CN105596348A - Hydrochlorothiazide compound sustained-release tablet and preparation method - Google Patents
Hydrochlorothiazide compound sustained-release tablet and preparation method Download PDFInfo
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- CN105596348A CN105596348A CN201510641548.9A CN201510641548A CN105596348A CN 105596348 A CN105596348 A CN 105596348A CN 201510641548 A CN201510641548 A CN 201510641548A CN 105596348 A CN105596348 A CN 105596348A
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Abstract
The invention discloses a hydrochlorothiazide compound sustained-release tablet and a preparation method. The sustained-release tablet comprises the following components by weight: 30-50 parts of hydrochlorothiazide, 35-45 parts of potassium citrate, 120-150 parts of a diluent, 80-120 parts of a disintegration agent, 10-15 parts of a surfactant, 80-150 parts of a sustained-release material, and 10-15 parts of a lubricant. The preparation method of the sustained-release tablet includes material preparation, granulation and tabletting. According to the invention, hydrochlorothiazide and potassium citrate are made into the compound sustained-release tablet, which not only has high drug effective proportion, is convenient for medication, but also realizes lasting and slow drug release in vivo, the blood concentration is stable and has small fluctuation, thus having certain protection to organs of patients. The hydrochlorothiazide compound sustained-release tablet not only improves patient compliance, but also increases the survival rate of medicated patients, reduces the cost of accessories and packaging, and is conducive to mass production.
Description
Technical field
The invention belongs to medical technical field, particularly a kind of hydrochlorothiazide Compound sustained release tablets and preparation method.
Background technology
Hydrochioro is diuretics, antihypertensive. Mainly be applicable to cardiac edema, hepatic edema andRenal edema, as nephrotic syndrome, acute glomerulonephritis, chronic renal failure and adrenal cortexOedema, hypertension, urine spring disease that hormone and hyperestrogenism cause.
Hydrochioro is oral, and rapidly but incomplete, bioavilability is 60～80%, and feed can increase uptake,May extend relevant in the holdup time of small intestine with medicine. After oral 2h, produce diuresis, peak time is4h, produces hypotensive effect after 3～6h, acting duration is 6～12h. This medicine part is combined with plasma protein,Protein binding rate is 40%, and another part enters in cell, placenta. After absorbing, this medicine eliminates phase incipient stage bloodLiquid concentration declines very fast, and later blood concentration declines and obviously slows down, and may be because after-stage medicine enters redRelevant in cell, mainly with original shape by homaluria. This product half-life T1/2 is 15h, congestive heart failure,Impaired renal function person extends. This product 50～70% is discharged by urine with original shape, also can be through galactosis.
Hydrochioro mechanism of drug action mainly suppresses distal tubule leading portion and proximal tubule (acting on lighter) is rightThe suction of sodium chloride is received, thereby increases the Na of distal tubule and concetrated pipe+-K+Exchange, K+Secretion increasing. LongThe appropriate to the occasion sylvite that suitably supplements of phase application. Take inconvenience, compressing tablet supplementary product consumption is relatively many separately, is packaged intoThis height, not only facilitates medication after therefore two kinds or two or more medicines being made to compound preparation, and reducesAuxiliary material and packing cost, be conducive to large production.
Summary of the invention
The present invention seeks to, in order to overcome the defect of two kinds or two or more Drug combinations, to propose oneKind can diuresis, antihypertensive medicament sustained-release tablets, the present invention combines two kinds of medicines,The effective ratio of medicine is high, taking convenience.
The present invention seeks to be realized by following technical scheme:
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: HydrochioroLive in 30～50 parts, 35～45 parts of potassium citrates, 120～150 parts of diluents, 80～120 parts of disintegrants, surface10～15 parts of agent of property, 80～150 parts of slow-release materials, 10～15 parts of lubricants.
The object of the invention can also be realized by following technical scheme:
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: Hydrochioro 30Part, 35 parts of potassium citrates, 120 parts of diluents, 80 parts of disintegrants, 10 parts, surfactant, slowly-releasing materialExpect 10 parts of 80 parts, lubricant.
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: Hydrochioro 40Part, 40 parts of potassium citrates, 130 parts of diluents, 100 parts of disintegrants, 12 parts, surfactant, slowly-releasing120 parts of materials, 11 parts of lubricants.
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: Hydrochioro 50Part, 45 parts of potassium citrates, 150 parts of diluents, 120 parts of disintegrants, 15 parts, surfactant, slowly-releasing150 parts of materials, 15 parts of lubricants.
A kind of hydrochlorothiazide Compound sustained release tablets, diluent comprises in lactose, amylum pregelatinisatum, microcrystalline celluloseAt least one.
A kind of hydrochlorothiazide Compound sustained release tablets, disintegrant comprises in dried starch, PVPPAt least one.
A kind of hydrochlorothiazide Compound sustained release tablets, surfactant comprises in fatty glyceride, polysorbateAt least one.
A kind of hydrochlorothiazide Compound sustained release tablets, slow-release material comprises sodium carboxymethylcellulose pyce, alginate, de-secondAt least one in acyl chitin.
A kind of hydrochlorothiazide Compound sustained release tablets, lubricant comprises at least one in dolomol, talcum powderKind.
The present invention also provides a kind of preparation method of hydrochlorothiazide Compound sustained release tablets, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to component and the parts by weight of described a kind of hydrochlorothiazide Compound sustained release tablets, itsMiddle Hydrochioro, potassium citrate were pulverized respectively 120 mesh sieves, diluent, disintegrant, surfactant,Slow-release material, lubricant were pulverized respectively 80 mesh sieves;
2) granulate, by appropriate to Hydrochioro, diluent, disintegrant, surfactant is appropriate, lubricant is suitableAmount mixes wet granulation and the whole grain of 20 orders obtains particle A, by potassium citrate, and slow-release material, surplusThe whole grain of diluent, surfactant, the even wet granulation of mix lubricant 30 orders obtains particle B;
3) compressing tablet, adopts high speed bi-layer tablet press by particle A and particle B compressing tablet, first presses particle B to press againParticle A, specification is with Hydrochioro content meter 25～50mg/ sheet.
Beneficial effect of the present invention
Sustained release tablets of the present invention combines two kinds of medicine Hydrochioros, potassium citrates, overcomesThe appropriate to the occasion sylvite that suitably supplements of prolonged application Hydrochioro, take inconvenience, compressing tablet supplementary product consumption is relative separatelyThe defect more, packing cost is high. The present invention makes Hydrochioro, potassium citrate medicine after compound slow-release tablet,Not only the effective ratio of medicine is high, facilitates medication, and realizes and discharge lastingly, slowly medicine, blood in vivoConcentration is steady, fluctuates little, and patient's internal organs are also had to certain protection. Not only improve patient compliance,The survival rate that has also improved medication patient, has reduced auxiliary material and packing cost, is conducive to large production.
Detailed description of the invention
According to following embodiment, the present invention may be better understood. But those skilled in the art is easyUnderstand, the described concrete material proportion of embodiment, process conditions and result thereof are only for illustrating the present inventionAnd should can not limit the present invention described in detail in claims yet.
Embodiment 1
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: Hydrochioro 30Part, 35 parts of potassium citrates, 120 parts of lactose, 80 parts of dried starch, 10 parts of fatty glycerides, methyl fibreTie up 80 parts, plain sodium, 10 parts of talcum powder.
A preparation method for hydrochlorothiazide Compound sustained release tablets, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to component and the parts by weight of described a kind of hydrochlorothiazide Compound sustained release tablets, itsMiddle Hydrochioro, potassium citrate were pulverized respectively 120 mesh sieves, lactose, dried starch, fatty glyceride,Sodium carboxymethylcellulose pyce, talcum powder were pulverized respectively 80 mesh sieves;
2) granulate, by Hydrochioro, lactose parts by weight 1/2nd, dried starch, fatty glycerideParts by weight 1/2nd, talcum powder parts by weight 1/2nd mix wet granulation and 20 orders wholeGrain particle A, by potassium citrate, lactose parts by weight 1/2nd, fatty glyceride parts by weight1/2nd, sodium carboxymethylcellulose pyce, talcum powder parts by weight 1/2nd mix wet granulation alsoThe whole grain of 30 orders obtains particle B;
3) compressing tablet, adopts high speed bi-layer tablet press by particle A and particle B compressing tablet, first presses particle B to press againParticle A, specification is with Hydrochioro content meter 25mg/ sheet.
Usage and dosage: 1～2 time on the oral one, one time 1～2 or follow the doctor's advice.
Embodiment 2
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: Hydrochioro 40Part, 40 parts of potassium citrates, 60 parts of lactose, 70 parts of amylum pregelatinisatums, PVPP 100Part, 6 parts of fatty glycerides, 6 parts of polysorbates, 120 parts of sodium alginates, 6 parts of dolomols, sliding5 parts of stone flours.
A preparation method for hydrochlorothiazide Compound sustained release tablets, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to component and the parts by weight of described a kind of hydrochlorothiazide Compound sustained release tablets, itsMiddle Hydrochioro, potassium citrate were pulverized respectively 120 mesh sieves, lactose, amylum pregelatinisatum, crosslinked polyethylenePyrrolidones, fatty glyceride, polysorbate, sodium alginate, dolomol, talcum powder are pulverized respectivelyCross 80 mesh sieves;
2) granulate, by Hydrochioro, lactose, PVPP, fatty glyceride, tristearinAcid magnesium mixes wet granulation and the whole grain of 20 orders obtains particle A, by potassium citrate, amylum pregelatinisatum, poly-mountainPear ester, sodium alginate, talcum powder mix wet granulation and the whole grain of 30 orders obtains particle B;
3) compressing tablet, adopts high speed bi-layer tablet press by particle A and particle B compressing tablet, first presses particle B to press againParticle A, specification is with Hydrochioro content meter 40mg/ sheet.
Usage and dosage: 1～2 time on the oral one, one time 1～2 or follow the doctor's advice.
Embodiment 3
A kind of hydrochlorothiazide Compound sustained release tablets, component and the parts by weight of this sustained release tablets comprise: Hydrochioro 50Part, 45 parts of potassium citrates, 150 parts of microcrystalline celluloses, 120 parts of PVPPs, poly-sorb15 parts of esters, 150 parts of chitosans, 15 parts of talcum powder.
A preparation method for hydrochlorothiazide Compound sustained release tablets, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to component and the parts by weight of described a kind of hydrochlorothiazide Compound sustained release tablets, itsMiddle Hydrochioro, potassium citrate were pulverized respectively 120 mesh sieves, microcrystalline cellulose, crosslinked polyethylene pyrrolidinesKetone, polysorbate, chitosan, talcum powder were pulverized respectively 80 mesh sieves;
2) granulate, by Hydrochioro, microcrystalline cellulose parts by weight 1/2nd, crosslinked polyethylene pyrrolesAlkane ketone, polysorbate parts by weight 1/2nd, talcum powder parts by weight 1/2nd mix wetMethod granulate and the whole grain of 20 orders particle A, by potassium citrate microcrystalline cellulose parts by weight 1/2nd, poly-Sorb ester parts by weight 1/2nd, 1/2nd the mixing of chitosan, talcum powder parts by weightEvenly the whole grain of wet granulation 30 orders obtains particle B;
3) compressing tablet, adopts high speed bi-layer tablet press by particle A and particle B compressing tablet, first presses particle B to press againParticle A, specification is with Hydrochioro content meter 50mg/ sheet.
Usage and dosage: 1～2 time on the oral one, one time 1～2 or follow the doctor's advice.
Embodiment 4
Friability inspection of the present invention
Check according to " Chinese pharmacopoeia " 2010 editions (two) annex XG tablet friability inspection technique.
Instrument: friability tester.
Method: get some, make its gross weight be about 6.5g; Blow away the powder coming off with hair-dryer, precise weighing,Put in cylinder, rotate 100 times. Take out, remove powder with method, precise weighing, less loss weight must not cross 1%,And the sheet that must not detect fracture, be full of cracks and pulverize. This test is generally only done 1 time. While exceeding 1% as less loss weight,Should recheck 2 times, the average less loss weight of 3 times must not cross 1%, and the sheet that must not detect fracture, be full of cracks and pulverize.
Result: embodiments of the invention 1-3 gained sample checks and all conforms with the regulations through friability test.
Embodiment 5
Release inspection of the present invention
According to 2010 editions two annex XD drug release determination method first methods of Chinese pharmacopoeia, adopt dissolution determinationThe device of method the second method, taking water as solvent, rotating speed is per minute 50 to turn, 32 ± 0.5 DEG C of operations in accordance with the law of water temperature.Measure respectively the release of the obtained sample of embodiment 1-3. Each sample all, in 2h, 4h, 8h sampling, passes through HPLCDetect, potassium citrate release (%) the results are shown in following table.
Conclusion: compound slow-release tablet vitro release result of the present invention shows that this compound slow-release tablet has slowly and releasesPut medicine, drug concentration is steady, and little feature fluctuates.
Embodiment 6
Toxicity Analysis of the present invention
To the hypotensive activity of Hypertensive Rats, adopt the spontaneous hypertensive rat (SHR) in 20～26 week ageMale rat, single dose, with compound dose oral administration respectively, detects its hypotensive effect. By I type ratTail is pressed heart rate measurement instrument to measure rat tail and is pressed.
Positive controls adopts folk prescription single oral dose administration Hydrochioro 0.25mg/kg/d, potassium citrate 0.3mg/kg/d。
Test group adopts compound single oral dose administration Hydrochioro 0.25mg/kg/d, potassium citrate 0.3Mg/kg/d is sustained release tablets prepared by the embodiment of the present invention 1.
Result of the test:
Folk prescription single dose systolic pressure can reduce by 5.65～28.55mmHg, and diastolic pressure reduces by 8.79～11.56mmHg,Year survival rate is 70.4%. Compound single dose systolic pressure can reduce by 24.21～29.42mmHg, and diastolic pressure reduces25.26～27.33mmHg, a year survival rate is 89.1%, antihypertensive effect is good, and has greatly improved medication mouseSurvival rate.
Above embodiment is only explanation technical conceive of the present invention and feature, and its object is to allow is familiar with thisThe people of technology understands content of the present invention and is implemented, and can not limit the scope of the invention with this, allThe equivalence that Spirit Essence does according to the present invention changes or modifies, and all should be encompassed in protection scope of the present invention.
Claims (10)
1. a hydrochlorothiazide Compound sustained release tablets, is characterized in that, the component of this sustained release tablets and parts by weight bagDraw together: 30～50 parts of Hydrochioros, 35～45 parts of potassium citrates, 120～150 parts of diluents, disintegrant 80～120Part, 10～15 parts, surfactant, 80～150 parts of slow-release materials, 10～15 parts of lubricants.
2. a kind of hydrochlorothiazide Compound sustained release tablets according to claim 1, is characterized in that this slowly-releasingComponent and the parts by weight of sheet comprise: 30 parts of Hydrochioros, 35 parts of potassium citrates, 120 parts of diluents,80 parts of disintegrants, 10 parts, surfactant, 80 parts of slow-release materials, 10 parts of lubricants.
3. a kind of hydrochlorothiazide Compound sustained release tablets according to claim 1, is characterized in that this slowly-releasingComponent and the parts by weight of sheet comprise: 40 parts of Hydrochioros, 40 parts of potassium citrates, 130 parts of diluents,100 parts of disintegrants, 12 parts, surfactant, 120 parts of slow-release materials, 11 parts of lubricants.
4. a kind of hydrochlorothiazide Compound sustained release tablets according to claim 1, is characterized in that this slowly-releasingComponent and the parts by weight of sheet comprise: 50 parts of Hydrochioros, 45 parts of potassium citrates, 150 parts of diluents,120 parts of disintegrants, 15 parts, surfactant, 150 parts of slow-release materials, 15 parts of lubricants.
5. according to a kind of hydrochlorothiazide Compound sustained release tablets described in claim 1～4 any one, it is characterized in that,Diluent comprises at least one in lactose, amylum pregelatinisatum, microcrystalline cellulose.
6. according to a kind of hydrochlorothiazide Compound sustained release tablets described in claim 1～4 any one, it is characterized in that,Disintegrant comprises at least one in dried starch, PVPP.
7. according to a kind of hydrochlorothiazide Compound sustained release tablets described in claim 1～4 any one, it is characterized in that,Surfactant comprises at least one in fatty glyceride, polysorbate.
8. according to a kind of hydrochlorothiazide Compound sustained release tablets described in claim 1～4 any one, it is characterized in that,Slow-release material comprises at least one in sodium carboxymethylcellulose pyce, alginate, chitosan.
9. according to a kind of hydrochlorothiazide Compound sustained release tablets described in claim 1～4 any one, it is characterized in that,Lubricant comprises at least one in dolomol, talcum powder.
10. a preparation method for hydrochlorothiazide Compound sustained release tablets, is characterized in that, comprises the following steps:
1) get the raw materials ready, according to the component of a kind of hydrochlorothiazide Compound sustained release tablets described in claim 1～4 any oneAnd parts by weight get the raw materials ready, wherein Hydrochioro, potassium citrate were pulverized respectively 120 mesh sieves, diluent, collapsedSolution agent, surfactant, slow-release material, lubricant were pulverized respectively 80 mesh sieves;
2) granulate, by appropriate to Hydrochioro, diluent, disintegrant, surfactant is appropriate, lubricant is suitableAmount mixes wet granulation and the whole grain of 20 orders obtains particle A, by potassium citrate, and slow-release material, surplusThe whole grain of diluent, surfactant, the even wet granulation of mix lubricant 30 orders obtains particle B;
3) compressing tablet, adopts high speed bi-layer tablet press by particle A and particle B compressing tablet, first presses particle B to press againParticle A, specification is with Hydrochioro content meter 25～50mg/ sheet.
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4966776A (en) * | 1983-04-11 | 1990-10-30 | Board Of Regents, The University Of Texas System | Compositions and methods of treating calcium renal stones |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4966776A (en) * | 1983-04-11 | 1990-10-30 | Board Of Regents, The University Of Texas System | Compositions and methods of treating calcium renal stones |
Non-Patent Citations (2)
| Title |
|---|
| 张惠琴 等: "枸橼酸钾对高血压患者血压的影响", 《河北医学》 * |
| 高明明: "噻嗪类利尿剂治疗高血压的定位", 《临床药物治疗杂志》 * |
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Application publication date: 20160525 |