Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol

Definitions

• the invention relates to an agent for oral litholysis of cholesterol gallstones.
• a commercial terpene mixture has also already been used for oral litholysis of cholesterol gallstones.
• Bell, GD, Doran, J. describe in: "Gall stone dissolution in man using an essential oil preparation" (Brit.Medical J., 6, 24 (1979)) that with 24 X-ray negative gallstone patients after an average treatment period of 6 months
• With a daily dose of approx. 6.5 mg terpene / kg of commercial terpene mixture complete dissolution was achieved in 3 patients and partial stone dissolution in 4 patients. As expected, smaller stones ( ⁇ 10mm) were easier to dissolve.
• Litholysis successes were 67%. of patients with Gallstones> 7 mm after 12 months of treatment with the terpene mixture in a maintenance dose of approx. 200 mg / per day from Ellis, WR, Bell, GD in "Treatment of biliary duct stones with a terpene preparation" (Brit.Medical J. 282 , 611 (1981)).
• the development outlined above in this area shows a considerable need for an effective agent which enables rapid litholysis of cholesterol gallstones with the smallest possible amounts of the expensive active ingredient ursodeoxycholic acid.
• the object of the invention is to create such a means.
• the combination of ursodeoxycholic acid and menthol because of their different mechanisms of action in litholysis, achieves an increased synergistic effect.
• the dose of ursodeoxycholic acid can be reduced to a third of the doses previously used.
• the cholesterol gallstone dissolution is accelerated.
• the agent can contain 80% by weight to 20% by weight ursodeoxycholic acid and 20% by weight to 80% by weight of X-L menthol as active ingredients.
• a composition of 50% by weight ursodeoxycholic acid and 50% by weight L-menthol has proven to be particularly effective.
• microfine crushed ursodeoxycholic acid with a grain size in the order of 5-50 ⁇ m, particularly advantageously 10-20 ⁇ m, can be used with the agent.
• the active ingredients can be particularly advantageous Ursodeoxycholic acid and menthol can be contained in a small gel soluble soft gelatin capsule. Clinical tests have shown that capsules with 100 mg ursodeoxycholic acid and 100 mg chemically pure menthol are particularly effective for the treatment.
• the following human study shows the effectiveness of the combination therapy of ursodeoxycholic acid / L-menthol in the oral litholysis of cholesterol gallstones.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Steroid Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=6330745

Family Applications (1)

Country Status (2)

• 1987
  • 1987-06-29 DE DE19873721846 patent/DE3721846A1/de active Granted
• 1988
  • 1988-06-23 WO PCT/DE1988/000380 patent/WO1989000046A1/de unknown

Non-Patent Citations (4)

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