CN102133205B - 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 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.The beginning of the eighties is for clinical, the glipizide oral absorption is quick and complete, and without 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 the tissue sensitivity to insulin, significantly strengthen the ability of peripheral tissues's ingestion of glucose.Simultaneously, glipizide also has the characteristics that reduce serum cholesterol and triglyceride, raising high density lipoprotein, increase the fibrinolysis activity, to improving and reduce diabetic complication, important meaning being arranged, is the effective and safe first-line drug for the treatment of noninsulindependent diabetes.
The Half-life in vivo of conventional glipizide ordinary tablet is shorter, is about 2～4 hours, within one day, need take two to three times.Pfizer company adopts GITS/OROS patented technology (US 5024843, US 5091190, US 5545413, US6361795) the exploitation controlled releasing penetrant pump of Alza company, and within 1994, in U.S.'s listing, commodity are by name
xL, Chinese commodity are by name auspicious easy
with conventional tablet, compare, osmotic pump tablet can 24 hours in vivo and in vitro in constant speed or approach the constant release medicine, with other sustained-release preparations, compare, its blood concentration fluctuation is minimum, the untoward reaction minimum.Administration number of times reduces simultaneously, and patient's compliance increases.Not affected by the factors such as media environment pH value, enzyme, gastrointestinal peristalsis, food, the inside and outside dependency is good.This osmotic pumps label is comprised 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 macromole in body fluid enter in the clothing film, only makes hydrone see 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 the 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 (being double-deck single chamber type osmotic pump preparation, also referred to as the push-pull osmotic pump preparation); Different is that the method adds merely the adjuvants such as alkaline auxiliary solvent to increase the dissolubility of glipizide, consequently the alkaline auxiliary solvent load is more, label weight is larger, 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 the method, consequently glipizide discharges comparatively fast, but release is not desirable zero level release or approaches zero level release.Method provided by the invention is to adopt solid dispersion technology, and glipizide is distributed in molecularity in the mixture of multiple auxiliary materials, for improving dissolubility, has adopted the cosolvents such as sodium lauryl sulphate, Polysorbate, meglumine.
The patents such as US 5024843, US 5091190, US 5545413, CN 200610114125.2 are all that glipizide is prepared into to the double layer osmotic pump preparation, adopt the push-pull osmotic pump technology, and this preparation method needs Double layer pellet, twice coating.Need to use bi-layer tablet press in preparation, this equipment price costliness, need accurately to control medicated layer and push layer in preparation process.Need bi-layer tablet press due to double-layer osmotic pump tablet in preparation process, need controlled Factory Building facility, therefore technique is more complicated, inject capital into larger.Material melts at higher temperature when improving Double layer pellet, existing adopt polyvidone or and copolyvidone replace polyoxyethylated method (CN 200610114125.2).For simplifying technique, 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, the 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 the polyoxyethylene of high molecular, but adopts the combination of the multiple materials such as polyvidone, copolyvidone, carboxymethyl starch sodium, hypromellose, carbomer.This method is greatly improved the problem of high temperature melting in technique, make operating environment require to be reduced, but the 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 containing beta-cyclodextrin clathrate permeation pump release-controlling preparation, the method is that glipizide and beta-schardinger dextrin-are prepared into to cyclodextrin clathrate, be pressed into label with other adjuvants such as osmotic pressure promoter, tabletting excipient again, then wrap semi-transparent rete.The 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 technique 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 the method is not need to use bi-layer tablet press, shortcoming is the tablet weight prepared large (every agreement that contracts a film or TV play to an actor or actress reaches 700mg), supplementary product consumption is larger, 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 techniques are improved still comparatively complicated, CN 01128292.4 technique 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) the middle method of reporting, 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 been to provide a kind of preparation method for the glipizide osmotic pump preparation, the method adopts solid dispersion technology to significantly improve the dissolution velocity of glipizide, the hydrotropy adjuvant added has improved the dissolubility of glipizide, and the appropriate short penetrating agent added makes glipizide reach constant speed or approaches constant release.
A kind of preparation method of glipizide osmotic pump controlled release tablet, comprise the glipizide label will prepared, and through wrapping semi-transparent rete, laser boring and bag damp-proof layer, makes, and it is characterized in that preparing the glipizide label and comprise the steps:
(1) prepare solid dispersion: glipizide and pharmaceutically acceptable adjuvant are scattered in solvent, stir, after drying, pulverizing, obtain the glipizide solid dispersion;
(2) prepare label: by glipizide solid dispersion and pharmaceutically acceptable auxiliary materials and mixing, tabletting, prepare the glipizide label.
Glipizide consumption described in step (1) accounts for 5～60wt.% of solid dispersion gross weight, preferred 10～40wt.%, and solvent volume, with the ml metering, be 2～20 times of solid dispersion gross weight, solid dispersion be take g as the unit metering.
Glipizide solid dispersion described in step (2) accounts for 5～50wt.% of label gross weight, preferably 10～40wt.%.
Pharmaceutically acceptable adjuvant described in 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 sodium stearyl fumarate.
Pharmaceutically acceptable adjuvant described in step (1) is that polyvidone is or/and meglumine.
Pharmaceutically acceptable adjuvant described in 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 sodium stearyl fumarate.
Pharmaceutically acceptable adjuvant described in step (2) is hypromellose, sodium chloride and magnesium stearate.
Solvent described in step (1) is a kind of or its combination in water, acetone, ethanol, isopropyl alcohol or methanol, preferably acetone.
Wrapping semi-transparent rete, laser boring and bag damp-proof layer carries out according to existing conventional osmotic pumps technique.
Wrap semi-transparent rete: cellulose acetate 398-10 and plasticizer are dissolved in acetone, make coating solution, the glipizide label prepared is carried out to coating and drying.Described plasticizer is one or more the combination in triacetin, Polyethylene Glycol, dimethyl phthalate, triethyl citrate, and wherein Polyethylene Glycol is one or more the combination in PEG400, Macrogol 4000, Macrogol 600, polyethylene glycol 6000 and PEG3350.
Laser boring: the tablet that will wrap after semi-transparent rete carries out laser boring.Wrap the tablet after semi-transparent rete, can only make a call to an aperture on one side, also can on 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.
At first the present invention prepares solid dispersion, more successively through preparing label, wrap semi-transparent rete, laser boring and bag damp-proof layer make, and both do not increase the complexity of technique, also do not strengthen the weight of tablet.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, employing primary osmotic pump technology can solve the stripping problem of glipizide, and the release curve is zero level or approaches 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.), by adding in right amount short penetrating agent (as sodium chloride etc.) to regulate osmotic pressure, make glipizide reach constant speed or approach constant release.The present invention has advantages of that technique is simple, cost is low, patient easily accepts and therapeutic effect is good.
The accompanying drawing explanation
Fig. 1 is tablet schematic diagram after the bag semipermeable membrane:
1, glipizide label; 2, semi-transparent rete.
Fig. 2 is tablet schematic diagram after the bag damp-proof layer:
1, glipizide label; 2, semi-transparent rete; 3, damp-proof layer.
The releasing curve diagram that Fig. 3 is Glipizide XL.
The releasing curve diagram that Fig. 4 is embodiment 1.
The releasing curve diagram that Fig. 5 is embodiment 2.
The releasing curve diagram that Fig. 6 is embodiment 3.
The releasing curve diagram that Fig. 7 is embodiment 4.
The releasing curve diagram that Fig. 8 is 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, lower with) put in a container, add PVP K30 (American I SP company, lower with) and sodium lauryl sulphate (German Congis company, lower same) make its dissolving or be uniformly dispersed, the acetone soln insulation, at 35 ℃, is added to glipizide (Weihai Disu Pharmaceutical Co., Ltd., lower same) while stir, lasting stirring is uniformly dispersed it, drying, make loss on drying in 2%, crosses 24 mesh sieves.
B: the preparation of label
Prescription:
Get glipizide solid dispersion, meglumine (Shanghai Pharmaceutical Group company limited, PVP K30, hypromellose E50 (U.S. Dow company down together),, sodium chloride (Tianjin sea light pharmaceutcal corporation, Ltd down together),, lower same) mix homogeneously, add again magnesium stearate (Liaocheng A Hua pharmaceutical Co. Ltd, lower same) mix homogeneously.Be placed in rotary tablet machine (C& The C800 type, Beijing wound Bo Jiawei Science and Technology Ltd., lower same) middle tabletting, Hardness Control is at 85N.
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in a container, while stir, add cellulose acetate (U.S. Eastman company, lower same), stir until dissolve, add again water and PEG400 (Huian, Xi'an cellulose chemical industry company limited), stir until dissolve, as coating solution.By above-mentioned label be placed in high-efficiency coating machine (the BGB-5B type, Pharmaceutical Equipment Factory, Wenzhou City, lower with) in, it is 30 ℃ that inlet temperature is set, the rotating speed of seed-coating machine is 6rpm, air intake air pressure is 0.1MPa, the control strip temperature remains on 20 ℃, make its weightening finish 5.5%.Tablet after the taking-up coating, be placed in 40 ℃ of dry 24h of baking oven.
D: above-mentioned tablet is got in laser boring, is placed in laser-beam drilling machine (Nanjing Ruichi Electronic Technology Engineering Industrial Co., Ltd., lower with) hopper, at tablet, wherein on one side, carries out laser boring.Regulate parameter, it is 0.8mm that pore size is set.
E: the coating of damp-proof layer is got the Europe bar that the trade mark is YS-2-7063
coating powder (Shanghai Colorcon Coating Technology Co., Ltd, lower same), the preparation solid content is about 8% coating solution, and the tablet after above-mentioned laser boring is carried out to 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 a container; add Tween 80 (Shanghai holy space chemical industry company limited; lower with), lactose (Shanghai Huamao Pharmaceutical Co, lower with) and hypromellose E3 (U.S. Dow company, lower with) 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, PVP K30, PEG-8 000 (Huian, Xi'an cellulose chemical industry company limited), sodium chloride mix homogeneously, then add the magnesium stearate mix homogeneously.Tabletting, Hardness Control is at 100N.
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in a container, while stir, add cellulose acetate, stir until dissolve, then add successively PEG3350 (German Clariant company) and triacetin (U.S. Eastman company), stir until dissolving, as coating solution.Above-mentioned label is placed in to high-efficiency coating machine, and it is 35 ℃ that inlet temperature is set, and the rotating speed of seed-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 after the taking-up coating, be placed in 40 ℃ of dry 48h of baking oven.
D: above-mentioned tablet is got in laser boring, is placed in the laser-beam drilling machine hopper, tablet wherein the one side on carry out laser boring.Regulate parameter, it is 0.8mm that pore size is set.
E: the coating of damp-proof layer is got the Europe bar that the trade mark is YS-2-7063
coating powder, the preparation solid content is about 8% coating solution, and the tablet after above-mentioned laser boring is carried out to 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 a container, adds meglumine, hypromellose E15 (U.S. Dow company, lower with) and mannitol (French Roquette company) make its dissolving or are uniformly dispersed, as water, standby.Get 95% ethanol and put in another container, add glipizide to make its dispersion, as the ethanol phase.Under continue stirring, by water slowly join ethanol mutually in.Continue stir about 30 minutes after adding, drying, make loss on drying in 2%, crosses 24 mesh sieves again.
B: the preparation of label
Prescription:
Get the 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
The Europe bar that to get the trade mark be 03B-63148
coating powder (Shanghai Colorcon Coating Technology Co., Ltd, lower same), water is mixed with solid content and is about 8% coating solution, and above-mentioned label is carried out to coating, drying.
D: the coating of semipermeable membrane
Prescription:
Get acetone and put in a container, while stir, add cellulose acetate, stir until dissolve, then add successively water, Macrogol 4000 and dimethyl phthalate (U.S. Eastman company), stir until dissolve, as coating solution.Above-mentioned label is placed in to high-efficiency coating machine, and it is 40 ℃ that inlet temperature is set, and the rotating speed of seed-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 after the taking-up coating, be placed in 40 ℃ of dry 48h of baking oven.
E: above-mentioned tablet is got in laser boring, is placed in the laser-beam drilling machine hopper, and on the two sides of tablet, each makes a call to an aperture, and pore size is 0.8mm.
F: the damp-proof layer coating is got the Europe bar that the trade mark is YS-2-7063
coating powder, the preparation solid content is about 8% coating solution, and the tablet after above-mentioned laser boring is carried out to 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 a container, adds meglumine, poloxamer and PEG 8000 make its dissolving or are uniformly dispersed, as water, standby.Get 95% ethanol and put in another container, add glipizide to make its dispersion, as the ethanol phase.Under continue stirring, by water slowly join ethanol mutually in.Continue stir about 30 minutes after adding, drying, make loss on drying in 2%, crosses 18 mesh sieves again.
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 again magnesium stearate, mix 5min.Tabletting, Hardness Control is at 130N.
C: the coating of sealing coat
The Europe bar that to get the trade mark be 03B-63148
coating powder, water is mixed with solid content and is about 8% coating solution, and above-mentioned label is carried out to coating, drying.
D: the coating of semipermeable membrane
Prescription:
Get acetone and put in a container, while stir, add cellulose acetate, stir until dissolve, then add successively Macrogol 600 and triethyl citrate, stir until dissolve, as coating solution.Above-mentioned label is placed in to high-efficiency coating machine, and it is 30 ℃ that inlet temperature is set, and the rotating speed of seed-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 after the taking-up coating, be placed in 40 ℃ of dry 48h of baking oven, to remove unilateral residual organic solvent.
E: above-mentioned tablet is got in laser boring, is placed in the laser-beam drilling machine hopper, and on the two sides of tablet, each makes a call to an aperture, and pore size is 0.8mm.
F: the damp-proof layer coating is got the Europe bar that the trade mark is YS-2-7063
coating powder, the preparation solid content is about 8% coating solution, and the tablet after above-mentioned laser boring is carried out to 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 a container, add PVP K30 and meglumine make its dissolving or are uniformly dispersed, the acetone soln insulation, at 35 ℃, is added to glipizide while stir, 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, then add the magnesium stearate mix homogeneously.Tabletting, Hardness Control is at 55N.
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in a container, while stir, add cellulose acetate, stir until dissolve, then add water and Macrogol 600, stir until dissolve, as coating solution.Above-mentioned label is placed in to high-efficiency coating machine, and it is 30 ℃ that inlet temperature is set, and the rotating speed of seed-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 after the taking-up coating, be placed in 40 ℃ of dry 48h of baking oven.
D: above-mentioned tablet is got in laser boring, is placed in the laser-beam drilling machine hopper, tablet wherein the one side on carry out laser boring.Regulate parameter, it is 0.8mm that pore size is set.
E: the coating of damp-proof layer is got the Europe bar that the trade mark is YS-2-7063
coating powder, the preparation solid content is about 8% coating solution, and the tablet after above-mentioned laser boring is carried out to coating, drying.
The above-mentioned glipizide osmotic pump controlled release tablet that makes 5mg.
Glipizide XL and embodiment 1～5 are measured to release:
Drug release determination method: adopt " two dissolutions of Chinese pharmacopoeia version in 2010 the 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, accurately weighed, add dissolve with methanol and be settled to 50ml, as stock solution.Get stock solution 1ml, add pH 7.4 phosphate buffer dilutions and be settled to 200ml, product solution (1) in contrast; Get stock solution 1ml, add pH 7.4 phosphate buffer dilutions and be settled to 100ml, product solution (2) in contrast; Get stock solution 1ml, add pH 7.4 phosphate buffer dilutions and be settled to 50ml, product solution (3) in contrast; Get stock solution 3ml, add pH 7.4 phosphate buffer dilutions and be settled to 100ml, product solution (4) in contrast; Get reference substance solution (1) 25ml, add pH 7.4 phosphate buffer dilutions and be settled to 50ml, product solution (5) in contrast; Get reference substance solution (4) 25ml, add pH 7.4 phosphate buffer dilutions and be settled to 50ml, product solution (6) in contrast; Get reference substance solution (5) 25ml, add pH 7.4 phosphate buffer dilutions and be settled to 50ml, product solution (7) in contrast.The test sample of above each time point and reference substance solution (1)～(7) are injected to liquid chromatograph, measure the glipizide release.
Liquid phase chromatogram condition: measure according to high performance liquid chromatography (Chinese Pharmacopoeia version appendix VD in 2010).With octadecylsilane chemically bonded silica, it is filler; With 0.1mol/L sodium dihydrogen phosphate (sodium hydroxide of take regulate pH to 6.00 ± 0.05): methanol (55: 45) is as 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 and is not less than 2000 by the glipizide peak, and the separating degree of glipizide peak and adjacent impurity peaks should meet the requirements.
Claims (1)
1. the preparation method of a glipizide osmotic pump controlled release tablet is characterized in that comprising the following steps:
A: the preparation of solid dispersion
Prescription:
Get acetone and put in a container, add PVP K30 and meglumine make its dissolving or are uniformly dispersed, the acetone soln insulation, at 35 ℃, is added to glipizide while stir, 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, then add the magnesium stearate mix homogeneously, tabletting, Hardness Control is at 55N;
C: the coating of semipermeable membrane
Prescription:
Get acetone and put in a container, while stir, add cellulose acetate, stir until dissolve, add again water and Macrogol 600, stir until dissolve, as coating solution, above-mentioned label is placed in to high-efficiency coating machine, it is 30 ℃ that inlet temperature is set, and the rotating speed of seed-coating machine is 8rpm, and air intake air pressure is 0.2MPa, the control strip temperature remains on 25 ℃, make its weightening finish 6.5%, the tablet after the taking-up coating, be placed in 40 ℃ of dry 48h of baking oven;
D: laser boring
Get above-mentioned tablet, be placed in the laser-beam drilling machine hopper, tablet wherein on one side, carry out laser boring, regulate parameter, it is 0.8mm that pore size is set;
E: the coating of damp-proof layer
Get the Opadry that the trade mark is YS-2-7063
coating powder, the preparation solid content is about 8% coating solution, and the tablet after above-mentioned laser boring is carried out to coating, drying;
The above-mentioned glipizide osmotic pump controlled release tablet that makes 5mg.
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| CN105213335B (en) * | 2015-09-28 | 2017-04-26 | 宁夏康亚药业有限公司 | Glipizide tablet as well as preparation method and application thereof |
| BR112020025689A2 (en) * | 2018-06-18 | 2021-03-16 | Subcuject Aps | OSMOTIC ACTUATOR FOR INJECTION DEVICE AND INJECTION DEVICE UNDERSTANDING SUCH OSMOTIC ACTUATOR |
| CN110917158B (en) * | 2019-12-09 | 2022-04-12 | 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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|---|---|---|---|---|
| CN1622799A (en) * | 2001-01-30 | 2005-06-01 | 科学和工业研究委员会 | Pharmaceutical composition for sustained or continuous releasing therapeutic active components |
| CN1692900A (en) * | 2005-03-01 | 2005-11-09 | 沈阳药科大学 | Single-chamber, double-layered osmosis pump control-release system with holes on two sides |
| CN1850057A (en) * | 2006-02-27 | 2006-10-25 | 合肥立方制药有限公司 | Method for preparing insoluble drug single-tablet-core single-chamber osmotic pump sustained-release preparations and its product |
| CN101940578A (en) * | 2010-08-25 | 2011-01-12 | 山东新华制药股份有限公司 | Medicament composition for curing type 2 diabetes and preparation method thereof |
-
2011
- 2011-03-17 CN CN201110065155XA patent/CN102133205B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1622799A (en) * | 2001-01-30 | 2005-06-01 | 科学和工业研究委员会 | Pharmaceutical composition for sustained or continuous releasing therapeutic active components |
| CN1692900A (en) * | 2005-03-01 | 2005-11-09 | 沈阳药科大学 | Single-chamber, double-layered osmosis pump control-release system with holes on two sides |
| CN1850057A (en) * | 2006-02-27 | 2006-10-25 | 合肥立方制药有限公司 | Method for preparing insoluble drug single-tablet-core single-chamber osmotic pump sustained-release preparations and its product |
| CN101940578A (en) * | 2010-08-25 | 2011-01-12 | 山东新华制药股份有限公司 | Medicament composition for curing type 2 diabetes and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 温利民 等.格列吡嗪渗透泵片的水分散体包衣法研制及其体外释药行为考察.《中国药业》.2009,第18卷(第22期),44-46. * |
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| Publication number | Publication date |
|---|---|
| CN102133205A (en) | 2011-07-27 |
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