IE68933B1 - Pharmaceutical preparation - Google Patents
Pharmaceutical preparationInfo
- Publication number
- IE68933B1 IE68933B1 IE921734A IE921734A IE68933B1 IE 68933 B1 IE68933 B1 IE 68933B1 IE 921734 A IE921734 A IE 921734A IE 921734 A IE921734 A IE 921734A IE 68933 B1 IE68933 B1 IE 68933B1
- Authority
- IE
- Ireland
- Prior art keywords
- preparation
- asa
- enema
- suspension
- weight
- Prior art date
Links
- 239000000825 pharmaceutical preparation Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 claims description 18
- KBOPZPXVLCULAV-UHFFFAOYSA-N mesalamine Chemical compound NC1=CC=C(O)C(C(O)=O)=C1 KBOPZPXVLCULAV-UHFFFAOYSA-N 0.000 claims description 16
- 229960004963 mesalazine Drugs 0.000 claims description 16
- 239000000725 suspension Substances 0.000 claims description 16
- 241000792859 Enema Species 0.000 claims description 11
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims description 11
- 239000007920 enema Substances 0.000 claims description 11
- 229940095399 enema Drugs 0.000 claims description 11
- 239000004408 titanium dioxide Substances 0.000 claims description 6
- 239000003963 antioxidant agent Substances 0.000 claims description 5
- 239000000126 substance Substances 0.000 claims description 5
- 239000002738 chelating agent Substances 0.000 claims description 4
- 239000000872 buffer Substances 0.000 claims description 2
- 239000003755 preservative agent Substances 0.000 claims description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 239000001301 oxygen Substances 0.000 description 4
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 229940071106 ethylenediaminetetraacetate Drugs 0.000 description 3
- 230000007717 exclusion Effects 0.000 description 3
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 2
- 239000004698 Polyethylene Substances 0.000 description 2
- 229960004909 aminosalicylic acid Drugs 0.000 description 2
- 230000003078 antioxidant effect Effects 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229920000573 polyethylene Polymers 0.000 description 2
- 239000005711 Benzoic acid Substances 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- PECIXCWDKCWSTQ-UHFFFAOYSA-N benzoic acid oxygen(2-) titanium(4+) Chemical compound C(C1=CC=CC=C1)(=O)O.[O-2].[O-2].[Ti+4] PECIXCWDKCWSTQ-UHFFFAOYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-ZSJDYOACSA-N heavy water Substances [2H]O[2H] XLYOFNOQVPJJNP-ZSJDYOACSA-N 0.000 description 1
- 239000007970 homogeneous dispersion Substances 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 208000028774 intestinal disease Diseases 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 231100000915 pathological change Toxicity 0.000 description 1
- 230000036285 pathological change Effects 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- -1 polyethylene Polymers 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 229940037001 sodium edetate Drugs 0.000 description 1
- LDTLADDKFLAYJA-UHFFFAOYSA-L sodium metabisulphite Chemical compound [Na+].[Na+].[O-]S(=O)OS([O-])=O LDTLADDKFLAYJA-UHFFFAOYSA-L 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Description
Technical Field The invention relates to an enema preparation for 5aminosalicylic acid. g£ig.r Art -Aminosalicylic acid (5-ASA) is a known active compound which is employed, in particular, for the treatment of inflammatory intestinal disorders, such as ulcerative colitis. The administration of 5-ASA as an enema preparation is particularly convenient, since the active principle can hereby be brought directly to the site of the pathological changes. In these preparations, however, the known chemical instability of 5-ASA in solutions or suspensions presents considerable difficulties. In the past, various paths were followed to get to grips, in particular, with the light and oxygen sensitivity of 5-ASA.
US Patent 4,657,900 thus proposes an enema preparation in which highly pure 5-ASA is present as an aqueous suspension which, after preparation with exclusion of oxygen and addition of bisulphite as an antioxidant, is sealed into an opaque polyethylene rectal applicator which, for its part, is heatsealed into a polyester/aluminum film/polyethylene bag.
US Patent 4,664,256 discloses a very similar administration form in which, apart from bisulphite, a chelating agent, such - 2 as e.g. ethylenediaminetetraacetate (EDTA) is additionally contained as an antioxidant.
The problem of instability in enema preparations is apparently reasonably solved by these measures.
Apart from the expensive packing in the case of the 5-ASA enema preparations according to the prior art, the preparations, however, exhibit problems which have to do with the resuspendibility of the 5-ASA suspension before use. The known preparations must be shaken very vigorously and persistently, especially before use, in order to achieve a homogeneous dispersion of the active compound which is desirable for administration. It goes without saying that this laborious resuspension is only managed inadequately, in particular by infirm patients and on the whole is not conducive to patient compliance.
Description of the invention It has now surprisingly been found that 5-ASA enema preparations according to the prior art can be improved in numerous respects by the addition of titanium dioxide. The light and oxidation stability of 5-ASA suspensions is increased by this addition according to the invention to such an extent that it is no longer necessary to make the 5-ASA suspension available in a double-walled container. A further advantage is that the stability of the suspension is increased such that the tiresome resuspension before administration by shaking can foe dispensed with.
The invention therefore relates to an aqueous 5-aminosalicylic acid enema suspension preparation, which comprises titanium dioxide in addition to the customary auxiliaries.
Customary auxiliaries are understood as meaning those auxiliaries which are customarily employed for suspensions and those which can be used for the stabilisation of 5-ASA suspensions. The first group includes e.g. the customary viscosity-enhancing substances, preservatives, such as e.g. benzoic acid, pH-regulating substances, such as buffers, chelating agents, such as e.g. EDTA, and antioxidants, such as, in particular, the bisulphites customary in 5-ASA preparations .
Titanium dioxide is added according to the invention in an amount of from 0.1 to 3, preferably 0.1 to 1, and, in particular, 0.5% by weight.
-ASA is contained in the suspensions according to the invention in an amount of from 0.5 to 10, preferably 2 to 6, and, in particular, about 4% by weight.
Bisulphites as antioxidants are contained in the suspensions according to the invention in an amount of from 0.05 to 0.5, preferably 0.1 to 0.2, and, in particular, about 0.15% by weight.
Viscosity-enhancing substances are contained in the suspensions according to the invention in an amount of from 0.05 to 2, preferably 0.1 to 1, and, in particular, about 0.5% by weight.
Chelating agents are contained in the suspension according to 25 the invention in an amount of from 0.01 to 0.5. preferably 0.05 to 0.2, and in particular, about 0.1% by weight.
The suspension according to the invention is prepared according to the processes known from the prior art with the exclusion of oxygen. The finished suspension is then packed with exclusion of oxygen in customary flexible enema applicators, which are preferably manufactured from opaque plastic.
Preparation iexample V, A suspension is prepared according to the customary processes 5 and packed in enema containers which, per 50 g enema pack, contain the following constituentss -aminosalicylic acid sodium dihydrogen phosphate x 2H2O sodium edetate benzoic acid titanium dioxide E 171 sodium disulphite xanthan gum sodium hydroxide solution 10 M purified water 2.000 g 0.500 g 0.050 g 0.100 g 0.250 g 0.075 g 0.250 g (to pH 4.0) to 50.00 g
Claims (5)
1. An aqueous 5-aminosalicylic acid enema suspension preparation, which comprises titanium dioxide in addition to customary auxiliaries.
2. The preparation as claimed in claim 1, which contains 0.1 to 3% by weight of titanium dioxide.
3. The preparation as claimed in claim 1, which contains 5aminosalicylic acid in an amount of from 0.5 to 10% by weight.
4. The preparation as claimed in claim 1, which, as auxiliaries, contains viscosity-enhancing substances, preservatives, chelating agents, buffers and antioxidants .
5. A preparation substantially as hereinbefore described with reference to the Examples.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH169091 | 1991-06-07 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IE921734A1 IE921734A1 (en) | 1992-12-16 |
| IE68933B1 true IE68933B1 (en) | 1996-07-24 |
Family
ID=4216334
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IE921734A IE68933B1 (en) | 1991-06-07 | 1992-05-29 | Pharmaceutical preparation |
Country Status (3)
| Country | Link |
|---|---|
| IE (1) | IE68933B1 (en) |
| RU (1) | RU2086241C1 (en) |
| ZA (1) | ZA924111B (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5498608A (en) * | 1994-01-07 | 1996-03-12 | Salix Pharmaceuticals | Use of 2-hydroxy-5-phenylazobenzoic acid derivatives as colon cancer chemopreventative and chemotherapeutic agents |
| RU2155585C2 (en) * | 1998-03-13 | 2000-09-10 | Пятигорская государственная фармацевтическая академия | Medicinal form for children showing anti-inflammatory and antipyretic effect |
| RU2286156C2 (en) * | 2001-10-15 | 2006-10-27 | Ферринг Бв | Method for production of pharmaceutical composition containing 5-aminosalicylic acid useful in treatment of non-specific ulcerative colitis and cron's disease |
-
1992
- 1992-05-29 IE IE921734A patent/IE68933B1/en not_active IP Right Cessation
- 1992-06-05 ZA ZA924111A patent/ZA924111B/en unknown
- 1992-06-05 RU RU9293058458A patent/RU2086241C1/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA924111B (en) | 1993-11-15 |
| RU2086241C1 (en) | 1997-08-10 |
| IE921734A1 (en) | 1992-12-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Patent lapsed |