专利摘要:
Die Erfindung beschreibt ein neues Verfahren zur zeitlichen Steuerung der Wirkstofffreisetzung aus Retardzubereitungen, insbesondere Arzneimittelzubereitungen. Die Freigabegeschwindigkeit wird erfindungsgemäss eingestellt durch Zugabe von hydrophilen Polymeren einer bestimmten Viskosität, wobei von der Gesetzmässigkeit Gebrauch gemacht wird, dass die Freigabegeschwindigkeit der Wirkstoffe mit steigender Viskosität zunimmt.
公开号:SU1375114A3
申请号:SU823452763
申请日:1982-06-21
公开日:1988-02-15
发明作者:Кнехт Адольф;Аугарт Гельмут
申请人:Гедеке Аг (Фирма);
IPC主号:
专利说明:

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ate
FIELD OF THE INVENTION The present invention relates to pharmaceutical industry, namely to means for the preparation of prolonged action preparations. .
The purpose of the invention is to simplify the method.
The method is carried out as follows.
The active substance is mixed with auxiliary substances and hydrophilic, while the hydrophilic polymer is taken with a viscosity of 0.02-40 Pa-s in an amount of 0.1-10% by weight of the product.
The method is illustrated by the following examples.
Example 1. 100 g hydrogenated-. Castor oil, 150 g of stearic acid and 750 g of lactose are homogeneously mixed with 10 g (0.99% by weight of the composition) of carboxymethylcellulose with the following viscosity and the resulting mixture is granulated from the melt a.
Carboxymethylcellulose with the following viscosity is used. Pas: 0.05; 0.3; 0.6; 3; 6; 20; 40
In each case, the granules are processed into round convex tablets weighing 490 mg and 11 mm in diameter using one syringe pressure. Pad dosage is determined by their weight loss after storage in artificial gastric and intestinal juices according to the standard. When this tablet is removed from the juice, dried at 45 ° C for 10 h and weighed.
Example 2. 300 mg tablets containing 60 mg of diltiazem hydrochloride as the active substance are prepared. Carboxymethylcellulose with viscosity is used.
five
0
ABOUT
0
five
five
0.3 Pa.s in an amount of 0.1% by weight of the product. The following results are obtained on the release of the active substance: 34% after 1 h; 52% after 2 h; 75% after 3.5 hours and 83% after 5 hours.
Example 3. Example 1 is repeated with the difference that 1% by weight of carboxymethylcellulose with a viscosity of 0.02 is used. The weight loss is 22% after 1 hour, 27% after 2 hours, 36% after 3.5 hours, 53% after 5 hours and 79% after 7 hours.
Example 4. Example 1 is repeated with the difference that carboxymethylcellulose with a viscosity of 0.3 Pa-s is used in an amount of 10% by weight of the agent. The weight loss is 33% after 1 hour, 52% after 2 hours, 85% after 3.5 hours.
The proposed method simplifies the process of obtaining a prolonged action agent by eliminating the stage of coating by using a hydrophilic polymer with a specific viscosity and in a certain amount.
A low viscosity polymer leads to an increased degree of slow release of the active substance.
权利要求:
Claims (1)
[1]
Invention Formula
A method of obtaining an agent of prolonged action by mixing the active substance with auxiliary substances and a hydrophilic polymer, characterized in that, in order to simplify the process, a hydrophilic polymer is taken with a viscosity of 0.02-40 Pa-s in an amount of 0-10% by weight facilities.
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同族专利:
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AU8536182A|1983-01-06|
FI78391B|1989-04-28|
CA1208556A|1986-07-29|
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引用文献:
公开号 | 申请日 | 公开日 | 申请人 | 专利标题

DE1492019A1|1963-06-20|1969-02-20|Ministerul Ind Petrolului Si C|Surcharge for medicinal tablets and methods of obtaining them|
NL159577B|1968-02-15|1979-03-15|Organon Nv|PROCESS FOR PREPARING FAST DISINTEGRATING SOLID PARTS.|
GB2042888B|1979-03-05|1983-09-28|Teijin Ltd|Preparation for administration to the mucosa of the oral or nasal cavity|
US4226849A|1979-06-14|1980-10-07|Forest Laboratories Inc.|Sustained release therapeutic compositions|
US4259314A|1979-12-10|1981-03-31|Hans Lowey|Method and composition for the preparation of controlled long-acting pharmaceuticals|GB8403360D0|1984-02-08|1984-03-14|Erba Farmitalia|Pharmaceutical compositions|
GB8403361D0|1984-02-08|1984-03-14|Erba Farmitalia|Pharmaceutical composition|
US4608248A|1985-11-08|1986-08-26|Warner-Lambert Company|Process for time-controlled release of active ingredients|
DE3737741A1|1987-11-06|1989-05-18|Goedecke Ag|ORAL MEDICAL FORM FOR THE ONLY DAILY TREATMENT OF HYPERTENSION WITH DILTIAZEMHYDROCHLORIDE|
FR2630913A1|1988-05-09|1989-11-10|Delalande Sa|DILTIAZEM WATER SOLUBLE SALTCOMPRESSES WITH PROGRAMMED RELEASE AND METHOD OF MANUFACTURING THE SAME|
ES2036123B1|1990-12-03|1994-01-16|Neila Nieto Jorge Juan|MANUFACTURING PROCESS OF SOLID INORGANIC FERTILIZERS CONDITIONED WITH WATER RETAINING POLYMERS.|
ES2042418B1|1992-05-18|1994-07-01|Tecno Holding S A|METHOD FOR THE EXTERNAL TREATMENT OF VEGETABLE CROPS.|
US6440457B1|1993-05-27|2002-08-27|Alza Corporation|Method of administering antidepressant dosage form|
GB2370775A|2001-01-04|2002-07-10|Nimrod Israely|Insecticidal composition based on attractant, insecticide and stabilizer, the outer surface of which expands & loses viscosity on contact with humidity|
法律状态:
优先权:
申请号 | 申请日 | 专利标题
DE19813125178|DE3125178A1|1981-06-26|1981-06-26|METHOD FOR THE TIMED CONTROL OF THE RELEASE OF ACTIVE SUBSTANCES FROM ACTIVE SUBSTANCE PREPARATIONS, IN PARTICULAR DRUG PREPARATIONS|
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