Dapoxetine hydrochloride tablet and preparation method thereof

Abstract

The application discloses a dapoxetine hydrochloride tablet and a preparation method thereof. The dapoxetine hydrochloride tablet comprises the following components in percentage by mass: 15-45% of dapoxetine hydrochloride, 45-75% of a filling agent, 0.1-2% of a solubilizing agent, 2-10% of a disintegrating agent and 0.5-3% of a lubricant. The dapoxetine hydrochloride tablet is prepared by optimizing the types and proportions of the components, thereby effectively improving the stability and dissolution rate during accelerated storage and long-term storage, and reducing the impurity content. Specifically, the impurity contents during accelerated storage for 6 months and long-term storage for 36 months are lower than 0.06% and 0.05% respectively; the 15min dissolution rate during accelerated storage for 6 months is 99-100%; and the 15min dissolution rate during long-term storage for 36 months is 99.2-100.2%.

Description

Technical Field

[0001] This invention belongs to the pharmaceutical field, specifically relating to a dapoxetine hydrochloride tablet and its preparation method. Background Technology

[0002] Dapoxetine hydrochloride, chemically named (+)-(S)-N,N-dimethyl-(α)-[2-(1-naphthoxy)ethyl]benzylamine hydrochloride, has the following structural formula:

[0003]

[0004] Dapoxetine hydrochloride is a potent selective serotonin reuptake inhibitor (SSRI) that was launched in Europe in 2009 and was the first oral medication used to treat premature ejaculation (PE) in men. The drug is rapidly absorbed, reaching its maximum plasma concentration (C60) approximately 1-2 hours after oral administration. max The absolute bioavailability was 42% (range 15-76%). Following a single oral dose of 30 mg and 60 mg of dapoxetine in an empty stomach, peak plasma concentrations were reached at 1.01 and 1.27 hours, respectively (297 ng / mL and 498 ng / mL).

[0005] Dapoxetine hydrochloride belongs to the BCS3 class (high solubility-low permeability) drugs. According to the "Guidelines for Dissolution Technology of Common Oral Solid Dosage Forms," ​​for BCS3 (high solubility-low permeability) drug formulations, when the dissolution rate is greater than 85% in 0.1 mol / L HCl medium after 15 minutes, the bioavailability of the drug is not limited by dissolution behavior. Therefore, ensuring rapid dissolution of the drug in this medium is crucial to ensuring bioavailability. Experimental studies have found that the original formulation, Priligy... Samples of generic formulations that have recently been manufactured typically exhibit rapid dissolution in this medium (dissolution rate greater than 85% within 15 minutes). However, as storage time increases, the dissolution rate of the drug in this medium significantly decreases, failing to achieve rapid dissolution (i.e., dissolution rate less than 85% within 15 minutes), leading to reduced bioavailability and thus affecting clinical efficacy. Furthermore, with prolonged storage, related substances in dapoxetine hydrochloride tablets also increase significantly. Long-term use of dapoxetine hydrochloride formulations may lead to accumulation in the body, posing certain safety risks.

[0006] Currently, the preparation methods of dapoxetine hydrochloride tablets include: (1) dry granulation followed by tableting. This method has the following problems: since the raw material is granulated once, impurities are easy to grow during the dry pressing process, so the impurity level of the finished product is high; (2) first dissolve dapoxetine hydrochloride in an organic solvent (ethanol, acetic acid, ethyl acetate, acetone), then granulate and dry it with dextrin to form a solid dispersion granule, and finally mix it with excipients and compress it to obtain tablets. This method has the following problems: pure organic solvents are used in the process, which poses a series of safety production problems. It has extremely high requirements for equipment, factory and personnel management, and dextrin has a strong inclusion complex. The product is prone to solvent residue; on the other hand, the wet granulation process requires a wet heat process, which leads to an increase in related substances and poor stability; (3) Dapoxetine and filler are micronized together, and the particle size is controlled to be 0.5-20μm. The fine powder and some disintegrant are then used to make soft material with ethanol aqueous solution. After granulation and drying, it is mixed with disintegrant, flavoring agent and lubricant and tableted. This method has the following problems: the process uses micronization process, and the pulverization process will inevitably cause the growth of related substances; in addition, the preparation process involves wet granulation, and the product stability is poor; the preparation process is complicated and difficult to industrialize. The above methods for preparing dapoxetine hydrochloride tablets all have problems such as high impurity content and poor stability. Therefore, it is urgent to provide a dapoxetine hydrochloride tablet and its preparation method that can be rapidly dissolved, has high bioavailability, low content of related substances and good quality stability. Summary of the Invention

[0007] In order to overcome the problems existing in the prior art, one of the objectives of the present invention is to provide a dapoxetine hydrochloride tablet, which has the advantages of rapid dissolution, high bioavailability, low impurity content, and good quality stability.

[0008] The second objective of this invention is to provide a method for preparing dapoxetine hydrochloride tablets.

[0009] To achieve the above objectives, the technical solution adopted by the present invention is as follows:

[0010] The first aspect of the present invention is to provide a dapoxetine hydrochloride tablet comprising the following components in weight percentages: dapoxetine hydrochloride 15%–45%; filler 45%–75%; solubilizer 0.1%–2%; disintegrant 2%–10%; lubricant 0.5%–3%;

[0011] The solubilizer is selected from at least one of polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, poloxamer 188, and copovidone.

[0012] The solubilizers used in this invention are all nonionic surfactants, which have good solubilizing effect, can promote dissolution, and improve bioavailability. At the same time, the solubilizers used in this invention have good chemical stability and good adhesion. After being compressed into tablets, they are fully combined with dapoxetine hydrochloride, which effectively reduces the porosity of the tablet core, effectively isolates external oxygen, and improves the stability of dapoxetine hydrochloride tablets, so that dapoxetine hydrochloride tablets maintain extremely low impurity levels even after long-term storage.

[0013] Preferably, the mass percentage of the solubilizer is 0.5-1.5%; more preferably, the mass percentage of the solubilizer is 0.7-1.3%. The solubilizer in this invention acts as a solubilizer, binder, disintegrator, and stabilizer in addition to its solubilizing effect.

[0014] Preferably, the mass percentage of dapoxetine hydrochloride is 20-40%; more preferably, the mass percentage of dapoxetine hydrochloride is 25-35%.

[0015] Preferably, the particle size D90 value of the dapoxetine hydrochloride is 100-200 μm.

[0016] Preferably, the filler has a mass percentage of 50-70%; more preferably, the filler has a mass percentage of 55-65%.

[0017] Preferably, the filler is selected from at least one of microcrystalline cellulose, mannitol, lactose, cellulose-lactose, starch, pregelatinized starch, dicalcium phosphate, and silicified microcrystalline cellulose; more preferably, the filler is selected from at least one of microcrystalline cellulose, lactose, and cellulose-lactose.

[0018] Preferably, the disintegrant has a mass percentage of 2-8%; more preferably, the disintegrant has a mass percentage of 3-6%.

[0019] Preferably, the disintegrant is selected from at least one of crospovidone, crospovidone sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, sodium carboxymethyl starch, and low-substituted hydroxypropyl cellulose.

[0020] Preferably, the mass percentage of the lubricant is 0.5-2%; more preferably, the mass percentage of the lubricant is 0.5-1.5%.

[0021] Preferably, the lubricant is selected from at least one of silica, talc, magnesium stearate, and sodium stearate fumarate.

[0022] The second aspect of the present invention is to provide a method for preparing dapoxetine hydrochloride tablets as provided in the first aspect of the present invention, comprising the following steps:

[0023] S1: Granulate the solubilizer and filler in one step to obtain pharmaceutical excipient granules;

[0024] S2: The pharmaceutical adjuvant granules are mixed with dapoxetine hydrochloride, disintegrant and lubricant and then compressed into tablets to obtain the dapoxetine hydrochloride tablets.

[0025] Preferably, the particle size of the pharmaceutical adjuvant granules is 40-80 mesh.

[0026] Preferably, step S1 is: granulating the solubilizing alcohol solution and the filler in one step.

[0027] Preferably, the alcohol comprises ethanol or isopropanol; more preferably, the alcohol is ethanol; even more preferably, the alcohol is an ethanol solution with a volume fraction of 20-60%.

[0028] Preferably, in the granulation step, the inlet air temperature is 40–100°C; the fan frequency is 10–30 Hz; the spray pressure is 0.1–1.0 MPa; and the spray speed is 10–30 r / min.

[0029] Preferably, step S2 is as follows: mixing the pharmaceutical adjuvant granules, dapoxetine hydrochloride and disintegrant for 10-30 minutes, then adding lubricant and mixing for 5-10 minutes, and compressing to obtain the dapoxetine hydrochloride tablets.

[0030] This invention utilizes a solubilizer to dissolve the filler, which has the highest content, and then granulates it in one step to form whole pharmaceutical excipient granules. This one-step granulation method, also known as fluidized bed granulation, involves spraying a solution containing a solubilizer into the powder while hot air flows upwards, keeping the powder (i.e., the filler) in a fluidized state, causing the powder to agglomerate into granules. It completes the three steps of conventional wet granulation—mixing, granulation, and drying—in a single, closed-loop process. The advantages of one-step granulation include simplified operation, reduced hardware equipment, improved production efficiency, optimized resource allocation, and more uniform intermediate granules.

[0031] This invention employs a one-step granulation process, which allows the solubilizer to be fully dispersed and exist in the form of extremely small particles, greatly increasing its specific surface area. This has the following advantages: the solubilizer dissolves rapidly in water, allowing it to exert its solubilizing effect more quickly and effectively; the full dispersion of the solubilizer greatly improves the internal bonding force of the tablet core, reduces porosity, and effectively reduces the contact between dapoxetine hydrochloride and external oxygen, ensuring that the product maintains extremely low impurity levels even after long-term storage.

[0032] The beneficial effects of this invention are as follows: By optimizing the types and ratios of components, the dapoxetine hydrochloride tablets of this invention effectively improve the stability and dissolution rate during accelerated and long-term storage, and reduce the content of impurities. Specifically, the impurity content is less than 0.06% and 0.05% after 6 months of accelerated storage and 36 months of long-term storage, respectively; the 15-minute dissolution rate is 99%–100% after 6 months of accelerated storage; and the 15-minute dissolution rate is 99.2%–100.2% after 36 months of long-term storage.

[0033] The preparation method of this invention is simple in production process, has a high yield, and is suitable for large-scale industrial production. Furthermore, the dapoxetine hydrochloride tablets prepared by the preparation method of this invention have the advantages of excellent storage stability, rapid release and dissolution even after long-term storage, high bioavailability, and extremely low impurity content during long-term storage. Detailed Implementation

[0034] The following examples provide a more detailed description of the specific implementation of the present invention, but the implementation and protection of the present invention are not limited thereto. It should be noted that any processes not specifically described below are those that can be implemented or understood by those skilled in the art by referring to existing technology. Reagents or instruments whose manufacturers are not specified are considered to be conventional products that can be purchased commercially.

[0035] Example 1

[0036] The dapoxetine hydrochloride tablets in this example include the following components:

[0037]

[0038] According to the above component ratio, 1000 tablets of dapoxetine hydrochloride were prepared.

[0039] The dapoxetine hydrochloride tablets in this example were prepared using the following method, which specifically includes the following steps:

[0040] 1) Dissolve the polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer in an appropriate amount of 30% ethanol, set the air inlet temperature to 60℃, the fan frequency to 24Hz, the spray pressure to 0.20MPa, and the spray speed to 18r / min, and granulate it in one step with microcrystalline cellulose and lactose, and then pass it through a 50-mesh sieve to obtain pharmaceutical excipient granules.

[0041] 2) Mix the pharmaceutical adjuvant granules with dapoxetine hydrochloride and calcium carboxymethyl cellulose for 20 minutes, then add talc and mix for 8 minutes. Compress the mixture into tablets to obtain the dapoxetine hydrochloride tablets in this example.

[0042] Example 2

[0043] The dapoxetine hydrochloride tablets in this example include the following components:

[0044]

[0045] According to the above component ratio, 1000 tablets of dapoxetine hydrochloride were prepared.

[0046] The dapoxetine hydrochloride tablets in this example were prepared using the following method, which specifically includes the following steps:

[0047] 1) Dissolve copovidone in an appropriate amount of 40% ethanol, set the air inlet temperature to 70℃, the fan frequency to 18Hz, the spray pressure to 0.15MPa, and the spray speed to 16r / min, and granulate it in one step with cellulose-lactose, and then pass it through a 60-mesh sieve to obtain pharmaceutical excipient granules.

[0048] 2) Mix the pharmaceutical adjuvant granules with dapoxetine hydrochloride and croscarmellose sodium for 20 minutes, then add magnesium stearate and mix for 8 minutes. Compress the mixture into tablets to obtain the dapoxetine hydrochloride tablets in this example.

[0049] Example 3

[0050] The dapoxetine hydrochloride tablets in this example include the following components:

[0051]

[0052] According to the above component ratio, 1000 tablets of dapoxetine hydrochloride were prepared.

[0053] The dapoxetine hydrochloride tablets in this example were prepared using the following method, which specifically includes the following steps:

[0054] 1) Dissolve poloxamer 188 in an appropriate amount of 50% ethanol, set the air inlet temperature to 55℃, the fan frequency to 22Hz, the spray pressure to 0.10MPa, and the spray speed to 14r / min, and granulate it in one step with microcrystalline cellulose and starch, and then pass it through a 70-mesh sieve to obtain pharmaceutical excipient granules.

[0055] 2) Mix the pharmaceutical adjuvant granules with dapoxetine hydrochloride and low-substituted hydroxypropyl cellulose for 20 minutes, then add sodium stearate fumarate and mix for 8 minutes. Compress the mixture into tablets to obtain the dapoxetine hydrochloride tablets in this example.

[0056] Example 4

[0057] The dapoxetine hydrochloride tablets in this example include the following components:

[0058]

[0059] According to the above component ratio, 1000 tablets of dapoxetine hydrochloride were prepared.

[0060] The dapoxetine hydrochloride tablets in this example were prepared using the following method, which specifically includes the following steps:

[0061] 1) Polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and copovidone are dissolved in an appropriate amount of 40% ethanol. The air inlet temperature is set at 65℃, the fan frequency at 20Hz, the spray pressure at 0.15MPa, and the spray speed at 16r / min. The mixture is then granulated in one step with microcrystalline cellulose and mannitol and passed through a 60-mesh sieve to obtain pharmaceutical excipient granules.

[0062] 2) Mix the pharmaceutical adjuvant granules with dapoxetine hydrochloride and crospovidone for 20 minutes, then add magnesium stearate and mix for 8 minutes. Compress the mixture into tablets to obtain the dapoxetine hydrochloride tablets in this example.

[0063] Comparative Examples 1-12

[0064] Comparative Examples 1-12 all followed the formulation and preparation method of Example 2. 1000 tablets of dapoxetine hydrochloride were prepared for each comparative example. The only difference between Comparative Examples 1-5 and Example 2 was the type or amount of solubilizer. The difference between Comparative Examples 6-8 and Example 2 was that they did not contain a solubilizer and used an equal mass of binder instead of a solubilizer. The only difference between Comparative Examples 9-12 and Example 2 was the preparation process. The differences between Comparative Examples 1-12 and Example 2 are shown in Table 1 below.

[0065] Table 1. Differences between Comparative Examples 1-12 and Example 2

[0066]

[0067] Performance testing:

[0068] (1) Stability test

[0069] Examples 1-4, Comparative Examples 1-12, and commercially available original formulations. Stability studies were conducted under long-term conditions (30℃±2℃, 65%±5%RH) and accelerated conditions (40℃±2℃, 75%±5%RH). The testing method was as follows: referring to the imported registration standard for dapoxetine hydrochloride tablets (standard number: JX20150184), high-performance liquid chromatography (HPLC) was used to investigate the content of key quality attributes, i.e., related substances, with total impurities as the indicator. Specific stability test results are recorded in Table 2.

[0070] Table 2. Stability test results of Examples 1-4, Comparative Examples 1-12, and the original formulation (unit: %)

[0071]

[0072] As shown in Table 2, the total impurity content of dapoxetine hydrochloride tablets in Examples 1-4 was no higher than 0.03% after 0 months of storage, which was lower than the total impurity content of the original formulation after 0 months of storage (0.08%). After 6 months of accelerated storage and 36 months of long-term storage, the total impurity content was still no higher than 0.06%. Compared with the original formulation and Comparative Examples 1-12, the total impurity content was at an extremely low level during long-term storage, and the total impurity content hardly increased during storage, showing better stability than the original formulation. In contrast, the total impurity content in Comparative Examples 1-12 was at a relatively high level.

[0073] Compared to Example 2, the solubilizer in Comparative Example 1 had a lower proportion in the formulation, resulting in a weak adhesive effect and an inability to effectively increase the internal binding force of the tablet core. Its oxygen barrier effect was poor, making it difficult to increase tablet stability. Comparative Example 2 had an excessive amount of solubilizer. Because the solubilizer (using surfactant as a solubilizer) has strong hydrophilicity, it caused an increase in tablet moisture content, thus affecting its role as an oxygen barrier and stabilizer in the tablet. Compared to Example 2, Comparative Examples 3-5 used other types of surfactants as solubilizers, and Comparative Examples 6-8 used other types of binders instead of solubilizers. However, Comparative Examples 3-5 and 6-8 failed to effectively increase tablet stability. Comparative Examples 9-11 used three different preparation processes, and the resulting tablets also had poor stability. Comparative Example 12 differed from Example 2 only in the method of preparing the pharmaceutical excipient granules. Comparative Example 12 used a conventional wet granulation followed by drying and sieving process to prepare the pharmaceutical excipient granules, resulting in improved tablet stability, but not as good as in Example 2. A comparison of Comparative Examples 1-8 and Example 2 shows that the components of the dapoxetine hydrochloride tablets in this invention have a synergistic effect. Changing the type and amount of components reduces the stability of the dapoxetine hydrochloride tablets, and the content of impurities increases significantly with prolonged storage time. A comparison of Comparative Examples 9-12 and Example 2 shows that changing the overall tablet preparation process or only changing the preparation method of the pharmaceutical excipient granules reduces the stability of the resulting dapoxetine hydrochloride tablets.

[0074] (2) Dissolution test

[0075] Examples 1-4, Comparative Examples 1-12, and commercially available original formulations. Dissolution was tested after treatment under long-term conditions (30℃±2℃, 65%±5%RH) and accelerated conditions (40℃±2℃, 75%±5%RH). The test method was as follows: referring to the imported registration standard for dapoxetine hydrochloride tablets (standard number: JX20150184), the dissolution test method (European Pharmacopoeia 8.0 version 2.9.3 Method II) was used to examine the key quality attribute, dissolution. To focus on whether the dissolution rate of the product changed significantly during storage, the dissolution test time point was 15 minutes. The measured dissolution data are shown in Table 3.

[0076] Table 3. Dissolution test results of Examples 1-4, Comparative Examples 1-12, and the original formulation (unit: %)

[0077]

[0078]

[0079] As shown in Table 3, the 15-minute dissolution rate of dapoxetine hydrochloride tablets in Examples 1-4 was 97.5%-99.3% after 0 months of storage, 99%-100% after 6 months of accelerated storage, and 99.2%-100.2% after 36 months of long-term storage. This means that the 15-minute dissolution rate did not decrease after 6 months of accelerated storage and 36 months of long-term storage, remaining at essentially the same level as the freshly prepared tablets, demonstrating excellent rapid release. The original formulation showed no significant change in dissolution rate after 6 months of accelerated storage, but its 15-minute dissolution rate after 36 months of long-term storage was only 75.1%, failing to meet the requirement for rapid dissolution (i.e., 15-minute dissolution rate ≥ 85%). Therefore, the dapoxetine hydrochloride tablets in this invention exhibit better dissolution stability than the original formulation. Comparative Examples 1-12 showed no significant change in dissolution rate during accelerated storage for 6 months, but after long-term storage for 36 months, the dissolution rate at 15 minutes all showed a significant decrease, even failing to meet the requirements for rapid dissolution, thus affecting the release and absorption of the drug in vivo. Specifically: in Comparative Example 1, the proportion of solubilizer in the formulation was low, and the solubilizing effect of the solubilizer was not significant, failing to effectively stabilize the dissolution rate during storage; in Comparative Example 2, the solubilizer content was too high, and due to the strong hydrophilicity of the solubilizer (i.e., surfactant), the moisture content of the tablets increased, affecting the disintegration of the tablets; in Comparative Examples 3-12, changes in excipients or processes failed to effectively maintain the stability of tablet dissolution. Among them, the dissolution stability of the tablets in Comparative Example 12 was improved, but it was still not as good as that in Example 2.

[0080] The method for preparing dapoxetine hydrochloride tablets disclosed in this invention involves adding a solubilizer that simultaneously functions as a binder to the formulation. The solubilizer and filler are then granulated in a one-step process to form pharmaceutical excipient granules, facilitating thorough dispersion of the solubilizer and maximizing both solubilizing and binding effects. The results of two key performance tests—stability and dissolution—clearly demonstrate that this invention, by selecting a solubilizer with binding properties and granulating the solubilizer and filler in a one-step process, maximizes the solubilizing effect, enabling rapid dissolution of the tablets and maintaining stable dissolution over a longer period. Simultaneously, it maximizes the binding effect, ensuring the highest internal binding force within the tablet, thereby minimizing core porosity, reducing contact between the active pharmaceutical ingredient and the external environment, and guaranteeing good stability.

[0081] In Comparative Examples 1-12, changing the amount or type of the selected solubilizer, using a different adhesive, or employing other preparation processes did not achieve the good results shown in the embodiments of the present invention, and thus failed to achieve the purpose of the present invention.

[0082] Compared with other existing methods for preparing dapoxetine hydrochloride tablets, this invention does not require micronization of the active pharmaceutical ingredient (API) or dry or wet granulation. The preparation process is simple, which is conducive to industrial production. Furthermore, the product dissolves rapidly, which is beneficial to improving bioavailability in vivo. It also has better stability, which is beneficial to the storage and transportation of the product. This invention provides a novel and efficient approach and process for preparing tablet drugs.

[0083] The embodiments of the present invention have been described in detail above. However, the present invention is not limited to the above embodiments. Within the scope of knowledge possessed by those skilled in the art, various changes can be made without departing from the spirit of the present invention. Furthermore, the embodiments of the present invention and the features thereof can be combined with each other unless otherwise specified.

Claims

1. A dapoxetine hydrochloride tablet, characterized in that: It comprises the following components by weight percentage: dapoxetine hydrochloride 15%~45%; filler 45%~75%; solubilizer 0.1%~2%; disintegrant 2%~10%; lubricant 0.5%~3%; The solubilizer is selected from at least one of the following: polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, poloxamer 188, and copovidone. The dapoxetine hydrochloride tablets are prepared using a method comprising the following steps: S1: Granulate the solubilizer and filler in one step to obtain pharmaceutical excipient granules; S2: The pharmaceutical adjuvant granules are mixed with dapoxetine hydrochloride, disintegrant and lubricant and then compressed into tablets to obtain the dapoxetine hydrochloride tablets.

2. The dapoxetine hydrochloride tablets according to claim 1, characterized in that: The filler is selected from at least one of microcrystalline cellulose, mannitol, lactose, cellulose-lactose, starch, pregelatinized starch, dicalcium phosphate, and silicified microcrystalline cellulose; And / or, the disintegrant is selected from at least one of crospovidone, crospovidone sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, sodium carboxymethyl starch, and low-substituted hydroxypropyl cellulose; and / or, the lubricant is selected from at least one of silica, talc, magnesium stearate, and sodium stearate fumarate.

3. The dapoxetine hydrochloride tablets according to claim 1, characterized in that: The mass percentage of dapoxetine hydrochloride is 20-40%; And / or, the filler has a mass percentage of 50-70%; And / or, the mass percentage of the solubilizer is 0.5% to 1.5%; And / or, the disintegrant has a mass percentage of 2-8%; And / or, the lubricant has a mass percentage of 0.5-2%.

4. The dapoxetine hydrochloride tablets according to claim 1 or 3, characterized in that: The mass percentage of dapoxetine hydrochloride is 25-35%; And / or, the filler has a mass percentage of 55-65%; And / or, the mass percentage of the solubilizer is 0.7~1.3%; And / or, the disintegrant has a mass percentage of 3-6%; And / or, the mass percentage of the lubricant is 0.5% to 1.5%.

5. The dapoxetine hydrochloride tablets according to claim 1, characterized in that: The particle size D90 value of the dapoxetine hydrochloride is 100~200μm.

6. The method for preparing dapoxetine hydrochloride tablets according to any one of claims 1 to 5, characterized in that: Includes the following steps: S1: Granulate the solubilizer and filler in one step to obtain pharmaceutical excipient granules; S2: The pharmaceutical adjuvant granules are mixed with dapoxetine hydrochloride, disintegrant and lubricant and then compressed into tablets to obtain the dapoxetine hydrochloride tablets.

7. The method for preparing dapoxetine hydrochloride tablets according to claim 6, characterized in that: Step S1 is: granulating the solubilizing alcohol solution and the filler using a one-step granulation method.

8. The method for preparing dapoxetine hydrochloride tablets according to claim 7, characterized in that: The alcohols include ethanol or isopropanol.

9. The method for preparing dapoxetine hydrochloride tablets according to claim 6 or 7, characterized in that: In the granulation step, the inlet air temperature is 40~100℃; the fan frequency is 10~30Hz; the spray pressure is 0.1~1.0MPa; and the spray speed is 10~30r / min.

10. The method for preparing dapoxetine hydrochloride tablets according to claim 6, characterized in that: Step S2 is as follows: mix the pharmaceutical adjuvant granules, dapoxetine hydrochloride and disintegrant for 10-30 minutes, then add lubricant and mix for 5-10 minutes, and compress to obtain dapoxetine hydrochloride tablets.

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