• 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:
    1502580 Preparation of porous tablets BOEHRINGER MANNHEIM GmbH 13 Dec 1976 [16 Dec 1975] 51908/76 Addition to 1381588 Heading A5B Porous tablets are prepared by mixing the tablet components with an inert solvent which freezes at from -30 to +25‹C, the solvent constituting 5 to 80% by weight of the total mixture, solidifying the mixture by introduction into an inert cooling medium e.g. liquid nitrogen, pressing into tablets at a temperature below the freezing point of the solvent and then removing the solvent e.g. by lyophilisation. The solvent may be water, cyclohexane, benzene or tert-butanol or a mixture thereof with a C 1-4 alcohol. After pressing, the tablets may be warmed to a temperature from 15‹ to 30‹C and dried in the air. The tablets may be pressed at a pressure of 500 to 5000kg/cm<SP>2</SP>.
    公开号:SU719480A3
    申请号:SU762427754
    申请日:1976-12-13
    公开日:1980-02-29
    发明作者:Книч Карл-Вольфганг；Хаген Александер；Мунц Эберхард；Детерманн Хельмут
    申请人:Берингер Маннхайм Гмбх (Фирма)；
    IPC主号:
    专利说明:

    (54) METHOD FOR GETTING TABLETS
    This invention relates to medicine, in particular to the pharmaceutical industry. A known method of producing tablets by displacing the active substances, granulating, compressing and drying 1. However, such tablets are poorly soluble. The aim of the invention is to increase the dissolution rate of tablets. For this purpose, the displacement of substances such as sodium chloride, mannitol, albumin, glutamate oxalacetate, trans aminase, phosphatase or urease with an inertial solvent — water, cyclohexane or cyclohexane-ethanol mixture is carried out at a ratio solvent and mixtures of 5-80 wt.%; granulation in liquid nitrogen and the resulting granules are pressed at a temperature below the freezing point of an inert solvent, preferably (-20) (-25) ° C. The method for preparing the tablets is as follows. Substances to be tableted using a quantity of solvent sufficient for pore formation are processed into thick ka or with more significant quantities of solvent or more. High solubility. Travel - in solution. This mixture is crushed into fine particles and introduced into an inert cooled mixture, whereby the solvent and the active substances are separated into crystalline phases. If 1 solvent is present only in an insignificant concentration, then the thick porridge is pressed through a sieve with a corresponding hole diameter and the resulting granules are sent to the cooling mixture. For the case where the mixture is flowable, it can be sprayed through nozzles or spray devices and in the form of small droplets, be fed into the cooling mixture. In both cases, after separation from the coolant, granular granules are obtained, which can be pressed in the usual way on tablet presses into tablets of the desired shape and size. The pressing process must be carried out at a temperature below the melting point of the electrical mixture of substances that make up the contents of the tablet with the solvent. From the finished tablets, the solvent is removed either by lyophilization, or if the resulting tablets, even after thawing the solvent, are sufficiently form-stable; by air drying. The dissolution rate of the obtained tablets is regulated over a wide range due to the amount of solvent used and the size and number of pores remaining after evaporation. The hardness of the tablets is greater, the less solvent was added, and the smaller the number and size of pores. The hardness is also significantly influenced by the pressure of the presses, an, the tablets becoming harder the stronger the components are compressed and. with each other. Pressing pressure from 500 to 5000 kg / cm. Solvents can be chosen in which one of the substances to be tabletted is soluble, so that as a result of local heatings occurring during pressing, this substance dissolves and after that, when pressure is removed, it is compressing the particles of the mixture or drying and thus drying. tablet hardness. Particularly porous tablets can be obtained by slight pressing of pressure and removal of solvent by lyophilization at low temperatures, as well as by the addition of larger amounts of solvent, which increases the number and size of pores. Salts that are completely soluble to the solvent can also be tableted, in particular, these mixtures can be tableted without the addition of lubricants, without fear of sticking to the mold. The solvents used are those that are at room temperature. Perature does not adversely affect the substances that make up the contents of the tablet, freeze during cooling to technologically acceptable temperatures, t ". e .. up to temperatures of about, even in the presence of substances, dispose of the contents of the tablet, preferably with phase separation and can be easily evaporated or sublimated. Water, cyclohexane, benzene, and also mixtures of lower alcohols with water or cyclohexane are most acceptable. . The amount of solvent is chosen in accordance with the required tablet hardness and disintegration time ranging from 5 to 80%. The dd of obtaining relatively hard form-stable and dried at room temperature tablets applied to the porridge of the active substance with the solvent containing from 5 to 25%, and the solution of the active soft tablets with solvent content from about 30 to 80%, it is advisable from 30 to 50%. Example. Receiving a tablet of loric sodium. 99.5 parts of sodium chloride are finely ground and thoroughly mixed with 0.5 h / pbliviylpyrrolidone. The mixture is dissolved with 0% by weight of demineralized water and watered in liquid nitrogen by passing it through a sieve with a diameter of 4 mm, L mm. Frozen free-flowing rant t is compressed into tablets at a temperature of from -25 ° C to a pre-cooled tablet press at a pressure of 000 kg / cm. The obtained tablets are tubed at room temperature by ikktivom. Tablet size g diameter b mm, height 2.5 mm; weight - 88-69 mg; hardness - below 0.5 kg of Stokes hardness. Solubility in 1 ml of water -17c. - ,,. 11 p and measure 2. Albumin tablets, 0.5 parts of albumin, 0.5 parts of polyvinylpyrrolidone, 5.0 parts of sodium chloride and 94.0 parts of mannitol are thoroughly mixed together, dissolved with 40% by weight . Diclohexane and granularit into liquid nitrogen by forcing through a sieve with a hole diameter of 0.8 mm. The frozen granular granules are tabletted at a temperature of from -20 ° C to a pre-cooled tablet press according to Example 1. The obtained tablets are dried in air at room temperature with a stretch. Tablet dimensions: diameter 6 mm, height 4 mm, weight 98-99 mg, hardness less than 0.5 kg of Stoke hardness, solubility in 1 ml of water - 14 s. Example Glutam ta-oxalcetzta transaminase tablets. They take a composition containing, in parts: Ethylene diamine tetraacetate 1, 86 Tris- (oxymethyl) -amino-methane2, 42 L-aspartic acid26.62 Sodium carbonate (anhydrous) 14.34 Nicotine-amide-adenine dinucleotide (reduced - danatrylate salt (NADH -Hag) O15 Lactate dehydrogenase (lyophilisate) .2.00 Maleate dehydrogenase (lyophilisate) 2.00
    权利要求:
    Claims (1)
    [1]
    Claim
    A method of producing tablets by displacing active substances, granulation, pressing and drying, characterized in that, in order to increase the dissolution rate of the tablets, mixing substances such as sodium chloride, mannitol, albumin, glutamate-oxalacetate, transaminase, phosphatase or urease with an inert 'solvent - water, cyclohexane or with a mixture of cyclohexane - ethanol is carried out at a solvent to mixture ratio of 5: 80 weight: granulate in liquid nitrogen and the resulting granules are pressed at a temperature below the freezing temperature of inert solvent, preferably (-20) - (-25) ° C.
    类似技术:
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    同族专利:
    公开号 | 公开日
    FR2335205A2|1977-07-15|
    DE2556561C2|1983-04-14|
    JPS56120617A|1981-09-22|
    SE423967B|1982-06-21|
    IE44571B1|1982-01-13|
    BE849438A|1977-06-15|
    DE2556561A1|1977-06-30|
    FR2335205B1|1981-05-29|
    SE7613971L|1977-06-17|
    CH609563A5|1979-03-15|
    JPS5276420A|1977-06-27|
    GB1502580A|1978-03-01|
    JPS5824410B2|1983-05-20|
    IE44571L|1977-06-16|
    NL7613818A|1977-06-20|
    AT348133B|1979-01-25|
    US4134943A|1979-01-16|
    IT1124797B|1986-05-14|
    ATA927076A|1978-06-15|
    引用文献:
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    GB1548022A|1976-10-06|1979-07-04|Wyeth John & Brother Ltd|Pharmaceutial dosage forms|
    CH637014A5|1978-09-29|1983-07-15|Sandoz Ag|METHOD FOR PRODUCING SUPPOSITORIES.|
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    DE2925009A1|1979-06-21|1981-01-08|Basf Ag|PREPARATION FOR SUBSTANCES, METHOD FOR THE PRODUCTION AND USE THEREOF|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE19752556561|DE2556561C2|1975-12-16|1975-12-16|Process for the production of porous tablets|
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