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EP1722884A1 - Multi-microcapsules stables au stockage comportant des composants fonctionnels synergiquement actifs a liberation controlee - Google Patents

Multi-microcapsules stables au stockage comportant des composants fonctionnels synergiquement actifs a liberation controlee

Info

Publication number
EP1722884A1
EP1722884A1 EP04714290A EP04714290A EP1722884A1 EP 1722884 A1 EP1722884 A1 EP 1722884A1 EP 04714290 A EP04714290 A EP 04714290A EP 04714290 A EP04714290 A EP 04714290A EP 1722884 A1 EP1722884 A1 EP 1722884A1
Authority
EP
European Patent Office
Prior art keywords
substance
substance components
components
microcapsules
functional
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Withdrawn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
EP04714290A
Other languages
German (de)
English (en)
Inventor
Erich Windhab
Michael Zimmermann
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.)
Eidgenoessische Technische Hochschule Zurich ETHZ
Original Assignee
Eidgenoessische Technische Hochschule Zurich ETHZ
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 Eidgenoessische Technische Hochschule Zurich ETHZ filed Critical Eidgenoessische Technische Hochschule Zurich ETHZ
Publication of EP1722884A1 publication Critical patent/EP1722884A1/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Withdrawn legal-status Critical Current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
    • A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
    • B01J13/02—Making microcapsules or microballoons

Definitions

  • the invention relates to multi-microcapsules in which several, in the sense, for. B. pharmaceutical / medical and / or nutritional properties of functional substances or substance components are encapsulated.
  • the effectiveness of functional substances / components is also significantly affected by their interaction with other substances that are in the human digestive tract.
  • Such undesirable interacting substances in the digestive tract can originate from food and can also be part of the digestive system.
  • iron preparations added to remedy iron deficiency symptoms under the general conditions in the stomach of humans (low pH values), as well as through oxidation effects when interacting with e.g. B. oxidized phytic acids from plant foods or dairy products, so impaired in terms of their absorbability in the small intestine and thus limited in bioavailability.
  • Iron deficiency-related anemia, thyroid enlargement (goiter) resulting from iodine deficiency and vitamin A deficiency affect more than a third of the world's population. Often these shortcomings occur simultaneously, such. B. in regions of West and North Africa where approx. 1/3 of schoolchildren suffer from iron, iodine and vitamin A deficiency at the same time. These three nutritional components are extremely important for human metabolism. Iron and vitamin A deficiency affect the thyroid metabolism of iodine and reduce the effectiveness of iodized salt. Vitamin A deficiency also affects iron transport in the body and worsens iron deficiency-related anemia.
  • the object of the invention is to configure a multi-microcapsule for incorporating several pharmacologically / medically and / or nutritionally active functional substances / substance components in such a way that the encapsulated substances / substance components on the one hand show no interactions under storage conditions and on the other hand in coordination when applied
  • the encapsulated substances / substance components can be released in a defined manner to the ambient conditions with regard to the time of the release and the release rate.
  • the aim is also to combine the encapsulated substances in such a way that positive synergistic effects (e.g. mutual protective action against oxidation, improved bioavailability) can be achieved during storage, release and interaction.
  • multi-microcapsules By means of the multi-microcapsules according to the invention, several substances / substance components with functional properties can be integrated into a "multi-microcapsule" such that no interaction of the encapsulated substances / substance components takes place during the storage of such capsules. H. Storage stability is guaranteed.
  • Another important advantage results from the spatial proximity of the substances / substance components fixed in a microcapsule, since when they are released from the microcapsule, this leads to contact and, as a result of a corresponding combination, to targeted synergistic interactions
  • Another advantage is the adjustability according to the invention of the time of release and the rate of release of encapsulated functional substances / substance components by means of a suitable choice coordinated with the environmental conditions during use, which is around these functional ones Capsule materials forming shell layers, as well as their layer thickness and microstructure.
  • multi-microcapsules can be used to transport nutrient components, such as water-soluble iron salts (1st component), to the small intestine, who are deficient in oxidation, and to release these salts from the capsule synchronously with an antioxidant (2nd component).
  • nutrient components such as water-soluble iron salts (1st component)
  • 2nd component an antioxidant
  • the intensive interaction of these components in the microenvironment of the capsule will protect the iron salt from oxidation and the iron bioavailability d. H. significantly improve its absorption in the small intestine.
  • the multi-microcapsules according to the invention allow the integration / encapsulation of several functional substances / substance components in a multi-capsule with the possibility of setting separating layers between these substances / substance components with regard to diffusion permeability, time of release and release kinetics. This is the prerequisite for the production of a multi-microcapsule suitable for storage stability and optimized release of several functional synergistically interacting substances / substance components.
  • the invention is illustrated for example in the drawing. Show it: 1 shows a multi-microcapsule morphology;
  • Fig. 2 crystalline functional material phases with surrounding amorphous layer and additional outer amorphous boundary layer;
  • Fig. 3 shows the digestive route of a multi-microcapsule in the human gastrointestinal tract.
  • FIG. 1 The complex structure of a multi-microcapsule is shown in FIG. 1 for illustration.
  • the abbreviations used in the text below can be found in Figure 1 and Table 1 (nomenclature overview; Appendix).
  • multi microcapsules are made up of subcapsules (SKi) with encapsulated functional individual substance components (FSi) by embedding these SKi in a main capsule matrix phase (HKMP).
  • This main capsule matrix phase is chosen such that a diffusion-based exchange of the encapsulated functional substances / substance components (FSi) is largely prevented under storage conditions.
  • the FSi are preferably used in solid, mostly crystalline form.
  • the different FSi are preferably included in a subcapsule matrix phase (SKMPi). According to the invention, these SKMPi are chosen opposite to the FSi with regard to their hydrophilicity / hydrophobicity.
  • the molecular structure of the SKMPi is preferably largely amorphous (glass-like), possibly also crystalline or gel-like, via the composition and manufacturing process.
  • additional interface layers are created by means of surface-active substances as diffusion barriers between FSi and SKMPi and between SKMPi and HKMP.
  • such an interface layer can also surround the main capsule (GFH).
  • the following sizes of the multi-microcapsule are adapted according to the invention to set the time of release of the SKi and its release kinetics:
  • Geometric parameters • Diameter of the FSi particles: a few nanometers - 50 micrometers • Diameter of the subcapsules (SKi): 1 - 200 micrometers • diameter of the main capsule (HK): a few micrometers - a few millimeters • thickness of the interface layers (GSi)
  • the main capsule matrix phase corresponds to an additional coating layer. If necessary, this can also be omitted.
  • Individual encapsulation of the FSi in subcapsules and an increase in the number of "cladding layers" (GFi, SKMPi, HKMP) allow, on the one hand, an improvement in the stability properties of the capsules under storage conditions. On the other hand, these cladding layers allow flexible adaptation to the application conditions.
  • microcapsules in general is to transport the functional substances / substance components FSi to the preferred location for their release and to set their release kinetics as defined as possible.
  • An additional aim of the multi-microcapsules according to the invention is to release several FSi in the immediate vicinity at the same time or in a defined sequence, and thus to enable a reaction of these released FSi without significant interference from material components from the environment.
  • the combination of the encapsulated FSi takes place according to the invention in such a way that synergistic interactions are realized.
  • an antioxidant FS1
  • a nutritionally or pharmacologically / medically relevant compound FS2
  • destination location of the FSi release.
  • A. mouth / throat pH neutral; heavy mechanical stress, water-soluble enzyme activity
  • B. stomach pH low; mechanical stress
  • C. Gastric exit / small intestine pH neutral; introduction of enzymes (e.g. fat-soluble lipases (bile), water-soluble enzymes in the digestive juice).
  • the cladding layers enable the thermal, mechanical, pH and enzymatic stability properties to be set. It may also be desirable to break down the corresponding coating layer in order to ensure the release of the FSi at the destination.
  • fat-based layers for example, are affected by the action of lipa- and macromolecular networks in water-based layers are degraded by water-soluble enzymes (e.g. cellulases, proteases) at the stomach exit or in the small intestine. Adjusting the thickness of such layers allows the location of the FSi release e.g. B. move along the small intestine or influence the FSi release kinetics.
  • the step-by-step disruption of a multi-microcapsule in the human gastrointestinal tract is shown schematically as an example in FIG.
  • FSi contain the substances iron pyrophosphate (functional, nutritive component: iron), sodium iodate (functional, nutritive component: iodine and retinyl palmitats (functional Component: Vitamin A) in encapsulated form.
  • the encapsulation was carried out in hydrogenated (hardened) palm kernel fat as the common main capsule matrix phase.
  • the iron (Fe) -iodine (J) -Vitamin A multi-microcapsules short: FeJA-CAPS
  • Saline is considered the ideal vehicle for the nutritional reinforcement of food and is therefore also suitable for experiments on "three-component enrichment" with iron, iodine and vitamin A. So far, such enrichments have not been successful because water-soluble iron compounds with moisture from salt or Ambient air and impurities in the table salt caused unacceptable color changes, and iodine and vitamin A in enriched table salt were oxidized and thus lost in the presence of moisture and oxygen.
  • Table 1 shows the mean concentrations of vitamin A, iodine and iron from each of the 12 50 g salt samples examined for each storage period.
  • vitamin A showed losses of 80-90% in one month and iodine about 40-50% in six months.
  • Salt-enriched table salt The other group is the triple fortified salt TFS (FeJA-CAPS).
  • This example underlines the effectiveness of multi-microcapsules in terms of achieving good storage stability that has not yet been achieved, as well as improved functionality in terms of bioavailability of the investigated nutritional substance components.
  • HKMP main capsule - matrix phase
  • GFSi interface outer layers of the subcapsules
  • NMH network-forming macromolecules in the main capsule matrix phase
  • NMSi network-forming macromolecules in the subcapsule matrix phase

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne de nouveaux systèmes de capsules à plusieurs composants dans lesquels deux ou plus de deux substances fonctionnelles ou composants de substance fonctionnelle sont encapsulé(e)s de manière spatialement séparée, de façon que, lors du stockage des systèmes de multicapsules, les composants encapsulés ne puissent pas interagir, mais lorsque lesdites multicapsules sont administrées, les différent(e)s substances fonctionnelles ou composants de substance fonctionnelle encapsulé(e)s soient libéré(e)s de manière ciblée par rapport au site de libération, au moment de libération et à la vitesse de libération, simultanément ou successivement, en fonction de leur domaine d'application. Dans les multi-microcapsules selon l'invention, plusieurs substances fonctionnelles ou composants de substance fonctionnelle sont enveloppé(e)s au moyen d'une ou de plusieurs couches de matière présentant des propriétés de stabilité mécanique, thermique et physico-chimique ou biochimique définies, qui sont optimalisées en fonction des conditions d'utilisation pour que l'interaction et la libération des substances ou des composants de substance encapsulé(e)s soient telles que souhaitées.
EP04714290A 2004-02-25 2004-02-25 Multi-microcapsules stables au stockage comportant des composants fonctionnels synergiquement actifs a liberation controlee Withdrawn EP1722884A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2004/001840 WO2005079968A1 (fr) 2004-02-25 2004-02-25 Multi-microcapsules stables au stockage comportant des composants fonctionnels synergiquement actifs a liberation controlee

Publications (1)

Publication Number Publication Date
EP1722884A1 true EP1722884A1 (fr) 2006-11-22

Family

ID=34878405

Family Applications (1)

Application Number Title Priority Date Filing Date
EP04714290A Withdrawn EP1722884A1 (fr) 2004-02-25 2004-02-25 Multi-microcapsules stables au stockage comportant des composants fonctionnels synergiquement actifs a liberation controlee

Country Status (2)

Country Link
EP (1) EP1722884A1 (fr)
WO (1) WO2005079968A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102017111444A1 (de) 2017-05-24 2018-11-29 Henkel Ag & Co. Kgaa Mikrokapselsystem für polysensorische Dufteffekte
CN120530970B (zh) * 2025-07-29 2025-09-26 禾美思(山东)植物保护有限公司 一种高效除草剂制备工艺

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3429827A (en) * 1962-11-23 1969-02-25 Moore Business Forms Inc Method of encapsulation
US4532123A (en) * 1982-03-04 1985-07-30 Battelle Development Corporation Dual Microcapsules and process for their preparation
WO2002007710A2 (fr) * 2000-07-20 2002-01-31 Mw Encap Limited Dispositif de delivrance

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2005079968A1 *

Also Published As

Publication number Publication date
WO2005079968A1 (fr) 2005-09-01

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