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)

Applications Claiming Priority (2)

Publications (1)

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ID=40984892

Family Applications (1)

Country Status (5)

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Family Cites Families (9)

• 2008
  • 2008-04-24 DE DE102008020701A patent/DE102008020701A1/de not_active Withdrawn
• 2009
  • 2009-04-11 CN CN2009801142789A patent/CN102014875B/zh not_active Expired - Fee Related
  • 2009-04-11 US US12/934,286 patent/US20110021355A1/en not_active Abandoned
  • 2009-04-11 EP EP09735236A patent/EP2271319A1/de not_active Withdrawn
  • 2009-04-11 WO PCT/EP2009/002691 patent/WO2009129943A1/de active Application Filing

Non-Patent Citations (1)

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