• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The invention provides a method for preparing sustained release tablets comprising a hydrophilic polymer matrix, which amounts to at least 10% by weight of the composition, consisting of a 5:1-1:5 weight to weight ratio mixture of a VP-VA copolymer and of an acrylic acid homopolymer, cross-linked with polyallyl saccharose. The method of manufacturing of sustained release tablets according to the invention can be accomplished in two ways: either by manufacturing the granulate containing the active ingredient, or by supplementing the matrix granulate containing no active ingredient with the suitable amount of the active ingredient. The latter variant involves the advantage of a possible separation of large-scale manufacturing of pharmacons and that of a generally applicable retardizing system, the composition and, consequently, the retardizing ability of which can optionally be modified in accordance with the properties of the active ingredient(s) to be formulated.
    公开号:SU1577684A3
    申请号:SU843814617
    申请日:1984-11-09
    公开日:1990-07-07
    发明作者:Беззег Денеш；Фекете Пал；Тот Золтан；Бор Илона；Феллнер Эржебет
    申请人:Эдьт Дьедьсерведьесети Дьяр (Инопредприятие)；
    IPC主号:
    专利说明:

    (Ls
    This invention relates to the pharmaceutical and pharmaceutical industry and concerns a process for the preparation of tablets.
    The purpose of the invention is quality improvement.
    Example 1. The manufacture of tablets, which contain chlorpyramine hydrochloride as the active substance.
    The following substances are weighed into the fluidized bed spray granulation unit (Glatl WSG I type): 700 g of chloropyramine hydrochloride, 350 g of carbopol 934, 350 g of lyuviscol.
    Granulation is carried out using granulating solutions given in a table. one .
    Stearinova
    Acid 50 P 50 g Polyethylene glycol 50 g - Hydroxypropyl-cel-oba 50 g -
    .-and- - - - - - -.-. - l
    Carbovax 6000. Klucel.

    s
    The granulation is carried out at a temperature of 25 ° C applied for fluidization, an infusion rate of granulating liquid of 25 ml / min; and a spray pressure of 0.5 bar.
    In Experiment 3, it was not possible to produce suitable granules for further processing, since when spraying i-propanol, it was not granules with an hour size of a few tenths of mm, but aggregates with a particle size of a few cm. 1% magnesium stearate and 2% talc are mixed in and from the resulting product homogenizing press Gg on an eccentric tabletting machine (Fette EXI; a straight-edge mold for direct pressing, 8 mm in diameter) with a pressing force of 1,500 N tablets (weight 0917 g contained s active substance 75 mg). The dissolution of the active substance is determined in an apparatus for determining the decomposition of US P XX with the use of 0.1N. hydrochloric acid solution at 37 ° C. 700 ml of dissolving liquid are loaded into the dissolution vessel. Six tablets are placed in the dissolving tank. The container moves in the usual manner in a dissolving liquid. Samples are taken from the liquid hourly, the content of the active substance in which is determined by a spectrophotometer.
    The results of the dissolution of the active substance are shown in Table 2.
    Table 2
    Time h
    one
    21, 1
    29.9
    46.6
    PRI me R 3. The manufacture of tablets, which as the active substance contain benzcyclan.
    200 ma.ch. benzcyclan-fumarata, 57.5 ma.ch. Kollidona V A64 and
    Continuation of table 2

    PRI mme R 2. The manufacture of tablets, which as the active substance contain nitroglycerin.
    25.0 kg of luviscol VA 64 and 25.0 kg of carbopol 934 are weighed into the vessel of the fluidized-bed granulating apparatus (Glalt WSG120), after which the powder mixture is granulated with a solution of 2.7 kg of Karbovaks 6000, 2.7 kg of stearic acid and 32 kg isopropane © la (40 C). The granulating fluid is added at a rate of 1000 ml / min. The pressure applied during spraying is 3 bar, the air flow rate is 1000-1200 m3 / h and the outlet air temperature is 40 C. The granules formed are dried to a moisture content of 4% and homogenized as described in example 2 method with milk sugar containing 10% nitroglycerin.
    From the obtained homogenization product, tablets with a diameter of 6 mm, a nitroglycerin content of 2.5 mg and a total weight of 80 mg are pressed. The dissolution of nitro-glycerin from the tablets is determined by the method described in Example 1 according to the half-change method. The amount of dissolved nitroglycerin is measured between the first and the eighth hours every hour.
    The following results were obtained:
    60.7 73.4
    91.0
    100
    57.5 ma.ch. Carbopol 934 is stirred and moistened evenly with a solution of 9 mash, carbovax 6000, 9 parts by weight (stearic acid and 80 masses of isopropanol. The resulting wet aggregate
    passed through a sieve (sieve opening size 0.9 mm), dried and sieved again. After the addition of 7 mach. magnesium stearate and 10 ma.ch. Talcum from the resulting homogenization product compressed tablets containing an asset
    one
    20.0 42.4 44 ,:
    PRI me R 4. The manufacture of tablets, which as the active substance contain trilibet.
    80 ma.ch. trelibeta, 33.6 ma.ch. plazdona VA 630 and 33.6 ma.ch. Carbole 934 is mixed and thoroughly moistened with a solution and 3.2 parts by weight. Carbovax 6000, 1.6 mAh.h. stearic acid and 50 ma.ch. ethanol. The wet aggregate is passed through a sieve (the opening size of the sieve is 1.2 mm) is dried and
    Time, h Dissolved active substance,%
    one
    eight
    30.8 44.3 53.8 61.8 70.5 79.4 84.5 92.0
    Example 5. The manufacture of tablets, which as an active substance contain ferrous sulfate and vitamin C.
    To 1.00 kg of the matrix granules of a harmless medicine prescribed in Example 3, prescribed for calming the patient, add 3,200 kg 1.5 l 0.200 kg polyvinyl butyral (movital VZOT), 0.400 kg ascorbic acid (vitamin C); 0.15 kg of talc and 0.05 kg of magnesium stearate
    Time, h Dissolved active substance,%
    PRI me R 6. The content in the quality of the active substance Melipramine.
    100.00 g of powdered Melipramine, 75.0 g of Luviscol VA 64 and 75.0 g of Carbopol 934 are homogenized and uniformly moistened with a solution of 5.0 g of Carbowax 6000 heated to 40 C (polyethylene substance 200 mg, with a total weight of 350 mg and a diameter of 10 mm. The recoil of the active substance is checked on a decomposition apparatus (USP XX) using the half-change method. The following results are obtained.
    eight
    50.7
    59.0 68.7 77.4 84.8
    sift again (sieve opening size 0.9 mm). The granules are mixed with 4.8 mach. talc and 3.2 ma.ch. magnesium stearate and pressed into tablets weighing 160 mg with an active substance content of 80 mg and a diameter of 8 mm.
    The recoil of the active substance of the tablets is determined by the method of half change as described in Example 1, between the first and the eighth hour.
    The following results were obtained.
    eight
    neither From the homogenization product, tablets with a total weight of 0.500 g, a Geg content + 100 mg, a Vitamin C content of 40 mg and a diameter of 12 mm are made on a rotary tablet machine (EBM Manesty). The dissolution of the Fe2 + tablet is determined by the method of half-change using a device for determining the dissolution with rotating blades (USP XX) at a speed of 100 rpm.
    The following results were obtained:
    62.2 75.0 79.4 82.5 85.5
    lenglycol), 5.0 t of stearic acid and 60.0 ml of isopropane. The wet substance is granulated on an acid-resistant sieve (sieve opening size 18), and the wet granules are dried at 40 ° C to a moisture content below 1%.
    The dry granules are again granulated and then homogenized with 6.0 g of talc and 4.0 g of magnesium stearate. From the homogenization product, tablets with a total weight of 0.135 g and with a dia
    one
    30-35 45-55 55-65 65-75 75-85 85-95 Example 7. Production of a tablet of currents that contain theophylline as the active substance.
    Using the matrix granules of a harmless drug made according to Example 2 (test 4), prescribed Q to calm the patient, a powder mixture of the following composition is prepared;
    Theophylline Matrix is a harmless medication prescribed


    20-25 28-33 34-40 50-55 65-70 80-90
    The proposed method for the preparation of tablet-35 flyers provides an improvement in the quality of tablets compared to the known, since the resulting tablets have
    less hygroscopicity, no agrega40
    the polymers used.
    权利要求:
    Claims (1)
    [1]
    Invention Formula
    A method for producing tablets by mixing the active substance with fillers, granulating and tabletting.
    meter 7 mm. The dissolution rate of the tablets thus prepared was determined by the method of half change. “The following results were obtained:
    for calming the patient Carbovax 6000 Magnesium Stearate Talc
    Common
    weight 350.0
    From the powder mixture, tablets are pressed with a total weight of 0.350 g and a diameter of 10 mm. The dissolution of the active substance is determined by the method of half change and the following results are obtained:
    characterized in that, in order to improve the quality, the granulation is carried out by spraying in the fluidized bed, the mixing is carried out predominantly with chlorpyramine CM- (p-chlorobenzyl) -N- (2-pyridyl) -Y -N -dimethyl-ethylenediamine with vinylpyrrolidone-vinyl acetate and polyacrylic acid at a ratio of (5: 1) - (1: 5) in the presence of 0.5-10% by weight of stearic acid and / or cetyl stearin alcohol in an isopropanol solution.
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    同族专利:
    公开号 | 公开日
    GB8428369D0|1984-12-19|
    GB2149413B|1987-04-08|
    SE8405615D0|1984-11-09|
    HUT34892A|1985-05-28|
    UA5328A1|1994-12-28|
    FI78614B|1989-05-31|
    NL8403447A|1985-06-03|
    JPS60222413A|1985-11-07|
    FR2554717A1|1985-05-17|
    DD229030A5|1985-10-30|
    BE901007A|1985-05-08|
    CH665124A5|1988-04-29|
    FR2554717B1|1988-05-13|
    DE3441308C2|1994-03-31|
    GB2149413A|1985-06-12|
    JPH0751497B2|1995-06-05|
    FI844405A0|1984-11-09|
    SE8405615L|1985-05-12|
    ATA355084A|1990-02-15|
    HU190619B|1986-09-29|
    AT391078B|1990-08-10|
    SE455571B|1988-07-25|
    FI78614C|1989-09-11|
    US4647599A|1987-03-03|
    FI844405L|1985-05-12|
    DE3441308A1|1985-05-23|
    引用文献:
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    US3634584A|1969-02-13|1972-01-11|American Home Prod|Sustained action dosage form|
    US3590117A|1969-03-24|1971-06-29|Richardson Merrell Inc|Long-lasting troche containing guar gum|
    US3870790A|1970-01-22|1975-03-11|Forest Laboratories|Solid pharmaceutical formulations containing hydroxypropyl methyl cellulose|
    SE353229B|1970-06-04|1973-01-29|Haessle Ab|
    FR2247206B1|1973-01-24|1978-02-03|Sterwin Ag|
    US3851032A|1973-04-23|1974-11-26|Sterling Drug Inc|Process of preparing a solid fine crystalline paracetamol polymer complex composition|
    US3923974A|1973-04-23|1975-12-02|Sterling Drug Inc|Solid fine crystalline paracetamol polymer complex composition|
    GB1568837A|1975-10-10|1980-06-04|Squibb & Sons Inc|Controlled release tablet|
    FI63335B|1979-02-02|1983-02-28|Orion Yhtymae Oy|FARING REFERENCE FOR A TABLETTER WITH A LIGHT LIGHT OF AN EFFECTIVE|
    US4252786A|1979-11-16|1981-02-24|E. R. Squibb & Sons, Inc.|Controlled release tablet|
    IL61721A|1980-12-16|1984-03-30|Blank Izhak|Nitroglycerin preparations|
    HU183408B|1981-04-28|1984-05-28|Chinoin Gyogyszer Es Vegyeszet|Process for producing oral ratard pharmaceutical compositions|
    ZA822995B|1981-05-21|1983-12-28|Wyeth John & Brother Ltd|Slow release pharmaceutical composition|
    US4557925A|1982-07-08|1985-12-10|Ab Ferrosan|Membrane-coated sustained-release tablets and method|HU196711B|1986-06-24|1989-01-30|Istvan Racz|Process for producing long-acting, gastric acid neutralizing pharmaceutics with high acid-binding capacity and increased bioavailability|
    GB2201594B|1986-06-24|1991-02-13|Istvan Racz|Production of acid binding pharmaceutical preparations|
    US4844908A|1986-11-27|1989-07-04|Duphar International Research B.V.|Method of preparing tablets with clovoxamine fumarate and tablets thus prepared|
    US5030454A|1987-10-26|1991-07-09|Alza Corporation|Method for delivering drug in tiny pills in liquid carrier|
    US4853229A|1987-10-26|1989-08-01|Alza Corporation|Method for adminstering tiny pills|
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    US5051261A|1987-11-24|1991-09-24|Fmc Corporation|Method for preparing a solid sustained release form of a functionally active composition|
    US4925676A|1989-02-02|1990-05-15|Warner-Lambert Company|Extended release gemfibrozil composition|
    US4971804A|1989-02-02|1990-11-20|Warner-Lambert Company|Water dispersible gemfibrozil compositions|
    US4927639A|1989-02-02|1990-05-22|Warner-Lambert Company|Modified release gemfibrozil composition|
    DE4138513A1|1991-11-23|1993-05-27|Basf Ag|SOLID PHARMACEUTICAL RETARD FORM|
    ES2061394B1|1993-02-05|1995-06-16|Robert S A Lab|MANUFACTURING PROCEDURE OF A POTASSIC CITRATE GRANULATE WITH DELAYED ASSIGNMENT.|
    JP3732557B2|1995-07-12|2006-01-05|住友精化株式会社|Carboxyl group-containing polymer composition|
    US6492488B1|1998-08-02|2002-12-10|Pmd Holdings Corp.|Controlled release polyacrylic acid granules and a process for preparing the same|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    HU833859A|HU190619B|1983-11-11|1983-11-11|Process for producing tablets with controlled dissolution of active ingredients|
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