221 results about "Enhanced bioavailability" patented technology

The invention discloses pulsatilla saponin B4-oleanolic acid self-assembled nanoparticles as well as preparation and application thereof, and relates to the technical field of pharmaceutical preparations. Inspired by compatibility and solubilization of traditional Chinese medicines, the pulsatilla saponin B4-oleanolic acid self-assembled nanoparticles (AB4-OA NPs) are prepared by taking natural active components, namely micromolecular pulsatilla saponin B4 and oleanolic acid, as raw materials; the oleanolic acid has the effects of promoting dissolution and resisting inflammation, the water solubility of the oleanolic acid is improved, the bioavailability is improved, and the anti-inflammatory effect of the oleanolic acid is enhanced. Experimental results show that the AB4-OA NPs can effectively improve the dissolution rate of the oleanolic acid, so that the bioavailability of the oleanolic acid is effectively improved, meanwhile, the AB4-OA NPs has a better anti-inflammatory effect, and the effect is better than that of a single drug with the same dosage. In addition, the synthetic preparation method is simple and convenient, has the advantages of nano-scale drugs, realizes auxiliary-material-free pure drug self-delivery, and improves the delivery efficiency.

Several embodiments pertain to nanoparticle-based compositions and their use in methods for the delivery of active agents to subjects and to products. In several embodiments, the compositions are stable for prolonged periods of time and under hot conditions and provide enhanced bioavailability and / or dispersibility.

Novel compounds such as DHMP maintain DHM features and pharmacological activities with increased potency and efficacy, improved water solubility, enhanced bioavailability, increased permeability to the blood brain barrier (BBB), and increased stability. Because DHMP retains the therapeutic activities of DHM and has properties that improve its bioavailability, it can be used as a therapeutic agent for treating Alzheimer's disease-related diseases (ADRD) including Alzheimer's disease (AD), Vascular Dementia, Frontotemporal Dementia (FTD), Mixed Dementia as well as neurodegeneration such as Parkinson's disease. Administration of these compounds result in beneficial pathological changes including reduction of Aꞵ and Tau, improvement of neuroinflammation, reduction of cognitive / memory deficits, as well as improvement of anxiety, depression, and aggression. The disclosed DHM derivatives can also be used to treat sleep disorders, neurological disorders such as PTSD, Autism, Epilepsy / Seizures, and Alcohol Use Disorders (AUD), fetal alcohol syndrome (FAD), substance addictions, and cancers.

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.

The invention belongs to the technical field of biological medicines, and particularly relates to sodium pyruvate sustained-release gel nanoparticles based on redox response as well as a preparation method and application of the sodium pyruvate sustained-release gel nanoparticles. The preparation method comprises the following steps: adding modified gellan gum containing sulfydryl and catechol groups, phenylboronic acid modified gellan gum and sodium pyruvate into water to obtain a mixed solution; under the protection of inert gas, divalent metal salt and potassium persulfate are added into the mixed solution, stirring is performed for 3-5 h, after the reaction is finished, centrifugation is performed, precipitates are collected, washed and dried, and the composite material is obtained. Experimental results show that the sodium pyruvate sustained-release gel nanoparticles prepared by the invention can realize controlled release of drugs, reduce toxic and side effects caused by burst release of the drugs, improve the curative effect of the drugs and improve the bioavailability.

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.

The present invention relates to the technical field of diabetes, and in particular to a controlled-release diabetic wound healing promoting treatment method, comprising the following treatment experimental steps: step S1: preparation of Hst1@PNPs; step S2: Coomassie brilliant blue staining; step S3: scanning and transmission electron microscopy detection; in the present invention, a slow-release Hst1 treatment method is constructed by encapsulating Hst1 into platelet membrane vesicles derived from autologous blood. On the one hand, the PNPs encapsulate the linear Hst1 peptide structure to prevent it from being rapidly degraded by high proteases in diabetic wound exudate, thereby improving bioavailability. On the other hand, the PNPs can adsorb excess LPS in the wound exudate, and cooperate with Hst1 to achieve anti-inflammatory and anti-oxidative stress effects. Subsequent cell and animal experiments further confirmed that Hst1@PNPs have the effects of anti-inflammatory, scavenging ROS, promoting re-epithelialization, collagen deposition and angiogenesis, thereby promoting diabetic wound healing.

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.

The invention provides a propolis soft capsule which comprises a soft capsule shell and a content wrapped in the soft capsule shell, and the content comprises 400-750 g of propolis extract, 2000-2400 g of vegetable oil, 1000-1400 g of modified starch, 75-100 g of tea seed oil, 50-100 g of natural antioxidant and 75-125 g of cellulose on the basis of 10000 propolis soft capsules. One of the purposes of the invention is to provide the propolis soft capsule and the production process thereof, and by optimizing the formula and the production process of the propolis soft capsule, the purposes of improving the bioavailability, enhancing the stability of the product, improving the mouth feel, improving the safety of the product and improving the environmental friendliness of the product can be achieved on the premise of not influencing the active ingredients of the propolis.

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.

The present invention relates to the technical field of deep processing of tea, specifically to a preparation method of tea essences particles. The present invention provides a preparation method of tea essences particles, including a process of extraction, filtration and separation, purification and decontamination, activation of activity and improvement of bioavailability, and spray granulation, which enhances activity and bioavailability of the active ingredient of the tea essences, improves taste of the tea essences, and increases the product yield of the tea essences.

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 provides a fucoxanthin nano-emulsion preparation method, and relates to the technical field of biological medicine, fucoxanthin and medium chain triglyceride are used as raw materials to support an oil phase solvent, and the oil phase solvent is mixed with resistant dextrin, isomaltooligosacharide and fructo-oligosaccharide to prepare the fucoxanthin nano-emulsion. The oil-in-water fucoxanthin nano-emulsion with the particle size of 1-100nm is obtained by mixing water-phase solvents prepared from fucoxanthin, blood orange powder and the like, processing by a colloid mill and emulsifying and shearing by a vacuum tank, and the preparation increases the solubility of fucoxanthin, removes the unpleasant odor of fucoxanthin, reduces degradation of gastrointestinal tracts, improves the bioavailability, reduces the toxic and side effects of the fucoxanthin, improves the bioavailability of the fucoxanthin, and improves the bioavailability of the fucoxanthin. The controlled release and absorption of fucoxanthin are realized, and compared with traditional tablets and capsule products, the compliance of females, middle-aged people and old people who have difficulty in swallowing is greatly improved.

The invention discloses an ophthalmic micro-emulsion preparation of tacrolimus, an ophthalmic in-situ gel preparation of tacrolimus as well as a preparation method and application of the ophthalmic micro-emulsion preparation and the ophthalmic in-situ gel preparation of tacrolimus. The tacrolimus eye micro-emulsion preparation comprises tacrolimus, a solubilizer and water, and the solubilizer comprises stearic acid polyethylene glycol ester and caprylic / capric acid polyethylene glycol glyceride. The tacrolimus ophthalmic in-situ gel preparation is prepared from tacrolimus, a solubilizer, a gel matrix and water. The tacrolimus ophthalmic microemulsion preparation and the tacrolimus ophthalmic in-situ gel preparation both can improve the drug loading capacity of tacrolimus, so that the effective drug amount acting on an affected part is improved; according to the tacrolimus eye microemulsion preparation, the solubility of tacrolimus can be remarkably improved, and eye medicine absorption can be promoted; according to the tacrolimus ophthalmic in-situ gel preparation, the retention time of eyes can be prolonged, and the bioavailability can be effectively improved.

The invention discloses an allergy-progesterone nano preconcentrate and a preparation method and application thereof. The nano preconcentrate is made of the following raw materials in mass percentage: 0.5-2.5% allergy-progesterone; 15-29% ethyl oleate; 45-65% polyoxyethylene sorbitan monooleate; 15-30% ethyl carbitol; and 1-5% ethanol. The allergy-progesterone nano preconcentrate of the invention is easy to use and can be arbitrarily miscible with water, thereby solving the disadvantage that the traditional allergy-progesterone oil solution is immiscible with water; at the same time, it can promote the absorption of allergy-progesterone through lymphatic circulation and improve bioavailability. The bioavailability of the nano preconcentrate after oral absorption after hydration is 497% of that of the allergy-progesterone oil solution, thereby reducing the clinical dosage of allergy-progesterone or reducing the number of administrations, thereby alleviating stress on animals.

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 invention relates to a spherical crystal of a medicinal crystal form B of nilotinib hydrochloride and a preparation method of the spherical crystal. According to the method, nilotinib hydrochloride is used as a substrate, and a methanol-water binary solvent is used as a solvent system; the crystal form prepared by the method is uniform in particle size distribution and controllable in size, genotoxic impurities can be stably controlled below 3ppm, the inherent dissolution is obviously improved, and the bioavailability is favorably 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.