EP2271319A1 - Formulation à hygroscopicité réduite - Google Patents

Formulation à hygroscopicité réduite

Info

Publication number
EP2271319A1
EP2271319A1 EP09735236A EP09735236A EP2271319A1 EP 2271319 A1 EP2271319 A1 EP 2271319A1 EP 09735236 A EP09735236 A EP 09735236A EP 09735236 A EP09735236 A EP 09735236A EP 2271319 A1 EP2271319 A1 EP 2271319A1
Authority
EP
European Patent Office
Prior art keywords
formulation
formulations
hygroscopic
hygroscopic solid
solvent
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Withdrawn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
EP09735236A
Other languages
German (de)
English (en)
Inventor
Jesko Zank
Martin Steinbeck
Guido Becker
Udo Van Stiphout
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.)
Bayer Intellectual Property GmbH
Original Assignee
Bayer Technology Services 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 Bayer Technology Services GmbH filed Critical Bayer Technology Services GmbH
Publication of EP2271319A1 publication Critical patent/EP2271319A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics

Definitions

  • the invention relates to formulations of hygroscopic solids with a lipophilic coating layer, and to a process for their preparation.
  • a variety of fabrics, e.g. used as a pharmaceutical agent are hygroscopic. That the substances tend to absorb water, e.g. from the ambient air.
  • WO 2007/142628 further discloses a formulation comprising a moisture-sensitive active substance with at least one adjuvant, wherein the adjuvant is preferably a binder.
  • the disclosed method of making this formulation involves wet granulation of the active ingredient together with the binder.
  • the resulting formulation thus comprises a matrix material of at least one excipient and the active ingredient.
  • the formulation and the process for its preparation are disadvantageous because it does not prevent moisture from entering the formulation.
  • the disclosure that more stable formulations are obtained when solvents with 95% ethanol are used in the course of granulation instead of solvents with higher levels of water, that the stabilization of the active ingredient in such formulations are narrow limits. It can be assumed that stabilization of the active ingredient takes place only as long as the saturation of the at least one auxiliary with water does not occur Measure achieves that the affinity of the active ingredient for receiving water is similar to that of the excipient.
  • the active ingredients suitable for such formulation also include typical hygroscopic substances such as calcium carbonate and magnesium oxide.
  • the surface coating is carried out by granulation of the likewise pulverulent coating material with the active ingredient.
  • the coating material may also include hygroscopic substances such as calcium carbonate.
  • EP 1 161 941 is unfavorable with regard to the possibility of achieving stabilization of the active ingredient, since granulation of the active ingredient takes place with the coating material. As a result, agglomerates are generated which have a porosity as intrinsic property. This porosity leads to the fact that penetration of moisture into the core of the formulation can not be prevented, so that a stabilization of the active ingredient can not be done safely.
  • a lipophilic envelope surrounding the nucleus comprises, wherein the core and shell are connected by ionic interaction, can be solved.
  • a substance is considered to be hygroscopic if, under standard conditions, it has a relative mass increase over a period of 24 hours, based on its initial weight of at least 3%, by taking up water from the moisture contained in the environment. All substances which have lower mass increase under normal conditions are considered to be non-hygroscopic in connection with the present invention.
  • the lipophilic shell surrounding the core usually comprises a salt of the at least one hygroscopic solid with at least one organic acid which is characterized by a lipophilic portion and at least one acid group.
  • Acid group in the context of the present invention refers to that part of an organic acid molecule which leads to a lowering of the aqueous medium in the aqueous by dissociation of a proton (H + ) present in it.
  • Preferred are acid groups of the carboxylates, sulfonates and phosphates.
  • solubility in water is the mass of the hygroscopic, solid substance which can be dissolved in water at room temperature (20 ° C.) and atmospheric pressure (1013 hPa) at most in water.
  • the at least one organic acid of solution A of step a) comprises the organic acids already described in connection with the formulation according to the invention, as well as mixtures of these.
  • the temperature of the thermal drying at ambient pressure (1013 hPa) is preferably 100 ° C.
  • formulations according to the invention or the formulations according to the method of the invention are particularly suitable for use in connection with therapeutic methods on mammals, preferably humans or domestic animals.
  • the formulations according to the invention or the formulations according to the process of the invention preferably find use as fillers or auxiliaries of other formulations which are used as medicaments.
  • FIG. 1 shows the course of the relative change in weight in% of a formulation according to the invention (F) and pure magnesium hydroxide (Mg) when stored under air at 100% relative humidity and at 30 ° C.
  • FIG. 2 shows the course of the pH of a formulation (F) according to the invention and of magnesium hydroxide (Mg) recorded according to Example 3.

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (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)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)

Abstract

L'invention concerne des formulations de substances solides hygroscopiques comportant une couche d'enveloppe lipophile, ainsi qu'un procédé de fabrication de ces formulations.
EP09735236A 2008-04-24 2009-04-11 Formulation à hygroscopicité réduite Withdrawn EP2271319A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102008020701A DE102008020701A1 (de) 2008-04-24 2008-04-24 Formulierung mit reduzierter Hygroskopizität
PCT/EP2009/002691 WO2009129943A1 (fr) 2008-04-24 2009-04-11 Formulation à hygroscopicité réduite

Publications (1)

Publication Number Publication Date
EP2271319A1 true EP2271319A1 (fr) 2011-01-12

Family

ID=40984892

Family Applications (1)

Application Number Title Priority Date Filing Date
EP09735236A Withdrawn EP2271319A1 (fr) 2008-04-24 2009-04-11 Formulation à hygroscopicité réduite

Country Status (5)

Country Link
US (1) US20110021355A1 (fr)
EP (1) EP2271319A1 (fr)
CN (1) CN102014875B (fr)
DE (1) DE102008020701A1 (fr)
WO (1) WO2009129943A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103271895A (zh) * 2012-03-14 2013-09-04 南京先宇科技有限公司 一种稳定的含有羟苯磺酸钙的药物组合物及其制备方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB505362A (en) * 1937-03-01 1939-05-08 Armour & Co Improvements in compositions of matter containing anti-hygroscopic agents and processes of preparing the same
US2702747A (en) * 1951-08-27 1955-02-22 Phillips Petroleum Co Noncaking fertilizers
WO2000054752A1 (fr) 1999-03-15 2000-09-21 Kaken Pharmaceutical Co., Ltd. Comprimes a delitement rapide et procede de fabrication
US6878693B2 (en) * 2001-09-28 2005-04-12 Solubest Ltd. Hydrophilic complexes of lipophilic materials and an apparatus and method for their production
CA2511385A1 (fr) * 2002-12-19 2004-07-22 Pharmacia Corporation Intermediaire pour formulation a caractere non-hygroscopique acceptable comprenant un bouchon hydroscopique
AR050615A1 (es) * 2004-08-27 2006-11-08 Novartis Ag Composiciones farmaceuticas para la administracion oral
EP1917301B1 (fr) * 2005-08-05 2014-04-23 3M Innovative Properties Company Compositions présentant une aptitude à l'écoulement améliorée
ES2299157T3 (es) * 2006-06-02 2008-05-16 Teva Pharmaceutical Industries Ltd Formulacion estable que comprende un farmaco sensible a la humedad y procedimiento de preparacion del mismo.
CN101460191A (zh) 2006-06-02 2009-06-17 特瓦制药工业有限公司 包含湿敏性药物的稳定制剂及其制备方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2009129943A1 *

Also Published As

Publication number Publication date
WO2009129943A1 (fr) 2009-10-29
WO2009129943A8 (fr) 2010-11-18
CN102014875B (zh) 2013-07-24
DE102008020701A1 (de) 2009-10-29
CN102014875A (zh) 2011-04-13
US20110021355A1 (en) 2011-01-27

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