41 results about "Drug crystals" patented technology

The invention discloses a low-water-solubility medicine crystal as well as a preparation method and application thereof. The compound Z pamoate crystal form I has large characteristic diffraction peaks at one or more positions with diffraction angles 2 theta of 9.9 + / -0.2 degrees, 10.7 + / -0.2 degrees, 12.1 + / -0.2 degrees, 14.9 + / -0.2 degrees, 17.3 + / -0.2 degrees, 19.4 + / -0.2 degrees, 20.7 + / -0.2 degrees and 23.1 + / -0.2 degrees. Compared with an amorphous compound Z pamoate, the crystal provided by the invention has the advantages of good stability, no crystal transformation phenomenon, no obvious increase of related substances and low solubility; the production process is simple, only water is used as a solvent in the whole process, and no organic solvent is used; when the long-acting slow-release anti-Parkinson medicine composition is prepared from the compound Z pamoate crystal form I, the medicine encapsulation efficiency is high, the burst release is low, the composition continuously releases the medicine in vivo for more than 2 weeks, the administration frequency of a patient can be reduced, and the medication compliance is improved.

The invention relates to the field of medicine crystal forms, in particular to a chidamide crystal form I and a preparation method thereof. The chidamide crystal form I has better stability, flowability and solubility, good bioavailability and lower hygroscopicity, has the advantage of patent medicine, and can be developed as a medicinal crystal form; the preparation method of the crystal form I is simple, good in repeatability, high in yield, easy to operate, green, environmentally friendly, small in needed solvent amount and beneficial to recycling, the reagent cost can be effectively reduced, and large-scale production is easy to achieve.

The application discloses a baicalin ternary co-amorphous drug and a preparation method and application thereof, and the amorphous substance can effectively improve the solubility and dissolution of puerarin and baicalin. The application mixes metformin hydrochloride, puerarin and baicalin according to a molar ratio of 1:1:1, and obtains the baicalin ternary co-amorphous drug through a ball milling method or a solvent-assisted milling method, the preparation method is green and efficient, the co-amorphous substance has high light stability and thermal stability, the solubility is increased by 1.7 times compared with that of a puerarin raw drug crystal, the solubility is increased by 46.8 times compared with that of a baicalin raw drug crystal, and the solubility is reduced by 14.8 times compared with that of a metformin hydrochloride raw drug crystal. The baicalin ternary co-amorphous drug has certain application prospects in liver protection, blood sugar reduction, treatment of damp-heat type colitis and cervical cancer.

The present invention relates to a coating material for drug-coated balloons, drug-coated balloons, and a coating solution for drug-coated balloons, as well as their preparation and application. The coating solution comprises an aqueous solvent and a plurality of core-shell structures dispersed in the aqueous solvent, each of which comprises a lipid bilayer coated with a drug. The core of the core-shell structure contains a plurality of drug-loaded particles, and the shell of the core-shell structure is a lipid bilayer with an outer hydrophilic group and an inner hydrophobic group. The drug-loaded particles comprise a plurality of drug-loaded nanocrystalline particles. The combination of nanocrystals and liposomes combines the advantages of these two types of drug carriers. The resulting lipid bilayer improves the solubility of poorly soluble drugs in drug-coated balloons, resulting in a high drug loading capacity, high drug carrier stability, and stable drug crystal form, allowing for controllable drug release rates.

Provided is a balloon catheter with which a drug transferred from a balloon to a blood vessel wall does not easily separate from the blood vessel wall.　This balloon catheter has a balloon (20). The balloon (20) has a balloon body part (30) having a longitudinal direction x and a radial direction y, and a drug layer (40) that is disposed outward of the balloon body part (30) in the radial direction y and contains a drug. The drug layer (40) has a radial crystal group (42) including a plurality of columnar crystals (41) of the drug arranged radially. In a cross section in the longitudinal direction x, the radial crystal group (42) has a fan shape, and the central angle θ of the fan shape exceeds 180°.

The invention relates to a rapid identification method for a crystal form of a complex mixture conjugated estrogen drug obtained by separation and purification of a natural pregnant mare urine source, and adopts a scanning electron microscope-confocal microscopy ramann coupling technology to determine a natural conjugated estrogen bulk drug and a preparation thereof. And carrying out difference analysis with conjugated estrogen from a synthesis source. According to the detection method, a microscopic area is positioned through a scanning electron microscope, fixed-point chemical analysis is performed through confocal microscopic Raman, the corresponding relation between morphology and crystal form is revealed, and the method is high in spatial resolution (micron level), high in specificity and good in reproducibility. Therefore, the method can be used for simply, quickly and accurately detecting the characteristic peak of the sample to be detected, reveals the special molecular arrangement mode and crystal structure characteristics of the conjugated estrogen drug produced by a specific process, and has a very good application prospect in the field of crystal form quality control of the drug.

The invention relates to the technical field of medicine crystal forms, and particularly discloses a novel crystal form of an AXL kinase inhibitor, a dextro-camphorsulfonate crystal form I and a dextro-camphorsulfonate crystal form II are prepared, and the dextro-camphorsulfonate crystal form I and the dextro-camphorsulfonate crystal form II are both anhydrides and have good physical stability and chemical stability. After the camphor sulfonate crystal form I and the camphor sulfonate crystal form II are placed under the conditions of high temperature (60 DEG C), high humidity (92.5% RH) and illumination for 10 days, the appearance of the camphor sulfonate crystal form II has no obvious change and has no obvious difference in 0 day, and compared with the camphor sulfonate crystal form I and the camphor sulfonate crystal form II, the camphor sulfonate crystal form II is more stable in thermodynamic stability tests in ethanol and methanol supersaturated solutions.

A pharmaceutical crystal having low water solubility, a preparation method therefor, and the use thereof. A crystal form I of pamoate of a compound Z has characteristic diffraction peaks at the diffraction angles 2θ of 9.9±0.2°, 10.7±0.2°, 12.1±0.2°, 14.9±0.2°, 17.3±0.2°, 19.4±0.2°, 20.7±0.2° and 23.1±0.2°. Compared with amorphous pamoate of the compound Z, said crystal has good stability, is free of polymorphic transformation, does not involve obvious increases of related substances, and has a low solubility. A production process therefor is simple and only uses water as a solvent in the whole process without the need of using an organic solvent. Using the crystal form I of pamoate of the compound Z for preparing a long-acting sustained-releasing pharmaceutical composition for Parkinson's disease can achieve a high drug encapsulation ratio and low burst release, and enables drug release of the composition in vivo to last for over two weeks, so that the frequency of drug administration to patients can be reduced, and the medication compliance is improved.

The utility model relates to the field of plant area sweeping, and discloses a cement plant area medicament adding area sweeping system which comprises a sweeping device, supporting rollers are symmetrically arranged on the edge of one side of the sweeping device, a supporting holding rod is fixedly installed on one side of the upper surface of the sweeping device, and guide supporting rods are symmetrically welded to the two sides of the inner wall of the sweeping device. A movable support is movably installed on the outer surface of the guide supporting rod in the sweeping device, the bottom end of the movable support extends to the position below the sweeping device to be provided with a sweeping brush head, a fixed sliding groove is formed in one side of the inner wall of the sweeping device, and the middle of one side of the movable support penetrates through the fixed sliding groove to be fixedly connected with a connector. According to the cleaning device, the cleaning brush head is adjusted to reciprocate along the lower portion of the cleaning device, so that the effect of conveniently cleaning the drug crystals in the drug adding area is achieved, the cleanliness of the road surface in the drug adding area is improved, the problem that the drug crystals are bonded to the road surface and are inconvenient to clean is solved, and the overall cleaning efficiency of the drug crystals is improved.

The application relates to a microfluidic chip with a substrate surface functional modification and a crystallization control method, which solves the technical problem of how to apply the microfluidic chip to precisely control the crystallization process, and comprises a substrate and a cover plate, the substrate is provided with patterned SAMs, the cover plate comprises an upper layer and a lower layer, the upper layer is provided with a gas passage and a gas containing chamber, the upper layer is provided with a gas input through hole, a gas output through hole, a liquid input through hole and a liquid output through hole, the lower layer is provided with a liquid passage and a reaction chamber, the lower layer of the cover plate is bonded with the substrate, and the patterned SAMs are located in the reaction chamber. The application is suitable for precise preparation of drug crystals, biological materials, ceramic materials, nanometer materials and optical elements, and can be widely applied to the pharmaceutical industry, biomedical engineering, advanced material synthesis and other industries.

The invention relates to the field of medicines, and discloses a pharmaceutical composition for treating obstructive sleep apnea as well as a preparation method and application thereof. The pharmaceutical composition comprises a ternary co-amorphous compound containing zinc ions, and raw materials of the ternary co-amorphous compound comprise suthiamethoxam, L-arginine, a divalent zinc ion donor and a surface stabilizer. Wherein zinc ions form a cross-linked network with the suthiamethoxam and the L-arginine through coordination, so that drug lattices are destroyed, and molecular movement is limited. According to the preparation method, a liquid-assisted high-energy mechanical ball milling process is adopted, a trace amount of coordination catalytic liquid is added to reduce a solid-phase reaction energy barrier, and efficient conversion from a crystalline state to an amorphous state is realized. Through the synergistic effect of multiple components, the saturation solubility and the dissolution rate of the suthiamethoxam are remarkably improved, meanwhile, the coordination crosslinking of zinc ions and the steric hindrance effect of the surface stabilizer are utilized, crystal transformation of an amorphous system is effectively inhibited, and the physical stability and oral bioavailability of the medicine are enhanced.

The present disclosure includes methods for forming pharmaceutical crystals of narrow particle size distribution and desired size and morphology, including a recrystallization step and subsequent resizing step.

This invention provides a sulfathiazole-trimethoprim drug crystal salt, its preparation method, and its application, belonging to the field of drug crystal salt technology. The sulfathiazole-trimethoprim drug crystal salt provided by this invention is orthorhombic with a space group of [space group missing]. P bca; cell parameters are: a =17.3213(3)Å, b =12.2894(2)Å, c =23.7549(3)Å, α =90°, β =90°, c =90°; wherein the molar ratio of sulfathiazole to trimethoprim is 1:1, and there is no crystallizing solvent. The sulfathiazole-trimethoprim drug crystal salt provided by this invention has high solubility in water, which is beneficial to improving absorption and metabolism in humans and animals, and has excellent antibacterial effect.

The invention relates to a substrate surface functionalization modified micro-fluidic chip and a crystallization control method, and solves the technical problem of how to use the micro-fluidic chip to accurately control the crystallization process, the substrate comprises a substrate and a cover plate, the substrate is provided with patterned SAMs, the cover plate comprises an upper layer and a lower layer, the upper layer is provided with a gas channel and a gas accommodating chamber, and the lower layer is provided with a gas outlet. The upper layer is provided with a gas input through hole, a gas output through hole, a liquid input through hole and a liquid output through hole, the lower layer is provided with a liquid channel and a reaction chamber, the lower layer of the cover plate is bonded with the substrate, and the patterned SAMs are located in the reaction chamber. The method is suitable for precise preparation of drug crystals, biological materials, ceramic materials, nanometer materials and optical elements, and can be widely applied to the industries of pharmacy, biomedical engineering, advanced material synthesis and the like.

The present application belongs to the field of chemical engineering and medicine manufacturing, and particularly relates to a method for regulating drug crystal form by oxidizing nanocellulose and application. By inducing the generation of sulfathiazole crystals in TCNF solutions with different concentrations, the nucleation and growth process of the sulfathiazole crystals is controlled, so that different morphologies and structures of the sulfathiazole crystal forms are obtained, and the transformation of the sulfathiazole crystals from flaky, prismatic to regular hexagonal crystal forms is realized. The sulfathiazole crystal form prepared by the method has better crystal morphology and consistency, the method is simple and effective, is suitable for crystal form optimization and large-scale production of polymorphic drugs, and has important industrial application value.

The present disclosure is directed toward composite materials comprising high aspect ratio habits of drug crystals which can be partially or fully extending into a substrate, and additionally, can be projecting from a substrate at an angle of about 20° to about 90°. The present disclosure is directed toward medical devices, such as medical balloons, comprising said composite and methods of using and making the same. The described composite can be used for the local treatment of vascular disease. The present disclosure is also directed toward paclitaxel crystals with a hollow acicular habit.

The present application belongs to the technical field of pharmaceutical crystal, and relates to a solid salt type, a crystal form of an opioid receptor antagonist conjugate and a preparation method, a composition and a use thereof. Specifically, the conjugate has a structure as shown in formula I, and can form a stably existing solid phosphate salt, wherein the molar ratio of phosphoric acid to the compound of formula I is 1:1-3:1. The phosphate salt can be an amorphous substance or a polymorph having crystal form 1, 2, 3 or 4, and the preparation method is simple and easy to operate, and is suitable for preventing and treating intestinal function disorders caused by opioid drugs, such as constipation.

To develop pharmaceutical crystals suitable for formulation of a compound.SOLUTION: Polymorphic forms of a compound and a preparation method therefor and an application thereof are disclosed. A crystal form III of a compound A uses Cu-Kα radiation, and X-ray powder diffraction expressed at 2θ angles has characteristic peaks at 12.15±0.20°, 15.98±0.20°, 16.62±0.20°, 17.14±0.20°, 24.32±0.20°, and 26.08±0.20°. A crystal form VII of the compound A uses Cu-Kα radiation, and X-ray powder diffraction expressed at 2θ angles has characteristic peaks at 12.94±0.20°, 14.41±0.20°, 15.64±0.20°, 17.25±0.20°, 21.75±0.20°, and 24.23±0.20°. The polymorphic forms prepared by the present invention are good in stability, and can be stably stored under the conditions of high temperature and low relative humidity.SELECTED DRAWING: Figure 28

The application relates to the field of drug crystal forms, in particular to a new crystal form of a compound of formula I and a preparation method thereof. The crystal form II of the compound of formula I has the comprehensive advantages of good physical and chemical stability, low moisture absorption, good solubility and bioavailability, and thus has certain drug property and drug development value. In addition, the preparation method of the crystal form II of the compound of formula I is simple in steps, mild in conditions, good in process repeatability, high in purity and low in cost, and is suitable for industrial large-scale production.

The invention relates to the field of medicine crystal forms, in particular to an orselidine fumarate crystal form I. The obtained crystal form I has good physical stability and chemical stability, extremely low hygroscopicity and good solubility and can be developed as a raw material medicine, and the preparation process provided by the invention is simple, good in repeatability, excellent in purification effect and good in process amplification stability and can be used for industrial large-scale amplification production.

The application belongs to the technical field of pharmaceutical crystal, and relates to a crystalline form of nervonic acid and a preparation method thereof. In the X-ray powder diffraction pattern of the crystalline form, Cu-Kalpha radiation has characteristic peaks at diffraction angles 2theta of 5.2+ / -0.2, 8.8+ / -0.2, 12.4+ / -0.2, 16.0+ / -0.2, 19.2+ / -0.2, 23.9+ / -0.2 and 25.2+ / -0.2. The crystalline form provided by the application has good chemical purity and crystal stability, and exhibits excellent physical stability, which is beneficial to the development, production and storage of pharmaceutical preparations. In addition, research shows that the crystalline form also has suitable solubility characteristics, which is beneficial to improving the bioavailability and more beneficial to the related research and development of drugs.

The invention discloses a controlled release preparation and a preparation method thereof. Specifically, the controlled release preparation comprises a drug crystal and a polymer coating wrapping the drug crystal, the preparation method of the controlled release preparation comprises the following steps: carrying out polymerization reaction on a monomer on the surface of a drug crystal to form a polymer coating, or carrying out cross-linking reaction on a polymer on the surface of the drug crystal to form the polymer coating. The controlled release preparation is high in drug loading capacity, long in drug release time, capable of achieving long-acting zero-order release of drugs, simple in preparation method and high in encapsulation efficiency.

The invention relates to a capsaicin and local anesthetic liquid eutectic and a composition thereof, and more specifically, the capsaicin and local anesthetic liquid eutectic comprises (a) capsaicin; (b) local anesthetics; (c) water; wherein the molar ratio of the component (a) capsaicin to the component (b) local anesthetic is (1: 0.5)-(1: 10), preferably (1: 0.6)-(1: 6), and more preferably (1: 0.75)-(1: 5); the component (c) accounts for at least 1%, preferably at least 3%, preferably at least 5% and more preferably at least 6% of the mass percent of the eutectic; the invention also discloses a pharmaceutical composition containing the eutectic, the eutectic is stable at room temperature, and the further prepared pharmaceutical composition is free of drug crystal precipitation after being placed for a long time, and is stable and controllable in quality.

The present disclosure is directed toward composite materials comprising high aspect ratio habits of drug crystals which can be partially or fully extending into a substrate, and additionally, can be projecting from a substrate at an angle of about 20° to about 90°. The present disclosure is directed toward medical devices, such as medical balloons, comprising said composite and methods of using and making the same. The described composite can be used for the local treatment of vascular disease. The present disclosure is also directed toward paclitaxel crystals with a hollow acicular habit.

The invention relates to a high-concentration capsaicin composition, and more specifically, the composition comprises capsaicin and menthol, further comprises a high polymer material and an emulsifier, further comprises oil, and further comprises one or more of a thickening agent, a humectant, a preservative and an antioxidant. The composition does not need to use an organic solvent, contains high-concentration capsaicin, is free of drug crystal precipitation after being placed for a long time, is controllable in quality, and also has the beneficial effect that the transdermal rate is obviously higher than that of common cream.

The invention relates to the field of medicine crystal forms, in particular to a new crystal form of a fenerenone acetic acid solvate. The novel crystal form prepared by the invention has the characteristics of higher solubility, better flowability, safety and medicinal property. Meanwhile, the preparation method is stable, good in reproducibility and suitable for industrial production.

The invention belongs to the technical field of medicine crystals, and provides a colchicine eutectic crystal and a preparation method and application thereof, and the colchicine eutectic crystal comprises a eutectic substance of colchicine and tartaric acid. The colchicine eutectic crystal is good in fluidity, the solubility is effectively improved compared with a raw material medicine, and the photo-thermal stability is remarkably improved. The preparation method of the colchicine eutectic crystal is simple in process and suitable for industrialization.

The invention relates to the field of medicine crystal forms, in particular to an albendazole-acesulfame potassium salt crystal form A, a preparation method and application. The molar ratio of the albendazole anion to the acesulfame cation in the salt structure is 1: 1. The crystal form A of the albendazole-acesulfame potassium salt prepared by the preparation method disclosed by the invention has relatively good dissolving property and relatively good flowability. Meanwhile, the preparation method is simple, good in reproducibility, low in cost and environment-friendly.

The invention discloses a new crystal form of fenerenone, a preparation method and application. The invention relates to the field of medicine crystal forms, in particular to a novel crystal form of a fenerenone N-methyl pyrrolidone solvate. The novel crystal form prepared by the invention has higher apparent solubility and better flowability. Meanwhile, the preparation process is stable, good in reproducibility and suitable for industrial production.

The invention relates to the field of medicine crystal forms, in particular to a bezafibrate-L-lysine salt hydrate crystal form A and a preparation method thereof. In the bezafibrate-L-lysine salt hydrate crystal form A, the molar ratio of L-lysine cations to bezafibrate anions to water molecules is 2: 2: 3. According to the bezafibrate-L-lysine salt hydrate crystal form A prepared by the invention, the solubility and intrinsic dissolution rate of bezafibrate crystal form alpha in water can be improved, and the bezafibrate-L-lysine salt hydrate crystal form A has relatively good flowability. Meanwhile, the preparation method is simple, the reproducibility is good, the cost is low, no pollution is caused to the environment, and the application value is achieved in development of drugs for treating hyperlipidemia.