CN102144986A - Potassium chloride cyclopenthiazide sustained release tablet and preparation method thereof - Google Patents
Potassium chloride cyclopenthiazide sustained release tablet and preparation method thereof Download PDFInfo
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- CN102144986A CN102144986A CN 201110096136 CN201110096136A CN102144986A CN 102144986 A CN102144986 A CN 102144986A CN 201110096136 CN201110096136 CN 201110096136 CN 201110096136 A CN201110096136 A CN 201110096136A CN 102144986 A CN102144986 A CN 102144986A
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- cyclopenthiazide
- potassium chloride
- quaternary amine
- acrylate copolymer
- ylmethyl acrylate
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Abstract
The invention discloses a potassium chloride cyclopenthiazide sustained release tablet for treatment on edema and hypertension. The potassium chloride cyclopenthiazide sustained release tablet comprises potassium chloride, cyclopenthiazide, retardarce sustained release agent, binding agent and lubricant. The preparation technology comprises the following steps of: performing wet granulation, drying and sorting granules, adding proper amount of the lubricant, mixing the added constituents uniformly, tabletting the mixture, and coating the tablets to get products. The sustained release tablet provided by the invention can greatly reduce the dosage of accessories and the adverse reaction, is easy for industrial production and convenient to take, has steady in vitro releasing curve and long action time, and can continuously supply electrolyte lost in large amount of urination for the patient in the diuretic process.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of potassium chloride cyclopenthiazide slow releasing tablet and preparation method thereof.
Background technology
Cyclopenthiazide is middle effect diuretic, and its chemical name is 3-methyl cyclopentane-6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide.Its molecular formula: C
13H
18ClN
3O
4S
2, molecular weight is 379.88, structural formula is:
Cyclopenthiazide is applicable to polytype edema and hypertensive patient, also can be used for diabetes insipidus.Can suppress renal tubules medullary loop ascending branch cortex portion and Distal convoluted tubule to Na
+And Cl
-Heavily absorption, thereby the performance diuresis.This product also has hypotensive effect, and medication is early stage because diuresis reduces blood volume and blood pressure lowering, the slight sodium that loses in the medication later stage body, and the small artery parietal cell hangs down sodium, passes through Na
+-Ca
2+Exchanging mechanism makes Ca in the cell
2+Amount reduces, and blood vessel reduces Contractile response of artery supplying, and the diastole of hyperamization pipe, blood pressure drops.This product also has the hypotensive effect that strengthens other depressor and reaches the diabetes insipidus patient, and this product has antidiuretic activity, can reduce diabetes insipidus patient's urine amount.Long-term or should note replenishing potassium salt or share with the kalium replenishment diuretic than the large dose oral administration person, in case hypokalemia.At present existing cyclopenthiazide tablet listing.
Potassium chloride is for regulating water salt, electrolyte and acid-base balance medicine, and its molecular formula is KCl, and molecular weight is 74.55.
Potassium is intracellular main cation, and its concentration is 150～160mmol/L; And extracellular main cation is a sodium ion, and potassium concn only is that 3.5～5 mmol/L. bodies mainly rely on the Na on the cell membrane
+-K
+-ATP enzyme is kept intracellular K
+, Na
+Concentration difference.Intravital acid-base balance state is thanked influential to potassio, H during as acidosis
+Enter in the cell, in order to keep the potential difference of cell, K
+Be released to the extracellular, cause or increase the weight of hyperpotassemia. and metabolism disorder also can influence acid-base balance.Some critical function of the inside and outside potassium concentration of normal cell and concentration difference and cell has confidential relation, comprises keeping carbohydrate metabolism, glycogen storage, protein metabolism, osmotic pressure and acid-base balance in the cell, myocardial excitability and conductivity; Keep the conduction of skeletal muscle normal tension and neural impulse, and can make intestinal, uterus and the rising of bronchial smooth muscle tension force etc.
Acrylic resin comprises methacrylic acid copolymer and methacrylate copolymer.Be widely used in the skeleton adhesive material of the gastric solubleness coating, enteric coating of medicine agent, slow controlled release coat, protection isolation coat, sustained-release matrix material and percutaneous drug administration preparation.
The listing of potassium chloride slow releasing tablet is all arranged at present both at home and abroad, and do not see the report of relevant potassium chloride cyclopenthiazide slow releasing tablet.
Summary of the invention
Purpose of the present invention provides a kind of compound slow release preparation that contains cyclopenthiazide, potassium chloride, and the preparation method of said preparation is provided simultaneously, is to use novel tablet formulation processing technique to prepare slow releasing tablet.
The potassium chloride cyclopenthiazide slow releasing tablet that this patent is prepared when alleviating edema and hypertension symptom by diuretic, can slowly be replenished potassium ion, thereby reduces the side effect of diuretic.Reduce the fluctuation of concentration of potassium ion in patient's medicining times, the minimizing blood, prevented the generation of side effect such as hyperkalemia.And the tablet that utilizes preparation method of the present invention to make has significantly reduced adjuvant ground consumption in the label.Thereby it is heavy to reduce sheet, increases patient's compliance.
The prescription of potassium chloride cyclopenthiazide slow releasing tablet is:
Potassium chloride 450g
Cyclopenthiazide 0.125g
Quaternary amine ylmethyl acrylate copolymer A type 10-40 g
Quaternary amine ylmethyl acrylate copolymer Type B 10-50g
Water 1-20g
Ethanol (95%) 400-1000g
Plasticizer 4-10g
Antiplastering aid 5-50g
In this compound preparation, label comprises potassium chloride, cyclopenthiazide, quaternary amine ylmethyl acrylate copolymer Type B binding agent; Slow-release material comprises the mixture of the quaternary amine ylmethyl acrylate copolymer A type, quaternary amine ylmethyl acrylate copolymer Type B or the two kinds of macromolecular materials that add plasticizer; Label and slow-release material weight ratio are 15:1 to 10:1.Above-mentioned slow-release material is the insensitive slow-release material of pH, and is insoluble in water.Plasticizer is glycerol, propylene glycol, Oleum Ricini or derivatives thereof, monoacetin, triacetin, triethyl citrate, Macrogol 200-6000, tributyl citrate and decanedioic acid two fourths (second) ester, phthalic acid two fourths (second) ester or its arbitrary composition.Plasticizer dosage is the 10-20% of above-mentioned composition; Antiplastering aid is Pulvis Talci, magnesium stearate, glyceryl monostearate, micropowder silica gel or any mixture.The antiplastering aid consumption is the 25%-200% of above-mentioned composition; Can also add opacifier, can be titanium dioxide, also can add versicolor coloring agent as required.
The quaternary amine ylmethyl acrylate copolymer A type that the present invention selects for use, quaternary amine ylmethyl acrylate copolymer Type B are water-insoluble filmogen in this series adjuvant, selected concrete model is served as reasons and is won wound company product: strange RS100 of You Te and RL100, swellable in water is the cationic polymer that ethyl acrylate, methyl methacrylate and methacrylic acid chlorination trimethylamine groups ethyl ester are formed.
Swellability and the permeability of quaternary amine group content decision coating in water.The quaternary amine group content is lower in the quaternary amine ylmethyl acrylate copolymer Type B, and permeability and swellability are less, and the coating of its formation effectively blocking medicine discharges; The quaternary amine group content is higher in the quaternary amine ylmethyl acrylate copolymer A type, and permeability and swellability are bigger, can be used with quaternary amine ylmethyl acrylate copolymer Type B, regulates the rate of releasing drug of coated preparation.Drug main will discharge by the hydrophilic duct diffusion that coating quaternary amine group forms.
Slow releasing tablet preparation method provided by the present invention is as follows:
(1) cyclopenthiazide is dissolved in an amount of ethanol, evenly mixed with potassium chloride.
(2) add the binding agent for preparing by quaternary amine ylmethyl acrylate copolymer Type B slow-release material
[1]In right amount, 40-50 ℃ of oven dry, behind the 12-20 mesh sieve, the binding agent that continues the preparation of adding quaternary amine ylmethyl acrylate copolymer Type B slow-release material is an amount of, 40-50 ℃ of oven dry excessively.Control label weight is 450-500mg.
(3) arrangement, interpolation recipe quantity antiplastering aid, tabletting.
(4) use the common coating solution that disposes of quaternary amine ylmethyl acrylate copolymer A type and Type B slow-release material
[2]Carry out coating.The coating weightening finish is 1%-20%.
[1] preparation of binding agent: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is dissolved in recipe quantity 95% ethanol, the recipe quantity plasticizer is dissolved in the prescription water gaging (heating hydrotropy).Its aqueous solution is added in the quaternary amine ylmethyl acrylate copolymer Type B alcoholic solution, stirred 30 minutes, promptly.
[2] preparation of coating solution: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B and quaternary amine ylmethyl acrylate copolymer A type are dissolved in part 95% ethanol, the plasticizer of recipe quantity is dissolved in the prescription water gaging (heating hydrotropy).Its aqueous solution is added in quaternary amine ylmethyl acrylate copolymer Type B and the quaternary amine ylmethyl acrylate copolymer A type alcoholic solution, stirred 30 minutes.With the antiplastering aid mixing in the residue ethanol in.Suspension is added in the above-mentioned solution, stirred 10 minutes, also can add an amount of opacifier, promptly.
Use the quaternary amine ylmethyl acrylate copolymer A type and the quaternary amine ylmethyl acrylate copolymer Type B of different proportion to prepare coating solution, can adjust the coating weightening finish, make drug release stably under the prerequisite, prescription is easy to commercial production.
The present invention uses the method for secondary wet-granulation, and slow-release material is added in the label uniformly, makes drug release steady when reducing supplementary product consumption.When alleviating edema and hypertension symptom, can slowly replenish potassium ion, thereby reduce the side effect of diuretic by diuretic.Reduce the fluctuation of concentration of potassium ion in patient's medicining times, the minimizing blood, prevented the generation of side effect such as hyperkalemia.Make things convenient for clinical practice, increase patient's compliance.Used the solvent of 95% ethanol as coating solution, safer than other organic solvents uses, make things convenient for commercial production.
By cyclopenthiazide tablet explanation as can be known, the cyclopenthiazide oral absorption is complete, and diuresis starts from after the medication 1～2 hour, about 12 hours effect peakings, and effect continues 24～36 hours.Because using in the label, this patent do not contain water-soluable gel, the time lag phenomenon that the potassium chloride release in vitro causes when not existing owing to the gel aquation, and rapid-action.Replenish because the interior potassium ion of the body that the application diuretic causes runs off in good time.Slowly release behavior is sustainable 8 hours.The release in vitro curve is steady and complete.
The mensuration that external potassium chloride discharges: according to drug release determination method (two appendix X of Chinese Pharmacopoeia version in 2000 D, first method), adopt the device of dissolution method first method, with water 500ml is solvent, rotating speed is that per minute 100 changes, operation in accordance with the law, through 2 hours, got solution 15ml in 4 hours and 8 hours respectively, filter, and additional simultaneously uniform temp, the water of equal volume, precision is measured subsequent filtrate 10ml, add water 10ml, add mixed indicator (get the 0.5g diphenylcarbazone and the 0.05g bromophenol blue is dissolved in the 100ml ethanol) 1ml, transfer to after solution becomes yellow by blueness with 1% salpeter solution, add the about 1ml of 1% salpeter solution (regulating pH value to 3.3) again, change rose with mercuric nitrate complexometry liquid (0.005mol/L) volumetric soiutions into by yellow, and titration results is proofreaied and correct with blank assay, every 1ml mercuric nitrate complexometry liquid (0.005mol/L) is equivalent to the KCl of 0.7455mg, calculates every burst size at different time respectively.
The specific embodiment
Embodiment 1
[prescription is formed] 1000
The component name weighs
Potassium chloride 450g
Cyclopenthiazide 0.125g
Quaternary amine ylmethyl acrylate copolymer Type B adhesive 250g
Magnesium stearate 2.4g
Quaternary amine ylmethyl acrylate copolymer A type 21g
Quaternary amine ylmethyl acrylate copolymer Type B 9g
PEG6000 3g
Pulvis Talci 7.5g
Water 3g
Ethanol (95%) 456.5g
Quaternary amine ylmethyl acrylate copolymer Type B 30g
PEG6000 3g
Water 3g
Ethanol (95%) 214g
(1) recipe quantity potassium chloride was pulverized 100 mesh sieves, the recipe quantity cyclopenthiazide is dissolved in the 50ml ethanol.With the cyclopenthiazide alcoholic solution to add in the 100 order potassium chloride powder stirring and evenly mixing.
(2) with the binding agent of half recipe quantity
[1]Add in the above-mentioned powder 40 order system wet granulars, 40 ℃ of oven dry, 20 order granulate.The recipe quantity adhesive be will remain and 20 order system wet granulars, 40 ℃ of oven dry, 18 order granulate added in the granule of oven dry back.
(3) add the magnesium stearate of recipe quantity, mixing, tabletting.
(4) use coating solution
[2]Carry out coating, the coating weightening finish is the 4%-5% of label weight.
[1] preparation of binding agent: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is dissolved in recipe quantity 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in the quaternary amine ylmethyl acrylate copolymer Type B alcoholic solution, stirred 30 minutes, promptly.
[2] preparation of coating solution: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B and quaternary amine ylmethyl acrylate copolymer A type are dissolved in 400g 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in quaternary amine ylmethyl acrylate copolymer Type B and the quaternary amine ylmethyl acrylate copolymer A type alcoholic solution, stirred 30 minutes.With the Pulvis Talci mixing in the residue ethanol in.Suspension is added in the above-mentioned solution, stirred 10 minutes, promptly.
Adopt conventional film-coated technique to carry out, the coating weightening finish is controlled at the 4%-5% of label weight.
The different coating weightening finish of table 1 different time accumulative total discharges percentage ratio
Embodiment 2
Potassium chloride 450g
Cyclopenthiazide 0.125g
Quaternary amine ylmethyl acrylate copolymer Type B adhesive 250g
Magnesium stearate 2.4g
Quaternary amine ylmethyl acrylate copolymer A type 24g
Quaternary amine ylmethyl acrylate copolymer Type B 6g
PEG6000 3g
Pulvis Talci 7.5g
Water 3g
Ethanol (95%) 456.5g
Quaternary amine ylmethyl acrylate copolymer Type B 30g
PEG6000 3g
Water 3g
Ethanol (95%) 214g.
(1) recipe quantity potassium chloride was pulverized 100 mesh sieves, the recipe quantity cyclopenthiazide is dissolved in the 50ml ethanol.With the cyclopenthiazide alcoholic solution to add in the 100 order potassium chloride powder stirring and evenly mixing.
(2) with the binding agent of half recipe quantity
[1]Add in the above-mentioned powder 40 order system wet granulars, 40 ℃ of oven dry, 20 order granulate.The recipe quantity adhesive be will remain and 20 order system wet granulars, 40 ℃ of oven dry, 18 order granulate added in the granule of oven dry back.
(3) add the magnesium stearate of recipe quantity, mixing, tabletting.
(4) use coating solution
[2]Carry out coating, the coating weightening finish is the 5%-6% of label weight.
[1] preparation of binding agent: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is dissolved in recipe quantity 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in the quaternary amine ylmethyl acrylate copolymer Type B alcoholic solution, stirred 30 minutes, promptly.
[2] preparation of coating solution: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B and quaternary amine ylmethyl acrylate copolymer A type are dissolved in 400g 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in quaternary amine ylmethyl acrylate copolymer Type B and the quaternary amine ylmethyl acrylate copolymer A type alcoholic solution, stirred 30 minutes.With the Pulvis Talci mixing in the residue ethanol in.Suspension is added in the above-mentioned solution, stirred 10 minutes, promptly.
Adopt conventional film-coated technique to carry out, the coating weightening finish is controlled at the 5%-6% of label weight.
The different coating weightening finish of table 2 different time accumulative total discharges percentage ratio
Embodiment 3
Potassium chloride 450g
Cyclopenthiazide 0.125g
Quaternary amine ylmethyl acrylate copolymer Type B adhesive 250g
Magnesium stearate 2.4g
Quaternary amine ylmethyl acrylate copolymer A type 27g
Quaternary amine ylmethyl acrylate copolymer Type B 3g
PEG6000 3g
Pulvis Talci 7.5g
Water 3g
Ethanol (95%) 456.5g
Quaternary amine ylmethyl acrylate copolymer Type B 30g
PEG6000 3g
Water 3g
Ethanol (95%) 214g
(1) recipe quantity potassium chloride was pulverized 100 mesh sieves, the recipe quantity cyclopenthiazide is dissolved in the 50ml ethanol.With the cyclopenthiazide alcoholic solution to add in the 100 order potassium chloride powder stirring and evenly mixing.
(2) with the binding agent of half recipe quantity
[1]Add in the above-mentioned powder 40 order system wet granulars, 40 ℃ of oven dry, 20 order granulate.The recipe quantity adhesive be will remain and 20 order system wet granulars, 40 ℃ of oven dry, 18 order granulate added in the granule of oven dry back.
(3) add the magnesium stearate of recipe quantity, mixing, tabletting.
(4) use coating solution
[2]Carry out coating, the coating weightening finish is the 6%-7% of label weight.
[1] preparation of binding agent: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is dissolved in recipe quantity 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in the quaternary amine ylmethyl acrylate copolymer Type B alcoholic solution, stirred 30 minutes, promptly.
[2] preparation of coating solution: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B and quaternary amine ylmethyl acrylate copolymer A type are dissolved in 400g 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in quaternary amine ylmethyl acrylate copolymer Type B and the quaternary amine ylmethyl acrylate copolymer A type alcoholic solution, stirred 30 minutes.With the Pulvis Talci mixing in the residue ethanol in.Suspension is added in the above-mentioned solution, stirred 10 minutes, promptly.
Adopt conventional film-coated technique to carry out, the coating weightening finish is controlled at the 6%-7% of label weight.
The different coating weightening finish of table 3 different time accumulative total discharges percentage ratio
Embodiment 4
Potassium chloride 450g
Cyclopenthiazide 0.125g
Quaternary amine ylmethyl acrylate copolymer Type B adhesive 250g
Magnesium stearate 2.4g
Quaternary amine ylmethyl acrylate copolymer A type 30g
PEG6000 3g
Pulvis Talci 7.5g
Water 3g
Ethanol (95%) 456.5g
Quaternary amine ylmethyl acrylate copolymer Type B 30g
PEG6000 3g
Water 3g
Ethanol (95%) 214g
(1) recipe quantity potassium chloride was pulverized 100 mesh sieves, the recipe quantity cyclopenthiazide is dissolved in the 50ml ethanol.With the cyclopenthiazide alcoholic solution to add in the 100 order potassium chloride powder stirring and evenly mixing.
(2) with the binding agent of half recipe quantity
[1]Add in the above-mentioned powder 40 order system wet granulars, 40 ℃ of oven dry, 20 order granulate.The recipe quantity adhesive be will remain and 20 order system wet granulars, 40 ℃ of oven dry, 18 order granulate added in the granule of oven dry back.
(3) add the magnesium stearate of recipe quantity, mixing, tabletting.
(4) use coating solution
[2]Carry out coating, the coating weightening finish is the 8%-10% of label weight.
[1] preparation of binding agent: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is dissolved in recipe quantity 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in the quaternary amine ylmethyl acrylate copolymer Type B alcoholic solution, stirred 30 minutes, promptly.
[2] preparation of coating solution: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B and quaternary amine ylmethyl acrylate copolymer A type are dissolved in 400g 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in quaternary amine ylmethyl acrylate copolymer Type B and the quaternary amine ylmethyl acrylate copolymer A type alcoholic solution, stirred 30 minutes.With the Pulvis Talci mixing in the residue ethanol in.Suspension is added in the above-mentioned solution, stirred 10 minutes, promptly.
Adopt conventional film-coated technique to carry out, the coating weightening finish is controlled at the 8%-10% of label weight.
The different coating weightening finish of table 4 different time accumulative total discharges percentage ratio
Embodiment 5
Potassium chloride 450g
Cyclopenthiazide 0.125g
Quaternary amine ylmethyl acrylate copolymer Type B adhesive 250g
Magnesium stearate 2.4g
Quaternary amine ylmethyl acrylate copolymer Type B 30g
PEG6000 3g
Pulvis Talci 7.5g
Water 3g
Ethanol (95%) 456.5g
Quaternary amine ylmethyl acrylate copolymer Type B 30g
PEG6000 3g
Water 3g
Ethanol (95%) 214g
(1) recipe quantity potassium chloride was pulverized 100 mesh sieves, the recipe quantity cyclopenthiazide is dissolved in the 50ml ethanol.With the cyclopenthiazide alcoholic solution to add in the 100 order potassium chloride powder stirring and evenly mixing.
(2) with the binding agent of half recipe quantity
[1]Add in the above-mentioned powder 40 order system wet granulars, 40 ℃ of oven dry, 20 order granulate.The recipe quantity adhesive be will remain and 20 order system wet granulars, 40 ℃ of oven dry, 18 order granulate added in the granule of oven dry back.
(3) add the magnesium stearate of recipe quantity, mixing, tabletting.
(4) use coating solution
[2]Carry out coating, the coating weightening finish is the 8%-10% of label weight.
The preparation of binding agent: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is dissolved in recipe quantity 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in the quaternary amine ylmethyl acrylate copolymer Type B alcoholic solution, stirred 30 minutes, promptly.
The preparation of coating solution: recipe quantity quaternary amine ylmethyl acrylate copolymer Type B and quaternary amine ylmethyl acrylate copolymer A type are dissolved in 400g 95% ethanol, recipe quantity PEG6000 is dissolved in the prescription water gaging (heating hydrotropy).The PEG6000 aqueous solution is added in quaternary amine ylmethyl acrylate copolymer Type B and the quaternary amine ylmethyl acrylate copolymer A type alcoholic solution, stirred 30 minutes.With the Pulvis Talci mixing in the residue ethanol in.Suspension is added in the above-mentioned solution, stirred 10 minutes, promptly.
The preparation of label: recipe quantity potassium chloride was pulverized 100 mesh sieves, and the recipe quantity cyclopenthiazide is dissolved in the 50ml ethanol.With the cyclopenthiazide alcoholic solution to add in the 100 order potassium chloride powder stirring and evenly mixing.The alcoholic solution of half recipe quantity quaternary amine ylmethyl acrylate copolymer Type B is added in the above-mentioned powder 40 order system wet granulars, 40 ℃ of oven dry, 20 order granulate.The recipe quantity adhesive be will remain and 20 order system wet granulars, 40 ℃ of oven dry, 18 order granulate added in the granule of oven dry back.Add magnesium stearate, mixing.Tabletting.Coating promptly.The coating weightening finish is the 8%-10% of label weight.
Adopt conventional film-coated technique to carry out, the coating weightening finish is controlled at the 8%-10% of label weight.
The different coating weightening finish of table 5 different time accumulative total discharges percentage ratio
Claims (7)
1. potassium chloride cyclopenthiazide slow releasing tablet, its prescription is:
(1) potassium chloride 450g
(2) cyclopenthiazide 0.125g
(3) quaternary amine ylmethyl acrylate copolymer A type 10-40 g
(4) quaternary amine ylmethyl acrylate copolymer Type B 10-50g
(5) water 1-20g
(6) ethanol (95%) 400-1000g
(7) plasticizer 4-10g
(8) antiplastering aid 5-50g.
2. potassium chloride cyclopenthiazide slow releasing tablet as claimed in claim 1 is characterized in that adding opacifier.
3. as according to the described potassium chloride cyclopenthiazide of claim 1 slow releasing tablet, it is characterized in that label and slow-release material weight ratio are 15:1 to 10:1.
4. potassium chloride cyclopenthiazide slow releasing tablet as claimed in claim 1 is characterized in that the mixture of quaternary amine ylmethyl acrylate copolymer A type, quaternary amine ylmethyl acrylate copolymer Type B or two kinds of macromolecular materials of coating material different proportion.
5. potassium chloride cyclopenthiazide slow releasing tablet according to claim 1, it is characterized in that plasticizer is selected from glycerol, propylene glycol, Oleum Ricini or derivatives thereof, monoacetin, triacetin, triethyl citrate, Macrogol 200-6000, tributyl citrate and decanedioic acid two fourths (second) ester, phthalic acid two fourths (second) ester, or its arbitrary composition.
6. potassium chloride cyclopenthiazide slow releasing tablet according to claim 1 is characterized in that antiplastering aid is selected from Pulvis Talci, magnesium stearate, glyceryl monostearate, micropowder silica gel, or its arbitrary composition.
7. method for preparing potassium chloride cyclopenthiazide slow releasing tablet as claimed in claim 1 is characterized in that preparation technology is as follows:
(1) cyclopenthiazide is used 95% dissolve with ethanol, sneaked in the potassium chloride;
(2) label is blocked the alcoholic solution that slow-release material is configured to recipe quantity, adds plasticizer, with the potassium chloride cyclopenthiazide mixing species of (1) preparation, through twice wet granulation.
(3) oven dry, arrangement, interpolation recipe quantity magnesium stearate, tabletting;
(4) coating.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106466302A (en) * | 2015-08-14 | 2017-03-01 | 深圳澳美制药技术开发有限公司 | Oral potassium chloride slow releasing tablet and preparation method thereof |
| CN110124099A (en) * | 2019-06-14 | 2019-08-16 | 四川涑爽医疗用品有限公司 | A kind of compounding periodontal pack of long-acting bacteriostatic and preparation method thereof |
| CN110251472A (en) * | 2019-08-01 | 2019-09-20 | 广州誉东健康制药有限公司 | It is a kind of to produce modified-release tablets of potassium chloride method using hot melt sustained release technique |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1478467A (en) * | 2003-06-28 | 2004-03-03 | 南昌弘益科技有限公司 | Rapid disintegrate tablet in oral and its preparation method |
| CN1891218A (en) * | 2005-07-04 | 2007-01-10 | 齐鲁制药有限公司 | Ranolazine hydrochloride slow-release preparation and its preparing method |
-
2011
- 2011-04-18 CN CN201110096136A patent/CN102144986B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1478467A (en) * | 2003-06-28 | 2004-03-03 | 南昌弘益科技有限公司 | Rapid disintegrate tablet in oral and its preparation method |
| CN1891218A (en) * | 2005-07-04 | 2007-01-10 | 齐鲁制药有限公司 | Ranolazine hydrochloride slow-release preparation and its preparing method |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106466302A (en) * | 2015-08-14 | 2017-03-01 | 深圳澳美制药技术开发有限公司 | Oral potassium chloride slow releasing tablet and preparation method thereof |
| CN106466302B (en) * | 2015-08-14 | 2021-05-25 | 深圳澳美制药技术开发有限公司 | Oral potassium chloride sustained release tablet and preparation method thereof |
| CN110124099A (en) * | 2019-06-14 | 2019-08-16 | 四川涑爽医疗用品有限公司 | A kind of compounding periodontal pack of long-acting bacteriostatic and preparation method thereof |
| CN110251472A (en) * | 2019-08-01 | 2019-09-20 | 广州誉东健康制药有限公司 | It is a kind of to produce modified-release tablets of potassium chloride method using hot melt sustained release technique |
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|---|---|
| CN102144986B (en) | 2012-10-17 |
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