10 results about "Atorvastatin calcium" patented technology

[Problem] To provide an atorvastatin calcium anhydride crystal having higher solubility than that of a conventional hydrate crystal and being more stable than an amorphous form. [Solution] The present invention pertains to an atorvastatin calcium anhydride crystal that exhibits an X-ray diffraction pattern, which has peaks at 2θ = 8.7°, 10.4°, 18.1°, 19.5°, 20.9°, 22.5°, 24.1°, and 25.6°, by X-ray powder diffraction measurement (XRPD) using CuKα radiation.

The application belongs to the technical field of synthesis of medical intermediates, and particularly relates to a synthesis method of a chiral intermediate of atorvastatin calcium. 1,3-propanediol is used as raw material, a silicon-based protection reaction is carried out, and then oxidation is carried out, a ring addition reaction occurs under the catalysis of a chiral catalyst and a lithium salt, and a first chiral center is introduced; then, t-butyl acetate is added to carry out a ring opening reaction, a Narasaka-Prasad reduction reaction is carried out to induce a second chiral center; 2,2-dimethoxypropane is added to protect cis diol, finally, tetrabutylammonium fluoride is added to remove the silicon-based reaction, and a Fukuyama amine synthesis method is used to replace the hydroxyl group with the amino group to obtain the chiral intermediate of atorvastatin calcium. The application uses 1,3-propanediol which is cheap and easy to obtain as raw material, and various dangerous, toxic and expensive drugs are not used in the synthesis route process, the method has a simple route, high yield and good repeatability, and can be used for industrial production.

An atorvastatin calcium albumin nanoparticle, and a preparation method therefor and the use thereof. The atorvastatin calcium albumin nanoparticle consists of atorvastatin calcium and serum albumin in a mass ratio of 1:3-1:10. The preparation method comprises: adding absolute ethanol to atorvastatin calcium to obtain an organic phase, adding deionized water to serum albumin and adjusting the pH to obtain an aqueous phase, adding the organic phase in a dropwise manner to the aqueous phase, adding a glutaraldehyde solution for cross-linking, removing anhydrous ethanol, performing centrifugation, and collecting the lower precipitate layer to obtain the atorvastatin calcium albumin nanoparticle.

The invention discloses a semen cassiae naphthopyrone extraction enriched product as well as a preparation method and application thereof. The preparation method comprises the following steps: crushing semen cassiae, sieving, carrying out ball milling, carrying out ultrasonic extraction, carrying out vacuum concentration on an extract, and freeze-drying to obtain crude extract powder, carrying out gradient elution by virtue of AB-8 macroporous resin, and freeze-drying to obtain a naphthopyrone extraction enriched product; pharmacological experiments show that the enriched product can significantly reduce the levels of triglyceride, total cholesterol and low-density lipoprotein of mice induced by high-fat diet, and also can regulate the blood sugar level, and the lipid and blood sugar reducing level of the enriched product is close to that of a positive drug atorvastatin calcium group; according to network pharmacological mechanism research, it is speculated that the enrichment is mainly used for improving the metabolic syndrome through a phenotypic pathway with lipid and atherosclerosis as the core, and the metabolic syndrome is possibly activated by a PPAR signal pathway (especially PPAR gamma).

The invention discloses a blood fat reducing composition containing supramolecular group composite peptide, which is composed of raw materials and basic energy substrates, the raw materials comprise supramolecular group composite peptide, natto freeze-dried powder, black pepper extract and bamboo leaf flavone, and the basic energy substrates comprise proteins, dietary fibers, fatty acids and / or lipids; the composite peptide is composed of soybean peptide and bitter gourd peptide. The composition prepared by compounding the components of specific types and dosages has the effects of remarkably reducing the triglyceride level, reducing the content of low-density lipoprotein cholesterol and increasing the content of high-density lipoprotein cholesterol, and part of the composition can also cooperate with statin western medicines (such as atorvastatin calcium) to achieve the effects of enhancing the effect of reducing blood fat and improving the blood fat content. The effect of assisting in improving or preventing and reducing blood fat is achieved. Therefore, the method can be used for developing functional foods and medicines and has a considerable market prospect.

The invention relates to the technical field of medicines, and discloses a method for detecting related substances of an ezetimibe atorvastatin calcium composition, a sample solution is detected by adopting a liquid chromatography, octadecylsilane / pentafluorophenyl bonded silica gel is used as a filler, and a gradient elution method is adopted. One method can detect more than 20 related substances in ezetimibe and atorvastatin calcium at the same time, the separation and detection efficiency is improved, and the method is high in specificity, high in separation degree, high in sensitivity and good in accuracy and has positive effects and practical application value.

The invention belongs to the technical field of medical chemistry, and particularly relates to a preparation method of an atorvastatin calcium intermediate, which realizes continuous preparation through a fixed bed reactor.

The application discloses atorvastatin calcium albumin nanoparticles and a preparation method and application thereof. The atorvastatin calcium albumin nanoparticles are composed of atorvastatin calcium and serum albumin, and the mass ratio of atorvastatin calcium to serum albumin is 1:3-1:10. The preparation method comprises the following steps: weighing atorvastatin calcium, fully dissolving the atorvastatin calcium in anhydrous ethanol to obtain an organic phase; weighing serum albumin, fully dissolving the serum albumin in deionized water, adjusting the pH of the solution by sodium hydroxide to obtain an aqueous phase; under stirring, dropping the organic phase into the aqueous phase, adding glutaraldehyde solution, continuously stirring and crosslinking, after the crosslinking is completed, removing the anhydrous ethanol by rotary evaporation, centrifuging the obtained solution by using a high-speed refrigerated centrifuge, and taking the lower precipitate as the atorvastatin calcium albumin nanoparticles. The atorvastatin calcium albumin nanoparticles prepared in the application can prolong the in-vivo circulation time of atorvastatin calcium, improve the bioavailability, and especially improve the antitumor activity of atorvastatin calcium.

The application discloses amlodipine atorvastatin calcium tablet and a preparation method and application thereof, relates to the technical field of pharmaceutical preparations, and improves the dissolution rate of benzenesulfonic acid amlodipine and atorvastatin calcium by improving the component formula and micronization treatment of raw materials, and regulates the dissolution rate of benzenesulfonic acid amlodipine and atorvastatin calcium, so that the blood drug concentration is stably in an effective treatment range, thereby improving the bioavailability, reducing the frequency of taking medicine, enhancing the curative effect, and improving the medication compliance.

The invention belongs to the technical field of pharmaceutical preparations, and discloses a solid pharmaceutical composition containing atorvastatin calcium and a preparation method thereof. The solid pharmaceutical composition is formed by pressing a first quick-release layer and a second enteric-coated layer, wherein the first quick-release layer contains atorvastatin or pharmaceutically acceptable salt thereof; the second enteric-coated layer is a buffer compaction layer and comprises aspirin enteric-coated particles dispersed in a buffer matrix; the aspirin enteric coated particle is composed of an aspirin drug-containing core and an enteric coating film wrapping the aspirin drug-containing core. The buffer matrix comprises one or more plastically deformable auxiliary materials, and the weight ratio of the buffer matrix in the second enteric-coated layer is 20-80%; and the coating weight gain of the enteric coating film is 20-100% of the weight of the drug-containing core of the aspirin. According to the invention, through the cooperation of triple technical means of the high-weight-gain tough enteric coating, the plastically deformable buffer matrix and precise particle size control, the problems of drug stability reduction, gastric irritation increase and poor content uniformity caused by easy membrane rupture in the double-layer tabletting process of the existing enteric particles are effectively solved.