DE2050072B2 - - Google Patents

Description

3 4

Aluminum hydroxide 16 g of ointment

Diluents, such as nairium

alginate, talc, magnesium stearate, aluminum-tri-S-acetyl-ie / S-gly-

Polyoxyethylene stearate, starch cyrrhetinate 2 g

and / or lactose up to 100 g 5 lidocaine-P-diethylamino ^ '. o'-acet-

oxylidide) hydrochloride 2 g

Suppositories Distilled water 14.8 g

Methyl p-hydroxybenzoate 0.2 g

Aluminum tri-3-acetyl-18/3-gly diluents, such as polyethylene

cyrrhetinate 100 mg io lenglykol 4000, propylene glycol

Tri-glycerides of fatty acids up to 1400 g and / or ceryl alcohol up to .. 100 g

Claims (3)

1 2 From the German Auslegeschrift 1176 684 is patent claims: furthermore a process for the preparation of compounds of glycyrrhetinic acid, such as the disodium salt of 1. Alurainium-trW-acetyl-IS / J-glycyiThetinate. Glycyrrhetinic acid hemisuccinate and disodium 2. Process for the preparation of the compound 5 salt of glycyrrhetinic acid dihydrogen phosphate accordingly Claim 1, known thereby. draws that one S-Acetyl-ie ^ -glycyrrhetin- was also from the compounds of the Auslegeschrift acid with a known in a manner that they fight inflammatory lower alkanolate with 1 to 4 carbon atoms with symptoms of some kinds, including ulcer Room temperature or elevated temperature, purposeful phenomena of the digestive tract, are valuable are moderately in the presence of an organic solution, by means of, implements. When investigating the antiulcus efficacy 3. Pharmaceutical preparations, labeled with aluminum tri-3-acetyl-glycyrrhetinate by a content of the compound miniumglycyrrhetinat, Glycyrrhetinsäure, 3-o-Acetylnach Claim 1 together with a pharmaceutical 15 glycyrrhetinic acid and sodium hemisuccinylzeutisch acceptable diluent or glycyrrhetinic acid has now been found that the Carrier. Aluminum tri-3-acetyl-glycyrrhetinate the highest Has tiulcus effectiveness Only antiulcus effectiveness of aluminum glycyrrhetinate is sufficient ao this effectiveness approach. The aluminum glycyrrhetinate but has a relatively low anti-inflammatory effect Effectiveness on. The present invention relates to aluminum in studies of anti-inflammatory properties tri-S-acetyl-ie / S-glycyrrhetinate, process for its effectiveness by aluminum tri-3-acetyl-glycyrrhe manufacture and pharmaceutical tinate containing it, aluminum glycyrrhetinate and glycyrrhetinic acid Preparations. the aluminum tri-3-acetyl-glycyrrhetinate as It was surprisingly found that the most effective substance was found.
Aluminum tri-3-acetyl-18 /? - glycyrrhetinate optimal Medicinal and anti-inflammatory properties are provided by aluminum tri-3-acetyl-glycyrrhetinate, which is less toxic in the treatment of disorders of the 30 than glycyrrhetinic acid and Na digestive tract, such as gastric and duodenal triumhemisuccinyl-glycyrrhetinate, in particular for ulcers, gastritis and gastroduodenitis, especially intraperitoneal administration,
however, when medicated. The following examples illustrate the invention. Interference, is very useful. This substance can. · 1 1 in addition, in the therapy of pharyngitis, 35 B e 1 s ρ 1 e 1 1 Pharyngotracheitis, corneal ulcers, colitis (ins- 15.38 g S-acetyl-IS / J-glycyrrhetinic acid, dissolved in special ulcerative colitis), dermatitis, dormatosis, 500 ml of chloroform, became a solution of Decubitus ulcers, latent ulcers, varicose veins - 2.04 g of aluminum isopropylate in 50 ml of chloroform Ulcers, fissures, hemorrhoids and epithe'ero- added. Sions of the female genital passages applied 40 After 1 hour, the chloroform solution became will. Dry evaporated and aluminum-tri-3-acetyl- The pharmaceutical preparations can also contain 18/3 glycyrrhetinate as a white powder, enamel generally contain other drugs. Usable point 286 to 29O ⁰ C. (<*]? = 126 ° ± 2 ° (c = 1, carriers are starch, talc, sodium alginate and CHCl ₃ ). Magnesium stearate. The preparations can be used in 45 B e i s 0 i e 1 2 Form of tablets or suppositories or as Powders or ointments are administered. The pharmaceutical 4.08 g of aluminum isopropylate, dissolved in 50 ml of Zeutischen preparations can also means ethylene chloride, were to 30.76 g of 3-acetyl-18 /? - gly against Hyperacidity, such as aluminum hydroxide, glycine cyrrhetinic acid, dissolved in 200 ml methylene chloride, and aluminum silicate. go given. To complete the solution was The process for the production of aluminum - stirred at room temperature, then on about 50 ml of tri-3-acetyl-18 /? - glycyrrhetinate is thereby marked- concentrated and poured into 200 ml of hexane. Aluminum draws that 3-acetyl-18 /? -Glycyrrhetinic acid in tri-3-acetyl-18/3-glycyrrhetinate was obtained as a white, amoraneously known manner with a lower alkanolate phes, light powder by filtration,
with 1 to 4 carbon atoms at room temperature or 55 With the compound according to the invention at elevated temperature, advantageously in the presence of one of the following formulations, can be obtained:
organic solvent. As organic ", Solvents can be alcohols, ethers, ketones, bets chlorinated solvents (methylene chloride, chloro-aluminum-tri-3-acetyl-18 / S-gly- form), ethyl acetate, etc. can be used. 60 cyrrhetinate 50 mg In many cases the solubility of the salt in aluminum hydroxide is 400 mg organic solvents, while the soluble diluents such as sodium speed in water is generally low. alginate, magnesium stearate, talc From the German Auslegeschrift 1184 753 is a and / or strength up to 1.2 g Process for the preparation of 3-ketoglycyrrhetine-65 acids known. There is also ruder from this explanatory document show that the glycyrrhetinic acids for the aluminum - tri - 3 - acetyl -18/3 - gly- Treatment of symptoms of inflammation are suitable. cyrrhetinate 3 g