34 results about "Ethambutol Hydrochloride" patented technology

The invention relates to an antituberculosis drug combination, prepared of rifampicin, isonicotinyl hydrazine, pyrazinamide, ethambutol hydrochloride and other auxiliaries, able to effectively overcome problems of drug resistance, improving compliance of patient, etc. It is applied in a compound form, which can avoid curing by single antituberculosis drug, thus avoiding selective drug resistance caused by single drug; the patients are willing to accept this, avoiding irregular drug application caused by simultaneously taking several drugs and different numbers of drug tablets, or taking more or less drugs.

The invention belongs to the technical field of medicines, and provides a compound preparation of antituberculosis medicaments, and a preparation method thereof. Rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride as four leading antituberculosis medicaments are prepared into the compound preparation according to specific mixture ratio. The method comprises the steps of evenly mixing the leading drugs with an appropriate quantity of disintegrant and diluent, performing dry-process granulation, finishing granules, adding other auxiliary materials to the granules and preparing the obtained product into a suitable preparation. The invention solves the problems that patients are difficult to cooperate closely and complete normal chemotherapys because the antituberculosis medicaments are high in dosage, large in dosage form and troublesome in medicine-taking method, and the compound preparation and the preparation method accord with global tuberculosis direct-observation short-range supervision chemotherapy strategy (DOTS) recommended by the WHO. The antituberculosis fixed-dose compound preparation has important significance for simplifying medicine-taking method, carrying out the DOTS and controlling tuberculosis prevalence.

The invention provides methods for preparing ethambutol and ethambutol hydrochloride. The method for preparing the ethambutol comprises the step of utilizing (S)-2-aminobutanol and 1,2-dichloroethane to perform condensation reaction to prepare the ethambutol, wherein the condensation reaction is carried out in a low-boiling organic solvent, and HCl produced in the ammonia gas neutralization reaction process is utilized. Through the utilization of the method, the ethambutol of which the yield coefficient is improved can be obtained, so that the ethambutol hydrochloride of which the yield coefficient is improved can be obtained. Besides, the methods are simple in technology, safe, stable, low in cost and super-high in practical value in the industry.

The preparation process of new compound rifampicin preparation features that rifampicin, isoniazide, pyrazinamide and ethambutol hydrochloride are first prepared into granule, then coated and finally encapsulated. The preparation process can isolate the medicine components at most to avoid the avoid close contact of medicine components in the solid preparation environment so as to ensure the stability of the compound rifampicin preparation.

The invention relates to a compound antituberculous coating core tablet and a preparing method, and is characterized by improving bioavailability, overcoming drug-resistance and being convenient to take by patients. The compound antituberculous double-release preparation is designed and developed according to the optimum absorbing parts of rifampicin and isoniazide and interaction of the two, the isoniazide and excipient are tabletted in a wet granulation mode and are subjected to enteric coating to be taken as a tablet core, the rifampicin(or the rifampicin and ethambutol hydrochloride, or rifampicin, ethambutol hydrochloride and pyrazinamide) is used as the internal layer which is subjected to dry granulation with the excipient and then is pressed into the compound antituberculous coating core tablet with isoniazide enteric-coated tablet core, so that isoniazide can be released in the small intestine at fixed position, rifampicin can be rapidly disintegrated and released in the stomach, and absorption reduction caused by interaction of rifampicin and isoniazide in the stomach can be effectively avoided. The invention is particularly suitable for being taken by patients suffered from tuberculosis.

The invention discloses a pharmaceutical composition for treating intractable epilepsy and application thereof. The active components of the pharmaceutical composition comprise sodium valproate or divalproex sodium and ethambutol or medicinal salt thereof. The pharmaceutical composition has the advantages that the fact that low-dose ethambutol hydrochloride has an anti-epileptic effect is discovered for the first time, the ethambutol hydrochloride is combined with the sodium valproate or divalproex sodium to treat the intractable epilepsy, the pharmaceutical composition is evident in anti-epileptic effect, and the toxic and side effects of the pharmaceutical composition are lowered evidently.

The invention discloses a salt formation crystallization method of ethambutol hydrochloride. According to the salt formation crystallization method of ethambutol hydrochloride, the system temperature, the cooling rate and the falling temperature are strictly controlled during the salt formation, so that the purity of ethambutol hydrochloride can be increased, ethambutol hydrochloride meeting pharmacopeia standards can be produced through adopting ethambutol bulk drug with lower purity, and the higher yield is achieved. Through adoption of the salt formation crystallization method of ethambutol hydrochloride, an approach which is simple, convenient, and lower in cost is provided for synthesis of ethambutol hydrochloride.

The invention relates to a pharmaceutical preparation for resisting tuberculosis, which comprises rifampin, isoniazid, pyrazinamide and ethambutol hydrochloride, wherein the rifampin or the isoniazid is prepared into micropills and residual materials are prepared into granules. According to the invention, one of the rifampin and the isoniazid is prepared into micropills which are separated by isolation gown and the other one is prepared into granules, so that the rifampin and the isoniazid cannot be mutually influenced, the rifampin is ensured to not be basically degraded in the use process, and the bioavailability of the rifampin is improved.

The invention discloses a drug for clinically treating pulmonary tuberculosis and belongs to the technical field of drugs. The drug is prepared from ethambutol, starch and a biological agent. Clinicaltests prove that the drug better solves the problem that ethambutol hydrochloride sold in the market easily has side effects when used for treating pulmonary tuberculosis clinically.

Provided is an oral solid preparation of a compound anti-tubercular drug, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. The compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not contact directly. The compound oral solid preparation not only improves the stability of the compound preparation, but also improves the bioavailability of rifampicin.

The invention is a fixed-dose anti-tuberculosis drug compound preparation and a preparation method thereof, which has the characteristics of reducing the number of times of taking the medicine, reducing the occurrence of drug resistance, improving the curative effect of the medicine, and making the storage and transportation of the medicine more convenient. It is a fixed-dose compound preparation containing rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride, which also contains an appropriate amount of disintegrants, binders, lubricants, diluents and water-soluble packets. Clothing powder. First sieve rifampicin alone, pass through a 100 mesh sieve, and pass through a 60 mesh sieve, add binder, disintegrating agent and diluent, mix evenly, dry granulate, and then use disintegrating agent and diluent to mix with the above-mentioned The granules are mixed evenly and pressed into tablets to obtain the finished product. The invention is especially suitable for use by tuberculosis patients.

The invention discloses application of ethambutol or a pharmaceutically acceptable salt thereof as an active ingredient in preparation of a drug for treating intractable epilepsy and belongs to the technical field of medicines. Due to the fact that the dosage of the ethambutol hydrochloride is small, toxic and side effects are inevitably reduced, so that the toxic and side effects of medication ofa patient are reduced, meanwhile the medication dependence of the patient is improved, the prior art is enriched, and the potential new drug for resisting intractable epilepsy is added clinically andhas remarkable social significance and economic significance.

The invention relates to a process system for preparing ethambutol hydrochloride. The process system comprises, in an upstream-to-downstream arrangement, comprises a reaction kettle (1), a distillation kettle (2), a dissolving kettle (3) and a press filter (4), and also a recovery tank (5) which is located downstream of the distillation kettle (2), a collection tank (6) which is located downstream of the press filter (4), and a nitrogen protection device comprising a nitrogen inlet pipe (7), and pressure alarm devices (10). The nitrogen inlet pipe (7) is connected with the top of the reaction kettle (1) by means of a pipe, and also connected with a blowdown pipe (8) and a discharge pipe (9) of the reaction kettle (1) by means of pipes. The pressure alarm devices (10) are located on a connecting pipe between the nitrogen inlet pipe (7) and the blowdown pipe (8) and on a connecting pipe between the nitrogen inlet pipe (7) and the discharge pipe (9). The process system is applicable to process preparation of ethambutol hydrochloride.

According to the invention, cheap and easily available L-threonine is used as a raw material to synthesize L-2-aminobutyric acid, and then the L-2-aminobutyric acid is used as an intermediate to synthesize ethambutol hydrochloride. Firstly, an enzyme catalysis method is used, L-threonine is used as a raw material, and L-2-aminobutyric acid (D-2-aminobutanol and L-2-aminobutyric acid are both in Sconfiguration) is prepared through a 'one-pot method'; the intermediate reacts with oxalyl chloride to generate a dicarboxylic acid compound containing diamide groups, and then cobalt catalytic hydrogenation reduction is conducted to obtain ethambutol; and hydrogen chloride gas is introduced to generate ethambutol hydrochloride. The process has the characteristics of low cost, simplicity and convenience in operation, environmental friendliness, high conversion rate and high optical purity of the product.

The invention belongs to the technical field of medicines, and relates to a quadrigeminal compound preparation of anti-tuberculosis medicines and a preparation method thereof. The compound preparation is prepared by combining anti-tuberculosis first-line medicines rifampin, isoniazid, pyrazinamide and ethambutol hydrochloride according to a specific ratio. The compound preparation is a gastric-dissolved dressed tablet, and is characterized by being prepared according to the following steps: firstly preparing a quadrigeminal base tablet, wherein the quadrigeminal base tablet comprises proper amount of a stabilizing agent, a disintegrating agent, an adhesive, a filler, a flow aid and a lubricant; sieving rifampin by using a 80 mesh sieve, sieving the other raw materials and auxiliary materials by using a 20 mesh sieve; weighing the prescription amount of isoniazid, pyrazinamide and ethambutol hydrochloride, adding the disintegrating agent, the adhesive and the filler, mixing uniformly, and preparing an integral particle by employing a wet process; then adding the prescription amount of rifampin, the stabilizing agent, the flow aid and the lubricant and mixing uniformly; and tabletting and dressing, so as to obtain the preparation. The method is convenient in operation, simple in technology, free of equipment reconstruction and low in cost, and has important social and economic benefit.