CN106943364A - A kind of bendroflumethiazide piece and preparation method thereof - Google Patents
A kind of bendroflumethiazide piece and preparation method thereof Download PDFInfo
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- CN106943364A CN106943364A CN201710118070.0A CN201710118070A CN106943364A CN 106943364 A CN106943364 A CN 106943364A CN 201710118070 A CN201710118070 A CN 201710118070A CN 106943364 A CN106943364 A CN 106943364A
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- bendroflumethiazide
- piece
- parts
- preparation
- microcrystalline cellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/549—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
Abstract
The present invention discloses a kind of bendroflumethiazide piece and preparation method thereof, belongs to technical field of medicine, is made up of following components in parts by weight：0.25~0.5 part of bendroflumethiazide, 102 2~6 parts of microcrystalline cellulose PH, 4~8 parts of lactose, 0.2~0.6 part of carboxyrnethyl starch sodium, 0.02~0.04 part of magnesium stearate.The preparation method of bendroflumethiazide piece, comprises the following steps：Bendroflumethiazide is subjected to air-flow crushing；Take bendroflumethiazide, microcrystalline cellulose PH 102 and magnesium stearate well mixed, obtain mixed material；Lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；Using dry method direct tablet compressing, produce.In the present invention bendroflumethiazide content of bendroflumethiazide piece evenly, while drug-eluting is rapider in 5min；Preparation technology is simple, and other auxiliary materials outside microcrystalline cellulose PH 102 do not need special crushing, it is not necessary to complicated preparation equipment, it is easy to industrialized production.
Description
Technical field
The present invention relates to technical field of medicine, more particularly to a kind of bendroflumethiazide piece and preparation method thereof.
Background technology
Bendroflumethiazide be 3- benzyl -6- trifluoromethyl -7- sulfonamido -3,4- dihydro -2H-1,2,4- benzothiadiazines -
1,1- dioxide.
Effect：1st, edema disease, excretion internal excessive sodium and water, reduces ECFV, eliminates oedema.
Common includes congestive heart failure, cirrhotic ascites, nephrotic syndrome, acute and chronic nephritis oedema, chronic renal failure
In early days, adrenal gland matter cortin and sodium caused by estrin treatment, water retention.2nd, hypertension.It can be depressured individually or with other
Medicine use in conjunction.It is mainly used in treating essential hypertension.3rd, central or nephrogenic diabetes insipidus.4th, nephrolith disease.It is mainly used in pre-
The calculus of anti-calcic salt component formation.
Pharmacological action：
1st, to the influence of water, electrolyte excretion.1. diuresis, urinates sodium, potassium, chlorine, phosphorus and the excretion increase of magnesium plasma, and
Urinary calcium excretion is reduced.This class mechanism of drug action mainly suppresses distal tubule leading portion and proximal tubule (effect is lighter) to chlorination
The reabsorption of sodium, so that the Na+-K+ for increasing distal tubule and concetrated pipe is exchanged, K+ secretions increase.Its mechanism of action is not yet complete
Understand.This class medicine can suppress carbonic anhydrase activity to some extent, therefore can explain its effect to proximal tubule.This class medicine
Phosphodiesterase activity can also be suppressed, intake and mitochondria oxygen consumption of the renal tubule to aliphatic acid are reduced, so as to suppress renal tubule pair
Na+, Cl- active reabsorption.2. antihypertensive effect.In addition to diuresis row's sodium effect, there may be the outer mechanism of action of kidney to participate in step-down,
It is probably the excretion for increasing intestines and stomach to Na+.
2nd, to the influence of renal hemodynamics and detection of glomeruli filtration function.Because renal tubule is reduced to water, Na+ reabsorptions,
Pressure rise in renal tubule, and flow through the water and Na+ of distal convoluted tubule and increase, stimulate macula densa to be reflected by pipe-ball, make in kidney
Feritin, angiotensins secretion increase, cause Renal vascular to shrink, renal blood flow declines, glomerulus goal and efferent glomerular arteriole are received
Contracting, glomerular filtration rate(GFR also declines.Renal blood flow and glomerular filtration rate(GFR decline, and are this class medicines to Heng Shi loops without effect
Thing diuresis can not show a candle to the main cause of loop diuretics.
The common flow of existing bendroflumethiazide piece preparation technology is first to fill out lactose, cornstarch and pre-paying starch etc.
Fill agent and use wet granulation, compressing tablet is carried out after then other auxiliary materials such as bendroflumethiazide, glidant are mixed with particle.The technique will
Compressing tablet is carried out after the particle that bendroflumethiazide and filler are made directly mixing, due to the particle diameter and the grain of particle of the former grain of bendroflumethiazide
Footpath difference is big, easily causes content difference between tablet.
In addition, in terms of existing bendroflumethiazide piece auxiliary material selection, due to selecting substantial amounts of insoluble auxiliary material.Surveyed in dissolution rate
During fixed, even if disintegration of tablet, water-insoluble auxiliary material is easily deposited in stripping rotor bottom, hinders the scattered of medicine, so that
Make drug-eluting poor；In addition, it is ensured that micronized medicine is good with auxiliary material mixing uniformity, to auxiliary material requirement should granularity it is small, again
There is good mobility and compressibility.
The content of the invention
The invention provides a kind of bendroflumethiazide piece and preparation method thereof, the tablet of existing bendroflumethiazide piece having is solved
Between content difference it is larger the problem of.
In order to solve the above technical problems, the technical scheme is that：
A kind of bendroflumethiazide piece, is made up of following components in parts by weight：0.25~0.5 part of bendroflumethiazide, microcrystalline cellulose
Plain 2~6 parts of PH-102,4~8 parts of lactose, 0.2~0.6 part of carboxyrnethyl starch sodium, 0.02~0.04 part of magnesium stearate.
Wherein it is preferred to, a kind of bendroflumethiazide piece is made up of following components in parts by weight：Bendroflumethiazide 0.25~0.5
Part, 3~5 parts of microcrystalline cellulose PH-102,5~7 parts of lactose, 0.3~0.5 part of carboxyrnethyl starch sodium, magnesium stearate 0.02~0.04
Part.
A kind of preparation method of bendroflumethiazide piece, comprises the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is produced.
Wherein it is preferred to, air-flow crushing controls D90=30-60 microns in the step (1).
Beneficial effect of the present invention：
The present invention, as filler, is first well mixed, so using microcrystalline cellulose PH-102 with the bendroflumethiazide being micronized
After add other auxiliary materials it is well mixed after compressing tablet, can obtain that dissolution is rapid, the tablet of uniform content, steady quality.Reason can
Can be microcrystalline cellulose PH-102 and bendroflumethiazide particle size differences less, therefore mixture homogeneity is good, and because crystallite is fine
Tie up element PH-102 density small, cellulose rapid flotation after disintegration of tablet not but not makes medicine be deposited in stripping rotor bottom, and
Medicine can be driven to be suspended in dissolution medium, promote bendroflumethiazide dissolution.
Compared with prior art, bendroflumethiazide tablet of the present invention and its preparation technology have the following advantages that and significantly
Progressive：
(1) in preparation the content of bendroflumethiazide evenly, while drug-eluting is rapider in 5min；
(2) preparation technology is simple, and other auxiliary materials outside microcrystalline cellulose PH-102 do not need special crushing, granularity requirements
It is not harsh, it is not necessary to complicated preparation equipment, it is easy to industrialized production.
Embodiment
Below in conjunction with the specific embodiment of the invention, the technical scheme to the present invention carries out clear, complete description, institute
The example of description is only the section Example of the present invention, rather than whole embodiments.Based on the embodiment in the present invention, sheet
Field those of ordinary skill, the every other embodiment obtained under the premise of creative work is not made, belongs to this hair
Bright protection domain.
Embodiment 1
The present embodiment provides a kind of bendroflumethiazide piece, is made up of following components in parts by weight：It is bendroflumethiazide 0.25Kg, micro-
Crystalline cellulose PH-102 4Kg, lactose 6Kg, carboxyrnethyl starch sodium 0.4Kg, magnesium stearate 0.03Kg.
The preparation method of above-mentioned bendroflumethiazide piece, comprises the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing, air-flow crushing controls D90=30-60 microns；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is in batches 100,000, tablet format is 2.5mg/ pieces.
Embodiment 2
The present embodiment provides a kind of bendroflumethiazide piece, is made up of following components in parts by weight：It is bendroflumethiazide 0.25Kg, micro-
Crystalline cellulose PH-102 6Kg, lactose 4Kg, carboxyrnethyl starch sodium 0.6Kg, magnesium stearate 0.02Kg.
The preparation method of above-mentioned bendroflumethiazide piece, comprises the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing, air-flow crushing controls D90=30-60 microns；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is in batches 100,000, tablet format is 2.5mg/ pieces.
Embodiment 3
The present embodiment provides a kind of bendroflumethiazide piece, is made up of following components in parts by weight：It is bendroflumethiazide 0.25Kg, micro-
Crystalline cellulose PH-102 2Kg, lactose 8Kg, carboxyrnethyl starch sodium 0.2Kg, magnesium stearate 0.04Kg.
The preparation method of above-mentioned bendroflumethiazide piece, comprises the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing, air-flow crushing controls D90=30-60 microns；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is in batches 100,000, tablet format is 2.5mg/ pieces.
Embodiment 4
The present embodiment provides a kind of bendroflumethiazide piece, is made up of following components in parts by weight：It is bendroflumethiazide 0.5Kg, micro-
Crystalline cellulose PH-102 3Kg, lactose 7Kg, carboxyrnethyl starch sodium 0.3Kg, magnesium stearate 0.04Kg.
The preparation method of above-mentioned bendroflumethiazide piece, comprises the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing, air-flow crushing controls D90=30-60 microns；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is in batches 100,000, tablet format is 5mg/ pieces.
Embodiment 5
The present embodiment provides a kind of bendroflumethiazide piece, is made up of following components in parts by weight：It is bendroflumethiazide 0.5Kg, micro-
Crystalline cellulose PH-102 5Kg, lactose 5Kg, carboxyrnethyl starch sodium 0.5Kg, magnesium stearate 0.02Kg.
The preparation method of above-mentioned bendroflumethiazide piece, comprises the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing, air-flow crushing controls D90=30-60 microns；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is in batches 100,000, tablet format is 5mg/ pieces.
Bendroflumethiazide piece and uniformity of dosage units made from the various embodiments described above are measured.
(1) dissolution rate is detected：Inspection method is《Chinese Pharmacopoeia》Second method, slurry processes, rotating speed as defined in 2010 editions：50rpm,
900ml pH6.8 phosphate buffers, 5min sampling detections.
(2) uniformity of dosage units is detected：This product 1 is taken, is put in mortar, it is finely ground, plus 0.4% sodium hydroxide solution is in right amount, grinds
Mill, is transferred in 25ml measuring bottles, shake well dissolves bendroflumethiazide, uses 0.4% hydrogen-oxygen by several times with 0.4% sodium hydroxide solution
Change sodium solution and be diluted to scale, shake up, filter, precision measures subsequent filtrate 2ml, puts in 25ml measuring bottles, be diluted with water to scale, shake
It is even, according to the method mensuration absorbance under assay, and content is calculated, regulation (general rule 0941) should be met.
The bendroflumethiazide piece drug-eluting that it can be seen from above-mentioned experimental result prepared by the embodiment of the present invention 1~5 is rapid,
Complete dissolution in 5min, and uniformity of dosage units numerical value is small.After accelerated test, dissolution rate is basically unchanged.And above-described embodiment system
The sample obtained 0 day and acceleration are pressed for 6 months《Chinese Pharmacopoeia》The two bendroflumethiazide tablet quality standard detections of version in 2015, meet mark
Quasi- regulation.
Presently preferred embodiments of the present invention is the foregoing is only, is not intended to limit the invention, all essences in the present invention
God is with principle, and any modifications, equivalent substitutions and improvements made etc. should be included within the scope of the present invention.
Claims (4)
1. a kind of bendroflumethiazide piece, it is characterised in that be made up of following components in parts by weight：0.25~0.5 part of bendroflumethiazide,
2~6 parts of microcrystalline cellulose PH-102,4~8 parts of lactose, 0.2~0.6 part of carboxyrnethyl starch sodium, 0.02~0.04 part of magnesium stearate.
2. a kind of bendroflumethiazide piece according to claim 1, it is characterised in that be made up of following components in parts by weight：Benzyl
It is 0.25~0.5 part of flumethiazide, 3~5 parts of microcrystalline cellulose PH-102,5~7 parts of lactose, 0.3~0.5 part of carboxyrnethyl starch sodium, hard
0.02~0.04 part of fatty acid magnesium.
3. the preparation method of the bendroflumethiazide piece described in a kind of claim 1 or 2, it is characterised in that comprise the following steps：
(1) bendroflumethiazide is subjected to air-flow crushing；
(2) take bendroflumethiazide, microcrystalline cellulose PH-102 and magnesium stearate well mixed, obtain mixed material；
(3) lactose, carboxyrnethyl starch sodium are added in mixed material, are well mixed；
(4) dry method direct tablet compressing is used, is produced.
4. a kind of preparation method of bendroflumethiazide piece according to claim 1, it is characterised in that：Gas in the step (1)
Stream crushes D90=30-60 microns of control.
Priority Applications (1)
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|---|---|---|---|
| CN201710118070.0A CN106943364A (en) | 2017-03-01 | 2017-03-01 | A kind of bendroflumethiazide piece and preparation method thereof |
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| CN201710118070.0A CN106943364A (en) | 2017-03-01 | 2017-03-01 | A kind of bendroflumethiazide piece and preparation method thereof |
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| CN106943364A true CN106943364A (en) | 2017-07-14 |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4304773A (en) * | 1980-06-26 | 1981-12-08 | E. R. Squibb & Sons, Inc. | Novel bendroflumethiazide formulations and method |
-
2017
- 2017-03-01 CN CN201710118070.0A patent/CN106943364A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4304773A (en) * | 1980-06-26 | 1981-12-08 | E. R. Squibb & Sons, Inc. | Novel bendroflumethiazide formulations and method |
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| PB01 | Publication | ||
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Application publication date: 20170714 |