CN102133205A - Preparation method of glipizide osmotic pump controlled release tablet - Google Patents
Preparation method of glipizide osmotic pump controlled release tablet Download PDFInfo
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Abstract
The invention relates to a preparation method of a glipizide osmotic pump controlled release tablet. A glipizide tablet core is prepared by the following steps of semipermeable membrane wrapping, laser boring and damp-proof layer wrapping. The preparation method is characterized in that the preparation of the glipizide tablet core comprises preparation of solid dispersoid and preparation of the tablet core. In the preparation method, a solid dispersion technology is utilized, so that the dissolving speed of medicines is improved; the solubility of the glipizide is improved through the fluxing auxiliary materials; and a proper amount of penetration promoter is added to adjust the osmotic pressure so as to achieve constant-speed or approximately-constant-speed release. The invention has the advantages that the process is simple, the cost is low, the release tablet is easy to accept by patients and the treating effect is good.
Description
Technical field
The present invention relates to a kind of preparation method of glipizide osmotic pump controlled release tablet, particularly adopt solid dispersions technique and primary osmotic pump technology to prepare the glipizide osmotic pump controlled release tablet.
Background technology
Diabetes have become the third-largest disease of serious harm human health after cardiovascular and cerebrovascular vessel, malignant tumor.Glipizide (glipizide) is a kind of lipotropy weak acid, and the pKa value is 5.9, is second filial generation sulfonylurea oral antidiabetic drug.Be used for clinical the beginning of the eighties, the glipizide oral absorption is quick and complete, and there is not first pass effect, its mechanism of action is the insulin secretion ability that increases diabetics, strengthen the peripheral action of insulin, strengthen insulin and receptor binding capacity and tissue sensitivity, significantly strengthen the ability of peripheral tissues's ingestion of glucose insulin.Simultaneously, glipizide also has the serum cholesterol of reduction and triglyceride, raising high density lipoprotein, increases the active characteristics of fibrinolysis, to improving and reduce diabetic complication important meaning being arranged, is an effective and safe line medicine of treatment noninsulindependent diabetes.
The interior half-life of the body of conventional glipizide ordinary tablet is shorter, is about 2～4 hours, need take two to three times in one day.Pfizer company adopts GITS/OROS patented technology (US 5024843, US 5091190, US 5545413, US6361795) the exploitation controlled releasing penetrant pump of Alza company, and commodity were by name in U.S.'s listing in 1994
XL, Chinese commodity are by name auspicious easy
Compare with conventional tablet, osmotic pump tablet can 24 hours in vivo and in vitro in constant speed or near the constant release medicine, compare with other sustained-release preparations, its blood concentration fluctuation is minimum, the untoward reaction minimum.Administration number of times reduces simultaneously, and patient's compliance increases.Because drug release behavior is not subjected to factor affecting such as media environment pH value, enzyme, gastrointestinal peristalsis, food, the inside and outside dependency is good.This osmotic pumps label is made up of two-layer, and one deck is for containing the glipizide medicine layer, and another layer is the push layer of parmacodynamics-less activity (but having osmotically active).This label comprises the semi-transparent rete of cellulose acetate outward, and this semipermeable membrane can not make medicine and adjuvant see through the clothing film, can not make that macromole enters in the clothing film in the body fluid, and hydrone is seen through.
Document (Rajan K.Verma is arranged, Sanjay Garg.Development and evaluation of osmotically controlled oral drug delivery system of glipizide[J] .European Journal of Pharmaceutics and Biopharmaceutics.2004,57:513-525) the preparation method of report Glipizide controlled release tablets, what this method was identical with the present invention is all to belong to monolayer single chamber type osmotic pump preparation, is different to have gone on the market
XL (be double-deck single chamber type osmotic pump preparation, be also referred to as plug-type osmotic pump preparation); Different is that this method adds the dissolubility that adjuvants such as alkaline auxiliary solvent increase glipizide merely, consequently the alkaline auxiliary solvent load is more, label weight is bigger, simultaneously, in order to strengthen releasing degree, a large amount of PEG400 (PEG-400) and triacetin (Triacetin) have been used in the semi-transparent rete of this method, consequently glipizide discharges comparatively fast, is that ideal zero level discharges or discharges near zero level but discharge.Method provided by the invention is to adopt solid dispersion technology, and glipizide is distributed in molecularity in the mixture of multiple adjuvant, for improving dissolubility, has adopted cosolvents such as sodium lauryl sulphate, Polysorbate, meglumine.
Patents such as US 5024843, US 5091190, US 5545413, CN 200610114125.2 all are that glipizide is prepared into the double layer osmotic pump preparation, adopt plug-type osmotic pumps technology, and this preparation method needs double-deck tabletting, twice coating.Need to use bi-layer tablet press in preparation, this equipment price costliness needs accurately control medicated layer and push layer in the preparation process.Because double-layer osmotic pump tablet needs bi-layer tablet press in preparation process, need controlled Factory Building facility, so technology is complicated, it is bigger to inject capital into.Material melts at higher temperature when improving double-deck tabletting, existing adopt polyvidone or and copolyvidone replace polyoxyethylated method (CN 200610114125.2).For simplifying technology, the method (CN 01128292.4) that adopts cyclodextrin technology and primary osmotic pump technology to prepare osmotic pump tablet is arranged.
CN 200610114125.2 discloses a kind of preparation method of glipizide controlled releasing penetrant pump, this method is different from US5024843, US 5091190, US 5545413, US 6361795, the short osmopolymer of medicated layer is not to adopt low-molecular-weight polyoxyethylene, but adopts polyvidone, copolyvidone; The short osmopolymer of push layer neither adopt high-molecular weight polyoxyethylene, but adopts the combination of multiple materials such as polyvidone, copolyvidone, carboxymethyl starch sodium, hypromellose, carbomer.This method is greatly improved the problem of high temperature melting in the technology, make operating environment require to be reduced, but this method may be difficult to make stripping curve consistent with the sample that goes on the market.
CN 01128292.4 discloses a kind of preparation method that contains beta-cyclodextrin clathrate permeation pump release-controlling preparation, this method is that glipizide and beta-schardinger dextrin-are prepared into cyclodextrin clathrate, be pressed into label with other adjuvants such as osmotic pressure promoter, tabletting excipient again, wrap semi-transparent rete again.This method changes double-layer tablet into conventional single-layer sheet, and equipment changes conventional tablet machine into by bi-layer tablet press, and osmotic pumps technology is greatly improved.The preparation method that CN 01128292.4 patent provides is to adopt the primary osmotic pump technology to prepare the mono-layer osmotic pump preparation, though the advantage of this method is need not use bi-layer tablet press, shortcoming is the tablet weight prepared big (every agreement that contracts a film or TV play to an actor or actress reaches 700mg), supplementary product consumption is bigger, cost is higher, and the patient is difficult to take simultaneously.Prepare the cyclodextrin clathrate complex process simultaneously, consuming time longer, dry difficulty.
Though CN 200610114125.2 technologies have raising still comparatively complicated, CN 01128292.4 technology improves a lot, and the tablet of preparing is excessive, and cost is higher, and the patient is difficult to accept simultaneously.
The preparation method of glipizide osmotic pump preparation provided by the invention is different from existing patent, and (US 5024843, US5091190, US 5545413, US 6361795, CN 200610114125.2, CN 01128292.4) middle reported method, certainly (CN 03803286.4 also to be different from employing skeleton technology, CN 200410018247.2, US 6270797) prepare the method for slow releasing tablet, also be different from the method that adopts skeleton slow release while film controlled-release technology (US 6348469) to prepare slow releasing tablet, also be different from the method that adopts enteric coating technology (CN 200510200033.1) to prepare enteric-coated sustained-release tablet, (US 6720005 also to be different from employing stomach flotation technique, US 6733784) prepare the method for gastric residential tablet.
Summary of the invention
Technical problem to be solved by this invention has provided a kind of preparation method that is used for the glipizide osmotic pump preparation, this method adopts solid dispersion technology to significantly improve the dissolution velocity of glipizide, the hydrotropy adjuvant that adds has improved the dissolubility of glipizide, and an amount of short penetrating agent that adds makes glipizide reach constant speed or near constant release.
A kind of preparation method of glipizide osmotic pump controlled release tablet comprises the glipizide label that will prepare, and makes through wrapping semi-transparent rete, laser boring and bag damp-proof layer, it is characterized in that preparing the glipizide label and comprises the steps:
(1) preparation solid dispersion: glipizide and acceptable accessories are scattered in the solvent, stir, after drying, the pulverizing, get the glipizide solid dispersion;
(2) preparation label: with glipizide solid dispersion and acceptable accessories mixing, tabletting, preparation glipizide label.
Glipizide consumption described in the step (1) accounts for 5～60wt.% of solid dispersion gross weight, preferred 10～40wt.%, and solvent volume with the ml metering, is 2～20 times of the solid dispersion gross weight, solid dispersion is the unit metering with g.
Glipizide solid dispersion described in the step (2) accounts for 5～50wt.% of label gross weight, preferred 10～40wt.%.
Acceptable accessories described in the step (1) is one or more the combination in polyvidone, copolyvidone, Polyethylene Glycol, polyethylene glycol-vinyl alcohol graft copolymer, hypromellose, hyprolose, poloxamer, sodium lauryl sulphate, Polysorbate (Tween 80), meglumine, lactose, mannitol, sucrose or the sodium stearyl fumarate.
Acceptable accessories described in the step (1) is that polyvidone is or/and meglumine.
Acceptable accessories described in the step (2) is one or more the combination in polyvidone, copolyvidone, hypromellose, hyprolose, methylcellulose, polyoxyethylene, lactose, mannitol, sucrose, poloxamer, sodium lauryl sulphate, Polysorbate (Tween 80), meglumine, sodium chloride, magnesium stearate, stearic acid or the sodium stearyl fumarate.
Acceptable accessories described in the step (2) is hypromellose, sodium chloride and magnesium stearate.
Solvent described in the step (1) is a kind of or its combination in water, acetone, ethanol, isopropyl alcohol or the methanol, preferred acetone.
Wrapping semi-transparent rete, laser boring and bag damp-proof layer carries out according to existing conventional osmotic pumps technology.
Wrap semi-transparent rete: cellulose acetate 398-10 and plasticizer are dissolved in the acetone, make coating solution, the glipizide label for preparing is carried out coating and drying.Described plasticizer is one or more the combination in triacetin, Polyethylene Glycol, dimethyl phthalate, the triethyl citrate, and wherein Polyethylene Glycol is one or more the combination in PEG400, Macrogol 4000, Macrogol 600, polyethylene glycol 6000 and the Polyethylene Glycol 3350.
Laser boring: the tablet that will wrap behind the semi-transparent rete carries out laser boring.Wrap the tablet behind the semi-transparent rete, can only on one side, make a call to an aperture, also can on the two sides, each make a call to an aperture.
Bag damp-proof layer: adopt gastric solubility moistureproof coating powder preparation coating solution, will carry out coating and drying through the tablet of laser boring.
The present invention at first prepares solid dispersion, more successively through the preparation label, wrap semi-transparent rete, laser boring and bag damp-proof layer and make, both do not increased the complexity of technology, do not strengthen the weight of tablet yet.But adopt conventional tabletting method, prepare osmotic pump preparation.Test is found, adopt solid dispersion technology can significantly improve the dissolution velocity of glipizide, but the dissolubility of different adjuvant appreciable impact glipizide, based on above theory and test, adopt the primary osmotic pump technology can solve the stripping problem of glipizide, and the release curve is zero level or near zero level.
Compared with prior art, beneficial effect of the present invention is as follows:
The present invention adopts solid dispersion technology to significantly improve the dissolution velocity of medicine, improve the dissolubility of glipizide by the adjuvant of hydrotropy (as polyvidone and meglumine etc.), regulate osmotic pressure by the short penetrating agent of an amount of adding (as sodium chloride etc.) and make glipizide reach constant speed or near constant release.The present invention has the advantage that technology is simple, cost is low, patient easily accepts and therapeutic effect is good.
Description of drawings
Fig. 1 is a tablet sketch map behind the bag semipermeable membrane:
1, glipizide label; 2, semi-transparent rete.
Fig. 2 is a tablet sketch map behind the bag damp-proof layer:
1, glipizide label; 2, semi-transparent rete; 3, damp-proof layer.
Fig. 3 is the releasing curve diagram of Glipizide XL.
Fig. 4 is the releasing curve diagram of embodiment 1.
Fig. 5 is the releasing curve diagram of embodiment 2.
Fig. 6 is the releasing curve diagram of embodiment 3.
Fig. 7 is the releasing curve diagram of embodiment 4.
Fig. 8 is the releasing curve diagram of embodiment 5.
The specific embodiment
Below in conjunction with embodiment the present invention is described further.
A kind of preparation method of glipizide osmotic pump controlled release tablet:
A: the preparation of solid dispersion
Prescription:
Get acetone (Sinopec Group, down with) put in the container, add 30 POVIDONE K 30 BP/USP 30 (American I SP company, down with) and sodium lauryl sulphate (German Congis company, down with) make its dissolving or be uniformly dispersed, the acetone soln insulation at 35 ℃, is added glipizide (Weihai Disu Pharmaceutical Co., Ltd., down together) while stir, lasting stirring is uniformly dispersed it, drying makes loss on drying in 2%, crosses 24 mesh sieves.
B: the preparation of label
Prescription:
Get glipizide solid dispersion, meglumine (Shanghai medicine Group Co.,Ltd, 30 POVIDONE K 30 BP/USP 30, hypromellose E50 (U.S. Dow company down together),, sodium chloride (Tianjin sea light pharmaceutcal corporation, Ltd down together),, mix homogeneously down together), add magnesium stearate (Liaocheng A Hua pharmaceutical Co. Ltd, down together) mix homogeneously again.Place rotary tablet machine (C﹠amp; The C800 type, Beijing wound Bo Jiawei Science and Technology Ltd., down together) middle tabletting, Hardness Control is at 85N.
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in the container, add cellulose acetate (U.S. Eastman company, down together), stir, add entry and PEG400 (Huian, Xi'an cellulose chemical industry company limited) again, stir until dissolving, as coating solution until dissolving while stir.Above-mentioned label is placed in the high-efficiency coating machine (BGB-5B type, Pharmaceutical Equipment Factory, Wenzhou City are descended together), and it is 30 ℃ that inlet temperature is set, and the rotating speed of coating machine is 6rpm, and air intake air pressure is 0.1MPa, and the control strip temperature remains on 20 ℃, makes its weightening finish 5.5%.Tablet behind the taking-up coating places 40 ℃ of dry 24h of baking oven.
D: above-mentioned tablet is got in laser boring, places in laser-beam drilling machine (Nanjing Ruichi Electronic Technology Engineering Industrial Co., Ltd., the down with) hopper, wherein carries out laser boring on the one side at tablet.Adjusting parameter, it is 0.8mm that pore size is set.
E: the coating of damp-proof layer is got the Europe crust that the trade mark is YS-2-7063
Coating powder (Shanghai Colorcon Coating Technology Co., Ltd, down together), the preparation solid content is about 8% coating solution, the tablet after the above-mentioned laser boring is carried out coating, drying.
The above-mentioned glipizide osmotic pump controlled release tablet that makes 5mg.
A kind of preparation method of glipizide osmotic pump controlled release tablet:
A: the preparation of solid dispersion
Prescription:
Getting isopropyl alcohol puts in the container; add Tween 80 (Shanghai holy space chemical industry company limited; down with), lactose (Shanghai Huamao Pharmaceutical Co, down with) and hypromellose E3 (U.S. Dow company, down together) make its dissolving or be uniformly dispersed; aqueous isopropanol is incubated at 35 ℃; add glipizide while stirring, lasting stirring is uniformly dispersed it, drying; make loss on drying in 2%, cross 24 mesh sieves.
B: the preparation of label
Prescription:
Get glipizide solid dispersion, meglumine, 30 POVIDONE K 30 BP/USP 30, Polyethylene Glycol-8000 (Huian, Xi'an cellulose chemical industry company limited), sodium chloride mix homogeneously, add the magnesium stearate mix homogeneously again.Tabletting, Hardness Control is at 100N.
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in the container, add cellulose acetate while stir, stir until dissolving, add Polyethylene Glycol 3350 (German Clariant company) and triacetin (U.S. Eastman company) more successively, stirring is until dissolving, as coating solution.Above-mentioned label is placed high-efficiency coating machine, and it is 35 ℃ that inlet temperature is set, and the rotating speed of coating machine is 12rpm, and air intake air pressure is 0.1Mpa, and the control strip temperature remains on 25 ℃, makes its weightening finish 5.5%.Tablet behind the taking-up coating places 40 ℃ of dry 48h of baking oven.
D: above-mentioned tablet is got in laser boring, places the laser-beam drilling machine hopper, tablet wherein the one side on carry out laser boring.Adjusting parameter, it is 0.8mm that pore size is set.
E: the coating of damp-proof layer is got the Europe crust that the trade mark is YS-2-7063
Coating powder, the preparation solid content is about 8% coating solution, and the tablet after the above-mentioned laser boring is carried out coating, drying.
The above-mentioned glipizide osmotic pump controlled release tablet that makes 2.5mg.
A kind of preparation method of glipizide osmotic pump controlled release tablet:
A: the preparation of solid dispersion
Prescription:
Water intaking is put in the container, adds meglumine, hypromellose E15 (U.S. Dow company, down with) and mannitol (French Roquette company) and makes its dissolving or be uniformly dispersed, and is as water, standby.Get 95% ethanol and put in another container, add glipizide and make its dispersion, as the ethanol phase.Under continue stirring, with water slowly join ethanol mutually in.Continue stir about 30 minutes after adding again, drying makes loss on drying in 2%, crosses 24 mesh sieves.
B: the preparation of label
Prescription:
Get materials such as above glipizide solid dispersion, poloxamer (German BASF AG), hyprolose E50, polyoxyethylene N80 (U.S. Dow company), sodium chloride and magnesium stearate, mix homogeneously.Tabletting, Hardness Control is at 110N.
C: the coating of sealing coat
Getting the trade mark is the Europe crust of 03B-63148
Coating powder (Shanghai Colorcon Coating Technology Co., Ltd, down together), water is mixed with solid content and is about 8% coating solution, and above-mentioned label is carried out coating, drying.
D: the coating of semipermeable membrane
Prescription:
Get acetone and put in the container, add cellulose acetate, stir, add entry, Macrogol 4000 and dimethyl phthalate (U.S. Eastman company) more successively, stir until dissolving, as coating solution until dissolving while stir.Above-mentioned label is placed high-efficiency coating machine, and it is 40 ℃ that inlet temperature is set, and the rotating speed of coating machine is 14rpm, and air intake air pressure is 0.3MPa, and the control strip temperature remains on 30 ℃, makes its weightening finish 6.0%.Tablet behind the taking-up coating places 40 ℃ of dry 48h of baking oven.
E: above-mentioned tablet is got in laser boring, places the laser-beam drilling machine hopper, and each makes a call to an aperture on the two sides of tablet, and pore size is 0.8mm.
F: the damp-proof layer coating is got the Europe crust that the trade mark is YS-2-7063
Coating powder, the preparation solid content is about 8% coating solution, and the tablet after the above-mentioned laser boring is carried out coating, drying.
The above-mentioned glipizide osmotic pump controlled release tablet that makes 7.5mg.
A kind of preparation method of glipizide osmotic pump controlled release tablet:
A: the preparation of solid dispersion
Prescription:
Water intaking is put in the container, and adding meglumine, poloxamer and Polyethylene Glycol 8000 make its dissolving or be uniformly dispersed, and be as water, standby.Get 95% ethanol and put in another container, add glipizide and make its dispersion, as the ethanol phase.Under continue stirring, with water slowly join ethanol mutually in.Continue stir about 30 minutes after adding again, drying makes loss on drying in 2%, crosses 18 mesh sieves.
B: the preparation of label
Prescription:
Get above glipizide solid dispersion, poloxamer, 30 POVIDONE K 30 BP/USP 90 (American I SP company), hypromellose E5 (U.S. Dow company), sucrose (packet header, Inner Mongol Chinese-capital Industrial Co., Ltd.), sodium chloride mix homogeneously, add magnesium stearate again, mix 5min.Tabletting, Hardness Control is at 130N.
C: the coating of sealing coat
Getting the trade mark is the Europe crust of 03B-63148
Coating powder, water are mixed with solid content and are about 8% coating solution, and above-mentioned label is carried out coating, drying.
D: the coating of semipermeable membrane
Prescription:
Get acetone and put in the container, add cellulose acetate, stir, add Macrogol 600 and triethyl citrate more successively, stir until dissolving, as coating solution until dissolving while stir.Above-mentioned label is placed high-efficiency coating machine, and it is 30 ℃ that inlet temperature is set, and the rotating speed of coating machine is 12rpm, and air intake air pressure is 0.1MPa, and the control strip temperature remains on 20 ℃, makes its weightening finish 7.0%.Tablet behind the taking-up coating places 40 ℃ of dry 48h of baking oven, to remove the unilateral residual organic solvent that goes up.
E: above-mentioned tablet is got in laser boring, places the laser-beam drilling machine hopper, and each makes a call to an aperture on the two sides of tablet, and pore size is 0.8mm.
F: the damp-proof layer coating is got the Europe crust that the trade mark is YS-2-7063
Coating powder, the preparation solid content is about 8% coating solution, and the tablet after the above-mentioned laser boring is carried out coating, drying.
The above-mentioned glipizide osmotic pump controlled release tablet that makes 10mg.
Embodiment 5
A kind of preparation method of glipizide osmotic pump controlled release tablet:
A: the preparation of solid dispersion
Prescription:
Get acetone and put in the container, adding 30 POVIDONE K 30 BP/USP 30 and meglumine make its dissolving or are uniformly dispersed, and the acetone soln insulation at 35 ℃, is added glipizide while stir, and lasting stirring is uniformly dispersed it, and drying makes loss on drying in 2%, crosses 24 mesh sieves.
B: the preparation of label
Prescription:
Get glipizide solid dispersion, hypromellose E3, sodium chloride mix homogeneously, add the magnesium stearate mix homogeneously again.Tabletting, Hardness Control is at 55N.
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in the container, add cellulose acetate, stir, add entry and Macrogol 600 again, stir until dissolving, as coating solution until dissolving while stir.Above-mentioned label is placed high-efficiency coating machine, and it is 30 ℃ that inlet temperature is set, and the rotating speed of coating machine is 8rpm, and air intake air pressure is 0.2MPa, and the control strip temperature remains on 25 ℃, makes its weightening finish 6.5%.Tablet behind the taking-up coating places 40 ℃ of dry 48h of baking oven.
D: above-mentioned tablet is got in laser boring, places the laser-beam drilling machine hopper, tablet wherein the one side on carry out laser boring.Adjusting parameter, it is 0.8mm that pore size is set.
E: the coating of damp-proof layer is got the Europe crust that the trade mark is YS-2-7063
Coating powder, the preparation solid content is about 8% coating solution, and the tablet after the above-mentioned laser boring is carried out coating, drying.
The above-mentioned glipizide osmotic pump controlled release tablet that makes 5mg.
Glipizide XL and embodiment 1～5 are measured release:
Drug release determination method: adopt " two dissolutions of Chinese pharmacopoeia version in 2010, second device (oar method), 37 ℃, 50rpm, pH 7.4 phosphate buffers (40.8g potassium dihydrogen phosphate and 9.48g sodium hydroxide, join in the 6000mL purified water, regulate pH to 7.4 with hydrochloric acid or sodium hydroxide) 900ml, respectively 2,4,6,8,10,12,16,20h gets subsequent filtrate 3ml as test sample, adds pH 7.4 phosphate buffer 3ml simultaneously.Get the about 25mg of glipizide reference substance, the accurate title, decide, and adds dissolve with methanol and be settled to 50ml, as stock solution.Get stock solution 1ml, add the dilution of pH 7.4 phosphate buffers and be settled to 200ml, product solution (1) in contrast; Get stock solution 1ml, add the dilution of pH 7.4 phosphate buffers and be settled to 100ml, product solution (2) in contrast; Get stock solution 1ml, add the dilution of pH 7.4 phosphate buffers and be settled to 50ml, product solution (3) in contrast; Get stock solution 3ml, add the dilution of pH 7.4 phosphate buffers and be settled to 100ml, product solution (4) in contrast; Get reference substance solution (1) 25ml, add the dilution of pH 7.4 phosphate buffers and be settled to 50ml, product solution (5) in contrast; Get reference substance solution (4) 25ml, add the dilution of pH 7.4 phosphate buffers and be settled to 50ml, product solution (6) in contrast; Get reference substance solution (5) 25ml, add the dilution of pH 7.4 phosphate buffers and be settled to 50ml, product solution (7) in contrast.Liquid chromatograph is injected in the test sample and reference substance solution (1)～(7) of above each time point, measure the glipizide release.
Liquid phase chromatogram condition: measure according to high performance liquid chromatography (Chinese Pharmacopoeia version appendix in 2010 VD).With octadecylsilane chemically bonded silica is filler; With 0.1mol/L sodium dihydrogen phosphate (regulating pH to 6.00 ± 0.05 with sodium hydroxide): methanol (55: 45) is mobile phase; The detection wavelength is 225nm, and flow velocity is 1.0ml/min, 35 ℃ of column temperatures, sample size 20 μ L.Number of theoretical plate calculates by the glipizide peak and is not less than 2000, and the separating degree of glipizide peak and adjacent impurity peaks should meet the requirements.
Claims (9)
1. the preparation method of a glipizide osmotic pump controlled release tablet comprises the glipizide label that will prepare, and makes through wrapping semi-transparent rete, laser boring and bag damp-proof layer, it is characterized in that preparing the glipizide label and comprises the steps:
(1) preparation solid dispersion: glipizide and acceptable accessories are scattered in the solvent, stir, after drying, the pulverizing, get the glipizide solid dispersion;
(2) preparation label: with glipizide solid dispersion and acceptable accessories mixing, tabletting, preparation glipizide label.
2. preparation method according to claim 1, it is characterized in that: the glipizide consumption described in the step (1) accounts for 5～60wt.% of solid dispersion gross weight, preferred 10～40wt.%, solvent volume, with ml metering, be 2～20 times of solid dispersion gross weight.
3. preparation method according to claim 1 is characterized in that: the glipizide solid dispersion described in the step (2) accounts for 5～50wt.% of label gross weight, preferred 10～40wt.%.
4. preparation method according to claim 1 is characterized in that: the acceptable accessories described in the step (1) is one or more the combination in polyvidone, copolyvidone, Polyethylene Glycol, polyethylene glycol-vinyl alcohol graft copolymer, hypromellose, hyprolose, poloxamer, sodium lauryl sulphate, Polysorbate, meglumine, lactose, mannitol, sucrose or the sodium stearyl fumarate.
5. preparation method according to claim 4 is characterized in that: the acceptable accessories described in the step (1) is that polyvidone is or/and meglumine.
6. preparation method according to claim 1 is characterized in that: the acceptable accessories described in the step (2) is one or more the combination in polyvidone, copolyvidone, hypromellose, hyprolose, methylcellulose, polyoxyethylene, lactose, mannitol, sucrose, poloxamer, sodium lauryl sulphate, Polysorbate, meglumine, sodium chloride, magnesium stearate, stearic acid or the sodium stearyl fumarate.
7. preparation method according to claim 6 is characterized in that: the acceptable accessories described in the step (2) is hypromellose, sodium chloride and magnesium stearate.
8. preparation method according to claim 1 is characterized in that: the solvent described in the step (1) is a kind of or its combination in water, acetone, ethanol, isopropyl alcohol or the methanol.
9. preparation method according to claim 8 is characterized in that: the solvent described in the step (1) is an acetone.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105213335A (en) * | 2015-09-28 | 2016-01-06 | 宁夏康亚药业有限公司 | Glipizide tablet and preparation method thereof and application |
| CN110917158A (en) * | 2019-12-09 | 2020-03-27 | 济南精合医药科技有限公司 | Gliclazide microporous membrane osmotic pump sustained-release tablet 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 |
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| CN105213335A (en) * | 2015-09-28 | 2016-01-06 | 宁夏康亚药业有限公司 | Glipizide tablet and preparation method thereof and application |
| CN112601565A (en) * | 2018-06-18 | 2021-04-02 | 萨博库杰克特有限公司 | Osmotic actuator for an injection device and injection device including an osmotic actuator |
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| CN115300475A (en) * | 2022-07-20 | 2022-11-08 | 广西纯正堂制药有限公司 | Benzbromarone osmotic pump controlled release tablet and preparation method and application thereof |
| CN116407514A (en) * | 2023-05-10 | 2023-07-11 | 迪沙药业集团有限公司 | A kind of glipizide tablet composition and preparation method |
| CN116407514B (en) * | 2023-05-10 | 2025-03-14 | 迪沙药业集团有限公司 | Glipizide tablet composition and preparation method thereof |
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