DE2631281A1 - Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds. - Google Patents

Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.

Info

Publication number
DE2631281A1
DE2631281A1 DE19762631281 DE2631281A DE2631281A1 DE 2631281 A1 DE2631281 A1 DE 2631281A1 DE 19762631281 DE19762631281 DE 19762631281 DE 2631281 A DE2631281 A DE 2631281A DE 2631281 A1 DE2631281 A1 DE 2631281A1
Authority
DE
Germany
Prior art keywords
glyceride
gelatin capsules
opt
pharmaceuticals
dissolving
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.)
Withdrawn
Application number
DE19762631281
Other languages
German (de)
Inventor
Theodor Prof Dr Eckert
Fritz H Prof Dr Kemper
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 DE19762631281 priority Critical patent/DE2631281A1/en
Priority to GB2798577A priority patent/GB1544576A/en
Priority to IE137977A priority patent/IE45448B1/en
Priority to IL5247277A priority patent/IL52472A/en
Priority to AU26927/77A priority patent/AU515932B2/en
Priority to NZ18461277A priority patent/NZ184612A/en
Priority to CA282,536A priority patent/CA1087985A/en
Publication of DE2631281A1 publication Critical patent/DE2631281A1/en
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)

Abstract

The solubility of pharmaceuticals for application in gelatin capsules is increased by dissolving them in monoglycerides- and opt. diglycerides of 8-12C fatty acids. The process increases the reabsorption from the gastrointestinal tract and gives greater dosage accuracy. In an example, 1 ml. of fatty acid glyceride mixt. was used to dissolve (a) 5 mg. g-strophanthin; (b) 100 mg. benzanone; (c) 5 mg. digoxin.

Description

Verfahren zur Erhöhung der Löslichkeit von Process for increasing the solubility of

schwerlöslichen Arzneistoffen zum Zwecke deren Applikation in Gelatinekapseln. poorly soluble medicinal substances for the purpose of their application in gelatin capsules.

Die Erfindung betrifft ein Verfahren zur Erhöhung der Löslichkeit von in den üblichen Füllmitteln für Gelatinekapseln schwerlöslichen Arzneistoffen, mit dem Ziel, einerseits eine bessere Dosierungsgenauigkeit zu erzielen, andererseits eine bessere Resorption aus dem Magen-Darm-Trakt zu erreichen.The invention relates to a method for increasing solubility of drugs that are sparingly soluble in the usual fillers for gelatine capsules, with the aim of achieving better dosing accuracy on the one hand, and on the other hand to achieve better absorption from the gastrointestinal tract.

Die gastro-enterale Aufnahme und die Resorptionsgeschwindigkeit von schwerlöslichen Arzneistoffen, die in Gelatinekapseln konfektioniert sind, ist häufig unzulänglich; als Vehikel werden bisher vorzugsweise flüssige Triglyceride von Fettsäuren ( fette Öle ) verwendet.The gastrointestinal uptake and the rate of absorption of poorly soluble drugs that are packaged in gelatin capsules is common inadequate; Liquid triglycerides of fatty acids have hitherto been the preferred vehicle (fatty oils) are used.

Die Erfindung besteht darin, die schwerlöslichen Arzneimittel in flüssigen Monoglyceriden oder Gemischen von Mono- und Diglyceriden mittelkettiger Fettsäuren ( C8 bis C12 ) zu lösen und diese Lösungen in Gelatinekapseln zu verarbeiten.The invention consists in the sparingly soluble drugs in liquid Monoglycerides or mixtures of mono- and diglycerides of medium-chain fatty acids (C8 to C12) and to process these solutions in gelatin capsules.

Ein Beispiel, das für die Ausführung des Verfahrens in Frage ko-st ist etwa folgendes Lösungsmittel: Ein Gemisch aus Mono- und Diglyceriden der Fettsäuren C8-C12.An example that is cost-effective to carry out the procedure in question is about the following solvent: A mixture of mono- and diglycerides of fatty acids C8-C12.

Die folgenden Beispiele erläutern die Erfindung.The following examples illustrate the invention.

Beispiel 1 5 mg g-Strophanthin werden unter Rühren bei Raumtemperatur in 1 ml eines Gemisches von Mono- und Diglyceriden mittelkettiger Fettsäuren ( C8 bis C12 ) gelöst.Example 1 5 mg of g-strophanthin are added with stirring at room temperature in 1 ml of a mixture of mono- and diglycerides of medium-chain fatty acids (C8 up to C12).

Beispiel 2 100 mg. Benzaron werden unter Rühren bei Raumtemperatur in 1 ml eines Gemisches von Nono- und Diglyceriden mittelkettiger Fettsäuren ( CB bis C12 ) gelöst.Example 2 100 mg. Benzaron are stirred at room temperature in 1 ml of a mixture of nono- and diglycerides of medium-chain fatty acids (CB up to C12).

BeisPiel 3 20 mg Sylimarin werden unter gelindem Erwärmen in lml eines Gemisches von Mono- und Diglyceride mittelkettiger Fettsäuren ( CB bis C12 ) gelöst.EXAMPLE 3 20 mg of Sylimarin are poured into 1 ml of one under gentle warming Mixture of mono- and diglycerides of medium-chain fatty acids (CB to C12) dissolved.

Beispiel 4 5 mg Digoxin werden unter Rühren bei Raumtemperatur in 1 ml eines Gemisches von Moho- und Diglyceriden mittelkettiger Fettsäuren ( C8 bis C12 ) gelöst.Example 4 5 mg digoxin are in 1 ml of a mixture of moho and diglycerides of medium-chain fatty acids (C8 to C12) solved.

Formelzusammenstellung Silymarin =Gemisch aus: z. Silybin II. silydianiz III. Silyshristin Fortsetzung Formeizusammenstellung Benzaron g.Strophynthin.Composition of formulas Silymarin = mixture of: z. Silybin II. Silydianiz III. Silyshrist Continuation of the form composition Benzaron g.Strophynthin.

Ouabain, Strophanthinum Digoxin Ouabain, strophanthinum Digoxin

Claims (1)

Patentansprüche Verfahren zur Erhöhung der Löslichkeit von in Triglyceriden schwerlöslichen Arzneimitteln zur Applikation in Gelatine -kapseln mit dem Ziel der Erzielung einer höheren Dosierungsgenauigkeit sowie einer verEesserten Resorption aus dem Magen-Darm-Trakt, dadurch gekennzeichnet, daß die Arzneimittel in Monoglyceriden mittelkettiger Fettsäuren ( C8 bis C12 ) oder in Gemischen aus solchen Mono- und Diglyceriden gelöst werden.Process for increasing the solubility of triglycerides poorly soluble drugs for application in gelatine capsules with the aim the achievement of a higher dosage accuracy as well as an improved absorption from the gastrointestinal tract, characterized in that the drugs are in monoglycerides medium-chain fatty acids (C8 to C12) or in mixtures of such mono- and Diglycerides are dissolved.
DE19762631281 1976-07-12 1976-07-12 Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds. Withdrawn DE2631281A1 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
DE19762631281 DE2631281A1 (en) 1976-07-12 1976-07-12 Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.
GB2798577A GB1544576A (en) 1976-07-12 1977-07-04 Enterally highly-absorbable preparations of cardiac glycosides which by themselves are absorbable with difficulty and process for the production of such preparations
IE137977A IE45448B1 (en) 1976-07-12 1977-07-04 Enterally highly-absorbable preparations of cardiac glycosides which by themselves are absorbable with difficulty and process for the production of such preparations
IL5247277A IL52472A (en) 1976-07-12 1977-07-06 Enterally absorbable preparations of cardiac glycosides and their production
AU26927/77A AU515932B2 (en) 1976-07-12 1977-07-11 Enterally highly-absorbable preparations of cardiac glycosides which by themselves are absorbable with difficulty, and process forthe production of such preparations
NZ18461277A NZ184612A (en) 1976-07-12 1977-07-11 Enterally absorbale preparations containing cardiac glycosides
CA282,536A CA1087985A (en) 1976-07-12 1977-07-12 Readily enterally absorbable pharmaceutical compositions of cardiac glycosides and preparation thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19762631281 DE2631281A1 (en) 1976-07-12 1976-07-12 Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.

Publications (1)

Publication Number Publication Date
DE2631281A1 true DE2631281A1 (en) 1978-01-19

Family

ID=5982790

Family Applications (1)

Application Number Title Priority Date Filing Date
DE19762631281 Withdrawn DE2631281A1 (en) 1976-07-12 1976-07-12 Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.

Country Status (2)

Country Link
AU (1) AU515932B2 (en)
DE (1) DE2631281A1 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0005121A2 (en) * 1978-04-25 1979-10-31 Pharmaceutical Licences Company Ltd. Process for stabilisation of 4-methyl-5-(2'-chlorethyl)-thiazol
FR2427100A1 (en) * 1978-06-02 1979-12-28 Kali Chemie Pharma Gmbh Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid
US4829057A (en) * 1984-07-24 1989-05-09 R. P. Scherer Corporation Oxytetracycline capsules with increased stability and methds of producing the same

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0005121A2 (en) * 1978-04-25 1979-10-31 Pharmaceutical Licences Company Ltd. Process for stabilisation of 4-methyl-5-(2'-chlorethyl)-thiazol
EP0005121A3 (en) * 1978-04-25 1979-11-28 Pharmaceutical Licences Company Ltd. Stabilisation process
FR2427100A1 (en) * 1978-06-02 1979-12-28 Kali Chemie Pharma Gmbh Highly soluble and stable basic pharmaceuticals in glyceride mixt. - are prepd. by converting to fatty acid salts by addn. of free fatty acid
US4829057A (en) * 1984-07-24 1989-05-09 R. P. Scherer Corporation Oxytetracycline capsules with increased stability and methds of producing the same

Also Published As

Publication number Publication date
AU2692777A (en) 1979-01-18
AU515932B2 (en) 1981-05-07

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Legal Events

Date Code Title Description
OI Miscellaneous see part 1
OI Miscellaneous see part 1
OI Miscellaneous see part 1
8141 Disposal/no request for examination