CN1207294A - Potassium and magnesium controlled-release tablet and producing method thereof - Google Patents

Potassium and magnesium controlled-release tablet and producing method thereof Download PDF

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Publication number
CN1207294A
CN1207294A CN 97109186 CN97109186A CN1207294A CN 1207294 A CN1207294 A CN 1207294A CN 97109186 CN97109186 CN 97109186 CN 97109186 A CN97109186 A CN 97109186A CN 1207294 A CN1207294 A CN 1207294A
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China
Prior art keywords
magnesium
potassium
release
deionized water
controlled
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CN 97109186
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Chinese (zh)
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CN1090483C (en
Inventor
谢理峰
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Gong Xiaobing
Xie Lifeng
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Individual
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Abstract

A slow-released potassium-magnessium tablet for treating hypertension, arrhythmia and peptic ulcer contains 180-300 mg of K ions and 8-68 mg of Mg ions in each tablet and is prepared through proportioning, drying, mixing, press tabletting, preparing coating liquid, coating, preparing slow-releasing liquid, coating, drying and packing. Its advantages are increasing the concentrations of K and Mg ions in cells, speed-up tricarboxylic acid cycle, activating the cells, slow releasing, high utilization rate, no stimulation to mucosa in digestive tract and no environmental pollution during its production.

Description

Potassium magnesium controlled-release tablet and production method thereof
The present invention relates to the medicine of the release type that is surrounded by release membranes.
The potassium magnesium ion is an important electrolyte of keeping normal activities, and intracellular potassium ion accounts for 98%, and the extracellular only accounts for 1-2%.The normal human must keep this Concentraton gradient, and intravital biochemical process could normally be carried out.Potassium is first cation in the cell, and it shifts in cell is a contrary concentration difference transport process, must consumed energy.Magnesium is second largest cation in the cell, and it participates in the synthetic and metabolism of 300 plurality of enzymes, can also make the adenosine diphosphate (ADP) (ADP) of degraded be converted into adenosine triphosphate (ATP).With potassium magnesium ion compound recipe together, can quicken the potassium magnesium ion shifts in cell, improve intracellular potassium magnesium ion concentration, can keep the normal irritability of myocardial cell, self-disciplining and conductivity, intracellular calcium load be can reduce again, blood vessel, the normal excitation-contraction coupling of myocardial cell kept; Can also improve the activity of plurality of enzymes in the body, quicken tricarboxylic acid cycle, quicken to make adenosine diphosphate (ADP) be converted into adenosine triphosphate etc.Thereby make blood vessel, the unusual excitation-contraction coupling of myocardial cell recover normal and treatment hypertension; Make irritability, self-disciplining and the conductivity of myocardial cell recover normal and the treatment arrhythmia; Can also make the hydrogen-potassium exchange of parietal cell recover normal, make gastric acid secretion normally treat peptic ulcer.
Potassium ion is the very active electrolyte of a kind of metalline, and the potassium ion of high concentration has a tangible stimulation to gastrointestinal tract mucous, and the potassium ion of low concentration does not then have stimulation; The magnesium sulfate of high concentration has the effect that height oozes catharsis, reduces concentration and then can avoid, and can also improve bioavailability.Therefore must have slow-release function when requiring oral potassium magnesium ion, reduce instantaneous drug level, avoid above-mentioned side effect, to satisfy the physiological need of human body.
A kind of aspartic acid magnesium sheet is arranged at present, and it does not have slow-release function, and every contains 18.1 milligrams of potassium ions and 5.9 milligrams of magnesium ions, and human body need replenish potassium chloride 2-6 gram (about 1-3 gram potassium ion) every day, and the aspartic acid magnesium sheet is difficult to satisfy the needs of human body.
Guangzhou Xinghua Pharmaceutic Factory produces " Slow-K " of " benefit reaches show " and the production of Beijing Novartis, is the potassium chloride slow releasing tablet.It does not contain magnesium ion, merely is used for hypokalemia clinically.
A large amount of zooperies and clinical research show that hypokalemia often is accompanied by hypomagnesemia.Magnesium plays crucial effect in potassio is thanked, magnesium deficiency can cause potassium loss in the cell.Patient wants Mg supplementation ion simultaneously when replenishing potassium ion, could obviously improve intracellular potassium magnesium ion concentration.
The object of the present invention is to provide a kind of oral potassium magnesium controlled-release tablet that is surrounded by release membranes that supplies, every contains 180-300 milligram potassium ion and 8-68 milligram magnesium ion, can satisfy the needs of human body to the potassium magnesium ion.Owing to adopted slow release technology, reduced the instantaneous concentration of medicine, can in human body alimentary canal, discharge more lentamente, non-stimulated to the human body alimentary canal mucosa, avoided the magnesium sulfate height to ooze the effect of catharsis, improved bioavailability of medicament.Thereby improve intracellular potassium magnesium ion concentration simultaneously, reach the purpose of treatment hypertension, arrhythmia and peptic ulcer.
Technical scheme of the present invention realizes in the following manner:
The present invention is made up of label, basilar cloth film and release membranes.
Label includes material and the adjuvant that contains potassium ion, magnesium ion, its every label:
The content of potassium ion is: the 180-300 milligram
The content of magnesium ion is: the 8-68 milligram
Adjuvant: an amount of
Adjuvant can be magnesium stearate, zinc sulfate, hydroxypropyl methylcellulose etc.
Label can be made up of potassium chloride, magnesium sulfate and adjuvant; Can also form or potassium chloride, magnesium oxide and adjuvant are formed by potassium chloride, magnesium chloride and adjuvant.
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1-30%
(or II medical acrylic acid enteric resin)
Polyethylene Glycol 0.1-3.0%
Hydroxypropyl methylcellulose 0-3.0%
Deionized water 0-3.0%
Magnesium stearate 0-2.5%
Pulvis Talci 0-2.5%
Ethanol 60-96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1-40%
Polyethylene Glycol 0.1-3.0%
Pulvis Talci 1-16%
Magnesium stearate 0-10%
Tween 80 0-1.0%
Tris 0-1.0%
Deionized water 50-90%
Another object of the present invention is to provide the production method of potassium magnesium controlled-release tablet.
The present invention is after the material that will contain the material of potassium ion and contain magnesium ion mixes in 4: 1~5: 1 ratio drying, adds 0.4~0.5% magnesium stearate again by the weight of both mixture, and the three mixes the back and make label on tablet machine.Remove ionized water 0-3%, add hydroxypropyl methylcellulose 0-3%, dissolved about 24 hours; Getting in a small amount again, 95% ethanol adds Polyethylene Glycol 0.1-3%, be warmed up to and make it dissolving about 50 ℃, add medical No. 4 acrylic acid gastric solubleness resin 1-30% again, Pulvis Talci 0-2.5%, magnesium stearate 0-2.5% gets 60-96% ethanol at last as solvent, and is interrupted concussion, after it is fully dissolved, with above-mentioned two kinds of solution mixing promptly becoming basilar cloth liquid.Basilar cloth liquid is sprayed on the label, label is wrapped one deck basilar cloth film again.
And then bag release membranes and produce and be finished medicines or nutrition sheet.Getting in a small amount, deionized water adds Polyethylene Glycol 0.1-3%, be warmed up to about 50 ℃, and then add 1-16% Pulvis Talci, the tween 80 of 0-1%, add deionized water and stirring in a small amount again, and add acrylic resin latex 1-40% simultaneously, and add deionized water again, three times adding deionized water 50-90% stirs, simultaneously, also must regulate pH value and become sustained-release liquid to 6.5-7, sustained-release liquid is sprayed on the label that is surrounded by basilar cloth film again, promptly become finished product with the 0.01-1% Tris.
At last with medicine bottle or aluminum-plastic packaged.
Advantage of the present invention is as follows:
1. because the material great majority that contain the material of potassium ion and contain magnesium ion all are the neutral chemical salt of selecting for use.PH value to human body does not have direct influence; They can quicken potassium, magnesium ion shifts in human body cell, thereby potassium, magnesium ion concentration in the raising human body cell, the circulation of acceleration tri hydroxy acid, the biological activity intensity of recovery human body cell reaches the purpose for the treatment of hypertension, arrhythmia and peptic ulcer.
2. the present invention has adopted slow release technology, has covered the adverse drug taste, has reduced the instantaneous concentration of medicine, can discharge more lentamente in human body alimentary canal, has avoided the magnesium sulfate height to ooze the effect of catharsis, and has improved bioavailability of medicament; Non-stimulated to the human body alimentary canal mucosa.
3. basilar cloth film of the present invention and release membranes are nontoxic polymer substance, and be simple to operate in the production process, do not have environmental pollution.
4. the present invention is the powder direct compression, has saved granulation process, and the shortening of coating time, thereby the energy energy savings, improves work efficiency, increases output.
5. the present invention is for oral protracted release drug or slow-release nutrient sheet, so patient or non-patient's taking convenience.
In conjunction with the embodiments, the invention will be further described:
Embodiment 1:
Potassium chloride 1Kg is put into temperature be controlled at drying baker inner drying 10-30 minute about 70 ℃, the magnesium sulfate 0.2Kg that contains 7 water of crystallization puts into vacuum drying oven, temperature is controlled at about 70-90 ℃, negative pressure is about 0.08mPA dry 10-30 minute, make it take off partially crystallizable water, pulverize after cooling.Mix with the magnesium sulfate after above-mentioned dried potassium chloride and the drying and crushing then, add the 4.5g magnesium stearate again, on tablet machine, be pressed into label behind three's mix homogeneously.
Preparation basilar cloth liquid: remove the about 10ml adding of ionized water hydroxypropyl methylcellulose 2.5g and dissolved about 24 hours; Get 95% ethanol 20ml, add Polyethylene Glycol 4.0g, be warmed up to about 50 ℃, make the Polyethylene Glycol dissolving; Add medical IV acrylic acid gastric solubleness resin 25g again, 1% Pulvis Talci and 1% magnesium stearate add to 490ml as solvent with 95% ethanol, and are interrupted vibration, allow its medical IV acrylic acid gastric solubleness resin fully dissolve about 24 hours in ethanol; Then above-mentioned two liquid are mixed, can use.
The sub-coating film; Label is put into coating pan, and ceaselessly rotates coating pan and add 40-50 ℃ hot blast, treat the label preheating after, with spray gun basilar cloth liquid is sprayed on the sheet wicking surface, make every label wrap one deck basilar cloth film.
Preparation release membranes liquid: remove the about 100ml of ionized water, add Polyethylene Glycol 16g, be warmed up to about 50 ℃, make the Polyethylene Glycol dissolving; Add Pulvis Talci 120g and 2g tween 80 then, add the about 300ml of deionized water, stir, slowly add 400ml acrylic resin latex simultaneously, add deionized water again, stir, regulate with trihydroxy methyl chloro methane then, make liquid pH value 6.5-7.0 to 2000ml.
The bag release membranes: the label that will wrap basilar cloth film still is placed in the coating pan, and ceaselessly rotates coating pan and add 40-50 ℃ hot blast, changes spray gun, with spray gun release membranes liquid is sprayed on the sheet wicking surface, makes every label wrap in one deck release membranes.Blow a cold wind over again after waiting to dry, make the temperature of tablet be reduced to room temperature.
Dry: above-mentioned tablet is put into drying baker, and 37-50 ℃ of control temperature dry 12-16 hour, is finished product.
Packing: the finished product of potassium magnesium controlled-release tablet is divided in the medicine bottle or in aluminum-plastic packaged routinely.
Embodiment 2:
Clinical efficacy of the present invention:
The potassium magnesium controlled-release tablet, every 600 milligrams (containing 500 milligrams in potassium chloride, 100 milligrams in sulfur acid magnesium).
Case (1): Lee * *, the man, 58 years old, suffered from hypertension 1 year, oral always " captopril ", blood pressure can be reduced to normal range.But spirit is poor, and sense is dizzy, limbs fatigue, and after the drug withdrawal, blood pressure rises to 160/105mmHg again once in a while, and electrocardio illustrates the artrial premature beat that takes place frequently, ventricular premature contraction.After this change 4 of clothes " potassium magnesium controlled-release tablet " every day, add " nifedipine " 20 milligrams.The back spirit improvement of 1 week, the check electrocardiogram, arrhythmia disappears, and blood pressure is reduced to 120/80mmHg.Withdraw " nifedipine " after January, 4 of every days still oral " potassium magnesium controlled-release tablet ", spirit takes a turn for the better, no giddy and limbs fatigue, and blood pressure is normal.Over nearly 2 years, be interrupted and take the potassium magnesium controlled-release tablet, blood pressure is normal always, the not normal generation of the no rhythm of the heart.
Case (2): the king * *, the woman, 46 years old, suffer from surplus the hypertension 10 year, oral always " FUFANG JIANGYA PIAN ", blood pressure can be reduced to 130-140/105-110mmHg.Spirit is poor, and sense is dizzy, and left limb is weak.After this add " potassium magnesium controlled-release tablet " 4 every day, the back spirit improvement of 1 week, the dizzy and weak disappearance of left limb.Withdraw " FUFANG JIANGYA PIAN " after January, 4 of every days still oral " potassium magnesium controlled-release tablet ", spirit takes a turn for the better, no giddy and limbs fatigue, and blood pressure is normal.Closely over the past half year, be interrupted and take the potassium magnesium controlled-release tablet, blood pressure is normal always, the not normal generation of the no rhythm of the heart.
Case (3): Lee * *, the man, 53 years old, suffered from hypertension 17 years, once oral " captopril ", " nifedipine ", " benazepril ", blood pressure can be reduced to normal range.Closely over the past half year, " nifedipine " every day to 60 milligram, blood pressure still is 180/130mmHg, and spirit is poor, and the sense giddy is weak.After this add " potassium magnesium controlled-release tablet " 4 every day, containing " nifedipine " is 10 milligrams after 3 days, the blood pressure 30mHg that can descend in 10 minutes.4 of existing every days oral " potassium magnesium controlled-release tablet " and " nifedipine " 10-20 milligram, blood pressure is built in about 125-135/95-100mmHg, and is in high spirits, no giddy and limbs fatigue.
Case (4): old * *, the man, 46 years old, upper abdomen dull pain 6 years, pain increased the weight of 3 days, and the companion returns acid, no melena.Gulp down the barium inspection and show the coat of the stomach niche, be diagnosed as gastric ulcer.Take " potassium magnesium controlled-release tablet " 4 every day, pain relief after 3 days, the back pain disappearance of 1 week gulps down the barium check after 8 weeks, and the coat of the stomach niche disappears.

Claims (6)

1. a potassium magnesium controlled-release tablet is made up of label, basilar cloth film and release membranes, it is characterized in that: label includes the material and the adjuvant that contain potassium ion, magnesium ion and forms its every label:
The content of potassium ion is: the 180-300 milligram
The content that magnesium is heard son is: the 8-68 milligram
Adjuvant: an amount of
The component of basilar cloth film and percentage by weight are:
Medical IV acrylic acid gastric solubleness resin 1-30%
Polyethylene Glycol 0.1-3.0%
Hydroxypropyl methylcellulose 0-3.0%
Deionized water 0-3.0%
Magnesium stearate 0-2.5%
Pulvis Talci 0-2.5%
Ethanol 60-96%
The component of release membranes and percentage by weight are:
Acrylic resin latex 1-40%
Polyethylene Glycol 0.1-3.0%
Pulvis Talci 1-16%
Magnesium stearate 0-10%
Tween 80 0-1.0%
Tris 0-1.0%
Deionized water 50-90%
2. potassium magnesium controlled-release tablet according to claim 1 is characterized in that: label can be made up of potassium chloride, magnesium sulfate and adjuvant; Or form by potassium chloride, magnesium oxide and adjuvant; Or form by potassium chloride, magnesium chloride and adjuvant.
3. potassium magnesium controlled-release tablet production method is characterized in that: batching-drying-mixing-tabletting core-join basilar cloth liquid-sub-coating film-join sustained-release liquid-bag release membranes-drying-finished product-packing.
4. potassium magnesium controlled-release tablet production method according to claim 3, it is characterized in that: raw material by potassium chloride, magnesium sulfate or potassium chloride, magnesium chloride in 4: 1~5: 1 ratio dry mixed after, on tablet machine, make label after adding 0.4~0.5% magnesium stearate mix homogeneously by the weight of mixture again.
5. potassium magnesium controlled-release tablet production method according to claim 3 is characterized in that: remove ionized water 0-3%, add hydroxypropyl methylcellulose 0-3%, dissolved about 24 hours; Getting in a small amount again, 95% ethanol adds Polyethylene Glycol 0.1-3%, be warmed up to and make it dissolving about 50 ℃, add medical No. 4 acrylic acid gastric solubleness resin 1-30% again, Pulvis Talci 0-2.5%, stearyl ester magnesium 0-2.5% gets 60-96% ethanol at last as solvent, and is interrupted concussion 24 hours, after it was fully dissolved, above-mentioned two kinds mixed solution promptly became basilar cloth liquid.
6. potassium magnesium ion slow releasing tablet production method according to claim 3, it is characterized in that: getting in a small amount, deionized water adds Polyethylene Glycol 0.1-3%, be warmed up to about 50 ℃, and then adding the 1-6% Pulvis Talci, the tween 80 of 0-1% adds deionized water and stirring in a small amount again, and add acrylic resin latex 1-40% simultaneously, add deionized water again, three times adding deionized water 50-90% stirs, and regulates pH value to 6.5-7 with the 0-1% Tris then.
CN97109186A 1997-07-31 1997-07-31 Potassium and magnesium controlled-release tablet and producing method thereof Expired - Fee Related CN1090483C (en)

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Application Number Priority Date Filing Date Title
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CN1090483C CN1090483C (en) 2002-09-11

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2448413A1 (en) * 2009-07-01 2012-05-09 Magceutics, Inc. Slow release magnesium composition and uses thereof
CN103006696A (en) * 2012-12-27 2013-04-03 上海海虹实业(集团)巢湖今辰药业有限公司 Preparation method of potassium chloride sustained-release tablet
US8470352B2 (en) 2007-03-22 2013-06-25 Magceutics, Inc. Magnesium compositions and uses thereof for metabolic disorders
US10251909B2 (en) 2007-02-09 2019-04-09 Board Of Regents, The University Of Texas System Potassium-magnesium citrate as a surrogate of the DASH diet in managing hypertension
CN116420877A (en) * 2022-08-11 2023-07-14 郭志福 NMN, potassium, magnesium and selenium composition nutrition tablet and preparation method thereof

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100398122C (en) * 2005-01-28 2008-07-02 北京北大药业有限公司 Enteric coated Chinese medicine composition for treating cervical and lumbar spondylopathy

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH677612A5 (en) * 1987-09-11 1991-06-14 Ciba Geigy Ag
IE60383B1 (en) * 1988-05-27 1994-07-13 Elan Corp Plc Controlled release pharmaceutical formulation
CN1108535A (en) * 1994-09-20 1995-09-20 广州市红十字会医院 Heart basal liquid and preparation technology thereof

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10251909B2 (en) 2007-02-09 2019-04-09 Board Of Regents, The University Of Texas System Potassium-magnesium citrate as a surrogate of the DASH diet in managing hypertension
US9125878B2 (en) 2007-03-22 2015-09-08 Magceutics, Inc. Magnesium compositions and uses thereof for neurological disorders
US9757414B2 (en) 2007-03-22 2017-09-12 Neurocentria, Inc. Magnesium compositions and uses thereof for neurological disorders
US9737563B2 (en) 2007-03-22 2017-08-22 Neurocentria, Inc. Magnesium compositions and uses thereof for neurological disorders
US8470352B2 (en) 2007-03-22 2013-06-25 Magceutics, Inc. Magnesium compositions and uses thereof for metabolic disorders
US8637061B2 (en) 2007-03-22 2014-01-28 Magceutics, Inc. Magnesium compositions and uses thereof for neurological disorders
US9616038B2 (en) 2007-03-22 2017-04-11 Neurocentria, Inc. Magnesium compositions and uses thereof for neurological disorders
US8734855B2 (en) 2009-07-01 2014-05-27 Magceutics, Inc. Slow release magnesium composition and uses thereof
CN102573496B (en) * 2009-07-01 2015-08-26 玛格塞蒂克斯公司 Slow release magnesium composition and uses thereof
EP2448413A1 (en) * 2009-07-01 2012-05-09 Magceutics, Inc. Slow release magnesium composition and uses thereof
EP2448413A4 (en) * 2009-07-01 2013-02-13 Magceutics Inc Slow release magnesium composition and uses thereof
CN102573496A (en) * 2009-07-01 2012-07-11 玛格塞蒂克斯公司 Slow release magnesium composition and uses thereof
CN103006696A (en) * 2012-12-27 2013-04-03 上海海虹实业(集团)巢湖今辰药业有限公司 Preparation method of potassium chloride sustained-release tablet
CN116420877A (en) * 2022-08-11 2023-07-14 郭志福 NMN, potassium, magnesium and selenium composition nutrition tablet and preparation method thereof

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