preparation, a methimazole pulvis or powder which can be directly administrated and completely covers the bitter taste and the peculiar smell of the drug is prepared, and the drug can be administrated without water.

A composition contains a BCS Class II or IV drug that is acid-base solubilized with a pharmaceutically acceptable acid, and which is complexed with β-cyclodextrin. The β-cyclodextrin complexed drug exhibits enhanced bioavailability. The drug may be formulated for oral administration and / or to exhibit rapid release when administered. Preferable compositions may contain no crosslinked or polymerized non-active components.

Solid lipid nanoparticles (SLNs) for delivery of bioactive compounds are disclosed. The SLNs comprise a lipid matrix and surfactant layer encapsulating at least one bioactive compound selected from vitamins, minerals, enzymes, algae-derived bioactives, proteins, peptides, amino acids, antioxidants, small synthetic molecules, plant-derived volatile compounds, or botanical extracts. The SLNs exhibit submicron particle size, low polydispersity, and sufficient surface charge to ensure colloidal stability and efficient delivery. In one embodiment, algae-based bioactives, such as phycocyanin or fucoxanthin, are encapsulated using only natural and sustainable lipids and surfactants to improve bioavailability and support environmentally friendly formulations. The SLNs may be formulated for oral, topical, transdermal, injectable, ophthalmic, mucosal, textile, veterinary, or agricultural administration. Applications include human and animal health, functional foods, skincare, nutrient supplementation, and crop treatment. The disclosed SLNs offer a biocompatible and scalable delivery system that protects sensitive compounds, enables sustained release, and enhances absorption across diverse industries.

Aspects of disclosure relate to a composition and methodology for treating menopause symptoms utilizing a cannabinoid-based nanoplatform composition. The composition includes phytocannabinoids like CBD, CBG, and CBN, alongside isoflavones and polyphenols, all integrated into nanoplatform designed for enhanced bioavailability and controlled release. The formulation is designed to alleviate key menopause-related issues, including vasomotor symptoms (VMS), genitourinary syndrome of menopause (GSM), bone loss, mood disturbances, and sleep disorders, while addressing cardiovascular disease (CVD) risks. The composition combines cannabinoids, such as CBD, with isoflavones and polyphenols, and is incorporated into nanoplatforms for enhanced delivery and efficacy. Additionally, the disclosure includes a kit comprising oral capsules, intravaginal ovules, and instructions for use. The capsules contain a blend of cannabinoids, flavonoids, and polyphenols, while the ovules are composed of CBD and cocoa butter. The kit provides a comprehensive solution for managing menopause symptoms and mitigating cardiovascular risks.

We are disclosing derivatives of 5-hydroxylated polymethoxyflavones. The derivatives offer enhanced oral bioavailability and improved intestinal permeability. The derivatives of the invention release the biologically active 5-hydroxylated polymethoxyflavones that are activated by chemical or enzymatic processes in the GI Tract. The derivatives are constructed as bioreversible prodrugs containing the bioactive molecules covalently linked with lipids like fatty acids, glycerides or phospholipids. The derivatives are useful against inflammatory conditions and aging. Formulations including the derivatives are also disclosed.

The invention relates to a portable traditional Chinese medicine drenching and soaking rapidly disintegrated and mixed effervescent tablet and a preparation method thereof, and belongs to the technical field of traditional Chinese medicine preparations. The invention provides an effervescent tablet for treating eczematous dermatitis. The effervescent tablet is prepared from the following components in parts by mass: 10 to 40 parts of extract powder, 20 to 30 parts of citric acid, 15 to 25 parts of sodium bicarbonate, 1 to 3 parts of polyvinylpyrrolidone absolute ethyl alcohol solution, 1 to 9 parts of polyethylene glycol 6000, 15 to 30 parts of lactose and 3 to 7 parts of sodium carboxymethyl cellulose. The effervescent tablet obtained by the preparation method is convenient to use, convenient to carry and store, short in disintegration time, proper in pH value, large in foaming amount, smooth in appearance and clear in solution after disintegration, and the superfine powder for preparing the extract powder can improve the drug wall breaking rate, promote dissolution of effective components, improve the bioavailability and the treatment effect, improve the resource utilization rate and reduce the production cost. The invention provides a brand new dosage form of external medicine for treating eczematous dermatitis.

The invention discloses a multi-system function regeneration factor composition as well as a preparation method and application thereof. The multi-system function regeneration factor composition is prepared from the following components in parts by mass: 0.8 to 2.4 parts of melatonin, 84 to 126 parts of nicotinamide ribose and 42 to 84 parts of resveratrol. According to the multi-system functional regeneration factor composition disclosed by the invention, through scientific proportioning and synergistic effect of melatonin, nicotinamide ribose and resveratrol, the functions of stem cells are strongly activated, proliferation of the stem cells is remarkably promoted, the stemness maintaining capability of the stem cells is improved, osteogenesis and adipogenesis differentiation potential is enhanced, and the regeneration effect of the stem cells is improved. Meanwhile, an NAD < + > metabolic pathway is activated so as to strengthen cell energy and anti-aging capability. The capsule adopts the design of combining quick-release pellets and sustained-release pellets, the quick-release part can quickly release melatonin, the local drug concentration can be increased in a short time, and stem cell activation signals can be quickly started; and the sustained release part slowly releases nicotinamide ribose and resveratrol to maintain the long-acting stability of the drug concentration, so that the effect taking speed is ensured, the action time is prolonged, and the bioavailability is greatly improved.

The present application relates to a kind of bone repair compositions and its preparation method, belong to biological medicine technical field, pharmaceutical composition includes acid anhydride bovine beta-lactoglobulin peptide, casein phosphopeptide, yak bone peptide, loquat leaf extract, pterostilbene, honeysuckle chlorogenic acid and cyperus rotundus extract;Acid anhydride bovine beta-lactoglobulin peptide is prepared using special enzymolysis method.Acid anhydride bovine beta-lactoglobulin peptide, casein phosphopeptide and yak bone peptide are loaded using carboxymethyl chitosan-hydroxyapatite composite microspheres, then using sodium alginate-sodium carboxymethyl cellulose containing loquat leaf extract, pterostilbene, honeysuckle chlorogenic acid and cyperus rotundus extract one coating, then using sodium alginate-sodium carboxymethyl cellulose secondary coating.The present application develops high-efficiency pharmaceutical combination component, using polymer material to coat drug to form sustained-release system, improve bioavailability, using granular carrier to increase the stability and solubility of drug, promote intestinal absorption, improve bone repair process.

The present invention relates to a protein tyrosine kinase inhibitor and an ophthalmic preparation thereof. The protein tyrosine kinase inhibitor not only effectively antagonizes the activity of a VEGFR receptor tyrosine kinase, but also improves the pharmacokinetic properties thereof, while exhibiting high selectivity in inhibiting the activity of an "off-target" EGFR tyrosine kinase, thereby reducing or avoiding side effects, particularly those affecting the eyes. The preparation can greatly improve the solubility of the protein tyrosine kinase inhibitor compound, prolong the residence time of the compound on the ocular surface, increase exposure in fundus tissue, and improve the bioavailability.

The present application belongs to the technical field of oral solid preparation, and particularly relates to a mosapride citrate orally disintegrating tablet and a preparation method thereof. Raw and auxiliary materials comprise mosapride citrate, a filling agent, a disintegrating agent, a glidant, a lubricant and a flavoring agent. The present application screens and optimizes the auxiliary material formula, adopts dry granulation, optimizes the preparation process, improves the compressibility and fluidity of the material, saves energy, improves the production quality and stability, makes the prepared orally disintegrating tablet disintegrate rapidly, has excellent taste, greatly improves the medication compliance of patients, simultaneously improves the drug dissolution and improves the bioavailability. In addition, compared with other types of solid oral preparations of the product, the mosapride citrate orally disintegrating tablet is particularly suitable for the elderly and patients with difficulty in swallowing, and provides convenience in special and urgent situations such as lack of drinking water for taking medicine.

A composition for enhanced bioavailability of curcumin comprising a curcuminoid mixture and an essential oil of turmeric, wherein the curcuminoid mixture comprises a curcumin-keto compound, a curcumin-enol compound, a bisdemethoxycurcumin, a demethoxycurcumin, wherein a weight ratio of the curcumin-keto compound to the curcumin-enol compound ranges from about 0.12 - 0.20 : 0.8 - 0.88. A composition for enhanced lymphatic bioavailability of curcumin comprising a curcuminoid mixture and an essential oil of turmeric, wherein the curcuminoid mixture comprises a curcumin-keto compound, a curcumin-enol compound, a bisdemethoxycurcumin, a demethoxycurcumin, wherein a weight ratio of the curcumin-keto compound to the curcumin-enol compound ranges from about 0.12 - 0.20 : 0.8 - 0.88. Methods for making the composition for enhanced bioavailability of curcumin. Methods for making the composition for enhanced lymphatic bioavailability of curcumin.

The invention belongs to the technical field of fungal keratitis medicines. The invention provides application of cyclic adenosine monophosphate and metal salt thereof in preparation of an external product for preventing or treating fungal keratitis, aiming at the problems of poor permeability, low solubility, low bioavailability and possibility of generating toxic and side effects on cornea after long-term use of a clinically common local antifungal drug for treating fungal keratitis. As an antifungal active molecule for external administration, the cAMP has good water solubility, corneal permeability, broad-spectrum antifungal activity and biological safety. Compared with a traditional antifungal drug, the cAMP can be efficiently delivered to a cornea infection part and directly acts on pathogenic fungi by virtue of excellent water solubility and cornea permeability, so that the toxic and side effects on cornea tissues are reduced, and meanwhile, the bioavailability is improved. The cAMP shows good antifungal activity when the pH (Potential of Hydrogen) value is in a range of 4 to 7.5.

The present invention relates to a propranolol hydrochloride sustained release tablet, the sustained release tablet is prepared by filling a 3D printing shell with a 3D printing propranolol hydrochloride tablet core, and the tablet core contains 5-20% by weight of propranolol hydrochloride, 35-50% by weight of a lipid material, 20-35% by weight of a filler and 15-25% by weight of a plasticizer. The propranolol hydrochloride sustained-release tablet with the core-shell structure is prepared by filling the 3D printing shell with the 3D printing propranolol hydrochloride tablet core for the first time, medicine release is precisely regulated and controlled, precise administration is realized, plasma concentration release is stable, and bioavailability, medication safety and effectiveness and medication compliance are remarkably improved.

The invention discloses a five-ingredient meconopsis Tibetan medicine composition as well as a preparation method and application thereof, and relates to the technical field of medicines, the five-ingredient meconopsis Tibetan medicine composition is prepared from the following raw material components in parts by mass: 80-120 parts of meconopsis, 30-70 parts of tabasheer, 80-120 parts of safflower, 80-120 parts of emblic leafflower fruit and 5-15 parts of saffron. The five-ingredient concentrated pill provided by the invention is prepared by adopting a new dosage form, a dosage form compared with a 25-ingredient meconopsis meconopsis pill is changed into the concentrated pill from a watered pill, and the pill is prepared by extracting and concentrating part of medicinal materials, so that the concentration of effective components of the concentrated pill is improved, the bioavailability is good, and the drug effect is improved; the concentrated pill is small in size, small in taking dosage, relatively concentrated in effective components and less in impurities; in the aspect of storage, the concentrated pill is more stable than a water pill and is convenient to carry and store.

An antifungal solution, a preparation method and use thereof are provided, belonging to the technical field of medicine. The antifungal solution includes an antifungal drug and a solvent as raw materials; where the antifungal drug and the solvent are at a mass ratio of (0.1-1):(18-318); and the solvent includes an ionic liquid, an alcohol organic solvent, and water. The ionic liquid has excellent solubility, skin penetration-promoting performance, and antifungal effect; the water can destroy an original polar network of the ionic liquid, forming smaller soluble ion groups, which greatly increase a miscibility window; the alcohol organic solvent can form a cosolvent with the ionic liquid and the water, thereby helping miscibility. The antifungal solution can ensure that the drug in a system is maintained in a dissolved state, thereby improving bioavailability and ensuring better therapeutic effects while reducing dosage.

The invention features methods for the treatment of cystinosis and other cysteamine sensitive disorders in a subject including administration of a disulfide convertible to cysteamine in vivo. The methods can include the separate administration of a reducing agent to the subject to increase the bioavailablity and extend the plasma pharmacokinetic profile of the cysteamine produced following administration of the disulfide. The methods permit sustained cysteamine plasma concentrations in a subject.

The invention relates to the technical field of medicine and functional food delivery, in particular to a high-stability lipidosome coating containing hydrogen molecules and active substances and a preparation method of the lipidosome coating. The core of the coating is lipidosome loaded with nano-bubble hydrogen-rich water and active substances, and the outer layer of the coating is formed by coating an edible high-barrier material. Generally, in the coating and the method, a physical barrier is constructed by utilizing the primary protection of the lipidosome on the active substance and the extremely high barrier property of the beewax or the hard candy film on the active substance, especially gas, so that the rapid dissipation of hydrogen molecules in the inner core lipidosome is effectively prevented, and the problem of stable storage of the hydrogen molecules in the wrapping substance is solved. The stability of the active ingredients is jointly improved. The liposome has targeting property, can realize intestinal targeted release and slow release effects of active substances and hydrogen molecules, and improves bioavailability. And finally, the product can be prepared into various forms such as microspheres, sugar capsules or wrappers and the like, and can be conveniently delivered and eaten as functional foods, health-care products or medicines and the like.

The invention provides a traditional Chinese medicine composition for preventing and treating cardiovascular and cerebrovascular diseases, which is based on differentiation treatment of cold and heat properties of medicinal materials and is integrated with a modern preparation technology to improve the efficacy. Cold medicinal materials are subjected to superfine grinding and subcritical CO2 blasting pretreatment, and multi-enzyme step-by-step fermentation and a dynamic water extraction technology are combined, so that dissolution of active ingredients is enhanced; warm medicinal materials are subjected to gradient ethanol extraction assisted by microwave-ultrasonic synergistic effect, so that the enrichment efficiency of thermosensitive components is optimized; the neutral medicinal materials are separated by adopting an acid-base adaptive separation method, and polysaccharide and flavonoid substances are selectively retained. The components are constructed into an inner-layer, middle-layer and outer-layer structure, so that the bioavailability and the multi-target synergistic effect can be remarkably improved, and the composition has a good effect in preventing and treating cardiovascular and cerebrovascular diseases.

A composition for enhanced bioavailability of curcumin comprising a curcuminoid mixture and an essential oil of turmeric, wherein the curcuminoid mixture comprises a curcumin-keto compound, a curcumin-enol compound, a bisdemethoxycurcumin, a demethoxycurcumin, wherein a weight ratio of the curcumin-keto compound to the curcumin-enol compound ranges from about 0.12 - 0.20 : 0.8 - 0.88. A composition for enhanced lymphatic bioavailability of curcumin comprising a curcuminoid mixture and an essential oil of turmeric, wherein the curcuminoid mixture comprises a curcumin-keto compound, a curcumin-enol compound, a bisdemethoxycurcumin, a demethoxycurcumin, wherein a weight ratio of the curcumin-keto compound to the curcumin-enol compound ranges from about 0.12 - 0.20 : 0.8 - 0.88. Methods for making the composition for enhanced bioavailability of curcumin. Methods for making the composition for enhanced lymphatic bioavailability of curcumin.

The invention relates to an formulation for cardiac support supplements and the method of its preparation by using molecular-level mixing technology. The method involves preparing molecular-level emulsions of alpha-lipoic acid, acetyl L-carnitine, and coenzyme Q10, followed by spray drying to produce a homogeneous powder premix. This approach ensures precise dosage control, enhanced bioavailability, and improved stability, making it a valuable advancement in the field of nutraceutical and pharmaceutical formulations.

The application belongs to the technical field of pharmaceutical chemistry, and provides a high-purity milrinone-nicotinic acid crystal, a preparation method thereof is simple in operation, a crystallization process is easy to control, and reproducibility is good. The prepared milrinone-nicotinic acid crystal has significantly enhanced stability and solubility compared with free base and crystal forms thereof, thereby being beneficial to storage, transportation and application in preparation of a preparation of a product, and having enhanced bioavailability and absorption performance.

The present application provides a transdermal patch containing donepezil. The transdermal patch comprises a backing layer, a drug-containing matrix layer, and a release layer, wherein the drug-containing matrix layer comprises donepezil or a pharmaceutically acceptable salt thereof, a pressure-sensitive adhesive, and a permeation enhancer group; and the permeation enhancer group comprises at least three of lauryl lactate, sorbitan laurate, triethyl citrate, propylene glycol, sorbitan monolaurate, and isopropyl myristate. The donepezil or the pharmaceutically acceptable salt thereof in the transdermal patch of the present application can maintain the blood concentration for a long time, can improve the permeation efficiency of the transdermal patch and the bioavailability, and can also improve the adhesion of the transdermal patch, thereby improving the use comfort of a patient.

The embodiment of the invention provides a buccal product and a preparation method thereof, the buccal product provided by the embodiment of the invention comprises a functional layer, the functional layer comprises active substances, a slow-release base material and a film-forming base material, the active substances comprise nicotine and nicotine salt, and at least part of nicotine is embedded in the slow-release base material; wherein the nicotine and the nicotine salt are compounded into an active substance, the nicotine salt can realize quick release, and the sustained-release base material is used for embedding the nicotine, so that the nicotine can be inhibited from volatilizing in the drying process and is gradually dissociated in saliva, long-acting sustained release is realized, the bioavailability is improved, the release rate of the active substance can be controlled, and the sustained-release effect of the nicotine is improved. Therefore, the effects of early-stage quick release and later-stage slow release are achieved, the volatilization loss after drying can be reduced, and the validity period is prolonged; therefore, the buccal product provided by the embodiment of the invention can effectively solve the problem that the active substances in the existing buccal product are easy to release too fast in the initial stage or insufficient in the later stage.