41 results about "L-Hyoscyamine" patented technology

A pharmaceutical dosage form which comprises two or more different hyoscyamine formulations, at least one of the formulations being an immediate release hyoscyamine formulation and at least one other one being a controlled release hyoscyamine formulation. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.

The invention relates to the application of microwave and ultrasonic technologies in synthesizing tiotropium bromide anhydride, in particular to a method for preparing the refined product of a finished product, namely, tiotropium bromide anhydride through crystallization and recrystallization processes by using a crude product of tiotropium bromide prepared through bromization reaction after hydrolytic reaction of scopolamine hydrobromide under microwave function, substitution and coupling reaction of bromothiophene, magnesium, and oxalic acid dimethyl ester under the microwave function, and condensation reaction of scopine and thiophen methyl glycollate under the microwave function. Using the invention to prepare tiotropium bromide anhydride, not only the reaction time is short, the side reaction is less, and the yield rate is high in the room temperature condition, but also the product quality is stable, controllable, safe and effective.

The invention discloses a medical composition for treating piglet diarrhea, comprising the following raw materials in parts: 50-100 parts of neomycin sulfate, 10-50 parts of scopolamine methobromide, 100-150 parts of montmorillonite, 1-5 parts of VB1, 1-5 parts of VB2, 1-5 parts of VB6, 10-50 parts of nicotinamide, 10-50 parts of calcium pantothenate, 1-10 parts of sodium chloride, 1-12 parts of sodium bicarbonate, 1-10 parts of potassium chloride and 100-150 parts of anhydrous dextrose. The medical composition disclosed by the invention is used for treating piglet diarrhea and dehydration caused by diarrhea, so that morbidity and mortality of the piglet diarrhea are effectively prevented and controlled.

The present invention discloses a hyoscyamine aldehyde reductase synthase(HAR) and its application, the hyoscyamine aldehyde reductase synthase has an amino acid residue sequence shown as SEQ ID NO. 4, and a nucleotide sequence shown as SEQ ID NO. 3; the catalyzed reaction product hyoscyamine aldehyde after the prokaryotic expression is hyoscyamine, the hyoscyamine aldehyde is used to transform atropa belladonna, which can increase the content of hyoscyamine in atropa belladonna cell line, and has important meaning to increase the content of tropane alkaloids in atropa belladonna.

The invention provides application of a radix physochlainae extract in preparation of drugs for preventing and treating myopia. Effective compositions such as anisodamine, scopolamine and scopoletin in the radix physochlainae extract are obtained through tests, the purpose of preventing and treating myopia can be achieved, and the defect that clinical application cannot be achieved due to potential side effects caused by long-term single use of anticholinergic drugs can be effectively overcome. The radix physochlainae extract has a remarkable treatment effect on myopia, is high in safety, andis expected to be popularized and applied clinically. Experiments prove that the radix physochlainae extract can be used for improving myopia by regulating scleral fibrous layers and retinal pigment cells, influencing expression of matrix metalloproteinase 2, matrix metalloproteinase inhibitor 2 and the like, regulating spasm of ciliary muscles and the like. The invention also provides a composition. The composition comprises effective components of the radix physochlainae extract; and the composition provides a new way for preventing and treating myopia.

The invention provides a method of genetically transforming the datura arborea by genetic engineering and obtaining the hairy root for producing hyoscyamine and scopolamine. The invention relates to a method of genetically transforming the datura arborea by agrobacterium rhizogenes. The genetically transforming can obtain the hairy root of the datura arborea used for producing hyoscyamine and scopolamine. The method can provide a continuous novel medicine source used for producing hyoscyamine and scopolamine.

The invention relates to application of neostigmine hyoscyamine in preparation of a medicine for treating an acute cerebral ischemic injury, wherein the neostigmine hyoscyamine means a combined medicine of the neostigmine and the hyoscyamine. The invention has the following advantages: the application reveals that the neostigmine hyoscyamine has the remarkable functions of protecting the acute cerebral ischemic injury and improving the neurological functions of the acute cerebral ischemic injury, so that a new application field is provided for the neostigmine hyoscyamine; and meanwhile, a new way for treating the acute cerebral ischemic injury is provided.

The invention provides a pharmaceutical composition for treating a respiratory disease, wherein the pharmaceutical composition comprises one or more components selected from picrinine, vallesamine, scholaricine, and 19-epischolaricine. The pharmaceutical composition has a good protective effect on the respiratory system, and can be used in treatment of a relevant disease.

The invention discloses a method for increasing the content of tropane alkaloid in atropa belladonna. The gene expression quantity of a TAs alkaloid synthesis pathway is effectively increased by expressing a gene rolC or rolB in the atropa belladonna, and the content of hyoscyamine and anisodamine in the atropa belladonna is increased, but variation influence is caused on plant phenotype; and thegene rolC or rolB expressed by H6H-p tissue localization does not influence plant phenotypic growth while the alkaloid content is increased. By selective control of the gene rolC or rolB, a foundationis laid for further cultivating a high-alkaloid-yield atropa belladonna strain in the medicinal field of the atropa belladonna, and a new method is provided for further developing TAs alkaloid gene engineering metabolism research of the atropa belladonna.

The present invention discloses a medicine for preventing and treating Alzheimer's disease. The active ingredient is meletin-3-O-beta-D-xylopyransoyl(1-2)-beta-D-galactopyranoside. The active ingredient RNFG of medicine according to the invention has estrogenic activity, oxidation resisting activity, neuroprotection function for restricting Abeta aggregation and toxicity, and can reduce the memory damage caused by scopolamine. The active ingredient RNFG of medicine according to the invention can be used for preparing the medicine and health product for preventing and treating AD and further has the advantages of usual crude raw material for extracting and easy acquisition.

The invention discloses a medicine capable of treating refractory insomnia, and a preparation method of the medicine. The medicine comprises the following ingredients: propofol, hyoscine hydrobromide,croscarmellose sodium, mannitol, low-substituted hydroxypropyl cellulose and magnesium stearate. Specifically, the medicine is optimally a sublingual tablet, and the medicine can effectively alleviate the symptoms of patients and improve the sleep and living quality of a patient by aiming at the inducement of the refractory insomnia.

The present invention relates to a novel process for the preparation of tiotropium bromide there is provided a process for preparing tiotropium bromide comprising (i) reacting scopine oxalate with diethylamine in an inert solvent to form scopine; (ii) reacting scopine and methyl di-(2-dithienyl)glycolate (MDTG) in the presence of an inorganic base, and in an inert solvent to form N-demethyltiotropium; (iii) reacting N-demethyltiotropium with bromomethane in an inert solvent to form tiotropium bromide; (iv) crystallizing tiotropium bromide in a mixture of methanol and acetone, and optionally thereafter, (v) micronizing the tiotropium bromide so formed.

The invention belongs to the technical field of atropa belladonna extract extraction, and concretely relates to a percolation extraction method of atropa belladonna extract. The percolation extractionmethod comprises the steps of medicinal material treatment, wetting, barreling, percolation, and dry extract preparation, and the medicinal material treatment process comprises the steps of taking roots of atropa belladonna, removing impurities and mildewed parts, washing with a saline solution with the mass concentration of 3%, taking out, rubbing with a rubbing machine, and removing non-shredded parts after rubbing to obtain atropa belladonna rubbing shreds; wherein the percolation speed and the solvent temperature are adjusted in the percolation process. Compared with the prior art, the method has the following advantages that the impregnation time and the percolation time can be shortened, and meanwhile, the obtained dry extract can meet the provisions about the belladonna herb dry extract; the extraction time can be shortened by about a half from the traditional 10h, 168-173g of dry extract can be prepared by rubbing every 1000g of atropa belladonna shreds, and the yield of hyoscyamine reaches 85.5% or above.

The invention provides a combined drug for treating psoriasis. The combined drug includes an anticholinergic drug and a sedative drug used in combination. According to the combined drug provided by the invention, the anticholinergic drug and the sedative drug are used according to a specific ratio, so that the treatment effect can be effectively enhanced, onset of psoriasis patients can be delayed, and the degree of skin damage to scalps, nails, hands and feet can be improved; the combined drug provided by the invention has little or no side effects and high safety; and at the same time, the combined drug provided by the invention can effectively treat the psoriasis, the effect is better than that of an anticholinergic drug scopolamine alone, so that results indicate that the drug providedby the invention has a synergistic effect when used in combination according to the specific ratio, and has a good clinical application prospect.

The invention discloses two polyketide synthases (PKS) EnPKS1 and EnPKS2 from Erythroxylum novogratin, as well as a coding gene and application of the two polyketide synthases. An amino acid sequence of the EnPKS1 is as shown in SEQ ID NO. 4, and a nucleotide sequence of the EnPKS1 is as shown in SEQ ID NO. 3; and an amino acid sequence of the EnPKS2 is as shown in SEQ ID NO. 8, and a nucleotide sequence of the EnPKS2 is as shown in SEQ ID NO. 7. A protein expressed by escherichia coli can be used for catalyzing the condensation of two molecules of malonyl-CoA (malonyl-CoA) to generate acetone dicarboxylic acid. The polyketide synthases can be applied to production of tropane alkaloids (such as hyoscyamine, scopolamine and cocaine) in synthetic biology and production of natural products of acetone dicarboxylic acid intermediates in a biosynthetic route; or the polyketide synthases are used for guiding molecular breeding of related medicinal plants.

The invention relates to an atropa belladonna calmodulin AbCaM1 gene and a recombinant plant expression vector and applications thereof. The nucleotide sequence of the AbCaM1 gene is as shown in SEQ ID NO.1. A gene engineering method is adopted, and the AbCaM1 gene is transferred into atropa belladonna plants through the mediation of agrobacterium tumefaciens. Compared with wild atropa belladonna,the contents of hyoscyamine and scopolamine in the trans-AbCaM1 gene atropa belladonna are obviously improved. The establishment of the method provides a new idea for reducing the production cost andefficiently producing the hyoscyamine and the scopolamine.

The invention provides atropine separated and purified from alkaloid extract and a preparation method of the atropine, and relates to the technical field of pharmaceutical preparations. According to the preparation method for separating and purifying the atropine from the alkaloid extract, scopolamine remained in the alkaloid extract is secondarily utilized, and the purity of the atropine is improved, so that on one hand, the economic benefit can be improved, the industrial development can be promoted, and the waste of raw medicinal materials can be reduced; on the other hand, compared with a synthesis method, damage to the environment is reduced. The invention further relates to atropine, and the atropine is good in quality and physiological activity, high in purity, good in medicinal effect and high in medical value.

The invention provides a scopolamine butylbromide injection and a preparation method thereof. The scopolamine butylbromide injection comprises 200 mg of scopolamine butylbromide, 10-100 mg of a pH buffer pair, 1.2-36 mg of a stabilizer and the balance of water for injection, the pH value of the injection is 4.8-5.4, and the scopolamine butylbromide injection is prepared through the following steps: (1), 60-80% of the water for injection in the formula amount is added into the pH buffer pair in the formula amount, carrying out stirring for 10-30 min so that the water for injection can be completely dissolved, and controlling the pH value to 4.8-5.2; (2) adding scopolamine butylbromide in the formula amount, and performing stirring for dissolving; adding the stabilizer and the residual water for injection in the formula amount, and carrying out stirring for 15-45 min; and (3) performing filtering with a 0.22 [mu] m microfiltration membrane, carrying out filling, introducing nitrogen for protection in the whole preparation and filling process, and performing sterilizing at 121 DEG C for 12 min to obtain the scopolamine butylbromide injection. The scopolamine butylbromide injection can effectively promote spasmolysis of smooth muscles of a patient, and has small adverse reaction; and the storage stability is high, the process is simple and the production cost is low.

The invention discloses a hybridoma cell strain capable of secreting a scopolamine monoclonal antibody and application of the hybridoma cell strain, and belongs to the field of food safety immunodetection. The hybridoma cell strain Pba capable of secreting the scopolamine monoclonal antibody is preserved in the China General Microbiological Culture Collection Center (CGMCC), is classified and named as a monoclonal cell strain, is preserved on April 23, 2020, and has the preservation number of CGMCC No.19678. A complete antigen of hyoscyamine is used for immunizing a BALB / c mouse, splenocytes of a high-titer and low-IC50 mouse are fused with myeloma cells of the mouse through a PEG method, and a selective culture medium is adopted to screen out hybrid cells after fusion of the two cells; and screening cells by an indirect competitive enzyme-linked immunosorbent assay method, and subcloning for three times to finally obtain the hybridoma cell strain Pba. The monoclonal antibody secreted by the Pba has better detection sensitivity (IC50 value is 1.03 ng / mL) to the hyoscyamine, and can be used for residue detection of the hyoscyamine.

The invention provides a scopolamine butylbromide injection and a preparation method thereof. The scopolamine butylbromide injection comprises 200 mg of scopolamine butyl bromide, a pH buffer of 10-100 mg, a stabilizer of 1.2-36 mg, water for injection to 10 ml, and the injection The pH value is 4.8-5.4, and the following method is used for preparation: (1) Take 60-80% of the formula amount of water for injection, add the prescribed amount of pH buffer pair, stir for 10-30min to completely dissolve it, and control the pH to 4.8-5.2 (2) Add the prescribed amount of scopolamine butylbromide, stir and dissolve; add the prescribed amount of stabilizer and remaining water for injection, and stir for 15-45min; (3) Filter through a 0.22 μm microporous membrane, fill, and prepare and fill Fill it with nitrogen protection during the loading process, and sterilize it at 121°C for 12 minutes. The scopolamine butylbromide injection of the invention can effectively promote smooth muscle spasmolysis of patients, has little adverse reaction, high storage stability, simple process and low production cost.

The invention provides a combined medicine for treating ALS. The combined medicine comprises an anti-choline medicine and a sedative medicine which are combined for use. The anti-choline medicine andsedative medicine are used according to a specific ratio, so that a treatment effect can be effectively enhanced. The combined medicine has small side effects or no side effects and has high safety. Meanwhile, the combined medicine can effectively treat ALS and has an effect better than that of single use of the anti-choline medicine scopolamine, indicating that the medicines have a synergistic interaction effect when used in cooperation according to a specific proportion, and the combined medicine has a good clinical application prospect.

The present invention discloses hyoscyamine aldehyde reductase synthase (hyoscyamine aldehyde reductase synthase, HAR) and its application, which has the amino acid residue sequence shown in SEQ ID NO.4 and the nucleotide sequence shown in SEQ ID NO.3; The hyoscypolamine reduction reaction product catalyzed by prokaryotic expression is hyoscypolamine, and the hyoscypolamine content in belladonna cell lines can be increased after the hyoscypolaldehyde reductase is used to transform belladonna cell lines. Significance.

The invention belongs to the technical field of health food, and discloses an application of PAYCS in regulating intestinal flora, metabolites and cranial neurotransmitters, and PAYCS is used for rescuing scopolamine-induced mouse dysmnesia by improving oxidation and inflammatory stress and regulating intestinal microorganism-metabolite-cranial neurotransmitter axis. The PAYCS can significantly reduce serum MDA and LDH levels and significantly increase the SOD content of the liver through a channel for improving memory through intestinal microorganisms-metabolites and neurotransmitter axes; the PAYCS-H can inhibit the rise of TNF-alpha (tumor necrosis factor-alpha) and IL-1beta (interleukin-1beta) of the liver, and the PAYCS-L can only reduce the content of the TNF-alpha of the liver; therefore, the PAYCS-L changes the ratio of bacteroides / bacteroides, the PAYCS improves the relative abundance of plants such as the cactaceae, the prevotella and the like, and tryptophan metabolism related neurotransmitters in the brain are improved.

The invention relates to the technical field of scald treatment, compound anisodamine is composed of a neostigmine injection and an anisodamine injection according to the proportion of 1: 500, and the proportion has good effects on hemorrhagic shock, allergic shock and increase of tolerance of mice to lethal dose endotoxin in the previous research of the unit. The pharmacological basis of the compound preparation is as follows: neostigmine is a reversible cholinesterase (AChE) inhibitor, temporarily inhibits cholinesterase activity, and increases the amount of acetylcholine (ACh) in vivo to excite an M receptor and an N receptor; a large dose of anisodamine has the effects of improving microcirculation and blocking M receptors, blocking of the M receptors enables N receptors to be more fully excited, in the excited N receptors and subtypes of the N receptors, after alpha 7 is excited, release of inflammatory factors can be reduced, and therefore it is proved that the compound anisodamine injection can remarkably reduce the mortality rate of serious scalds, and the compound anisodamine injection can be used for treating the severe scalds. The survival time after injury is prolonged.

The present invention relates to a transdermal therapeutic system without a release-determining membrane for delivering scopolamine, comprising a skin contact layer, an active substance-containing reservoir layer, an active substance-impermeable backing layer, and optionally a protective layer which is detachable from the skin contact layer, wherein the skin contact layer is in direct contact with the active substance-containing reservoir layer. The skin layer or the skin layer and the reservoir layer may be equipped with adhesive strength-increasing additives, for example silicone oils. Furthermore, the system may be equipped with an active substance-free over-patch in order to ensure a sufficient adhesion onto the skin over the application duration. In comparison to comparable systems with a release-determining membrane, a similar bioavailability of the active substance was achieved, such that these systems are bioequivalent to the membrane-containing systems. The present invention additionally relates to the aforementioned transdermal therapeutic systems for use in the treatment of motion sickness and / or post-operative nausea as well as to methods for producing same.

The present invention discloses a process for synthesis of piperidine alkaloids selected from fagomine, 4-epi-fagomine and nojirimycin from tri-O-benzyl-D-glucal or tri-O-benzyl-D-galactal.

The invention provides a method for detecting belladonna alkaloids in animal tissues, which adopts dispersive solid-phase extraction-high performance liquid chromatography triple quadrupole mass spectrometry to simultaneously determine anisodamine, racanisodamine, anisodine, atropine, scopolamine, tropine acid, noratropine and the like in the animal tissues by taking tropine as an internal standard substance. The pretreatment and separation detection conditions are optimized. A target compound is good in linearity within the range of 0.5 ng / L-200ng / L, the detection limit of the method is 0.05-0.1 mu g / kg, the quantification limit of the method is 0.2-0.5 mu g / kg, the matrix blank adding standard recovery rate is 80.2-119%, and the relative standard deviation of parallel determination is 1.13-14.5%. According to the method, the belladonna alkaloids in the animal tissues can be accurately measured, the measurement result is accurate and reliable, reliable data is provided for measurement of the belladonna alkaloids, and the method has remarkable economic benefits and wide market prospects. The method has a good reference value for guiding the measurement of drug residues.

The invention discloses a medical scopolamine butylbromide preparation method which comprises the following steps: (1) scopolamine butylbromide crude product preparation: evenly mixing scopolamine, butyl bromide and a solvent A, performing heating and refluxing reaction and adding a solvent B to perform vacuum concentration after reaction to obtain a scopolamine butylbromide crude product; (2) purification: recrystallizing the scopolamine butylbromide crude product by a solvent C and vacuum drying to obtain medical scopolamine butylbromide. The scopolamine butylbromide preparation method disclosed by the invention has the advantages of convenience in technological operation, high yield, low cost, high product purity, easiness in industrialized production and the like.

The invention discloses a tropane alkaloid transport protein AbTAUP1 and application thereof. An amino acid sequence of the tropane alkaloid transport protein AbTAUP1 is as shown in SEQ ID NO. 8, or an amino acid sequence which is obtained in a manner that the sequence as shown in the SEQ ID NO.8 is subjected to substitution, mutation or deletion of one or more amino acid residues and is encoded with the same function. The expression level of the protein in lateral roots is highest, the expression level of the protein in main roots is relatively low, the protein is located in a cytoplasmic membrane and speculated to have a hyoscyamine transport function, the hyoscyamine transport function of the protein is verified through a yeast transport experiment, the yield of hyoscyamine in atropa belladonna is increased by overexpressing the AbTAUP1 in atropa belladonna plants, so that the AbTAUP1 can be used for providing hyoscyamine transport capacity in hyoscyamine synthesis plants and increasing the hyoscyamine yield and has an important significance in increasing the content of tropane alkaloids in plant species.