39 results about "Carbidopa" patented technology

The invention relates to the technical field of pharmacy, and discloses a carbidopa-levodopa sustained release tablet and a preparation method thereof.The carbidopa-levodopa sustained release tablet is prepared from, by mass, 65.4%-68.0% of levodopa, 17.0%-18.5% of carbidopa, 0.1%-0.5% of an adhesive, 0.1%-0.5% of a lubricant and 0.1%-0.5% of a coloring agent. And the mass percentage of the sustained-release material is 8.0%-9.0%. According to the carbidopa-levodopa sustained-release tablet and the preparation method thereof, polyvinyl acetate-crotonic acid copolymer is selected as a sustained-release material, hydroxypropyl cellulose is selected as an adhesive, the defects existing in the prior art are overcome, the carbidopa-levodopa sustained-release tablet can well control slow release of carbidopa and levodopa, and the sustained-release effect is good. According to the present invention, the release curve is highly consistent with the release curve of the original development agent, such that the safety and the effectiveness of the medication can be significantly improved, the wet granulation process is adopted, the addition mode of the adhesive is adjusted, the granulation process problem that the granulation is not easily performed when the active component content is large is solved, the preparation process is simple, and the industrial production is easy.

The invention provides an oral solid formulation comprising (a) a plurality of controlled release components comprising (i) a core comprising a mixture of levodopa and at least one pharmaceutically acceptable excipient, (ii) a controlled release coating surrounding the core, (iii) a muco-adhesive coating surrounding the controlled release coating and (iv) an enteric coating surrounding the muco-adhesive coating; and (b) one or more immediate release components comprising levodopa. The oral solid formulation also contains carbidopa and about 80% to 100% of the carbidopa in the oral solid formulation is present in the one or more immediate release components.

The invention relates to the technical field of pharmaceutical analysis, in particular to a chromatographic method for determining optical isomers in a carbidopa raw material medicine and a preparation thereof by using an HPLC (High Performance Liquid Chromatography) method. The detection method is simple, convenient, rapid and accurate to operate, and specifically comprises the following steps: dissolving a proper amount of a sample with a solvent, diluting to a certain concentration, taking a certain volume of the sample, carrying out isocratic elution at a certain column temperature by adopting a high performance liquid chromatography, using a hand-type chromatographic column, a mobile phase A and a mobile phase B, and carrying out quantitative analysis by adopting a self-control method with correction factors. And calculating the isomer in the test solution. The method is good in specificity, solution stability, linearity, repeatability, intermediate precision and durability, and the detection result is accurate and reliable through verification.

A method for measuring the content of hydrazine in a carbidopa-containing drug, comprising the following steps: (1) in a solvent, under the action of acid, mixing a sample under test with an aldehydes substance, said sample being a carbidopa-containing drug, and hydrazine in said sample and the aldehydes substance being derivatized to obtain a test solution; and (2) measuring the content of the hydrazine in the test solution. Compared with the prior art, the method for measuring the content of hydrazine in a carbidopa-containing drug does not require pretreatment to remove carbidopa, introduces negligible hydrazine during measurement, is easy to operate, does not need to accurately control derivatization time and sample introduction time, and exhibits good repeatability and accurate measurements.

The present invention relates to the simultaneous use of L-tryptophan (L-Try) and L-5-hydroxytryptophan (5-HTP) and a peripheral degradation inhibitor for the prevention and therapy of pain, depression, sleeping disorders and other serotonin-dependent diseases or disorders of the CNS. All the components of the medicament are supposed to be released together. Carbidopa and / or benserazide are to be used as said peripheral degradation inhibitors for the tryptophan and the 5-hydroxytryptophan.

The invention relates to the technical field of biological medicine, and particularly discloses application of carbidopa in preparation of a medicine for treating melanoma. Carbidopa can target CD147 and has an inhibition effect on CD147, so that invasion, migration and growth of melanoma cells are inhibited, Carbidopa can be used for preparing drugs for treating melanoma, and new safe and effective drugs are provided for the field of melanoma treatment.

The invention relates to a method for determining hydrazine in carbidobar by derivatization high performance liquid chromatography. Specifically, the invention relates to a method for quality control of Carbidopa as an anti-Parkinson disease drug, and especially relates to a method for determining trace impurity hydrazine in Carbidopa by using derivatization high performance liquid chromatography. In the method, octadecylsilane chemically bonded silica is used as a chromatographic column of a filling agent, and a test solution is prepared by the following steps: taking a to-be-detected test sample Carbidopa raw material medicine, putting the Carbidopa raw material medicine into a measuring flask, precisely adding water, shaking, immediately and precisely adding a diluent containing benzaldehyde and glacial acetic acid, shaking at proper time, immediately adding a proper amount of triethylamine, and uniformly stirring; and diluting to the scale by using a diluent, and uniformly shaking to obtain the test solution. The method provided by the invention can effectively and accurately determine the trace impurity hydrazine in the carbidopa bulk drug. The method provided by the invention has excellent methodological characteristics.

Disclosed is a method for the treatment of a neurological or movement disorder, e.g., Parkinson's disease, in an individual in need thereof, by parenteral administration of levodopa and a dopa decarboxylase inhibitor (DDCI), such as carbidopa, benserazide or any combination thereof, concomitantly with oral administration of levodopa, a DDCI, such as carbidopa, benserazide, or any combination thereof.

The present disclosure provides a method for the treatment of Parkinson's disease comprising simultaneously or sequentially administering to a patient in need of treatment of Parkinson's disease a dosage form comprising(i) levodopa in an amount ranging from 50 mg to 300 mg,(ii) carbidopa in an amount ranging from 25 mg to 150 mg or a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor, and(iii) entacapone in an amount ranging from 50 mg to 300 mg, wherein the proportion of entacapone to carbidopa in said dosage form ranges from 0.3:1.0 to 3.2:1.0 by weight, a moderately potent COMT inhibitor in an amount ranging from 25 mg to 200 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.16:1.0 to 3.08:1.0 by weight, or a highly potent COMT inhibitor in an amount ranging from 1 mg to 100 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.006:1.0 to 1.54:1.0 by weight. Pharmaceutical dosage form used in said method are also disclosed.

The application belongs to the technical field of medicine, and particularly relates to a kind of opicapone oral disintegrating tablets and a preparation method thereof.The active component of the opicapone oral disintegrating tablet is opicapone, and the components are as follows according to weight percentage: opicapone 15-25%; filler 60-70%; glidant 1-4%; lubricant 1-4%; first disintegrating agent 2-6%; and second disintegrating agent 2-6%, wherein the first disintegrating agent and the second disintegrating agent are different, and preferably, the weight content of the opicapone is 15-20%.The opicapone oral disintegrating tablet of the application is suitable for the adjuvant therapy of levodopa / carbidopa, has a fast disintegration rate, stable product quality, does not need to be taken with water, and has strong patient compliance; in addition, the preparation process of the opicapone oral disintegrating tablet of the application is simple, has low cost, and is suitable for mass production.

The invention provides a carvolevodopa sustained-release capsule and a preparation method thereof. The carvolevodopa sustained-release capsule comprises a cured hollow soft capsule, and the cured hollow soft capsule is sequentially coated with a drug-containing layer and a thin film layer; the cured hollow soft capsule is obtained by curing a hollow soft capsule with a curing agent; the drug-containing layer comprises carbidopa, levodopa, a sustained-release material and an adhesive. The cardopa-levodopa sustained-release capsule provided by the invention has a unique gastric floating mechanism, has better gastric floating performance, and also has an in-vitro dissolution curve similar to that of a reference preparation. Meanwhile, raw materials and auxiliary materials are easy to obtain in the preparation process of the Carbidopa-levodopa sustained-release capsule, the preparation process is simple, the cost is low, and continuous and commercialized production is facilitated.

The present invention relates to a solid pharmaceutical composition manufactured by a wet granulation method comprising carbidopa and levodopa or pharmaceutically acceptable salts thereof, one or more disintegrant, one or more diluent, at least one binder, at least one lubricant, and one or more pharmaceutically acceptable excipients. The orodispersible tablet prepared using these excipients exhibits desirable properties such as facilitating disintegration, and dissolution of the drug for oral administration. Further, the present invention also relates to the process for preparing the said solid pharmaceutical composition.

Disclosed is a method for the treatment of a neurological or movement disorder, e.g., Parkinson's disease, in an individual in need thereof, by parenteral administration of levodopa and a dopa decarboxylase inhibitor (DDCI), such as carbidopa, benserazide or any combination thereof, concomitantly with oral administration of levodopa, a DDCI, such as carbidopa, benserazide, or any combination thereof.

The invention relates to the treatment of neurodegenerative diseases such as Parkinson patients with motor complications in need of Continuous Dopaminergic Stimulation. According to the invention a kit of pharmaceutical preparations is provided comprising levodopa and an AADC-inhibitor. Levodopa is applied via continuous subcutaneous infusion or by an oral modified release formulation and Continuous Dopaminergic Stimulation is achieved by almost complete inhibition of the peripheral levodopa metabolism. To reach far-going blockage of levodopa metabolism, an AADC-inhibitor (e.g., benserazide, carbidopa) is given orally in a much higher than normal dose and, as an indispensable prerequisite, the AADC-inhibitor has to be applied evenly distributed over the day. e.g., via a Modified Release formulation. In order to prevent levodopa conjugation over the COMT pathway, an oral COMT-inhibitor (e.g., opicapone) is also added. In addition, a drug-drug-interaction between the AADC-inhibitor and opicapone further increasing the activity of the former is likely to occur. The resulting effective inhibition of peripheral levodopa metabolism allows a marked reduction of the necessary (equivalent) levodopa (or prodrug) doses to 300-600 mg / day, which is, however, sufficient to reach high levodopa plasma levels of 1500 to 3000 ng / ml. The low daily levodopa dose is infused subcutaneously via minipump and is well-tolerated at the infusion site. Alternatively, the low daily levodopa dose is provided as an oral modified release formulation. The high steady-state levodopa plasma levels reached, allow effective Continuous Dopaminergic Stimulation-therapy for Parkinson's disease patients of any degree of severity. As additional benefit, the largely complete AADC-inhibition prevents the peripheral generation of dopamine and the cumbersome dopaminergic adverse effects (e.g., nausea, cardiovascular and gastro-intestinal adverse effects) are prevented.

The present disclosure relates to compositions of levodopa 4′-monophosphate and carbidopa 4′-monophosphate having a weight by weight ratio of about 20:1 and methods of treating Parkinson's disease and associated conditions by subcutaneous administration of such compositions.

To provide compositions for treating Parkinson's disease and associated conditions.SOLUTION: Pharmaceutical combinations and compositions comprise a carbidopa prodrug such as formula (I-a) and an L-dopa prodrug such as formula (II-a).SELECTED DRAWING: None

The application belongs to the technical field of pharmaceutical preparations, and specifically provides a carbidopa levodopa sustained-release tablet, which contains carbidopa, levodopa, potassium hydrogen tartrate, a sustained-release material, a binder and a lubricant. The carbidopa in the sustained-release tablet has good stability and is not prone to oxidative degradation, thereby improving the drug efficacy of the carbidopa levodopa sustained-release tablet. In addition, the wet granulation technology is used in the application, the preparation process is simple, the cost is low, and the application is suitable for industrial production.

The present disclosure provides (a) a pharmaceutical composition comprising a levodopa active agent and a carbidopa active agent and (b) methods of treating Parkinson's disease and associated conditions comprising administering the pharmaceutical composition to a subject with Parkinson's disease.

The application relates to the technical field of medicines, and discloses a novel oral dissolving film which is composed of the following components in mass fractions: soluble polymer 38-48 parts, plasticizer 10-20 parts, filling agent 5-15 parts, solvent 20-30 parts, acid-base regulator 0.5-2 parts, sweetening agent 1-3 parts, and medicine or other active ingredients 5-25 parts; on the basis of the oral dissolving film, the application further provides a racemic carbidopa oral dissolving film which is composed of the following components in mass fractions: racemic carbidopa 45-55 parts, the above-mentioned oral dissolving film 40-50 parts, sweetening agent 1-3 parts, essence 0.5-2 parts, and other auxiliary materials 1-8 parts; the oral dissolving film has good solubility, accurate dosage, high drug loading, and the preparation method is simple and easy for industrialized production.

An orodispersible solid pharmaceutical composition in tablet form is disclosed comprising a) carbidopa and levodopa or pharmaceutically acceptable salts thereof, b) one or more diluent, c) one or more

Disclosed is a system and method for a non-oral dopaminergic therapy for patients with Parkinson's disease, the administration thereof having the benefit of no change in risk to the patient. The disclosed therapy is capable of delivering prescribed doses of carbidopa / levodopa through the skin into the bloodstream where it may circulate systemically in the body, bypassing the digestive system and avoiding first-pass metabolism in the liver. The dislosed drug delivery system enables therapeutic dosages of carbidopa / levodopa to reach the target tissue site in a controlled manner while maintaining the concentration in the therapeutic window.

Provided here within is a saliva-activated pharmaceutical composition for use in an intra-oral sustained-release sachet. The formulation includes acacia powder in defined acacia-to-levodopa ratios effective to increase levodopa solubility by at least 300% at 25° C., maintain a localized pH of 3-5, and suppress levodopa oxidation during and after intra-oral use. In combination with levodopa, carbidopa, ascorbic acid, and optional palatability or swallowing-stimulation agents, the acacia forms a hydrocolloid matrix that stabilizes drug particles, enhances dispersion, and enables sustained, uniform release for several hours. The composition further supports consistent distribution of flavoring agents and prolonged intra-oral retention with improved sensory persistence. This acacia-dependent hydrocolloid system provides controlled salivary dissolution, biochemical stabilization, and predictable sustained delivery of levodopa / carbidopa, achieving performance not obtained with prior acacia-based formulations or with the parent sachet device.

The invention relates to the technical field of pharmaceutical technology, in particular to a preparation method of a carbidopa-levodopa sustained release tablet capable of improving stability, which comprises the following steps: acquiring an actual fluidization number and a fluidization uniformity index to determine a standardized fluidization efficiency coefficient, and determining a pellet core particle circulating fluidization state based on the standardized fluidization efficiency coefficient and the fluidization uniformity index; a real-time evaporation potential ratio is determined based on the current maximum theoretical evaporation capacity and the real-time moisture input rate, it is determined that the drying capacity of the spraying procedure is not in an efficient deposition area based on the real-time evaporation potential ratio, and whether a potential over-moisture risk or an over-drying risk exists or not is determined; adjusting the liquid spraying rate based on existence of the potential over-humidity risk or the drying over-risk, and adjusting the air inlet temperature based on the fact that the liquid spraying rate is adjusted to reach the preset safety upper limit or lower limit and the real-time evaporation potential ratio deviates from the target interval. Spraying parameters are adjusted and controlled in a self-adaptive mode according to the fluidized state of the drug-loaded particles and the formation of the coating in combination with the characteristics of the precursor drug, and the product quality is improved.

The present disclosure relates to compositions of levodopa 4′-monophosphate and carbidopa 4′-monophosphate having a weight by weight ratio of about 20:1 and methods of treating Parkinson's disease and associated conditions by subcutaneous administration of such compositions.

The invention discloses a process and a device for preparing carbidopa through continuous flow reaction, and the process comprises the following steps: firstly mixing cyclohexanone and a solvent, then reacting with ammonia water and sodium hypochlorite to generate 1-oxa-2-azaspiro [2.5] octane, and carrying out gas-liquid-liquid phase separation to obtain an organic phase and 2-amino-3-(3, 3, 5, 6-tetramethyl-2-oxo-2-azaspiro [2.5] octane; the preparation method comprises the following steps: reacting 2-[(cyclohexyl) hydrazino]-3-(3, 4-dihydroxyphenyl)-2-methyl propionate (methyl dopa methyl ester) to generate 2-[(cyclohexyl) hydrazino]-3-(3, 4-dihydroxyphenyl)-2-methyl propionate, and finally hydrolyzing with hydrochloric acid to obtain carbidopa. According to the invention, the synthesis of high-purity and high-content carbidopa is realized through the full-flow continuous flow reactor. The yield reaches 90%, and the purity reaches 99% or above. The reaction system solves the problems that the reaction temperature is difficult to control, the production efficiency is low, an intermediate product is unstable and the like in an existing kettle type process, the yield and the purity of a target product are remarkably improved, material consumption is greatly reduced, and the reaction system has the advantages of being short in production period, high in selectivity, continuous in production and intrinsically safe.

The invention relates to the technical field of pharmacy, in particular to a carbidopa-levodopa sustained release tablet and a preparation method thereof.The preparation method comprises the steps that carbidopa monohydrate, levodopa, hydroxy propyl cellulose, hydroxypropyl methyl cellulose, magnesium stearate and a coloring agent are prepared according to a preset proportion; the preparation method comprises the following steps: pre-mixing carbidopa monohydrate, levodopa and hydroxy propyl cellulose to obtain a first mixture, adding the hydroxy propyl methyl cellulose and a coloring agent into the first mixture, and uniformly mixing to obtain a second mixture; performing wet granulation on the second mixture based on the wet granulation parameters to obtain mixed wet particles; and carrying out fluidized bed drying treatment on the mixed wet granules / mixed wet whole granules, adding magnesium stearate, carrying out total mixing and tabletting, and testing to obtain the water solubility characteristics of the carbidopa-levodopa sustained release tablets so as to adjust wet granulation parameters or preset screening test conformity conditions. The stability and the slow-release effect of the carbidopa-levodopa sustained-release tablet can be improved.

The invention provides an oral solid formulation comprising (a) a plurality of controlled release components comprising (i) a core comprising a mixture of levodopa and at least one pharmaceutically acceptable excipient, (ii) a controlled release coating surrounding the core, (iii) a muco-adhesive coating surrounding the controlled release coating and (iv) an enteric coating surrounding the muco-adhesive coating; and (b) one or more immediate release components comprising levodopa. The oral solid formulation also contains carbidopa and about 80% to 100% of the carbidopa in the oral solid formulation is present in the one or more immediate release components.

The invention relates to a method for detecting hydrazine content in a medicine containing carbidopa, which comprises the following steps: (1) mixing a sample to be detected and an aldehyde substance in a solvent under the action of an acid, deriving hydrazine in the sample to be detected and the aldehyde substance to obtain a test solution, and (2) detecting the content of hydrazine in the test solution. Compared with the prior art, the method for detecting the hydrazine content in the medicine containing the carbidopa has the advantages that the carbidopa does not need to be removed through pretreatment, the hydrazine introduced in the determination process can be ignored, the operation is simple, the derivatization time and the sample injection time do not need to be accurately controlled, the repeatability is good, and the quantification is accurate.

The application discloses a detection method and application of entacapone double-dopa tablets, and operation steps of the detection method include sample pretreatment, chromatographic separation detection and quantification; the sample pretreatment comprises the following operation steps: grinding the entacapone double-dopa tablets into uniform fine powder, precisely taking a proper amount of tablet powder, adding a diluent to dissolve and stabilize, performing ultrasonic treatment, then constant volume and filtration, and taking the filtrate as a test sample solution; a solvent in the diluent is a mixed solution of methanol and water, and solutes in the diluent include sodium metabisulfite and disodium ethylenediaminetetraacetate. The application can realize synchronous analysis of entacapone, levodopa and carbidopa with rapidness, high separation degree, high sensitivity and high stability, so as to meet strict quality control requirements of the compound preparation.

The present invention provides a method for treatment of a neurological or movement disorder, e.g., Parkinson's disease, in an individual in need thereof, by parenteral administration of a composition comprising carbidopa and levopoda, or pharmaceutically acceptable salts thereof, and concomitant oral administration of a catechol-O-methyl transferase (COMT) inhibitor, e.g., entacapone or tolcapone.