353results about How to "Reduce toxic and side effects" patented technology

The invention relates to a nano micelle of a biodegradable macromolecular-bonding Pt(IV) anti-cancer medicament and a preparation method thereof. The structural formula of the anti-cancer medicament is defined in the specification, wherein the biodegradable macromolecule is tri-block copolymer, namely polyethylene glycol-b-polyester-b-polylysine; and tetravalency platinum coordination compound Pt(IV) is connected with a side amino on the block of polylysine on a macromolecular carrier through alpha, omega-polyethylene glycol. The carrier is non-toxic and is water-soluble, thus being convenient for reacting with the platinum(IV) coordination compound in water phase; a nano micelle form can be formed through self assembly; a platinum(IV) coordination compound is reduced to platinum(II), namely, cis-platinum, Carboplatin or Oxaliplatin, and the anti-cancer effect is known; the synthesis of the nano micelle is easy; the reduction potential of platinum(IV) is low, so that the platinum(IV) can be rapidly reduced to platinum(II) in cancer cells to take treatment effect; and the platinum(IV) is connected to the side chain of the macromolecule rather than the end of a chain, a macromolecular chain can be connected with multiple platinum(IV)s, and the content of platinum can be as high as 10-20%.

The invention provides a low-concentration vesicular phospholipid gel formulation of a small-molecule peptide drug and also provides a preparation method of the vesicular phospholipid gel formulation of the small-molecule peptide drug. In the low-concentration vesicular gel formulation, the content of phospholipids ranges from 20% to 40%, and the small-molecule peptide drug with a molecular weight ranging from about 300 D to about 3300 D is encapsulated in the phospholipids. The low-concentration vesicular phospholipid gel formulation is available in various drug administration forms suitable for injection drug administration, external drug administration and the like, has good biocompatibility, high drug-carrying capacity and good stability, and particularly has a long-acting slow release effect.

The invention discloses a temozolomide freeze-dried preparation. Every 100ml of the preparation comprises 1 to 2,000 mg of temozolomide, 1 to 2,000 mg of solubilizer, 801 to 2,000 mg of polysorbate, 5 to 5,000 mg of mannitol, 1 to 2,000 mg of buffering agent, 0.5 to 1,000 mg of hydrochloric acid and the balance of water. The preparation of the invention overcomes the shortcomings of slow dissolving speed, poor redissolution, fussy operation and unqualified solution clarity of the freeze-dried preparation, has the technical effects that: the preparation of the invention has high redissolution; solid is completely dissolved to be clear and colorless by adding water into the freeze-dried preparation and shaking slightly; purity is over 99.5 percent and single impurity content is below 0.3 percent by detecting the purity and the content by using HPLC; through stability experimental investigation, relative substances and content of the preparation are not changed remarkably; and quality is stable.

The invention provides a ready-to-use adjuvant of livestock vaccines, preparation and applications thereof, belonging to the field of the adjuvant of livestock vaccines. The ready-to-use adjuvant is prepared from the following substances: 5-30 percent of oil, 0.1-10 percent of hydrophilic surfactant, 0.1-10 percent of oleophilic surfactant, 0.1-10 percent of polymeric micelle substance and 40-90 percent of water. The invention also provides a preparation method of the ready-to-use adjuvant, and the method comprises the following steps: respectively weighing the substances, mixing and then emulsifying, and degerming to obtain the ready-to-use adjuvant of the livestock vaccines. The invention also provides an oil-in-water type vaccine with the ready-to-use adjuvant. The ready-to-use adjuvant is an oil-in-water type adjuvant and has the advantages of simple ingredients, stable dosage form, convenience in use and easiness in injection. The preparation method of the ready-to-use adjuvant has a simple process and is low in cost, and the obtained dosage form is stable. The oil-in-water type vaccine has the advantages of long stable period, easiness in storage, good immune effect, protection period prolonging, easiness in injection and small side reaction.

The present invention discloses a transcutaneous plaster containing tulobuterol, its preparation method and application. The pressure-sensitive adhesive used by said invention is a hot-melt pressure-sensitive adhesive whose melting point is 50-250 deg.C. the described hot-melt pressure-sensitive adhesive is an adhesive made up by using thermoplastic polymer as main raw material, and hs the hot-melting and pressure-sensitive double characteristics. Said product contains no organic solvent, and its coating speed is quick, and its cost is low.

The invention provides an antitumor prodrug with novel amphiphilic hyper branched polyester as a carrier and a preparation method thereof. The novel biodegradable amphiphilic hyper branched polyester is constructed as being based on dimethylol propionic acid, an oligomer of glycolic acid or lactic acid and polyethyleneglycol or polyethylene glycol monomethyl ether. A peripheral functional group of the obtained hyper branched polymer is a hydroxyl group. The hyper branched polymer is reacted with estolide to be transformed into the hydroxyl group, the hydroxyl group is esterified with antitumor drug with the existence of condensing agent to obtain a prodrug of the antitumor drug. The introduction of the oligomer of the glycolic acid or the lactic acid or an alternative oligomer thereof improves the biocompatibility of drug carrier material, and the degrading speed of the oligomer in body is controlled by regulating the polymerization degree and the chemical composition of the oligomer to realize the action of controlling the release speed of the drug, so that the invention has very good drug sustained controlled release action and avoids the toxic side effect to normal cells caused by the burst release of the antitumor drug. The prodrug has an amphiphilic property, so that the prodrug can be made into a water-based preparation and improves the hydrophilicity of the antitumor drug greatly.

The invention relates to a lipidosome-polymer hybrid nano particle and a preparation method and an application thereof. The lipidosome-polymer hybrid nano particle comprises an amphiphilic polymer nano particle and a lipid bilayer coating the surface of the amphiphilic polymer nano particle as well as medicines embedded into the amphiphilic polymer nano particle and between the amphiphilic polymer nano particle and the lipid bilayer and having different water solubilities. The nano particle provided by the invention has a multi-layered structure to embed medicines with different water solubilities, thereby realizing a synergistic effect of different medicines. The particle is high in biocompatibility, can circulate in blood for a long time, has the targeted and sustained-release effects, improves the curative effect of the medicines and reduces the toxic and side effects of the medicines, and can be used as a carrier system of an anti-tumor medicine. The preparation method provided by the invention is simple in process, convenient in operating process, and can be produced in a small scale in a laboratory and also can be industrially produced in a large scale.

The invention provides an industrialized production method for high-purity decitabine. The method comprises the following steps of: 1, performing silanization reaction of 5-azacytosine, bis(trimethylsilyl)amine and trimethyl chlorosilane, which serve as raw materials, to prepare 2,4-bis(trimethylsilyl)-5-azacytosine; 2, performing reaction of the product obtained by the step 1 and 1-chloro-3,5-bis-(4-chlorobenzoyl)-2-deoxy-D-ribofuranose, which serve as raw materials, to prepare a crude product of 1-(3,5-bis-(4-chlorobenzoyl)-2-deoxy-beta-D-ribofuranose)-5-azacytosine; 3, dissolving the product obtained by the step 2 in a C5 to C7 hydrocarbon, stirring, filtering and drying to obtain a refined product; and 4, producing the high-purity decitabine by using the product obtained by the step 3, methyl alcohol and sodium methoxide as raw materials. The method overcomes the disadvantages of need of column purification, low purity, difficult industrial production in the prior art, and has the advantages of simple and convenient operation, small solvent consumption, small influence on the environment, low labor intensity, short period, high product purity, single impurity and less than 0.1 percent total impurity content.

The invention relates to complex paclitaxel and its derivates docetaxel intralipid which includes the following ingredients: paclitaxel or docetaxel, vegetable oil, solubilizing agent, lecithin, glycerine, and water for injection at a ratio of 0.5-10:10-100:10-100:10-20:20-25:700-950. The preparing method includes the following steps: stirring with high speed homogenating machine or ultrasonic oscillating to get the protogala; preparing the complex paclitaxel intralipid with high pressure homogenizer. The preparation is intralipid in O/W type which packages paclitaxel or docetaxel into the compound oil phase. The compound oil phase has good solubility for paclitaxel or docetaxel which has prevented the phenomenon of precipitation after diluting the emulsion; the ingredients of compound oil has the function of coordinated antitumous effect; it can also release the injecting irritative response, haemolysis and hypersensitiveness; it has the function of targeting which has increased the drug action.

The invention provides a Chinese traditional medicament composition emplastrum for curing rheumatism or rheumatoid diseases, which has the functions of nourishing liver and kidney, strengthening muscles and bones, dispelling rheumatism and dredging meridian, and is applicable to the patient having the symptoms of arthralgia for a long time and deficient body, arthralgia, local intumescence, rigidity and malformation, unfavorable flexion and extension, and rheumatoid arthritis. The efficacy composition of the invention is that the proportion by weight of the materials is radix rehmanniae 15-25, prepared radix rehmanniae 15-25, black aconite 10-20, japanese teasel 10-20, pubescent angelica 5-15, drynaria fortunei 10-20, cassia twig 5-15, ledebouriella root 5-15, barrenwort 10-20, gleditsia sinensis sting 5-15, sheep bone 15-25, clematis root 10-20, white peony root 10-20, common anemarrhena 10-20, processed cibotium barometz 10-20, safflower 5-15, and lycopodii herb 5-15. The emplastrum of the invention can be directly pasted on the affected part, thereby having convenient utilizing, quick execution and short period of treatment.

The invention provides an externally used medicine for expelling wind and clearing away cold, activating meridians to stop pain and a preparation method thereof. The medicine is prepared by 25 types of medicinal materials such as radix aconiti preparata, wild aconite root, nux vomica (processed), epimedium, achyranthes root, notopterygium root, cyrtomium fortunei, phellodendron, zaocys dhumnade, hairy antler, dipsacus root, dark plum, asarum, Chinese ephedra, cassia twig, safflower, acanthopanax, honeysuckle, earth worm, loranthus, licorice, drynaria (scald), anisetree bark, myrrh gum (processed) and red ginseng. The medicine links closely with pathogen and pathogenesis of a disease and a plurality of medicines are compatible reasonably, thus expelling wind and clearing away cold as well as activating meridians to stop pain. As an externally used cataplasm, the medicine is taken through skin, thus avoiding the irritation of an oral preparation to gastrointestinal tract; in addition, relatively slow percutaneous absorption process inevitably greatly mitigates drug toxicity to the whole body. Neither skin sensibility nor skin irritation occurs. Therefore, the transdermal drug delivery of new preparation improves the safety of medicine taking to a certain extent and provides new choices for safe clinical medicine use.

The invention provides a Chinese traditional medicine composition for treating tumor and a preparing method thereof. The Chinese traditional medicine composition is prepared from radix curcumae, agrimony, trogopterus dung, white vitriol, saltpeter, resina toxicodendri, bitter orange and nux vomica powder, wherein the nux vomica poser is prepared from strychnos alkaloid and auxiliary material, and the auxiliary material is one or a mixture of some of dextrine, starch, mannite, microcrystalline cellulose and calcium bicarbonate. The composition has functions of supporting healthy energy, cleaning heat and toxins, and the like, can regulate immune function of an organism, reduce side and toxic effects and combine cancer prevention with cancer treatment, thereby improving the treating effect for tumor.

The invention relates to nimodipine lyophilization dry emulsion for injection. Before freeze-dried or reconstituted, according to percentage concentration per 1000 ml of fat emulsion, the lyophilization dry emulsion contains 0.001 percent to 0.2 percent of nimodipine, 0.5 percent to 30 percent of oiliness solvent, 0.1 percent to 5 percent of emulsifier, 5 percent to 40 percent of the freeze-drying protective agent and 0.1 percent to 10 percent of isotonic regulator. The invention also relates to a preparation method of nimodipine lyophilization dry emulsion. The invention has the advantages that ethanol is avoided to decrease irritation; the product can be mixed with any proportion of water for injection, sodium chloride solution, glucose solution, blank fat emulsion or other aqueous solution without phenomena of precipitation or crystallization; in addition, compared with the fat emulsion, the lyophilization dry emulsion is more helpful to improve the stability of nimodipine and excipient of the nimodipine, thereby lowering the requirements of production, transportation and storage conditions and prolonging the period of validity.

The invention discloses a multifunctional carrier based on cytogenic vesicle in body fluid, a preparation method and an application. The method comprises the following steps: (1) collecting human body fluid, performing gradient ultra-centrifugation, removing supernatant and using sterile PBS heavy suspension for precipitating and (2) adding the cytogenic membrane vesicle from the body fluid, ultra-small luminescent material and electroporation buffer solution into an electric shock cup, uniformly mixing, placing onto an electroporation instrument and treating, placing under room temperature and repairing after the ending of electroporation, performing ultra-centrifugation and then using sterile PBS heavy suspension for precipitating, thereby acquiring the multifunctional carrier based on the cytogenic membrane vesicle from the body fluid and marked with the ultra-small luminescent material. The carrier is used for preparing a chemotherapeutic drug or gene therapeutic drug for treating or preventing tumor, has high biocompatibility, is convenient to carry various therapeutic drugs, is capable of effectively restraining tumor growth, is suitable for diagnosis and treatment of various innocent and malignant tumors and especially supplies a choice for the diagnosis and treatment of deep tumors in skull, thoracic cavity and abdominal cavity.

The invention belongs to the technical field of medicament and provides a Levetiracetam osmotic pump controlled-release tablet and a preparation method thereof. The invention consists of the accessory of the Levetiracetam playing the effect of release control and a semi-transparent membrane; in the invention, proper accessory and medicament are mixed to press a tablet core at first; then a layer of semi-transparent membrane is coated outside the tablet core; then at least one small hole is punched on the semi-transparent membrane so as to lead active matters to be released from the semi-transparent membrane, thereby controlling the release of the medicament. Compared with a common preparation, the controlled-release preparation prepared by the invention has the advantages of small wave range of the blood medicine concentration, reducing toxic and side effect, being taken once in one day and improving the compliance of sufferers. The controlled-release preparation is applied on the adjunctive therapy for the partial seizure of epileptics in clinic.

A Chinese medicine in the form of suppository for treating lumbar vertebra disease, lumbar intervertebral disc protrusion, tonic rachitis and hyperosteogeny is prepared from 10 Chinese-medicinal materials including astragalus root, capejasmine fruit, musk, cinnamon twig, etc through pulverizing, extracting in alcohol, filtering, concentrating by distilling, to obtain concentrated liquid, immersing catgut suture in physiologic saline, baking, shearing short, putting them in bottle, filling said concentrated liquid, sealing and magnetizing.

A combination preparation for remedying the gastroesophageal reflux disease (GERD) and the functional dyspepsia is characterized in that the prescription of the combination preparation consists of a proton pump depressor and a gastrointestinal power drug of itopride; the proton pump depressor is selected from one of a Pantoprazole, a Omeprazole, a Esomeprazole, a Lansoprazole, a Rabeprazole, a Tenatoprazole and a Leminorazole, wherein the Pantoprazole is preferential, and at the same time the neutral form of the basic salt of the proton pump depressor is also included, such as Na^plus, Mg^2plus, Ca^2plus, K^plus or Li ^plus salt and a pure optical stereoisomer of the proton pump depressor or an active metabolite of the proton pump depressor; the gastrointestinal power drug is the itopride and a ramification of the itopride or one of the medicinal salts of the itopride; in the combination preparation, the weight ratio of the Pantoprazole and the itopride is 2 to 5 to 2 to 7. The invention has important affect for remedying the gastroesophageal reflux disease and the functional dyspepsia, and the preparation method of the invention is simple and convenient; the cost is low; the invention is fit for being orally taken by the patient; the invention has good conformance performance, high curative effect, low recrudescence rate and little adverse reaction.

The invention discloses a pingyangmycin polyethylene glycol (PEG)-polycaprolactone (PCL)-polyethylene glycol (PEG) temperature-sensitive slow-release gel, as well as a preparation method and the application of the gel. The Pingyangmycin PEG-PCL-PEG temperature-sensitive slow-release gel mainly consists of two parts comprising PEG (polyethylene glycol)-PCL (polycaprolactone)-PEG (polyethylene glycol) co-polymer and Pingyangmycin, is liquid at room temperature, and is solid gel under the in vivo 37 DEG C condition; the gel system has significant slow-release effect, thereby having functions in prolonging the half-life period and the acting time of the Pingyangmycin, reducing drug concentration in plasma, and reducing systemic toxic and side effects. The gel can be formed in situ after the medicine is injected in a high-flow-speed vessel, and then location embolism is realized, and so as to realize the, and muscularization and closing of muscle is caused, so that the sclerotherapy and the interventional therapy are combined effectively, the gel has excellent biocompatibility and degradability, is beneficial for treating hemangiomas, vascular malformations and cancers, particularly, a new selection is provided to the treatment of the vein malformation and partial malformation of cancers.

The invention relates to application of artesunate as a drug for treating systemic lupus erythematosus, adopting the artesunate with a molecular formula of C19H2808 for treating the systemic lupus erythematosus. The invention overcomes the defects that the prior common drug for treating SLE, such as cyclophosphamide, glucocorticoid, mycophenolate mofetil, hydroxychloroquine sulfate, leflunomide, azathioprine and the like has multiple side effects, is expensive, influences the life quality of a patient and even causes the patient to die because of some side effects, and the like. The invention has the advantages of cheap raw materials, easy availability, non or low toxicity, no pollution, mature production technology of a artesunate finished product, stable and reliable quality and little toxic side effects. Through comparison and study on a lupus mouse show that the efficacy of the artesunate is superior to a contrast group with little side effect. Therefore, the artesunate has a favorable prospect to treat the systemic lupus erythematosus.

The invention relates to an amphiphilic self-assembled nanomicelle based on nano Low-generation PAMAM (polyamidoamine) dendrimer and application thereof, particularly obtained conjugating low-generation PAMAM dendrimer and a hydrophobic agent and self-assembling in water via ultrasonic vibration. The nanomicelle has active molecules or a prodrug with drug loading capacity; the chemical conjugation of the hydrophobic agent and the low-generation PAMAM dendrimer helps improve the defects of poor solubility of the hydrophobic drug and low bioavailability, and a new idea is provided to solve the problem that traditional clinical chemotherapeutics are high in toxicity and low in safety coefficient; the nanomicelle can also function as a nanocarrier to carry other hydrophobic drugs, enabling joint use of drugs and enhancing therapeutic effect.

A Chinese medicine for treating the tumor in digestive tract is proportionally prepared from 8 Chinese-medicinal materials including pseudostellaria root, Chinese angelica root, ganoderma, yam, etc.