• 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:
    METHOD OF GETTING A PLEASANT REMEDY by treating the ground seeds of the plantain with water, drying, granulating followed by draining, so that the plantain seeds are mixed with separately to reduce the side effects of substances associated with senna fruit. senna fruits with a ratio of fruits and seeds
    公开号:SU1145911A3
    申请号:SU813238931
    申请日:1981-01-16
    公开日:1985-03-15
    发明作者:Мадаус Рольф；Герлер Клаус
    申请人:Др.Мадаус Унд Ко. (Фирма)；
    IPC主号:
    专利说明:

    4 C71
    o i The invention relates to the chemical and pharmaceutical industry and is concerned with the production of a laxative agent. A known method of producing a laxative by treating the seeds of plantain with water, drying the granulation followed by draining 1. However, the preparation obtained by the known method causes undesirable side effects that. reduced to a strong irritation of the mucous membrane with a massive effect of alkaline-sensitive and susceptible to oxidation oxy-acid compounds in the fruit of senna and the negative effect of their decomposition products. The aim of the invention is to eliminate the side effects of substances which are not present in the fruit of senna. The goal is achieved by the fact that according to the method of obtaining a laxative by treating the ground seeds of the plantain with water, raising granulation followed by draining, the seeds of the plantain are mixed with the separately ground fruits of senna at a ratio of fruits and seeds (4-5): 1 with the addition of ground husks from the seeds of plantain in the amount of 3-4 wt.% of the mixture, then add 30 to 40 wt.% water, and granulate at 50 atm to a granule size of 2-2.5 m, then dried in a suspended f then ntga: E air flow for 0.5 h to residual lazhnosti 3.50 wt.% water. Example. Plantago ovata seeds are free from impurities and other seeds, dried at about 80 ° C to a moisture content of 3.5% and milled to a particle size distribution that corresponds approximately to the following sieve analysis: 99% smaller than 500 urn 85% smaller than 400 urn 50% smaller than 200 urn During grinding, the material is not heated up. Separately, sennosides of 2.2% are determined in the senna fruits (Sennae fructus arigustifoliae), if necessary, by mixing different batches. Grinding is carried out to the grain size corresponding to the specified sieve in preliminary stages of d12121 with preliminary grinding and fine grinding. with the addition of ground seed coat, Plantago ovata is mixed dry with carrier medium from traganth in the following proportions: 104.0 kg of psyllium seed (grinding product) 24.8 kg of senna fruit 4.4 kg of psyllium of plantain li-S - ESr SSIS 134.7 kg This powder mixture from the mixer is transferred to the mixing path of the extruder and mixed continuously with 30-40% water. In the wetted state, the mass is left for 1-2 hours in order to facilitate the spreading of the Micilago layers on the particles of senna fruit. The material is then pressed in an extruder with a large D-ratio at a pressure of about 50 atm and, at the exit of the press, is crushed into a pellet with a length of 2.1-2.2 mm using a separately controlled rotary knife. The moisture content of the granules should be 35%. Subsequent drying is carried out in a dryer containing a fluidized bed, with a vibratory feeding mechanism up to a moisture content of not more than 3.5% for about 25 minutes at air temperature and air passing 8000 m / h. Dried granules are processed using a slurry for coating (except for sucrose, it may contain aromatic essences common in pharmaceutical technology, such as peppermint oil, caraway and sage oils, as well as pigments). The obtained laxative in daily doses of 1-5 g is used for constipation and for regulating stool. The proposed laxative has the following composition, kg per 100 kg of pelletized granulate: Ground grinding product Plantaginis ovatae 52,000 Ground seed grinding product Plantaginis ovatae 2,200 Fruit grinding product; Sennae august foliae 12,400 17,600 0,035 Oleum Carvi Oleum Salviae Oleum Menthae piperitae 12,459 Gum arabic Tragant Paraffinum subliguidum Paraffinum durum Ferrium oxydatum Test for toxicity and adverse effects. Acute toxicity was tested on rats and mice of both sexes (labor of 40 animals). They were injected with a pulverized laxative of the indicated dostak in a freshly suspended form in water orally. Then the animals were observed for 8 days. Accurate determination of HHso was not possible, since the laxative toxicity is too low. Even a one-hundred-fold exercise of the daily dose recommended for humans did not lead to any harmful effect on animals. Thus, you can specify only the following minimum. for rats, 5 g / kg; for a smaller one, 10 g / kg. Additionally, super-acute toxicity was investigated in rats and mice by daily administration of drugs in the amount of 0.5, 1.0 and 2 g / kg orally for 15 days. Fatal outcomes are not. To test chronic toxicity, a laxative was administered to two groups of Sprague Danley rats of both sexes weighing 150 g each at a dose of 0.5 g / kg and 1.0 g / kg. In animals, before and after treatment, the increase in the number of erythrocytes, leukocytes, differential hemogram, blood sugar, prothrombin, trans-amyase and residual nitrogen was determined. With this, no noticeable changes were found compared to the unproductive control group of animals. At the end of the study, all animals were killed and subjected to complete autopsy: the weight of the spleen, liver, heart, kidneys, adrenal glands, thyroid glands, ichchek and hypfiza showed no noticeable anomalies compared with contractile 14 animals. Histology and iita lysis did not show ikakrth deviations: cell and fatty infiltration, adenomatous hyperplasia of the liver, nephrosis, sinusoidal expansion of the adrenal glands, cell infiltration of the heart, adenomatous hyperplasia of the thyroid gland and cell infpration of the spleen and chypods and chypitis, and cell infpstrama, and adrenal hyperplasia of the thyroid gland and cell infpration of the spleen and chypes and chypes and chyroids, and adenomatous hyperplasia of the thyroid gland and cell infpration of the spleen and chypes and chyroids, and adenomatous hyperplasia of the thyroid gland and cell infpration of the spleen and chypes and chypes and chypes To determine the over-acute toxicity of the proposed formulation, it was administered orally to rats and dogs of both sexes in an amount that was 5 and 10 times higher than the dose recommended for humans for 30 days. It is noted that the proposed agent is well tolerated. Next, oral toxicity was determined on rats and dogs for 180 days. Sprague Danley rats and hybrid dogs of both sexes were injected 2.5 and 3 times the dose recommended for humans, which animals tolerated well. During and after the treatment, no changes were observed in the development of body weight, hematological and urological functions, blood composition, the same result was obtained by macroscopic and microscopic studies of the main organs. It is especially necessary to notice that there was no bleeding or formation of abscesses in the gastrointestinal tract. Studies of male and female rabbits with daily administration of 1.0 g / kg orally in a 6-week cross-section did not show any adverse effects on body weight, red blood cell count and leukocyte count, differential hematogram, residual nitrogen and blood sugar. The teratogenic effect of the proposed laxative was tested on rats and rabbits at daily doses of 1 g / kg orally, which were administered to rats from the 7th to the 21st day of gestation and to rabbits from the 7th to the 15th day of gestation. The fruits were removed from animals, respectively, on the 21st and 27-1 days and examined. The specific teratogenic effect of the proposed laxative has not been established: obviously, the laxative has no effect on embryonic development. Testing the laxative effect Single doses of 2.5 and 5 g / kg of the orally proposed laxative were administered to mice, respectively. After 3-4 hours after administration, the effect of the substance was observed depending on the dose (an increase in the amount and softening of feces). The effect of the laxative on intestinal motors and on the duration of the passage of the intestinal contents was studied in Spragae-Danley rats of both sexes weighing 240 g. Groups of 10 animals after 24 hours of fasting were administered 22 ml / mg of aqueous suspension with 10% animal coal and 0, 5% carboxymethylcellulose, as well as 2.5 and 5 g / kg of the test laxative. Forty minutes after administration, the animals were sacrificed and the length of the small intestine was measured, and the length of its part, filled with suspension, was measured. We measured (Fri: Am. Swiss): with an average weight of 24 g and rat-Ea-Danley rat with an average weighing 230 g. After a 3-hour fast, the animals were placed in a cell with partitions, the bottom of which is lined with filter paper so that feces can be collected. Animals whose soft stools are not subjected to expert testing. The remaining animals are placed in a cage for treatment. They were administered orally (using an oral syringe) 2.5 and 5 g / kg laxative. At regular intervals of time up to 8 hours after the administration of the laxative, the number and type of FEGs are evaluated. The results are presented in the table. The results show a distinct laxative effect of the proposed laxative, which is expressed in an increase in the number of feces and a significant increase in the number of soft, fecal balls compared to solid balls. 16 The study also found that the proposed product does not have any choleretic effect. A diuresis test showed a decrease in kidney secretion, which seems to be associated with intestinal fluid secretion. The product, administered in doses of 1.0 and 2.0 g / kg in male rats weighing 280 g, does not cause any noticeable changes in arterial blood pressure and cardiac activity. Also, no inflammatory changes in the gastrointestinal tract were found. Thus, the proposed formulation has a good liblium mibile effect, while its toxicity is extremely low, and intolerance is not observed. No inflammatory changes in the gastrointestinal tract of animals that were treated with a high dose of laxative or subjected to prolonged treatment with this laxative were found. The proposed laxative does not affect embryonic development (no deviation from the normal development of the fruit, their number, weight was observed). The laxative effect of the agent appears 3-4 hours after administration to the experimental animals. It directly depends on the dose and manifests itself in the acceleration of the passage time of the intestinal contents, and that; - the same in the increase and softening of the stool. A study of treated diuresis shows a decrease in urinary cracking, which can be associated with an increase in intestinal fluid. Not set to - what changes in the flow of bile, smooth muscle function, arterial blood pressure or cardiac arthritis. The administration of the proposed laxative also does not affect daily food intake.
    Rats (groups of 10 animals)
    Note. In the table the prints are M - mild notation: T - solid feces,
    权利要求:
    Claims (1)
    [1]
    METHOD FOR PRODUCING A LIABILITY by treating the crushed seeds of plantain with water, drying, granulating followed by pelleting, characterized in that, in order to eliminate the side effects of substances accompanying the fruits of senna, the seeds of plantain are mixed with separately milled fruits of senna at a ratio of plaids and seeds ( 4-5): 1 with the addition of crushed husk from plantain seeds in an amount of 3 - 4 wt.% Of the mixture, then add 30-40 ma.Z of water and granulate at 50 atm to a granule size of 2-2.5 mm, then dried in suspension nnom state in air flow for 0.5 hours to a residual moisture content of 3.50 mae.Ya water.
    g s c ί
    类似技术:
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    同族专利:
    公开号 | 公开日
    GB2067402B|1984-01-25|
    ZA81254B|1982-02-24|
    IT8119154D0|1981-01-15|
    FI810095L|1981-07-17|
    HK75984A|1984-10-12|
    NL188452C|1992-07-01|
    DE3001357A1|1981-07-23|
    AU6624181A|1981-07-23|
    NZ196034A|1984-05-31|
    NO153594C|1986-05-21|
    AT372280B|1983-09-26|
    DE3001357C2|1986-08-21|
    GB2067402A|1981-07-30|
    DK153774C|1989-04-10|
    AR222269A1|1981-04-30|
    NL8100167A|1981-08-17|
    YU42551B|1988-10-31|
    FI75095C|1988-05-09|
    DK153774B|1988-09-05|
    FR2473311A1|1981-07-17|
    NO153594B|1986-01-13|
    IE50621B1|1986-05-28|
    MX7112E|1987-06-29|
    PT72358B|1981-12-18|
    SE454744B|1988-05-30|
    CH650403A5|1985-07-31|
    NL188452B|1992-02-03|
    DK15181A|1981-07-17|
    GR73649B|1984-03-26|
    LU83058A1|1981-06-04|
    CA1167769A|1984-05-22|
    ATA14681A|1983-02-15|
    YU9581A|1984-02-29|
    SE8100207L|1981-07-17|
    FI75095B|1988-01-29|
    BE887111A|1981-07-16|
    NO810133L|1981-07-17|
    PT72358A|1981-02-01|
    IT1135052B|1986-08-20|
    IE810074L|1981-07-16|
    FR2473311B1|1984-03-30|
    CS227324B2|1984-04-16|
    AU547152B2|1985-10-10|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    FR120M|Madaus & Co Dr|New laxative composition.|
    US1847247A|1931-02-14|1932-03-01|Jones William Thomas|Mechanical laxative|
    DE1003916B|1954-05-12|1957-03-07|Westminster Lab Ltd|Process for the production of Sennespraeparaten|
    GB829068A|1958-04-09|1960-02-24|Mundipharma Ag|Improvements in novel laxative agents|
    DE1103520B|1959-08-12|1961-03-30|Madaus & Co Dr|Process for making a laxative|
    DE2629773C2|1976-07-02|1985-06-27|Thiele, Henry, Dipl.-Ing. Dr., 7534 Birkenfeld|Product made from bran and pectin|US4321263A|1980-09-30|1982-03-23|Rowell Laboratories, Inc.|Psyllium compositions|
    EP0144644B1|1983-12-12|1989-09-06|THE PROCTER & GAMBLE COMPANY|Psyllium mucilloid products|
    US5009916A|1983-12-12|1991-04-23|The Procter & Gamble Company|Psyllium mucilloid fiber food products|
    US4950689A|1987-03-31|1990-08-21|Yang Robert K|Pectin delivery system|
    DE69002561T2|1989-08-10|1993-11-18|Procter & Gamble|Agglomerated psyllium husk containing edible acid.|
    US5219570A|1989-08-10|1993-06-15|The Procter & Gamble Company|Agglomerated psyllium husk containing edible acid|
    US5126150A|1990-10-01|1992-06-30|The Procter & Gamble Company|Compositions containing psyllium|
    GB2272374B|1992-11-13|1996-07-03|Asta Medica Ag|Stable senna extract formulations|
    FR2723318B1|1994-08-04|1999-09-03|Chicouri Marcel|NOVEL LAXATIVE COMPOSITIONS AND THEIR PREPARATION PROCESS|
    US20050053676A1|2003-09-05|2005-03-10|Madaus Ag|Powdered composition for use as laxative|
    ES2320827B1|2006-12-29|2010-03-03|Madaus, S.A.|"PHARMACEUTICAL COMPOSITION CONTAINING PSYLLIUM AND SENNA".|
    DE202007007143U1|2007-05-02|2008-06-12|Madaus Gmbh|New pharmaceutical composition for use as a laxative|
    DE102007023397B4|2007-05-02|2015-03-26|Madaus Gmbh|New pharmaceutical composition for use as a laxative|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE3001357A|DE3001357C2|1980-01-16|1980-01-16|Granulated laxative based on plantago seeds and senna pods and process for the manufacture of the same|
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