18 results about "Benserazide" patented technology

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 application relates to the technical field of medicine preparation, and particularly discloses a levodopa-benserazide tablet, a preparation method and application thereof, which comprises levodopa granules, benserazide hydrochloride granules, cross-linked polyvinylpyrrolidone and magnesium stearate; the levodopa granules are composed of levodopa, anhydrous calcium hydrogen phosphate, pregelatinized starch, cross-linked polyvinylpyrrolidone, red iron oxide and sodium docusate; and the benserazide hydrochloride granules are composed of benserazide hydrochloride, mannitol, microcrystalline cellulose, colloidal silicon dioxide, red iron oxide and ethyl cellulose. The related substances and the friability of the levodopa-benserazide tablet meet the production requirements, the stability is high, and the tablet is suitable for large-scale production.

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

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 invention belongs to the technical field of analytical chemistry, and particularly relates to a method for separating and determining benserazide hydrochloride SM2 and related substances thereof. According to the self-built high performance liquid chromatography, octadecylsilane chemically bonded silica is used as a chromatographic column filler, a phosphoric acid aqueous solution is used as a mobile phase A, and methanol is used as a mobile phase B; the impurity BES-SM2a, the impurity BES-SM2c, the impurity BES-SM2d, the benserazide hydrochloride SM2 and / or the impurity BES-SM2e are sequentially separated through gradient elution; and then detecting in a detector with the wavelength of 215nm to obtain a chromatogram, and calculating the content of each component according to the peak area by adopting a correction factor-added principal component self-contrast method. The analysis method provided by the invention can be used for determining benserazide hydrochloride SM2 and related substances thereof within 50 minutes, and has the characteristics of strong specificity, high sensitivity and good reproducibility.

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

The invention belongs to the technical field of pharmaceutical analysis, and particularly relates to a method for separating related impurities in a dopurazide tablet and determining the content of each component. According to the method, octadecyl silane bonded silica gel is adopted as a filling agent, a potassium hexafluorophosphate solution is adopted as a mobile phase A, methyl alcohol is adopted as a mobile phase B, and benserazide hydrochloride, a benserazide hydrochloride impurity C and a benserazide hydrochloride impurity E are sequentially separated through gradient elution; and then the sample enters a detector with the detection wavelength of 210 nm to be detected. And calculating the content of each component by adopting an external standard method according to the measured chromatogram. The self-established high performance liquid chromatography is not interfered by other impurities or auxiliary materials, and separation and determination of the benserazide hydrochloride, the benserazide hydrochloride impurity C and the benserazide hydrochloride impurity E can be realized within 35 minutes. The method is high in specificity, high in accuracy and good in precision and durability.

The present invention provides a preparation method for a compound levodopa and benserazide hydrochloride dual-release preparation. By means of the addition method of benserazide hydrochloride, the wet granulation of the first group of sustained-release materials, and the moisture control during dry screening in the preparation process of the drug-containing sustained-release layer granules, the influence of moisture and temperature on benserazide hydrochloride is reduced, the degradation of benserazide hydrochloride is reduced, and the stability of the compound levodopa and benserazide hydrochloride dual-release preparation is improved. The present invention provides a compound levodopa and benserazide hydrochloride dual-release preparation, which adopts the design of a double-layer tablet of a drug-containing immediate-release layer and an adjacent drug-containing sustained-release layer. After the patient takes the medicine, the drug can take effect quickly; and the drug release can be stably controlled to maintain long-term effectiveness, thereby reducing the number of times the patient takes the medicine, keeping the blood drug concentration stable, and increasing the patient's compliance.

The application belongs to the field of medicine synthesis, and particularly discloses a preparation method of benserazide hydrochloride. The benserazide hydrochloride is prepared by the following steps: 2,3,4-trihydroxybenzaldehyde is used as a starting material to react with hydrazine hydrate to obtain 2,3,4-trihydroxybenzylhydrazine, and then the 2,3,4-trihydroxybenzylhydrazine is subjected to esterolysis reaction with serine methyl ester hydrochloride to obtain the target product benserazide hydrochloride. Compared with the method reported in the prior art, the method has the advantages of short reaction steps, simple reaction conditions, less process impurities, good quality control, simple raw materials, low large-scale production cost, and the like, and therefore the benserazide hydrochloride prepared by the method is good in application in a pharmaceutical composition.

The invention discloses a benserazide hydrochloride spherocrystal and a preparation method thereof. The spherocrystal benserazide hydrochloride prepared by the method has the characteristics of large granularity, higher yield, excellent product quality, capability of improving the powder flowability and density and reducing static electricity, simplified process operation and easiness in realization of industrialization.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an entacapone and didopa compound tablet and a preparation method thereof. The entacapone and didopa compound tablet is prepared from the following raw materials in parts by mass: 200 parts of entacapone, 90 to 110 parts of levodopa, 22 to 28 parts of carbidopa, 110 to 130 parts of mannitol, 150 to 170 parts of disintegrating diluent, 25 to 30 parts of disintegrating agent, 0.5 to 1.5 parts of stabilizer and 13 to 17 parts of lubricant. The stabilizer comprises citric acid and succinic acid. The specific stabilizer can adjust the pH value of the microenvironment so as to stabilize the main drug, enhance the antioxidant effect of the main drug and improve the disintegration performance at the same time. By screening and designing the raw materials, the entacapone and didopa compound tablet is similar to an original product in dissolution rate, equivalent to an original product in bioequivalence, good in friability, not easy to stick and excellent in stability.

This invention provides a pharmaceutical composition for improving memory function, relating to the field of pharmaceutical technology. The composition comprises vitamin B6, vitamin B12, lutein, anthocyanins, phosphatidylserine, docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA), levodopa, benserazide, and selegiline. Vitamin B6, vitamin B12, lutein, anthocyanins, phosphatidylserine, DHA, and EPA nourish the brain; levodopa, benserazide, and selegiline are used for neuropharmacological treatment; anthocyanins, lutein, and EPA synergistically improve cerebral microcirculation, enhance blood oxygen supply, scavenge free radicals, reduce inflammation, and decrease brain cell aging and necrosis, thereby delaying the process of memory decline; levodopa, benserazide, and selegiline synergistically supplement and protect dopamine, with benserazide enhancing the bioavailability of levodopa and selegiline inhibiting dopamine degradation.

The application belongs to the technical field of biological medicine, and specifically discloses application of benserazide hydrochloride in preparation of anxiolytic drugs. The application first finds that benserazide hydrochloride plays an anxiolytic role by regulating the kynurenine metabolic pathway. Animal experiments prove that benserazide hydrochloride can promote the generation of kynurenine and its downstream metabolite 3-hydroxyanthranilic acid, and maintain the stable level of 3-hydroxykynurenine, thereby improving the function of the metabolic pathway and restoring the nervous system homeostasis. Behavioral experiments show that benserazide hydrochloride can increase the exploration behavior of zebrafish and reduce the avoidance behavior, and meanwhile, does not cause inhibition of motor function or sedative effect, and shows good safety and selectivity. The application provides a theoretical basis and a new drug source for the prevention and / or treatment of anxiety.

The present invention provides conjugates comprising a sugar such as mannitol and one or more L-DOPA and / or DOPA decarboxylse inhibitors including, inter alia, L-DOPA, carbidopa, benserazide, or a combination thereof, wherein the sugar is conjugated to the carboxyl group of the L-DOPA and / or DOPA decarboxylse inhibitor / s) via a hydroxyl group of the sugar. The present invention further provides related pharmaceutical compositions and methods of producing the conjugates, as well as methods of use for treating medical disorders responsive to dopamininergic stimulation such as movement disorders including, inter alia, Parkinson's Disease.

Disclosed is a method for treating a nervous system disorder or a movement disorder, such as Parkinson's disease, in a patient in need thereof by parenteral administration of levodopa and a dopa decarboxylase inhibitor (DDCI) such as carbidopa, benserazide, or any combination thereof.

The invention relates to develop of a stable pharmaceutical fixed-dose formulation for oral administration comprising therapeutically effective amounts of levodopa and benserazide or pharmaceutically ассерtаblе salts thereof, wherein the levodopa containing and benserazide containing granules constituting the said tablet composition are prepared by separate granulation.