CN104473892A - Faropenem sodiumcomposition for direct tabletcompression and preparation method of faropenem sodiumcomposition - Google Patents
Faropenem sodiumcomposition for direct tabletcompression and preparation method of faropenem sodiumcomposition Download PDFInfo
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- CN104473892A CN104473892A CN201410821747.3A CN201410821747A CN104473892A CN 104473892 A CN104473892 A CN 104473892A CN 201410821747 A CN201410821747 A CN 201410821747A CN 104473892 A CN104473892 A CN 104473892A
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Abstract
The invention belongs to the technical field of medicinepreparation, and particularly relates to faropenem sodiumcomposition for direct tabletcompression and a preparation method of the faropenem sodiumcomposition. The composition comprises, in percentage by weight, 40%-70% of faropenem sodium and 30%-60% of an auxiliary material, wherein the faropenem sodium is fine powder with theaverageparticle size ranging from 150 mum to 250 mu m; the auxiliary material comprises a disintegrating agent, a binding agent, 0%-5% of a lubricating agent, 0%-5% of a flow aid and one or more of microcrystalline cellulose, cellulose, starch, saccharides and inorganic salts. Compared with the prior art, thefaropenem sodiumcomposition has the advantages that tablets can be prepared from the faropenem sodiumcomposition with a direct tabletcompression method, processes that medicines are contacted with humid and heat are omitted, the product stability is improved, technological steps are reduced, work hours are saved, the production cost is reduced, and the production efficiency is improved.
Description
Technical field
The invention belongs to field of medicine preparing technology, specifically, relate to a kind of Faropenem sodium composition and method of making the same for direct compression.
Background technology
Faropenem sodium is a typical beta-Lactam antibiotic, is the derivant belonging to penems.It is up to the present in the world first orally active, the blue or green enzyme carbapenem antibiotic stable to beta-lactamase.It has efficiently to suppressing G+ and G-bacterium and anaerobe widely, the particularly the most effective beta-Lactam antibiotic of anaerobe resistant, and from the trend of antibiotic development, Faropenem sodium is rising.But penems antibiotics also has obvious shortcoming, very poor at wet heat condition stability inferior.And the preparation technology of conventional tablet needs through processes such as soft material processed, granulation and oven dry, in the process, binding agent brings a large amount of moisture into, again through hyperthermia drying heating, greatly have impact on the stability of Faropenem sodium.After direct compression refers to that drug powder mixes with suitable adjuvant, the method for direct compression without granulation.Its advantage is that production process is few, and equipment is simple, decreases supplementary product consumption, product disintegrate or stripping very fast.In addition, the method is not through the process that contact is damp and hot, especially suitable at the medicine of wet heat condition stability inferior difference to some.But it is less that Faropenem sodium adopts direct compression but to study at present.
Summary of the invention
For solving the problems of the technologies described above, the invention provides a kind of simple, stable Faropenem sodium composition and method of making the same for direct compression.
A kind of faropenem composition of sodium for direct compression of the present invention, described compositions, by weight calculating, is made up of 40%-70% Faropenem sodium and 30%-60% adjuvant; Described Faropenem sodium is fine powder, and its particle mean size is between 150 μm-250 μm; Described adjuvant comprises disintegrating agent and binding agent, 0%-5% lubricant and 0%-5% fluidizer.
A kind of faropenem composition of sodium for direct compression of the present invention, described disintegrating agent and binding agent be selected from microcrystalline Cellulose class, cellulose, starch based, saccharide, inorganic salts one or more.
A kind of faropenem composition of sodium for direct compression of the present invention, described microcrystalline Cellulose class comprise in microcrystalline Cellulose 102, microcrystalline Cellulose 112, microcrystalline Cellulose 212 one or more.
A kind of faropenem composition of sodium for direct compression of the present invention, described saccharide comprise in lactose, mannitol, sorbitol, xylitol and carbomer one or more.
A kind of faropenem composition of sodium for direct compression of the present invention, described inorganic salts comprise in calcium hydrogen phosphate, calcium phosphate, calcium sulfate and calcium carbonate one or more.
A kind of faropenem composition of sodium for direct compression of the present invention, described lubricant is one or more in magnesium stearate, Pulvis Talci, castor oil hydrogenated, Polyethylene Glycol, magnesium laurylsulfate, sodium stearyl fumarate.
A kind of faropenem composition of sodium for direct compression of the present invention, described cellulose is that hypromellose is or/and hyprolose; Described starch based comprises pregelatinized Starch; Described fluidizer is micropowder silica gel.
The preparation method of faropenem composition of sodium of the present invention, described preparation method concrete steps are: get lubricant and fluidizer is separately put, for subsequent use; By Faropenem sodium fine powder and residue adjuvant mix homogeneously, obtain homomixture; Homomixture is mixed homogeneously with lubricant and fluidizer again, obtains mixture; Mixture is directly compressed into the label of tablet by tablet machine; For preventing the label moisture absorption, to label film coating.
Compared with prior art, faropenem composition of sodium of the present invention can adopt direct compression process to prepare tablet, avoids the process that medicament contact is damp and hot, improves product stability; Decrease processing step, saved man-hour, reduced production cost, improve production efficiency.
Detailed description of the invention
Below in conjunction with specific embodiment, the Faropenem sodium composition and method of making the same for direct compression of the present invention is described further, but protection scope of the present invention is not limited to this.
Embodiment 1
100g particle mean size 150 μm-160 μm Faropenem sodium (in faropenem), 50g microcrystalline Cellulose 112,30g pregelatinized Starch, 20g hyprolose, the medicinal micropowder silica gel of 1g, 1g magnesium stearate, make 1000.
Method for making: take Faropenem sodium, microcrystalline Cellulose 112, pregelatinized Starch and hyprolose by recipe quantity, mix homogeneously.Add medicinal micropowder silica gel and magnesium stearate mix homogeneously again, tabletting, film coating, to obtain final product.
Embodiment 2
100g Faropenem sodium particle mean size 180 μm-190 μm (in faropenem), 60g Lactis Anhydrous, 40g pregelatinized Starch, 30g calcium hydrogen phosphate, the medicinal micropowder silica gel of 1g, 1g magnesium stearate, 3g Pulvis Talci, make 1000.
Method for making: take Faropenem sodium, Lactis Anhydrous and pregelatinized Starch by recipe quantity, mix homogeneously.Add medicinal micropowder silica gel, magnesium stearate and Pulvis Talci mix homogeneously again, tabletting, film coating, to obtain final product.
Embodiment 3
100g particle mean size 180 μm-190 μm Faropenem sodium (in faropenem), 60g Lactis Anhydrous, 40g pregelatinized Starch, 30g calcium hydrogen phosphate, the medicinal micropowder silica gel of 1g, 1g weight average molecular weight Mn=2.717 × 10
5and number-average molecular weight Mw=1.232 × 10
5seed watermelon polysaccharide sulfate, 1g magnesium stearate, 3g Pulvis Talci, make 1000.
Method for making: take Faropenem sodium, Lactis Anhydrous and pregelatinized Starch by recipe quantity, mix homogeneously.Add medicinal micropowder silica gel, seed watermelon polysaccharide sulfate, magnesium stearate and Pulvis Talci mix homogeneously again, tabletting, film coating, to obtain final product.
Embodiment 4
100g particle mean size 240 μm-250 μm Faropenem sodium (in faropenem), 50g microcrystalline Cellulose 102,20g pregelatinized Starch, 15g calcium sulfate, 15g calcium carbonate, 2g hypromellose, 2g hyprolose, 1g sorbitol, 1g carbomer, the medicinal micropowder silica gel of 1g, 1g Pulvis Talci, 1g sodium stearyl fumarate, make 1000.
Method for making: take Faropenem sodium, microcrystalline Cellulose 102, pregelatinized Starch, calcium sulfate, calcium carbonate, hypromellose, hyprolose, sorbitol, carbomer by recipe quantity, mix homogeneously.Add medicinal micropowder silica gel, Pulvis Talci and sodium stearyl fumarate mix homogeneously again, tabletting, film coating, to obtain final product.
Matched group
100g particle mean size 180 μm-190 μm Faropenem sodium (in faropenem), 50g microcrystalline Cellulose, 30g pregelatinized Starch, 10g carboxymethyl starch sodium, 70ml 5%PVP
k30the medicinal micropowder silica gel of 50% alcoholic solution, 1g, 1g magnesium stearate, make 1000.
Method for making: take Faropenem sodium, microcrystalline Cellulose, pregelatinized Starch and 2/3 carboxymethyl starch sodium by recipe quantity, mix homogeneously.Add 5%PVP
k3050% alcoholic solution makes soft material, and 18 orders are granulated.Granule, in 50 DEG C of oven dry, adds medicinal micropowder silica gel and magnesium stearate, and 16 orders are granulated, mix homogeneously.Tabletting, film coating, to obtain final product.
Quality testing
Index dissolution important in tablet test item, content, isomer and related substance is selected to be explained in further detail the present invention.
1. dissolution rate compares
Assay method: get this product, check according to dissolution method (Chinese Pharmacopoeia version in 2010 two annex Ⅹ C second methods), with water 900ml for solvent, rotating speed is 50 turns per minute, operate in accordance with the law, through 30 minutes time, get solution 10ml, filter precision and measure subsequent filtrate 1ml, put in 10ml measuring bottle, be diluted with water to scale, shake up, as need testing solution; Separately get faropenem reference substance appropriate, accurately weighed, with water dissolution and the reference substance solution made containing 16 μ g in every 1ml.Get above-mentioned two kinds of solution, respectively according to ultraviolet visible spectrophotometry (Chinese Pharmacopoeia version in 2010 two annex IV A), measure absorbance at the wavelength place of 306nm, calculate the stripping quantity of every sheet.Get above embodiment sample and carry out dissolution determination, respectively at 5,10,15,20,30 minutes sample analysis, comparative result.As shown in table 1.
Table 1 various sample dissolution determination result
Result shows, adopts direct compression, and drug-eluting comparatively wet granule compression tablet is fast, stripping substantially in 15 minutes.
2. content, isomer and related substance compare
Content assaying method: adopt the content of high performance liquid chromatography to Faropenem sodium to measure.Chromatographic condition and system suitability octadecylsilane chemically bonded silica are filler; With methanol-buffer (get trifluoracetic acid and each 1g of phosphoric acid, add 0.01mol/L four butyl bromation amine solubilize and be diluted to 1000ml, adjust pH to 6.0 with triethylamine, mixing), (40:60) be mobile phase; Determined wavelength is 305nm.Number of theoretical plate calculates should be not less than 2000 by faropenem peak.Isomer assay method: adopt high effective liquid chromatography for measuring, measures according to the method under assay item, calculates isomer.Determination of related substances method: adopt high effective liquid chromatography for measuring, measures according to the method under assay item, calculates related substance.Get above embodiment sample and carry out content, isomer and determination of related substances, result is as shown in table 2.
The various sample size of table 2, isomer and determination of related substances result
Result shows, adopt direct compression, in preparation process, stability is obviously better than wet granule compression tablet.
3. stability test
Study on the stability method: investigate 6 months under acceleration environment, respectively at 1,3, June time sampling detect; Room temperature is long-term 24 months, detects respectively at sampling when 6,12,18,24 months.Result is as shown in table 3, table 4, table 5.
Assay result under the different investigation condition of table 3
Isomer measurement result under the different investigation condition of table 4
Determination of related substances result under the different investigation condition of table 5
Result shows, the sample stability that the sample adopting direct compression to prepare is prepared compared with wet granulation in storing process is better.
Claims (9)
1. for a faropenem composition of sodium for direct compression, it is characterized in that, described compositions calculates in mass ratio, is made up of 40%-70% Faropenem sodium and 30%-60% adjuvant; Described Faropenem sodium is fine powder, and its particle mean size is between 150 μm-250 μm; Described adjuvant comprises disintegrating agent and binding agent, 0%-5% lubricant and 0%-5% fluidizer.
2. a kind of faropenem composition of sodium for direct compression according to claim 1, is characterized in that, described disintegrating agent and binding agent be selected from microcrystalline Cellulose class, cellulose, starch based, saccharide, inorganic salts one or more.
3. a kind of faropenem composition of sodium for direct compression according to claim 2, is characterized in that, described microcrystalline Cellulose class comprise in microcrystalline Cellulose 102, microcrystalline Cellulose 112, microcrystalline Cellulose 212 one or more.
4. a kind of faropenem composition of sodium for direct compression according to claim 2, is characterized in that, described saccharide comprise in lactose, mannitol, sorbitol, xylitol and carbomer one or more.
5. a kind of faropenem composition of sodium for direct compression according to claim 2, is characterized in that, described inorganic salts comprise in calcium hydrogen phosphate, calcium phosphate, calcium sulfate and calcium carbonate one or more.
6. a kind of faropenem composition of sodium for direct compression according to claim 1, it is characterized in that, described lubricant is one or more in magnesium stearate, Pulvis Talci, castor oil hydrogenated, Polyethylene Glycol, magnesium laurylsulfate, sodium stearyl fumarate.
7. a kind of faropenem composition of sodium for direct compression according to claim 2, is characterized in that, described cellulose is that hypromellose is or/and hyprolose; Described starch based is pregelatinized Starch.
8. a kind of faropenem composition of sodium for direct compression according to claim 1, it is characterized in that, described fluidizer is micropowder silica gel.
9. the preparation method of faropenem composition of sodium according to claim 1, is characterized in that, described preparation method concrete steps are: get lubricant and fluidizer is separately put, for subsequent use; By Faropenem sodium and residue adjuvant mix homogeneously, obtain homomixture; Homomixture is mixed homogeneously with lubricant and fluidizer again, obtains mixture; Mixture is directly compressed into the label of tablet by tablet machine; For preventing the label moisture absorption, to label film coating.
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| CN106390094A (en) * | 2016-11-11 | 2017-02-15 | 上海雅本化学有限公司 | Trandolapril-containing pharmaceutical composition and preparation method thereof |
| CN106890150A (en) * | 2015-12-17 | 2017-06-27 | 康芝药业股份有限公司 | A kind of faropenem sodium tablets |
| CN111202714A (en) * | 2020-02-26 | 2020-05-29 | 江苏艾立康药业股份有限公司 | Faropenem sodium particles and preparation method thereof |
| CN115590832A (en) * | 2021-06-28 | 2023-01-13 | 山东新时代药业有限公司（Cn） | Faropenem sodium tablet and preparation method thereof |
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