SE503233C2 - Sucralfate preparation and process for preparing the same - Google Patents
Sucralfate preparation and process for preparing the sameInfo
- Publication number
- SE503233C2 SE503233C2 SE8701787A SE8701787A SE503233C2 SE 503233 C2 SE503233 C2 SE 503233C2 SE 8701787 A SE8701787 A SE 8701787A SE 8701787 A SE8701787 A SE 8701787A SE 503233 C2 SE503233 C2 SE 503233C2
- Authority
- SE
- Sweden
- Prior art keywords
- polyethylene glycol
- sucralfate
- turbidity
- acceleration
- preparing
- Prior art date
Links
Classifications
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
Description
503 233 liggande uppfinnarna funnit att detta syfte kan uppnås genom att blanda sukralfat med polyetylenglykol. Föreliggande upp- finning har fullbordats på basis av detta konstaterande. 503 233 found that this object can be achieved by mixing sucralfate with polyethylene glycol. The present invention has been completed on the basis of this finding.
Figur l och 2 visar profilerna för desintegration och disper- sion av sukralfatberedningar som gjorts i överensstämmelse med föreliggande uppfinning och jämförelseberedningar.Figures 1 and 2 show the profiles for disintegration and dispersion of sucralfate formulations made in accordance with the present invention and comparative formulations.
Enligt föreliggande uppfinning blandas ett sukralfat med 0,l% (vikt/vikt) eller mer polyetylenglykol. Fastän den övre grän- sen för polyetylenglykol inte är kritisk, kan den vanligen användas i en mängd mindre än 50% (vikt/vikt). Molekylvikten för den polyetylenglykol som skall blandas med sukralfatet I begränsas inte till något särskilt värde. När den administre- ras peroralt låter sukralfatberedningen enligt föreliggande uppfinning sukralfatet bli effektivt bundet till det såran- gripna området. Sukralfatberedningen enligt föreliggande uppfinning kan formuleras i olika doseringsformer såsom pulver, fint granulat, granula, tablettgrwgcgnkapslar. För detta ändamål kan olika tillsatsämnen användas såsom binde- medel, sönderdelningsmedel, smörjmedel, konstituens och färgämnen.According to the present invention, a sucralfate is mixed with 0.1% (w / w) or more polyethylene glycol. Although the upper limit for polyethylene glycol is not critical, it can usually be used in an amount of less than 50% (w / w). The molecular weight of the polyethylene glycol to be mixed with the sucralfate I is not limited to any particular value. When administered orally, the sucralfate formulation of the present invention allows the sucralfate to be effectively bound to the wound area. The sucralphate formulation of the present invention may be formulated in various dosage forms such as powders, fine granules, granules, tablet granules. For this purpose, various additives can be used such as binders, disintegrants, lubricants, excipients and dyes.
De följande exemplen avser att ytterligare belysa den före- liggande uppfinningen men får på intet sätt tas som en begränsning.The following examples are intended to further illustrate the present invention but should in no way be taken as a limitation.
Exempel l Ett aluminiumsalt av sackarossulfatester (sukralfat: 3.920 g) blandades omsorgsfullt med 2.000 g av en vattenlösning av 4% polyetylenglykol (molvikt 1.500) i en blandare. Blandningen granulerades i en cylindrisk granulator försedd med ett nät med en maskstorlek på 0,7 mmø. Granulatet torkades vid 60°C under 3 timmar i en torkapparat. Det torkade granulatet sikta- des genom en 16-masksikt för att göra granula. Jämförelse- granula framställdes genom samma metod som beskrivits ovan -503 233 utom att vattenlösningen med 4 procent polyetylenglykol ersattes med vatten.Example 1 An aluminum salt of sucrose sulfate ester (sucralfate: 3,920 g) was carefully mixed with 2,000 g of an aqueous solution of 4% polyethylene glycol (molecular weight 1,500) in a mixer. The mixture was granulated in a cylindrical granulator equipped with a mesh with a mesh size of 0.7 mm 2. The granules were dried at 60 ° C for 3 hours in a dryer. The dried granules were sieved through a 16-mesh sieve to make granules. Comparative granules were prepared by the same method as described above -503 233 except that the aqueous solution with 4 percent polyethylene glycol was replaced with water.
Desintegrations- och dispersionsförmågan hos de två granula- proven visas i figur 1 i form av den förändring i grumligheten som förekom, med värdet hos en kontrollsuspension taget som 1.The disintegration and dispersion capacity of the two granule samples is shown in Figure 1 in the form of the change in turbidity that occurred, with the value of a control suspension taken as 1.
Kontrollsuspensionen framställdes genom att noggrant disperge- ra 1 g av ett sukralfat i 1.000 ml vatten med ultraljudvågor och grumligheten hos denna kontrollsuspension mättes vid 540 nm med skikttjockleken 1 cm i detektorcellen. Mätningen av grumligheten beskrives mer specifikt nedan: suspensioner vardera innehållande 200 mg sukralfat fylldes i fem provrör i en desintegrationsprovapparat (testvätska: 1.000 ml vatten vid 37 i 2°C) och grumligheten hos vätskeproverna tagna omkring 5 cm under testvätskornas yta mättes. Baserade på erhållna data beräknades sedan den specifika grumligheten hos de individu- ella proven.The control suspension was prepared by carefully dispersing 1 g of a sucralfate in 1,000 ml of water with ultrasonic waves and the turbidity of this control suspension was measured at 540 nm with the layer thickness of 1 cm in the detector cell. The measurement of turbidity is described more specifically below: suspensions each containing 200 mg of sucralfate were filled into five test tubes in a disintegration tester (test liquid: 1,000 ml of water at 37 at 2 ° C) and the turbidity of the liquid samples taken about 5 cm below the test liquid surface was measured. Based on the data obtained, the specific turbidity of the individual samples was then calculated.
De två granulaproven utsattes för ett accelerationstest vid 40°C x 75% r.h. under 6 månader och deras dispersionstillstånd utvärderades i form av specifik grumlighet som beräknades på ovan beskrivet sätt. Resultaten visas i tabell 1.The two granule samples were subjected to an acceleration test at 40 ° C x 75% r.h. for 6 months and their dispersion state was evaluated in the form of specific turbidity calculated as described above. The results are shown in Table 1.
Tabell l Ändring i specifik grumlighet som ett resultat av acceleration vid 40°C x 75% r.h. under 6 månader Tid 2 min. 5 min. 20 min.Table l Change in specific turbidity as a result of acceleration at 40 ° C x 75% r.h. for 6 months Time 2 min. 5 minutes. 20 min.
Prov Granula _före acceleration 0,93 0,95 0,96 enligt uppfinningen efter acceleration 0,85 0,92 0,95 ßämförelse- före acceleration 0,28 0,33 0,41 ranula efter acceleratio 0,16 0,18 0,19 503 233 Exempel 2 Sukralfat (4.000 g) blandades noggrant med 2.000 g av en vattenlösning av 10% polyetylenglykol (molvikt 6.000) i en blandare. Blandningen siktades genom en 16-mesh sikt för att göra ett granulat, som torkades vid 60°C under 3 timmar i en torkapparat och sorterades genom passage genom en 10-mesh sikt.Sample Granula - before acceleration 0.93 0.95 0.96 according to the invention after acceleration 0.85 0.92 0.95 Comparison - before acceleration 0.28 0.33 0.41 ranula after acceleration 0.16 0.18 0, Example 2 Sucralfate (4,000 g) was thoroughly mixed with 2,000 g of an aqueous solution of 10% polyethylene glycol (6,000 molecular weight) in a mixer. The mixture was sieved through a 16-mesh sieve to make a granulate, which was dried at 60 ° C for 3 hours in a dryer and sorted by passage through a 10-mesh sieve.
Erhållna granula (4.000 g) blandades med 1.376 g kristallinisk cellulosa och 24 g magnesiumstearat och blandades under 5 minuter i en V-typ blandare.The resulting granules (4,000 g) were mixed with 1,376 g of crystalline cellulose and 24 g of magnesium stearate and mixed for 5 minutes in a V-type mixer.
Det erhållna pulvret placerades i en roterande tablettmaskin utrustad med matriser och stansar (12 mmo) och komprimerades under ett totalt tryck på omkring 2,5 ton för att ge tabletter som vardera vägde 700 mg.The resulting powder was placed in a rotary tablet machine equipped with dies and punches (12 mmo) and compressed under a total pressure of about 2.5 tons to give tablets each weighing 700 mg.
Jämförelsetabletter gjordes på samma sätt som beskrivits ovan utom att vattenlösningen av 10% polyetylenglykol ersattes med en vattenlösning av 10% hydroxipropylcellulosa (Nisso HPC-L från Nippon Soda Co., Ltd.).Comparative tablets were made in the same manner as described above except that the aqueous solution of 10% polyethylene glycol was replaced with an aqueous solution of 10% hydroxypropylcellulose (Nisso HPC-L from Nippon Soda Co., Ltd.).
Desintegrationsförmågan och dispersionsförmågan hos de två tablettproven visas i figur 2 i form av den ändring i grum- lighet som förekom, med värdet hos en kontrollsuspension taget. som l. Kontrollsuspensionen framställdes genom noggrann dispergering av 1.000 mg sukralfat, 344 mg kristallinisk cellulosa och 6 mg magnesiumstearat i 1.000 ml vatten med ultraljudvågor och grumligheten hos denna kontrollsuspension mättes vid 540 nm i en detektorcell med en skikttjocklek på l cm. Mätning av grumligheten beskrives mer specifikt nedan: två tabletter av varje prov placerades i en desintegrationsprov- apparat (testvätska: 1.000 ml vatten vid 37 i 2°C) och grumligheten hos vätskemängderna som tagits ungefär 5 cm under testvätskornas yta mättes. Baserat på erhållna data beräknades den specifika grumligheten hos de individuella proverna. ^5Û3 233 De två tablettproverna utsattes för ett accelerationstest vid 40°C x 75% r.h. under 6 månader och deras dispersionstillstánd utvärderades i form av specifik grumlighet som beräknades på ovan beskrivet sätt.The disintegration capacity and dispersion capacity of the two tablet samples are shown in Figure 2 in the form of the change in turbidity that occurred, with the value of a control suspension taken. The control suspension was prepared by carefully dispersing 1,000 mg of sucralfate, 344 mg of crystalline cellulose and 6 mg of magnesium stearate in 1,000 ml of ultrasonic water and the turbidity of this control suspension was measured at 540 nm in a detector cell with a layer thickness of 1 cm. Measurement of turbidity is described more specifically below: two tablets of each sample were placed in a disintegration tester (test liquid: 1,000 ml of water at 37 at 2 ° C) and the turbidity of the amounts of liquid taken approximately 5 cm below the surface of the test liquids was measured. Based on the data obtained, the specific turbidity of the individual samples was calculated. The two tablet samples were subjected to an acceleration test at 40 ° C x 75% r.h. for 6 months and their dispersion state was evaluated in the form of specific turbidity calculated as described above.
Resultaten visas i tabell 2.The results are shown in Table 2.
Tabell 2 Ändring i specifik grumlighet som ett resultat av acceleration vid 40°C x 75% r.h. under 6 månader Tid 2 min. 5 min. 20 min.Table 2 Change in specific turbidity as a result of acceleration at 40 ° C x 75% r.h. for 6 months Time 2 min. 5 minutes. 20 min.
Prov Tabletter före acceleration 0,79 0,85 0,95 enligt uppfinningen efter acceleration 0,63 0,80 0,92 Jämförelse- före acceleration 1 0,20 0,25 0,30 tabletter efter acceleration1"0,09 0,13 0,16Sample Tablets before acceleration 0.79 0.85 0.95 according to the invention after acceleration 0.63 0.80 0.92 Comparison before acceleration 1 0.20 0.25 0.30 tablets after acceleration 0.09 0.13 0.16
Claims (2)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP9990186 | 1986-04-30 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| SE8701787D0 SE8701787D0 (en) | 1987-04-29 |
| SE8701787L SE8701787L (en) | 1987-10-31 |
| SE503233C2 true SE503233C2 (en) | 1996-04-22 |
Family
ID=14259677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SE8701787A SE503233C2 (en) | 1986-04-30 | 1987-04-29 | Sucralfate preparation and process for preparing the same |
Country Status (9)
| Country | Link |
|---|---|
| JP (1) | JP2542210B2 (en) |
| DE (1) | DE3714159C2 (en) |
| DK (1) | DK167735B1 (en) |
| ES (1) | ES2017805A6 (en) |
| FI (1) | FI89457C (en) |
| FR (1) | FR2598084B1 (en) |
| IT (1) | IT1208416B (en) |
| NO (1) | NO174085C (en) |
| SE (1) | SE503233C2 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2735559B2 (en) * | 1988-03-02 | 1998-04-02 | 中外製薬株式会社 | Suspension |
| BR9507533A (en) * | 1994-04-26 | 1997-09-02 | Chugai Pharmaceutical Co Ltd | Fused granulated sucralfate preparations and a process for their production |
| KR19980701891A (en) * | 1995-02-02 | 1998-06-25 | 나가야마 나오루 | Sucralate formulations |
| ES2112765B1 (en) * | 1995-08-02 | 1999-03-01 | Cantabria Ind Farmaceutica Sa | PROCEDURE FOR OBTAINING RADIOLOGICAL CONTRAST FORMULATIONS, FOR GASTROINTESTINAL EXPLORATIONS FOR EXTEMPORARY AND DIRECT USE. |
| TW201132646A (en) * | 2010-02-22 | 2011-10-01 | Daiichi Sankyo Co Ltd | Oral solid extended release dosage form |
| TW201141544A (en) | 2010-02-22 | 2011-12-01 | Daiichi Sankyo Co Ltd | Oral solid extended release dosage form |
| KR102127625B1 (en) | 2012-09-03 | 2020-06-29 | 다이이찌 산쿄 가부시키가이샤 | Hydromorphone hydrochloride-containing oral sustained-release pharmaceutical composition |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3430809A1 (en) * | 1984-08-22 | 1986-03-06 | Merck Patent Gmbh, 6100 Darmstadt | SUCRALFAT SUSPENSION |
-
1987
- 1987-04-28 NO NO871759A patent/NO174085C/en unknown
- 1987-04-28 DE DE3714159A patent/DE3714159C2/en not_active Expired - Lifetime
- 1987-04-28 FI FI871852A patent/FI89457C/en not_active IP Right Cessation
- 1987-04-29 IT IT8767365A patent/IT1208416B/en active
- 1987-04-29 ES ES8701280A patent/ES2017805A6/en not_active Expired - Lifetime
- 1987-04-29 SE SE8701787A patent/SE503233C2/en not_active IP Right Cessation
- 1987-04-29 DK DK218587A patent/DK167735B1/en not_active IP Right Cessation
- 1987-04-30 JP JP62104612A patent/JP2542210B2/en not_active Expired - Lifetime
- 1987-04-30 FR FR878706196A patent/FR2598084B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| NO174085B (en) | 1993-12-06 |
| DK218587D0 (en) | 1987-04-29 |
| FI871852A (en) | 1987-10-31 |
| FR2598084B1 (en) | 1991-04-26 |
| ES2017805A6 (en) | 1991-03-01 |
| FR2598084A1 (en) | 1987-11-06 |
| FI89457C (en) | 1993-10-11 |
| NO174085C (en) | 1994-03-16 |
| IT1208416B (en) | 1989-06-12 |
| SE8701787D0 (en) | 1987-04-29 |
| DK218587A (en) | 1987-10-31 |
| NO871759L (en) | 1987-11-02 |
| JPS63107933A (en) | 1988-05-12 |
| DE3714159A1 (en) | 1987-11-05 |
| SE8701787L (en) | 1987-10-31 |
| NO871759D0 (en) | 1987-04-28 |
| DE3714159C2 (en) | 1996-09-19 |
| FI89457B (en) | 1993-06-30 |
| DK167735B1 (en) | 1993-12-13 |
| JP2542210B2 (en) | 1996-10-09 |
| IT8767365A0 (en) | 1987-04-29 |
| FI871852A0 (en) | 1987-04-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| NUG | Patent has lapsed |