CN111759820A - Oxcarbazepine tablet and preparation method thereof - Google Patents
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Abstract
The invention provides an oxcarbazepine tablet and a preparation method thereof, relating to the field of pharmaceutical preparations, wherein the oxcarbazepine tablet comprises a film coating premix and an oxcarbazepine tablet core; the oxcarbazepine tablet core comprises the following raw materials in percentage by weight: 60 to 80 percent of oxcarbazepine, 13 to 22 percent of microcrystalline cellulose, 3 to 5 percent of hydroxypropyl methylcellulose, 2 to 8 percent of croscarmellose sodium, 0.5 to 1 percent of colloidal silicon dioxide, 1 to 3 percent of sodium dodecyl sulfate and 0.5 to 1 percent of magnesium stearate. The oxcarbazepine tablet prepared by optimizing the components, the proportion and the preparation method can be produced commercially, is environment-friendly and economical, has better dissolution rate in a short time and is easy to be absorbed by human bodies.
Description
Technical Field
The invention relates to the field of pharmaceutical preparations, in particular to oxcarbazepine tablets and a preparation method thereof.
Background
Oxcarbazepine is the second generation antiepileptic drug, and is a derivative of the first generation antiepileptic drug carbamazepine. The drug acts primarily through its pharmacologically active metabolite (10-monohydroxy derivative, MHD). The quality of the oxcarbazepine tablets sold in China is uneven, whether the oxcarbazepine tablets are clinically equivalent to the original product is not clear, and the quality of the oxcarbazepine tablets needs to be improved through consistency evaluation. However, the preparation technology adopted by the existing oxcarbazepine tablet invention has various defects, such as:
the method disclosed in the chinese patent (oxcarbazepine pharmaceutical preparation and the preparation method thereof, application No. 2007800023534.8) requires the use of a broad and multimodal particle size distribution of the bulk drug oxcarbazepine, which is practically only available in laboratories and by technicians trained in good expertise, and is cumbersome and costly in procedures and cannot be used for the commercial production of oxcarbazepine tablet preparations.
The method disclosed in the chinese patent (an oxcarbazepine sustained release tablet and a method for preparing the same, application No. 201510823709.6) requires the use of KG-802 compound, and the bulk drug is pulverized several times during the pulverization process. The yield of micronized raw material medicines is very low easily due to multiple times of crushing, and the raw material medicines after multiple times of crushing are likely to have two-pole differentiation (double peaks) of particle sizes, so that the target particle size range and uniform distribution of the raw material medicines are difficult to control, and the in-vivo absorption is difficult. The possibility of practical application of this scheme to commercial production is 0. The purpose of the patent is to prepare the oxcarbazepine sustained release tablet, which is different from the oxcarbazepine quick release tablet prepared by the invention.
Oxcarbazepine is a BCS4 compound, has poor solubility and permeability, and is added with a proper amount of surfactant to improve the dissolution speed of oxcarbazepine in gastrointestinal tract, promote absorption in vivo and improve bioavailability. Sodium dodecyl sulfate is a surfactant which can be added into oral tablets, and an FDA (food and drug administration) adjuvant toxicity database shows that the maximum dosage of the sodium dodecyl sulfate for the oral tablets is single dose (tablet) 51.69mg, but no method for improving release and bioavailability of oxcarbazepine by using the sodium dodecyl sulfate is searched in Chinese patent on oxcarbazepine preparations.
Aiming at the problems of the difficult-to-dissolve and hypotonic biopharmaceutics characteristics of oxcarbazepine and the difficulty in converting most preparation methods in the prior art into a prescription process for practical production, the development of an environment-friendly and economical oxcarbazepine tablet production prescription process which can be commercially produced and is beneficial to in vivo absorption is needed.
Disclosure of Invention
The invention provides an oxcarbazepine tablet and a preparation method thereof, aiming at the problems in the prior art. The preparation method can be used for commercial production, is environment-friendly and economical, and the prepared oxcarbazepine tablet has excellent dissolution rate in a short time and is easy to be absorbed by human bodies.
In order to achieve the purpose, the technical scheme adopted by the invention is as follows:
the invention provides an oxcarbazepine tablet, which comprises a film coating premix and an oxcarbazepine tablet core; the oxcarbazepine tablet core comprises the following raw materials: oxcarbazepine, microcrystalline cellulose, hypromellose, croscarmellose sodium, colloidal silicon dioxide, sodium lauryl sulfate, and magnesium stearate.
Further, the oxcarbazepine tablet core comprises the following raw materials in percentage by weight:
preferably, the oxcarbazepine tablet core comprises the following raw materials in percentage by weight:
oxcarbazepine 72%
Microcrystalline cellulose 15.85%
4 percent of hydroxypropyl methylcellulose
Croscarmellose sodium 5%
0.65 percent of colloidal silicon dioxide
Sodium dodecyl sulfate 1.85%
0.65 percent of magnesium stearate.
Further, the weight of the film coating premix accounts for 2-4% of the total weight of the oxcarbazepine core.
Further, the weight ratio of the colloidal silicon dioxide to the sodium dodecyl sulfate is 0.5-1: 1-3. Preferably 0.65: 1.85.
Further, the oxcarbazepine tablet further comprises soy isoflavones.
Further, the content of the soybean isoflavone accounts for 2-5% of the total weight of the oxcarbazepine tablet core.
In some specific embodiments, the oxcarbazepine core comprises the following raw materials in weight percent:
preferably, the oxcarbazepine tablet core comprises the following raw materials in percentage by weight:
oxcarbazepine 70%
Microcrystalline cellulose 15.55%
Hydroxypropyl methylcellulose 3.8%
4.6 percent of croscarmellose sodium
0.7 percent of colloidal silicon dioxide
Sodium dodecyl sulfate 1.65%
Magnesium stearate 0.7%
3 percent of soybean isoflavone.
The invention also provides a preparation method of the oxcarbazepine tablet, which comprises the following steps:
(1) premixing: uniformly mixing oxcarbazepine, sodium dodecyl sulfate and colloidal silicon dioxide;
(2) micronization: performing jet milling on the premixed mixed material, and controlling the particle size distribution after milling;
(3) and (3) granulating: stirring and shearing the micronized mixed material, microcrystalline cellulose and hydroxypropyl methylcellulose, mixing uniformly, and adding pure water for granulation;
(4) drying;
(5) finishing the grains;
(6) totally mixing;
(7) tabletting: tabletting to obtain an oxcarbazepine core;
(8) coating: mixing the film coating premix and pure water, stirring until the film coating premix and the pure water are completely dissolved, filtering to obtain a coating solution, and coating the oxcarbazepine tablet core by using the coating solution.
Further, when the soybean isoflavone is added, the step (1) mixes the soybean isoflavone with oxcarbazepine, sodium dodecyl sulfate, and colloidal silicon dioxide.
Further, the adding amount of the pure water in the step (3) is 15-25% of the weight of the granulated dry powder feeding material.
Further, the solid content of the coating liquid in the step (8) is 10-15%.
Further, in some specific embodiments, the oxcarbazepine tablet is prepared by a process comprising the steps of:
(1) premixing: the oxcarbazepine raw material medicine, sodium dodecyl sulfate and colloidal silicon dioxide in the prescription amount are put into a mixer and mixed evenly.
(2) Micronization: and (3) carrying out air flow crushing on the premixed mixed material, and controlling the particle size distribution after crushing.
(3) And (3) granulating: and sequentially adding the micronized mixture, microcrystalline cellulose and hydroxypropyl methylcellulose into a high-shear wet granulator. Stirring and shearing are started, mixing is carried out until the mixture is uniform, and sampling is carried out to detect the content uniformity. Stirring and shearing are started, and a proper amount of purified water is added into the granulator for granulation.
(4) And (3) drying: drying with a fluidized bed dryer, starting steam to enter a system, lifting the hopper after the hopper is positioned, and pumping the prepared wet particles into a fluidized bed dryer bin to start drying. When the moisture of the particles reaches the control range, the heating is stopped. And (4) connecting the dry granules to a conveying hose of the bin granulator, and pumping the dry granules to the bin granulator for granulation through the conveying hose.
(5) Straightening: and (3) granulating the dry particles by using a bin granulator, starting a vacuum feeder of the bin granulator, setting granulation frequency, hermetically conveying the dry particles in the bin of the fluidized dryer into the bin of the bin granulator, and finally starting a motor of the bin granulator to start granulation. The appearance granularity of the checking particles is uniform and has no foreign matters. The particles are loaded in a lifting and feeding special barrel and are transported to a total mixing chamber.
(6) Total mixing: lifting the whole granules by a hydraulic lifter, aligning the whole granules with a feed inlet of a total mixing tank of a high-efficiency three-dimensional motion mixer, connecting and fastening a flexible connection, opening a valve, and enabling the whole granules to enter the total mixing tank in a free-falling mode. And after all the whole granules are added, closing the opening of the tank and starting the machine. The granules were checked for their behavior after the total mixing and were visually checked for light yellow granules and powder.
(7) Tabletting: and calculating the theoretical tablet weight according to the content of the prepared particles, and adding a lifting and feeding special barrel filled with the prepared particles into a blanking bin of the tablet press in a lifting and feeding mode. Normal compression was started to give tablet cores.
(8) Coating: taking the tablet core, weighing the film coating premix by using an electronic counting scale, and filling into a clean medicinal plastic bag. According to the proportion of the solid content of the coating liquid being 10 percent, the purified water quantity required to be added in each part is obtained, weighed by an electronic scale and poured into a premixing stirring tank. And adding the weighed film coating premix into weighed purified water, stirring until the film coating premix is completely dissolved, and filtering by using a 100-target standard sample sieve for later use. When in use, the filtrate is poured into a stirring tank of a coating machine, and the stirring paddle is started to stir slowly. The received plain tablets are coated in a coating operation room by a high-efficiency coating machine, and coating is started.
The technical effects obtained by the invention are as follows:
1. the invention combines the surface activity of the sodium dodecyl sulfate and the huge specific surface area of the silicon dioxide with the mixed micro powder of the bulk drug, the sodium dodecyl sulfate and the colloidal silicon dioxide, thereby reducing the material flow difficulty and the electrostatic aggregation when the oxcarbazepine is micronized at one stroke, and leading the oxcarbazepine micronization to be efficient and economic. The oxcarbazepine tablet has the oxcarbazepine content of 60-80% and poor flowability, so that micronization is difficult to feed and long in micronization time, and the oxcarbazepine tablet is easy to aggregate after micronization. The colloidal silicon dioxide has extremely large specific surface area and is commonly used as a glidant, so that the micronization feeding and crushing process can be accelerated when the colloidal silicon dioxide is mixed into the oxcarbazepine bulk drug. Meanwhile, the sodium dodecyl sulfate has better hydrophilicity and surface activity, is beneficial to eliminating static electricity and improving the state of the micronized raw material medicine. In addition, in the research, a small amount of soybean isoflavone is additionally added into the raw materials, so that the accelerated dissolution of the oxcarbazepine tablets can be promoted.
2. Oxcarbazepine is a BCS4 compound, has poor solubility and permeability, and is added with a proper amount of surfactant to improve the dissolution speed of oxcarbazepine in gastrointestinal tract, promote absorption in vivo and improve bioavailability. Sodium dodecyl sulfate is a surfactant which can be added into oral tablets, and an FDA (food and drug administration) adjuvant toxicity database shows that the maximum dosage of the sodium dodecyl sulfate for the oral tablets is single dose (tablet) 51.69mg, but no method for improving release and bioavailability of oxcarbazepine by using the sodium dodecyl sulfate is searched in Chinese patent on oxcarbazepine preparations. The invention adopts sodium dodecyl sulfate as one of the tablet core auxiliary materials, the dosage of the sodium dodecyl sulfate does not exceed the specification of an FDA (food and drug administration) auxiliary material maximum dosage database (IIG), the potential toxicity hazard is avoided, the dissolution speed of the oxcarbazepine in gastrointestinal tracts is improved, the in-vivo absorption is promoted, and the bioavailability is improved.
Detailed Description
It should be noted that the film coating premix used in the present invention is opadry produced by kallikrein, and the other raw materials are all common commercial products, so the source thereof is not particularly limited.
The oxcarbazepine core materials and the corresponding amounts added in examples 1-6 are shown in table 1:
TABLE 1
Example 1
A process for the preparation of oxcarbazepine tablets comprising the steps of:
(1) premixing: the oxcarbazepine raw material medicine, sodium dodecyl sulfate and colloidal silicon dioxide in the prescription amount are put into a mixer and mixed evenly.
(2) Micronization: and (3) carrying out air flow crushing on the premixed mixed material, and controlling the particle size distribution after crushing.
(3) And (3) granulating: and sequentially adding the micronized mixture, microcrystalline cellulose and hydroxypropyl methylcellulose into a high-shear wet granulator. Stirring and shearing are started, mixing is carried out until the mixture is uniform, and sampling is carried out to detect the content uniformity. Stirring and shearing are started, and a proper amount of purified water is added into the granulator to granulate, wherein the adding amount of the purified water is 25 percent of the weight of the granulated dry powder.
(4) And (3) drying: drying with a fluidized bed dryer, starting steam to enter a system, lifting the hopper after the hopper is positioned, and pumping the prepared wet particles into a fluidized bed dryer bin to start drying. When the moisture of the particles reaches the control range, the heating is stopped. And (4) connecting the dry granules to a conveying hose of the bin granulator, and pumping the dry granules to the bin granulator for granulation through the conveying hose.
(5) Straightening: and (3) granulating the dry particles by using a bin granulator, starting a vacuum feeder of the bin granulator, setting granulation frequency, hermetically conveying the dry particles in the bin of the fluidized dryer into the bin of the bin granulator, and finally starting a motor of the bin granulator to start granulation. The appearance granularity of the checking particles is uniform and has no foreign matters. The particles are loaded in a lifting and feeding special barrel and are transported to a total mixing chamber.
(6) Total mixing: lifting the whole granules by a hydraulic lifter, aligning the whole granules with a feed inlet of a total mixing tank of a high-efficiency three-dimensional motion mixer, connecting and fastening a flexible connection, opening a valve, and enabling the whole granules to enter the total mixing tank in a free-falling mode. And after all the whole granules are added, closing the opening of the tank and starting the machine. The granules were checked for their behavior after the total mixing and were visually checked for light yellow granules and powder.
(7) Tabletting: and calculating the theoretical tablet weight according to the content of the prepared particles, and adding a lifting and feeding special barrel filled with the prepared particles into a blanking bin of the tablet press in a lifting and feeding mode. Normal compression was started to give tablet cores.
(8) Coating: taking the tablet core, weighing the film coating premix by using an electronic counting scale, and filling into a clean medicinal plastic bag. According to the proportion of the solid content of the coating liquid being 10 percent, the purified water quantity required to be added in each part is obtained, weighed by an electronic scale and poured into a premixing stirring tank. And adding the weighed film coating premix into weighed purified water, stirring until the film coating premix is completely dissolved, and filtering by using a 100-target standard sample sieve for later use. When in use, the filtrate is poured into a stirring tank of a coating machine, and the stirring paddle is started to stir slowly. The received plain tablets are coated in a coating operation room by a high-efficiency coating machine, and coating is started.
Example 2
The preparation method is different from the example 1 only in that the adding amount of the pure water in the step (3) is 25 percent of the weight of the fed granulating dry powder, and the solid content of the coating liquid in the step (8) is 15 percent.
Example 3
The preparation method is different from the example 1 only in that the adding amount of the pure water in the step (3) is 20 percent of the weight of the fed granulating dry powder, and the solid content of the coating liquid in the step (8) is 12 percent.
Example 4
In the step (1), soybean isoflavone, oxcarbazepine, sodium dodecyl sulfate and colloidal silicon dioxide are mixed together, and the other preparation methods are the same as those in example 1.
Example 5
The preparation method is different from the example 4 only in that the adding amount of the pure water in the step (3) is 25 percent of the weight of the fed granulating dry powder, and the solid content of the coating liquid in the step (8) is 15 percent.
Example 6
The preparation method is different from the example 4 only in that the adding amount of the pure water in the step (3) is 20 percent of the weight of the fed granulating dry powder, and the solid content of the coating liquid in the step (8) is 12 percent.
Example 7
The only difference from example 6 is that no soy isoflavones were present (no soy isoflavones were added in step (1) of the preparation process) and the amounts of the remaining raw materials (parts by weight rather than percentages) were identical to example 6.
Comparative example 1
The difference from example 3 is only that the oxcarbazepine core comprises the following raw materials in weight percent:
comparative example 2
The difference from example 6 is only that the oxcarbazepine core comprises the following raw materials in weight percent:
comparative example 3
The only difference from example 3 is that the weight ratio of colloidal silica to sodium dodecylsulfate is 1.2:0.8 (the total weight of both is in accordance with example 3).
Comparative example 4
The only difference from example 6 is that the weight ratio of colloidal silica to sodium dodecylsulfate is 1.2:0.8 (the total weight of both is in accordance with example 6).
Oxcarbazepine tablet dissolution test of the present invention
Test subjects: oxcarbazepine tablets prepared in examples 1 to 7 and comparative examples 1 to 4, reference formulation (600 mg of nordstrand).
The test method comprises the following steps: the dissolution of oxcarbazepine tablets and reference tablets in different examples at different times was examined (the measurement method refers to the second method of 0931 in the appendix of the fourth part of the 'Chinese pharmacopoeia 2020 edition', and the measurement conditions refer to the dissolution curve determination conditions of oxcarbazepine tablets recommended by the US FDA, namely aqueous medium, 1% SDS, 60rpm, and slurry method), and the test results were counted in Table 1 and a dissolution similarity factor was calculated (f 2).
TABLE 1
As can be seen from table 1, the dissolution conditions of the oxcarbazepine tablets in the examples of the present invention reach more than 60 f2 compared with the reference preparation, which indicates that the oxcarbazepine tablets of the present invention have bioavailability consistent with the original imported product, and the oxcarbazepine tablets in the examples of the present invention can reach better dissolution rate in a shorter time. The dissolution conditions of comparative example 1 and comparative example 3 are inferior to those of example 3, and the dissolution conditions of comparative example 2, comparative example 4 and example 7 are inferior to those of example 6, so that the components and contents of the oxcarbazepine tablet greatly influence the dissolution conditions of the oxcarbazepine tablet, and the dissolution conditions are better within the protection range of the present invention.
Finally, it should be noted that the above-mentioned contents are only used for illustrating the technical solutions of the present invention, and not for limiting the protection scope of the present invention, and that the simple modifications or equivalent substitutions of the technical solutions of the present invention by those of ordinary skill in the art can be made without departing from the spirit and scope of the technical solutions of the present invention.
Claims (10)
1. Oxcarbazepine tablet formulation characterized by: comprises a film coating premix and an oxcarbazepine core; the oxcarbazepine tablet core comprises the following raw materials: oxcarbazepine, microcrystalline cellulose, hypromellose, croscarmellose sodium, colloidal silicon dioxide, sodium lauryl sulfate, and magnesium stearate.
2. Oxcarbazepine tablet according to claim 1, wherein: the oxcarbazepine tablet core comprises the following raw materials in percentage by weight:
3. oxcarbazepine tablet according to claim 1, wherein: the weight of the film coating premix accounts for 2-4% of the total weight of the oxcarbazepine tablet core.
4. Oxcarbazepine tablet according to claim 1, wherein: the weight ratio of the colloidal silicon dioxide to the sodium dodecyl sulfate is 0.5-1: 1-3.
5. Oxcarbazepine tablet according to claim 1, wherein: the oxcarbazepine tablets further comprise soy isoflavones.
6. Oxcarbazepine tablet according to claim 5, wherein: the content of the soybean isoflavone accounts for 2-5% of the total weight of the oxcarbazepine tablet core.
7. Oxcarbazepine tablet according to claim 6, wherein: the oxcarbazepine tablet core comprises the following raw materials in percentage by weight:
8. the process for the preparation of oxcarbazepine tablets according to any of claims 1 to 4, wherein: the method comprises the following steps:
(1) premixing: uniformly mixing oxcarbazepine, sodium dodecyl sulfate and colloidal silicon dioxide;
(2) micronization: performing jet milling on the premixed mixed material, and controlling the particle size distribution of the milled mixed material to be D90 which is less than or equal to 15 mu m;
(3) and (3) granulating: stirring and shearing the micronized mixed material, microcrystalline cellulose and hydroxypropyl methylcellulose, mixing uniformly, adding purified water, starting stirring and shearing for granulating;
(4) drying;
(5) finishing the grains;
(6) totally mixing;
(7) tabletting: tabletting to obtain an oxcarbazepine core;
(8) coating: mixing the film coating premix and pure water, stirring until the film coating premix and the pure water are completely dissolved, filtering to obtain a coating solution, and coating the oxcarbazepine tablet core by using the coating solution.
9. The method of claim 8, wherein: and (3) adding the pure water in an amount which is 15-25% of the weight of the granulated dry powder.
10. The method of claim 8, wherein: the solid content of the coating liquid in the step (8) is 10-15%.
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| CN1522140A (en) * | 2001-05-18 | 2004-08-18 | 兰贝克赛实验室有限公司 | Oxcarbazepine dosage forms |
| US20060057203A1 (en) * | 2002-09-20 | 2006-03-16 | Marie-Christine Wolf | Modified release formulations of oxcarbazepine and derivatives thereof |
| US20090196919A1 (en) * | 2004-10-25 | 2009-08-06 | Ajay Singla | Oxcarbazepine dosage forms |
| US20060264497A1 (en) * | 2005-03-28 | 2006-11-23 | Zeligs Michael A | Diindolylmethane-based compositions and methods of use thereof for promoting oral mucosal and bone health |
| WO2007011349A1 (en) * | 2005-07-15 | 2007-01-25 | Teva Pharmaceutical Industries Ltd. | Novel granulation process and granulate produced therefrom |
| WO2007133476A2 (en) * | 2006-05-08 | 2007-11-22 | Scolr Pharma, Inc. | Competitive substrate inhibition to increase drug bioavailability |
| WO2008037044A1 (en) * | 2006-09-27 | 2008-04-03 | Medley S.A. Indústria Farmacêutica | Oxcarbazepine-containing oral formulation and a process to obtain the same |
| CN106794986A (en) * | 2014-09-02 | 2017-05-31 | 布平德尔·辛格 | Deuterate or non-deuterate molecule and pharmaceutical preparation |
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