CA1236773A - Sucralfate suspension - Google Patents
Sucralfate suspensionInfo
- Publication number
- CA1236773A CA1236773A CA000467594A CA467594A CA1236773A CA 1236773 A CA1236773 A CA 1236773A CA 000467594 A CA000467594 A CA 000467594A CA 467594 A CA467594 A CA 467594A CA 1236773 A CA1236773 A CA 1236773A
- Authority
- CA
- Canada
- Prior art keywords
- sucralfate
- weight
- suspensions
- xanthan gum
- pharmaceutical
- 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.)
- Expired
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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
Abstract
Abstract The invention relates to formulations in the form of suspensions containing sucralfate, characterised in that they contain, based on the sucralfate, 1-5% by weight of xanthan gum and 1-12.5% by weight of at least one peptiser.
Description
Sucralfate Suspension The invention relates to pharmaceutical formu-lations in the form of suspensions containing sucralfate as the pharmaceutical active compound.
Sucralfate (Ulcogant(R)) ;s a basic alum;nium sucrose sulfate. It is known from German Offenlegungs-schrift 1,568,346 and is used in human medicine for relieving the symptoms of gastric and duodenal ulcers and for accelerating the healing of ulcers. An advan-tageous act;on of sucralfate in combating emesis and/or diarrhoea in veterinary medicine has moreover been des cribed in German Patent Application P 3,322,078.
The action of sucralfate is characterised by pepsin-binding and antacid effects. Sucralfate, which is tolerated very well, displays its action in the acid medium of the digestive tract, in particular at pH
values below 4, where it lines the mucous membranes of the stomach and duodenum with a protective coating. As a result of its preferential binding affinity for areas of the mucous membrane which have been attacked, in-creased protection and accelerated healing of ulcers aswell as regeneration of the mucous membrane and its functions occur there.
Formulations containing sucralfate have hitherto usually been employed only in the form of solid adminis-tration forms, such as tablets, granules or powders.However, liquid formulations, -for example in the form of suspensions, would be advantageous for the particular mode of action of sucralfate, especially in view of a rapid and complete lining of the mucous membranes in the digestive tract. It is indeed possible to suspend the commercially available solid administration forms, for example in water, before use and to take them in this form~ However, this proves to be inconvenient and is frequently found to be unpleasant in taste for the pati-ent taking the medicament, and is thus not very practic-able. Attempts to prepare sucralfate-containing finished medicaments in the form of suspensions have hitherto failed, since no suspensions which are stable ~,3~ 7 for a prolonged period could be obtained with the cus~o-mary auxil;aries. In such suspensions, the solid sedi-mented out after a short time and formed lumps to such an extent that in some cases it could not be shaken up again.
The invent;on was thus based on the object of discovering a method of stabil;sing pharmaceutical formulations in the form of suspensions containing suc-ralfate, and a corresponding stable formulation as the f;n;shed medicament.
For the formulation of pharmaceutical suspen-s;ons, attempts are made to prevent sedimentation of the suspended particles, or at least to keep the sed;ment-at;on as low as possible, by suitable additives. This is to ensure that the agent remains homogeneous and can be used appropriately even after prolonged storage. If sedimentation nevertheless takes place in the course of time, it should be ensured that the solid can readily be shaken up. Moreover, suspensions for oral use should be g;ven, as far as possible, a pleasant or at least neut-ral taste. In particular, .he solid content should beincorporated such that this or the solid particles are not found to be troublesome when the suspens;on is taken. In the case of aqueous suspensions, the proper-ties mentioned can usually be achieved by adding liquids which increase the viscosity, such as glycerol, propane-diol, sorb;tol solution and/or liquid polyethylene gly-cols, and by ;ncorporat;ng suspending agents and thick-eners~ Agents of th;s type wh;ch ;ncrease the v;scosity and prevent sedimentation of the solid particles are usually high molecular weight cellulose derivatives or polysaccharide gums, such as, for example, carboxy-methylcelluloses, methylcelluloses, alginates or traga-canth.
Numerous attempts have been made, with only little or no success, to achieve the object of develop-ing a stable sucralfate susp~ension which does not sedi-ment. For this, the essential familiar suspending agents and thickeners customary in the technology of pharmaceutical suspensions and corresponding auxiliaries ~3~73 ancl additives were tested. It was found that, evidently due to the property of the sucralfate of releasing Al3~
ions in an aqueous medium, interactions are induced with v;rtually all the thickening substances, and these some-times lead to drastic decreases or increases in viscos-ity and to precipitation of the thickeners. This means that the sucralfate particles in such suspension formul-at;ons sediment very rapidly, forming lumpy precipitates which deposit and stick to the walls of the packaging material and can no longer be shaken up.
It has been found that, surprisingly, stable formulations can be obtained in the form of suspensions containing sucralfate if 1-5~ by weight of xanthan gum and 1-12.5~o by weight of at least onr- peptiser, based on the content of sucralfate, are added to these formulations.
The invention accordingly relates to pharmaceut-;cal formulations in the form of suspensions containing sucralfate, ~hich have a content~ based on the sucral-fate, of 1-5X by weight of xanthan gum and 1-12.5% by ~0 weight of at least ore peptiser.
The invention particularly reLates to such a pharmaceutical formulation in which the peptiser is at least one salt of phosphoric acidand/or citric acid.
The invention moreover relates to a method of stabilising pharmaceutical formulations in the form of suspensions containing sucralfate, 1-5% by weight of xanthan gum and 1-12.5~ by weight of at least one peptiser, bclsecl on the conterlt oF sucralFate, being adcled to thesr ForllluLations S(l Xanthlll guln L5 a hiqh moLecllla[ \ueight polysaccl-lcl-ricle which carl be obtained by Fermentltiorl oF carbohydratrs wLtl1 pseudolllonas microL)es, partlcuLarly with XarltL1omonas canlF)es-tris, and is usually in the form of its alkali metal and/or alkaline earth metal salts. It is known that xanthan gum, inter alia, can also be used as a suspend-ing agent and thickener for pharmaceutical and cosmetic products (see H.P. Fiedler, Lexikon der Hilfsstoffe ~Lexicon of Auxiliaries), page 1016, 2nd edition (1981) or The United States Pharmacopeia, Twentieth Revision (1~80)). Thus, for example, a basic aluminiurn salt of xanthan gurn is also known as a pharmac~u~icat excipient, as well as the use thereof as a suspending agent for barium sulfate in radiographic contrast media (compare Chemical Abstracts 79 (1973) 23582m and 81 (1973) ~6461x). On the other hand, however, xanthan gum is used for flocculating metal oxicles, hydroxides, carbonates, in par-ticular of alurninium, from suspensions (Chemical Abstracts 9~ (1981) 52786w, 95 (1981) 12692b and 96 L~ (1982) 24726z). From the prior art, it could thus not be assumed that xanthan gum is generally suitabLe for stabilising pharmaceutical suspensions containing suc-ralfate. Rather, it was found in the numerous experi-ments carried out that a satisfactory solution of the problem was hardly to be seen in xanthan gum, as in all the other usual thickeners, even in combination with other au~iliaries and addit;ves customary in the techno-logy of pharmaceutical suspensions.
The result that a combination of the medicinal substance sucralfate, the thickener xanthan gum and at least one peptiser leads to a stable sucralfate suspension which fulfils the requirements of galenics and of medicinal use in an outstanding manner if the amounts in the com-position are chosen according to the invention was all the more surprising.
The sucralfate used for the preparation of the sucralfate suspensions accordiny to the invention is a familiar pharmaceutical active compound and is used here, preFerabLy, ir-l the Finely grouncl Forrn with a partlcle si7e oF
S[) t~r?Lou/ 50 ~rll.
rhe xanthan gum usecl, accorclirlg to the Ln~entlon, ~:1'3 the suspencling agent ancl thickener can be preparecl on an industrial scale by fermentation processes and is commercially available in accordance with the quality specifications of the pharmacopoeias of various countries.
The peptisers to be added, according to the invention, to the suspension are salts of inorganic or ~;~3~i73 organic acids, which are intended to ensure that the high molecular we;ght add;t;ve xanthan gum remains in the sol state, that i5 to say in homogeneous distrib-ution, in disperse systems such as the present suspen-sions, and does not separate out by gel formation.
These peptisers can be, for example, physiologically acceptable salts of phosphoric acid, citric acid or other tribasic acids. Salts of phosphoric acid and cit-ric acid are particularly suitable here. Sodium di hydrogen phosphate ;s particularly preferred.
According to the invention, 1-5X by weight of xanthan gum and 1-12.5% by weight of at l~ast one peptiser, basecl on the content of sucralfate, are added to the sucralfate suspensions for effective, permanent stabilisation. The content of sucralfate in these formulations can vary within wide limits.
As a rule, such suspensions can contain 1-40% by weight of sucralfate, based on the total amount. Typi-cal formulations of sucralfate suspensions according to the invention contair, based on the total amount, 1-40%
by weight, preferably 10-25X by weight, of sucralfate, 0.01-2% by weight, preferably 0.1-1% by we;ght, of xan-than gum and 0.01-5% by weight, preferably 0.1-3% by weight, of peptiser. Besides water as the liquid med-ium, the suspensions according to the invention can alsocontain liquids which increase the viscosity, preferably glycerol or propanediol, in an amount of 1-50% by weight~ preferably 10-20% by weight. Moreover, the add-ition of other auxiliaries and additives customary in the technology of pharmaceutical suspensions is pos-s;ble. These chiefly include preservatives, such as, for example, sodium methyl-4-hydroxybenzoate and sodium propyl-4-hydroxybenzoate, which are added together or ind;vidually ;n the usual concentrat;ons of, for ex-ample, about 0.1% by weight. Flavour-improving aromas, sweeteners and flavour correctants can also be added.
Additives of this type as a rule scarcely exceed a con-tent of 1X by weight, based on the total amount. Other active compounds can also be added to the sucralfate ~L~3~ 7 ~3 suspensions according to the invention, for example those with which it is known that sucralfate can be com-bined, such as, for example, antacids, spasmolytics, antiflatulents, H2-receptor blockers, non-steroid anti-rheumatics and generally acid secretion-inhibiting drugs. These also include those aminoacids described in European Patent A1-0,107,209 which intens;fy the effect of sucralfate in lining the mucous membrane or wh;ch are to retain this effect in the case of adverse storage condi-t;ons of correspond;ng products.
The sucralfate suspensions according to theinvention are prepared in a manner which is known per se, by mi~ing the components and homogenising. They can then be filled into the customary means of packaging for pharmaceutical suspensions, such as~ for example, bottles, drinking ampoules or portion packs for oral or rectal administration. The active compound remains sus-pended for a storage time of any desired length, without sedimenting irreversibly and without forming lumps or 2û precipitating on the walls of the vessel.
The medical field of application of the sucral-fate suspensions according to the invention is com-pletely analogous to that for the known administration forms containing sucralfate as the active compound, in particular protection and healing of mucous membranes which have been attacked in the digestive tract in humans, in particular relief of symptoms and healing in cases of gastric and duodenal ulcers. However, the agent can also be advantageously used in veterinary medic;ne for combating emesis and/or diarrhoea. For corresponding treatments, the suspension is usually administered orally in a dosage analogous to the known administration forms of sucralfate. If appropriate, however, such suspensions can also be administered rec-tally. This is a particular advantage of the sucralfatesuspensions according to the invention, since this type of use was virtually impossible with the previously known forms of administration.
7~
Example 1 5 ml. of a suspension for oral application with a content of 20~o by weight of sucralfate contain:
sucralfate 1.118 9 S Nall2P04 O.û3 9 xanthan gurn 0.02 9 glycerol 5.00 9 methyl 4-hydroxybenzoate, Na salt 0.00259 propyl 4-hydroxybenzoate, Na salt 0.00259 flavour correctantsq. s.
water ad 5.0 ml.
Example 2 100 ml. of a suspension for rectal application with a content ~f 10,o by weight of sucralfate contain:
sucralfate 11.18 9 Nall2P0~ 0.40 9 xanthan gum 0.19 9 Z() glycerol 10.00 9 rmethyL 4-hyclroxybenzoate, Na salt 0.05 9 propyL 4-hydroxybenzoate, Na salt 0.05 9 water ad 100 ml.
Sucralfate (Ulcogant(R)) ;s a basic alum;nium sucrose sulfate. It is known from German Offenlegungs-schrift 1,568,346 and is used in human medicine for relieving the symptoms of gastric and duodenal ulcers and for accelerating the healing of ulcers. An advan-tageous act;on of sucralfate in combating emesis and/or diarrhoea in veterinary medicine has moreover been des cribed in German Patent Application P 3,322,078.
The action of sucralfate is characterised by pepsin-binding and antacid effects. Sucralfate, which is tolerated very well, displays its action in the acid medium of the digestive tract, in particular at pH
values below 4, where it lines the mucous membranes of the stomach and duodenum with a protective coating. As a result of its preferential binding affinity for areas of the mucous membrane which have been attacked, in-creased protection and accelerated healing of ulcers aswell as regeneration of the mucous membrane and its functions occur there.
Formulations containing sucralfate have hitherto usually been employed only in the form of solid adminis-tration forms, such as tablets, granules or powders.However, liquid formulations, -for example in the form of suspensions, would be advantageous for the particular mode of action of sucralfate, especially in view of a rapid and complete lining of the mucous membranes in the digestive tract. It is indeed possible to suspend the commercially available solid administration forms, for example in water, before use and to take them in this form~ However, this proves to be inconvenient and is frequently found to be unpleasant in taste for the pati-ent taking the medicament, and is thus not very practic-able. Attempts to prepare sucralfate-containing finished medicaments in the form of suspensions have hitherto failed, since no suspensions which are stable ~,3~ 7 for a prolonged period could be obtained with the cus~o-mary auxil;aries. In such suspensions, the solid sedi-mented out after a short time and formed lumps to such an extent that in some cases it could not be shaken up again.
The invent;on was thus based on the object of discovering a method of stabil;sing pharmaceutical formulations in the form of suspensions containing suc-ralfate, and a corresponding stable formulation as the f;n;shed medicament.
For the formulation of pharmaceutical suspen-s;ons, attempts are made to prevent sedimentation of the suspended particles, or at least to keep the sed;ment-at;on as low as possible, by suitable additives. This is to ensure that the agent remains homogeneous and can be used appropriately even after prolonged storage. If sedimentation nevertheless takes place in the course of time, it should be ensured that the solid can readily be shaken up. Moreover, suspensions for oral use should be g;ven, as far as possible, a pleasant or at least neut-ral taste. In particular, .he solid content should beincorporated such that this or the solid particles are not found to be troublesome when the suspens;on is taken. In the case of aqueous suspensions, the proper-ties mentioned can usually be achieved by adding liquids which increase the viscosity, such as glycerol, propane-diol, sorb;tol solution and/or liquid polyethylene gly-cols, and by ;ncorporat;ng suspending agents and thick-eners~ Agents of th;s type wh;ch ;ncrease the v;scosity and prevent sedimentation of the solid particles are usually high molecular weight cellulose derivatives or polysaccharide gums, such as, for example, carboxy-methylcelluloses, methylcelluloses, alginates or traga-canth.
Numerous attempts have been made, with only little or no success, to achieve the object of develop-ing a stable sucralfate susp~ension which does not sedi-ment. For this, the essential familiar suspending agents and thickeners customary in the technology of pharmaceutical suspensions and corresponding auxiliaries ~3~73 ancl additives were tested. It was found that, evidently due to the property of the sucralfate of releasing Al3~
ions in an aqueous medium, interactions are induced with v;rtually all the thickening substances, and these some-times lead to drastic decreases or increases in viscos-ity and to precipitation of the thickeners. This means that the sucralfate particles in such suspension formul-at;ons sediment very rapidly, forming lumpy precipitates which deposit and stick to the walls of the packaging material and can no longer be shaken up.
It has been found that, surprisingly, stable formulations can be obtained in the form of suspensions containing sucralfate if 1-5~ by weight of xanthan gum and 1-12.5~o by weight of at least onr- peptiser, based on the content of sucralfate, are added to these formulations.
The invention accordingly relates to pharmaceut-;cal formulations in the form of suspensions containing sucralfate, ~hich have a content~ based on the sucral-fate, of 1-5X by weight of xanthan gum and 1-12.5% by ~0 weight of at least ore peptiser.
The invention particularly reLates to such a pharmaceutical formulation in which the peptiser is at least one salt of phosphoric acidand/or citric acid.
The invention moreover relates to a method of stabilising pharmaceutical formulations in the form of suspensions containing sucralfate, 1-5% by weight of xanthan gum and 1-12.5~ by weight of at least one peptiser, bclsecl on the conterlt oF sucralFate, being adcled to thesr ForllluLations S(l Xanthlll guln L5 a hiqh moLecllla[ \ueight polysaccl-lcl-ricle which carl be obtained by Fermentltiorl oF carbohydratrs wLtl1 pseudolllonas microL)es, partlcuLarly with XarltL1omonas canlF)es-tris, and is usually in the form of its alkali metal and/or alkaline earth metal salts. It is known that xanthan gum, inter alia, can also be used as a suspend-ing agent and thickener for pharmaceutical and cosmetic products (see H.P. Fiedler, Lexikon der Hilfsstoffe ~Lexicon of Auxiliaries), page 1016, 2nd edition (1981) or The United States Pharmacopeia, Twentieth Revision (1~80)). Thus, for example, a basic aluminiurn salt of xanthan gurn is also known as a pharmac~u~icat excipient, as well as the use thereof as a suspending agent for barium sulfate in radiographic contrast media (compare Chemical Abstracts 79 (1973) 23582m and 81 (1973) ~6461x). On the other hand, however, xanthan gum is used for flocculating metal oxicles, hydroxides, carbonates, in par-ticular of alurninium, from suspensions (Chemical Abstracts 9~ (1981) 52786w, 95 (1981) 12692b and 96 L~ (1982) 24726z). From the prior art, it could thus not be assumed that xanthan gum is generally suitabLe for stabilising pharmaceutical suspensions containing suc-ralfate. Rather, it was found in the numerous experi-ments carried out that a satisfactory solution of the problem was hardly to be seen in xanthan gum, as in all the other usual thickeners, even in combination with other au~iliaries and addit;ves customary in the techno-logy of pharmaceutical suspensions.
The result that a combination of the medicinal substance sucralfate, the thickener xanthan gum and at least one peptiser leads to a stable sucralfate suspension which fulfils the requirements of galenics and of medicinal use in an outstanding manner if the amounts in the com-position are chosen according to the invention was all the more surprising.
The sucralfate used for the preparation of the sucralfate suspensions accordiny to the invention is a familiar pharmaceutical active compound and is used here, preFerabLy, ir-l the Finely grouncl Forrn with a partlcle si7e oF
S[) t~r?Lou/ 50 ~rll.
rhe xanthan gum usecl, accorclirlg to the Ln~entlon, ~:1'3 the suspencling agent ancl thickener can be preparecl on an industrial scale by fermentation processes and is commercially available in accordance with the quality specifications of the pharmacopoeias of various countries.
The peptisers to be added, according to the invention, to the suspension are salts of inorganic or ~;~3~i73 organic acids, which are intended to ensure that the high molecular we;ght add;t;ve xanthan gum remains in the sol state, that i5 to say in homogeneous distrib-ution, in disperse systems such as the present suspen-sions, and does not separate out by gel formation.
These peptisers can be, for example, physiologically acceptable salts of phosphoric acid, citric acid or other tribasic acids. Salts of phosphoric acid and cit-ric acid are particularly suitable here. Sodium di hydrogen phosphate ;s particularly preferred.
According to the invention, 1-5X by weight of xanthan gum and 1-12.5% by weight of at l~ast one peptiser, basecl on the content of sucralfate, are added to the sucralfate suspensions for effective, permanent stabilisation. The content of sucralfate in these formulations can vary within wide limits.
As a rule, such suspensions can contain 1-40% by weight of sucralfate, based on the total amount. Typi-cal formulations of sucralfate suspensions according to the invention contair, based on the total amount, 1-40%
by weight, preferably 10-25X by weight, of sucralfate, 0.01-2% by weight, preferably 0.1-1% by we;ght, of xan-than gum and 0.01-5% by weight, preferably 0.1-3% by weight, of peptiser. Besides water as the liquid med-ium, the suspensions according to the invention can alsocontain liquids which increase the viscosity, preferably glycerol or propanediol, in an amount of 1-50% by weight~ preferably 10-20% by weight. Moreover, the add-ition of other auxiliaries and additives customary in the technology of pharmaceutical suspensions is pos-s;ble. These chiefly include preservatives, such as, for example, sodium methyl-4-hydroxybenzoate and sodium propyl-4-hydroxybenzoate, which are added together or ind;vidually ;n the usual concentrat;ons of, for ex-ample, about 0.1% by weight. Flavour-improving aromas, sweeteners and flavour correctants can also be added.
Additives of this type as a rule scarcely exceed a con-tent of 1X by weight, based on the total amount. Other active compounds can also be added to the sucralfate ~L~3~ 7 ~3 suspensions according to the invention, for example those with which it is known that sucralfate can be com-bined, such as, for example, antacids, spasmolytics, antiflatulents, H2-receptor blockers, non-steroid anti-rheumatics and generally acid secretion-inhibiting drugs. These also include those aminoacids described in European Patent A1-0,107,209 which intens;fy the effect of sucralfate in lining the mucous membrane or wh;ch are to retain this effect in the case of adverse storage condi-t;ons of correspond;ng products.
The sucralfate suspensions according to theinvention are prepared in a manner which is known per se, by mi~ing the components and homogenising. They can then be filled into the customary means of packaging for pharmaceutical suspensions, such as~ for example, bottles, drinking ampoules or portion packs for oral or rectal administration. The active compound remains sus-pended for a storage time of any desired length, without sedimenting irreversibly and without forming lumps or 2û precipitating on the walls of the vessel.
The medical field of application of the sucral-fate suspensions according to the invention is com-pletely analogous to that for the known administration forms containing sucralfate as the active compound, in particular protection and healing of mucous membranes which have been attacked in the digestive tract in humans, in particular relief of symptoms and healing in cases of gastric and duodenal ulcers. However, the agent can also be advantageously used in veterinary medic;ne for combating emesis and/or diarrhoea. For corresponding treatments, the suspension is usually administered orally in a dosage analogous to the known administration forms of sucralfate. If appropriate, however, such suspensions can also be administered rec-tally. This is a particular advantage of the sucralfatesuspensions according to the invention, since this type of use was virtually impossible with the previously known forms of administration.
7~
Example 1 5 ml. of a suspension for oral application with a content of 20~o by weight of sucralfate contain:
sucralfate 1.118 9 S Nall2P04 O.û3 9 xanthan gurn 0.02 9 glycerol 5.00 9 methyl 4-hydroxybenzoate, Na salt 0.00259 propyl 4-hydroxybenzoate, Na salt 0.00259 flavour correctantsq. s.
water ad 5.0 ml.
Example 2 100 ml. of a suspension for rectal application with a content ~f 10,o by weight of sucralfate contain:
sucralfate 11.18 9 Nall2P0~ 0.40 9 xanthan gum 0.19 9 Z() glycerol 10.00 9 rmethyL 4-hyclroxybenzoate, Na salt 0.05 9 propyL 4-hydroxybenzoate, Na salt 0.05 9 water ad 100 ml.
Claims (4)
1. Pharmaceutical formulations in the form of sus-pensions containing sucralfate, characterised in that they contain, based on the sucralfate, 1-5% by weight of xanthan gum and 1-12.5% by weight of at least one peptiser.
2. Pharmaceutical formulations according to Claim 1, characterised in that the peptiser is at least one salt of phosphoric acid and/or citric acid.
3. Pharmaceutical formulations according to Claim 1 or 2, characterised in that they contain 1-40% by weight of sucralfate, based on the total amount.
4. Method of stabilising pharmaceutical formul-ations in the form of suspensions containing sucralfate, characterised in that 1-5% by weight of xanthan gum and 1-12.5% by weight of peptiser, based on the content of sucralfate, are added to these formulations.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19843430809 DE3430809A1 (en) | 1984-08-22 | 1984-08-22 | SUCRALFAT SUSPENSION |
| DE3430809.1 | 1984-08-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1236773A true CA1236773A (en) | 1988-05-17 |
Family
ID=6243590
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000467594A Expired CA1236773A (en) | 1984-08-22 | 1984-11-13 | Sucralfate suspension |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US4885281A (en) |
| EP (1) | EP0192640B1 (en) |
| JP (1) | JPS61503031A (en) |
| CN (1) | CN85109551A (en) |
| AT (1) | ATE41308T1 (en) |
| AU (1) | AU567257B2 (en) |
| CA (1) | CA1236773A (en) |
| DE (2) | DE3430809A1 (en) |
| DK (1) | DK164479C (en) |
| ES (1) | ES537578A0 (en) |
| FI (1) | FI80592C (en) |
| GR (1) | GR852023B (en) |
| HK (1) | HK62889A (en) |
| IE (1) | IE58201B1 (en) |
| IL (1) | IL76138A (en) |
| IN (1) | IN164763B (en) |
| IT (1) | IT1178235B (en) |
| NO (1) | NO170126C (en) |
| NZ (1) | NZ213185A (en) |
| PH (1) | PH21250A (en) |
| PT (1) | PT79610A (en) |
| SG (1) | SG35889G (en) |
| SU (1) | SU1544173A3 (en) |
| WO (1) | WO1986001406A1 (en) |
| ZA (1) | ZA848884B (en) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO174085C (en) * | 1986-04-30 | 1994-03-16 | Chugai Pharmaceutical Co Ltd | Process for the preparation of sucralfate preparations |
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| US3692898A (en) * | 1970-11-05 | 1972-09-19 | Sterling Drug Inc | Aqueous magnesium hydroxide suspensions |
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| CA1218601A (en) * | 1983-09-02 | 1987-03-03 | Angel B. Casillan | Sucralfate suspension |
-
1984
- 1984-08-22 DE DE19843430809 patent/DE3430809A1/en not_active Withdrawn
- 1984-09-22 DE DE8484903631T patent/DE3477138D1/en not_active Expired
- 1984-09-22 AT AT84903631T patent/ATE41308T1/en not_active IP Right Cessation
- 1984-09-22 JP JP59503613A patent/JPS61503031A/en active Granted
- 1984-09-22 EP EP84903631A patent/EP0192640B1/en not_active Expired
- 1984-09-22 AU AU34382/84A patent/AU567257B2/en not_active Expired
- 1984-09-22 WO PCT/EP1984/000294 patent/WO1986001406A1/en active IP Right Grant
- 1984-11-12 ES ES537578A patent/ES537578A0/en active Granted
- 1984-11-13 CA CA000467594A patent/CA1236773A/en not_active Expired
- 1984-11-14 ZA ZA848884A patent/ZA848884B/en unknown
- 1984-11-14 IT IT49164/84A patent/IT1178235B/en active
- 1984-12-04 PT PT79610A patent/PT79610A/en unknown
-
1985
- 1985-08-19 IL IL76138A patent/IL76138A/en not_active IP Right Cessation
- 1985-08-21 NZ NZ213185A patent/NZ213185A/en unknown
- 1985-08-21 SU SU853946153A patent/SU1544173A3/en active
- 1985-08-21 PH PH32675A patent/PH21250A/en unknown
- 1985-08-21 GR GR852023A patent/GR852023B/el unknown
- 1985-08-21 IE IE205885A patent/IE58201B1/en not_active IP Right Cessation
- 1985-10-31 IN IN768/CAL/85A patent/IN164763B/en unknown
- 1985-11-15 CN CN198585109551A patent/CN85109551A/en active Pending
-
1986
- 1986-04-18 NO NO86861545A patent/NO170126C/en not_active IP Right Cessation
- 1986-04-21 DK DK183386A patent/DK164479C/en not_active IP Right Cessation
- 1986-04-21 FI FI861674A patent/FI80592C/en not_active IP Right Cessation
-
1988
- 1988-03-21 US US07/171,347 patent/US4885281A/en not_active Expired - Lifetime
-
1989
- 1989-06-07 SG SG358/89A patent/SG35889G/en unknown
- 1989-08-03 HK HK628/89A patent/HK62889A/en not_active IP Right Cessation
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