Glipizide controlled release tablet and preparation method thereof

Abstract

The invention relates to a glipizide controlled-release tablet, the controlled-release tablet comprises a sustained-release pellet and pharmaceutically acceptable auxiliary materials, the sustained-release pellet comprises (a) a blank pellet core, (b) a drug coating layer wrapping the blank pellet core, and (c) a sustained-release coating layer wrapping the drug coating layer; the in-vitro release degree similarity factor f2 of the controlled release tablet and a commercially available glipizide osmotic pump tablet, namely, reiligenin, is greater than or equal to 50. According to the glipizide controlled release tablet, the defects that in the preparation process of commercially available glipizide osmotic pump tablets, a large amount of acetone is used as a coating solvent, and laser drilling has high requirements on production equipment and technological process are overcome, the production process is simple, and the product reproducibility is good.

Description

Technical Field

[0001] The present invention relates to the field of pharmaceutical preparations, and in particular to a glipizide controlled-release tablet and a preparation method thereof. Background Art

[0002] Diabetes is a common and frequently occurring disease in clinical practice. In recent years, the incidence of diabetes in my country has been on the rise. Diabetes is mainly divided into type 1 and type 2. The former is mainly caused by congenital insulin deficiency, while the latter is also known as adult-onset diabetes. The causes of the latter include genetic inheritance, obesity, mental state, infection, long-term excessive food intake, lack of exercise and other factors. Among them, the main pathology of type 2 diabetes is the abnormal secretion and insulin resistance of pancreatic β cells in tissues such as fat, liver and skeletal muscle.

[0003] Sulfonylureas are the first-line drugs for the treatment of type 2 diabetes. The hypoglycemic effect of sulfonylureas is mainly through binding to the sulfonylurea receptors on the pancreatic β-cell membrane, causing the closure of ATP-sensitive potassium ion channels, thereby causing the depolarization of the β-cell membrane and the opening of voltage-dependent calcium channels, increasing the intracellular calcium level, and then promoting insulin secretion.

[0004] Glipizide is a second-generation sulfonylurea oral hypoglycemic drug. It is mainly used clinically for patients with mild to moderate non-insulin-dependent type 2 diabetes who have no satisfactory effect with diet control alone and do not have severe diabetic complications. Glipizide is a potassium channel inhibitor. Its mechanism of action is to specifically bind to the sulfonylurea receptors on the pancreatic β cell membrane, thereby inhibiting K + The channel closes, causing a change in membrane potential, Ca 2+ The channel opens, increasing the intracellular Ca 2+ concentration, prompting pancreatic β cells to secrete insulin, thereby playing a role in lowering blood sugar.

[0005] Glipizide controlled-release tablets (trade name: ) is a special oral hypoglycemic dosage form that uses advanced gastrointestinal treatment system (GITS) technology. It consists of an osmotic-active drug core and a semipermeable membrane wrapped around the drug core. The semipermeable membrane that wraps the tablet is permeable to water, but not to drugs or osmotic excipients. When water from the gastrointestinal tract enters the tablet, the pressure of the permeation layer increases, squeezing the drug layer and releasing the drug through a tiny laser drilled hole on the film that wraps the drug. Glipizide controlled-release tablets release drugs uniformly and in a controlled manner through laser micropores, producing a stable plasma glipizide concentration within 24 hours, reducing the peak-to-valley fluctuations in glipizide concentrations, and only need to be taken once a day, which solves the inconvenience of taking medication multiple times a day and improves patient compliance.

[0006] Commercially available glipizide controlled-release tablets ( ) Using the osmotic pump process, the large amount of acetone coating solvent used in the preparation process will cause environmental pollution; and this process will cause the drug to be unable to be fully released, and 10% of the drug is overdosed during production. In addition, the quality of the osmotic pump product is affected by the laser drilling process, which has high requirements for production equipment and process, and the product quality is difficult to control, resulting in a high batch scrap rate and even product recall.

[0007] Currently, no similarity has been found between the currently available glipizide osmotic pump formulations ( )Related reports on glipizide controlled-release preparations that are equivalent in vitro and in vivo, do not require overdose, have a simple production process, and have good product reproducibility. Summary of the invention

[0008] The object of the present invention is to provide a glipizide controlled-release tablet which has similar in vitro dissolution behavior to the commercially available glipizide osmotic pump tablet Reiining, has a simple and environmentally friendly production process, low production cost, and controllable product quality.

[0009] In order to solve the above technical problems, the first aspect of the present invention provides a glipizide controlled-release tablet, which comprises sustained-release pellets and pharmaceutically acceptable excipients, wherein the sustained-release pellets comprise: (a) a blank pellet core, (b) a drug coating layer wrapped around the blank pellet core, and (c) a sustained-release coating layer wrapped around the drug coating layer; the in vitro release similarity factor f2 of the controlled-release tablet and the commercially available glipizide osmotic pump tablet Reining is greater than or equal to 50.

[0010] Preferably, the blank pellet core material in the sustained-release pellets is selected from one or more of sucrose, starch, lactose, microcrystalline cellulose, silicon dioxide, and calcium hydrogen phosphate. More preferably, the blank pellet core material is selected from one or more of sucrose, starch, microcrystalline cellulose, and silicon dioxide. Further preferably, the blank pellet core is a sucrose pellet core.

[0011] Preferably, the blank pill core accounts for 10-30% of the total weight of the controlled release tablet. More preferably, the blank pill core accounts for 15-25% of the total weight of the sustained release tablet. Further preferably, the blank pill core accounts for 18-22% of the total weight of the sustained release tablet. Further preferably, the blank pill core accounts for 20.9% of the total weight of the sustained release tablet.

[0012] Preferably, the drug coating layer contains glipizide and a binder.

[0013] Preferably, the glipizide in the drug coating layer accounts for 1-15% of the total weight of the controlled release tablet. More preferably, the glipizide in the drug coating layer accounts for 3-10% of the total weight of the controlled release tablet. Further preferably, the glipizide in the drug coating layer accounts for 5-8% of the total weight of the controlled release tablet. Further preferably, the glipizide in the drug coating layer accounts for 6.7% of the total weight of the controlled release tablet.

[0014] Preferably, the binder in the drug coating layer is selected from one or more of povidone, hydroxypropyl cellulose, and hydroxypropyl methylcellulose. More preferably, the binder is selected from one or more of povidone and hydroxypropyl methylcellulose. Further preferably, the binder is povidone. Further preferably, the binder is povidone K30.

[0015] Preferably, the binder in the drug coating layer accounts for 1-15% of the total weight of the controlled release tablet. More preferably, the binder in the drug coating layer accounts for 3-10% of the total weight of the controlled release tablet. Further preferably, the binder in the drug coating layer accounts for 5-8% of the total weight of the controlled release tablet. Further preferably, the binder in the drug coating layer accounts for 6.7% of the total weight of the controlled release tablet.

[0016] Preferably, the sustained-release coating layer comprises a sustained-release material, a plasticizer, a pore-forming agent and an anti-adhesive agent.

[0017] Preferably, the sustained-release material in the sustained-release coating layer is selected from one or more of ethyl cellulose and polymethacrylate. More preferably, the sustained-release material is polymethacrylate. Further preferably, the sustained-release material is one or more of Eudragit RL and Eudragit RS. Further preferably, the sustained-release material is Eudragit RL. Further preferably, the sustained-release material is Eudragit RL PO.

[0018] Preferably, the sustained-release material in the sustained-release coating layer accounts for 1-10% of the total weight of the controlled-release tablet. More preferably, the sustained-release material in the sustained-release coating layer accounts for 2-8% of the total weight of the controlled-release tablet. Further preferably, the sustained-release material in the sustained-release coating layer accounts for 3-7% of the total weight of the controlled-release tablet. Further preferably, the sustained-release material in the sustained-release coating layer accounts for 5-6% of the total weight of the controlled-release tablet. Further preferably, the sustained-release material in the sustained-release coating layer accounts for 5-5.7% of the total weight of the controlled-release tablet.

[0019] Preferably, the plasticizer in the sustained-release coating layer is selected from one or more of triethyl citrate, diethyl phthalate, and dibutyl sebacate. More preferably, the plasticizer is selected from one or more of triethyl citrate and diethyl phthalate. Further preferably, the plasticizer is triethyl citrate.

[0020] Preferably, the plasticizer in the sustained-release coating layer accounts for 0.1-3% of the total weight of the controlled-release tablet. More preferably, the plasticizer accounts for 0.3-2% of the total weight of the controlled-release tablet. Further preferably, the plasticizer accounts for 0.5-1.5% of the total weight of the controlled-release tablet. Further preferably, the plasticizer accounts for 0.6-1.3% of the total weight of the controlled-release tablet.

[0021] Preferably, the pore-forming agent in the sustained-release coating layer is selected from one or more of polyethylene glycol, polyvinyl pyrrolidone, and hydroxypropyl methylcellulose. More preferably, the pore-forming agent is polyethylene glycol. Further preferably, the pore-forming agent is polyethylene glycol 4000.

[0022] Preferably, the pore-forming agent in the sustained-release coating layer accounts for 0.1-1% of the total weight of the controlled-release tablet. More preferably, the pore-forming agent accounts for 0.2-0.8% of the total weight of the controlled-release tablet. Further preferably, the pore-forming agent accounts for 0.3-0.7% of the total weight of the controlled-release tablet. Further preferably, the pore-forming agent accounts for 0.33-0.67% of the total weight of the controlled-release tablet.

[0023] Preferably, the anti-adherent in the sustained-release coating layer is selected from one or more of talc, magnesium stearate, and silicon dioxide. More preferably, the anti-adherent is selected from one or more of talc and magnesium stearate. Further preferably, the anti-adherent is talc.

[0024] Preferably, the anti-adherent in the sustained-release coating layer accounts for 0.5-5% of the total weight of the controlled-release tablet. More preferably, the anti-adherent accounts for 1-4% of the total weight of the controlled-release tablet. Further preferably, the anti-adherent accounts for 1.5-3% of the total weight of the controlled-release tablet.

[0025] Preferably, the pharmaceutically acceptable excipients added to the sustained-release pellets in the controlled-release tablets are fillers, binders and lubricants.

[0026] Preferably, the filler added to the sustained-release pellets is selected from one or more of microcrystalline cellulose, lactose, polyethylene glycol, mannitol, and calcium hydrogen phosphate. More preferably, the filler is a composition of microcrystalline cellulose and polyethylene glycol. Further preferably, the filler is a composition of microcrystalline cellulose and polyethylene glycol 4000 in a weight ratio of 3:1-1:3. Further preferably, the filler is a composition of microcrystalline cellulose and polyethylene glycol 4000 in a weight ratio of 2:1-1:2. Further preferably, the filler is a composition of microcrystalline cellulose and polyethylene glycol 4000 in a weight ratio of 1:1. Further preferably, the filler is a composition of microcrystalline cellulose 101 and polyethylene glycol 4000 in a weight ratio of 1:1.

[0027] Preferably, the filler added to the sustained-release pellets accounts for 30-70% of the total weight of the controlled-release tablets. More preferably, the filler accounts for 40-60% of the total weight of the controlled-release tablets. Further preferably, the filler accounts for 47.7-54.3% of the total weight of the controlled-release tablets.

[0028] Preferably, the binder added to the sustained-release pellets is selected from one or more of povidone, hydroxypropyl cellulose, and hydroxypropyl methylcellulose. More preferably, the binder is selected from one or more of povidone and hydroxypropyl methylcellulose. Further preferably, the binder is povidone. Further preferably, the binder is povidone K30.

[0029] Preferably, the binder added to the sustained-release pellets accounts for 1-10% of the total weight of the controlled-release tablets. More preferably, the binder accounts for 3-8% of the total weight of the controlled-release tablets. Further preferably, the binder accounts for 4-6% of the total weight of the controlled-release tablets.

[0030] Preferably, the lubricant added to the sustained-release pellets is selected from one or more of magnesium stearate, talc or colloidal silicon dioxide. More preferably, the lubricant is selected from one or more of magnesium stearate or talc. Further preferably, the lubricant is magnesium stearate.

[0031] Preferably, the lubricant added to the sustained-release pellets accounts for 0.05-1% of the total weight of the controlled-release tablets. More preferably, the lubricant accounts for 0.1-0.5% of the total weight of the controlled-release tablets. Further preferably, the lubricant accounts for 0.1-0.3% of the total weight of the controlled-release tablets. Further preferably, the lubricant accounts for 0.13% of the total weight of the controlled-release tablets.

[0032] Preferably, the controlled-release tablet comprises sustained-release pellets, 40.7 mg microcrystalline cellulose 101, 40.7 mg polyethylene glycol 4000, 9 mg povidone K30 and 0.2 mg magnesium stearate, and the sustained-release pellets comprise (a) 31.3 mg sucrose pellet core, (b) a drug coating layer comprising 10 mg glipizide and 10 mg povidone K30, and (c) a sustained-release coating layer comprising 4.5 mg Eudragit RLPO, 0.5 mg polyethylene glycol 4000, 0.9 mg triethyl citrate and 2.3 mg talc.

[0033] Preferably, the controlled-release tablet comprises sustained-release pellets, 38 mg microcrystalline cellulose 101, 38 mg polyethylene glycol 4000, 9 mg povidone K30 and 0.2 mg magnesium stearate, and the sustained-release pellets comprise (a) 31.3 mg sucrose pellet core, (b) a drug coating layer comprising 10 mg glipizide and 10 mg povidone K30, and (c) a sustained-release coating layer comprising 7.5 mg Eudragit RLPO, 0.8 mg polyethylene glycol 4000, 1.5 mg triethyl citrate and 3.8 mg talc.

[0034] Preferably, the controlled-release tablet comprises sustained-release pellets, 37.1 mg microcrystalline cellulose 101, 37.1 mg polyethylene glycol 4000, 9 mg povidone K30 and 0.2 mg magnesium stearate, and the sustained-release pellets comprise (a) 31.3 mg sucrose pellet core, (b) a drug coating layer comprising 10 mg glipizide and 10 mg povidone K30, and (c) a sustained-release coating layer comprising 8.6 mg Eudragit RLPO, 0.9 mg polyethylene glycol 4000, 1.7 mg triethyl citrate and 4.3 mg talc.

[0035] Preferably, the controlled-release tablet comprises sustained-release pellets, 35.8 mg microcrystalline cellulose 101, 35.8 mg polyethylene glycol 4000, 9 mg povidone K30 and 0.2 mg magnesium stearate, and the sustained-release pellets comprise (a) 31.3 mg sucrose pellet core, (b) a drug coating layer comprising 10 mg glipizide and 10 mg povidone K30, and (c) a sustained-release coating layer comprising 10 mg Eudragit RLPO, 1 mg polyethylene glycol 4000, 2 mg triethyl citrate and 5 mg talc.

[0036] Preferably, the in vitro release similarity factor f2 of the controlled-release tablet and the commercially available glipizide osmotic pump tablet Reyining is greater than or equal to 55. More preferably, the in vitro release similarity factor f2 of the controlled-release tablet and the commercially available glipizide osmotic pump tablet Reyining is greater than or equal to 60.

[0037] The second aspect of the present invention provides a method for preparing the above-mentioned glipizide controlled-release tablets, which comprises the following steps:

[0038] (1) suspending glipizide and a binder in a solvent to prepare a drug suspension;

[0039] (2) placing blank pill cores in a bottom-spray fluidized bed, and using the drug suspension prepared in step (1) to fluidize the bed to obtain drug-loaded pill cores;

[0040] (3) dissolving the sustained-release material, plasticizer, and pore-forming agent in an organic solvent, and dispersing the anti-adhesive agent in the organic solvent to prepare a sustained-release layer coating suspension;

[0041] (4) placing the drug-loaded pellet cores obtained in step (2) into a bottom-spray fluidized bed, and coating the fluidized bed sustained-release layer with the coating suspension prepared in step (3) to obtain sustained-release pellets;

[0042] (5) mixing the sustained-release pellets obtained in step (4) with the filler in a high-efficiency wet granulator, spraying an aqueous binder solution, and drying in a fluidized bed to obtain dry granules;

[0043] (6) The dry granules obtained in step (5) are mixed evenly with a lubricant and pressed into glipizide controlled-release tablets.

[0044] Preferably, the solvent in step (1) is a mixed solvent of purified water and ethanol. More preferably, the solvent in step (1) is a mixed solvent of purified water and ethanol in a weight ratio of 8:2.

[0045] Preferably, the process parameters of the fluidized bed in step (2) are as follows: atomization pressure 1.3-1.7 bar, liquid spraying speed 5-20 g / min, air inlet temperature 50-60°C, and air inlet speed 70-150 cfm. More preferably, the process parameters of the fluidized bed in step (2) are as follows: atomization pressure 1.4-1.6 bar, liquid spraying speed 8-15 g / min, air inlet temperature 53-58°C, and air inlet speed 80-120 cfm. Further preferably, the process parameters of the fluidized bed in step (2) are as follows: atomization pressure 1.5 bar, liquid spraying speed 10 g / min, air inlet temperature 55°C, and air inlet speed 100 cfm.

[0046] Preferably, the organic solvent in step (3) is ethanol.

[0047] Preferably, the solid content of the sustained-release layer coating suspension in step (3) is 5-20% by weight. More preferably, the solid content of the sustained-release layer coating suspension in step (3) is 7-15% by weight. Further preferably, the solid content of the sustained-release layer coating suspension in step (3) is 10% by weight.

[0048] Preferably, the process parameters of the fluidized bed in step (4) are as follows: atomization pressure 1.3-1.7 bar, liquid spraying speed 5-20 g / min, air inlet temperature 30-40°C, and air inlet speed 70-150 cfm. More preferably, the process parameters of the fluidized bed in step (4) are as follows: atomization pressure 1.4-1.6 bar, liquid spraying speed 8-15 g / min, air inlet temperature 33-38°C, and air inlet speed 80-120 cfm. Further preferably, the process parameters of the fluidized bed in step (4) are as follows: atomization pressure 1.5 bar, liquid spraying speed 10 g / min, air inlet temperature 35°C, and air inlet speed 100 cfm.

[0049] Preferably, the process parameters of the fluidized bed in step (5) are as follows: inlet air temperature 40-50°C, inlet air speed 100-200cfm. More preferably, the process parameters of the fluidized bed in step (5) are as follows: inlet air temperature 43-48°C, inlet air speed 120-180cfm. Further preferably, the process parameters of the fluidized bed in step (5) are as follows: inlet air temperature 45°C, inlet air speed 150cfm.

[0050] The third aspect of the present invention provides use of the above-mentioned glipizide controlled-release tablets in the preparation of a drug for treating diabetes.

[0051] Preferably, the diabetes is type 2 diabetes.

[0052] The technical effects produced by the present invention are:

[0053] 1. The sustained-release pellets in the glipizide controlled-release tablets of the present invention contain both a drug coating layer and a sustained-release coating layer. By optimizing the type of sustained-release material (e.g., Eudragit RLPO) and content in the sustained-release coating layer, the sustained-release pellets are comparable to the commercially available glipizide osmotic pump tablets ( ) and ultimately achieve in vivo bioequivalence with commercially available osmotic pump preparations.

[0054] 2. Commercially available glipizide osmotic pump tablets ( ) The large amount of acetone coating solvent used in the preparation process will pollute the environment, and this process will cause the drug to be unable to be fully released. In the production, 10% of the drug is overdosed. In addition, the quality of the osmotic pump product is affected by the laser drilling process, and laser drilling has high requirements for production equipment and process. The product quality is difficult to control, resulting in a high batch scrap rate and even product recall. The glipizide controlled-release tablets of the present invention overcome the shortcomings of the above-mentioned osmotic pump preparations in terms of preparation process, do not require overdosing, have a simple production process, and have good product reproducibility. DETAILED DESCRIPTION

[0055] The following is a detailed description of an embodiment of the present invention. This embodiment is implemented on the premise of the technical solution of the present invention, and a detailed implementation method and a specific operation process are given, but the protection scope of the present invention is not limited to the following embodiment.

[0056] Test Example 1: In vitro release test of glipizide controlled-release tablets of the present invention

[0057] 1. Test prescription

[0058] 1.1. Prescription of controlled-release tablets

[0059] The prescriptions of Examples 1-4 are shown in the following table, the content of each component is in mg / tablet, and the specification is 10 mg.

[0060]

[0061] The prescriptions of Comparative Examples 1-3 are shown in the following table, the content of each component is in mg / tablet, and the specification is 10 mg.

[0062]

[0063]

[0064] 1.2. Preparation method of controlled release tablets

[0065] The preparation methods of Examples 1-4 and Comparative Examples 1-3 of the present invention are as follows:

[0066] (1) suspending 19000 times the single tablet prescription amount of povidone K30 and glipizide in 1.52 kg of a mixed solvent of purified water and ethanol (80 / 20, w / w) to prepare a drug suspension;

[0067] (2) placing sucrose pellet cores with a single-piece prescription amount of 19,000 times into a bottom-spray fluidized bed, adjusting the atomization pressure to 1.5 bar, the spray rate to 10 g / min, the inlet air temperature to 55 ° C, and the inlet air rate to 100 cfm, and performing fluidized bed drug deposition to obtain drug-loaded pellet cores;

[0068] (3) Dissolve 19000 times the single tablet prescription amount of Eudragit RL PO or Eudragit RS PO, triethyl citrate, and polyethylene glycol 4000 in an appropriate amount of ethanol, and disperse talc in the ethanol to prepare a sustained-release layer coating suspension (solid content of the suspension is 10%, w / w);

[0069] (4) placing the drug-loaded pellet cores with a single-tablet prescription weight of 19,000 times into a bottom-spray fluidized bed, adjusting the atomization pressure to 1.5 bar, the spray rate to 10 g / min, the inlet air temperature to 35° C., and the inlet air rate to 100 cfm, and coating the sustained-release layer to obtain sustained-release pellets;

[0070] (5) mixing the glipizide sustained-release pellets obtained in step (4) with 19,000 times the single-tablet prescription amount of microcrystalline cellulose 101 and polyethylene glycol 4000 (if any) in a high-efficiency wet granulator, and spraying the aqueous solution of povidone K30 (the amount of povidone K30 in the aqueous solution is 19,000 times the single-tablet prescription amount);

[0071] (6) drying the obtained wet granules in a fluidized bed to remove moisture to obtain dry granules, wherein the drying parameters are an inlet air temperature of 45° C. and an inlet air velocity of 150 cfm;

[0072] (7) The obtained dry granules were mixed evenly with 19,000 times the single-tablet prescription amount of magnesium stearate, and pressed into 19,000 glipizide controlled-release tablets.

[0073] 2. Test methods

[0074] The samples prepared in Examples 1-4 and Comparative Examples 1-3 and the original commercially available preparation (trade name: Ruiyining) were taken, and the release rate of glipizide controlled-release tablets was measured by the following method: the release medium was 675 ml of 0.1N HCl for the initial 2 hours, and adjusted to 900 ml of pH 6.8 phosphate buffer after 2 hours, paddle method, rotation speed 150 rpm, release medium temperature 37°C ± 0.5°C, samples were taken at 1, 2, 4, 8, 12, and 24 hours, respectively, and the release rate (%) of each test product at each time point was measured, and the dissolution similarity factor f2 of each embodiment and comparative example and the commercially available preparation (Ruiyining) was calculated.

[0075] 3. Test results

[0076] The in vitro release data of glipizide in the examples of the present invention and the comparative example control tablets are shown in Table 1 below.

[0077] Table 1 In vitro release of glipizide in the controlled release tablets of the present invention

[0078]

[0079] From the comparison of the dissolution data in Table 1 above, it can be seen that the in vitro dissolution similarity factors (f2) of glipizide of the controlled release tablets of Examples 1-4 of the present invention and the original commercially available preparation are all greater than or equal to 50, indicating that the in vitro release behaviors of the controlled release tablets of the present invention and the original commercially available osmotic pump preparation are highly similar, and it is expected that the controlled release tablets of Examples 1-4 of the present invention can achieve bioequivalence with the original commercially available preparation in vivo. In comparison, the in vitro dissolution similarity factor (f2) between Comparative Example 1 with a lower content of Eudragit RL PO and the original commercially available preparation is 41, the in vitro dissolution similarity factor (f2) between Comparative Example 2 using Eudragit RS PO as the sustained-release material and the original commercially available preparation is only 16, and the in vitro dissolution similarity factor (f2) between Comparative Example 3 using only microcrystalline cellulose as the external filler and the original commercially available preparation is 48, which confirms that the type and content of the sustained-release material in the sustained-release layer and the type of the external filler will have a significant impact on the in vitro release behavior of glipizide in the tablet, and thus produce a significant difference in the in vitro release rate from the original commercially available preparation. It is expected that the tablets of Comparative Examples 1-3 will be difficult to achieve bioequivalence with the original commercially available preparation in vivo.

[0080] Although specific embodiments of the present invention have been described, it will be appreciated by those skilled in the art that various changes and modifications may be made to the present invention without departing from the scope or spirit of the present invention. Therefore, the present invention is intended to cover all such changes and modifications that fall within the scope of the appended claims and their equivalents.

Claims

1. A glipizide controlled-release tablet, characterized in that: The controlled-release tablet comprises sustained-release pellets and pharmaceutically acceptable excipients, wherein the sustained-release pellets comprise: (a) a blank pellet core, (b) a drug coating layer wrapped around the blank pellet core, and (c) a sustained-release coating layer wrapped around the drug coating layer; the in vitro release similarity factor f2 of the controlled-release tablet and the commercially available glipizide osmotic pump tablet Reining is greater than or equal to 50.

2. The glipizide controlled-release tablet according to claim 1, characterized in that: The blank pellet core in the sustained-release pellet is selected from one or more of sucrose, starch, lactose, microcrystalline cellulose, silicon dioxide and calcium hydrogen phosphate.

3. The glipizide controlled-release tablet according to claim 1, characterized in that: The drug coating layer contains glipizide and a binder.

4. The glipizide controlled-release tablet according to claim 1, characterized in that: The sustained-release coating layer comprises a sustained-release material, a plasticizer, a pore-forming agent and an anti-adhesive agent.

5. The glipizide controlled-release tablet according to claim 1, characterized in that: The sustained-release material in the sustained-release coating layer is selected from one or more of ethyl cellulose and polymethacrylate.

6. The glipizide controlled-release tablet according to claim 5, characterized in that: The sustained-release material is Eudragit RL.

7. The glipizide controlled-release tablet according to claim 1, characterized in that: The pharmaceutically acceptable excipients added to the sustained-release pellets in the controlled-release tablets are fillers, adhesives and lubricants.

8. The glipizide controlled-release tablet according to claim 1, characterized in that: The in vitro release similarity factor f2 of the controlled-release tablet and the commercially available glipizide osmotic pump tablet Reyining is greater than or equal to 55.

9. The method for preparing the glipizide controlled-release tablets according to any one of claims 1 to 8, characterized in that: The following steps are involved: (1) suspending glipizide and a binder in a solvent to prepare a drug suspension; (2) placing blank pill cores in a bottom-spray fluidized bed, and using the drug suspension prepared in step (1) to fluidize the bed to obtain drug-loaded pill cores; (3) dissolving the sustained-release material, plasticizer, and pore-forming agent in an organic solvent, and dispersing the anti-adhesive agent in the organic solvent to prepare a sustained-release layer coating suspension; (4) placing the drug-loaded pellet cores obtained in step (2) into a bottom-spray fluidized bed, and coating the fluidized bed sustained-release layer with the coating suspension prepared in step (3) to obtain sustained-release pellets; (5) mixing the sustained-release pellets obtained in step (4) with the filler in a high-efficiency wet granulator, spraying an aqueous binder solution, and drying in a fluidized bed to obtain dry granules; (6) The dry granules obtained in step (5) are mixed evenly with a lubricant and pressed into glipizide controlled-release tablets.

10. Use of the glipizide controlled-release tablet according to any one of claims 1 to 8 in the preparation of a medicament for treating diabetes.

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