CN105213335A - Glipizide tablet and preparation method thereof and application - Google Patents
Glipizide tablet and preparation method thereof and application Download PDFInfo
- Publication number
- CN105213335A CN105213335A CN201510626347.1A CN201510626347A CN105213335A CN 105213335 A CN105213335 A CN 105213335A CN 201510626347 A CN201510626347 A CN 201510626347A CN 105213335 A CN105213335 A CN 105213335A
- Authority
- CN
- China
- Prior art keywords
- glipizide
- agent
- tablet
- starch
- granulate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of glipizide tablet and preparation method thereof and application.Wherein Green's pyrazine tablet comprises with weight: grain diameter D50 is the glipizide 1% ~ 5% of 50 μm ~ 100 μm, solubilizing agent 1% ~ 10%, filler 50% ~ 90%, disintegrating agent 5% ~ 15%, lubricant 0.1% ~ 5%, and the binding agent of 2% ~ 15% is appropriate.Wherein, glipizide is preferably the glipizide that grain diameter D50 is 50 μm ~ 75 μm.In the present invention by by effective ingredient glipizide micronization, reduce the particle diameter of crude drug glipizide, increase solubilizing agent simultaneously and coordinate to improve drug release rate with glipizide, thus improve bioavailability, and then improve the quality of products.
Description
Technical field
The present invention relates to a kind of field of medicine preparation, be specifically related to the pharmaceutical preparation (tablet) of glipizide and preparation method and application.
Background technology
The prevalence of diabetes in the world in continuous ascendant trend, and has become a kind of chronic epidemic disease of serious harm human health.Sulfonylureas drugs for diabetes, as a line medication of type 2 diabetes mellitus, from the fifties, through the application of nearly half a century, has obtained the accreditation of numerous doctors, is the oral antidiabetic drug that current use experience is the abundantest.
Glipizide is a kind of lipotropy weak acid, is second filial generation sulphanylureas oral antidiabetic drug.Oral Gastrointestinal Tract absorbs complete, rapid, and without first pass effect.After 30 minutes, both visible blood glucose obviously declines, and pKa is 5.9, t
1/2for 2-4 hour, as taken with food simultaneously, absorption can postpone 30-40 minute, and protein binding rate is 92-99%, mainly albumin.Within after administration 1-2 hour, reach blood drug level peak, maintain hypoglycemic activity for up to more than 10 hours.Within 24 hours, 97% of dose can be drained, can all remove in 3 days, glipizide is eliminated mainly through liver biology transforms, the dosage being less than 10% is with original shape through urine and defecate, and the dosage of about 90% is drained through urine (80%) and feces (10%) with bioconversion product.The main metabolites of glipizide is aromatic hydroxy group product, without hypoglycemic activity.Secondary metabolite is not enough 2% of dosage, be a kind of acetamide ethylbenzene derivant, it has the hypoglycemic activity of parent 1/10-1/3, therefore without or seldom produce the side effect of " hypoglycemia " because of accumulation.
The mechanism of action of glipizide is that it mainly acts on Sulfonylurea receptor (SUR) on beta Cell of islet film, impels ATP dependent potassium to close, membrane depolarization, uelralante, thus reduces blood glucose.Except uelralante in pancreas, also acted on outward by its pancreas, insulin deactivation in liver is reduced, and hepatic glycogen is synthesized to be increased, and decomposing and reduces, by acting on after target tissue receptor or receptor, surrounding tissue being strengthened the sensitivity of insulin.
Glipizide tablet has the unique distinction in many advantages pharmacologically and curative effect compared with other antidiabetic drug: 1. quick-acting-to absorb rapidly, act on soon, within oral 1-2.5 hour, both reached blood drug level peak.2. efficiently-effect is remarkable, 2.5 milligrams of glipizide are equivalent to tolbutamide 500 milligrams or gliclazide 80 milligrams.3. extensively imitate-with other antidiabetic drug ratio, the dual pharmacological advantages that the effect of its existing stimulation islet β cell insulin has again very important islets of langerhans to act on outward; It not only has the effect of blood sugar lowering, and have the effect for the treatment of diabetic complications concurrently, as: early diabetes microangiopathies can be reversed, the pathological changes of prevention retina and glomerule, reduce the level of serum cholesterol and sodium lauryl sulphate three fat, improve high density lipoprotein composition, prevention coronary heart disease; Reduce platelet aggregation, increase the lytic activity of fibrin.4. safety-half-life is short, and excretion is fast, stores up, cause the hypoglycemic danger of persistency very little in body without any metabolite.5. convenient-patient that the state of an illness is lighter, if taking dose only needs 10-15 milligram, general single dose take both morning a decoction being taken at a draught on an empty stomach, do not need take every day 2-3 time.
This medical instrument is effective in cure significantly, blood sugar reducing function efficiently, safely, take medicine conveniently, the advantage such as side effect is little, be particularly useful for through diet control and physical training 2-3 unsatisfied light, the moderate type 2 diabetes mellitus patient of month curative effect, the beta Cell of islet of this kind of diabetics still has certain excreting insulin function, and without acute complications (as infection, wound, ketoacidosis, hyperosmolar coma etc.), nonjoinder gestation, without serious chronic complicating diseases.
According to known under Chinese Pharmacopoeia version in 2010 two glipizide items, glipizide crude drug is insoluble drug, the dissolubility how improving glipizide always pay attention to by scientific research personnel, but also fail the solution that obtained.
Summary of the invention
Technical problem to be solved by this invention there are provided a kind of glipizide tablet and preparation method thereof and application, to improve the drug dissolution of glipizide tablet.
To achieve these goals, the invention provides a kind of glipizide tablet, this glipizide tablet comprises with weight: grain diameter D50 is the glipizide 1% ~ 5% of 50 μm ~ 100 μm, solubilizing agent 1% ~ 10%, filler 50% ~ 90%, disintegrating agent 5% ~ 15%, lubricant 0.1% ~ 5%, and the binding agent of 2% ~ 15%.Wherein, glipizide preferred particulates particle diameter D50 is the glipizide of 50 μm ~ 75 μm.
In the present invention by by effective ingredient glipizide micronization, reduce the particle diameter of crude drug glipizide, increase solubilizing agent simultaneously and coordinate to improve drug release rate with glipizide, thus improve bioavailability, and then improve product quality.
In a kind of optimal way of the present invention, above-mentioned glipizide tablet comprises with weight: glipizide 2% ~ 5%, solubilizing agent 2% ~ 7%, filler 60% ~ 85%, disintegrating agent 5% ~ 10%, lubricant 0.1% ~ 3%, and the binding agent of 5% ~ 15%.
State on the invention in glipizide tablet, optional solubilizing agent includes but not limited to a kind of, two or more compositions in poloxamer, tween 80, sodium lauryl sulphate, wherein preferably adopts poloxamer.
State on the invention in glipizide tablet, optional filler includes but not limited to a kind of, two or more compositions in microcrystalline Cellulose, mannitol, starch, pregelatinized Starch, dextrin; Wherein, preferably adopt the mixture of microcrystalline Cellulose and starch, being more preferably weight ratio is the microcrystalline Cellulose of 5:1 ~ 1:5 and the mixture of starch.
State on the invention in glipizide tablet, optional disintegrating agent includes but not limited to as a kind of, two or more the compositions in sodium carboxymethyl cellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, polyvinylpolypyrrolidone or low-substituted hydroxypropyl cellulose; Wherein preferred carboxymethyl starch sodium.
State on the invention in glipizide tablet, optional lubricant includes but not limited to as a kind of, two or more the compositions in magnesium stearate, stearyl alcohol fumaric acid sodium, micropowder silica gel; Wherein preferred magnesium stearate.
State on the invention in glipizide tablet, optional binding agent includes but not limited to as a kind of, two or more the compositions in hydroxypropyl emthylcellulose, polyvidone, starch slurry, ethanol.The wherein mixture of preferred polyvidone and ethanol.
In the preferred embodiment of the present invention, above-mentioned glipizide tablet (in the label of described tablet) comprises with weight: the glipizide of 2.3%, the microcrystalline Cellulose of 54.2%, the starch of 18%, the binding agent of 9%, the Sodium Hydroxymethyl Stalcs of 7.2%, the poloxamer of 9%, 0.3% magnesium stearate.
Meanwhile, additionally provide a kind of preparation method of above-mentioned glipizide tablet in the present invention, it comprises the following steps: (1) takes each raw material in proportion; (2) glipizide that grain diameter D50 is 50 μm ~ 100 μm will be obtained after glipizide micronization, the glipizide after micronization, filler, solubilizing agent will be mixed with partial disintegration agent, form mixture A; (3) binding agent is mixed with the binding agent serosity that concentration is 5 ~ 50wt%, binder paste is joined soft material processed in mixture A, cross 15 ~ 20 mesh sieves to granulate, wet granular is dry under 30 ~ 50 DEG C of conditions, crosses 15 ~ 20 mesh sieves and carry out granulate after dry 0.5 ~ 1.5 hour; (4) the dry granule after granulate and lubricant and remaining disintegrating agent are mixed, scrobicula rushes in row tabletting, obtains glipizide tablet.
Preparation method of the present invention, technique is simple, easily prepares, and by controlling the granularity of glipizide, controlling the order by merging of each raw material simultaneously, can improve drug release rate, thus improves bioavailability, and then improves product quality.
In a kind of preferred implementation of the present invention, the glipizide that grain diameter D50 is 50 μm ~ 75 μm is obtained after glipizide micronization in the step (2) of above-mentioned preparation method, simultaneously, glipizide after sieving, filler, solubilizing agent with in formula ratio 4/5 disintegrating agent mix, form mixture A.More preferably, in mixture A, each raw material mixes by equal increments method.
Glipizide tablet prepared by the present invention is light in treatment, application in the medicine of moderate type 2 diabetes mellitus.Be specially adapted in the application for the treatment of in the medicine of light, the moderate type 2 diabetes mellitus (patient) of diet control and physical training 2-3 month unsatisfactory curative effect (being unsatisfied with).
Accompanying drawing illustrates:
Fig. 1 is according to embodiments of the invention 5,7,8 and the glipizide tablet accumulation dissolution determination result prepared according to comparative example 1-3 (glipizide and different solubilizing agent by variable grain particle diameter).
Detailed description of the invention:
Below in conjunction with the accompanying drawing in the embodiment of the present invention, technical scheme in embodiments of the invention is described in detail, but following embodiment and accompanying drawing are only understand the present invention, and the present invention can not be limited, the multitude of different ways that the present invention can be defined by the claims and cover is implemented.Unless otherwise, all technology used herein and scientific terminology have the identical meanings usually understood with general technical staff of the technical field of the invention.
Embodiment 1
Prescription
Preparation technology
(1) starch (binding agent) is mixed with 8wt% starch slurry by purified water is taken, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 100 μm, and take the glipizide sieved by recipe quantity, with in microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5 carboxymethyl starch sodium mix by equal increments method;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 2
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 75 μm, and take micronized glipizide by recipe quantity, with in microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5 polyvinylpolypyrrolidone mix by equal increments method;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain polyvinylpolypyrrolidone and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 3
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 50 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch, SDS and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 4
Prescription
Preparation technology:
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 50 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 15 mesh sieves and granulate, wet granular is dry under 30 DEG C of conditions, crosses 15 mesh sieves and carry out granulate after dry 1.5 hours;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 5
Prescription
Preparation technology:
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 50 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 6
Prescription
Preparation technology:
(1) measure recipe quantity ethanol, be mixed with the solution of 50wt% by purified water, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 50 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the polyvinylpolypyrrolidone of microcrystalline Cellulose, starch, tween 80 and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain polyvinylpolypyrrolidone and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 7
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with the PVP K30-alcoholic solution of 5wt%, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 75 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the crosslinked carboxymethyl fecula sodium of microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 50 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 0.5 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain crosslinked carboxymethyl fecula sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 8
Prescription
Preparation technology
(1) take the hypromellose of recipe quantity, be mixed with the solution of 2wt% by purified water, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 100 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 9
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50% alcoholic solution, is mixed with 5% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 100 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the low-substituted hydroxypropyl cellulose of microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain low-substituted hydroxypropyl cellulose and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 10
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 100 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Embodiment 11
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 100 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of mannitol, starch, poloxamer, SDS and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by magnesium stearate, the silicon dioxide of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Comparative example 1
Prescription
Preparation technology
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) take by recipe quantity the glipizide that grain diameter D50 is 180 μm, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch, poloxamer and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Comparative example 2
Prescription
Preparation technology:
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 50 μm, and take micronized glipizide by recipe quantity, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Comparative example 3
Prescription
Preparation technology:
(1) take recipe quantity PVP K30, joining concentration is in 50wt% alcoholic solution, is mixed with 5wt% PVP K30-alcoholic solution, in this, as binding agent;
(2) take by recipe quantity the glipizide that grain diameter D50 is 180 μm, mix by equal increments method with the carboxymethyl starch sodium of microcrystalline Cellulose, starch and recipe quantity 4/5;
(3) add suitable amount of adhesive soft material, cross 20 mesh sieves and granulate, wet granular is dry under 40 DEG C of conditions, crosses 20 mesh sieves and carry out granulate after dry 1 hour;
(4) by the magnesium stearate of the dry granule after granulate and recipe quantity and remain carboxymethyl starch sodium and mix;
(5) rush in row tabletting by Φ 6.5mm scrobicula after mix homogeneously, to obtain final product.
Quality investigation
Glipizide tablet sample prepared by Example 1-11 and the glipizide tablet sample prepared by comparative example 1-3, check its appearance character, content, related substance and dissolution according to quality standard under Chinese Pharmacopoeia version in 2010 two items, and compare.
Assay adopts high performance liquid chromatography (Chinese Pharmacopoeia version in 2010 two annex V D) to measure, by external standard method with calculated by peak area and get final product.
Related substances separation adopts high performance liquid chromatography (Chinese Pharmacopoeia version in 2010 two annex V D) to measure.
Dissolution test is according to dissolution method (Chinese Pharmacopoeia version in 2010 two annex XC first methods), with phosphate buffered solution (pH7.4) 500ml for dissolution medium, rotating speed is 100 turns per minute, operate in accordance with the law, through 30 minutes time, get solution 10ml, filter, get subsequent filtrate according to ultraviolet visible spectrophotometry (Chinese Pharmacopoeia version in 2010 two annex IV A), measure absorbance at the wavelength place of 222nm; Separately get glipizide reference substance and be about 12mg, accurately weighed, put in 50ml measuring bottle, add phosphate buffered solution (pH7.4) appropriate, put in water-bath and heat, dissolve, let cool to room temperature, add phosphate buffered solution (pH7.4) and be diluted to scale, shake up, precision measures 5ml, put in 200ml measuring bottle, be diluted to scale with dissolution medium, shake up, be measured in the same method.Calculate the stripping quantity of every sheet, limit is 80% of labelled amount, should conform with the regulations.
Content of the test
Example sample and reference examples sample, check its appearance character, content, related substance and dissolution according to quality standard under Chinese Pharmacopoeia version in 2010 two items, and compare.Result of the test is in table 1 and Fig. 1 (according to embodiments of the invention 5,7,8 and the glipizide tablet accumulation dissolution determination result prepared according to comparative example 1-3 (glipizide and different solubilizing agent by variable grain particle diameter)).
The each embodiment of table 1 and comparative example quality control assays result
| Sample ID | Appearance character | Assay (%) | Related substance (%) | Dissolution (%) |
| Quality standard | For white tablets or off-white color sheet | 90.0～110.0 | <1.0 | >80％ |
| Embodiment 1 | White tablets | 99.5 | 0.31 | 92.3 |
| Embodiment 2 | White tablets | 99.5 | 0.35 | 91.7 |
| Embodiment 3 | White tablets | 99.3 | 0.41 | 88.4 |
| Embodiment 4 | White tablets | 99.4 | 0.37 | 84.1 |
| Embodiment 5 | White tablets | 99.5 | 0.42 | 96.0 |
| Embodiment 6 | White tablets | 101.3 | 0.34 | 90.1 |
| Embodiment 7 | White tablets | 99.7 | 0.31 | 87.1 |
| Embodiment 8 | White tablets | 99.1 | 0.42 | 80.4 |
| Embodiment 9 | White tablets | 99.6 | 0.35 | 86.2 |
| Embodiment 10 | White tablets | 100.2 | 0.37 | 82.6 |
| Embodiment 11 | White tablets | 99.9 | 0.46 | 89.8 |
| Comparative example 1 | White tablets | 99.7 | 0.38 | 54.1 |
| Comparative example 2 | White tablets | 100.7 | 0.49 | 56.7 |
| Comparative example 3 | White tablets | 99.8 | 0.41 | 32.4 |
As can be seen from embodiment in table 1 and Fig. 1 and comparative example quality versus experimental result, the dissolution of embodiment in dissolution medium is obviously better than comparative example group, and single use solubilizing agent or its result of extraction of single pulverizing are obviously inferior to and had both added solubilizing agent and carry out micronizing to crude drug simultaneously, equally also absolutely proved the advantage of solubilizing agent and crude drug micronizing conbined usage in the present invention, the glipizide tablet obtained by the present invention is improving the advantage in dissolution.
As can be seen here, drug regimen of glipizide provided by the present invention and preparation method thereof improves the dissolution of medicine preferably, effectively raise the bioavailability of medicine, make the glipizide tablet stripping aspect in vitro obtained by the present invention have unique superiority.And glipizide tablet provided by the present invention has good stability, improve the quality of medicine preferably, preparation is simple, reproducible, quality controllable, is applicable to suitability for industrialized production.
Claims (10)
1. a glipizide tablet, it is characterized in that, described glipizide tablet comprises with weight: grain diameter D50 is the glipizide 1% ~ 5% of 50 μm ~ 100 μm, solubilizing agent 1% ~ 10%, filler 50% ~ 90%, disintegrating agent 5% ~ 15%, lubricant 0.1% ~ 5%, and the binding agent of 2% ~ 15%.
2. the glipizide tablet according to claims 1, it is characterized in that, described glipizide tablet comprises with weight: glipizide 2% ~ 5%, solubilizing agent 2% ~ 7%, filler 60% ~ 85%, disintegrating agent 5% ~ 10%, lubricant 0.1% ~ 3%, and the binding agent of 5% ~ 15%.
3. the glipizide tablet according to claims 1, is characterized in that, described glipizide to be grain diameter D50 the be glipizide of 50 μm ~ 75 μm.
4. the glipizide tablet according to claims 1, is characterized in that, in described active label,
Described solubilizing agent is a kind of, two or more compositions in poloxamer, tween 80, sodium lauryl sulphate;
Described filler is a kind of, two or more compositions in microcrystalline Cellulose, mannitol, starch, pregelatinized Starch, dextrin;
Described disintegrating agent is a kind of, two or more compositions in sodium carboxymethyl cellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, polyvinylpolypyrrolidone or low-substituted hydroxypropyl cellulose;
Described lubricant is a kind of, two or more compositions in magnesium stearate, stearyl alcohol fumaric acid sodium, micropowder silica gel;
Described binding agent is a kind of, two or more compositions in hydroxypropyl emthylcellulose, polyvidone, starch slurry, ethanol.
5. the glipizide tablet according to claims 1, is characterized in that, described filler is the mixture of microcrystalline Cellulose and starch; Preferably, the weight ratio of microcrystalline Cellulose and starch is 5:1 ~ 1:5.
6. the glipizide tablet according to claims 1, it is characterized in that, described glipizide tablet comprises with weight: the glipizide of 2.3%, the microcrystalline Cellulose of 54.2%, the starch of 18%, the binding agent of 9%, the Sodium Hydroxymethyl Stalcs of 7.2%, the poloxamer of 9%, 0.3% magnesium stearate.
7. a preparation method for glipizide tablet according to claim 1, is characterized in that, comprises the following steps:
(1) each raw material is taken in proportion;
(2) by glipizide micronization, obtain the glipizide that grain diameter D50 is 50 μm ~ 100 μm, the glipizide after micronization, filler, solubilizing agent are mixed with partial disintegration agent, form mixture A;
(3) binding agent is mixed with the binding agent serosity that concentration is 5 ~ 50wt%, described binder paste is joined soft material processed in described mixture A, cross 15 ~ 20 mesh sieves to granulate, wet granular is dry under 30 ~ 50 DEG C of conditions, crosses 15 ~ 20 mesh sieves and carry out granulate after dry 0.5 ~ 1.5 hour;
(4) the dry granule after granulate and lubricant and remaining disintegrating agent are mixed, scrobicula rushes in row tabletting, obtains described glipizide tablet.
8. preparation method according to claim 7, it is characterized in that, the glipizide that grain diameter D50 is 50 μm ~ 75 μm is obtained after glipizide micronization in described step (2), simultaneously, glipizide after sieving, filler, solubilizing agent with in formula ratio 4/5 disintegrating agent mix, form described mixture A.
9. preparation method according to claim 8, is characterized in that, in described mixture A, each raw material mixes by equal increments method.
10. the application in the medicine of a glipizide tablet as claimed in claim 1, moderate type 2 diabetes mellitus light in treatment.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510626347.1A CN105213335B (en) | 2015-09-28 | 2015-09-28 | Glipizide tablet as well as preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510626347.1A CN105213335B (en) | 2015-09-28 | 2015-09-28 | Glipizide tablet as well as preparation method and application thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105213335A true CN105213335A (en) | 2016-01-06 |
| CN105213335B CN105213335B (en) | 2017-04-26 |
Family
ID=54982857
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510626347.1A Active CN105213335B (en) | 2015-09-28 | 2015-09-28 | Glipizide tablet as well as preparation method and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105213335B (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI607533B (en) * | 2016-08-31 | 2017-12-01 | 奇鋐科技股份有限公司 | Water-cooling radiator structure |
| CN107961224A (en) * | 2017-12-06 | 2018-04-27 | 齐鲁制药(海南)有限公司 | A kind of pazopanib piece and preparation method thereof |
| CN108042613A (en) * | 2017-12-29 | 2018-05-18 | 广州仁恒医药科技股份有限公司 | A kind of pharmaceutical composition containing Glipizide and preparation method thereof |
| CN112535665A (en) * | 2020-12-14 | 2021-03-23 | 宁夏医科大学 | Glipizide solid dispersion, preparation method thereof, glipizide solid dispersion tablet containing glipizide solid dispersion and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1726916A (en) * | 2004-07-27 | 2006-02-01 | 江西省药物研究所 | Oral disintegration tablet for dropping blood sugar and preparation method |
| CN1742730A (en) * | 2005-09-29 | 2006-03-08 | 周卓和 | Method for preparing high stripping-degree hautriwaic glipizide capsule |
| CN102133205A (en) * | 2011-03-17 | 2011-07-27 | 山东新华制药股份有限公司 | Preparation method of glipizide osmotic pump controlled release tablet |
-
2015
- 2015-09-28 CN CN201510626347.1A patent/CN105213335B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1726916A (en) * | 2004-07-27 | 2006-02-01 | 江西省药物研究所 | Oral disintegration tablet for dropping blood sugar and preparation method |
| CN1742730A (en) * | 2005-09-29 | 2006-03-08 | 周卓和 | Method for preparing high stripping-degree hautriwaic glipizide capsule |
| CN102133205A (en) * | 2011-03-17 | 2011-07-27 | 山东新华制药股份有限公司 | Preparation method of glipizide osmotic pump controlled release tablet |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI607533B (en) * | 2016-08-31 | 2017-12-01 | 奇鋐科技股份有限公司 | Water-cooling radiator structure |
| CN107961224A (en) * | 2017-12-06 | 2018-04-27 | 齐鲁制药(海南)有限公司 | A kind of pazopanib piece and preparation method thereof |
| CN108042613A (en) * | 2017-12-29 | 2018-05-18 | 广州仁恒医药科技股份有限公司 | A kind of pharmaceutical composition containing Glipizide and preparation method thereof |
| CN112535665A (en) * | 2020-12-14 | 2021-03-23 | 宁夏医科大学 | Glipizide solid dispersion, preparation method thereof, glipizide solid dispersion tablet containing glipizide solid dispersion and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN105213335B (en) | 2017-04-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Batchelor et al. | Formulations for children: problems and solutions | |
| CN105147662A (en) | Pharmaceutical composition comprising glucopyranosyl diphenylmethane derivatives, pharmaceutical dosage form thereof, process for their preparation and uses thereof for improved glycemic control in a patient | |
| US9724374B2 (en) | Capsule containing total flavonoids of desmodium styracifolium, method for preparing the same and use | |
| CN101590007A (en) | A kind of metformin hydrochloride/voigelibo sugar-lowering oral preparation compositions and preparation thereof | |
| CN105213335A (en) | Glipizide tablet and preparation method thereof and application | |
| CN101816637B (en) | Leflunomide tablet preparation and preparation method thereof | |
| CN103893258A (en) | Oral solid preparation containing desmodium styracifolium general flavone and application thereof | |
| CN102267959B (en) | Repaglinide crystal, preparation method thereof, and solid oral preparation containing same | |
| CN103402506A (en) | Combination for treatment of diabetes mellitus | |
| CN112138007B (en) | Application of oxidized berberine in preparation of medicine for treating metabolic diseases and medicine composition containing oxidized berberine | |
| CN115120566A (en) | Oral pharmaceutical preparation containing repaglinide | |
| CN101167731A (en) | Dispersible tablet containing metformin and glibenclamide and preparation method thereof | |
| CN102716135B (en) | Lupenone prevents in preparation or treats the application in the product of diabetes | |
| CN102727894B (en) | A kind of pharmaceutical composition and application thereof for the treatment of diabetes and complication thereof | |
| CN102228457B (en) | Pharmaceutical composition for treating diabetes and complication thereof | |
| CN1331470C (en) | Method for preparing high stripping-degree hautriwaic glipizide capsule | |
| CN110302386A (en) | Combination product comprising limonoid and sulfonylureas | |
| CN103505466B (en) | Solid compound preparation containing metformin hydrochloride and glimepiride and its production and use | |
| CN107693555A (en) | A kind of medicine and purposes for treating diabetes | |
| CN100490808C (en) | Gliquilone slow-releasing preparation | |
| CN114557976B (en) | Scutellarin sustained release tablet and preparation method thereof | |
| JPH04368330A (en) | Sustained release preparation of pemirolast potassium | |
| US20210169839A1 (en) | Pediatric immediate-release formulation of the potassium channel opener ezogabine | |
| CN1686150A (en) | Notoginseng total saponin slow release preparation | |
| CN101756980A (en) | Melbine/migltol hypoglycemic oral preparation composition and preparation thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CP01 | Change in the name or title of a patent holder | ||
| CP01 | Change in the name or title of a patent holder |
Address after: 750002 the Ningxia Hui Autonomous Region street, Jinfeng District, Yinchuan City Fu Ning Lane No. 57 Patentee after: Ningxia Kang Ya pharmaceutical Limited by Share Ltd Address before: 750002 the Ningxia Hui Autonomous Region street, Jinfeng District, Yinchuan City Fu Ning Lane No. 57 Patentee before: Kangya Pharmaceutical Industry Co., Ltd., Ningxia |