Method of producing prolonged-term preparation

专利摘要:
A method of preparing a preparation made up by bodies comprising an active component in decreasing concentration towards the surface of the bodies. The method comprises coating a particle with a composition comprising the active component in a continuous coating operation whereby the concentration of the active component is decreased. The active component may be a drug, a pesticide or an agent having some other effect.
公开号:SU1326180A3
申请号:SU762420506
申请日:1976-11-17
公开日:1987-07-23
发明作者:Бере Богентофт Конны；Генры Аппелгрен Курт
申请人:Аб Хессле (Фирма)；
IPC主号:

专利说明:

eleven
This invention relates to medicine and relates to a method for the preparation of a sustained release preparation.
The purpose of the invention is to improve the accuracy of controlling the release rate of the active substance.
Example 1. For 500 g of granules with a diameter of 0.5-0.75 mm, serving as a core and consisting of 50% alphenolol-HCl, 25% lactose and 25% starch, a solution is sprayed in a fluidized bed apparatus alpre nolol and cetanol for 75 min. In addition, alprenolol and cetanol are used in the amount of 300 g each. Alprenolol “HC1 methylene chloride / methanol stock solution is sprayed for 11 minutes, after which the concentration of alprenolol hydrochloride in the solution is continuously reduced during the deposition process by adding cetanol in methylene chloride and methanol solution in an amount of 4.7 g / min during last 64 minutes The grain size of the resulting preparation is 0.75-1.0 mm.
Alprenolol recoil rate (in water at) 0-5 min 4.8% / min, 5-10 min 5.2% / min, 10-20 min 4.7% / / min.
An additional coating of the following composition can be applied to the obtained granules: 50 g of ethylcellulose (this is the target of N - 10) and 10 g of acetyltributyl citrate (citroflex A-4). In addition, the application process is also carried out in a fluidized bed apparatus. After this treatment, the following recoil rate is obtained: 1-6 h 0.18% / min 6-9 h 0.14% / min.
EXAMPLE 2. For 500 g of metoprolol tartrate in the form of granules with a diameter of 0.5–0.75 mm, a solution containing 90 g of metoprolol tarrate, 40 g of talc, 10 g of finely divided silicic acid ( aerosil) and 10 g of cetanol. In the period from 30 to 89 minutes, a solution containing 300 g of cetanol in the amount of 5.1 g of cetanol per minute is added to the solution. The consumption of cetanol is 300.9 g. After the application process is complete, the granule size is 0.75-1.0 mm. In this example, the ratio of the active substances of the core and the coating is 1: 0.18, and the ratio of the added inactive substance to the active substance is applied
Q 5 0 5
about
d

five
five
802
my coverage is 1: 0.3. The release rate of the active substance in water is 2.3% / min.
Example A solution containing 200 g of caffeine and 10 g of polyvinylpyrrolidone (PVP K 30) is sprayed onto 500 g of sugar granules (0.6-0.75 mm) for 70 minutes. The ratio of the inactive substance of the core to the active substance of the coating is 1: 0.4. After 15, 30, 45 minutes and 250-rpa fMO portions of a solution containing 50 g of polyethylene glycol 6000 (polyethylene glycol consumption 200 g) are added. Thus, the ratio of inactive substance added to the coating to the active substance of the coating is 1: 1.
Example4. A solution containing 200 g of cetanol, 50 g of quinidine bisulfate and a solvent is sprayed onto 500 g of quinidine used as dra bisulfate in the form of granules with a diameter of 0.75-1.0 mm. The obtained granules are coated with 50 g of ethyl cellulose (Ethocel No. 10), 10 g of copolymer (acrylic and methacrylic acid esters — RS-100) and 10 g of acetyl tributyl citrate (citroflex A-4). The size of the obtained granules is 1.0-12 mm. The recoil rate is 6% / hour for 16 hours.
Example5. 250 g of K4 grade used as a sugar core are sprayed with 250 g of quinidine bisulfate solution in a fluidized bed apparatus. For 500 g of the granules thus obtained, a solution containing 300 g of quinidine bisulfate is applied for 73 minutes in the same apparatus. During the first 56 minutes, a solution containing 200 g of cetanol is continuously added to this solution at a rate of 3.6 g cetanol / min . The recoil rate is 1.8% / min.
Example For 500 g of urea granules (granule diameter 2 mm) spray for 75 min 1650 g of a solution that contains 50 g of urea and 100 g of cetanol (0.1 g of the active substance and 0.2 g of inactive substance per 1 g of the active substance of the core) . After 45 minutes, 225 g of a 25% solution of cetanol (0.1 g of inactive substance per 1 g of active ingredient core) are added, and after 70 minutes an additional 375 g of this solution (0.19 g of inactive substance per g of active ingredient core ). Granules are coated with a film which consists of IDO g of ethyl cellulose No. 10, 20 g of aydragite RS 00, and 20 g of citroflex A-4. The rate of release of the active substance is presented in the table.

权利要求:
Claims (1)
[1]
Invention Formula
The method of obtaining a drug of prolonged action, including P. Geresi
Compiled by V. Brusilovsk
Tehred N.Glushchenko Proofreader i.Musk
Order 3128/58 Circulation 595 Subscription
VNIIPI USSR State Committee
for inventions and discoveries 113035, Moscow, Zh-35, Raushsk nab., 4/5
Production and printing company, Uzhgorod, st. Project, 4
1326180
at room temperature per core, containing one pharmacologically active substance and / or one inactive substance, a coating containing an active substance and an inactive substance that is insoluble in water, characterized in that, in order to improve the accuracy of controlling the release rate of the active substance, coating The nucleus is carried out in the fluidized bed for 0.5-2 hours with the ratio of the active substances of the core and the coating (1: 0.11: 1, 2) or the inactive substance of the core and the active substance of the coating in the ratio 1: 0.006-1: 2.2 last which was added continuously or intermittently added to the coating inactive
substance to a ratio of 1: 0.013– 1: 2.75, while pesticide, herbicide, plant growth regulator or fertilizer is used as the active substance, and as inactive
the substances are lipophilic compounds, a water soluble polymer, or dispersing agents.

类似技术:

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SU1326180A3|1987-07-23|Method of producing prolonged-term preparation

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同族专利:

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公开号 | 公开日

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FR2331375B1|1981-12-31|

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ZA766669B|1977-10-26|

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MY8400019A|1984-12-31|

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FI763257A|1977-05-18|

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DK146213C|1984-01-16|

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NL7612728A|1977-05-20|

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DK513476A|1977-05-18|

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IE44353L|1977-05-17|

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AU1961776A|1978-05-25|

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AU508266B2|1980-03-13|

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US4289795A|1981-09-15|

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FI62462C|1983-01-10|

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BE848406A|1977-05-17|

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IE44353B1|1981-11-04|

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SE418247B|1981-05-18|

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DD128170A5|1977-11-02|

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DE2651176A1|1977-05-18|

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JPS5283921A|1977-07-13|

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FR2331375A1|1977-06-10|

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AT354636B|1979-01-25|

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DE2651176C2|1987-06-11|

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GB1560841A|1980-02-13|

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ATA850576A|1979-06-15|

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LU76215A1|1977-06-06|

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NL187259C|1991-08-01|

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US4341759A|1982-07-27|

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HU173461B|1979-05-28|

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JPS5919526B2|1984-05-07|

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NO763807L|1977-05-20|

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NO144763B|1981-07-27|

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CS207374B2|1981-07-31|

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NO144763C|1981-11-04|

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NZ182621A|1978-12-18|

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FI62462B|1982-09-30|

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NL187259B|1991-03-01|

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DK146213B|1983-08-01|

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SE7512883L|1977-05-18|

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CA1075031A|1980-04-08|

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HK14683A|1983-05-13|

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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SE7512883A|SE418247B|1975-11-17|1975-11-17|SET TO MAKE BODIES WITH REGULATED RELEASE OF AN ACTIVE COMPONENT|

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