KR20200077712A - Moxifloxacin solid preparation and method for preparing the same - Google Patents

Abstract

The present invention relates to a solid preparation, including a moxifloxacin-containing core; and a releasable coating, wherein each of the core and the releasable coating includes a cellulose ether having an average hydroxypropyl group content of 5-16 wt%, and the total content of the cellulose ether is 5-25 wt% based on the total weight of the ingredients forming the solid preparation. According to the present invention, the solid preparation shows a high initial dissolution rate of moxifloxacin to realize expression of a rapid pharmacological action, retains a high level of final dissolution rate, and is effectively prevented from being damaged by moisture. The present invention also relates to a method for preparing the moxifloxacin solid preparation.

Description

Moxifloxacin solid preparation and preparation method thereof {Moxifloxacin solid preparation and method for preparing the same}

The present invention relates to a moxifloxacin solid preparation and a method for manufacturing the same, and more specifically, the initial dissolution rate of moxifloxacin is high, thereby realizing rapid pharmacological action and maintaining the final dissolution rate of the solid preparation at a high level. Moxifloxacin solid formulation that can effectively prevent the damage by and relates to a method for manufacturing the same.

Moxifloxacin (Moxifloxacin) is a fourth-generation synthetic fluoroquinolone antibiotic developed by Bayer AG (Germany), and is known to be effective against both Gram-positive and Gram-negative bacteria and inhibit cell replication. Moxifloxacin includes moxifloxacin or a salt and/or hydrate thereof, and the hydrochloride salt of moxifloxacin represented by the following formula (1) is also referred to as Moroxacin.

When oral administration of moxifloxacin, bioavailability is relatively high, about 90%, and T _max (time to reach the highest blood concentration) is about 2 hours, so absorption can be said to be a drug suitable for oral administration. Accordingly, they are sold under the trade names such as Avelox, Avalox, or Avelon, respectively, in the form of oral tablets.

However, a product containing moxifloxacin, for example, a tablet formulation is a formulation in which dissolution patterns and dissolution rate deviations, which play an important role in the absorption and use of drugs, differ greatly depending on the additives included. For example, when granules are prepared by using dibasic calcium phosphate (DCP) as a filler, the final dissolution rate of moxifloxacin is about 85%, which is a significantly lower value than the final dissolution rate of the control drug about 97%. It was only a degree. In addition, it is an important agent for moisture management because it shows a decrease in stability in the state of moisture exposure.

Related technologies have been disclosed in the prior patent documents 1 to 3, etc., but there is still a need for technology development to overcome this.

Patent Document 1: Korean Patent Publication No. 10-2013-0141391 (published on December 26, 2013) Patent Document 2: Korean Registered Patent No. 10-0531065 (Registered on November 18, 2005) Patent Literature 3: Korean Registered Patent 10-1093781 (registered on Dec. 7, 2011)

In order to solve the above problems, the present inventors intensively researched a method for increasing the initial dissolution rate of moxifloxacin and maintaining the final dissolution rate at a high level while preventing damage caused by moisture, as shown in FIG. 2. By effectively controlling the dissolution rate of moxifloxacin, it was confirmed that the composition maintains a final dissolution rate of tablets of about 95% or more, and the present invention has been completed.

That is, the object of the present invention is to increase the initial dissolution rate of moxifloxacin and maintain the final dissolution rate, thereby maintaining clinical effectiveness, and to provide a moxifloxacin solid preparation capable of exhibiting an effect of preventing damage from moisture and a method for manufacturing the same have.

In one aspect of the present invention, in a solid preparation comprising a moxifloxacin-containing core and an emissive coating, the core and the emissive coating each contain cellulose ethers having an average hydroxypropyl group content of 5 to 16 wt% And, the total amount of the cellulose ether is used to provide a moxifloxacin solid preparation in the range of 5 to 25% by weight relative to the total weight of all components constituting the solid preparation.

Another aspect of the invention,

(i) mixing one or more pharmaceutically acceptable additives including moxifloxacin, (ii) cellulose ether, (i) insoluble excipients and binders in an appropriate proportion to prepare a mixture;

Wet granulating the mixture in a polar solvent;

Preparing a core by mixing a binder with the wet granulation treatment and then mixing a lubricant;

Preparing the core as a solid preparation using a tableting machine; And

Forming a release coating on the tableted solid preparation,

The core and the emissive coating each contain cellulose ethers having an average hydroxypropyl group content of 5 to 16% by weight, and the total amount of the cellulose ether used is 5 to 25 based on the total weight of all components constituting the solid preparation. It provides a method for preparing a moxifloxacin solid preparation in a weight percent range.

According to the present invention, the initial dissolution rate of moxifloxacin is high, thereby realizing rapid pharmacological action, and the final dissolution rate of the solid preparation is maintained at a high level, and damage due to moisture can be effectively prevented.

1 is a process schematic for the preparation of a moxifloxacin solid formulation.
Figure 2 is a graph showing the dissolution rate of the moxifloxacin solid preparation prepared according to Examples and Comparative Examples.

One embodiment of the present invention relates to a solid preparation comprising a moxifloxacin-containing core and a release coating. In one embodiment, the initial dissolution rate of moxifloxacin is higher than that of Avelox (Avelox ^tab® , Bayer ) to realize rapid pharmacological action, and the final dissolution rate of the solid preparation is maintained at a high level, and damage caused by moisture is prevented. A solid preparation that can be effectively prevented is provided.

The moxifloxacin solid preparation contains cellulose ethers having an average hydroxypropyl group content of 5 to 16% by weight in the core and the emissive coating, respectively. In addition, the release coating further contains a cellulose ether having an average hydroxypropyl group content of 53.4 to 77.5 wt%.

The cellulose ether having the average content of the hydroxypropyl group prevents crystal growth of the drug during the preparation of the solid preparation, thereby improving the stability of the pharmaceutical formulation, increasing the initial dissolution rate, and maintaining the final dissolution rate, and has the ability to absorb moisture by itself. It also has the effect of preventing damage from moisture. Compared to the moxifloxacin composition that does not contain cellulose ether, the cellulose ether is present in a concentration sufficient to significantly reduce the formation of crystals within the moxifloxacin composition.

The total amount of the cellulose ether is preferably 5 to 25% by weight, or 8 to 23% by weight based on the total weight of all the components constituting the solid preparation. At this time, if the amount of cellulose ether is used below the above range, the dissolution rate may be inferior, and if it is used beyond the above range, the tablet may be repelled by excessive absorption of moisture and may be damaged in the processing process. It is preferred.

The cellulose ether may be, for example, hydroxypropyl cellulose and hydroxypropyl methyl cellulose (hypomellose), or a combination thereof, and it is more preferable to use hydroxypropyl cellulose. Particularly, cellulose ethers having an average hydroxypropyl group content in the core of 5 to 16% by weight are hydroxypropyl ethers of cellulose obtained by etherifying a part of the hydroxy groups of the pyranose ring of cellulose with propylene oxide groups. , It corresponds to the content value when quantifying dry. Examples of the cellulose ether include L-HPC (LH-11, LH-20, LH-21, LH-22, LH-30, LH-31 or LH-32) manufactured by Shin-Etsu Chemical.

In addition, cellulose ethers having an average hydroxypropyl group content of 5 to 16% by weight contained in the emissive coating are hypromelloses, which correspond to the content when quantifying dryness. Furthermore, cellulose ethers having an average hydroxypropyl group content of 53.4 to 77.5 wt% further contained in the emissive coating are distinguished from cellulose ethers contained in the core, and correspond to content values when quantifying dryness. . Examples of such cellulose ethers can be obtained as Nippon Soda's HPC-L, L (fine powder) or the like.

If necessary, the core and/or emissive coating of the present invention may further include a cellulose ester such as cellulose acetate.

The core according to an embodiment of the present invention includes moxifloxacin and cellulose ether as main components. The ratio of cellulose ether to moxifloxacin is 3:97 (w/w) to 29:71 (w/w). The ratio of cellulose ether to moxifloxacin 3:97 (w/w) means that the weight of moxifloxacin is 97% of the total weight of moxifloxacin and cellulose ether.

The core may further include at least one additive selected from insoluble excipients and binders. The non-dissolvable excipient may use a material that has the ability to rapidly absorb water in a dispersion medium and has a wicking effect that produces improved dispersion/disintegration properties. Examples include microcrystalline cellulose, silicified microcrystalline cellulose, and the like.

The incorporation of these insoluble excipients into the core provides an advantageous dispersibility or disintegration action compared to other controls. For reference, the wicking action may result in faster dispersion and may be advantageous as it can bypass the solubilization process. The insoluble excipient may be present in the core or coated solid formulation in an amount of 1% to 20% by weight, or 5% to 10% by weight. The core may further include a binder and a lubricant. Although these additives may be added at the same time, it is more preferable that they are added sequentially. As an example of the sequential input, the binder may be first added to the core and then the lubricant may be added.

The present invention includes solid preparations with non-functional coatings. The non-functional coating may have an immediate release coating action as described above. The release coating may further include at least one additive selected from a lubricant, a cellulose ether having an average hydroxypropyl group content of 53.4 to 77.5 wt%, a binder, and a colorant. In one example, the emissive coating contains 50 to 80% by weight of hypromellose, and one or more additives selected from the lubricant, a cellulose ether having an average hydroxypropyl group content of 53.4 to 77.5% by weight, a binder, and a colorant. It may contain within 20 to 50 weight range.

Specific examples of pharmaceutical additives that can be used in the solid formulation are described in Handbook of Pharmaceutical Excipients (RC Rowe, et al., Handbook of Pharmaceutical Excipients, Pharmaceutical Press, Fifth Edition, 2006), for preparing solid formulations The technique is described in Remington: The Science and Practice of Pharmacy (DB Troy, Remington: The Science and Practice of Pharmacy, Lippincott Williams & Wilkins, Twenty-first Edition, 2005).

The amount of the at least one pharmaceutical additive selected from the binder, lubricant, or colorant included in the solid preparation of the present invention is, for example, 0.1 to 40% by weight of the binder relative to the total weight with respect to the total weight constituting the solid preparation, The colorant may be composed of 1 to 10% by weight, and the lubricant may be 0.1 to 10% by weight.

The moxifloxacin solid formulation of the present invention may include an amount of moxifloxacin of 300 mg to 500 mg. That is, in containing moxifloxacin, solid preparations containing 300 mg, 400 mg, 450 mg, and 500 mg of moxifloxacin can be exemplified. The moxifloxacin used in the present invention includes pharmaceutically acceptable salts including moxifloxacin hydrochloride. Among these, moxifloxacin hydrochloride called moroxacin can be preferably used.

The term “solid preparation” used in the present invention refers to tablets, powders, capsules or granules, unless stated otherwise.

The solid preparation of the present invention can be prepared by a general wet granulation method. That is, after sufficiently mixing the above components, granulated using water as a polar solvent that may contain a lower alcohol such as ethanol or isopropanol, dried and separated as needed, and then tableted by tableting with a tableting machine. . Further, the tablet may be coated.

As a specific example, the solid preparation of the present invention may be prepared by a method comprising the following steps: (i) moxifloxacin, (ii) cellulose ether, (i) at least one agent comprising a non-soluble excipient and a binder. Mixing a scientifically acceptable additive in an appropriate ratio to prepare a mixture; Wet granulating the mixture in a polar solvent; Preparing a core by mixing a binder with the wet granulation treatment and then mixing a lubricant; Preparing a solid preparation using a tableting machine for the core; And forming a release coating on the tableted solid preparation.

In one example, (ii) half of the cellulose ether is charged to a blender such as a V-blender or an empty blender, moxifloxacin is added, and the remaining half of (ii) cellulose ether is added, and (i) fine Materials such as crystalline cellulose and croscarmellose sodium are mixed.

Subsequently, wet granules are prepared by adding purified water as a binder using a high shear granulator or the like.

Magnesium stearate can be screened with a 20 mesh screen or the like to increase the bonding strength by adding an equivalent amount of croscarmellose sodium to the wet granules and then crushing any mass. The screened magnesium stearate is added to the wet granules containing the moxifloxacin/cellulose ether mixture and mixed for several minutes to form a core.

Tablets, granules and the like are prepared as solid preparations using the core tableting machine. The tableted solid preparation can then be coated in a coater. The coating may be carried out by coating a hypromellose, a lubricant, a cellulose ether having an average hydroxypropyl group content of 53.4 to 77.5 wt%, a binder, and a colorant.

The polar solvent is purified water as an example, the non-soluble excipient is microcrystalline cellulose as an example, the binder is sodium carboxymethyl cellulose as an example, and the lubricant is, for example, at least one selected from talc and magnesium stearate, and the colorant For example, it may be one or more selected from titanium dioxide and iron oxide red.

The moxifloxacin solid preparation of the present invention not only maintains the clinical effectiveness of moxifloxacin, has a high dissolution rate of moxifloxacin, is rapidly absorbed, and the prepared solid preparation exhibits a water protection effect.

The moxifloxacin solid preparation according to one embodiment of the present invention was tested at 37±0.5°C, water, and 50 rpm without dissolution aid according to the dissolution test method second method of the Korean Pharmacopoeia General Test Method, and 15 minutes elapse from the start of elution. The dissolution rate of the city is 91% or more. In addition, the moxifloxacin solid preparation has a dissolution rate of 95% or more 45 minutes after the start of dissolution under the same test.

Hereinafter, examples are provided to help understanding of the present invention. However, the following examples are only provided to more easily understand the present invention, and the contents of the present invention are not limited by the following examples.

[Example]

Examples 1 to 5. Moxifloxacin solid preparations

Each component shown in Table 1 was weighed, and each component except purified water was mixed with a stirring mixer for 10 minutes. Subsequently, purified water (refer to Table 1 content) to which granules having a particle diameter of 100 to 500 μm could be produced was added, and the resulting mixture was stirred for 10 minutes and granulated with a high shear granulator. The obtained granules were crushed and dried. Magnesium stearate was added to the obtained dried granules, mixed with a V-type mixer for 2 minutes and tableted to obtain tablets with a diameter of 7 mm, a thickness of 3 mm and a weight of 100 mg.

On the other hand, as a cellulose ether of a certain degree of substitution, L-HPC (LH-22) manufactured by Shin-Etsu Chemical (8% by weight of hydroxypropoxyl group and average particle diameter of 45 µm) was used. In the table below, MCC represents microcrystalline cellulose and CrosCMC Na represents croscarmellose sodium, respectively.

ingredient Example 1 Example 2 Example 3 Example 4 Example 5 mg/T Enteric coating Moroxacin 436.80 436.80 436.80 436.80 436.80 MCC 109.00 109.00 109.00 109.00 109.00 LH-22 14.00 41.00 82.00 164.00 192.00 CrosCMC Na 30.00 30.00 30.00 30.00 30.00 (D.W) (160.00) (160.00) (160.00) (160.00) (160.00) Sub Total 589.80 616.80 657.80 739.80 767.80 After mixing CrosCMC Na 40.00 40.00 40.00 40.00 40.00 St-Mg 18.00 18.00 18.00 18.00 18.00 Sub Total 647.80 674.80 715.80 797.80 825.80

Additional Examples 1 to 5. Film Coated Solid Formulations

The solid formulation cores of Table 1 can be film coated. Experimental examples of the coated solid formulations are described in Table 2 below.

On the other hand, as a cellulose ether of a specific degree of substitution, Nippon Soda Co., Ltd. HPC-L [hydroxypropyl group average content 53.4 wt% to 77.5 wt%] was used. In addition, in the following table, Hypromellose 2910 is a cellulose-based polymer, and the average content of methoxyl group is 28 to 30% by weight, and the average content of hydroxypropyl group is 7 to 12% by weight of hypomerose.

ingredient Additional Example 1 Additional Example 2 Additional Example 3 Additional Example 4 Additional Example 5 mg/T coating Hypromellose 2910 16.00 16.00 16.00 16.00 16.00 Talc 0.40 0.40 0.40 0.40 0.40 HPC-L 4.00 4.00 4.00 4.00 4.00 TiO ₂ 3.60 3.60 3.60 3.60 3.60 Iron oxide red 0.24 0.24 0.24 0.24 0.24 Total solid formulation 672.04 699.04 740.04 822.04 850.04

Comparative Example 1. Commercial formulation

A commercially available moxifloxacin tablet “Abelose” tablet (Bayer) was used.

Comparative Examples 2 to 5. Moxifloxacin solid preparation

The same process as in Example 1 was repeated except that the composition in Table 1 was replaced with the composition in Table 3 below.

ingredient Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 mg/T Enteric coating Moroxacin 436.80 436.80 436.80 436.80 MCC 109.00 109.00 109.00 150.00 LH-22 - 205.00 - - DCP - - 41.0 - CrosCMC Na 30.00 30.00 30.00 30.00 (D.W) (160.00) (160.00) (160.00) (160.00) Sub Total 575.80 780.80 616.80 616.80 After mixing CrosCMC Na 40.00 40.00 40.00 40.00 St-Mg 18.00 18.00 18.00 18.00 Sub Total 633.80 838.80 674.80 674.80

Additional Comparative Examples 2 to 5. Film-coated solid preparations

The solid formulation core of Table 3 can be film coated. Experimental examples of the coated solid formulations are described in Table 4 below.

ingredient Additional Comparative Example 2 Additional Comparative Example 3 Additional Comparative Example 4 Additional Comparative Example 5 mg/T coating Hypromellose 2910 16.00 16.00 16.00 16.00 Talc 0.40 0.40 0.40 0.40 HPC-L 4.00 4.00 4.00 4.00 TiO ₂ 3.60 3.60 3.60 3.60 Iron oxide red 0.24 0.24 0.24 0.24 Total 658.04 863.04 699.04 699.04

All of the above experimental examples include a 400 mg standard as moxifloxacin per tablet.

Test Example 1. Dissolution test of moxifloxacin solid preparation

Table 5 provides the dissolution profiles of various moxifloxacin dosage forms. The dissolution test was carried out according to the dissolution test method 2 of the general pharmacopoeia general test method for the solid preparations of further comparative examples 1 to 5 and further examples 1 to 5, and the conditions are as follows. The elution of moxifloxacin is given in% weight. The obtained results are shown in Table 5 and FIG. 2, and for reference, Comparative Examples 2 to 5 and Examples 1 to 5 in the following tables indicate additional Comparative Examples 2 to 5 and Additional Examples 1 to 5, respectively.

<dissolution conditions>

Device: Dissolution test method 2nd method (paddle method)

Eluent: Water (D.W)

Capacity: 900mL

Number of revolutions: 50 rpm

Dissolution time: 30 minutes

Temperature: 37±0.5℃

<Liquid chromatography analysis method>

Column: 4.0 x 150mm, 5μm, Phenylsilyl silica column or similar column

Mobile phase: Methanol (MeOH): Buffer = 28:72

Buffer solution: 0.5 g of Tetrabutylammonium hydrogen sulfate, 1.0 g of potassium dihydrogen phosphate, and 3.4 g of phosphoric acid dissolved in 1000 mL of purified water

Column temperature: 45℃

Detector: Ultraviolet absorption photometer (wavelength 293mm)

Flow rate: 1.3 mL/min

Injection volume: 10 μL

Elution time (minute) 0 5 10 15 30 45 Comparative Example 1 Avg 0 85.71 91.44 94.71 96.85 97.03 SD 0 2.83 1.57 0.64 0.98 0.98 Comparative Example 2 Avg 0 72 80.73 82 84.63 85.73 SD 0 7.74 2.52 1.44 0.58 0.78 Comparative Example 3 Avg 0 85 89.16 95.2 96.78 98.76 SD 0 4.22 3.88 1.05 0.77 0.6 Comparative Example 4 Avg 0 70 79.45 83.45 85.79 86.12 SD 0 6.8 5.5 1.78 0.79 0.23 Comparative Example 5 Avg 0 76.45 79.44 81.48 85.62 86.66 SD 0 7.74 3.12 1.22 0.49 0.36 Example 1 Avg 0 80.98 89.01 91.85 93.48 95 SD 0 2.69 2.55 1.59 1.12 0.4 Example 2 Avg 0 81.41 89.19 92.91 94.49 95.11 SD 0 3.99 1.13 1.11 0.77 0.6 Example 3 Avg 0 83.61 92.77 94.57 95.8 98.22 SD 0 2.33 1.57 0.88 0.6 0.45 Example 4 Avg 0 86.83 92.37 94.99 97.11 96.68 SD 0 2 1.94 1.06 0.8 0.55 Example 5 Avg 0 86.99 93.48 95.61 95.84 97.55 SD 0 3.1 2.46 2.11 1.98 1.86

As shown in Table 5 and Figure 2, Comparative Examples 1 (commercially available products, Comparative drug Avelox tab) showed similar dissolution rates in Examples 1 to 5, and in the case of dissolution patterns, an excess of L-HPC was added. In Comparative Example 3, a relatively improved dissolution pattern was confirmed.

On the other hand, as a result of confirming Comparative Examples 2, 4 and 5, a relatively low dissolution pattern was confirmed when DCP or MCC excess was used except for L-HPC.

Test Example 2. Properties of moxifloxacin solid preparation

The evaluation of the properties in Table 6 below confirms the number of tablets that have been damaged, such as tablet breakage, capping, cracking, and wear, using a total of 100 tablets. For reference, Comparative Examples 2 to 5 and Examples 1 to 5 in the following table indicate additional Comparative Examples 2 to 5 and Additional Examples 1 to 5, respectively.

Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Example 1 Example 2 Example 3 Example 4 Example 5 Count 0 14 21 10 One One One 4 6 7 ratio 0% 14% 21% 10% One% One% One% 4% 6% 7%

As shown in Table 6, in the case of the prescription in which L-HPC was completely excluded, as in Comparative Example 2, it was confirmed that the tablets were relatively easy to cause problems due to poor binding strength. When the amount of MCC was added to replace it and put it as an excipient, it was confirmed that the properties of the tablets were relatively improved, but the properties of the tablets were poor compared to Examples 1 to 5.

As in the case of Comparative Example 3, when an excessive amount of L-HPC was added to a certain level, L-HPC with moisture affinity was tableted into tablets, and the tablets were easily absorbed to confirm the shape of the tablets. Through this, it was confirmed that the addition of L-HPC at an appropriate level was very important, and the range was limited to 5% or more and 25% or less.

Test Example 3. Tableting property of moxifloxacin solid preparation

The evaluation of the tableting properties of Table 7 is a result of confirming the tabletting properties of the corresponding conditions in the tableting process. For reference, Comparative Examples 2 to 5 and Examples 1 to 5 in the following table indicate additional Comparative Examples 2 to 5 and Additional Examples 1 to 5, respectively.

Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Example 1 Example 2 Example 3 Example 4 Example 5 standard ++: Very good +: Good-: Bad -: Very bad ratio ++ ­ - + + + + ++ + +

As shown in Table 7, in the case of Comparative 3, it was confirmed that the tableting property was deteriorated when L-HPC was added in excess, as in Test Example 2. Tablet properties evaluation. This confirmed that L-HPC adsorbed moisture to have excess moisture in the granules, which made tablets such as sticking worse during tableting.

However, as can be seen from Comparative Examples 2, 4 and 5 and Examples 1 to 5, it was confirmed that as a result of using an appropriate amount of L-HPC as an excipient, it had excellent tableting properties compared to the case of using other excipients as in Comparative Examples 4 and 5 Therefore, it was judged to be a pharmaceutical meaningful agent.

Claims (14)

In the solid preparation comprising a moxifloxacin-containing core and a release coating,
The core and the emissive coating each contain cellulose ethers having an average hydroxypropyl group content of 5 to 16% by weight,
The moxifloxacin solid preparation in which the total amount of the cellulose ether is in the range of 5 to 25% by weight relative to the total weight of all components constituting the solid preparation. The method according to claim 1,
The core comprises moxifloxacin and cellulose ether, and the ratio of cellulose ether to moxifloxacin is 3:97 (w/w) to 29:71 (w/w). The method according to claim 2,
The core comprises at least one additive selected from non-soluble excipients and binders, and the non-soluble excipient is at least one selected from microcrystalline cellulose and silicified microcrystalline cellulose. The method according to claim 3,
The core is moxifloxacin solid formulation further comprising a binder and a lubricant. The method according to claim 1,
The release coating is a moxifloxacin solid formulation further comprising a cellulose ether having an average hydroxypropyl group content of 53.4-77.5% by weight. The method according to claim 1,
The emissive coating contains 50 to 80% by weight of hypromellose, a lubricant, a cellulose ether having an average hydroxypropyl group content of 53.4 to 77.5% by weight, one or more additives selected from a binder and a colorant within a range of 20 to 50% by weight. A moxifloxacin solid preparation that contains. The method according to claim 1,
The cellulose ether is a moxifloxacin solid preparation of at least one selected from hydroxypropyl cellulose and hydroxypropylmethyl cellulose. The method according to claim 1,
The moxifloxacin is a moxioxacin solid preparation. The method according to claim 1,
The solid preparation comprises an amount of moxifloxacin from 300 mg to 500 mg; According to Method 2 of the Dissolution Test Method of the Korean General Pharmacopoeia General Test Method, the dissolution rate at the time of 15 minutes from the start of dissolution was 91% or more and the dissolution rate at 45 minutes without dissolution aid, at 37±0.5°C, water, and 50 rpm. A moxifloxacin solid preparation having more than 95%. The method according to claim 1,
The solid preparation is a moxifloxacin solid preparation, which is a tablet, powder, capsule or granule. (i) mixing one or more pharmaceutically acceptable additives including moxifloxacin, (ii) cellulose ether, (i) insoluble excipients and binders in an appropriate proportion to prepare a mixture;
Wet granulating the mixture in a polar solvent;
Preparing a core by mixing a binder with the wet granulation treatment and then mixing a lubricant;
Preparing the core as a solid preparation using a tableting machine; And
Forming a release coating on the tableted solid preparation,
The core and the emissive coating each contain cellulose ethers having an average hydroxypropyl group content of 5 to 16% by weight, and the total amount of the cellulose ether used is 5 to 25 based on the total weight of all components constituting the solid preparation. A method for preparing a moxifloxacin solid preparation in a weight percent range. The method according to claim 11,
The (i) moxifloxacin is moroxacin, and the ratio of (i) moxifloxacin and (ii) cellulose ether is 3:97 (w/w) to 29:71 (w) of the cellulose ether to moxifloxacin ratio. /w) A method for preparing a moxifloxacin solid preparation that is mixed to be within a range. The method according to claim 11,
The release coating is a method for preparing a moxifloxacin solid preparation, which is performed by coating a lubricant, a cellulose ether having an average hydroxypropyl group content of 53.4 to 77.5 wt%, a binder, and a colorant. The method according to claim 11 or 13,
The insoluble excipient is microcrystalline cellulose or silicified microcrystalline cellulose, the polar solvent is purified water, the binder is sodium carboxymethylcellulose, the lubricant is at least one selected from talc and magnesium stearate, and the colorant is dioxide Method for preparing a moxifloxacin solid preparation of at least one selected from titanium and iron oxide red.

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