CN1121221C - Medicine preparation containing ferrous saccharin - Google Patents
Medicine preparation containing ferrous saccharin Download PDFInfo
- Publication number
- CN1121221C CN1121221C CN 00130114 CN00130114A CN1121221C CN 1121221 C CN1121221 C CN 1121221C CN 00130114 CN00130114 CN 00130114 CN 00130114 A CN00130114 A CN 00130114A CN 1121221 C CN1121221 C CN 1121221C
- Authority
- CN
- China
- Prior art keywords
- saccharin
- ferrous
- tablet
- capsule
- add
- 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 - Fee Related
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a medicine preparation (an oral tablet and a capsule) containing ferrous saccharin, which is characterized in that ferrous saccharin is mixed with a solid stroma which comprises general excipients, such as diluting agents, lubricating agents, adhesives, disintegrating agents and antioxidants. The oral tablet or capsule containing ferrous saccharin can be used as medicine for treating and/or preventing various disease symptoms caused by the iron deficiency of human bodies.
Description
Technical field
The present invention relates to a kind of pharmaceutical preparation (oral tablet, capsule) that contains ferrous saccharin.It can be used as the iron supplement medicine of treatment resistance to iron deficiency disease.
Background technology
Usually, the iron supplement medicine as the resistance to iron deficiency disease is Feratab and ferrous sulfate syrup.Because ferrous sulfate has the metallic taste of tasting bad, when preparing oral ferrous sulfate medicament, must add sweeting agent, antiseptic, coated tablet made by flavoring agent or syrup can.In the preparation process, gone bad by microbial contamination easily.
Summary of the invention
It can be used as resistance to iron deficiency disease medicine to the object of the present invention is to provide a kind of pharmaceutical preparation (oral tablet, capsule) that contains ferrous saccharin, in order to treatment or prevention iron deficiency disease.
Ferrous saccharin is yellow green monoclinic system crystal, and it is dissolved in hot water, is slightly soluble in water under the room temperature, dissociates into glucide root and ferrous ion after water-soluble.The ferrous saccharin crystal is a hexahydrate, generates by ferrous chloride and saccharin sodium reaction, or by highly purified iron powder or ferrous oxide and glucide reaction generation.Its chemical name is: adjacent sulphonyl benzene (first) acid imide is ferrous, and structural formula is:
, the ferrous saccharin crystal contains ferrum element 10.57%, becomes anhydrous ferrous saccharin after the oven dry dehydration:
, anhydrous ferrous saccharin contains ferrum element 13.29%.Ferrous saccharin can be used in preparation resistance to iron deficiency disease drug.Medicinal ferrous saccharin can directly use 40-80 purpose ferrous saccharin crystallite.
Pharmacodynamic study shows that ferrum is the main constituent of hemoglobin and Myoglobin.Hemoglobin is the person that mainly takes oxygen in the erythrocyte.Myoglobin is the position that muscle cell is stored oxygen, oxygen supply needs when helping muscular movement.Most of enzymes relevant and the equal iron content of substrate, or only competence exertion effect when ferrum exists with tricarboxylic acid cycle.So behind the actively additional chalybeate of iron deficiency patient, the dehematize red eggs are synthetic in vain quicken outside, with organize active relevant symptom such as growth retardation, the dystropy that reduces of iron deficiency and iron enzyme, be short of physical strength, mucosal tissue variation and skin, fingernail pathological changes also all can be corrected gradually.
Ferrous saccharin is lighter to GI irritation.After ferrous saccharin dissociated in human body, ferrous ion mainly reached the jejunum near-end and absorbs in duodenum.Ferrum absorption back combines with transferrins and enters blood circulation, and is used for making erythrocyte, also can ferritin or the cumulative liver of hemosiderin form, spleen, bone marrow and other reticuloendothelium.Every day in human body drained denier by ferrum, sees in urine, excrement, perspiration, the intestinal mucosa cells that comes off and the enzyme, and its forfeiture total amount every day is 0.5-1.0mg, can not all discharge with feces from intestinal absorption person behind the oral chalybeate.
Glucide can not be utilized in human body, and is most of with the urine discharge, and do not damage renal function, do not change body endoenzyme system activity, also do not influence the utilization of vitamin.On May 15th, 2000, when delivering the carcinogen research report, points out by American National Environmental Health institute.Owing to studies confirm that the high dose glucide makes the carcinogenic situation of mouse and is not suitable for the mankind.Therefore, no longer glucide is classified as may be carcinogenic material.Like this, can illustrate that the edible glucide of amount is still very safe in accordance with regulations.
Ferrous saccharin has the sweet taste of good mouthfeel, its sugariness is about 300 times of sucrose, when being used to make pharmaceutical preparation, need not add sugar sweetener, flavoring agent again, no longer add or reduce the addition of antiseptic, the ferrous saccharin tablet need not be made coated tablet, thereby can reduce the toxic and side effects that produces because of the additive compatibility, also can avoid being gone bad, help prolonging the shelf-life of medicament by microbial contamination.In addition, because ferrous sulfate dissolubility in water is big, dissolution velocity is fast, and its effective drug duration is shorter, and under the ferrous saccharin room temperature in water dissolubility less, dissolving slowly, thereby make the effective drug duration significant prolongation.Like this, ferrous saccharin tablet, capsule are compared with Feosol, have the effect of slow releasing preparation, therefore, compare with existing Feratab, syrup and to have substantive distinguishing features and obvious improvement.
Ferrous saccharin oral tablet provided by the invention, capsule, be that ferrous saccharin is blended in a kind of solid matrix, this solid matrix is selected from the usual excipients of diluent, lubricant, binding agent, disintegrating agent, antioxidant and so on, and excipient is the pharmaceutical aids that is used for the raw material principal agent is made certain dosage form.With the tablet that ferrous saccharin makes as supplements-iron, it is 0.2-0.9g that every g contains the ferrous saccharin general quantity, is preferably 0.4-0.8g, and the general content of ferrous saccharin is 0.1-0.5g in every of the capsule that makes, and is preferably 0.3-0.5g.
Capsule of the present invention is meant a certain amount of ferrous saccharin added adjuvant or do not add adjuvant after making powder or granule, and filling is in Capsules and the pharmaceutical preparation of making.And Capsules be by the suitable medicinal materials (as: methylcellulose, calcium alginate, sodium alginate, polyvinyl alcohol, metagelatin) of gelatin or other add that adjuvant makes have elasticity and can be mutually tight two pitch circle tubes of fit.
Described diluent (or filler) be when medicine because of dosage too small so that make that certain dosage form adds when having any problem in order to increase the excipient of unit formulation (as 1,1) volume.The suitable diluents that the present invention selects for use is that starch and/or pregelatinized Starch (claim amylum pregelatinisatum again, be that starch destroys the product that the starch structure makes the part gel through physical method, be the white dried powder, odorless, tasteless, stable in properties), also available diluent comprises: lactose, glucose, mannitol, Sorbitol, cellulose, xylitol, dextrose, fructose, calcium sulfate, light magnesium oxide, sucrose and composition thereof.Diluent generally accounts for 1% to 20% of ferrous saccharin tablet, capsule.
Described wetting agent itself is inviscid, but it is energy moistening material, brings out the excipient of the viscosity of material own.The suitable wetting agent that the present invention is suitable for is distilled water or ethanol.Wetting agent vapors away when preparation is dried, so not as the composition of preparation.
Described binding agent is to be used for making granule to have the excipient of viscosity, to make the more stable dosage unit of physical characteristic, comprising: microcrystalline Cellulose, hypromellose, polyvidone, starch slurry, dextrin, syrup, maltose, crystallite glucose, sodium carboxymethyl cellulose, Mel, carboxymethyl dextran sodium are basic binding agent.Be used for binding agent preferably microcrystalline cellulose of the present invention or dextrin.Binding agent generally accounts for 1% to 5% of ferrous saccharin tablet weight.
Described disintegrating agent is to be added to make it take back easy disintegrate and the material of stripping or mixture of this material in gastrointestinal tract in the tablet.General this class material is: cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, dried starch, carboxymethyl starch sodium, hydroxypropyl starch, low-substituted hydroxypropyl cellulose.What the present invention preferably used is cross-linking sodium carboxymethyl cellulose or carboxymethyl starch sodium.Disintegrating agent generally accounts for 0.5% to 6% of prepared particle weight.
Described lubricant is to improve the tablet and powder turnover rate, prevents that the tabletting material is bonded at punch die and press surface, reduces intergranular friction, and helps the excipient that tablet is discharged the punch die groove.Lubricant commonly used has Pulvis Talci, hydrogenated vegetable oil, Polyethylene Glycol, Stepanol MG, liquid Paraffin.The lubricant that the present invention adopts is preferably Stepanol MG.Lubricant generally accounts for 0.2% to 5% of prepared particle weight.
Described polyphenoils is to prevent that airborne oxygen from causing the adjuvant of pharmaceutical preparation oxidation.Antioxidant commonly used has sodium sulfite, sodium sulfite, sodium pyrosulfite.Be used for the preferred sodium pyrosulfite of antioxidant of the present invention.The consumption of antioxidant generally accounts for 0.05% to 0.3% of resulting granules weight.
And it also is admissible using other typical additives or other excipient such as coloring agent, aromatic.
Solid-based mass-energy of the present invention is made into tablet, capsule, and this technology is known in the prior art, and is disclosed in " pharmaceutics " (Bi Dianzhou chief editor, the People's Health Publisher publishes, July in 1999 the 4th edition) 300-302 page or leaf, 325-334 page or leaf.
The specific embodiment
Further describe the present invention below in conjunction with embodiment.
Embodiment 1:
Get dried starch 30g, place under 105 ℃ of temperature dry 1 hour, standby.Get ferrous saccharin crystallite 300g, cross 60 mesh sieve, be mixed together evenly with 60g microcrystalline Cellulose, 10g Stepanol MG, 20g dried starch, 0.5g sodium pyrosulfite, 1.5g Oleum menthae, 3.0g cross-linking sodium carboxymethyl cellulose then, cross twice of 40 mesh sieve, through after the assay was approved, adopt the direct compression process known technology, be pressed into 1000 oral tablets, sealing is preserved.
This tablet is the pistac sheet, and it is sweet to distinguish the flavor of.Every contains ferrous saccharin 0.3g, contains the about 32mg of elemental iron.Wherein, dried starch is that diluent, disintegrating agent, microcrystalline Cellulose are dilution, binding agent, and Stepanol MG is a lubricant, and sodium pyrosulfite is an antioxidant, and Oleum menthae is an aromatic, and cross-linking sodium carboxymethyl cellulose is a disintegrating agent.
Described ferrous saccharin crystallite is after carrying out displacement reaction by glucide and iron powder, to form through crystallization or recrystallization.Its concrete preparation method is: add the 2000ml distilled water in the glass reaction still, add give money as a gift 89% glucide 250g and 200 purpose iron powder 40g again, stir also heating, when temperature rises to 80 ℃, can see having many micro-bubbles to generate, this gas is hydrogen.Keep 80-90 ℃ of temperature half an hour, most of material is reacted, reheat also keeps 90-100 ℃ of temperature half an hour, iron powder and glucide are fully reacted, and reactant liquor becomes oyster, and pH value is 6.0, add active carbon 2g, continue to stir 20 minutes, be incubated 85 ℃ and carry out heat filtering, filtrate is moved in the crystallization kettle.Ferrous saccharin solution is under the subacidity state of pH=6.0, cooling rate is to fall 2 ℃ in 1 minute, ferrous saccharin crystal grain is folded and grow, last till when temperature drops to 20 ℃ always, crystallite is separated with liquid glucose, centrifuge dripping is removed the plane of crystal attached water, can get 40-80 purpose ferrous saccharin crystallite crystal 2 55g.Through chemical examination, the content of gained ferrous saccharin crystallite is 99.1%, and moisture content is 19.3%.
The determination of ferrous saccharin is as follows:
Accurately take by weighing the ferrous saccharin sample 500mg of drying, insert in the separatory funnel, add 10ml water and dilute hydrochloric acid test solution (TS-117) 2ml, use the mixed solvent that is made into by 9 parts of chloroforms and 1 part of ethanol (v/v) then, the glucide of extraction precipitation, for the first time use the 30ml solvent, all the other all use 20ml five times, and extract is evaporated on steam bath dried (helping drying with blowing), residue is dissolved in the 75ml hot water, cooling, add 3 of phenolphthalein test solutions (TS-167) after, carry out titration with the NaOH standard solution of 0.1N, simultaneously, carry out blank assay, and should avoid various errors as far as possible, the NaOH standard solution of every 1ml0.1N is equivalent to anhydrous ferrous saccharin 21.01mg.
Embodiment 2:
Get dried starch 100g, placed under 105 ℃ of temperature dry 1 hour, cross 60 mesh sieve, standby.With 1g sodium pyrosulfite porphyrize, cross 60 mesh sieve, standby.With 60 purpose ferrous saccharin 450g and 50g dried starch, 0.8g sodium pyrosulfite mix homogeneously is crossed twice of 40 mesh sieve, abundant mix homogeneously, equivalent branch are packed in the double-colored opaque hollow capsule for medicine, the 0.5g powder of packing in every capsules, promptly make 1000 capsules medicaments, sealing is preserved.Every capsules contains ferrous saccharin 0.45g, contains elemental iron 48mg.Wherein said ferrous saccharin makes by the method for embodiment 1, and its detection method of content is with embodiment 1.
The general chemistry method of inspection of ferrous saccharin preparation is as follows:
One, differentiate:
1, gets ferrous saccharin tablet or capsule 0.2g, add the 10ml distilled water, add 1 of dilute hydrochloric acid, shook 10 minutes, filter.Get filtrate 5ml and place little flask, low baking temperature heating, evaporated under reduced pressure moisture, add the 40mg resorcinol, the 0.5ml concentrated sulphuric acid heats this mixture 3 minutes in 200 ℃ liquid bath, cool, add the sodium hydroxide solution of 10ml distilled water and 100ml4%, then be formed with the liquid of green fluorescence.The existence of provable glucide thus.
2, get 1 of 1 in ferrous saccharin tablet or capsule, add 1 of dilute hydrochloric acid and distilled water 20ml, jolting makes the ferrous saccharin dissolving, filters, and filtrate is equipped with examination.Get and try filtrate 3ml fully, add an alcoholic solution number promptly apparent peony of 1% orthophenanthroline.Get and try filtrate 5ml fully, add iron potassuim cyanide test liquid, dark blue precipitate promptly takes place; Separate, be deposited in the dilute hydrochloric acid insolublely, but hydro-oxidation sodium test solution promptly decomposes and generates brown precipitate.Provable thus ferrous ion exists.
Two, assay:
Get 3 of 5 in ferrous saccharin tablet or capsules, put in the 200ml measuring bottle, it is an amount of with the cold water that newly boiled to add dilute sulfuric acid 30ml, jolting makes the ferrous saccharin dissolving, is diluted to scale with the cold water that newly boiled, and shakes up, filter rapidly with dry filter paper, discard filtrate just, precision is measured subsequent filtrate 50ml, adds orthophenanthroline (C
12H
8N
2H
2O) indicator solution number droplet is used 0.1mol/L ceric sulfate [Ce (SO immediately
4)
24H
2O] the volumetric solution titration.Simultaneously, carry out blank assay, and do necessary the correction, every ml0.1mlo/L ceric sulfate is equivalent to ferrous saccharin (C
14H
8N
2O
6S
2Fe6H
2O) 52.83mg.
Except that carrying out chemical analysis, the tablet, the capsule that contain ferrous saccharin also should be tested by the rules of preparations of Chinese Pharmacopoeia regulation.
Claims (3)
1, a kind of medicinal tablet, the capsule used of treatment iron deficiency disease, contain ferrous saccharin and with the blended a kind of solid matrix of ferrous saccharin, this fixedly substrate be selected from the usual excipients of diluent, lubricant, binding agent, disintegrating agent, antioxidant and so on.
2, the tablet that contains ferrous saccharin as claimed in claim 1, the content that it is characterized in that ferrous saccharin among the every g of tablet is 0.2-0.9g.
3, the capsule that contains ferrous saccharin as claimed in claim 1 is characterized in that the content of ferrous saccharin in every of the capsule is 0.1-0.5g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 00130114 CN1121221C (en) | 2000-10-16 | 2000-10-16 | Medicine preparation containing ferrous saccharin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 00130114 CN1121221C (en) | 2000-10-16 | 2000-10-16 | Medicine preparation containing ferrous saccharin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1288726A CN1288726A (en) | 2001-03-28 |
| CN1121221C true CN1121221C (en) | 2003-09-17 |
Family
ID=4593972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 00130114 Expired - Fee Related CN1121221C (en) | 2000-10-16 | 2000-10-16 | Medicine preparation containing ferrous saccharin |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1121221C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100344326C (en) * | 2005-09-30 | 2007-10-24 | 北京康比特威创体育新技术发展有限公司 | Iron-supplementing preparation |
-
2000
- 2000-10-16 CN CN 00130114 patent/CN1121221C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1288726A (en) | 2001-03-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP1827386B1 (en) | Oral compositions for absorption of phosphorus compounds | |
| TWI375555B (en) | Pharmaceutical-grade ferric organic compounds, uses thereof and methods of making same | |
| EP2598123A1 (en) | Compositions | |
| CN101011372A (en) | Preparing method of alpha-ketoglutaric acid-arginine salt and its use for treating hepatic disease | |
| CN105920024A (en) | Acarbose-containing compound preparation for treating diabetes mellitus complicated essential hypertension and preparation method thereof | |
| CN102716135B (en) | Lupenone prevents in preparation or treats the application in the product of diabetes | |
| CN111388436A (en) | Sodium alginate chewable tablet and preparation method thereof | |
| CN1121221C (en) | Medicine preparation containing ferrous saccharin | |
| JP4484338B2 (en) | Coenzyme A oral preparation useful for lowering blood lipid and preparation method thereof | |
| CN1695738B (en) | Composition of medication for treating high blood pressure | |
| TWI725317B (en) | Use of composition of neoandrographolide in lowering blood sugar | |
| CN102727894A (en) | Pharmaceutical composition for treating diabetes and its complications and application thereof | |
| CN101954090B (en) | Dihydroartemisinin beta-cyclodextrin inclusion compound, preparation method thereof and antimalarialdrug with same | |
| RU2747985C1 (en) | Solid-phase composition for correction of metabolic disorders in type 2 diabetes mellitus | |
| CN1081032C (en) | Medicinal preparation containing saccharin zinc | |
| CN1203049C (en) | Rapid-dissoved ambroxol salt and preparing method thereof | |
| US10894059B2 (en) | NADH compound composition, and preparation and use thereof | |
| CN102100695B (en) | High-safety medicinal composition of cinepazide, and preparation method and application thereof | |
| CN102093234B (en) | Tromethamine salt compound of dibasic ester acid, preparation method and medicinal application thereof | |
| CN101708179B (en) | Cinepazide medicinal composition with high safety, preparation method and application thereof | |
| CN104138363A (en) | Nifedipine sustained-release tablet and preparation method thereof | |
| JP2948122B2 (en) | Pharmaceutical for enhancing muscle protein formation and muscle substance metabolism and method for producing the pharmaceutical | |
| CN1689579A (en) | Application of burdock glycoside or its aglycon in preparation of medicine for treating diabetes or its complications | |
| US11744870B2 (en) | Traditional Chinese medicine composition for treating metabolic syndrome and preparations thereof | |
| TWI721282B (en) | Use of composition of neoandrographolide for improving renal function |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C19 | Lapse of patent right due to non-payment of the annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |