CA2273055A1 - Agent for producing a long-lasting saturation effect - Google Patents

Agent for producing a long-lasting saturation effect Download PDF

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Publication number
CA2273055A1
CA2273055A1 CA002273055A CA2273055A CA2273055A1 CA 2273055 A1 CA2273055 A1 CA 2273055A1 CA 002273055 A CA002273055 A CA 002273055A CA 2273055 A CA2273055 A CA 2273055A CA 2273055 A1 CA2273055 A1 CA 2273055A1
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CA
Canada
Prior art keywords
sponge
composition according
oesophagus
stomach
preparation
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.)
Abandoned
Application number
CA002273055A
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French (fr)
Inventor
Gunther Beisel
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Individual
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Individual
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 Individual filed Critical Individual
Publication of CA2273055A1 publication Critical patent/CA2273055A1/en
Abandoned legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0065Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/20Reducing nutritive value; Dietetic products with reduced nutritive value
    • A23L33/21Addition of substantially indigestible substances, e.g. dietary fibres
    • A23L33/25Synthetic polymers, e.g. vinylic or acrylic polymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nutrition Science (AREA)
  • Mycology (AREA)
  • Physiology (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Medicinal Preparation (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cosmetics (AREA)

Abstract

The present invention relates to an orally administered agent, containing material which is insoluble or poorly soluble in water and gastro-intestinal fluids, existing in the shape of a spongy formed body composed of an elastic material, which can be deformed by mastication and deglutition, reduced in form and compressed, so that it can pass through the oesophagus and can be decompressed once it has left the oesophagus in drinking liquids and gastro-intestinal fluids, thereby increasing the volume in the stomach, producing an effect of physiological saturation during its time in the stomach and causing delayed release of integrated active substances and constituents, and which then leaves the body via the intestine after several hours in the stomach in an unabsorbed or poorly absorbable state.

Description

n G~inther Beisel 09.05.199?
C~sitica< !or psa~aiaa a load-la~stiaQ aatiatioas ~ll~oe The present invention relates to a compositioa for oral ingestion, comprising a material which is insoluble or poorly soluble in water and gastro-intestinal fluids, in the form of a sponge-like structure, a process for its preparation and its use for the preparation of compositions for producing a l0 satiation :ffect and for the E~reparation of orally a~ninistrable medicaments) food supplements or food-stuffs having a 'Eime-delayed and g~tle release of active compound.
Numerous axperimoats have been undertaken to break down, medicinally, sup~rfluous concentrations of fat in the human article or to prevent th~ir formation.
There are, for example, so-called appetite suppressants which atteQapt to suggest to the article biochsmically a reluctance to assimilate food. to soma cases, these agents have considerable harmful aide effects.
In addition to the numerous known diet proposals, there are also mechanical and electro-mechanical means with which a specific breakdown of fat or build-up of muscle is supposed to tak0 place. The ~5 action of such means, however, is very doubtful.
German Patent Specification DE 402591 dis-clo~es a composition for oral ingestion, which consists o! a container which can be dissolvee!~.in the stomach where it releases its contents. This is filled with a substance which, after its release in the stomach, increases its volume and thereby guQgests to the article a feeling of satiation.
The disadvantage with this aystan is that the preparation of a special coating is necessary. Hafors the composition eau display its action in the atoa~aeh) some time accordingly elapses. Moreover, the preparation of the coating and the compressed form of the co~osition is associated with considerable outlay.

-a-It is accordingly the object of the present invention to make available a couipogitioa having a satiation effect for oral ingestion, which does not have the described disadvantages of the previous corc~position~. In particular, the outlay for the preparation of the compressed form is intended to be decreased and a foodstuff-like consumption made possible.
This object is achieved by the eompositioa consisting of an elastic material - which is defortnable, shap~-reducible and cvanpressible by chewing and palatine swallowing motion so that it can pass through the oesophagus °
- which, after leaving the oesophagus, is decompressible in drink fluids and in gastrointestinal fluids in the stomach in a volume-building manner) - which during the gastric residence produces a physiological satiation effect, and releases bound active compounds and ingredients in a delayed manner, and - which, after residence in the stomach for a number of hours, leaves the article again unabsorbed or poorly absorbable through the intestine.
In other words. the material is co~anprassed with a simple chewing and swallowing motion and assistance by ingestion of fluid on pas:age through the human oesophagus and, attar leaving the oesophagus.
decompresses in v~ater sad gastrointestinal fluids is the stomach, where it largely regains its original spatial volume.
Sponge-like structures are understood according to the invention as meaning foams which consist of gas-filled, sphere/polyhedron-like cells, which are delineated by highly viscous or solid cell webs. Both naturally occurring sponges sad synthetically prepared sponge-like structures can be employed according to the invention.
The sponge-like or spangiform ~tructure9 are prepared by methods known per se according to the prior art. Depending on the starting material Toyed, in the simplest case a foam can be obtained by blowing, beating, shaking, spraying or stirring in the gas atmosphere concerned. In the ease of the polymers, the foam structure results on account o! cheiaical reactions. Thus the polyurethaaes are foamed by addition of blowing agents, which decompos~ at a certain temperature during the processing with gas formation, or by addition of fluid solvents during the polymerization. Foaming takes place either on leaving the extrusion tocZ7., i.s. following the extrusion or injection moulding or in open moulds. ~4ring is carried out under the conditions characteristic for the respective chemical combination of the material.
an indispensable prerequisite for the employ-ability of the material according to the inveatiod and of the sponge structure is that the material is compressible without the cell webs breaking. In order to be able to employ the material according to the invention specifically for oral ingestion, the foamy or foam-like material must be able to be compressed oa passage through the oesophagus without problems. =n particular, symptoms must not occur oa passing through the oesophagus.
It is furthmrmore essential for the choice of the material and the type of foam formation that it remains swellable' without the cell webs being destroyed. After the passage throu~h'the oesophagus, the sponge-like structure should at least again assume the size which it had before entry into the oesophagus.
z! appropriate, the material can also swell to a size which exceeds the original volume.
The volume of the decompressed, sponge-like structure is 2, preferably 40, em3. The volume in the coa~ressed state is 0.5) preferably 3, Cm3.
The sponge-like structure can have any desired shape is the decompressed state. However, square or rectangular or round esabodimeats are preferred. The surface areas is this case are 6 to 60 cms.
._ Preferably, the material is designed such that the sponge-like structure is compressible to 1/2 to 1/20th, preferably 1/~ to 1/l0th of its volume or its size. Under physiological conditions, the material, which is reduced in shape and compressed by chewing and swallowing motion. should preferably be able to expand to two- to twenty-fold, particularly preferably to four- to tea-fold its volume, in the stomach after exit from the oesophagus.
Materials employed according to the invention for the sponge-like structure can b~ natural, semi-synthetic or synthetic polymers. Examples of suitable synthetic polymers are polyurethanes, polyacrylates, poly(meth)acrylic acid esters) homo- and copolymers of vinyl acetate. The natural and semi-ayathetic polymers include, inter alia) cellulose, ethers) diethyl-celluloae or cellulose esters, such as cellulose diacetate, cellulose triacetate, cellulose acetate propionate and cellulose ac~tate butyrat~. Those suitable according to the invention are, for example, cellulose derivatives, in particular appropriate ethers) e.Q. methylcellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose, or sodium carbo~nethyl-cellulose (preferably those compounds having higher viscosity); certain polymers, such as polyacrylic acid and salt9 thereof; natural (anionic) mucilaginous substances, e.g. xsntha~a gum, guar guw" tragacanth or alginic acid and salts thereof and the like. Moreover) the e~loyment of insoluble polysaccharides) such as chitin or chitin derivatives or microcrystalline cellulose i9 conceivable. Linear high molecular weight polymers are particularly preferred according to the invention. Recording to the invention, those polymers can especially be employed which have a fibre structure. Exat~les of such substances are the scleroproteins, such as keratins, conchagens, fibrin) elastins) chitin and collagen. The latter is parti-cularly preferred according to the invention. =t is possible for the composition according to the invention, inter alia, also to contain pharmaceutically active substances, foodstuffs or food supplements.
minerals, e.g. vitamins, bulk materials, proteins and other foodstuffs or tlavouriags.
sesides the substances mentioned. furthsr auxiliaries can also be aided to the carrier material.
Inter alia, in the case-of the employment of pharma-e~utieally active substances, delaying substances are additionstlly possible.
Moreover,_~the compositions according to the present invention can additionally contain fillers, disintegrants, binders and lubricants and also excipiants.
The present invention also relates to a process for the preparation of the composition described above.
zn this process, in principle) a suspension of the material for the spoaqs-like structure is initially prepared and then freeze-dried. If desired, the material for the sponge-like structure is coma~inuted beforehand and/or subjected to an alkaline and/or an acidic pretreatu~ent. The freeze-drying is preferably carried out at -50 to -150oC) in particular at -80 to -120~C.
Before, during or after the preparation of the sponge-like stsvcture, the material eaa be loaded with the abovementioneiw pharmaceutically active aubatnnces) foodstuffs or food supplsnnents. ~faerals) e.g.
vitamins) bulk materials, proteins and other foodstuffs or flavourings. All eust~ry m~thode are suitable for this. In the simplest case. this can be carried out during the preparation phase of the sponge material by mixing carrier material sad active compound. Likewise, pharmaceuticals, flavourings or luxury foods such as chocolate, icing sugar or similar substances can be applied to the surface.
The purpose of th~ process according to the invention is to obtain a material v~hich oa passage through the oesophagus is sufficiently compressible and moreover is sot decomposed in the case of a relatively ...:

long residence time in the stomach. This aim is achieved using the proves;s steps mentioned. Unlike other foodstuff/food supplement/diet or pharmaceutical products, which are decomposed in the short term by gastric juice or even pass into the stomach in comminuted form and thus again pass through (leave) the stomach in a short time, the sponge or foam article consisting of natural or synthetic fibres and prepared in the manner described regains its original form for several hours as a~ result ot: special fibre crosslinking sites, such that it passes through t~ stomach only after several hours. The fibre sponge is not absorbed in thQ stomach but excreted unabsorbed.
In a variant of the process according to the invention, soluble collagen from the hides of young cattle or pigs (animals) can be employed. The soluble collagen components in the hide of animals specifically become smaller and smaller with increasing age of the article, since the collagexx;~ forms an insoluble three dimensional network as a result of intermolecular crosslinking. The crosslinki_ng sites are solid chemical bonds between individual collagen molecules.
During the preparation of the necessary collagen suspension~ for foam preparation) the hides must therefore come from 1 to 2 year-old animals (bulls). Here too'; the collagen fords an insoluble network. As a result of strongly alkaline and acidic pretreatment of the hide a.nd mechanical forces during preparation of the sponge suspension, it can result that individual chemical and physical crosslinking sites in the collagen are dissolved.
During the drying of the sponge by freeze-drying, preferably at up t,o -120°C, new crosslinking sites are again introduced as a result of the relatively high temperaturs~s in the sponge material.
This brings about the long~lasting insolubility of the sponge article in the gastric juice. This relative gastrfc juice insolubility is a prerequisite fox the ~.

- T -satiation effect lasting due to the long residence of the sponge in the stomach.
The invention is not restricted to the process described, but also applies to all other processes in which sponges or sponge-lake structures are prepared which should or caa achieve a long-term satiation effect due to the relative water and gastric juice insolubility and the long residence time in the stomach thereby resulting.
The composition according to ahe invention is ingested orally. The solid sponge article or solid foam article passes through the oropharyngeal and oesophageal passage by means of addition of drinking fluid and slight chewing or swallowing motions and, due to the gastric fluid) swells again in the stomach.
preferably to its original volume. If appropriate, th~
volume can also be larg.r or smaller than the original.
By means of the oral ingestion of the com posiCion according to the invention, the residence of the solid sponge article or solid foam article in the stomach for several hours is achieved by means of the poor solubility in the stomach. As a result, a long-term feeling of satiation o~r fullness can be achieved, which results in reduced assimilation of food.
Depending.~on the dNSired degree of satiation, one to fifteen foam articlea can be i'Tigested daily at different time intervals. The "satiation sensors' responding due to the foam volume in the stomach produce a satiation effect via the midbrain, which only decreases again on emptying of the stomach. Thus the satiation period can be controlled by the length of residence and the magnitude of the volumes of the sponges.
In the following, the invention is explained in greater detail with reference to the figure:
1. Gastric juice- and water-resistant cube of foam 2. As a result of addition of some fluid, the dry cube of foam loses its solid form and can be swallowed - g -without problems in its aqueous-slippery form like other foodstuffs.
3. The slippery deformed cube of foam passes through the oesophagus.
4. Having reached the stomach, the foam absorbs the gastric and drinking fluid there, and resumes its old spatial volume again.
5. The cube of foam, which :is non-digestible due to its particular fibre structure, residesL in the stomach for 2-20 hours by retaining its volume. As a result of its volume, it does nvt pass through the pylorus.
6. The sponge loses its cube shape again (without being absorbed) only due to the continuous stomach movement (peristaltic, 1-20 hours) and the action of the gastric acid and as a result only has the possibility after 1-20 hours of passing through the pylorus in order to be removed through the intestine. Normal foodstuffs, such as meat or vegetables) are reduced to small pieces and dissolved by the gastric acid even after only a short time in order also to pass through the pylorus after a few minutes. As a result of the special fibre structure described, the composition according to the invention, however, retains its original volume in the stomach due to the resistance to gastric acid so tit the gastric residence which is hours long and thus satiating is caused biologically (physiologically).
a

Claims (14)

Claims:
1. Composition for oral ingestion, comprising a material which is insoluble or poorly soluble in water and gastrointestinal fluids, in the form of a sponge-like structure, characterized in that it consists of an elastic material, - which is deformable, shape-reducible and compressible by chewing and palatine swallowing motion so that it can pass through the oesophagus and - which, after leaving the oesophagus, is decompressible in water and in gastrointestinal fluids in the stomach in a volume-building manner.
2. Composition according to Claim 1, characterized in that after leaving the oesophagus it is decompressible to approximately the size which it had before entry into the oesophagus by oral ingestion.
3. Composition according to one of Claims 1 or 2, characterized in that the sponge-like structure is compressible to 1/2 to 1/20th, preferably 1/4 to 1/10th, its size.
4. Composition according to one of Claims 1 to 3, characterized in that the sponge-life structure is decompressible after leaving the oesophagus to two- to twenty-fold, preferably four- to ten-fold, its size in the compressed state.
5. Composition according to one of Claims 1 to 4, characterized in that the materials for the sponge-like structures are viscose sponges.
6. Composition according to one of Claims 1 to 5, characterized in that the material for the sponge-like structure consists of natural, semi-synthetic or synthetic polymers.
7. Composition according to one of Claims 1 to 6, characterized in that the material for the sponge-like structure consists of long-fibre, linear colloidal, high molecular weight polymers.
8. Composition according to Claim 7, characterized in that the material for the sponge-like structure consists of polymers with fibre structure, preferably of proteins.
9. Composition according to Claim 8, characterized in that the material for the sponge-like structure consists of scleroproteins, preferably collagens.
10. Composition according to one of Claims 1 to 9, characterized in that the sponge-like structure contains foodstuffs and/or medicaments or active compounds or flavourings and/or is coated or covered externally with pharmaceuticals, lacquers or foodstuffs (luxury foods) such as chocolate, icing sugar, fruit material, etc.
11. Process for the preparation of the composition according to one of Claims 1 to 10. characterized in that a collagen-containing suspension of the material for the sponge-like structure is prepared and then freeze-dried.
12. Process for the preparation of the composition according to one of Claims 1 to 11, characterized in that the material for the sponge-like structure is comminuted and/or subjected to an alkaline and/or an acidic pretreatment.
13. Process for the preparation of the composition according to one of Claims 1 to 12, characterized in that the heating during the freeze-drying is carried out at -50°C to -150°C, preferably at -80 to -120°C.
14. Use of the composition according to one of Claims 1 to 13 for the preparation of compositions for producing a satiation effect and for the preparation of orally administrable medicaments, food supplements, foodstuffs or luxury foods having a time-delayed and gentle release of active compound and contents.
CA002273055A 1996-11-27 1997-05-26 Agent for producing a long-lasting saturation effect Abandoned CA2273055A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
WOPCT/EP96/05240 1996-11-27
EP9605240 1996-11-27
PCT/EP1997/002676 WO1998023259A1 (en) 1996-11-27 1997-05-26 Agent for producing a long-lasting saturation effect

Publications (1)

Publication Number Publication Date
CA2273055A1 true CA2273055A1 (en) 1998-06-04

Family

ID=8166411

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002273055A Abandoned CA2273055A1 (en) 1996-11-27 1997-05-26 Agent for producing a long-lasting saturation effect

Country Status (15)

Country Link
EP (1) EP0948316B1 (en)
CN (1) CN1247467A (en)
AT (1) ATE246488T1 (en)
AU (1) AU727639B2 (en)
BR (1) BR9713303A (en)
CA (1) CA2273055A1 (en)
CZ (1) CZ187999A3 (en)
DE (1) DE59710550D1 (en)
HU (1) HUP0003422A3 (en)
NZ (1) NZ335956A (en)
RO (1) RO120688B1 (en)
SI (1) SI20007A (en)
SK (1) SK70299A3 (en)
TR (1) TR199901192T2 (en)
WO (1) WO1998023259A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2383523A1 (en) * 1999-09-06 2001-03-15 Gunther Beisel Cross-linked agent for generation of a long-lasting satiety effect and method for the production of the said
AU7001300A (en) * 1999-09-06 2001-04-10 Gunther Beisel Agent for stimulating bowel function and method for producing the same
CA2384046A1 (en) * 1999-09-06 2001-03-15 Gunther Beisel Method for improving and maintaining bowel function as well as a method for the production thereof
US6677318B1 (en) 2000-09-05 2004-01-13 Beisel Guenther Cross-linked agent for generation of a long-lasting satiety effect and method for the production of the said
DE10044846A1 (en) * 2000-09-11 2002-04-04 Guenther Beisel Agent with prolonged gastric residence time to produce a long-lasting satiety effect and its use
NO20011199A (en) * 2001-03-08 2002-07-08 Alf Reidar Sandstad Method for recovering fluids from the gastrointestinal tract of animals, as well as feed for carrying out this method
DE10216551A1 (en) * 2002-04-15 2003-10-30 Guenther Beisel Orally administered composition for obtaining satiation effect, reducing body weight and regulating cholesterol levels, comprising dried porous gel or foam of anionic polymer in aluminum salt form
AU2003296628A1 (en) * 2002-12-19 2004-07-14 Gunther Beisel Agent with a retarded release of substances
DE10259507A1 (en) * 2002-12-19 2004-07-08 Beisel, Günther Agent giving a repletion effect and weight loss contains both a volume- expanding material which is insoluble or difficultly-soluble in gastric or bodily fluids and a release material.
CN104799290A (en) * 2015-05-04 2015-07-29 程晋生 Compressed fiber particle and method for absorbing fat, expelling toxin and clearing bowels by use of compressed fiber particle

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4298002A (en) * 1979-09-10 1981-11-03 National Patent Development Corporation Porous hydrophilic materials, chambers therefrom, and devices comprising such chambers and biologically active tissue and methods of preparation
JPS5668608A (en) * 1979-11-06 1981-06-09 Lion Corp Sponge base for medicine
DE69105323T2 (en) * 1990-03-27 1995-06-01 Bioelastics Res Ltd Bioelastomeric drug delivery system.
DE4119140C2 (en) * 1991-06-11 1994-05-11 Merz & Co Gmbh & Co Porous spongeoid moldings soluble in body fluids and secretions, their preparation and use
IL105529A0 (en) * 1992-05-01 1993-08-18 Amgen Inc Collagen-containing sponges as drug delivery for proteins
CA2232489A1 (en) * 1995-12-01 1997-06-12 Janssen Pharmaceutica N.V. Cisapride sustained release
AU1090697A (en) * 1995-12-19 1997-07-14 Thermicedge Corporation Spheres useful in a detachable connective medium for ball grid array assemblies

Also Published As

Publication number Publication date
AU727639B2 (en) 2000-12-21
RO120688B1 (en) 2006-06-30
CZ187999A3 (en) 1999-10-13
EP0948316A1 (en) 1999-10-13
SK70299A3 (en) 2000-01-18
ATE246488T1 (en) 2003-08-15
AU3091997A (en) 1998-06-22
WO1998023259A1 (en) 1998-06-04
SI20007A (en) 2000-02-29
EP0948316B1 (en) 2003-08-06
HUP0003422A2 (en) 2001-02-28
CN1247467A (en) 2000-03-15
TR199901192T2 (en) 1999-07-21
BR9713303A (en) 2000-03-21
NZ335956A (en) 2000-09-29
HUP0003422A3 (en) 2001-03-28
DE59710550D1 (en) 2003-09-11

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EEER Examination request
FZDE Discontinued