77 results about "A huperzine" patented technology

The present invention provides a composition of transdermally administered huperzine for improving memory and cognitive function. In one aspect, huperzine is delivered in a sufficient amount to achieve and maintain a blood plasma Huperzine level of about 0.5 ng/mL to about 30 ng/mL. Huperzine may be delivered by itself, or in combination with other elements, such as additional cholinesterase inhibitors, drugs or treatment agents, or positive health promoting substances. Various formulations for the transdermal delivery of huperzine are disclosed, and may include selected penetration enhancers.

The present invention provides compositions and methods for treating, preventing, or reversing neuronal dysfunction including cognitive decline, such as cognitive decline associated with aging and minimal cognitive impairment; severe neurodegenerative disorders, such as Alzheimer's disease; and neuronal dysfunction associated with loss of motor skills, such as Parkinson's disease and amyotrophic lateral sclerosis. The compositions and methods of the invention can also treat or prevent neuronal dysfunction resulting from CNS injury, such as stroke, spinal-cord injury, and peripheral-nerve injury. The compositions of the invention comprises a huperzine compound and a nicotinic compound.

The invention discloses a huperzine A polymorph, its preparation method, a medicinal composition containing huperzine A polymorph and its application. Part of the huperzine A polymorph has better dissolvability than currently saled medicinal crystal forms, thus being more conducive to medicine absorption. Also, part of the huperzine A polymorph has substantially lower hygroscopicity than saled medicinal crystal forms, thus being more conducive to preparation and storage of medicinal preparations.

The invention relates to the technical field of microbes and especially relates to huperzia serrata endophytic fungi and its use in production of huperzine a. The huperzia serrata endophytic fungi are named as Colletotrichum sp. SY-1, are preserved in the China center for type culture collection (CCTCC) on August 19, 2011, and have the preservation number CCTCC M2011293. Through fermentation, the huperzia serrata endophytic fungi can produce a huperzine a compound. Through utilization of characteristics of microbe-based huperzine a production and the modern fermentation breeding technology, huperzine a industrial production is realized; bottleneck problems of huperzine a exploitation are solved; and the endangered huperzine a natural resource is protected.

The invention discloses a huperzine A high-producing strain and a method for producing huperzine A by fermenting the same, belonging to the technical field of biology. The huperzine A high-producing strain is Colletotrichum gloeosporioidesisolate YLJ-13 preserved in the China Center for Type Culture Collection on July 17, 2010, and the preservation number is CCTCC No. M2010181. The strain provided by the invention is separated and purified from huperzia crispate through pressure screening, and the strain is identified as a new variety of Colletotrichum gloeosporioidesisolate through a molecular biological means. The strain is fermented in an improved potato liquid culture medium, and huperzine A is obtained from the fermentation liquid. Huperzine A obtained through fermentation production can be secreted to be out of cell, the improved potato liquid culture medium is used as a precursor of biological transformation, and up to 199.6 mg/L huperzine A can be obtained from each liter of culture system. The strain provided by the invention is used for producing huperzine A. The existing rare medicinal huperziaceae plant resources can be protected, but also the shortage situation of huperzine A medication demand can be alleviated.

The invention discloses a huperzine A double-layer osmotic pump controlled-release tablet. The tablet comprises a double-layer tablet core consisting of a drug containing layer and a pushing layer, and a semipermeable coating membrane coating the double-layer tablet core, wherein one side of the drug containing layer of the coating membrane is provided with a drug release hole; the drug containing layer of the tablet core contains huperzine, a suspending agent, osmotic pressure active matters and pharmaceutical excipients which are all in effective dosage; the pushing layer contains an expanding agent, a permeation enhancer, and a binder; and the coating membrane contains polyethylene glycol used as a plasticizer, the weight gain of the coating membrane against the weight of the tablet core is between 8 and 20 percent, and the aperture of the drug release hole on the surface of the drug containing layer of the coating membrane is between 0.2 and 2.0 millimeters. The invention also discloses a method for preparing the controlled-release tablet. After patients take the controlled-release tablet, the blood concentration of the patients is relatively stable; the accumulated drug release rate in 12 hours reaches more than 90 percent, thereby greatly reducing the drug taking frequency of the patients; and the invention provides a novel formulation which is safer, more effective, stable, controllable and convenient for application in clinically treating senile dementia.

The invention relates to a huperzine A oral formulation and a preparation method thereof. The formulation is prepared from huperzine A and officinal auxiliary materials, wherein the officinal auxiliary materials comprise water-insoluble excipient, disintegrant, adhesive and lubricant. The formulation is prepared from the following components by weight percentage: 0.005-1% of huperzine A, 0.1-99% of water-insoluble excipient, 0.1-10% of adhesive, 0.1-80% of disintegrant and 0.1-10% of lubricant. The invention improves the compliance of patients on the medicament and enhances the bioavailability of the medicament.

The invention discloses a method for extracting huperzine A from a serrate clubmoss herb. The method comprises the following steps: (1) pre-treatment; (2) ultrasonic countercurrent extraction: carrying out ultrasonic countercurrent extraction on the serrate clubmoss herb and filtering to obtain leach liquor; (3) membrane separation and purification: centrifuging, and carrying out ultrafiltration and nanofiltration on the leach liquor to obtain trapped fluid; (4) concentration, namely concentrating the trapped fluid into paste; (5) acid dissolution, dissolving the paste by using acid liquid, filtering, and adjusting pH to alkalinity; (6) extraction: extracting by using chloroform and collecting extract liquor; (7) concentration: concentrating the extract liquor to obtain dry powder; (8) crystallization and recrystallization: dissolving to obtain the dry powder, crystallizing and recrystallizing to obtain white crystals; and (9) drying, namely drying the white crystal to obtain a huperzine A product. According to the method disclosed by the invention, the purity of the huperzine A extracted from the serrate clubmoss herb is greater than or equal to 99%, the product yield is greater than or equal to 0.026%, the final yield is 50-55%, and the yield, yield coefficient and purity of huperzine A is high, the extraction time is short, and the cost is low; therefore, the method for extracting huperzine A from a serrate clubmoss herb is suitable for industrial production.

The invention relates to a huperzine A high yield strain TCM-01 of which classified nomenclature is Endophyte sp.TCM-01, conservation address is the China center for type culture collection, conservation date is April 16, 2010 and CCTCC NO is M2010086. The high yield strain uses Penicillium chrysogenum Thom as parent strain and is prepared through microwave mutagenesis-screening. The invention further optimizes the condition of fermentation culture of the strain; and under the condition of culture, the yield of huperzine A is up to 4.761mu g/ml. Under the same condition of fermentation, the yield of the product is greatly increased, and the cost can be largely saved.

The invention relates to a huperzine A preparation for treating schizophrenia and nervous function damage and a preparation method thereof. The preparation method comprises the following steps: using a solvent dispersing method and a solid-liquid phase dispersing and melting method to properly dissolve huperzine A by solvent, preparing stable huperzine A hydrochloride solution, spraying the huperzine A hydrochloride solution in an auxiliary material by dispersion, or preparing solid dispersoid mixture with uniform phase dispersion, crushing, mixing and stirring uniformly, directly adding a lubricating agent for tabletting, also being capable of adding a binding agent, granulating, drying, adding the lubricating agent, and tabletting. The phase-dispersing mixture of huperzine A also can be added with the lubricating agent with proper amount for mixing, and then filled into a capsule. The preparation is used for treating the symptoms of all the periods of schizophrenia, and has the advantages of having the effects of protecting oxidative stress toxicity of nerve cells generated by resisting Beta amyloid peptide and inducing cell apoptosis, promoting the growth of nerve growth factor, being effective for treating inflammation in cerebral hemorrhage and inflammation of cerebral ischemic injury, having long action time of drugs, being convenient to application of oral administration/containing administration and the like. The invention has high content of huperzine A preparation, stable preparation quality and good bioavailability and can improve the medication compliance of patients with schizophrenia and senile dementia.

A huperzine A compound is provided. The huperzine A compound has following formula:

wherein X comprises O or S, Y comprises —O—, —S—, —CH(R₄)—, —C(R₄)(R₅)—, —C(R₄)═C(R₅)—, —C≡C—, —NH— or —N(R₄)—, n is 0, 1 or 2, R₃ is C(═X)—(Y)_n-R₁ provided that R₂ is H or R₂ and R₃ are combined to form ═CH—Ar, wherein R₁, R₄ and R₅ independently comprise hydrogen, C₁-C₃₂ alkyl, C₁-C₃₂ alkenyl, C₁-C₃₂ alkynyl, C₁-C₃₂ aryl or C₁-C₃₂ heteroaryl, in which alkyl, alkenyl, alkynyl, aryl or heteroaryl with one or more substituents comprising halogen, hydroxyl, alkoxy, aryloxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, imino, alkylimino, arylimino, acylamido, diacylamido, acylimido, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, thio, sulfonyl or sulfinyl, and Ar comprises aryl or heteroaryl.

The invention belongs to the technical field of drug preparation, and particularly relates to a huperzine A tablet and a preparation method thereof. The huperzine A tablet comprises the following components in parts by mass: 0.5 parts of huperzine A, 500-700 parts of a filler, 5-15 parts of an adhesive, 20-50 parts of a disintegrating agent, and 1-5 parts of a lubricant, wherein the average particle size of huperzine A is controlled at 110-120 mu m. Compared with the prior art, by carrying out micronization treatment on raw materials, the particle size of huperzine A is controlled at 110-120 mu m, so that the disintegrating speed of the tablet can be increased, and the dissolution of huperzine A can be improved, thereby improving the bioavailability and stability of the huperzine A tablet.

The invention relates to a huperzine osmotic-pump controlled release tablet, which is composed of tablet core containing huperzine and semipermeable film coating with small holes. The huperzine osmotic-pump controlled release preparation is characterized in that the preparation comprises the following components by the weight percent: 0.2-0.6 percent of huperzine in the tablet core, 85-95 percent of osmotic pressure accelerating agent, 1-10 percent of suspending agent and o.1-5 percent of other components. A coating film contains cellulose acetate, PEG (polyethyleneglycol) 4000 and a plasticizing agent, and the proportion of the cellulose acetate, the PEG4000 and the plasticizing agent is 1: (0.3-0.4) : (0.1-0.2). The weight of the coating is increased by 11-13 percent.

The invention discloses a huperzine-A solid dispersion and a method for preparing a tablet thereof. The huperzine-A solid dispersion comprises huperzine-A and a carrier used as a dispersant; the weight ratio range of the carrier to the huperzine-A is 1-25:1; the carrier material may be one or more of polyvinylpyrrolidone, polyethylene glycol 4000, polyethylene glycol 6000, Poloxamer 188, mannitol, lactose or microcrystalline cellulose; and the huperzine-A solid dispersion is prepared by adopting a grinding method, and the obtained solid dispersion can be prepared into huperzine-A tablets by adopting a wet granulating and tabletting method. The huperzine-A solid dispersion can remarkably increase the solubility of a medicament and promote the absorption so as to greatly improve the dissolution and bioavailability of the medicament.

The invention provides a huperzine A solid composition, which comprises huperzine A, filler, a pH regulator and a lubricant. The invention also provides a method for preparing the composition, which comprises the following steps: dissolving the pH regulator in water; adding the huperzine A into the pH regulator solution; mixing and stirring the solution and the filler after the huperzine A is dissolved; pelletizing, drying and granulating the mixture; mixing the grains and the lubricant; and filling the grains into capsules or tabletting the grains.

The invention relates to a huperzine A dropping pill and a preparation method, which is characterized in that: the huperzine A is dissolved through proper solvent and then added into the matrix by the dispersion dropping method, is agitated evenly and condensed to be the pill.

The invention discloses a synthesis method for preparing a huperzine A intermediate, which comprises the following steps: carrying out substitution at the alpha site of the carbonylic group by using 1,4-cyclohexyl diketone ethylene glycol and N,N-dimethylformamide dimethyl acetal as raw materials to obtain a substitution product, cyclizing the substitution product under the action of methyl cyanoacetate to obtain a cyclization product, and decarboxylating the cyclization product under the action of a strong base to obtain 2-carbonyl-6-ethylene ketal-5,7,8-dihydro-quinoline. The method has the advantages of fewer synthesis reaction steps, mild reaction conditions, low requirements for operating personnel and low environmental pollution, greatly lowers the raw material cost, and is simple to operate and convenient for refinement; and the obtained 2-carbonyl-6-ethylene ketal-5,7,8-dihydro-quinoline has high quality and high yield.