28 results about "Desloratadine" patented technology

The invention discloses a method for determining impurities in a desloratadine oral solution, the impurities comprise a desloratadine impurity 1, the determination method adopts a high performance liquid chromatography, and the detection conditions of the high performance liquid chromatography are as follows: a chromatographic column is an octyl silane bonded silica gel column or an efficiency equivalent column; the detection wavelength is 254 + / -2nm; the detector is an ultraviolet detector; the column temperature is 35-45 DEG C; the flow rate is 1.1 to 1.3 mL / min; mobile phases: a dipotassium phosphate buffer solution, methanol and acetonitrile; the elution mode is isocratic elution. The determination method disclosed by the invention is good in specificity, good in separation degree, high in sensitivity and good in accuracy, can fully meet the requirements of impurity determination, has important meanings for evaluating the quality of raw material medicines and the advantages and disadvantages of a preparation process, controlling the quality of a final product and detecting a stable sample, and is high in practicability in actual quality control work.

To provide a desloratadine solid preparation that suppresses the time-dependent increase in analogs and exhibits superior stability.SOLUTION: The present invention provides a desloratadine solid preparation containing desloratadine and arginine, thereby suppressing the time-dependent increase in analogs, particularly N-formyl desloratadine. The solid preparation is preferably an orally disintegrating tablet.SELECTED DRAWING: None

The present invention combines the drugs desloratadine and betamethasone in a single dosage unit, which represents a set of important technological challenges due to the physicochemical properties and the difference in doses to guarantee obtaining a stable product for the treatment of allergic and inflammatory processes in a subject.

The invention discloses a synthesis method of a 2-amino-3-trifluoromethyl naphthoquinone compound, which comprises the following steps: by taking a 1, 4-naphthoquinone compound, a Togni reagent and alkylamine as substrates, stirring in the dark at room temperature under the promotion of a proper amount of alkali to realize the construction of the 2-amino-3-trifluoromethyl naphthoquinone compound. The synthesis method has the prominent advantages that the substrate is cheap and easy to obtain, the reaction condition is mild, the operation is simple, the product is diversified and the like, and the synthesis method can be applied to derivative modification of drug molecules such as doxazosin (Doxazosin), levocetirizine (Levocetirizine), risperidone (Risperidone), desloratadine (Desloratadine) and paroxetine (Paroxetine).

The present application relates to a kind of HPLC-MS / MS detection method of detecting in human plasma, desloratadine and 3-hydroxydesloratadine in human plasma, it includes the following steps: (1) human plasma sample pretreatment;(2) liquid chromatography-mass spectrometry detection, using mobile phase A and mobile phase B as mixed mobile phase is carried out gradient elution, wherein: mobile phase A is methanol-acetonitrile mixed solution, in mixed solution methanol and acetonitrile volume ratio is 4-6:6-4;Mobile phase B is 2-20mM ammonium formate aqueous solution;(3) the determination of the concentration of human plasma in lopatadine, desloratadine and 3-hydroxydesloratadine.The present application uses lopatadine-d4, desloratadine-d5, 3-hydroxydesloratadine-d4 as deuterium internal standard, using Agilent, ZORBAX Eclipse XDB-Phenyl is carried out gradient elution, deuterium internal standard and the measured substance has the same retention time, chemical property and matrix effect, the reproducibility, accuracy of determining the concentration of lopatadine, desloratadine and 3-hydroxydesloratadine in plasma are good.The method of the present application can be used to evaluate the bioequivalence of lopatadine.

The present invention provides a derivative having a desloratadine tetravalent platinum structure, a preparation method, and a use thereof. The compound having a desloratadine tetravalent platinum structure is shown in general formula (I), #imgabs0# wherein #imgabs1# is selected from cisplatin or oxaliplatin; L is hydroxyl or #imgabs2#. The desloratadine tetravalent platinum compound of the present invention has good anti-tumor proliferation activity and a good therapeutic effect on metastatic malignant tumors; it can effectively inhibit the tumor epithelial-mesenchymal transition (EMT) process and effectively activate tumor immune response, and can be used to prepare anti-tumor drugs, especially providing a new direction for the research and development of anti-metastatic malignant tumor drugs.

The invention discloses a medicine formula capable of treating various gastrointestinal diseases, and relates to the technical field of medicine formulas. According to a medicine formula capable of treating various gastrointestinal diseases, skin and smooth muscle are regarded as the same muscular tissue, the smooth muscle function is indirectly improved by adjusting the skin state, a medicine composition for treating digestive system diseases is developed based on the theory, and the medicine composition comprises 1 g of baked ginger powder, 4 mg of belladonna extract and 5 mg of desloratadine. The method specifically comprises the following steps: shredding 100g of baked ginger, baking at 150 DEG C for 30 minutes until the baked ginger is brown, grinding, and sieving with a 80-mesh sieve; 1 g of baked ginger powder, 4 mg of belladonna extract and 5 mg of desloratadine are mixed in proportion and pressed into tablets, and the weight of each tablet is 1.1 g. The traditional Chinese medicine composition can effectively treat various gastrointestinal diseases including stomachache and diarrhea, acute and chronic gastroenteritis and deficiency-cold diarrhea, the treatment rehabilitation rate reaches 60-80%, the cost is not complex, the formula is prepared according to the principle that skin and smooth muscle are similar in multiple aspects, and the traditional Chinese medicine composition is an gastrointestinal medicine with an obvious treatment effect.

The present invention provides a method of inhibiting dependence to an opioid by a human subject in need thereof. The method comprises administering an effective amount of a pharmaceutical composition to the subject during opioid therapy. The pharmaceutical composition comprises a) a non-steroidal anti-inflammatory drug (NSAID); and b) a co-agent selected from the group consisting of: fexofenadine, ketotifen, desloratadine, cetirizine, salts thereof and combinations thereof.

The invention discloses an application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide in preparation of drugs for treating allergic diseases, and belongs to the technical field of biological medicines. The invention discloses a new pharmaceutical application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide for the first time, and the N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide serving as an anti-allergic antagonist can effectively inhibit phospholipase C activity of stimulated cells and mediated calcium mobilization thereof in vitro. And the effective dose of the desloratadine, which is a positive drug, is lower in vivo to generate a comparable anti-allergic effect with the desloratadine. Meanwhile, in animal models of allergic rhinitis and atopic dermatitis, compared with a positive drug desloratadine, the compound can effectively inhibit the pathological progress of diseases at a lower dosage. Therefore, the compound has a definite effect of inhibiting in-vitro and in-vivo anaphylaxis, and can be effectively applied to the development of drugs for treating allergic diseases.

1. Name of the product of this design: Packaging box (desloratadine oral solution). 2. Purpose of this design product: used for product packaging. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the design points: three-dimensional picture.

The present invention provides a desloratadine orally dissolving film composition, a preparation method thereof, and applications thereof. The present invention provides a desloratadine orally dissolving film composition comprising an active drug, a film-forming material, a plasticizer, and a flavoring agent. The active drug is 8-chloro-6,11-dihydro-11-(4-piperidinyl)-5H-benzo-[5,6]heptylcyclo[1,2-b]pyridine as shown in Formula I. The desloratadine orally dissolving film composition of the present invention has a good dissolution rate, does not leave a gritty feeling after dissolving in the oral cavity, has a uniform appearance, good flexibility, does not settle during the film solution preparation process, and meets content uniformity requirements. #imgabs0#

This invention relates to the field of pharmaceutical technology for myocardial fibrosis. Specifically, it provides the application of histamine H1 receptor antagonists in the preparation of drugs for treating myocardial fibrosis. This invention utilizes a stress overload mouse model constructed via TAC surgery to simulate the in vivo process of myocardial fibrosis, and a TGF-β1-induced fibrotic cell model. Combined with network pharmacology analysis and histamine H1 receptor gene knockout mice, the anti-myocardial fibrosis effects and mechanisms of action of the histamine H1 receptor antagonists brompheniramine maleate (BHM) and desloratadine (DLT) were investigated at both the systemic and cellular levels, providing a theoretical and experimental basis for the development of new anti-myocardial fibrosis drugs.

The invention provides a desloratadine oral soluble film composition as well as a preparation method and application thereof. The present invention provides a desloratadine oral soluble film composition, which comprises an active drug, a film forming material, a plasticizer and a flavoring agent, and the active drug is 8-chloro-6, 11-dihydro-11-(4-piperidino)-5H-benzo-[5, 6] heptyl ring [1, 2-b] pyridine represented by a formula I. The desloratadine oral soluble film composition comprises a desloratadine compound, a desloratadine compound, a desloratadine compound, a desloratadine compound, a desloratadine compound, a desloratadine compound, a desloratadine compound and a The desloratadine oral soluble film composition disclosed by the invention has the advantages of good dissolution rate, no grit feeling after being dissolved in an oral cavity, uniform appearance, good flexibility, no sedimentation in a film liquid preparation process, and content uniformity meeting requirements. # imgabs0 #

The invention relates to the technical field of medicine detection, and particularly discloses a method for determining propylene glycol in a desloratadine oral solution and application of the method. The determination method is a gas chromatographic method, a capillary column taking 6% cyanopropyl phenyl-94% dimethyl polysiloxane as a stationary phase is taken as a chromatographic column, nitrogen is taken as carrier gas, a detector is a hydrogen flame ionization detector, ethanol is taken as a solvent, a reference solution and a test solution are respectively prepared, a direct sample injection mode is adopted for sample injection, and the detection accuracy is high. The programmed heating mode is as follows: the initial temperature is 78-83 DEG C and is maintained for 10 minutes, and the temperature is raised to 220 DEG C at the rate of 30 DEG C per minute and is maintained for 10 minutes. The gas chromatography detection method disclosed by the invention is good in specificity, high in sensitivity, good in linearity, precision (sample injection precision, repeatability and intermediate precision), stability and durability, simple to operate and reliable in result, and can be effectively used for quality control of the desloratadine oral solution.

The invention discloses a desloratadine derivative and application of the desloratadine derivative in preparation of a medicine for treating and / or preventing inflammatory neurodegenerative diseases. A BV2 cell model and a 3 * Tg-AD mouse verify that the desloratadine derivative can significantly inhibit the inflammation level of BV2 cells and improve cognitive impairment of the 3 * Tg-AD mouse, and has a significant effect on inflammatory neurodegenerative diseases, especially Alzheimer's disease.

The invention provides a desloratadine oral solution preparation and a preparation method thereof, the desloratadine oral solution preparation is a water aqua and is composed of a desloratadine active component, a stabilizer, a sweetening agent, pharmaceutically acceptable auxiliary materials of an antioxidant and a solvent water, the strong bitter taste of desloratadine is obviously reduced, and the desloratadine oral solution preparation has the advantages that the desloratadine oral solution preparation is suitable for oral administration of desloratadine; the stability of the desloratadine oral solution is obviously improved by controlling the quality of auxiliary materials, and the desloratadine oral solution and the preparation method thereof disclosed by the invention are simple in preparation process and good in patient compliance. The pharmaceutical composition is particularly useful for administration to teenagers and infants who are treating allergic rhinitis, urticaria with desloratadine.

The present invention relates to a renal disease treatment effect obtained by the co-administration of desloratadine, which is an antihistamine, and duloxetine, which is a serotonin reuptake inhibitor. It has been identified that, when desloratadine and duloxetine are co-administered, the formation and growth of cysts were inhibited in an ADPKD animal model, the renal function was also maintained at a normal value, liver cysts and liver fibrosis caused by ADPKD were treated, renal fibrosis was significantly treated in in vitro and animal renal fibrosis models, and, in particular, the effects were synergistically increased.

The invention provides a method for detecting related substances of desloratadine oral liquid, which is applicable to the technical field of detection of impurity control of organic chemical synthesis raw material medicines, particularly to the field of medicine quality control, and is a liquid chromatography detection method needing to monitor oxidation impurities and byproducts. The analysis method overcomes the limitation of a method for isocratic elution of desloratadine related substances, phosphoric acid is adopted to replace trifluoroacetic acid, the sensitivity and the accuracy are improved, the problems of low detection efficiency and low precision in the prior art are solved, and the separation degree and the detection efficiency are improved by optimizing conditions such as mobile phase composition and the like. A chromatographic column is a silica gel bonded octadecyl silane column and an ultraviolet detector, a mobile phase comprises a phosphate buffer solution added with SDS and an organic solvent, the mobile phase is simple in composition, a conventional chromatographic column is used, the cost is reduced, and a gradient elution mode is adopted for separation and detection. The method for detecting the desloratadine syrup-related substances is good in separation degree, high in specificity, high in precision and good in repeatability, and meets methodological research on determination of the desloratadine oral liquid-related substances.

The present application relates to a kind of preparation methods of desloratadine tablets, which includes pre-gelatinized starch slurry and desloratadine mixing, fluidized bed granulation, whole grain, total mixing, tabletting, coating and the like steps.The present application precisely controls the key process parameters in preparation process, so that the impurity content of product is less, and the product quality is improved.The preparation process of the method of the present application is relatively simple, easy to operate, easy to popularize and apply, and the formula of the method is relatively simple, and the cost is controllable.

1. The name of the product of this design: bottle sticker (desloratadine oral solution). 2. Purpose of this design product: to be affixed to packaging bottles for decoration and identification purposes. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the key points of the design: main view. 5. The back of the product with this design is a part that is difficult to see or cannot be seen during use, so the rear view is omitted; the product with this design is a flat product, so the left view, right view, top view and bottom view are omitted.

The present invention relates to the technical field of drug synthesis, and in particular to a method for preparing rupatadine fumarate. The method for preparing rupatadine fumarate of the present invention comprises the following steps: S1, reacting nitrogenmethylloratadine, phenyl chloroformate, and an organic amine in an organic solvent to obtain compound I; the structural formula of compound I being: #imgabs0#; S2, reacting compound I with a base in an organic solvent to obtain desloratadine; S3, reacting desloratadine, 3-chloromethyl-5-methylpyridine hydrochloride, and an organic amine in an organic solvent to obtain rupatadine; and S4, reacting rupatadine with fumaric acid in a salt-forming solvent to obtain rupatadine fumarate. The method for preparing rupatadine fumarate of the present invention has mild reaction conditions, short reaction time, a short route, simple operation, high yield, high product purity, and is suitable for large-scale industrial production.

The invention relates to the technical field of drug detection, and discloses a method for detecting mutagenic impurity desloratadine pyridine nitrogen oxide in a desloratadine oral solution, which comprises the following specific steps: S1, preparing a test solution: precisely weighing a to-be-detected sample, placing the to-be-detected sample in a measuring flask, adding a mobile phase, dissolving, diluting to a scale, and uniformly shaking to obtain the test solution; s2, preparation of a reference substance solution: precisely weighing a desloratadine pyridine nitrogen oxide reference substance, placing the reference substance in a measuring flask, adding a mobile phase for dissolving and diluting to a scale, and uniformly shaking to obtain the reference substance solution; and S3, determination: precisely measuring the test solution and the reference solution, respectively injecting into a liquid chromatograph, and recording a chromatogram to two times of the retention time of a main component peak. According to the present invention, with the method, the mutagenic impurity desloratadine pyridine nitrogen oxide in the desloratadine oral solution can be accurately and rapidly determined, and the detection method has characteristics of strong specificity and high sensitivity.

The invention discloses a desloratadine derivative and application of the desloratadine derivative in preparation of a medicine for treating and / or preventing peripheral neuropathy. A Schwann cell model and diabetic peripheral neuropathy mice verify that the desloratadine derivative can significantly inhibit Schwann cell inflammation level and improve motor nerve conduction velocity and sensory deficiency, and has a significant effect on peripheral neuropathy, especially diabetic peripheral neuropathy.

The invention belongs to the technical field of drug analysis, and particularly relates to a method for detecting nitrosamine impurities in drugs. According to the detection method, an HPLC method is adopted to detect the content of the nitrosamine impurities in the medicine, the nitrosamine impurities are desloratadine nitrosamine, and the structural formula of the nitrosamine impurities is shown in the formula I. The method provided by the invention not only can be used for effectively determining the content of the desloratadine nitrosamine in the medicine such as a desloratadine oral solution, but also is high in sensitivity and strong in specificity; the detection result is reliable and accurate, and a technical means is provided for detecting impurities in the medicine such as the desloratadine oral solution, so that the quality of the medicine can be controlled. Moreover, the quality detection method provided by the invention can provide a reference standard for quality control of drugs such as desloratadine oral solutions and safety detection of clinical safe medication, so that the safety and reliability of clinical medication are ensured. # imgabs0 #

The invention discloses a method for simultaneously detecting three nitrosamine impurities in a desloratadine oral solution, which comprises the following steps: dissolving the desloratadine oral solution in a diluent to obtain a test solution, enabling the concentration of desloratadine in the test solution to be 2-3mu g / mL, enabling the diluent to be a methanol aqueous solution, and enabling the concentration of the desloratadine in the methanol aqueous solution to be 2-3mu g / mL, the volume ratio of methanol to water is 1: (0.8-1.2); detecting the test sample solution by adopting an ultra-high performance liquid chromatography-triple quadrupole mass spectrometry method; a mobile phase A of the liquid chromatography is a formic acid aqueous solution with the volume percentage of 0.09-0.11%, and a mobile phase B is acetonitrile; the three kinds of nitrosamine impurities are N-nitroso-desloratadine, N-nitroso-remote loratadine and N-nitroso group-11-fluorine desloratadine. The detection method can be used for rapidly and accurately detecting three nitrosamine impurities in the loratadine oral solution.

The invention relates to the technical field of pharmaceutical analysis, and relates to a method for detecting nitrosamine impurity N-nitroso desloratadine in desloratadine. The detection method is a liquid chromatography-mass spectrometry method, and the chromatographic conditions of liquid chromatography are as follows: purified water is taken as a mobile phase A, methanol is taken as a mobile phase B, and gradient elution is performed; the flow velocity is 0.35 mL / min to 0.42 mL / min, and the column temperature is 20 DEG C to 30 DEG C. The gradient elution procedure is as follows: 0.00-(0.50-1.00) min, and the ratio of a mobile phase A to a mobile phase B is 9: 1; in the (1.00-2.00)-3.00 min, the ratio of the mobile phase A to the mobile phase B is 5: 5; in 4.50-5.50 min, the ratio of the mobile phase A to the mobile phase B is 2: 8; in 6.00-6.50 min, the ratio of the mobile phase A to the mobile phase B is 9: 1. The mass spectrum adopts a triple quadrupole, an ESI ion source, positive ion detection and an SRM mode, the temperature of the ion source is 330 DEG C, the spray voltage is 3500 V, the sheath gas is 10, and the auxiliary gas is 5. The method has the advantages of being simple, convenient, stable, high in precision, good in reproducibility and the like, the impurity N-nitroso desloratadine in the desloratadine raw material medicine can be rapidly and accurately detected, and the whole operation process is reliable and controllable.

1. Name of the product of this design: Packaging box (desloratadine oral solution). 2. Purpose of this design product: used for product packaging. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the key points of the design: main view.