RU2623871C1 - Method of obtaining euphilline - Google Patents
Method of obtaining euphilline Download PDFInfo
- Publication number
- RU2623871C1 RU2623871C1 RU2016109213A RU2016109213A RU2623871C1 RU 2623871 C1 RU2623871 C1 RU 2623871C1 RU 2016109213 A RU2016109213 A RU 2016109213A RU 2016109213 A RU2016109213 A RU 2016109213A RU 2623871 C1 RU2623871 C1 RU 2623871C1
- Authority
- RU
- Russia
- Prior art keywords
- theophylline
- aminophylline
- ethylenediamine
- producing
- euphilline
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
- C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Изобретение относится к области органической химии, а именно к способу получения фармакопейного эуфиллина (аминофиллина).The invention relates to the field of organic chemistry, and in particular to a method for producing pharmacopoeial aminophylline (aminophylline).
Известен способ получения эуфиллина, по которому смешивают теофиллин с этилендиамином (см. https://ru.wikipedia.org/wiki/Эуфиллин).A known method of producing aminophylline, by which theophylline is mixed with ethylenediamine (see https://ru.wikipedia.org/wiki/Eufillin).
Недостатком известного способа является то, что полученный по известному способу продукт нестабилен при хранении, кроме того, прямое смешение теофиллина и этилендиамина имеет ряд технологических недостатков вследствие физико-химических свойств этилендиамина, являющихся едкой летучей жидкостью.The disadvantage of this method is that the product obtained by the known method is unstable during storage, in addition, the direct mixing of theophylline and ethylenediamine has a number of technological disadvantages due to the physicochemical properties of ethylenediamine, which is a caustic volatile liquid.
Технический результат, на достижение которого направлено изобретение, заключается в получении эуфиллина фармакопейного качества с длительным сроком хранения, производство которого является менее опасным.The technical result to which the invention is directed is to obtain pharmacopoeial aminophylline with a long shelf life, the production of which is less dangerous.
Технический результат достигается распылением спиртового раствора этилендиамина на теофиллин при перемешивании, с последующей выдержкой под вакуумом и одновременной сушкой смеси от спирта изопропилового.The technical result is achieved by spraying an ethylene diamine alcohol solution onto theophylline with stirring, followed by exposure to vacuum and simultaneous drying of the mixture from isopropyl alcohol.
Полученный по предлагаемому способу продукт отвечает нормам и требованиям Государственной Фармакопеи и может быть использован в производстве лекарственных бронхолитических средств.Obtained by the proposed method, the product meets the standards and requirements of the State Pharmacopoeia and can be used in the manufacture of medicinal bronchodilators.
Сущность способа получения эуфиллина заключается в получении эуфиллина (аминофиллина) формулыThe essence of the method of producing aminophylline is to obtain aminophylline (aminophylline) of the formula
путем смешения теофиллина и этилендиамина.by mixing theophylline and ethylenediamine.
В смеситель загружается (180,0-220,0) кг теофиллина, на который при перемешивании распыляется предварительно полученный спиртовый раствор этилендиамина (10,0-12,0 л спирта изопропилового и 30,0-35,0 кг этилендиамина). Масса перемешивается в течение 1 часа, затем выдерживается под вакуумом в течение 1,5 часов при охлаждении. Одновременно происходит сушка смеси от спирта изопропилового. Затем масса анализируется на содержание этилендиамина и прозрачность раствора. Прозрачность раствора - опалесценция раствора не должна превышать опалесценцию эталонного раствора II. Содержание этилендиамина должно быть (13,5-15,0)% в пересчете на безводное вещество. Далее эуфиллин просеивается через вибросито и передается на стадию упаковки и маркировки.(180.0-220.0) kg of theophylline is loaded into the mixer, onto which a previously prepared ethylene diamine alcohol solution (10.0-12.0 l of isopropyl alcohol and 30.0-35.0 kg of ethylene diamine) is sprayed with stirring. The mass is stirred for 1 hour, then kept under vacuum for 1.5 hours with cooling. At the same time, the mixture is dried from isopropyl alcohol. The mass is then analyzed for ethylene diamine content and solution transparency. The transparency of the solution - the opalescence of the solution should not exceed the opalescence of the reference solution II. The content of ethylenediamine should be (13.5-15.0)% in terms of anhydrous substance. Further, aminophylline is sieved through a vibrating screen and transferred to the packaging and labeling stage.
Для получения эуфиллина для нестерильных лекарственных средств загрузку этилендиамина и теофиллина в пересчете на сухое вещество производят в соотношении 1:6.To obtain aminophylline for non-sterile drugs, the loading of ethylene diamine and theophylline in terms of dry matter is carried out in a ratio of 1: 6.
Для получения эуфиллина для стерильных лекарственных средств загрузку этилендиамина и теофиллина в пересчете на сухое вещество производят в соотношении 1:4.To obtain aminophylline for sterile drugs, the loading of ethylene diamine and theophylline in terms of dry matter is carried out in a ratio of 1: 4.
Claims (5)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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RU2016109213A RU2623871C1 (en) | 2016-03-15 | 2016-03-15 | Method of obtaining euphilline |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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RU2016109213A RU2623871C1 (en) | 2016-03-15 | 2016-03-15 | Method of obtaining euphilline |
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RU2623871C1 true RU2623871C1 (en) | 2017-06-29 |
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RU2016109213A RU2623871C1 (en) | 2016-03-15 | 2016-03-15 | Method of obtaining euphilline |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN114939393A (en) * | 2022-06-01 | 2022-08-26 | 青岛科技大学 | System and method for continuously producing aminophylline |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2481715A (en) * | 1947-02-26 | 1949-09-13 | Merck & Co Inc | Theophylline-ethylenediamine compound and method of preparing same |
US2629717A (en) * | 1951-12-22 | 1953-02-24 | Pfizer & Co C | Preparation of aminophylline |
US2752285A (en) * | 1950-10-09 | 1956-06-26 | Weissenburger Helmut | Process for the production of at least approximately neutral solutions of substituted xanthines |
US4368197A (en) * | 1979-02-21 | 1983-01-11 | Research Corporation | Zinc aminophylline and its use in the treatment of bronchospasms |
-
2016
- 2016-03-15 RU RU2016109213A patent/RU2623871C1/en active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2481715A (en) * | 1947-02-26 | 1949-09-13 | Merck & Co Inc | Theophylline-ethylenediamine compound and method of preparing same |
US2752285A (en) * | 1950-10-09 | 1956-06-26 | Weissenburger Helmut | Process for the production of at least approximately neutral solutions of substituted xanthines |
US2629717A (en) * | 1951-12-22 | 1953-02-24 | Pfizer & Co C | Preparation of aminophylline |
US4368197A (en) * | 1979-02-21 | 1983-01-11 | Research Corporation | Zinc aminophylline and its use in the treatment of bronchospasms |
Non-Patent Citations (1)
Title |
---|
Халецкий А.М. Фармацевтическая химия // Л.: Медицина, 1966. - 706 с. (с.518-519). * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN114939393A (en) * | 2022-06-01 | 2022-08-26 | 青岛科技大学 | System and method for continuously producing aminophylline |
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