FR2427100A1 - Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid - Google Patents

Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid

Info

Publication number
FR2427100A1
FR2427100A1 FR7816523A FR7816523A FR2427100A1 FR 2427100 A1 FR2427100 A1 FR 2427100A1 FR 7816523 A FR7816523 A FR 7816523A FR 7816523 A FR7816523 A FR 7816523A FR 2427100 A1 FR2427100 A1 FR 2427100A1
Authority
FR
France
Prior art keywords
fatty acid
addn
prepd
converting
highly soluble
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
FR7816523A
Other languages
French (fr)
Other versions
FR2427100B1 (en
Inventor
Theodor Eckert
Fritz H Kemper
Martin Wischniewski
Reinhard Hempel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abbott Products GmbH
Original Assignee
Kali Chemie Pharma GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kali Chemie Pharma GmbH filed Critical Kali Chemie Pharma GmbH
Priority to NL7806048A priority Critical patent/NL7806048A/en
Priority to FR7816523A priority patent/FR2427100A1/en
Publication of FR2427100A1 publication Critical patent/FR2427100A1/en
Application granted granted Critical
Publication of FR2427100B1 publication Critical patent/FR2427100B1/fr
Granted legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The solubility and stability of basic pharmaceuticals (I) in mixts. of mono- an di-glycerides of 6-12C fatty acids are improved by adding to (I) free 6-18C (6-10C) fatty acids. The resulting salts are then dissolved in the glyceride mixt. Better resorption of (I) from the gastro-intestinal tract. The fatty acid salts of (I) are more soluble in the glyceride mixt. than free bases or hydrochlorides.
FR7816523A 1978-06-02 1978-06-02 Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid Granted FR2427100A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
NL7806048A NL7806048A (en) 1978-06-02 1978-06-02 MEDICINAL PRODUCT WITH BETTER RESORPTION PROPERTIES AND METHOD OF PREPARATION.
FR7816523A FR2427100A1 (en) 1978-06-02 1978-06-02 Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR7816523A FR2427100A1 (en) 1978-06-02 1978-06-02 Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid

Publications (2)

Publication Number Publication Date
FR2427100A1 true FR2427100A1 (en) 1979-12-28
FR2427100B1 FR2427100B1 (en) 1981-07-31

Family

ID=9208998

Family Applications (1)

Application Number Title Priority Date Filing Date
FR7816523A Granted FR2427100A1 (en) 1978-06-02 1978-06-02 Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid

Country Status (2)

Country Link
FR (1) FR2427100A1 (en)
NL (1) NL7806048A (en)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0127426A1 (en) * 1983-05-23 1984-12-05 Takeda Chemical Industries, Ltd. Percutaneous pharmaceutical compositions for external use
EP0152896A3 (en) * 1984-02-22 1986-01-22 F. Hoffmann-La Roche Ag Suppositories containing ceftriaxone
FR2569112A1 (en) * 1984-08-14 1986-02-21 Israel Inst Biolog Res TRANSCUTANEOUS DRUG DELIVERY SYSTEM
EP0177342A2 (en) * 1984-10-04 1986-04-09 Genentech, Inc. Oral formulation of therapeutic proteins
WO1986005694A1 (en) * 1985-04-02 1986-10-09 Yesair David W Composition for delivery of orally administered substances
US4874795A (en) * 1985-04-02 1989-10-17 Yesair David W Composition for delivery of orally administered drugs and other substances
WO1990012583A1 (en) * 1989-04-20 1990-11-01 Cortecs Limited Pharmaceutical compositions
US5314921A (en) * 1990-08-13 1994-05-24 Yesair David W Mixed lipid-bicarbonate colloidal particles
US5571517A (en) * 1990-08-13 1996-11-05 Yesair; David W. Mixed lipid-bicarbonate colloidal particles for delivering drugs or calories
US5891466A (en) * 1990-08-13 1999-04-06 Yesair; David W. Mixed Liped-Bicarbonate colloidal particles for delivering drugs or calories

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2051574B (en) * 1979-05-10 1984-01-18 Kyoto Pharma Ind Adjuvant for promoting absorption of pharmacologically active substances through the rectum
GB2281697A (en) * 1993-09-14 1995-03-15 Euro Celtique Sa Laxative compositions in capsules

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2206943A1 (en) * 1972-11-18 1974-06-14 Sumitomo Chemical Co
FR2321892A1 (en) * 1975-08-27 1977-03-25 Akzo Nv PHARMACEUTICAL PREPARATIONS FOR ORAL ADMINISTRATION CONTAINING NANDROLONE-17B ESTER AND NEW NANDROLONE-17B ESTERS
DE2631281A1 (en) * 1976-07-12 1978-01-19 Kali Chemie Pharma Gmbh Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.
FR2365338A1 (en) * 1976-07-12 1978-04-21 Kali Chemie Pharma Gmbh PREPARATIONS WITH A HIGH CAPACITY OF RESORPTION BY ENTERIC ROUTE OF CARDIAC GLYCOSIDES REBUILD WITH DIFFICULTY AND PROCESS FOR MANUFACTURING SUCH PREPARATIONS
DE2700765A1 (en) * 1977-01-10 1978-07-20 Kali Chemie Pharma Gmbh Solid-liquid solns. of medicaments, e.g. G-strophanthin - having improved resorption in the gastrointestinal tract, use a solvent mixture of fatty acids and corresp. glyceride(s)
DE2700501A1 (en) * 1977-01-07 1978-07-20 Kali Chemie Pharma Gmbh Solid-liquid solns. of medicaments, e.g. G-strophanthin - having improved resorption in the gastrointestinal tract, use a solvent mixture of fatty acids and oleic acid mono:glyceride
DE2700433A1 (en) * 1977-01-07 1978-07-20 Kali Chemie Pharma Gmbh Pharmaceutical compsns. with good resorption - comprising solns. of e.g. cardiac glycoside(s), steroid hormones, antibiotics and antiinflammatories in free fatty acids

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2206943A1 (en) * 1972-11-18 1974-06-14 Sumitomo Chemical Co
FR2321892A1 (en) * 1975-08-27 1977-03-25 Akzo Nv PHARMACEUTICAL PREPARATIONS FOR ORAL ADMINISTRATION CONTAINING NANDROLONE-17B ESTER AND NEW NANDROLONE-17B ESTERS
DE2631281A1 (en) * 1976-07-12 1978-01-19 Kali Chemie Pharma Gmbh Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.
FR2365338A1 (en) * 1976-07-12 1978-04-21 Kali Chemie Pharma Gmbh PREPARATIONS WITH A HIGH CAPACITY OF RESORPTION BY ENTERIC ROUTE OF CARDIAC GLYCOSIDES REBUILD WITH DIFFICULTY AND PROCESS FOR MANUFACTURING SUCH PREPARATIONS
DE2700501A1 (en) * 1977-01-07 1978-07-20 Kali Chemie Pharma Gmbh Solid-liquid solns. of medicaments, e.g. G-strophanthin - having improved resorption in the gastrointestinal tract, use a solvent mixture of fatty acids and oleic acid mono:glyceride
DE2700433A1 (en) * 1977-01-07 1978-07-20 Kali Chemie Pharma Gmbh Pharmaceutical compsns. with good resorption - comprising solns. of e.g. cardiac glycoside(s), steroid hormones, antibiotics and antiinflammatories in free fatty acids
DE2700765A1 (en) * 1977-01-10 1978-07-20 Kali Chemie Pharma Gmbh Solid-liquid solns. of medicaments, e.g. G-strophanthin - having improved resorption in the gastrointestinal tract, use a solvent mixture of fatty acids and corresp. glyceride(s)

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0127426A1 (en) * 1983-05-23 1984-12-05 Takeda Chemical Industries, Ltd. Percutaneous pharmaceutical compositions for external use
EP0152896A3 (en) * 1984-02-22 1986-01-22 F. Hoffmann-La Roche Ag Suppositories containing ceftriaxone
FR2569112A1 (en) * 1984-08-14 1986-02-21 Israel Inst Biolog Res TRANSCUTANEOUS DRUG DELIVERY SYSTEM
DE3528979A1 (en) * 1984-08-14 1986-02-27 State Of Israel Represented By The Prime Minister's Office Israel Institute For Biological Research, Ness-Ziona DRUG RELEASE SYSTEM
EP0177342A3 (en) * 1984-10-04 1987-12-02 Genentech, Inc. Oral formulation of therapeutic proteins
EP0177342A2 (en) * 1984-10-04 1986-04-09 Genentech, Inc. Oral formulation of therapeutic proteins
WO1986005694A1 (en) * 1985-04-02 1986-10-09 Yesair David W Composition for delivery of orally administered substances
US4874795A (en) * 1985-04-02 1989-10-17 Yesair David W Composition for delivery of orally administered drugs and other substances
US5972911A (en) * 1985-04-02 1999-10-26 Yesair; David W. Composition for the delivery of orally administered drugs and other substances
WO1990012583A1 (en) * 1989-04-20 1990-11-01 Cortecs Limited Pharmaceutical compositions
US5314921A (en) * 1990-08-13 1994-05-24 Yesair David W Mixed lipid-bicarbonate colloidal particles
US5571517A (en) * 1990-08-13 1996-11-05 Yesair; David W. Mixed lipid-bicarbonate colloidal particles for delivering drugs or calories
US5707873A (en) * 1990-08-13 1998-01-13 Yesair; David W. Method of accessing mixed lipid transport properties of a drug
US5741822A (en) * 1990-08-13 1998-04-21 Yesair; David W. Mixed lipid-bicarbonate colloidal particles for delivering drugs
US5891466A (en) * 1990-08-13 1999-04-06 Yesair; David W. Mixed Liped-Bicarbonate colloidal particles for delivering drugs or calories

Also Published As

Publication number Publication date
NL7806048A (en) 1979-12-04
FR2427100B1 (en) 1981-07-31

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