CN118121557A - Paliperidone sustained release tablet and preparation method thereof - Google Patents
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Abstract
The invention provides a paliperidone sustained release tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The paliperidone sustained release tablet comprises the following components in percentage by weight: 1-9% of paliperidone, 15-25% of filler, 42-52% of tablet core slow release material, 10-19% of acidity regulator, 0.01-0.6% of antioxidant and 0.5-1% of lubricant; coating material: 4-5% of coating slow-release material, 0.5-1% of plasticizer, 1-2% of pore-forming agent and 1-2% of anti-adhesion agent. The paliperidone sustained release tablet provided by the invention selects a release mechanism of gel skeleton plus membrane control, the tablet core sustained release material and the acidity regulator are in a reasonable range, the dissolution of API is improved, and the types and the dosage of the acidity regulator improve the problems of unqualified related substances such as ketone impurities and oxidized impurities during the stability of the paliperidone sustained release tablet.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a paliperidone sustained release tablet and a preparation method thereof.
Background
Paliperidone is a metabolite of risperidone and is a novel antipsychotic agent for the treatment of schizophrenia, organic psychotic disorders, acute transient psychotic disorders, and manic episodes of bipolar disorders.
Paliperidone extended release tablets were developed by qinsheng corporation under the trade name: invega, FDA approval was obtained in 2006, specifications including 1.5mg, 3mg, 6mg and 9mg. The paliperidone sustained release tablet developed by Qiansheng company adopts OROS technology (oral osmotic pump administration controlled release system), and consists of a tablet core, an isolation coating layer, a semipermeable membrane coating layer and a coloring coating layer, wherein the tablet core consists of a boosting layer positioned at the bottom, a first drug layer positioned at the top and a second drug layer positioned in the middle, and 2 laser-perforated drug release pores are arranged on the isolation coating layer and the semipermeable membrane coating layer at one side of the first drug layer. Under the gastrointestinal tract environment, the coloring coating layer can be rapidly eroded, water enters the tablet core through the semipermeable membrane coating layer, hydrophilic materials in the tablet core and paliperidone form jelly, the medicine is pushed to be discharged from the medicine release small holes at the top end of the tablet, and insoluble components are discharged along with excrement. The semipermeable membrane coating layer can control the speed of water entering the tablet core, thereby controlling the drug release speed.
There are many reports in the prior art on paliperidone sustained release tablets, and as patent CN115737587B discloses a prescription composition of paliperidone sustained release tablets and a preparation process thereof, the paliperidone sustained release tablets consist of three parts of a drug-containing tablet core, a propelling tablet core and a permeable coating film. The drug-containing layer comprises active ingredients paliperidone, a framework material, a glidant and a lubricant, wherein the framework material in the drug-containing layer is a mixture of povidone and copovidone; the propulsion layer comprises a slow-release material, a framework material, an osmotic pressure promoter, a propulsion assisting material, pigments, a glidant and a lubricant, wherein the framework material in the propulsion layer is a mixture of polyvinyl acetate phthalate and copovidone, and the slow-release material is a mixture of carbomer 971PNF, carbomer 974PNF and carbomer 934 PNF. The invention also provides a preparation process of the paliperidone sustained release tablet, which firstly adopts a double-layer osmotic pump technology to control the release of the paliperidone, optimizes the use amount of carbomers in the propulsion layer, adopts carbomers with different viscosity grades to mix, and adopts polyvinyl acetate phthalate to replace hydroxypropyl cellulose to improve the stability of the propulsion layer under different pH values and different feeding states.
As further disclosed in patent CN114983961a, a paliperidone sustained-release tablet and a preparation method thereof are disclosed, the paliperidone sustained-release tablet comprises a tablet core and a semi-permeable coating layer coated outside the tablet core, the tablet core comprises a first drug-containing layer and a second drug-containing layer which are positioned at two ends, and a pushing layer between the two drug-containing layers; wherein the first drug-containing layer is added with a water absorbing agent and an extrusion lubricant, the pushing layer is added with a first retarder, and the second drug-containing layer is added with a second retarder. The paliperidone sustained release tablet can release part of paliperidone within 2 hours after administration, and can obviously improve the timeliness of paliperidone release under the condition of ensuring the sustained and controlled release effect.
Patent CN113616610B discloses a paliperidone sustained release tablet and a preparation method thereof, wherein the paliperidone sustained release tablet comprises a tablet core, an isolation layer coating, a sustained release layer coating and a color layer coating, a drug release small hole is formed on the sustained release coating layer, the isolation layer coating consists of hydroxypropyl cellulose and povidone, and the preparation method comprises the following steps: tablet core, isolation layer coating, slow release layer coating, perforation, and color layer coating. The paliperidone sustained release tablet has good stability, and related substances and contents of the paliperidone sustained release tablet all accord with the standard when the paliperidone sustained release tablet is placed for 6 months under the acceleration condition, and the dissolution curve is not changed obviously.
However, the stability of the existing product cannot better meet the requirement, so that a paliperidone sustained release tablet with good stability and a preparation method thereof are needed to be provided.
Disclosure of Invention
Based on the defects existing in the prior art, the invention aims to provide a paliperidone sustained release tablet and a preparation method thereof. The invention adopts a slow release mechanism of skeleton release and membrane controlled release, and the novel addition of the acidity regulator in the tablet core prescription improves the dissolution of the product in a medium with pH of 6.8, and simultaneously ensures the stability of the product.
In order to achieve the above purpose, the present invention adopts the following technical scheme:
The paliperidone sustained release tablet comprises the following components in percentage by weight:
Sheet core material: 1-9% of paliperidone, 15-35% of filler, 41.1-53% of tablet core slow release material, 9-20% of acidity regulator, 0.01-0.6% of antioxidant and 0.5-1% of lubricant;
coating material: 2-5% of coating slow-release material, 0.5-2% of plasticizer, 1-3% of pore-forming agent and 1-2% of anti-adhesion agent.
Wherein:
The filler is one or more of microcrystalline cellulose, anhydrous lactose, mannitol, starch and calcium hydrophosphate, and preferably anhydrous lactose.
The tablet core slow release material is one or more of polyoxyethylene, polyethylene glycol, hydroxypropyl methylcellulose, hydroxypropyl cellulose, ethyl cellulose and sodium alginate, and preferably the tablet core slow release material is a mixture of the hydroxypropyl methylcellulose and the polyoxyethylene; still preferably, the components account for 18-23% of hydroxypropyl methylcellulose and 20-30% of polyoxyethylene by weight percent of the tablet; more preferably, the components account for 19-22% of hydroxypropyl methylcellulose and 23-30% of polyoxyethylene by weight percent of the tablet.
The acidity regulator is inorganic acid, and the inorganic acid is potassium dihydrogen phosphate and/or sodium dihydrogen phosphate.
The antioxidant is one or more of butyl hydroxy anisole, dibutyl hydroxy toluene, propyl gallate and tertiary butyl hydroquinone; preferably, the antioxidant is butyl hydroxy anisole.
The lubricant is one or more of magnesium stearate, silicon dioxide, talcum powder, glyceryl behenate, stearic acid and sodium stearyl fumarate; preferably, the lubricant is magnesium stearate.
The pore-forming agent is one or more of hydroxypropyl methylcellulose, hydroxypropyl cellulose, methyl cellulose, polyvinyl alcohol and polyoxyethylene alcohol; preferably, the pore-forming agent is hypromellose.
The coating slow-release material is ethyl cellulose.
The plasticizer is triethyl citrate.
The anti-sticking agent is one or more selected from magnesium stearate, silicon dioxide, talcum powder, glyceryl behenate, stearic acid and sodium stearyl fumarate; preferably, the anti-sticking agent is talcum powder.
As some preferred embodiments, the mass ratio of the tablet core slow release material to the acidity regulator is 0.9:1-6:1, a step of;
Preferably, the mass ratio of the tablet core slow release material to the acidity regulator is 2:1-6:1.
The preparation method of the paliperidone sustained release tablet core is a direct-mixing tabletting method or a wet granulating method which are conventional in the field, and preferably a direct-mixing tabletting method.
Preferably, the preparation method of the paliperidone sustained release tablet comprises the following steps:
(1) Preparing a tablet core:
(1.1) mixing the active ingredient with a tablet core slow release material and an acidity regulator, and sieving to obtain a mixture;
(1.2) adding the mixture obtained in the step (1.1) and an antioxidant and a filler into a mixer, and uniformly mixing to obtain a premixed material;
(1.3) adding a lubricant into the premixed material obtained in the step (1.2), uniformly mixing, and tabletting to obtain tablet cores;
(2) Preparing a slow-release coating film:
(2.1) preparation of coating liquid: adding the pore-forming agent into the solvent, stirring until the pore-forming agent is completely dissolved, and obtaining a dispersion liquid for standby; adding the plasticizer and the coating slow-release material into the dispersion liquid, and stirring until the mixture is uniform to obtain coating liquid;
(2.2) coating: coating the tablet core obtained in the step (1.3) by using the coating liquid prepared in the step (2.1), and carrying out aging and drying treatment after the target weight gain is achieved to obtain the paliperidone sustained release tablet.
The solvent in the step (2.1) is purified water.
The solid content of the coating liquid in the step (2.1) is 10%; the target weight gain in step (2.2) is a coating weight gain of 6.5-7.5%;
the aging and drying operation in the step (2.2) is as follows: and (3) drying the coated tablet core for 3 hours at the temperature of 55 ℃ of a tablet bed.
Compared with the prior art, the invention has the beneficial effects that:
(1) The paliperidone sustained release tablet provided by the invention has different release mechanisms from a reference preparation, and the paliperidone sustained release tablet provided by the invention selects a release mechanism of gel skeleton and film control, and the dosage of the tablet core sustained release material and the acidity regulator is in a reasonable range, so that the dissolution of API is improved;
(2) The variety and the dosage of the selected acidity regulator improve the problem that the related substances ketone impurities and oxidized impurities are unqualified during the stability of the paliperidone sustained release tablets of other acidity regulators;
(3) Compared with the three-layer tablet of the reference preparation, the paliperidone sustained-release tablet provided by the invention can be prepared by adopting three-layer tabletting equipment based on simple process innovation and simple process direct mixing tabletting, a common tabletting machine and coating machine equipment, and has lower production cost.
Drawings
FIG. 1 dissolution profile of paliperidone extended release tablets prepared in example 1, examples 7-9 in pH6.8 medium.
Detailed Description
The following non-limiting examples will enable those of ordinary skill in the art to more fully understand the invention and are not intended to limit the invention in any way. The following is merely exemplary of the scope of the invention as it is claimed and many variations and modifications of the invention will be apparent to those skilled in the art in light of the disclosure, which should be construed to fall within the scope of the invention as claimed.
Where numerical ranges are provided in the examples, it is understood that unless otherwise stated herein, both endpoints of each numerical range and any number between the two endpoints are significant both in the numerical range. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.
The invention is further illustrated by means of the following specific examples. The various chemical reagents used in the examples of the present invention were obtained by conventional commercial means unless otherwise specified.
Example 1: paliperidone sustained release tablet
The prescription is as follows:
the preparation method comprises the following steps: the preparation method comprises the following steps:
(1) Preparing a tablet core:
(1.1) mixing paliperidone with hypromellose and polyoxyethylene through a screen to obtain a mixture;
(1.2) adding the mixture obtained in the step (1.1) and anhydrous lactose into a mixer, and uniformly mixing to obtain a premixed material;
(1.3) adding magnesium stearate into the pre-mixed material obtained in the step (1.2), uniformly mixing, and tabletting to obtain tablet cores;
(2) Preparing a slow-release coating film:
(2.1) preparation of coating liquid: adding hypromellose into purified water, stirring until the hypromellose is completely dissolved, and obtaining a dispersion liquid for standby; adding triethyl citrate, ethyl cellulose and talcum powder into the dispersion liquid, and stirring until the mixture is uniform to obtain coating liquid;
(2.2) coating: coating the tablet core obtained in the step (1.3) by using the coating liquid prepared in the step (2.1), and carrying out aging and drying treatment after the wet weight gain is 6.85%, wherein the treatment conditions are as follows: and (3) drying the coated tablet core for 3 hours at the temperature of 55 ℃ of a tablet bed to obtain the paliperidone sustained release tablet.
The dissolution behavior of the coated tablets in a medium at pH6.8 was examined and shown in Table 1 below.
TABLE 1
From the test data in Table 1, it can be seen that the dissolution rate of the 24h paliperidone extended release tablet was 65% and the 24h paliperidone extended release tablet could not be completely dissolved.
The paliperidone solubility decreases with increasing pH and the solubility of the paliperidone extended release tablets prepared in example 1 in solvents of different pH (20 ℃) was observed, see in particular table 2 below.
TABLE 2
Examples 2 to 6: paliperidone sustained release tablet
The tablet core prescription is as follows:
The preparation method comprises the following steps:
(1) Preparing a tablet core:
(1.1) mixing paliperidone with polyoxyethylene, hypromellose, and acidity regulator, and sieving to obtain a mixture;
(1.2) adding the mixture obtained in the step (1.1), butyl hydroxy anisole and anhydrous lactose into a mixer, and uniformly mixing to obtain a premixed material;
(1.3) adding magnesium stearate into the pre-mixed material obtained in the step (1.2), uniformly mixing, and tabletting to obtain tablet cores;
the slow release coating was prepared as in example 1.
The effect of different types of acidity regulators on related substances was tested, and the test results are shown in table 3 below.
TABLE 3 Table 3
As can be seen from the test results in Table 3, the stability of the addition of organic acid, namely, eudragit, vitamin C, succinic acid and fumaric acid, respectively, in the recipe is not as high as that of the addition of inorganic acid, namely, potassium dihydrogen phosphate, and thus, the stability of the recipe of adding inorganic acid, namely, potassium dihydrogen phosphate, in the recipe is better.
Examples 7 to 9: paliperidone sustained release tablet
The prescription is as follows:
The preparation method comprises the following steps:
(1) Preparing a tablet core:
(1.1) mixing paliperidone with hypromellose, polyoxyethylene, and potassium dihydrogen phosphate, and sieving to obtain a mixture;
(1.2) adding the mixture obtained in the step (1.1), butyl hydroxy anisole and anhydrous lactose into a mixer, and uniformly mixing to obtain a premixed material;
(1.3) adding magnesium stearate into the pre-mixed material obtained in the step (1.2), uniformly mixing, and tabletting to obtain tablet cores;
the slow release coating was prepared as in example 1.
The solubility (20 ℃) of paliperidone extended release tablets in solvents of different pH was tested and is specified in table 4 below.
TABLE 4 Table 4
The formulations of examples 7-9 with the addition of monobasic potassium phosphate significantly improved the endpoint dissolution in pH6.8 medium as compared to example 1, indicating that the addition of monobasic potassium phosphate can improve the dissolution of the paliperidone extended release tablet.
The above examples are provided for illustrating the technical aspects of the present invention and are not limited thereto, and although the present invention has been described in detail with reference to the above examples, one skilled in the art may make modifications and equivalents to the specific embodiments of the present invention without departing from the spirit and scope of the present invention, any modifications and equivalents thereof are within the scope of the appended claims.
Claims (10)
1. A paliperidone extended release tablet, characterized in that: the tablet comprises the following components in percentage by weight:
Sheet core material: 1-9% of paliperidone, 15-35% of filler, 40-53% of tablet core slow release material, 9-20% of acidity regulator, 0.01-0.6% of antioxidant and 0.5-1% of lubricant;
coating material: 2-5% of coating slow-release material, 0.5-2% of plasticizer, 1-3% of pore-forming agent and 1-2% of anti-adhesion agent.
2. The paliperidone extended release tablet of claim 1, wherein: the filler is one or more of microcrystalline cellulose, anhydrous lactose, mannitol, starch and calcium hydrophosphate.
3. The paliperidone extended release tablet of claim 1, wherein: the tablet core slow release material is one or more of polyoxyethylene, polyethylene glycol, hydroxypropyl methylcellulose, hydroxypropyl cellulose, ethyl cellulose and sodium alginate.
4. The paliperidone extended release tablet of claim 3, wherein: the tablet core slow release material is a mixture of hypromellose and polyoxyethylene; the components account for 17-23% of hydroxypropyl methylcellulose and 20-30% of polyoxyethylene by weight percent of the tablet.
5. The paliperidone extended release tablet of claim 1, wherein: the acidity regulator is inorganic acid.
6. The paliperidone extended release tablet of claim 5, wherein: the inorganic acid is potassium dihydrogen phosphate and/or sodium dihydrogen phosphate.
7. The paliperidone extended release tablet of claim 1, wherein: the pore-forming agent is one or more of hydroxypropyl methylcellulose, hydroxypropyl cellulose, methyl cellulose, polyvinyl alcohol and polyoxyethylene alcohol.
8. The paliperidone extended release tablet of claim 1, wherein: the mass ratio of the tablet core slow release material to the acidity regulator is 0.9:1-6:1.
9. The paliperidone extended release tablet of claim 8, wherein: the mass ratio of the tablet core slow release material to the acidity regulator is 2:1-6:1.
10. A method for preparing paliperidone extended release tablet as defined in any one of claims 1-9, wherein: the method comprises the following steps:
(1) Preparing a tablet core:
(1.1) mixing the active ingredient with a tablet core slow release material and an acidity regulator, and sieving to obtain a mixture;
(1.2) adding the mixture obtained in the step (1.1) and an antioxidant and a filler into a mixer, and uniformly mixing to obtain a premixed material;
(1.3) adding a lubricant into the premixed material obtained in the step (1.2), uniformly mixing, and tabletting to obtain tablet cores;
(2) Preparing a slow-release coating film:
(2.1) preparation of coating liquid: adding the pore-forming agent into the solvent, stirring until the pore-forming agent is completely dissolved, and obtaining a dispersion liquid for standby; adding the plasticizer and the coating slow-release material into the dispersion liquid, and stirring until the mixture is uniform to obtain coating liquid;
(2.2) coating: coating the tablet core obtained in the step (1.3) by using the coating liquid prepared in the step (2.1), and carrying out aging and drying treatment after reaching the target weight gain to obtain the paliperidone sustained release tablet;
the solid content of the coating liquid in the step (2.1) is 10%; the target weight gain in step (2.2) is a coating weight gain of 6.5-7.5%; the aging and drying operation in the step (2.2) is as follows: and (3) drying the coated tablet core for 3 hours at the temperature of 55 ℃ of a tablet bed.
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120301547A1 (en) * | 2009-11-26 | 2012-11-29 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Paliperidone double-layered osmotic pump controlled release tablet and preparation method thereof |
| WO2016050160A1 (en) * | 2014-10-01 | 2016-04-07 | 浙江华海药业股份有限公司 | Paliperidone oral controlled-release tablet and preparation method thereof |
| CN115350160A (en) * | 2022-10-20 | 2022-11-18 | 华润双鹤利民药业（济南）有限公司 | Paliperidone sustained-release preparation and preparation method thereof |
| CN115531339A (en) * | 2022-11-24 | 2022-12-30 | 山东则正医药技术有限公司 | Paliperidone sustained-release tablet and preparation method thereof |
| CN116983274A (en) * | 2023-07-28 | 2023-11-03 | 山东则正医药技术有限公司 | Single-layer coated paliperidone sustained release tablet and preparation method thereof |
-
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- 2024-05-06 CN CN202410546113.5A patent/CN118121557B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120301547A1 (en) * | 2009-11-26 | 2012-11-29 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Paliperidone double-layered osmotic pump controlled release tablet and preparation method thereof |
| WO2016050160A1 (en) * | 2014-10-01 | 2016-04-07 | 浙江华海药业股份有限公司 | Paliperidone oral controlled-release tablet and preparation method thereof |
| CN115350160A (en) * | 2022-10-20 | 2022-11-18 | 华润双鹤利民药业（济南）有限公司 | Paliperidone sustained-release preparation and preparation method thereof |
| CN115531339A (en) * | 2022-11-24 | 2022-12-30 | 山东则正医药技术有限公司 | Paliperidone sustained-release tablet and preparation method thereof |
| CN116983274A (en) * | 2023-07-28 | 2023-11-03 | 山东则正医药技术有限公司 | Single-layer coated paliperidone sustained release tablet and preparation method thereof |
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