CN104523651B - A kind of voglibose capsule and preparation method thereof - Google Patents
A kind of voglibose capsule and preparation method thereof Download PDFInfo
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- CN104523651B CN104523651B CN201410854236.1A CN201410854236A CN104523651B CN 104523651 B CN104523651 B CN 104523651B CN 201410854236 A CN201410854236 A CN 201410854236A CN 104523651 B CN104523651 B CN 104523651B
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Abstract
The invention belongs to field of medicine preparing technology, it particularly relates to arrive a kind of voglibose capsule and preparation method thereof.The preparation method is concretely comprised the following steps：1) by voglibose raw material micronization processes, size controlling is between 10 50um；2) raw material, filler, disintegrant of recipe quantity are weighed, is well mixed；3) the adhesive softwood of water or/and ethanol dissolving is added, the granulation of 20 eye mesh screens is crossed；4) particle is placed in after being dried in 60 DEG C of constant temperature ovens and adds the lubricant of recipe quantity, cross 18 mesh sieve whole grains；5) by the granule filling mixed in capsule.Compared with prior art, voglibose capsule of the present invention in the preparation, by the way that by raw material micronization processes, using in suitable plus disintegrant, it has, and disintegration time is short, dissolution rate is high, preparation technology is simple, lower-cost feature.
Description
Technical field
The invention belongs to field of medicine preparing technology, it particularly relates to arrive a kind of voglibose capsule and its preparation
Method.
Background technology
Voglibose is the alpha-glucosidase restrainer of new generation that Japanese military field pharmaceutical industries strain formula can be developed,
Suppress with competing Antagonism to advocate interior disaccharide class hydrolase after oral, so as to delay the digestion and absorption of carbohydrate, to improve
Postprandial hyperglycemia.Raised first in Japan's listing for treating diabetes postprandial blood sugar within 1994.In addition, this product is arranged in pyrroles
Ketone composition compound is used to improve sugar tolerance.The alpha-glucosidase restrainer listed at present mainly has voglibose and A Kabo
Sugar, is compared with acarbose, and voglibose activity is higher, and dosage is smaller；The selectivity of alpha-glucosidase is higher, intestines
Road side effect is lower.Because the mechanism of action of voglibose is the generation and absorption of delay glucose, therefore blood sugar reducing function is more
Plus stably, secreted with not stimulating insulin plus voglibose again, therefore the appearance without hyperinsulinemia after the meal, it is difficult out
Existing hypoglycemic effect.It is used alone and other hypoglycemic medicines is used in combination equally effectively, medication and drop can also be made during drug combination
Sugar effect is more synchronous, reduces the consumption of other hypoglycemic medicines, and the danger of hypoglycemia occurs in reduction, reduces the side effects such as obesity.
Clinical evaluation is good, and its sales volume gradually rises.
At present in the product of domestic listing, example has capsule preparations very much, even if having, and there is also many defects.For example, Chinese
A kind of voglibose capsule and preparation method thereof disclosed in patent (CN 101219127A), capsule includes:Voglibose,
Disintegrant, diluent, lubricant and glidant；Disintegrant is poly- selected from starch, modified starch, cellulose, microcrystalline cellulose, crosslinking
Tie up ketone, complete in methyl starch sodium, crosslinking shuttle sodium carboxymethylcellulose pyce, low-substituted hydroxypropyl cellulose, alginic acid, veegum
One or more；Described diluent is selected from lactose, mannitol, sorbierite, sucrose, calcium sulfate, kaolin, dextrin, chlorination
One or more in sodium.In this application, because its disintegration is slower, capsule shells swelling rate is slow, reduces voglibose
Utilization in vivo.
The content of the invention
In order to solve the above technical problems, the invention provides the voglibose that a kind of disintegration time is short, dissolution rate is higher
Capsule and preparation method thereof.
A kind of voglibose capsule of the present invention, the capsule is calculated in parts by mass, includes 1-2 parts of Fu Gelie
Ripple glycogen material, 450-750 parts of filler, 50-100 parts of adhesive, 20-45 parts of disintegrant and 5-15 parts of lubricant；
The voglibose raw material passes through micronization processes, and size controlling is between 10-50um.
A kind of voglibose capsule of the present invention, the filler include lactose, mannitol, microcrystalline cellulose,
One or more in pregelatinized starch, starch, dextrin, Icing Sugar, calcium monohydrogen phosphate and calcium carbonate.
A kind of voglibose capsule of the present invention, the disintegrant includes sodium carboxymethylcellulose, carboxymethyl and formed sediment
One or more in powder sodium, Ac-Di-Sol, PVPP.
A kind of voglibose capsule of the present invention, described adhesive includes starch slurry, hydroxypropyl methylcellulose, hydroxypropyl
One or more in cellulose, dextrin, PVPK30.
A kind of voglibose capsule of the present invention, the lubricant includes magnesium stearate, talcum powder, titanium dioxide
One or more in silicon, stearic acid, behenyl acid glyceride.
A kind of preparation method of voglibose capsule of the present invention, the preparation method is concretely comprised the following steps：1) will
Voglibose raw material micronization processes, size controlling is between 10-50um；2) raw material, filler, disintegration of recipe quantity are weighed
Agent is well mixed；3) the adhesive softwood of water or/and ethanol dissolving is added, the granulation of 20 eye mesh screens is crossed；4) particle is placed in
The lubricant of recipe quantity is added after being dried in 60 DEG C of constant temperature ovens, 18 mesh sieve whole grains are crossed；5) by the granule filling mixed in glue
In capsule.
Compared with prior art, voglibose capsule of the present invention in the preparation, by by raw material micronizing
Reason, using in suitable plus disintegrant, it has, and disintegration time is short, dissolution rate is high, preparation technology is simple, lower-cost spy
Point.
Embodiment
Voglibose capsule of the present invention and preparation method thereof is done further with reference to specific embodiment
Illustrate, but protection scope of the present invention is not limited to this.
Embodiment 1
Prescription：Voglibose 0.2, lactose 100g, microcrystalline cellulose 36g, Ac-Di-Sol 6g, 5%
PVPK30 50% ethanol solution 300ml, talcum powder 1g, is made 10000.
Preparation method：1) by voglibose raw material micronization processes, size controlling is between 10-25um；2) place is weighed
The voglibose of side's amount is well mixed with lactose by the equivalent method of progressively increasing, and adds microcrystalline cellulose, the crosslinking carboxylic first of recipe quantity
Base sodium cellulosate is well mixed；3) 5%PVPK30 of recipe quantity 50% ethanol solution softwood is added, 20 eye mesh screen systems are crossed
Grain；4) talcum powder that particle is placed in addition recipe quantity after being dried in 60 DEG C of constant temperature ovens crosses 18 mesh sieve whole grains；5) it will mix
Granule filling in capsule.
Embodiment 2
Voglibose 0.2g, lactose 110g, mannitol 30g, Ac-Di-Sol 6g, 5%PVPK30
50% ethanol solution 240ml, talcum powder 1g, are made 10000.
Preparation method：1) by voglibose raw material micronization processes, size controlling is between 35-50um；2) place is weighed
Mannitol, cross-linked carboxymethyl fibre that the voglibose of side's amount is well mixed by the equivalent method of progressively increasing with lactose, adds recipe quantity
The plain sodium of dimension is well mixed；3) 5%PVPK30 of recipe quantity 50% ethanol solution softwood is added, the granulation of 20 eye mesh screens is crossed；
4) talcum powder that particle is placed in addition recipe quantity after being dried in 60 DEG C of constant temperature ovens crosses 18 mesh sieve whole grains；5) by mixed
Grain is filling in capsule.
Embodiment 3
Voglibose 0.2g, lactose 100g, pregelatinized starch 36g, sodium carboxymethyl starch 8g, 8%PVPK30 solution
235ml, magnesium stearate 1.5g, are made 10000.
Preparation method：1) by voglibose raw material micronization processes, size controlling is between 10-25um；2) place is weighed
The voglibose of side's amount is well mixed with lactose by the equivalent method of progressively increasing, the pregelatinized starch that adds recipe quantity, carboxymethyl shallow lake
Powder sodium is well mixed；3) the 5%PVPK30 solution softwoods of recipe quantity are added, the granulation of 20 eye mesh screens is crossed；4) particle is placed in 60
The talcum powder for adding recipe quantity after being dried in DEG C constant temperature oven crosses 18 mesh sieve whole grains；5) by the granule filling mixed in capsule
In.
Embodiment 4
Prescription：Voglibose 0.2g, lactose 100g, microcrystalline cellulose 36g, Ac-Di-Sol 6g, 5%
PVPK30 50% ethanol solution 300ml, talcum powder 1g, rosasterol palmitate 1g, is made 10000.
Preparation method：1) by voglibose raw material micronization processes, size controlling is between 10-25um；2) place is weighed
The voglibose of side's amount is well mixed with lactose by the equivalent method of progressively increasing, and adds microcrystalline cellulose, the crosslinking carboxylic first of recipe quantity
Base sodium cellulosate is well mixed；3) 5%PVPK30 of recipe quantity 50% ethanol solution softwood is added, 20 eye mesh screen systems are crossed
Grain；4) talcum powder that particle is placed in addition recipe quantity after being dried in 60 DEG C of constant temperature ovens crosses 18 mesh sieve whole grains；5) it will mix
Granule filling in capsule.
Control group
Voglibose 0.2g, lactose 80g, microcrystalline cellulose 50g, sodium carboxymethyl starch 10g, 8%PVPK30 solution
220ml, magnesium stearate 1.5g, are made 10000.
Preparation method：1) voglibose raw material is without pulverization process；2) voglibose and breast of recipe quantity are weighed
Sugar is well mixed, added the pregelatinized starch of recipe quantity, sodium carboxymethyl starch by the equivalent method of progressively increasing and is well mixed；3) at addition
The 5%PVPK30 solution softwoods of side's amount, cross the granulation of 20 eye mesh screens；4) particle is placed in after being dried in 60 DEG C of constant temperature ovens and added
The talcum powder for entering recipe quantity crosses 18 mesh sieve whole grains；5) by the granule filling mixed in capsule.
Quality testing
Content, dissolution rate and the pass material of each embodiment of present invention selection detection, further to be explained the present invention
State and verify.
1. dissolution rate is detected
Chromatographic condition：It is filler with octadecylsilane chemically bonded silica；Mobile phase：The phosphoric acid of 0.12% perfluorooctane sulfonate
Salt buffer (pH3.5) (takes perfluorooctane sulfonate 1.2g, the phthalate buffer that phosphorates (pH3.5) (takes sodium dihydrogen phosphate 3.6g, added water
1000ml dissolves, with phosphorus acid for adjusting pH value is to 3.5) dissolving and is diluted to 1000ml)；Column temperature：35℃；Fluorescence detector, is excited
Wavelength:350nm launch wavelengths：430nm.Assay method：This product is taken, according to dissolution method (Chinese Pharmacopoeia version two in 2010
The methods of Ⅹ C of portion's annex the 3rd) check, using phosphate buffer (PH5.8) 100ml as dissolution medium, rotating speed is 40 turns per minute, according to
Method is operated, and during through 30 minutes, takes solution 10ml, is filtered with 0.45 μm of filter membrane, is taken subsequent filtrate as need testing solution.Separately take volt lattice
Array wave sugar reference substance about 10mg, it is accurately weighed, put in 100ml volumetric flasks, dissolved with water and be diluted to scale, shaken up, as right
According to product storing solution；Precision measures 2ml, puts in 100ml volumetric flasks, is diluted with water to scale, shake up, is used as reference substance solution.According to
High performance liquid chromatography measures above-mentioned need testing solution and the μ l of reference substance solution 50 respectively, is determined according to the method under assay,
Calculate the stripping quantity of every.Take above example sample and comparative examples to carry out dissolution determination, respectively 5,10,
15th, 20,30 minutes sampling analyses, comparative results.Stripping curve testing result is shown in Table 1.
Each embodiment dissolution rate (%) result of table 1
| Sample time (min) | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Control group |
| 0 | 0 | 0 | 0 | 0 | 0 |
| 5 | 68.57 | 66.33 | 66.33 | 71.33 | 45.59 |
| 10 | 93.86 | 92.99 | 89.65 | 94.12 | 67.32 |
| 15 | 98.16 | 96.30 | 95.86 | 97.34 | 88.07 |
| 20 | 99.20 | 97.04 | 99.50 | 99.30 | 95.02 |
| 30 | 100.26 | 99.08 | 99.79 | 99.81 | 99.73 |
In terms of embodiment 1-4 and the dissolution Comparative result of comparative examples, embodiment 1-4 is disintegrated substantially in 15min
It is complete, and comparative examples are just to be disintegrated substantially in 20min.Prove by the present invention by the way that raw material micronizing can be improved into preparation
Dissolution rate, be conducive to the disintegration of preparation, and result of extraction is high.
2. content, relevant material are detected
Chromatographic condition：It is filler with octadecylsilane chemically bonded silica；Mobile phase：The phosphoric acid of 0.12% perfluorooctane sulfonate
Salt buffer (pH3.5) (takes perfluorooctane sulfonate 1.2g, the phthalate buffer that phosphorates (pH3.5) (takes sodium dihydrogen phosphate 3.6g, added water
1000ml dissolves, with phosphorus acid for adjusting pH value is to 3.5) dissolving and is diluted to 1000ml)；Column temperature：35℃；Fluorescence detector, is excited
Wavelength:350nm launch wavelengths：430nm.Relevant substance detecting method：Take the content 1.6g (specification 0.2mg) of this product (quite
In voglibose 2.0mg), put in 10ml measuring bottles, plus appropriate mobile phase, shake well, dissolve voglibose, with flowing
Phase dilution shakes up to scale, is filtered with 0.45 μm of filter membrane, takes subsequent filtrate as need testing solution.Precision measures need testing solution
1ml, puts in 50ml measuring bottles, plus mobile phase is diluted to scale, shakes up, and is used as contrast solution.Precision measures need testing solution and right
Liquid chromatograph is injected separately into according to each 50 μ l of product solution, 2 times of record chromatogram to principal component retention time, in addition to auxiliary material peak,
If any impurity peaks in need testing solution chromatogram, each impurity peak area sum is measured, the main peak peak face of contrast solution is cannot be greater than
0.6 times long-pending (1.2%).Detection method of content：This product 20 is taken, the weight of accurately weighed content is well mixed, taken about
0.40g (is approximately equivalent to voglibose 0.5mg), accurately weighed, puts in 50ml measuring bottles, plus appropriate mobile phase, shake well, makes
Voglibose dissolves, and is diluted to scale with mobile phase, shakes up, and filters, and filtrate is used as need testing solution.Another precision weighs volt lattice
Array wave sugar reference substance about 10mg, puts in 100ml measuring bottles, plus flows phased soln and be diluted to scale, shakes up, precision draw 5ml in
In 50ml measuring bottles, plus mobile phase is diluted to scale, shakes up, and is used as reference substance solution.Precision measures need testing solution and reference substance
The μ l of solution 50, injecting chromatograph records chromatogram.By external standard method with the content of C10H21NO7 in calculated by peak area test sample.Contain
Amount, the testing result about material are shown in Table 2.
Table 2：The relevant material testing result of each embodiment content
| Content (%) | It is maximum single miscellaneous | It is total miscellaneous | |
| Embodiment 1 | 99.98 | 0.0014 | 0.0024 |
| Embodiment 2 | 99.26 | 0.0017 | 0.0031 |
| Embodiment 3 | 100.17 | 0.0021 | 0.0036 |
| Embodiment 4 | 99.93 | 0.0012 | 0.0021 |
| Control group | 99.67 | 0.0020 | 0.0029 |
Embodiment content and relevant material testing result show that the micronization processes of voglibose raw material are not to to system
The stability of agent is impacted.After isolated rosasterol palmitate is extracted in addition from wild pepper, voglibose
The dissolution rate and each side quality of capsule increase.
To sum up the explainable present invention of detection to each embodiment effect is feasible, its voglibose capsule provided
Composition and preparation method thereof has the advantages that technique is simple, dissolution rate is high, preparation stabilization.
Claims (1)
1. a kind of voglibose capsule, it is characterised in that the prescription of the voglibose capsule is：Voglibose
0.2g, lactose 100g, microcrystalline cellulose 36g, Ac-Di-Sol 6g, 5%,PVP,K30 50% ethanol solution 300mL,
Talcum powder 1g and rosasterol palmitate 1g, is made 10000；
The preparation method of the voglibose capsule is：1）By voglibose raw material micronization processes, size controlling is in 10-
Between 25 μm；2）The voglibose for weighing recipe quantity is well mixed with lactose by the equivalent method of progressively increasing, and adds the micro- of recipe quantity
Crystalline cellulose, Ac-Di-Sol are well mixed；3）The 50% ethanol solution system for adding the 5%PVPK30 of recipe quantity is soft
Material, crosses the granulation of 20 eye mesh screens；4）The talcum powder that particle is placed in addition recipe quantity after being dried in 60 DEG C of constant temperature ovens crosses 18 mesh sieves
Whole grain；5）By the granule filling mixed in capsule.
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| CN201410854236.1A CN104523651B (en) | 2014-12-31 | 2014-12-31 | A kind of voglibose capsule and preparation method thereof |
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| CN201410854236.1A CN104523651B (en) | 2014-12-31 | 2014-12-31 | A kind of voglibose capsule and preparation method thereof |
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| JPWO2016098459A1 (en) * | 2014-12-17 | 2017-09-28 | 株式会社ダイセル | Delayed disintegrating particle composition |
| CN104906107A (en) * | 2015-06-29 | 2015-09-16 | 白强 | Voglibose pharmaceutical preparation for preventing and treating diabetes and nephropathy |
| CN114699383B (en) * | 2022-06-06 | 2022-08-05 | 中孚药业股份有限公司 | Preparation method of voglibose capsule |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101084907A (en) * | 2007-07-02 | 2007-12-12 | 李建新 | Voglibose dispersion tablet |
| CN101219127A (en) * | 2006-12-30 | 2008-07-16 | 江苏万邦生化医药股份有限公司 | Voglibose dispersible tablet, capsule and method for preparing the same |
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| JP4408340B2 (en) * | 2002-03-22 | 2010-02-03 | 武田薬品工業株式会社 | Fast disintegrating solid preparation |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101219127A (en) * | 2006-12-30 | 2008-07-16 | 江苏万邦生化医药股份有限公司 | Voglibose dispersible tablet, capsule and method for preparing the same |
| CN101084907A (en) * | 2007-07-02 | 2007-12-12 | 李建新 | Voglibose dispersion tablet |
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