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
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
  • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Definitions

• the invention comprises a new use of a lipid of a specified kind.
• the lipid in question is of the type MLM and/or SLS.
• L which represents a long chain acyl radical, is an acyl radical with 14-24 C atoms, e.g. palmitoyi (CH 3 (CH 2 ) 14 CO-)
• M which represents a medium chain acyl radical, is an acyl radical with 6-13 C atoms, e.g. pelargoyl (CH 3 (CH 2 ) 7 CO-)
• S which represents a short chain acyl radical, is an acyl radical with 2-5 C atoms, e.g. valeroyl (CH 3 (CH 2 ) 3 CO-). It is understood that a lipid of the type MLM can be represented as
• enteral emulsions of lipids of the above indicated type are described, and likewise their use for nutritional purposes. Also, it is described that enteral emulsions of the above indicated type can be used as nutrition for seriously ill patients.
• the purpose of the invention is to provide other uses for lipids of the above indicated type.
• the lipids of the above indicated type can be used for treatment of patients with lipid malabsorption, e.g. patients suffering from pancreatic insufficiency, primary biliary cirrhosis or cystic fibrosis, i.e. that those lipids can be used for patients suffering from lipid malabsorption.
• lipid malabsorption e.g. patients suffering from pancreatic insufficiency, primary biliary cirrhosis or cystic fibrosis, i.e. that those lipids can be used for patients suffering from lipid malabsorption.
• One category of patients with lipid malabsorption has reduced capability in regard to secretion of pancreatic lipase, which is responsible for the major part of triglyceride hydrolysis in the gut.
• pancreatic lipase which is responsible for the major part of triglyceride hydrolysis in the gut.
• Structured lipids of the MLM type is easier hydrolyzed by pancreatic lipase (vide Example 1 ), meaning that even at a very low activity of pancreatic lipase, as in patients suffering from pancreatic insufficiency, the structured lipids of the MLM type will be hydrolyzed, and the formed 2- monoglycerides will be absorbed. It appears from Example 2 that feeding MLM to a pancreatic insufficient pig leads to as much lipid absorption as when feeding soy oil to a pancreatic sufficient pig. A study of pancreatic insufficient rats (vide E ⁇ xample 3) has shown that the total lipid absorption is greater when provided as structured MLM than as randomized MLM or a physical mixture of the corresponding lipids.
• the content of the essential fatty acid linoleic acid in the lymph was higher in the MLM group, meaning that the total absorption of linoleic acid was higher.
• the MLM also provides essential fatty acids for the functions of the cell, including formation of membrane lipids and intracellular mediators, e.g. eicosanoids.
• these results indicate that MLM can be absorbed through the gut mucosa without prior hydrolysis.
• the use according to the invention of a lipid of the type MLM and/or SLS is for production of a pharmaceutical preparation for treatment of lipid malabsorption.
• the lipid related to the use according to the invention can be formulated as a part of a dressing or an oil incorporated in the diet or as a part of an emulsion. Typically the lipid should be administered in an amount of 0.5-4.5 g per kg of body weight per day.
• the use according to the invention relates to lipid malabsorption in both humans and animals.
• lipid of the type MLM and/or SLS is for patients suffering from lipid malabsorption.
• the lipid contains more than 20% of lipids of the type MLM. This type of lipid is easily absorbed in the gut. In a preferred embodiment of the use according to the invention the lipid contains more than 10% of lipids of the type SLS. This type of lipid is easily absorbed in the gut.
• the 5 preparation is formulated as an enteral formulation.
• lipids of the type MLM or SLS are described, and so are their use as a nutritional agent, and also, use of lipids for treatment of lipid malabsorption are described, but not in relation to lipids of the type MLM or SLS; in particular WO-A-8,902,275 (New England Deaconess Hospital Corp.),
• Lipids for enteral nutrition of the type LLL can only be absorbed with difficulty by patients suffering from lipid malabsorption. Lipids for enteral nutrition of the type LLL can only be absorbed with difficulty by patients suffering from lipid malabsorption. Lipids for enteral nutrition of
• MMM cell membranes in the body.
• the absorption of MMM might be due to a smaller molecular weight and a more compact structure and also a facilitated diffusion across the unstirred water layer of the gut, compared to long chain triglycerides.
• the lipids of the above indicated type can be absorbed in individuals suffering from pancreatic insufficiency, thus providing essential fatty acids.
• Lipid emulsions (50 ml) were prepared from 5 ml of lipid, 41 ml of gum arabic (10% w/v) and 4 ml of water and emulsified with Ultra Turrax 3 x 5 minutes at 4°C. The particle size distribution was measured microscopically before and after the titrations.
• Fig. 2 shows the total lymphatic output.
• the absorption peak is seen 5 hours after dosage, which is later than when pancreatic lipase and bile is present. After the peak the absorption of MLM continues at a higher level than the two other lipids. This leads to a higher total absorption of MLM.
• the content of the essential fatty acid linoleic acid in the lymph fractions is shown in Fig. 3.
• the content of linoleic acid is at a significantly higher level in the MLM group than in the two other groups.
• the total absorption of linoleic acid is higher in the MLM group.

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• Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Emergency Medicine (AREA)
• Epidemiology (AREA)
• Gastroenterology & Hepatology (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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• 1992
  • 1992-05-08 JP JP4509155A patent/JPH06507161A/ja active Pending
  • 1992-05-08 EP EP92910106A patent/EP0583337A1/de not_active Withdrawn
  • 1992-05-08 WO PCT/DK1992/000150 patent/WO1992019237A1/en not_active Application Discontinuation

Non-Patent Citations (1)

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