82 results about "Pidotimod" patented technology

The invention discloses a synthesis method of pidotimod. The synthesis method comprises the following steps: reacting L-cysteine with paraformaldehyde or formaldehyde to generate L-thiazolidine-4-carboxylic acid, performing esterification to generate L-thiazolidine-4-carboxylate, or reacting L-cysteine ester hydrochloride with paraformaldehyde or formaldehyde to generate L-thiazolidine-4-carboxylate; and then carrying out condensation reaction on L-thiazolidine-4-carboxylate and L-pyroglutamic acid to generate (4R)-3-[[(2S)-5-oxo-2-pyrrolidinyl]carbonyl]-4-thiazolidine carboxylate, and then synthesizing pidotimod through hydrolysis reaction. Compared with the prior art, the technology in the invention is simple, is easy to operate, has high product yield and low production cost, is environmentally friendly and is suitable for industrial production.

The invention relates to a medical composition which is composed by antibiotic and pidotimod by the mass ratio of 1:0.01-15. The medical composition can be composed by the antibiotic and the pidotimod which are both compound preparation or by the antibiotic and the pidotimod which are independent medical preparation and are packaged in the same medicine box. The medical composition has the advantages that if the pidotimod or the derived salt thereof which is immunopotentiator can be supplied when the antibiotic is used for treating the bacterial infection, the treating effect of the antibiotic can be well improved, the antibiotic and the pidotimod can take effect synergistically, and the use amount of the antibiotic is reduced or the use period is shortened. The invention further discloses the preparation method and the medical application of the medical composition.

The invention discloses a pidotimod liposome solid preparation and a preparation method thereof. The pidotimod liposome with excellent quality is prepared by selecting pidotimod, phosphatidylinositol, cholesterol, stigmasterol and cremophor HEL 40 in specific weight ratios and then the pidotimod liposome is prepared into the solid preparation by a common preparation method. The liposome solid preparation and preparation method provided by the invention have the following beneficial effects: the liposome solid preparation has high encapsulation efficiency and uniform grain size; the retention time of medicaments in blood circulation is long; and the preparation method is simple and practical, is beneficial to improvement of the product quality and reduction of the toxic or side effect and is suitable for industrial large-scale production.

The invention provides a Pidotimod solution for intravenous injection, which comprise reactive compound of ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid by a content of 0.4-200mg / ml, solvent for injection and solubilizing agent for injection, the solvent for injection comprises water, non-water solvent or their mixture.

The invention discloses an injection containing Pidotimod sodium. Pidotimod and sodium hydroxide in equal mol are reacted in water or alcohol or mixed liquid of the water and the alcohol to generate the Pidotimod sodium, and then the Pidotimod sodium is prepared into the injection. The chemical name of the Pidotimod sodium is (R)-3-[(S)-(5-oxy-2-pyrrolidinyl) carbonyl]-thiazolidine-4-sodium carboxylate, the molecular formula is C9H11N2O4SNa, and the molecular weight is 266.28. The injection is characterized in that the active component Pidotimod in the injection exists in the form of Pidotimod sodium salt, and pH value of the solution is between 4 and 6. The injection can be prepared into transfusion solution for intravenous administration, and can be added into injection containing 5 percent glucose or 0.9 percent sodium chloride and into dissolvent crystallization subpackaged powder injection and frozen dried powder injection.

The invention relates to a method for preparing pidomud disperser and relative application. The invention comprises the active components as pidomud, adhesive, disintegration agent, stuff, and lubricant and sweat agent. The invention also provides relative preparation and application. The inventive disperser has better disperse state, short disintegration time and quick release, or the like, while it can be orally taken, eaten or mixed in water.

The invention provides an oral liquid preparation of pidotimod, which can promote immunoreaction of a human body, effectively reduces times and degree of treating acute attack of bacteria or virus induced infection, shortens the course of the disease, can serve as an auxiliary medicine of antibiotic during acute infection and belongs to the field of medicines. The oral liquid preparation comprises the pidotimod, a chemical stabilizer, a pH regulator, a flavoring agent and the like, wherein trihytdroxy methyl-aminomethane serves as the pH regulator; and stability of the solution can be effectively improved through quantitative proportion and synergistic effect of each ingredient. The oral liquid preparation has stable quality, is convenient to store for a long time and is particularly suitable for old people or children to take.

The invention provides a pidotimod-containing pharmaceutical composition and a preparation method thereof. The pidotimod-containing pharmaceutical composition consists of pidotimod and any antibacterial medicament. The antibacterial medicament may be any of beta-lactams (including as penicillins, cephems and unclassical beta-lactams), aminoglycosides, polymyxins, macrolides, lincomycins, norvancomycins, tetracyclines, chloromycetins, artificial antibacterial medicaments (including sulfonamides, quinolones and furofurans), cholesterols and antiviral medicaments. The unit dosage of the pidotimod is 0.1 to 2 grams, preferably 0.4 to 0.8 gram. The dosage of the antibacterial medicament is determined according to the dosage range of the antibacterial medicament. The composition of the pidotimod and the antibacterial medicament can exogenously and directly kill pathogenic bacteria through the antibacterial medicament and mobilize endogenous anti-infection immunity through an immunomodulator to improve anti-inflection effect, and has excellent synergy.

The invention discloses an injection containing a pidotimod potassium salt and a preparation method thereof. The preparation method comprises the following steps of: undergoing reaction between pidotimod and potassium hydroxide with equal mole in water or other solvent or a mixed solution of multiple solvents, preparing the pidotimod potassium salt and then preparing the injection. The injection containing the pidotimod potassium salt is characterized in that the effective component, the pidotimod, in the injection exists in the form of the pidotimod potassium salt, thus the solubility and the stability of the pidotimod in normal pH environment of a human body are improved. The injection containing the pidotimod potassium salt, disclosed by the invention, is used for treating the recurrent upper and lower respiratory tract infection (such as pharyngitis, tracheitis, bronchitis and tonsillitis), the recurrent infection (such as rhinitis, nasosinusitis and otitis), the urinary infection and gynecological infection, and can reduce the times of acute exacerbation, shorten the course of disease and relieve the degree of exacerbation; in addition, the injection can be also taken as the auxiliary treatment of antibiotics during the acute infection.

The invention provides an improved preparation method of pidotimod. According to the improved preparation method, a mixed anhydride method is adopted, and the improved preparation method comprises the following steps: under alkaline conditions, enabling L-pyroglutamic acid, ethyl chloroformate and L-thiazolidine-4-carboxylic acid to react, then acidifying, refining and devitrifying to prepare pidotimod. The method has the advantages of simplicity and convenience in operation, high yield and high product purity, and is more suitable for industrial production.

A pidotimod soft capsule is prepared from pidotimod and assistant chosen from diluent, cosolvent, solubilizer, suspending aid, and surfactant through proportional mixing, preparing soft capsule, solidifying by cooling in wind, drying, washing with proper solvent and drying.

The invention relates to immunologic stimulant oral syrup and a preparation method thereof. Each 100ml of immunologic stimulant oral syrup is prepared from the following raw materials by weight: 2 to 8g of pidotimod, 35 to 65g of sucrose, 0.5 to 1.5g of pH regulator, 0.02 to 0.06g of ethyl hydroxy benzoate, 0.6 to 1.8g of ethanol, 0.01 to 0.08g of essence and the balance of purified water, wherein the PH regulator is any one of anhydrous sodium carbonate, sodium carbonate, sodium hydroxide and sodium bicarbonate; and the essence is any one of ethyl maltol, lemon essence, banana essence, grapefruit essence and orange essence. The immunologic stimulant oral syrup has the characteristics of quick response, sweeter taste and better mouthfeel, is convenient to take and is particularly suitable for oral administration of infants and the elderly with low immune functions.

The invention provides a related medicinal composition of antiviral medicament and pidotimod. The mass ratio of the antiviral medicament to the pidotimod is 1: (0.01-10). The medicinal composition of the invention comprises two combination modes, namely in the first combination mode, the antiviral medicament and the pidotimod are prepared into a compound preparation; and in the second combination mode, the antiviral medicament and the pidotimod are prepared into an individual medicinal preparation respectively, and the two individual medicinal preparations are packed into the same medicinal box. The medicinal composition has the advantages that the medicinal composition can well improve the treatment effect of the antiviral medicament, play a role in synergy and reduce the using amount or the application treatment course of the antiviral medicament by providing the pidotimod or derivative salt thereof as immune promoter medicament at the same time when the antiviral medicament is used for treating viral infection. The invention further provides a preparation method for the medicinal composition and medicinal application thereof.

The invention discloses a Timicosin compound preparation and a preparation method and use thereof, which relate to the field of livestock breeding. The Timicosin compound preparation comprises the following components: Timicosin and Pidotimod. The invention also provides the preparation method and use of the Timicosin compound preparation. The Timicosin compound preparation provided by the invention is simple in composition and high in safety; and the Timicosin and Pidotimod in the compound preparation can produce a synergic effect in body, so that the Timicosin, at a lower use concentration, can reduce the number of the blue ear disease viruses in the bodies of newly borne piglets by inhibiting the blue ear disease virus content in the body of sows and thus improves the immunity in the bodies of the piglets and the indexes of the productivity of the piglets and reduce breeding benefit. The Timicosin compound preparation prepared by the invention can be used for breeding sows in a pregnant or lactation period. In addition, the preparation method provided by the invention is simple, and the prepared Timicosin compound preparation is stable.

The invention discloses an application of pidotimod as a medicine used for treating livestock and poultry immunosuppressive diseases. According to the invention, pidotimod is added in drinking water or feedstuff of livestock and poultry such as pig, chicken, cattle, sheep, and the like, wherein the concentration of pidotimod is 10-1000ppm. With the technical scheme provided by the invention, livestock and poultry immune functions can be enhanced, growth can be promoted, and various livestock and poultry immunosuppressive diseases can be prevented and treated.

The invention provides a preparation method of a pidotimod crude drug. The preparation method mainly comprises a condensation reaction and a hydrolysis reaction. The preparation method provided by the invention has the advantages of simplicity and convenience, easiness in operation, low environmental pollution, stable process, good repeatability, high product yield, high product purity and few impurities.

The invention provides a synthesis method of pidotimod disclosed as Formula (1). The synthesis method comprises the following steps: (1) carrying out condensation reaction on thioproline and cyprolidol under the actions of a catalyst and a condensation reaction solvent to obtain an intermediate I; (2) carrying out condensation reaction on the intermediate I and pyroglutamic acid under the actions of a catalyst and a condensation reaction solvent to obtain an intermediate II; and (3) dropwisely adding an acidic material into the intermediate II, and carrying out degreasing reaction in a degreasing reaction solvent. The synthesis method avoids using thionyl chloride, pentachlorophenol and other toxic reagents, and thus, has favorable environment friendliness. The method does not need strong alkali high-temperature esterolysis, so the synthesis process is milder. The intermediate I and intermediate II can absorb ultraviolet light, so that the whole synthesis progress can be monitored conveniently. In addition, the optical purity of the pidotimod prepared by the synthesis method is higher.

The invention provides a pharmaceutical composition for treating or / and preventing pet viral diseases. The pharmaceutical composition provided by the invention is a preparation prepared from the following medicinal raw materials in parts by weight: 25-50 parts of enrofloxacin, and 50-75 parts of pidotimod. The invention further provides a preparation method and use of the pharmaceutical composition. The pharmaceutical composition provided by the invention is used in the infection period of canine viral diseases and is capable of preventing secondary infection while increasing immunity; the pharmaceutical composition can be used for preventing epidemic viral diseases of infectious diseases; the pharmaceutical composition is initiatively taken by dogs; a way is unnecessary for a dog to find to take the pharmaceutical composition; and the process is simple to operate.

The invention relates to a pidotimod synthesis method and belongs to pure liquid phase synthesis. The method comprises the step that carboxyl group R protected L-thiazolidine-4-carboxylic acid ester or L-thiazolidine-4-carboxylic acid and nitrogen R1 protected pyroglutamic acid are condensed under a catalyst, namely, R2-substituted boronic acid, and the target compound pidotimod as shown in the general formula III is formed. A high-purity product can also be obtained by recrystallization. The invention also discloses an application of R2-substituted boronic acid in synthesis of pidotimod. With the adoption of the method, the synthesis cycle is greatly shortened, the mechanism of formation of oxazolidinone from all polypeptides with a traditional method is avoided, the problem of racemization is solved completely, the catalyst can be reused, and accordingly, the cost is greatly reduced, the yield is high, the product purity is good, and the method is applicable to industrial production.

The invention relates to a quality detection method for preparation of pidotimod. A pidotimod-containing reaction product is prepared by performing ionization, condensation and hydrolysis reaction insequence on L-sulfur-proline ethyl ester hydrochloride and L-pyroglutamic acid which are used as reactants. The quality detection method is characterized in that high-performance liquid chromatography-based measurement for the reaction product shows that a peak area of a compound A included in the reaction product is no more than 0.1 percent, and a peak area of a compound B included in the reaction product is no more than 0.1 percent. The compound A is of a structure as shown in Formula V, and the compound B is of a structure as shown in Formula VI. The quality detection method for preparationof the pidotimod is favorable for controlling the drug quality in a production process.

A compound medicine for treating infectious diseases is prepared from azimycin and Piduomode.

The invention provides a Pidotimod dry suspension which is composed of Pidotimod and an adjuvant, wherein the adjuvant comprises a filling agent, a suspending aid and a flavoring agent. The dry suspension is characterized in that the flavoring agent is a mixture of strawberry essence, trisodium citrate, sodium chloride and aspartame. The dry suspension has the advantages that the specific flavoring agent is adopted, thus well solving the taste problem of the Pidotimod dry suspension, and unexpectedly promoting the effect taking speed and facilitating the stability of the Pidotimod dry suspension.

The invention relates to seven-peptide produced with thymus gland five- peptide and pidotimod and the synthesizing method, beloning to chemical medicine production area. The method is to empoly solid synthesing method and connects five- peptide and pidotimod through amido bond. The invention is characterized in that the pidotimod is an artificially- synthesized high- purity dipeptide, which can promote non-specific immune response and specific reaction and is polyphase broad-spectrum immunologic enhancement agent, the new compound is synthesized through connection of carboxyl of pidotimod and amidol of arginine, the metabolic process of thymus gland five- peptide begins from amidol of arginine, so it protects amidol after connection withpidotimod, and changes traditional medicine type of thymus gland five- peptide, so the clinical value is great.

The invention relates to a composite agent of muxixacin and pidumode, used to treat bacterial infection. The agent comprises 100-800mg muxixacin and 200-1600mg pidumode, which are both made as composite agents, that directly kills bacterial externally via the muxixacin and improve anti-infection ability via the internal anti-infection immunity ability of pidumode, with better cooperate function and wide application on general clinical bacterial infections, controlling the generations of virus infection and other abnormal pathogene infections.

The present invention is directed to the use of pidotimod, or a physiologically acceptable salt thereof, to treat psoriasis. For the treatment of the present invention, pidotimod, or a physiologically acceptable salt thereof, may be administered either systemically or topically.

A compound medicine for treating venereal disease is prepared from Wannailuowei hydrochloride and Piduomode.

The invention discloses an oral liquid preparation capable of enhancing immunity, which can stimulate human immunoreaction, obviously reduce the emergent onset times and degree of infectious diseases, and shorten the development and progression courses of diseases. The oral liquid preparation contains components of pidotimod, chemical stabilizers, flavoring agents, and the like. The stability and flavor of the oral liquid preparation can be obviously improved through the quantitative proportion and synergic action by adopting water as a solvent, the bioavailability of the oral liquid preparation is obviously higher than that of a solid preparation, the dispersion degree is large, and the oral liquid preparation is more suitable for carrying and oral administration of old people or children.

The invention provides high concentration pidotimod oral liquid, which can promote human body immune response, effectively reduces times and degree of acute attack of infections caused by bacteria or virus, shortens disease course, can serve as auxiliary medicine antibiotic of acute infection and belongs to the field of medicines. The oral liquid contains constitutions of pidotimod, chemical stabilizer, a potential of hydrogen (pH) adjusting agent, a flavoring agent and the like. Tris-(hydroxymethyl)-aminomethane is used as the pH adjusting agent. The oral liquid is stable in quality and convenient to store for a long time. By means of quantitative proportioning and synergistic effect of all constitutions, when the concentration of the oral liquid is improved, simultaneously the stability and taste of the oral liquid are obviously improved. The oral liquid doesn't contain sugar capable of being absorbed and used by human bodies and is suitable for the old and children.

The invention discloses a pidotimod effervescent tablet and a preparation method thereof. The pidotimod effervescent tablet comprises the following components in parts by weight: 300 to 500 parts of pidotimod, 100 to 400 parts of filling agent, 100 to 200 parts of effervescent disintegrating agent, 5 to 15 parts of essence, 6 to 10 parts of lubricant, and a proper amount of adhesive. The preparation method comprises the following steps: weighing pidotimod and a filling agent according to abovementioned formula, sieving pidotimod and the filling agent by an 80-mesh sieve, evenly mixing, adding sodium chloride into a PVPK30 water solution (8%), then adding the solution into powder to prepare a soft material, sieving the soft material by a 24-mesh sieve, preparing granules, paving the granules on a disc, drying the granules in a drying box at a temperature of 60 DEG C, taking out the granules until the water content of the granules is qualified, adding an effervescent disintegrating agent, a flavoring agent, and a lubricant, evenly mixing, measuring the intermediate content, pressing the mixture to obtain tablets, and finally carrying out detection and packaging. The provided pidotimod effervescent tablet and the preparation method have the advantages that the concentration of pidotimod in the blood of human body is high, the bioavailability of pidotimod is increased, at the same time, the stability of the pidotimod effervescent tablet is very high, and the pidotimod effervescent tablet can be stored stably.