WO2004087114A1 - Capsules pour administration orale a action retardee du contenu de la capsule - Google Patents
Capsules pour administration orale a action retardee du contenu de la capsule Download PDFInfo
- Publication number
- WO2004087114A1 WO2004087114A1 PCT/EP2004/003400 EP2004003400W WO2004087114A1 WO 2004087114 A1 WO2004087114 A1 WO 2004087114A1 EP 2004003400 W EP2004003400 W EP 2004003400W WO 2004087114 A1 WO2004087114 A1 WO 2004087114A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- gelatin capsules
- oil
- capsule
- capsules according
- capsules
- Prior art date
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
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
-
- 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
- A61K9/485—Inorganic compounds
Definitions
- the present invention relates to gelatin capsules with delayed release of the capsule content for use as an oral dosage form for food supplements, diatetics and medicaments, the delay in the release being brought about by a plant extract contained in the capsule.
- the active ingredient is only released from the dosage form a certain time after ingestion or in a certain section of the gastrointestinal tract.
- the aim of this temporally or locally controlled release is either to protect the user from the unpleasant properties of the active ingredient (eg bad taste, mucous membrane irritant effect, unpleasant eructation) or to protect the active ingredient from being destroyed by the aggressive gastric juice or to improve absorption to achieve the active ingredients in the body through release in the small intestine.
- This delayed release is particularly desirable when the active ingredients to be applied are pear extracts which, if the capsule disintegrates too quickly, result in an unpleasant taste or smell when belching open or contain substances which can be broken down in the stomach.
- a preferred dosage form for these food supplements, diatetics and pharmaceuticals is the capsule, which can be filled with liquid, semi-solid or solid substances and whose shell mostly consists of gelatin.
- Soft gelatin capsules are particularly suitable because they are manufactured, filled and sealed in one step, the capsule contents are well protected against environmental influences such as moisture and oxygen and because these capsules are very easy to take.
- EP 0243930 B1 describes a gelatin-encapsulated composition with controlled release, consisting of a solid matrix, which is formed from a liquid filling of a vegetable gum and the active ingredient by adding cations.
- a disadvantage of this type of process is that additional special auxiliaries have to be added to the capsule filling compound in order to obtain a matrix which controls the release.
- Preparations and processes are used far more frequently in which the release is achieved by changing the capsule shell, either adding substances to the capsule shell material or applying a functional coating to the finished capsule.
- An example of controlling the release by means of additives to the capsule shell material is EP 0240581 B1, in which physiologically and toxicologically harmless aldehydes with at least 4 carbon atoms are added to the gelatin brew and the brew is further processed into capsules in a manner known per se.
- a disadvantage of this method is that additional substances have to be introduced into the capsule shell, which can have an undesirable influence on the properties of the capsule or the encapsulated ingredients.
- EP 1091659 B1 describes a special embodiment of these aldehyde-hardened gelatin capsules, in which finished capsules are sprayed with a solution of xylose, ethanol and water using heat and then heat-treated for a certain period of time. This process is technically and time-consuming, since the solvent used must be removed almost completely during the process and ethanol can only be used as a flammable organic solvent under special technical conditions.
- polymers are used which are insoluble in strongly acidic gastric juice, but soluble in almost neutral intestinal juice (ie from approx. PH 5-6).
- suitable poly- mers eg hydroxypropylmethyl cellulose phthalate
- this solution applied to the capsules in a rotating kettle or a coater.
- the solvent is evaporated by large amounts of heated air and the precipitated polymer forms a coating on the capsules. This process is technically and time-consuming.
- the object of the present invention is therefore to influence the disintegration of capsules and the release of the capsule contents during oral administration in a new, simplified and safe form.
- polyphenols includes simple phenol carboxylic acids such as. As gentisic acid, protocatechic acid, gallic acid or caffeic acid, flavones such as. B. camphor oil, quercetin, myricetin, isomamnetin, naringenin, 6-prenylnaringenin, 8-prenylnaringenin, isoxanthohumol and their glycosides, chalcones such as ⁇ . B. xanthohumol, isoflavones such as.
- anthocyanins such as. As pelargonidine, cyanidine, malvidin or delphinidine, tanning agents such as. B. catechin and epicatechin and their oligomers and polymers.
- Camellia sinensis Crataegus monogyna, Ginkgo biloba, Humulus lupulus, Hypericum perforatum, Krameria triandra, Potentilla tormantilla, Pterocarpus marsupium, Quercus species, Uncaria gambir, Vaccinitis myrtle vinifera.
- polyphenol-containing plant extracts are now used for the first time in order to specifically influence the release of active ingredients from gelatin capsules, this type of decay delay being able to be used with all capsule materials which show an interaction with polyphenols in the manner described.
- Another advantage of these preparations is that the plant extract used is at the same time one of the active ingredients to be applied, i.e. no additional additives such as Coating, hardening or thickening agents are added to achieve the sustained release.
- the extracts are filled into the capsules with lipophilic, water-immiscible liquid carriers such as e.g. Mixed vegetable oils.
- lipophilic, water-immiscible liquid carriers such as e.g. Mixed vegetable oils.
- This flowable mixture is well suited for filling in capsules.
- other substances such as Partially or fully hydrogenated vegetable oils, beeswax, lecithin, neutral oil, hard fat and highly disperse silicon dioxide are added to the capsule filling mass in order to adjust the consistency of the mixture and to prevent separation of the liquid carrier and solid plant extract.
- amphiphilic, surface-active substances and emuigators such as e.g. Sorbitan monooleate can be added.
- the extracts can be prepared in a variable composition with solvents such as e.g. B. water, methanol, ethanol, 2-propanol, acetone, etc. and their mixtures, at temperatures of room temperature. up to 100 ° C with gentle to vigorous mixing or by percolation within 10 minutes to 24 hours under normal pressure or increased pressure.
- solvents such as e.g. B. water, methanol, ethanol, 2-propanol, acetone, etc. and their mixtures
- further concentration steps can be carried out, e.g. B. liquid liquid distribution with z. B. 1-butanol / water or ethyl acetate / water, adsorption-desorption on ion exchanger, LH20, HP20 and other resins or chromatographic separations over RP18, silica gel, etc.
- the further processing to dry extracts is carried out according to known methods by removing the solvent increased temperature and / or reduced pressure.
- a particularly preferred embodiment of the capsules with delayed disintegration is the combination of a polyphenol-containing plant extract and an oil with a high content of omega-3 fatty acids, in particular periila seed oil, evening primrose seed oil, currant seed oil, fish oil, borage oil or linseed oil, because both the polyphenol-containing plant extracts and those mentioned Vegetable oils favorably influence chronic inflammatory or immunological diseases and fat metabolism disorders.
- Gelatin capsules containing one of the following combinations are preferred: extract from Vitis vinifera (grape seed extract, ie extract from seeds of red and / or white grapes) and periila seed oil, extract from Vitis vinifera (red wine extract, ie extract from red grapes) and periilase seed oil, extract from Potentilla tormentilla and linseed oil, extract from Crataegus monogyna and linseed oil, extract from Camellia sinensis and borage oil, extract from Ginkgo biloba and borage oil, extract from Krameria triandra and evening primrose oil, extract from Vaccinium myrtillus and evening primrose oil, extract from hyper extract Humulus lupulus and fish oil, extract from Uncaria gambir and currant seed oil, extract from Quercus and currant seed oil, extract from Pterocarpus marsupium and Periilasamenöl, extract from Camellia sinensis and Periilasa
- the delay in the release of active ingredient is independent of whether the gelatin capsules are hard or soft gelatin capsules, since these differ only in the plasticizer and water content.
- Example 1 the gelatin capsules are hard or soft gelatin capsules, since these differ only in the plasticizer and water content.
- Periila seed oil (75 parts) is mixed with hard fat (12 parts) and heated to 40 ° C with stirring.
- Granular silica (5 parts) and grape seed extract (8 parts) are added to the liquid phase and distributed with stirring.
- 0.6 g of the suspension obtained are filled into a gelatin capsule. The sealed capsules are stored at an elevated temperature.
- the capsules containing grape seed extract show a prolonged disintegration time in the disintegration test in artificial gastric juice compared to the capsules that do not contain grape seed extract.
- Periila seed oil (69 parts) is mixed with hard fat (11 parts) and heated to 40 ° C with stirring. Highly disperse silicon dioxide (5 parts) and red wine extract (15 parts) are added to the liquid phase and distributed with stirring. Each 0.65 g of the suspension obtained is filled into a gelatin capsule. The sealed capsules are stored at an elevated temperature.
- the capsules containing red wine extract show a prolonged disintegration time when tested in artificial gastric juice compared to capsules that do not contain red wine extract.
- the initial value for the capsule opening time before incubation at elevated temperature / humidity was 4 min. Without the addition of the polyphenol-containing plant extract, the disintegration time remains unchanged even when stored; the addition of the plant extract and storage increases the disintegration time of the capsules. Storage in the absence of water vapor leads to a longer increase in the decay time.
- the disintegration time of soft gelatin capsules can thus be influenced in a targeted manner, as has been shown on two capsule batches which contain two different batches of the red wine extract.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Medical Informatics (AREA)
- Botany (AREA)
- Alternative & Traditional Medicine (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04724576A EP1608345A1 (fr) | 2003-04-02 | 2004-03-31 | Capsules pour administration orale a action retardee du contenu de la capsule |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE2003115027 DE10315027A1 (de) | 2003-04-02 | 2003-04-02 | Kapseln mit verzögerter Freisetzung des Kapselinhaltes zur oralen Verabreichung |
DE10315027.7 | 2003-04-02 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2004087114A1 true WO2004087114A1 (fr) | 2004-10-14 |
Family
ID=32980962
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP2004/003400 WO2004087114A1 (fr) | 2003-04-02 | 2004-03-31 | Capsules pour administration orale a action retardee du contenu de la capsule |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP1608345A1 (fr) |
DE (1) | DE10315027A1 (fr) |
WO (1) | WO2004087114A1 (fr) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004087181A2 (fr) * | 2003-04-02 | 2004-10-14 | Bioplanta Arzneimittel Gmbh | Combinaisons de principes actifs d'huiles contenant des acides gras $g(v)3 avec des extraits vegetaux contenant des polyphenols et utilisation desdites combinaisons |
EP1698332A1 (fr) * | 2005-03-02 | 2006-09-06 | KAIROSmed GmbH | Compositions orales à libération modifiée contenant le composé 8-prénylnaringénine pour une substitution estrogénique continue |
WO2006092295A1 (fr) * | 2005-03-02 | 2006-09-08 | Kairosmed Gmbh | Formulations orales a liberation modifiee contenant de la 8-prenylnaringenine pour un soutien estrogenique continu |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107712902A (zh) * | 2017-11-23 | 2018-02-23 | 甘肃省徽县雅龙银杏产业开发有限责任公司 | 一种含银杏果和橄榄油的保健品及其制备方法 |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1011265A (en) * | 1961-09-25 | 1965-11-24 | Takeda Chemical Industries Ltd | A process for the preparation of a medicinal agent for the treatment of hypercholesterolemia from the oil of marine animals |
JPH02243622A (ja) * | 1989-03-16 | 1990-09-27 | Nippon Oil & Fats Co Ltd | 血中コレステロール低下用油脂組成物 |
EP0502766A1 (fr) * | 1991-03-05 | 1992-09-09 | Institut De Recherche Biologique S.A. | Compositions diététiques à base de lipides phosphorylés et leur utilisation dans l'amélioration des troubles de la vision |
EP0573777A1 (fr) * | 1992-05-11 | 1993-12-15 | INDENA S.p.A. | Compositions pharmaceutiques orales contenant des anthocyanosides |
US5955102A (en) * | 1998-09-04 | 1999-09-21 | Amway Corporation | Softgel capsule containing DHA and antioxidants |
CN1279072A (zh) * | 2000-07-03 | 2001-01-10 | 高林 | 一种防治心脑血管病的药物 |
-
2003
- 2003-04-02 DE DE2003115027 patent/DE10315027A1/de not_active Withdrawn
-
2004
- 2004-03-31 WO PCT/EP2004/003400 patent/WO2004087114A1/fr active Search and Examination
- 2004-03-31 EP EP04724576A patent/EP1608345A1/fr not_active Withdrawn
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1011265A (en) * | 1961-09-25 | 1965-11-24 | Takeda Chemical Industries Ltd | A process for the preparation of a medicinal agent for the treatment of hypercholesterolemia from the oil of marine animals |
JPH02243622A (ja) * | 1989-03-16 | 1990-09-27 | Nippon Oil & Fats Co Ltd | 血中コレステロール低下用油脂組成物 |
EP0502766A1 (fr) * | 1991-03-05 | 1992-09-09 | Institut De Recherche Biologique S.A. | Compositions diététiques à base de lipides phosphorylés et leur utilisation dans l'amélioration des troubles de la vision |
EP0573777A1 (fr) * | 1992-05-11 | 1993-12-15 | INDENA S.p.A. | Compositions pharmaceutiques orales contenant des anthocyanosides |
US5955102A (en) * | 1998-09-04 | 1999-09-21 | Amway Corporation | Softgel capsule containing DHA and antioxidants |
CN1279072A (zh) * | 2000-07-03 | 2001-01-10 | 高林 | 一种防治心脑血管病的药物 |
Non-Patent Citations (1)
Title |
---|
PATENT ABSTRACTS OF JAPAN vol. 0145, no. 62 (C - 0788) 13 December 1990 (1990-12-13) * |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004087181A2 (fr) * | 2003-04-02 | 2004-10-14 | Bioplanta Arzneimittel Gmbh | Combinaisons de principes actifs d'huiles contenant des acides gras $g(v)3 avec des extraits vegetaux contenant des polyphenols et utilisation desdites combinaisons |
WO2004087181A3 (fr) * | 2003-04-02 | 2005-04-21 | Bioplanta Arzneimittel Gmbh | Combinaisons de principes actifs d'huiles contenant des acides gras $g(v)3 avec des extraits vegetaux contenant des polyphenols et utilisation desdites combinaisons |
EP1698332A1 (fr) * | 2005-03-02 | 2006-09-06 | KAIROSmed GmbH | Compositions orales à libération modifiée contenant le composé 8-prénylnaringénine pour une substitution estrogénique continue |
WO2006092295A1 (fr) * | 2005-03-02 | 2006-09-08 | Kairosmed Gmbh | Formulations orales a liberation modifiee contenant de la 8-prenylnaringenine pour un soutien estrogenique continu |
Also Published As
Publication number | Publication date |
---|---|
EP1608345A1 (fr) | 2005-12-28 |
DE10315027A1 (de) | 2004-10-14 |
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