52 results about "Butylphthalide" patented technology

The invention belongs to the technical field of prevention and treatment of peanut southern blight, and particularly relates to a bactericidal composition for preventing and treating peanut southern blight. The invention relates to a sterilization composition. The effective component of the sterilization composition is formed by compounding butylphthalide and pyraclostrobin or tebuconazole according to the mass ratio of (1-150): (150-1). After the butylphthalide and the pyraclostrobin or the tebuconazole are compounded according to a certain mass ratio, the activity of the compounded formula is not simply superposed, but shows a very good synergistic effect. Compared with single pyraclostrobin or tebuconazole, the composition has the advantages that the prevention and treatment effect on the peanut southern blight can be improved, and on the basis, the dosage of medicaments can be reduced, and the environmental pollution can be reduced.

The invention provides an application of combination of indobufen and butylphthalide in preparation of a drug for preventing and / or treating cerebrovascular diseases, indobufen and butylphthalide are combined for use, have a synergistic effect, remarkably improve the treatment effect, can be used for preparing the drug for preventing, secondarily preventing or treating the cerebrovascular diseases, and has a wide application prospect. The medicine is especially suitable for treating cerebral apoplexy and transient ischemic attack, and can be used for prophylactically improving cerebral infarction caused by cerebral arterial thrombosis.

The invention provides a butylphthalide injection and a preparation method thereof, and relates to the technical field of medicines.The butylphthalide injection comprises butylphthalide, cholate, phospholipid and water for injection, the cholate is prepared through a reaction of cholic acid and sodium hydroxide; the molar ratio of the phospholipid to the cholic acid is (0.3-1.2): 1. The mass fraction of butylphthalide in the butylphthalide injection is 0.025%-1%, the butylphthalide, cholate and phospholipid are mixed and proportioned under the conditions of certain concentration and mass ratio and cholic acid and phospholipid in the cholate under the condition of certain molar ratio, and the butylphthalide injection of a clear solution is prepared; the preparation process of the butylphthalide injection is simple, the stability of the injection is further improved through repeated dissolving and stirring, clinical medication requirements are met, and industrial production is facilitated.

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.

Disclosed are a hydroxypentyl benzoic acid diester compound, a method preparing the same, and an application of the same. This application uses a combination principle, on the one hand, the medicine concentration of butylphthalide in cerebral vessels is improved through a function of promoting the medicine to penetrate through a blood-brain barrier of dexborneol, and a multi-target multi-channel synergistic brain protection effect of the medicine is exerted; on the other hand, the treatment effect of dexborneol on cerebral ischemia is exerted. Anti-cerebral ischemia in-vivo pharmacodynamic activity evaluation is carried out on the synthesized compound, a high-activity candidate medicine is obtained, and industrial production can be achieved through the synthesis method.

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.

The invention relates to the technical field of pharmaceutical analysis, and particularly discloses a detection method of butylphthalide related substances. A SUPELCOSILTML-DP chromatographic column is adopted to carry out liquid chromatographic analysis on a butylphthalide sample, accurate detection of sixteen related substances in butylphthalide and the content of the substances is achieved at the same time, separation of butylphthalide and impurities can be achieved, all impurity peaks do not interfere with a main peak, and all chromatographic peaks can be completely separated; the detection cost is low, the used mobile phase is simple, the preparation is convenient, and the time is saved. The detection method provided by the invention can meet the rapid detection of butylphthalide related substances, is high in accuracy and sensitivity and good in reproducibility and stability, can be used for quality control and comprehensive evaluation of butylphthalide, and provides reliable guarantee for improving and controlling the quality of butylphthalide.

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 present invention relates to a composition for prevention, improvement, or treatment of poor ovarian responders caused by aging, comprising butylphthalide or an acceptable salt thereof as an active ingredient, for which a statistically significant increase in the number and quality of mature oocytes was confirmed in 38- to 40-week-old mice (40 years old or older in humans) fed butylphthalide. Not only does the number of mature oocytes produced in the ovaries decrease in women as a result of aging, but also healthy mature oocytes (MII oocytes) decrease as a result thereof, thereby gradually reducing the possibility of pregnancy, but the active ingredient of the present invention may increase the number and quality of mature oocytes and thus has the effect of increasing the chances of pregnancy for older women. In addition, the present invention may inhibit a decrease in the number of primordial follicles caused by aging and thus has the effect of enabling the inhibition of diminished ovarian reserve caused by aging.

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 present invention relates to the technical field of pharmaceutical compositions, and in particular to a pharmaceutical composition for treating Alzheimer's disease and a preparation method thereof. Specifically, it is prepared from the following components by mass: 0.4-0.8 parts of butylphthalide, 0.3-0.7 parts of donepezil hydrochloride, 22-26 parts of ginkgo flavonoids, 30-40 parts of ginsenosides, 16-20 parts of gastrodia elata extract, 13-17 parts of codonopsis pilosula extract, 16-20 parts of raw dragon bone extract, 12-16 parts of calamus tatarinowii extract, 11-15 parts of astragalus extract, 10-16 parts of rhizoma anemarrhenae extract and 15-19 parts of trumpet creeper extract. The pharmaceutical composition provided by the present invention has an excellent effect in treating Alzheimer's disease, can cure patients with early Alzheimer's disease, can effectively alleviate their symptoms and prolong the life of patients with late Alzheimer's disease, and its therapeutic effect is significantly better than that of existing drugs.

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 provides a phthalide ring-opening derivative as shown in a formula (I-1) and a stereoisomer or pharmaceutically acceptable salt thereof and application thereof. Experimental results show that the compound disclosed by the invention has excellent pharmacokinetic properties, and the release of butylphthalide and dexcanthanol in vivo is superior to that of single drug butylphthalide and dexcanthanol and is also superior to that of a compound composition. The compound disclosed by the invention has an excellent brain protection effect and can greatly reduce the cerebral infarction area; the compound can be used for preventing and treating nerve injury, degenerative diseases and ischemic diseases. # imgabs0 #

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 present invention relates to a sterile injection of butylphthalide and a preparation method and use thereof, belonging to the technical field of pharmaceutical preparations, and mainly solves the problem that the impurity content increases after terminal sterilization when a butylphthalide raw material drug containing no organic acid impurities is dissolved by inclusion with hydroxypropyl beta-cyclodextrin to prepare an aqueous solution. The sterile injection of butylphthalide of the present invention comprises, by mass percentage, 0.02-0.03% butylphthalide, 0.5-0.8% cosolvent, 0.9% osmotic pressure regulator, an appropriate amount of pH regulator and an appropriate amount of solvent, wherein: the butylphthalide is butylphthalide prepared by a chemical synthesis method, the content of the butylphthalide is greater than 99.0%, and the butylphthalide does not contain organic acid impurities, the acid value is less than 0.5, and the pH of the butylphthalide injection is 4.5-5.5, preferably, the pH is 5.0-5.3, and more preferably, the pH is 5.1-5.2.

The present invention belongs to the field of pharmaceutical preparations, and particularly relates to a butylphthalide oral solution. The oral solution contains butylphthalide, hydroxypropyl-β-cyclodextrin and water, and is characterized in that the oral solution further comprises citric acid and / or citrate, and the mass ratio of butylphthalide, hydroxypropyl-β-cyclodextrin and water is 1:18-25:50-150. The butylphthalide oral solution of the present invention has stable quality, is safe and reliable, and has almost no pungent and throat-irritating feeling, and can be taken orally or by nasogastric feeding, solving the clinical pain points.

The invention provides an application of n-butylphthalide. According to the application, n-butylphthalide is used for providing a combination for inducing stem cells to differentiate into fat cells; the invention relates to an application of n-butylphthalide in preparation of a composition. The composition is used for inhibiting white fat accumulation, promoting white fat to be converted into brown fat, inhibiting weight gain, inhibiting obesity, reducing the liver fat content of an individual, reducing the fat content of liver cells, improving the antioxidant activity of the liver and / or reducing the content of triglyceride, glucose and total cholesterol in blood. The present invention relates to a pharmaceutical composition for preventing or treating obesity, preventing metabolic syndrome associated with obesity, preventing or treating fatty liver, improving liver lesion caused by fatty liver, and / or reducing liver damage in an individual, and to a use of n-butylphthalide in the manufacture of a pharmaceutical composition for preventing or treating obesity, preventing metabolic syndrome associated with obesity, preventing or treating fatty liver, and to a use of n-butylphthalide in the manufacture of a pharmaceutical composition for preventing or treating liver lesion caused by fatty liver.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a butylphthalide oral solution as well as a preparation method and application thereof. The present invention provides an oral solution comprising a therapeutically effective amount of butylphthalide and pharmaceutically acceptable excipients, the therapeutically effective amount being a single daily dose, the single daily dose reaching an average Cmax of from 1.2 ng / ml to 3.2 ng / ml for every 1 mg of butylphthalide after administration to a human subject, the single daily dose being 120 mg-160 mg. The butylphthalide oral solution disclosed by the invention is stable in curative effect and suitable for treating cerebral ischemic diseases including mild, moderate and severe acute ischemic cerebral apoplexy and the like.

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 the technical field of traditional Chinese medicine, and provides a pharmaceutical composition capable of preventing and treating headache and application thereof.The pharmaceutical composition is composed of ligusticum wallichii phthalide lactone extract and angelica dahurica coumarin extract which serve as effective components and pharmaceutically acceptable auxiliary materials or carriers, the weight ratio of the ligusticum wallichii phthalide lactone extract in terms of ligustilide to the radix angelicae coumarin extract in terms of imperatorin is 10: (1-10). The composition can enhance the effects of ligustilide and imperatorin which are known at present, can also achieve remarkable synergistic interaction and complementary effects in the aspect of the comprehensive effect of preventing and treating headache, can also avoid the loss and waste of senkyunolide A, butylphthalide and other more possible beneficial effective components, and has a good application prospect. The traditional Chinese medicine resources are fully and well utilized, and the production cost and the medicine price are remarkably reduced.

The present invention relates to a 2-pentanoylbenzonitrile reductase mutant and its use in preparing optically pure n-butylphthalide. Specifically, it relates to a 2-pentanoylbenzonitrile reductase mutant with improved activity, stability, and enantioselectivity, a gene encoding the 2-pentanoylbenzonitrile reductase mutant, a recombinant expression vector containing the gene sequence, and a recombinant expression transformant, as well as the use of the 2-pentanoylbenzonitrile reductase mutant as a catalyst for catalyzing the asymmetric reduction of 2-pentanoylbenzonitrile compounds, particularly catalyzing the asymmetric reduction of 2-pentanoylbenzonitrile to prepare optically pure n-butylphthalide (n-butylphthalide). Compared with the prior art, the present invention has the advantages of high enzymatic reaction substrate concentration, mild reaction conditions, environmental friendliness, high yield, and high product optical purity, and has good application prospects.

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 discloses a sulfide prodrug composition based on taking butylphthalide as a carrier, which has a structure as shown in the following formula I. The butylphthalide prodrug can improve the curative effect of the drug and reduce the toxic and side effects of the drug. # imgabs0 #

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.