260 results about "Lamivudine" patented technology

The invention involves A 1- beta-keto-5, 11(13)-diene eudesmane-12-acidum who has the structure as formula (1) shows and its medical salt, or solvate and its drug combinations and its medical usage in reducing hepatitis B surface antgien and inhibiting replication activity of aethyl- hepatovirus HBV-DNA medicinal. The invention compounds has strong inhibitory action in hepatitis B surface antgien (HBsAg) externalized by HepG2.2.15 cells and replication of aethyl- hepatovirus deoxyribonucleotide (HBV-DNA) in vitro, its inhibiting ability against HBsAg surpasses that of positive control Lamivudine in the same dose; it has obvious inhibiting ability against replication of aethyl- hepatovirus HBV-DNA under the concentration of 100 mu g/mL,20 mug/mL and 4 mug/mL DNA, it belongs to anti- aethyl- hepatovirus natural products of superactive non-nucleoside, can be expected for producing drugs for treating aethyl- hepatovirus infected disease.

The invention relates to application of diamine formyl dehydrogenated silybin serving as a medicament for curing viral hepatitis B, in particular to application of a flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents or pharmaceutically acceptable salts thereof in preparation of a medicament for clearing HBsAg and HBeAg and a medicament for inhibiting HBV DNA replication. The flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents has extremely high HBsAg and HBeAg inhibiting activities; when the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents is at a concentration of 20 mu g/ml, the inhibition rates of the HBsAg and the HBeAg are respectively 94.4 percent and 95.7 percent which exceed 5.9 times and 5.7 times those of a positive control alpha-interferon; and simultaneously the inhibition rate of the HBV DNA is 99.7 percent when the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents is at the same concentration, and the inhibition activity of the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents is higher than that of lamivudine and the alpha-interferon. In summary, the flavonolignan of dehydrogenated silibinin esters of which the ring A and the ring E have diamine formyl-methoxyl substituents or the pharmaceutically acceptable salts thereof can be expected for preparing non-nucleoside medicaments for clearing the HBsAg and the HBeAg, inhibiting the HBV DNA replication, and curing the hepatitis B virus infection diseases.

The invention relates to application of aromatic carbamoyl dehydro-silibinin as a medicament for treating viral hepatitis B, in particular to application of todehydro-silibinin flavonolignans with a ring A and a ring E which are substituted by double base aromatic carbamoyl methoxyl and pharmaceutically acceptable salt thereof for preparing medicaments for removing HBsAg and HBeAg and medicaments for inhibiting HBV DNA. The todehydro-silibinin flavonolignans has extremely obvious activity on inhibiting the HBsAG and the HBeAg, has the intensity of 46.2 percent and 68.9 percent for respectively removing the HBsAG and the HBeAg in the presence of the concentration of 100 microgram/milliliter, which is 2.9 times and 4.1 times higher than that of positive control medicament alpha-interferon, and has the inhibition ratio of 96 percent on HBV DNA in the presence of the concentration of 100 microgram/milliliter, which is higher than that of lamivudine and the alpha-interferon. Accordingly, the flavonolignans and the pharmaceutically acceptable salt thereof can be expected to be used for preparing non-nucleoside medicaments applied for removing HBsAg and HBeAg, inhibiting HBV DNA replication and treating hepatitis B virus infection diseases.

The invention relates to application of ring A coupling flavonolignan in preparing medicaments for treating viral hepatitis B, in particular to application of a compound of the formula (1) or a pharmaceutically acceptable salt thereof in preparing medicaments for clearing away HBsAg (Hepatitis B Surface Antigen) and HBeAg (Hepatitis B e Antigen) and suppressing the HBV (Hepatitis B Virus) DNA replication. The intensities of the flavonolignan for clearing away the HBsAg and the HBeAg are respectively 29.4 percent and 29.1 percent in the presence of a concentration of 20 micrograms/milliliter, which is respectively 1.8 times and 1.7 times of the corresponding activity of a positive control medicament (10,000 units/milliliter of alpha-interferon). What is even more exciting is that in the presence of the concentration, the suppression rate of the flavonolignan to the HBV DNA is higher than 83 percent, which is higher than that of Lamivudine which is a positive control and is 2.2 times of that of the alpha-interferon to the HBV DNA. Accordingly, the flavonolignan and the pharmaceutically acceptable salt thereof are indicated to be capable of being expected to be used for preparing non-nucleoside medicaments for clearing away the HBsAg and the HBeAg, suppressing the HBV DNA replication and treating HBV infection diseases.

The invention relates to application of E-ring demethoxy-silibinin for preparing medicaments for treating viral hepatitis B, and particularly to application of compound in formula (1) and pharmaceutically acceptable salt thereof for preparing medicaments for clearing HBsAg and HBeAg and suppressing HBV DNA replication. The invention has extremely superactive activity for suppressing the HBsAg and HBeAg; in the presence of the concentration of 20 microgram per millilitre, the intensities for clearing the HBsAg and HBeAg are 95.0% and 34.4% respectively, which are 5.9 and 2.0 times corresponding activity of a positive control medicament alpha-interferon; and it should be noticed that the suppression ratio of the medicament for HBV DNA at the concentration is about 91.5%, which is 13% higher than lamivudine and 2.4 times alpha-interferon suppression activity. In summary, the flavonolignans or pharmaceutically acceptable salt thereof can be prospectively used for preparing non-nucleoside medicaments for clearing the HBsAg and HBeAg, suppressing HBV DNA replication and treating hepatitis B virus infection disease.

The invention relates to application of dimethyl dehydrated silybin in preparing medicaments for treating virus hepatitis B, in particular to the application of 7 and 20-position methyl substituted dehydrated silybin or pharmaceutically acceptable salts thereof in preparing medicaments for removing HBsAG and HBsAg and medicaments for inhibiting HBV DNA replication. The dehydrated silybin has remarkably HBsAg and HBeAg inhibiting activity, wherein the strength for removing the HBsAg and the HBeAg at the concentration of 20 milligram/milliliter is 88.9 percent and 84.1 percent respectively, which are 5.5 times and 5.0 times that of a positive contrast medicament. More importantly, the dehydrated silybin shows the HBV DNA inhibition ratio of about 99.6 percent at the concentration of 20 milligram/milliliter, the activity exceeds lamivudine by 23 percent, which is 2.6 times that of interferon. Therefore, favonolignan or pharmaceutically acceptable salts thereof can be predictably used for preparing the non-nucleoside reverse transcriptase inhibitor medicaments for removing the HBsAg and HBeAg, inhibiting HBV DNA replication and treating hepatitis B virus infection diseases.

This invention prepn. method consists procedures (as shown in route chart) of: (1). hydrated glyoxalic acid is reacted with menthol in solvent and catalyst to product stable intermediate glyoxalic (1, R, 2.5, 5, R) menthol (V); then being reacted with 2,5-dihydroxy-1,4-dithiothiane to produce product and then proceeding crystallation to obtain menthol ester (IV); (2). proceeding acidylation by using hydroxy to obtain menthol ester (III); (3) being condensed by cytosine under protection of silanized reagent, to obtain menthol ester (II); (4) obove-said product is reduced by reducing agent to obain final invented product Lamifudin (I). This invention has advantages of: available raw material, high yield, high safety, and commercialization prodn.

A lamivudine diastereoselective synthesis method, which takes chiral auxiliary agent L-menthol as the initial material, synthesizes trans-5-hydroxyl-1, 3-oxygen thiacyclopentane-2-carboxylic acid-(1'R, 2'S, 5'R) menthol ester under the action of concentrated sulfuric acid, choose triethanolamine to obtain trans-isomer trans-5-hydroxyl-1, 3-oxygen thiacyclopentane-2-carboxylic acid-(1'R, 2'S, 5'R) menthol ester, and let the trans-isomer to react with acylating agent to obtain trans-5-acetoxy-1, 3-oxygen thiacyclopentane-2-carboxylic acid-(1'R, 2'S, 5'R) menthol ester, glycosidate with cytosine under the action of alkali to obtain 5S-cytosine-1'-radical-1, 3-oxygen thiacyclopentane-2-carboxylic acid-(1'R, 2'S, 5'R) menthyl ester, and then deoxidize with a deoxidizer, and salifying with aspirin, to ionize and liberate lamivudine. Since triethanolamine is added as in the course of reaction interconverting agent, the yield of lamivudine is increased greatly. Aspirin is added in the course of reaction, so that the lamivudine forms an aspirin salt that has poor water solubility, and therefore can effectively separate and liberate lamivudine from the medium.

The invention discloses a tri-combination compound mini-pill tablet co-prepared by disoproxil fumarate DF coated mini-pills, lamivudine coated mini-pills and efavirenz mini-pills and a preparation method thereof. The invention solves the problems that effective component degradation and dissolution delaying phenomena are generated due to interaction among the tri-combination compound components, tabletting is not facilitated during preparation and patient swallowing is not facilitated; and the single-layer tablet having the three component drugs without mutual contact is prepared by a mini-pill tabletting method, so as to obtain good stability and fast dissolving rate.

The invention discloses a preparation method of lamivudine and an intermediate thereof; (2R,5R)-5-hydroxyl-[1,3]oxathiolane-2-carboxylicacid(2S-isopropyl-5R-methyl-1R-cyclohexyl)ester, the structure of which is shown in formula (II) is used as a raw material; acyl compound, the structure of which is shown in formula (III) is obtained by the acylation reaction of acyl; acyl compound (III) reacts with cytimidine, the structure of which is shown in formula (IV) by condensation reaction to prepare the intermediate of lamivudine (V) and the intermediate is reducted to obtain lamivudine (I). The invention is characterized by safe and reliable operation, simplified process, low production cost and the like, thus being suitable for industrialized production.

The invention relates to the preparation of an absorption material and the application to medicament separation and enrichment, in particular to the preparation methods of a Lamivudine molecularly imprinted polymer and a Lamivudine molecularly imprinted solid phase extraction column and the applications thereof. The Lamivudine esterified ester is obtained through esterification synthesis. The molecularly imprinted polymer is synthesized by using the Lamivudine esterified ester as a template, methacrylic acid as a monomer, trimethoxy propane trimethyl acrylate as a crosslinker and chloroform as a porogen by adopting a body polymerization method; and molecularly imprinted polymer particles are uniformly filled in the solid-phase extraction column to obtain the Lamivudine molecular imprinting solid-phase extraction column. The invention realizes the efficient separation, enrichment and purification of Lamivudine in a biological sample and has high selectivity as compared with traditional related technologies, such as a common solvent extraction method, a C18 solid-phase extraction method, and the like. Moreover, the Lamivudine molecularly imprinted solid phase extraction column has low cost by being repeatedly used and can become a necessary method in the Lamivudine pretreatment in biological samples.

The invention discloses anti-HIV compound preparation. The anti-HIV compound preparation is prepared from the following ingredients in weight percentage: 10 to 35% of lamivudine, 10 to 35% of fumaric acid tenofovir ester, 5 to 20% of 3-((3-ethyl-2,6-dioxo-5-(propyl-2-radical)-1,2,3,6-tetrahydropyrimidine-4-radical)carbonyl)-5-tolunitrile and 10 to 75% of excipient. The anti-HIV compound preparation disclosed by the invention is single-layer tablet or double-layer tablet; in preparation, the fumaric acid tenofovir ester and compound of the 3-((3-ethyl-2,6-dioxo-5-(propyl-2-radical)-1,2,3,6-tetrahydropyrimidine-4-radical)carbonyl)-5-tolunitrile are independently pelletized and then totally mixed and compressed into tablets. The anti-HIV compound preparation disclosed by the invention has the advantages of good stability, a simple preparation technology and controllable quality, can restrain HIV virus from different targets, improves a treating effect of single drug use to AIDS, avoids side effects on a nervous system and has small toxicity and a wide safety dosage range.

The invention relates to examination mutant hepatitis virus method, especially the method of using DNA reverse dot blot hybridization technique to quickly and exactly distinguish clinic blood sample wild type and rummy fuding tolerance mutant hepatitis b virus. And it also relates to clinic measuring kit.

The invention discloses a lamivudine tablet, which is characterized in that a tablet core contains the followed raw materials by weight: 100 parts of lamivudine, 70-150 parts of filler, 0.1-10 parts of disintegrating agent, 0-5 parts of flow aid, and 0.1-3 parts of lubricant. The invention further provides a method for preparing the lamivudine tablet. The tablet core of the lamivudine tablet of the invention is prepared by directly pressing a mixture of active component lamivudine and accessories, so the dissolving-out speed is faster. Further, the tablet core of the invention is coated with a film coating, thereby preventing the tablet core form moisture absorption, and guaranteeing the medicine curative effect. The stability of the tablet is better. The method for preparing the lamivudine tablet in the invention, has advantages of simple technology, convenient operation and low production cost.

The chiral chromatographic fixed phase stuffing of vancomycin phenylisocyanate is prepared through bonding vancomycin as glycopeptide macrocyclic antiseptic chemical onto silicon gel carrier, and the subsequent derivation of phenylisocyanate to obtain chiral chromatographic fixed phase stuffing. The silicon gel carrier is first reacted with 3-aminopropyl triethoxy silane for silanation and then space arm activated; and the activated silicon gel carrier is bonded with vancomycin and finally derivated with phenylisocyanate. The chiral chromatographic fixed phase stuffing of vancomycin phenylisocyanate after assembled to column may be used in forward phase, reverse phase and polar organic phase chromatographic condition. The present invention may be used in simple polar organic phase mode to resolve the medicine antimer of zolmitriptan, lamivudine, etc.

The invention provides lamivudin stearate. The lamivudin stearate is characterized in that the lamivudin stearate is synthesized through lipophilicity modification of lamivudin, which is favorable for medicinal loads of targeted carrier materials; chitosan-stearate graft micelles having efficient cell intake and low toxicity are used for encapsulating antiviral medicaments of molecular targets incells so as to greatly increase medicament intake of viral cells and medicament concentration at the medicinal molecular targets; the increased medicament intake of the viral cells is favorable for reducing the distribution of the medicaments in normal tissues or cells and toxic and side effects of the medicaments; the increased medicament concentration at the medicinal molecular targets is favorable for improving the effects of the antiviral medicaments; and the lamivudin stearate can be applied to preparing the medicaments having efficient anti-HBV activity. The lamivudin stearate has the following chemical structural formula.

The invention discloses an application of lindley eupatorium herb in preparing anti-hepatitis B virus medicaments. Lindley eupatorium herb ethanol extract, lindley eupatorium herb flavone part, lindley eupatorium herb hemiterpene part, lindley eupatorium herb 70% ethanol water elution part and chain diterpene are prepared from lindley eupatorium herb and are subjected to hepatitis B virus (HBV) testing, and testing results indicate that the four extracts and the chain diterpene have the effect of remarkably inhibiting hepatitis B surface antigen (HBsAg) and hepatitis B core antigen (HBeAg), and have better drug activities than those of clinical medicament lamivudine (3TC) for treating hepatitis B. The lindley eupatorium herb can be used for preparing medicaments for resisting hepatitis B virus.

The invention provides an anti-HBV medicine combination which has more remarkable treatment effect and safety and no toxic and side effect and can evidently increase the negative conversion ratio of HBSAg. The invention takes HepG2.2.15 as a target cell and adds lamivudinevir, protocatechuic acid and the compatibility preparation of lamivudinevir and protocatechuic acid with a proper concentration to cell culturing medium. The cell is cultured by a regular method and HBsAg and HBeAg secreted by the cell is detected by ELISA method, HBV DNA content is measured by fluorescent quantitation PCR, HBV resistance effect of the drug is judged by depression rate calculation method to determine the medical treatment effect on HBV and the preparation proportion of medicine combination. The proportion of lamivudinevir to protocatechuic acid is between 1 to 50 and 1 to 100 (mass ratio) and generally the dosage of lamivudinevir is 0.05-5Mug and the protocatechuic acid is 5-500 Mug. The medicine combination can evidently improve the depression effect of the lamivudinevir on Hepatitis B antigen and reduce the toxic and side effect of the lamivudinevir when being used separately.