EP0725626A1 - Substance a pouvoir moussant garnissant une gelule de gelatine - Google Patents

Substance a pouvoir moussant garnissant une gelule de gelatine

Info

Publication number
EP0725626A1
EP0725626A1 EP94931124A EP94931124A EP0725626A1 EP 0725626 A1 EP0725626 A1 EP 0725626A1 EP 94931124 A EP94931124 A EP 94931124A EP 94931124 A EP94931124 A EP 94931124A EP 0725626 A1 EP0725626 A1 EP 0725626A1
Authority
EP
European Patent Office
Prior art keywords
carbonate
pharmaceutical product
product according
oil
fill
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Withdrawn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
EP94931124A
Other languages
German (de)
English (en)
Inventor
Keith Sugden
Keith Graeme Hutchison
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.)
Reckitt Benckiser Healthcare UK Ltd
Original Assignee
Reckitt and Colman Products Ltd
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
Priority claimed from GB939322314A external-priority patent/GB9322314D0/en
Application filed by Reckitt and Colman Products Ltd filed Critical Reckitt and Colman Products Ltd
Publication of EP0725626A1 publication Critical patent/EP0725626A1/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Withdrawn legal-status Critical Current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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus

Definitions

  • This invention relates to pharmaceutical products and in particular to compositions for the treatment of reflux oesophagitis, gastritis or peptic ulceration.
  • Reflux oesophagitis occurs when small amounts of gastric juice, food and/or bile acids pass into the lower part of the oesophagus and cause oesophageal inflammation accompanied by pain which may manifest itself in the form of heartburn.
  • One approach to the problem of reflux oesophagitis comprises the administration of a preparation which on contact with gastric acid generates a carbonated gelatinous foam or raft which floats on the stomach contents. When reflux occurs it is this raft which precedes the stomach contents into the oesophagus thus protecting the mucosa from further irritation.
  • a pharmaceutical product for the treatment of reflux oesophagitis, gastritis or peptic ulceration in the form of a chewable soft gelatin capsule with a fill comprising (a) polymeric material selected from alginic acid, alginates, pectin, xanthan, gellan, carageenan and mixtures thereof; (b) a carbonate or bicarbonate salt; (c) an oil-based or hydrophilic based liquid vehicle; wherein on oral ingestion the gelatin capsule shell ruptures and the fill reacts with the acid contents of the stomach thereby producing a carbonated floating gelatinous raft of such rigidity that in the penetration test as hereinafter defined there is not complete penetration.
  • the polymeric material is the sodium, potassium, ammonium, magnesium or calcium salt of alginic acid or the propylene glycol esters or mixtures thereof.
  • rafts of improved strength are obtained if the composition includes a source of divalent calcium or trivalent aluminium ion which act as cross-linking agents.
  • Suitable sources of calcium ions are those derived from the carbonate, lactate, chloride, gluconate, phosphate, hydrogen phosphate, sulphate, tartrate or citrate salts.
  • Suitable sources of aluminium ions are those derived from the carbonate, lactate, glycinate or phosphate salts or from aluminium magnesium carbonate hydroxide, agaldrate, aluminium sodium carbonate hydroxide or aluminium sodium silicate. Conveniently the relative quantities by weight of the calcium salt or aluminium compound to the alginic acid or alginate calculated as ions are 4 to 120 Ca 2+ to 500 alginate " or 2 to 80 Al 3+ to 500 alginate" respectively.
  • Suitable carbonate or bicarbonate salts are potassium carbonate or bicarbonate, sodium carbonate or bicarbonate, calcium carbonate, sodium glycine carbonate, magnesium carbonate or aluminium carbonate.
  • the carbonate or bicarbonate salt is present in an amount so as to provide an adequate volume of gas (carbon dioxide) to float the gel produced when the polymeric material contacts the gastric acid in the stomach.
  • gas carbon dioxide
  • the relative quantities by weight of polymeric material to the carbonate or bicarbonate calculated as ions is 35 to 300 CO 3 2 " or HC0 3 ⁇ to 500 polymeric material.
  • the rigidity and thickness of the carbonated raft formed on contact with the gastric acid will depend upon the ratio of carbonate or bicarbonate to the polymeric material and upon the grade of the polymeric material.
  • Suitable oil-based liquid vehicles are natural oils such as soya bean oil, fractionated coconut oil, mineral oils, triacetin, ethyl oleate, hydrogenated natural oil and mixtures thereof.
  • Suitable hydrophilic based liquid vehicles are polyethylene glycols (PEG's) particularly PEG 400 and PEG 600, glycofurol, polyglycerols, propylene glycol, Transcutol, polysorbate and propylene carbonate and mixtures thereof.
  • the invention also includes a method of treating reflux oesophagitis, gastritis or peptic ulceration which comprises administration of an effective amount of a product which is capable of forming a floating gelatinous raft when contacted with the acid contents of the stomach said raft being of such rigidity that in the penetration test as hereinafter defined there is not complete penetration and said product being in the form of a chewable soft gelatin capsule with a fill comprising (a) polymeric material selected from alginic acid, alginates, pectin, xanthan, gellan, carageenan and mixtures thereof; (b) a carbonate or bicarbonate salt; (c) an oil-based or hydrophilic based liquid vehicle.
  • a fill comprising (a) polymeric material selected from alginic acid, alginates, pectin, xanthan, gellan, carageenan and mixtures thereof; (b) a carbonate or bicarbonate salt; (c) an oil-based or hydrophilic based liquid vehicle.
  • the gelatin capsules may be simultaneously formed and filled using conventional methods and apparatus such as disclosed, for example, in an article by H. Seager in Pharmaceutical Technology September 1985.
  • All the ingredients of the fill material including the liquid vehicle are mixed together, with heating if necessary, until the desired consistency for filling and the desired unifor ity is obtained.
  • the encapsulation machine is suitably an R P Scherer encapsulation machine.
  • a surfactant may be included in the fill.
  • the polymeric materials will have a thickening effect upon the liquid fill.
  • This thickening effect may be further increased if so desired by the inclusion of a thickening agent such as hydrogenated vegetable oils, glyceryl monostearate, glyceryl monopalmitate, beeswax (or other high melting point fat or wax) or a dispersed thickener such as colloidal silicon dioxide.
  • a suitable thickening agent may be one or more high molecular weight PEG's.”
  • the capsules will be suitably shaped and sized so as to be readily ingestible by a person following chewing.
  • Example 1 The invention is illustrated by the following Examples: Example 1
  • Capsules in a standard gelatin shell were prepared having the following fill:
  • Capsules were prepared as in Example 1 except that the amount of calcium carbonate in the fill materials was increased to 100 mg.
  • Example 3
  • Capsules were prepared as in Example 1 having the following fill: Quantity/Capsule
  • Example 4 were prepared as in Example 1 having the following fill:
  • Example 5 1500 mg Example 5 Capsules were prepared as in Example 1 having the following fill:
  • Capsules were prepared as in Example l having the following fill:
  • the appropriate amount of product (equivalent to 6 doses of lg of polymeric material) was weighed and added to a 250ml tall-form beaker (height 120mm & diameter 60mm) previously weighed. A volume of 120ml of deionised water was added and the mixture homogenized for 5 minutes using the Silverson Model L4R ho ogenizer with a Turbular Unit 1" in diameter and a square hole high shear screen. The speed of the homogenizer was set at speed 4 / 5000-5200 rpm. In the case of Liquid Gaviscon and Algicon Mint, 120ml of the product was taken and added to a 250ml tall-form beaker.

Landscapes

  • Health & Medical Sciences (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Produit pharmaceutique pour le traitement du reflux gastro-oesophagien, de la gastrite ou de l'ulcère gastro-duodénal, se présentant sous la forme d'une gélule de gélatine souple que l'on peut mastiquer, l'intérieur de cette gélule comprenant: (a) un matériau polymère choisi parmi un acide alginique, des alginates, une pectine, du xanthane, du gellane, de la carraghénane et des mélanges de ces substances; (b) un sel carbonaté ou bicarbonaté; (c) un véhicule liquide à base d'huile ou à base hydrophile; l'ingestion orale de cette gélule par un patient provoque la rupture de l'enveloppe gélatineuse de la gélule et les substances contenues peuvent réagir avec les substances acides contenues dans l'estomac afin de produire une barrière gélatineuse carbonée flottante de consistance spécifiée.
EP94931124A 1993-10-29 1994-10-28 Substance a pouvoir moussant garnissant une gelule de gelatine Withdrawn EP0725626A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB939322314A GB9322314D0 (en) 1993-10-29 1993-10-29 Foam generating capsules
GB9322314 1993-10-29
GB9411350 1994-06-07
GB9411350A GB2283171B (en) 1993-10-29 1994-06-07 Pharmaceutical products
PCT/GB1994/002380 WO1995011668A1 (fr) 1993-10-29 1994-10-28 Substance a pouvoir moussant garnissant une gelule de gelatine

Publications (1)

Publication Number Publication Date
EP0725626A1 true EP0725626A1 (fr) 1996-08-14

Family

ID=26303761

Family Applications (1)

Application Number Title Priority Date Filing Date
EP94931124A Withdrawn EP0725626A1 (fr) 1993-10-29 1994-10-28 Substance a pouvoir moussant garnissant une gelule de gelatine

Country Status (9)

Country Link
EP (1) EP0725626A1 (fr)
JP (1) JPH09504286A (fr)
CN (1) CN1133558A (fr)
AU (1) AU8000494A (fr)
BR (1) BR9407916A (fr)
CA (1) CA2174777A1 (fr)
NO (1) NO961638D0 (fr)
NZ (1) NZ274901A (fr)
WO (1) WO1995011668A1 (fr)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3959192B2 (ja) * 1998-12-03 2007-08-15 株式会社大塚製薬工場 経管栄養食品
SE0103722D0 (sv) * 2001-10-30 2001-10-30 Astrazeneca Ab Novel formulation
GB2384986B (en) * 2002-02-12 2004-01-07 Reckitt Benckiser Healthcare Compositions for the treatment of disorders of the upper gastrointestinal tract
US8293270B2 (en) * 2005-10-26 2012-10-23 Banner Pharmacaps, Inc. Lipophilic vehicle-based dual controlled release matrix system
KR100919508B1 (ko) * 2007-08-14 2009-09-28 강원대학교산학협력단 매트릭스에 칼슘 카보네이트를 함유한 알지네이트 입자 및그 제조방법
GB0814376D0 (en) * 2008-08-06 2008-09-10 Reckitt Benckiser Healthcare Formulation
KR20130091250A (ko) * 2010-04-23 2013-08-16 에스-바이오텍 홀딩 에이피에스 위산 중화용 고체 약학 조성물
ITUB20156821A1 (it) * 2015-12-09 2017-06-09 Altergon Sa CAPSULE DI GELATINA MOLLE A RILASCIO pH INDIPENDENTE
FR3071728B1 (fr) * 2017-09-29 2019-09-27 Laboratoires Arkopharma Composition adaptee pour former un radeau gastrique gelifie
IL312094A (en) * 2018-03-02 2024-06-01 Pharagen Llc Formulations treating acid reflux comprising sodium alginate
CN110353271B (zh) * 2019-06-13 2022-07-22 陕西科技大学 一种抑制食道反流的特殊医学食品增稠组件及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH630257A5 (en) * 1975-03-17 1982-06-15 Hoffmann La Roche Sustained release formulation
CH652025A5 (de) * 1981-09-14 1985-10-31 Hoffmann La Roche Pharmazeutisches praeparat.
NZ230701A (en) * 1988-09-20 1992-01-29 Glaxo Group Ltd Pharmaceutical compositions comprising ranitidine, alginic acid and a carbonate or bicarbonate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9511668A1 *

Also Published As

Publication number Publication date
NO961638L (no) 1996-04-24
WO1995011668A1 (fr) 1995-05-04
CA2174777A1 (fr) 1995-05-04
AU8000494A (en) 1995-05-22
NZ274901A (en) 1997-03-24
BR9407916A (pt) 1996-11-26
CN1133558A (zh) 1996-10-16
NO961638D0 (no) 1996-04-24
JPH09504286A (ja) 1997-04-28

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