26 results about "Butylphthalide" patented technology

The invention discloses an aromatic alkylamine ferroptosis inhibitor based on a butylphthalide structure and a preparation method and application thereof. The chemical structural formula of the ferroptosis inhibitor is shown as a formula 1 or a formula 2. The ferroptosis inhibitor can inhibit ferroptosis caused by a ferroptosis inducer and can reduce the level of active oxygen in cells. Nerve injury caused by cerebral ischemia reperfusion can be relieved, and symptoms of neurological diseases such as Alzheimer's disease and Parkinson's disease can be relieved; compared with a ferroptosis inhibitor Ferrostatin-1, the aryl alkyl amine compound disclosed by the invention has better metabolic stability and is suitable for in-vivo drug effect evaluation. Therefore, the novel aryl alkyl amine compound provided by the invention has a very good application value in treatment of neurological diseases related to ferroptosis.

This invention discloses butylphthalide nanoparticles, comprising: a layered double hydroxide and butylphthalide, wherein the butylphthalide is loaded onto the layered double hydroxide. This invention also discloses a method for preparing the above-mentioned butylphthalide nanoparticles, comprising the following steps: mixing the layered double hydroxide, butylphthalide, and water, adsorbing, separating the solid and liquid phases, and drying to obtain butylphthalide nanoparticles. This invention further discloses the application of the above-mentioned butylphthalide nanoparticles in the preparation of drugs for treating acute renal ischemia-reperfusion injury. This invention also discloses a drug for treating acute renal ischemia-reperfusion injury, comprising: the above-mentioned butylphthalide nanoparticles and pharmaceutically acceptable excipients. The butylphthalide nanoparticles of this invention have high drug loading capacity, good stability, and can target and activate the PI3K-AKT signaling pathway, effectively inhibit HK-2 cell apoptosis and oxidative stress, restore mitochondrial function, and improve renal ischemia-reperfusion injury.

Disclosed are an aromatic alkylamine ferroptosis inhibitor based on a butylphthalide structure, a preparation method therefor, and an application thereof. The chemical structural formula of the ferroptosis inhibitor is as shown in formula (1) or formula (2). The ferroptosis inhibitor is capable of inhibiting ferroptosis caused by a ferroptosis inducer, and reduces the level of intracellular reactive oxygen species. The ferroptosis inhibitor reduces neurological damage caused by cerebral ischemia-reperfusion, and alleviates symptoms of neurological disorders such as Alzheimer's disease and Parkinson's disease. Compared to the ferroptosis inhibitor Ferrostatin-1, the arylalkylamine compound exhibits better metabolic stability and is suitable for in-vivo efficacy evaluation. Therefore, the novel arylalkylamine compound provided by the present invention demonstrates great application value in the treatment of ferroptosis-related neurological disorders.

The invention provides a method for extracting phthalide chemical components in angelica sinensis, which comprises the following steps of: firstly, shearing and emulsifying the angelica sinensis at a high speed, carrying out high-speed shearing and extraction by using petroleum ether and ethyl acetate as extraction solvents, and recovering the solvents from the extract under reduced pressure through a rotary evaporator to obtain angelica sinensis essential oil; wherein the extracted essential oil contains senkyunolide A, ligustilide and butylphthalide. Aiming at the characteristics that the phthalide component in the angelica volatile oil is thermally unstable and is easy to oxidize, the phthalide component in the angelica volatile oil can be rapidly extracted under a low-temperature condition by combining a petroleum ether-ethyl acetate solution system with a high-speed shearing, dispersing and emulsifying technology, and the activity of the angelica volatile oil can be better maintained. The method has the characteristics of low temperature, simplicity in operation, short time and low cost.

The invention belongs to the technical field of biological medicine preparation, and particularly discloses a preparation method of a curcumin-butylphthalide-phospholipid complex, which comprises the following steps: dissolving curcumin, butylphthalide and lecithin in an organic solvent A, carrying out mixed reaction in a water bath, removing the organic solvent A after the mixed reaction is finished, and purifying by adopting an organic solvent B to obtain the curcumin-butylphthalide-phospholipid complex. And removing the organic solvent B, so as to obtain the curcumin synergistic butylphthalide phospholipid compound. The invention relates to a preparation method of nanoparticles of a curcumin synergistic butylphthalide phospholipid compound, which comprises the following steps: dissolving the curcumin synergistic butylphthalide phospholipid compound in deionized water, oscillating in a water bath to fully dissolve, and filtering through a microfiltration membrane to obtain the nanoparticles of the curcumin synergistic butylphthalide phospholipid compound. Through the synergistic effect of curcumin and butylphthalide, the treatment effect on nervous system diseases is remarkably improved, and a new thought and strategy are provided for treatment of nervous system diseases.

The application provides a triazole compound for protecting brain tissue and a preparation method thereof, and belongs to the technical field of biological medicines, and provides a triazole compound as shown in formula (I) and chiral isomers, enantiomers, diastereoisomers, geometric isomers, free forms or pharmaceutically acceptable salts, hydrates, solvates or esters thereof; and also provides a preparation method thereof; compared with the prior art, the application combines the internal ester ring-opening product of butylphthalide and ligustrazine through triazole to synthesize a novel triazole compound which can be used for protecting brain tissue; the preparation method of the triazole compound is simple and the raw materials are easy to obtain; the triazole compound has better biological activity and brain tissue protection effect than butylphthalide / ligustrazine, and has significant protection activity on a SH-SY5Y cell damage model.

The present invention relates to a butylphthalide dimer and a preparation method and application thereof, and the structural formula thereof is as follows: The present invention isolates butylphthalide dimer enantiomers from Lycopodiella vulgaris. The neuroprotective effect of the compound of the present invention is evaluated in a glutamate-induced neuronal cell HT-22 injury model. In particular, (-)-(6S,7R,6'R,7'S)-lycocasuarolide B(-)-2 exhibits significant neuroprotective activity in the model. At concentrations of 5μM, 10μM, 15μM, and 20μM, the cell survival rates are increased by 29.3%, 25.45%, 21.96%, and 21.57%, respectively, which is equivalent to the activity of the positive control drug 3-n-Butylphthalide. Compound (-)-2 can alleviate glutamate-induced neuronal cell death by inhibiting the apoptosis pathway.

The application provides a butylphthalide sublingual tablet and a preparation method thereof, wherein the butylphthalide sublingual tablet contains the following components by weight percentage based on 100% of the total weight of the butylphthalide sublingual tablet: 10%-25% of an active substance, 10%-40% of an emulsifier, 10%-75% of an excipient, 0.2%-2% of a binder, 1%-30% of a sweetening agent, and 0.1%-2% of a fragrance agent; and the active substance is butylphthalide or a butylphthalide derivative. The application does not need to add a disintegrating agent, the auxiliary materials used are water-soluble, and the amount is small, so that the preparation can be rapidly disintegrated in the oral cavity without grit feeling, thereby overcoming the slow disintegration in the oral cavity and grit feeling of the oral disintegration tablet prepared by using a direct compression method.

The invention relates to oily butylphthalide gel for treating traumatic brain injury as well as a preparation method and application of the oily butylphthalide gel. The preparation method of the oily butylphthalide gel comprises the following steps: mixing a proper amount of ethyl isobutyl sucrose ester (SAIB) and butylphthalide, adding a small amount of pure water, and violently shaking to obtain the oily butylphthalide gel. Experimental results show that the oily butylphthalide gel prepared by the method has modulus which is very matched with that of brain tissues and is beneficial to tissue regeneration. Therefore, the oily butylphthalide gel disclosed by the invention has an excellent effect of treating traumatic encephalopathy.

The invention designs a compound with a novel structure, and provides a new direction for the development of PSD-95 inhibitors and butylphthalide drugs. Test results show that the compound can quickly release the PSD-95 inhibitor compound and butylphthalide, almost all of the compound are hydrolyzed into the PSD-95 inhibitor compound and butylphthalide, few other metabolites are generated, and the compound has good in-vivo pharmacokinetics and has patent medicine potential.

The invention belongs to the technical field of medicines, and particularly relates to a butylphthalide injection and a preparation method thereof. The butylphthalide injection comprises butylphthalide, polyvinylpyrrolidone, a stabilizer, a pH regulator, an osmotic pressure regulator and water for injection. The stabilizer is selected from one or more of succinyl gelatin, polygelatin peptide and hydrolyzed gelatin. According to the butylphthalide injection prepared by the invention, cyclodextrin and other antioxidants and stabilizers are completely abandoned, so that the safety is improved, and the clinical use requirements are met.

The application relates to the field of drug chemical synthesis, in particular to a synthesis process of a butylphthalide derivative. The synthesis method of the butylphthalide derivative comprises the following steps: butylphthalide and lithium aluminum hydride are mixed in tetrahydrofuran, reacted with tert-butyl dimethyl chlorosilane, then reacted with acid and tetrabutylammonium fluoride trihydrate, esterified with 2-morinol or a derivative thereof after oxidation, and purified to obtain the butylphthalide derivative. The synthesis method has the characteristics of mild conditions, simple operation, fewer side reactions, high selectivity, better industrial adaptability of the prepared butylphthalide derivative, and high purity of the finished product.

The invention relates to butylphthalide hydrogel for treating traumatic brain injury as well as a preparation method and application of the butylphthalide hydrogel. The preparation method of the hydrogel comprises the following steps: step 1, taking a proper amount of butylphthalide injection, and adding a proper amount of multi-arm polyethylene glycol with a double-bond end group into the butylphthalide injection to form a solution containing the multi-arm polyethylene glycol with the double-bond end group and the butylphthalide; 2, taking a proper amount of butylphthalide injection, and adding a proper amount of the polysulfhydryl compound to form a solution containing the polysulfhydryl compound and butylphthalide; and step 3, mixing the solutions prepared in the step 1 and the step 2 to prepare the hydrogel. Experimental results show that the butylphthalide hydrogel prepared by the method disclosed by the invention can be continuously released in a slow-first and fast-second manner within several weeks, and the release property is matched with pathological change characteristics of traumatic brain injury. Therefore, the butylphthalide hydrogel disclosed by the invention has an excellent effect of treating traumatic encephalopathy.

The invention relates to a pharmaceutical composition for oral mucosa delivery, a pharmaceutical preparation and application of the pharmaceutical composition and the pharmaceutical preparation. The pharmaceutical composition for delivery through the oral mucosa comprises the following components in parts by weight: 5-40 parts of a pharmaceutical active ingredient and 5-90 parts of a functional oil matrix, wherein the active pharmaceutical ingredient comprises one or more of butylphthalide and a butylphthalide derivative; the functional oil matrix comprises one or more of fatty acid esters.

The invention discloses application of butylphthalide in preparation of a medicine for preventing and treating obesity-related acute pancreatitis, and belongs to the technical field of medicines. The invention discloses application of butylphthalide in treatment of obesity-related acute pancreatitis. Pancreatic necrosis, systemic inflammation and distant organ injury caused by obesity-related acute pancreatitis can be remarkably improved. Wherein after intervention of butylphthalide, pathological scores of lung, kidney and pancreas are obviously reduced by 73.08%, 70.00% and 59.26%; the expression level of the pancreatitis marker is obviously reduced and is reduced by 53.80% compared with that of a model group; the expression levels of proinflammatory factors IL-1beta, IL-6 and TNF-alpha in serum are obviously reduced, and are respectively reduced by 69.45%, 78.80% and 67.64% compared with a model group.

The invention discloses a pharmaceutical composition and application thereof, the pharmaceutical composition comprises butylphthalide and Ceridutinib, and the mass ratio of butylphthalide to Ceridutinib is (1000: 1)-(1: 1000). The pharmaceutical composition disclosed by the invention has a good effect on treating cerebrovascular diseases, butylphthalide and Ceridutinib show a synergistic effect, an excellent curative effect is favorably obtained, the dosage of the medicine is reduced, and the clinical medication safety is favorably improved.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a butylphthalide solid drug release system, a preparation method thereof and a pharmaceutical preparation. The butylphthalide solid drug release system comprises the following components: a microemulsion and an adsorption carrier, the microemulsion comprises butylphthalide and an emulsifier system, preferably, the emulsifier system comprises an emulsifier and a co-emulsifier. The obtained butylphthalide solid self-microemulsion has the advantages of good emulsifying capacity of liquid self-microemulsion and good stability of a solid preparation, has a very good drug solubilizing effect, can improve the probability that a drug is absorbed by gastrointestinal tracts in a dissolved state, improves the oral bioavailability of butylphthalide, and further improves the drug effect; moreover, the solid self-microemulsion is good in stability and low in toxicity, liquid medicine solidification is achieved, and the problem that a liquid preparation is inconvenient to transport, store and take is solved.

This invention belongs to the field of chemical pharmaceutical technology, specifically disclosing a method for preparing butylphthalide. In the method provided by this invention, crude 2-(α-hydroxypentyl)benzoic acid, obtained by the condensation reaction of o-formylbenzoic acid and an organometallic reagent, is subjected to alkali treatment, and the pH is adjusted to 3.8-4. The crude 2-(α-hydroxypentyl)benzoic acid is then separated and purified to obtain 2-(α-hydroxypentyl)benzoic acid and a filtrate. The pH of the filtrate is adjusted to 1.8-2, and o-formylbenzoic acid is separated and purified. The o-formylbenzoic acid is then used in the above condensation reaction to perform a ring-closing reaction on 2-(α-hydroxypentyl)benzoic acid, yielding butylphthalide. This invention, through reasonable experimental process design, provides a method for preparing butylphthalide with high yield, high purity, low energy consumption, and a simple process.

The present application relates to a butylphthalide impurity compound, a preparation method and use thereof. The impurity compound of the present application is similar to butylphthalide in structure, but has no significant effect on the secretion of TNF-alpha of LPS-induced mouse primary microglial cells; instead, the impurity compound has significant neurotoxicity on mouse brain neuroblastoma cell line (Neuro-2a), and can significantly inhibit the length of Neuro-2a nerve cell axon and the number of cells with axon. The content of peroxidized impurities has an effect on the treatment of butylphthalide composition on nerve function damage of tMCAO model rats, and the higher the content of peroxidized impurities, the greater the degree of nerve function damage. Limiting the impurity compound of the present application in the quality control of butylphthalide is beneficial to the quality control of butylphthalide drugs, and can ensure the effectiveness, safety and quality control of the drugs.

This invention relates to a butylphthalide cationic nanoemulsion, its preparation method, and its application, belonging to the field of pharmaceutical technology. The butylphthalide cationic nanoemulsion comprises an oil phase, an aqueous phase, butylphthalide, an emulsifier, a co-emulsifier, an osmotic pressure regulator, and a cationic surfactant. The butylphthalide content in the nanoemulsion is 0.30%–2.50% by mass. The average particle size of the butylphthalide cationic nanoemulsion is 80–200 nm, the polydispersity index is 0.070–0.200, and the zeta potential is 20–30 mV. This invention solves the problems of poor water solubility and low stability of butylphthalide by preparing it into a nanoemulsion formulation; furthermore, by administering it via nasal administration, it meets the need for rapid neuroprotection in ischemic stroke.

This invention discloses a platelet-loaded bio-nanomedicine containing ginkgolide and butylphthalide, its preparation method, and its application, relating to the field of pharmaceutical formulation technology. The bio-nanomedicine comprises an active ingredient, a core drug carrier, a biological shell, and a target-seeking peptide. The active ingredient includes at least ginkgolide B and butylphthalide. The core drug carrier includes a lipid carrier, and the target-seeking peptide is a CITP peptide. The mass ratio of the active ingredient to the core drug carrier is 1:5 to 1:10. The amino acid sequence of the CITP peptide is PHSSHIGTTEIGKL. The biological shell includes at least one of platelet membrane and exosome membrane. The bio-nanomedicine of this invention exhibits good targeting and therapeutic efficacy, providing a new approach for the treatment of thrombotic diseases.

The application discloses a sulfide prodrug combination based on butylphthalide as a carrier, which has the structure shown in the following formula I. The butylphthalide prodrug can increase the curative effect of drugs and reduce the toxic side effects.

The application discloses a kind of pharmaceutical composition and its application, the pharmaceutical composition includes butylphthalide and sedutin, the mass ratio of butylphthalide and sedutin is 1000:1~1:1000.The effect of the pharmaceutical composition of the application in treating cerebrovascular disease is good, butylphthalide and sedutin show synergistic effect, which helps to obtain excellent curative effect, and reduce drug dosage, which helps to improve the safety of clinical drug use.

This invention provides an environmentally friendly method for preparing the active pharmaceutical ingredient butylphthalide. Using butylphthalide as a raw material and water as a solvent, the active pharmaceutical ingredient butylphthalide is prepared in a simple, environmentally friendly one-pot process via hydrolysis with sodium hydroxide solution, acidification with sulfuric acid solution, and reductive lactone formation catalyzed by an iridium catalyst. After simple extraction, drying, and concentration, a product with a purity greater than 99% according to 1H NMR spectroscopy and a yield greater than 90% is obtained. The synthetic method provided by this invention features concise reaction conditions and steps, simple operation, is environmentally friendly, has high synthesis efficiency, and facilitates separation and purification. It has promising industrial applications and plays a positive role in organic synthesis, pharmaceutical production, and fine chemicals.

The invention provides a brain-targeted delivery system. The brain-targeted delivery system comprises mesoporous Prussian blue nano-enzyme serving as a drug carrier and an erythrocyte membrane wrapping the surface of the drug carrier, the erythrocyte membrane is modified by rabies virus glycoprotein polypeptide. The invention further provides a medicine which further comprises an active substance loaded on the medicine carrier, and the active substance comprises at least one of L-arginine and butylphthalide. When the brain-targeted delivery system is used for synergistically treating cerebral arterial thrombosis, the immune escape ability is remarkably enhanced, the brain-targeted efficiency is improved by more than 10 times compared with that of unmodified nanoparticles, and the retention time in the brain is more than or equal to 24 hours.

The invention relates to a pharmaceutical composition containing butylphthalide and a preparation method thereof, the pharmaceutical composition is composed of butylphthalide and a derivative of butylphthalide, and the derivative of butylphthalide comprises hydroxyl butylphthalide and optionally comprises one or more of butylene phthalide and propylphthalide. The pharmaceutical composition can be used for treating mild and moderate acute ischemic cerebral apoplexy, is stable in quality, remarkably improves side effects such as anorexia caused by abdominal discomfort, and can improve the clinical curative effect and medication safety of a butylphthalide preparation.