CN110840851A - Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof - Google Patents

Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof Download PDF

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CN110840851A
CN110840851A CN201910759120.2A CN201910759120A CN110840851A CN 110840851 A CN110840851 A CN 110840851A CN 201910759120 A CN201910759120 A CN 201910759120A CN 110840851 A CN110840851 A CN 110840851A
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mixed powder
orally disintegrating
disintegrating tablet
agent
vardenafil hydrochloride
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左人杰
孙超
杨士珉
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Tianjin Renwei Biomedical Technology Co Ltd
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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a vardenafil hydrochloride orally disintegrating tablet and a preparation method thereof. The vardenafil hydrochloride orally disintegrating tablet comprises a main drug and auxiliary materials, wherein the main drug comprises vardenafil hydrochloride trihydrate, and the auxiliary materials comprise a filling agent, a disintegrating agent, a flow aid, a pH regulator, a flavoring agent, a lubricant and a sweetening agent. According to the vardenafil orally disintegrating tablet, the pH regulator component is added into the vardenafil orally disintegrating tablet, so that the stability of the main drug is improved, the situation that oxidation impurities are increased in the placing process of the orally disintegrating tablet is improved, and the medication safety is improved. Meanwhile, the acidic pH regulator also has the function of a flavoring agent, so that the taste of the orally disintegrating tablet is further improved. The preparation method of the orally disintegrating tablet adopts the powder direct-compression process technology to prepare the vardenafil hydrochloride orally disintegrating tablet, can ensure that vardenafil is quickly dissolved, has low requirements on equipment, is simple and easy to operate, saves cost, and is easy for industrial application.

Description

Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof
Technical Field
The invention belongs to the field of pharmaceutical preparations, and particularly relates to a vardenafil hydrochloride orally disintegrating tablet and a preparation method thereof.
Background
Vardenafil hydrochloride is a potent highly selective phosphodiesterase 5 inhibitor, has a rapid onset of action, is a second drug approved for the market after marigold for the treatment of male erectile dysfunction, and is one of the internationally recognized first-line oral drugs for the treatment of male erectile dysfunction.
Vardenafil hydrochloride orally disintegrating tablet (trade name: STAXYN), specification 10mg, preparation for erectile dysfunction developed by bayer corporation, marketed in the united states in 2010. This variety has not been on the market at present for a while. The vardenafil hydrochloride tablet (trade name: Levitra) which is the product of the previous generation has the annual sale amount of more than 4 hundred million euros.
The vardenafil hydrochloride orally disintegrating tablet can be automatically disintegrated in the oral cavity, any beverage is not needed to be supplemented during administration, the tablet is more convenient to use, and a user can secretly take the tablet. In the technology disclosed in the prior art, vardenafil hydrochloride solid preparations, two preparation technologies are mainly used, one is a common tablet with relatively slow dissolution, and the other is an orally disintegrating tablet with rapid dissolution. For example, patent CN1681481B discloses a process for preparing coated tablets containing vardenafil hydrochloride trihydrate in solid form at any water content. Patent CN101141950B discloses a fast-releasing orally disintegrating tablet using sugar alcohol as main filler and a preparation method thereof, wherein the method can effectively improve bioavailability. Patent CN102198140B discloses a fast-releasing orally disintegrating tablet using sugar alcohol as main filler and a preparation method thereof, wherein the method can effectively improve bioavailability. Patent CN103372014B discloses an antioxidant-added vardenafil hydrochloride oral preparation, which has rapid drug release and improved drug stability. In the prior art, the bioavailability of vardenafil is mainly improved or the stability of vardenafil is improved by adding an antioxidant.
Since vardenafil hydrochloride is easily oxidized, oxidation impurities are easily generated in the storage process, the curative effect of the medicament is influenced, and side effects are increased. Although the addition of antioxidants can reduce the generation of oxidation impurities to some extent, in recent years, countries have made some controversy about the toxic and side effects of synthetic antioxidants in use, and thus the addition of antioxidants is not the optimal choice for solving the problem. Therefore, a new vardenafil preparation which can be quickly dissolved out, is relatively stable and is not easy to generate oxidation impurities is urgently needed.
Disclosure of Invention
In order to solve the problems in the prior art, the invention provides a vardenafil hydrochloride orally disintegrating tablet and a preparation method thereof. By adding the pH regulator component into the vardenafil hydrochloride orally disintegrating tablet, the generation speed of oxidation impurities can be effectively reduced, and the medication safety is improved. In addition, the vardenafil hydrochloride orally disintegrating tablet is prepared by adopting a powder direct compression process technology, and the preparation method can ensure that vardenafil is quickly dissolved out, has low requirements on equipment, is simple and easy to operate, saves cost and is easy for industrial application.
In order to solve the problems, the invention adopts the following technical scheme:
the vardenafil hydrochloride orally disintegrating tablet comprises a main drug and an auxiliary material, wherein the main drug and the auxiliary material are related in parts by weight as follows:
composition (I) Parts by weight
Vardenafil hydrochloride trihydrate 1 part of
Filler 6-15 parts of
Disintegrating agent 2-5 parts of
Glidants 0.2 to 1 portion
pH regulator 0.1 to 0.5 portion
Flavouring agent 0.01 to 0.5 portion
Lubricant agent 0.2 to 1 portion
Sweetening agent 0 to 1 portion of
The main drug comprises vardenafil hydrochloride trihydrate, and the auxiliary materials comprise a filling agent, a disintegrating agent, a flow aid, a pH regulator, a flavoring agent, a lubricant and a sweetening agent.
In some embodiments, the main ingredient and the auxiliary ingredient are related in parts by weight as follows:
Figure BDA0002169704450000021
Figure BDA0002169704450000031
the main drug comprises vardenafil hydrochloride trihydrate, and the auxiliary materials comprise a filling agent, a disintegrating agent, a flow aid, a pH regulator, a flavoring agent, a lubricant and a sweetening agent.
In certain embodiments, the primary drug particle size D90Less than or equal to 20 μm (e.g., D)905 μm, 10 μm, 11-15 μm, 16 μm, 18 μm, 20 μm).
In certain embodiments, the filler is selected from one or more of microcrystalline cellulose, lactose, starch, silicified microcrystalline cellulose.
In certain embodiments, the disintegrant is selected from one or more of croscarmellose sodium, crospovidone, and sodium starch glycolate.
In certain embodiments, the glidant is selected from one or more of magnesium stearate, calcium stearate, and colloidal silicon dioxide.
In certain embodiments, the sweetener is selected from one or more of sucrose, aspartame, and sodium saccharin.
In certain embodiments, the pH adjusting agent is selected from one or more of citric acid, DL-tartaric acid, and fumaric acid.
In certain embodiments, the lubricant is selected from one or more of magnesium stearate, calcium stearate, colloidal silicon dioxide.
In certain embodiments, the flavoring agent is selected from mint flavors, cherry flavors, lemon flavors, and the like.
In certain embodiments, in the above orally disintegrating tablet, the filler is lactose and silicified microcrystalline cellulose, the disintegrant is crospovidone, the glidant is colloidal silicon dioxide, the pH adjusting agent is citric acid, and the lubricant is sodium stearyl fumarate and magnesium stearate.
The preparation method of the vardenafil hydrochloride orally disintegrating tablet adopts a dry mixing direct compression process to prepare the orally disintegrating tablet, and comprises the following steps:
(1) sieving the main drug, the filler, the disintegrant, the glidant and the sweetener together to obtain first mixed powder;
(2) sieving the flavoring agent and the pH regulator to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2), and sieving to obtain third mixed powder;
(4) mixing and sieving the third mixed powder prepared in the step (3) to obtain fourth mixed powder;
(5) mixing the fourth mixed powder prepared in the step (4) to obtain fifth mixed powder;
(6) sieving the lubricant to obtain sixth mixed powder;
(7) mixing the fifth mixed powder prepared in the step (5) and the sixth mixed powder prepared in the step (6) to obtain seventh mixed powder;
(8) and (4) tabletting the seventh mixed powder prepared in the step (7) by using a punch to obtain the orally disintegrating tablet.
In certain embodiments, in step (1), the sieving is through a 30-40 mesh sieve.
In certain embodiments, in step (2), the sieving is through a 50-60 mesh sieve.
In certain embodiments, in step (3), the sieving is through a 30-40 mesh sieve.
In certain embodiments, in step (4), the sieving is through a 30-40 mesh sieve.
In certain embodiments, in step (6), the sieving is through a 50-60 mesh sieve.
The vardenafil hydrochloride orally disintegrating tablet is prepared by adopting a dry mixing direct compression process, namely, the vardenafil hydrochloride orally disintegrating tablet is sieved and mixed for multiple times to eliminate the large particle size difference of raw materials and auxiliary materials, so that a material which has good mixing uniformity and is not easy to delaminate is obtained.
Compared with the prior art, the technical scheme of the invention has the following technical effects:
1. the vardenafil hydrochloride orally disintegrating tablet provided by the invention is added with a pH regulator component, so that the stability of vardenafil hydrochloride trihydrate is improved, the situation that oxidation impurities are increased in the standing process of the vardenafil hydrochloride orally disintegrating tablet is improved, and the medication safety is improved. Meanwhile, the acidic pH regulator also has the function of a flavoring agent, so that the taste of the orally disintegrating tablet is further improved.
2. The invention also provides a preparation method of the vardenafil hydrochloride orally disintegrating tablet, which adopts small-granularity materials as raw materials to increase the dissolution rate of vardenafil and solves the problem of mixing uniformity through a process of repeated mixing and sieving. The vardenafil hydrochloride orally disintegrating tablet is prepared by adopting a powder direct compression process technology, and the preparation method can ensure that vardenafil is quickly dissolved out, has low requirements on equipment, is simple and easy to operate, saves cost and is easy for industrial application.
Detailed Description
The present invention is described in detail below with reference to specific examples, but these exemplary embodiments are not intended to limit the actual scope of the present invention in any manner.
The raw materials, chemical reagents, instruments and the like used in the examples of the present invention are all commercially available products unless the conditions are specified.
Example 1
The prescription composition and the dosage are as follows:
composition (I) Prescription dose (mg)
Vardenafil hydrochloride trihydrate 11.85
Lactose 45.92
Silicified microcrystalline cellulose 55.13
Cross-linked polyvidone 38.00
Colloidal silica 6.40
Saccharin sodium salt 2.50
Citric acid monohydrate 2.40
Cherry essence 1.00
Stearic acid sodium fumarate 4.80
Magnesium stearate 2.00
Total weight of 170
Note: vardenafil hydrochloride trihydrate D9020.3 μm.
The preparation method comprises the following steps:
(1) weighing the vardenafil hydrochloride trihydrate, lactose monohydrate, silicified microcrystalline cellulose, crospovidone, colloidal silicon dioxide and saccharin sodium in the prescribed amount, and sieving the weighed materials with a 40-mesh sieve to obtain first mixed powder;
(2) weighing the essence and the citric acid monohydrate in the amount according to the prescription, and sieving the mixture through a 60-mesh sieve to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2) for 15 minutes, and sieving the mixture by a 30-mesh sieve to obtain third mixed powder;
(4) mixing the third mixed powder prepared in the step (3) for 15 minutes, and sieving the mixture by a 40-mesh sieve to obtain fourth mixed powder;
(5) mixing the fourth mixed powder prepared in the step (4) for 10 minutes to obtain fifth mixed powder;
(6) weighing magnesium stearate and sodium stearyl fumarate in the formula amount, and sieving with a 60-mesh sieve to obtain sixth mixed powder;
(7) mixing the fifth mixed powder prepared in the step (5) and the sixth mixed powder prepared in the step (6) for 3 minutes to obtain seventh mixed powder;
(8) the seventh mixed powder prepared in the step (7) is used
Figure BDA0002169704450000062
And (3) tabletting by using a standard concave punch to obtain the orally disintegrating tablet.
Example 2
The prescription composition and the dosage are as follows:
Figure BDA0002169704450000061
Figure BDA0002169704450000071
note: vardenafil hydrochloride trihydrate D9020.3 μm.
The preparation method comprises the following steps:
(1) weighing the vardenafil hydrochloride trihydrate, lactose monohydrate, silicified microcrystalline cellulose, crospovidone, colloidal silicon dioxide and saccharin sodium in the prescribed amount, and sieving the weighed materials with a 40-mesh sieve to obtain first mixed powder;
(2) weighing the essence according to the prescription amount, and sieving the essence with a 60-mesh sieve to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2) for 15 minutes, and sieving the mixture by a 30-mesh sieve to obtain third mixed powder;
(4) mixing the third mixed powder prepared in the step (3) for 15 minutes, and sieving the mixture by a 40-mesh sieve to obtain fourth mixed powder;
(5) mixing the fourth mixed powder prepared in the step (4) for 10 minutes to obtain fifth mixed powder;
(6) weighing magnesium stearate and sodium stearyl fumarate in the formula amount, and sieving with a 60-mesh sieve to obtain sixth mixed powder;
(7) mixing the fifth mixed powder prepared in the step (5) and the sixth mixed powder prepared in the step (6) for 3 minutes to obtain seventh mixed powder;
(8) the seventh mixed powder prepared in the step (7) is used
Figure BDA0002169704450000073
And (3) tabletting by using a standard concave punch to obtain the orally disintegrating tablet.
Example 3
The prescription composition and the dosage are as follows:
Figure BDA0002169704450000072
Figure BDA0002169704450000081
note: vardenafil hydrochloride trihydrate D9020.3 μm.
Example 3 the preparation method of orally disintegrating tablets is the same as example 1.
Example 4
The prescription composition and the dosage are as follows:
composition (I) Prescription dose (mg)
Vardenafil hydrochloride trihydrate 11.85
Lactose 47.4
Silicified microcrystalline cellulose 47.4
Cross-linked polyvidone 29.6
Colloidal silica 3.6
Saccharin sodium salt 1.17
Citric acid monohydrate 1.18
Cherry essence 0.6
Stearic acid sodium fumarate 2.3
Magnesium stearate 2.4
Total weight of 147.5
Note: vardenafil hydrochloride trihydrate D9020.3 μm.
Example 4 the preparation method of orally disintegrating tablets is the same as in example 1.
Example 5
The prescription composition and the dosage are as follows:
Figure BDA0002169704450000082
Figure BDA0002169704450000091
note: validan hydrochlorideNafina trihydrate D9020.3 μm.
The preparation method comprises the following steps:
(1) weighing the vardenafil hydrochloride trihydrate, lactose monohydrate, silicified microcrystalline cellulose, crospovidone, colloidal silicon dioxide and sucrose according to the prescription amount, and sieving the weighed materials with a 40-mesh sieve to obtain first mixed powder;
(2) weighing the essence and the citric acid monohydrate in the amount according to the prescription, and sieving the mixture through a 60-mesh sieve to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2) for 15 minutes, and sieving the mixture by a 30-mesh sieve to obtain third mixed powder;
(4) mixing the third mixed powder prepared in the step (3) for 15 minutes, and sieving the mixture by a 40-mesh sieve to obtain fourth mixed powder;
(5) mixing the fourth mixed powder prepared in the step (4) for 10 minutes to obtain fifth mixed powder;
(6) weighing magnesium stearate and sodium stearyl fumarate in the formula amount, and sieving with a 60-mesh sieve to obtain sixth mixed powder;
(7) mixing the fifth mixed powder prepared in the step (5) and the sixth mixed powder prepared in the step (6) for 3 minutes to obtain seventh mixed powder;
(8) the seventh mixed powder prepared in the step (7) is used
Figure BDA0002169704450000093
And (3) tabletting by using a standard concave punch to obtain the orally disintegrating tablet.
Example 6
The prescription composition and the dosage are as follows:
Figure BDA0002169704450000092
note: vardenafil hydrochloride trihydrate D9020.3 μm.
The preparation method comprises the following steps:
(1) weighing the vardenafil hydrochloride trihydrate, the lactose monohydrate, the silicified microcrystalline cellulose, the crospovidone and the colloidal silicon dioxide in the prescribed amount, and sieving the weighed materials with a 40-mesh sieve to obtain first mixed powder;
(2) weighing the essence and the citric acid monohydrate in the amount according to the prescription, and sieving the mixture through a 60-mesh sieve to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2) for 15 minutes, and sieving the mixture by a 30-mesh sieve to obtain third mixed powder;
(4) mixing the third mixed powder prepared in the step (3) for 15 minutes, and sieving the mixture by a 40-mesh sieve to obtain fourth mixed powder;
(5) mixing the fourth mixed powder prepared in the step (4) for 10 minutes to obtain fifth mixed powder;
(6) weighing magnesium stearate and sodium stearyl fumarate in the formula amount, and sieving with a 60-mesh sieve to obtain sixth mixed powder;
(7) mixing the fifth mixed powder prepared in the step (5) and the sixth mixed powder prepared in the step (6) for 3 minutes to obtain seventh mixed powder;
(8) the seventh mixed powder prepared in the step (7) is used
Figure BDA0002169704450000102
And (3) tabletting by using a standard concave punch to obtain the orally disintegrating tablet.
Example 7
EXAMPLE 7 vardenafil hydrochloride trihydrate compound D of example 1, example 790It was 9.8 μm.
Example 7 the preparation method of orally disintegrating tablets is the same as in example 1.
Example 8
EXAMPLE 8 formulation and amounts of the same D of vardenafil hydrochloride trihydrate as in examples 1 and 890And 40.5 μm.
Example 8 the preparation method of orally disintegrating tablets is the same as example 1.
Example 9
EXAMPLE 9 Vardenafil hydrochloride trihydrate, as in example 1, example 9Compound D9020.3 μm.
The preparation method comprises the following steps:
(1) weighing the vardenafil hydrochloride trihydrate, lactose monohydrate, silicified microcrystalline cellulose, crospovidone, colloidal silicon dioxide and saccharin sodium in the prescribed amount, and sieving the weighed materials with a 40-mesh sieve to obtain first mixed powder;
(2) weighing the essence and the citric acid monohydrate in the amount according to the prescription, and sieving the mixture through a 60-mesh sieve to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2) for 15 minutes, and sieving the mixture by a 30-mesh sieve to obtain third mixed powder;
(4) the third mixed powder prepared in the step (3) and the material in the step (4) are mixed for 10 minutes to obtain fourth mixed powder;
(5) weighing magnesium stearate and sodium stearyl fumarate in the formula amount, and sieving with a 60-mesh sieve to obtain fifth mixed powder;
(6) mixing the fourth mixed powder prepared in the step (4) and the fifth mixed powder prepared in the step (5) for 3 minutes to obtain sixth mixed powder;
(7) the sixth mixed powder prepared in the step (6) is used
Figure BDA0002169704450000111
And (3) tabletting by using a standard concave punch to obtain the orally disintegrating tablet.
Test example 1
The mixing uniformity RSD is not more than 5 percent and is judged to be qualified, and the measuring method of the mixing uniformity is as follows: sampling 5 different positions (upper middle, middle front, middle, middle lower and lower middle) of the total mixing (mixing powder before tabletting), detecting the content, calculating the RSD% after obtaining the content of different positions, wherein the RSD% is not more than 5%.
The content is qualified when the content is 95-105 percent, and the content measurement method comprises the following steps: the detection is carried out according to the method under the content item of JX20030240 content of Vardenafil hydrochloride tablet import medicine rechecking standard (34).
The identification method of the mouthfeel comprises the following steps: the tablets were distributed to 10 adult males and administered, and the mouth feel was scored (full score at 10, 9 based on the original Staxyn score), excellent at 7-10 on average, good at 6-7 on average, normal at 3-6 on average, and poor at 0-3 on average.
The comparative example was StaXYN, and the manufacturer was Bayer (Bayer).
The results of the above parameter measurements are detailed in Table 1.
TABLE 1
Group of RSD Content (wt.) Taste of the product
Example 1 Qualified Qualified Is excellent in
Example 2 Qualified Qualified Good effect
Example 3 Qualified Qualified Is excellent in
Example 4 Qualified Qualified Is excellent in
Example 5 Qualified Qualified In general
Example 6 Qualified Qualified In general
Example 7 Qualified Qualified Is excellent in
Example 8 Qualified Qualified Is excellent in
Example 9 Fail to be qualified / /
Comparative example Qualified Qualified Is excellent in
"/" indicates that no corresponding parameter was measured, due to an RSD value failure.
Test example 2 dissolution measurement
The specific test method for dissolution rate: the dissolution and release determination method of 0512 of part 4 of Chinese pharmacopoeia 2015 edition (paddle method) is adopted to detect under the condition of 900ml of 0.1N hydrochloric acid medium rotating speed of 50rpm, and the sampling time is 5 minutes, 10 minutes, 15 minutes and 30 minutes respectively. The comparative example is STAXYN, the samples at each time point are detected by high performance liquid chromatography, and the test results are shown in Table 2.
TABLE 2
Figure BDA0002169704450000131
As can be seen from table 2, the dissolution rates at the respective time points of the orally disintegrating tablets of examples 1 to 5 and example 7 were similar to those of the comparative examples, while the dissolution rates at the respective time points of the orally disintegrating tablets of examples 6 and example 8 were slower than those of the comparative examples.
Test example 3 measurement of oxidized impurities
Specific determination methods for oxidized impurities: the detection is carried out according to the method under the item of related substances of the vardenafil hydrochloride tablet import medicine rechecking standard (34) JX 20030240. The comparative example was STAXYN, and the specific measurement results are shown in Table 3.
TABLE 3
As can be seen from table 3, the content of the oxidized impurities in the orally disintegrating tablets of examples 1 and 3 to 8 is lower than that of the comparative example, wherein the content of the oxidized impurities in the orally disintegrating tablets of examples 1, 3 to 4 and 7 to 8 is obviously lower than that of the comparative example, while the content of the oxidized impurities in the orally disintegrating tablet of example 2 is similar to that of the comparative example, which shows that the orally disintegrating tablet of the present invention has better stability and higher safety.
It should be understood that these examples are for illustrative purposes only and are not intended to limit the scope of the present invention. Further, it should also be understood that various alterations, modifications and/or variations can be made to the present invention by those skilled in the art after reading the technical content of the present invention, and all such equivalents fall within the protective scope defined by the claims of the present application.

Claims (10)

1. A vardenafil hydrochloride orally disintegrating tablet is characterized by comprising a main drug and auxiliary materials,
the main medicine and the auxiliary materials have the following weight part relationship:
composition (I) Parts by weight Vardenafil hydrochloride trihydrate 1 part of Filler 6-15 parts of Disintegrating agent 2-5 parts of Glidants 0.2 to 1 portion pH regulator 0.1 to 0.5 portion Flavouring agent 0.01 to 0.5 portion Lubricant agent 0.2 to 1 portion Sweetening agent 0 to 1 portion of
The main drug comprises vardenafil hydrochloride trihydrate, and the auxiliary materials comprise a filling agent, a disintegrating agent, a flow aid, a pH regulator, a flavoring agent, a lubricant and a sweetening agent.
2. The vardenafil hydrochloride orally disintegrating tablet as claimed in claim 1, wherein the main drug and the auxiliary materials are in the following relationship in parts by weight:
composition (I) Parts by weight Vardenafil hydrochloride trihydrate 1 part of Filler 8-13 parts of Disintegrating agent 2.5 to 4 portions of Glidants 0.3 to 0.8 portion pH regulator 0.1 to 0.3 portion Flavouring agent 0.05 to 0.2 portion Lubricant agent 0.4 to 0.8 portion Sweetening agent 0.1 to 0.5 portion
The main drug comprises vardenafil hydrochloride trihydrate, and the auxiliary materials comprise a filling agent, a disintegrating agent, a flow aid, a pH regulator, a flavoring agent, a lubricant and a sweetening agent.
3. The vardenafil hydrochloride orally disintegrating tablet according to claim 1 or 2, wherein the principal drug particle size D is90≤20μm。
4. The vardenafil hydrochloride orally disintegrating tablet according to any one of claims 1 to 3, wherein the filler is one or more selected from the group consisting of microcrystalline cellulose, lactose, starch, silicified microcrystalline cellulose.
5. The vardenafil hydrochloride orally disintegrating tablet according to any one of claims 1 to 4, wherein the disintegrant is one or more selected from the group consisting of croscarmellose sodium, crospovidone, and sodium carboxymethyl starch.
6. Vardenafil hydrochloride orally disintegrating tablet according to any of claims 1 to 5, wherein the glidant is selected from one or more of magnesium stearate, calcium stearate colloidal silicon dioxide; preferably, the sweetener is one or more selected from sucrose, aspartame and saccharin sodium.
7. The vardenafil hydrochloride orally disintegrating tablet according to any one of claims 1 to 6, wherein the pH regulator is one or more selected from citric acid, DL-tartaric acid and fumaric acid; preferably, the pH adjusting agent is citric acid monohydrate.
8. The vardenafil hydrochloride orally disintegrating tablet according to any one of claims 1 to 7, wherein the lubricant is selected from one or more of magnesium stearate, calcium stearate, colloidal silicon dioxide; preferably, the flavoring agent is mint essence, cherry essence or lemon essence;
more preferably, the filler is lactose and silicified microcrystalline cellulose, the disintegrant is crospovidone, the glidant is colloidal silicon dioxide, the pH adjusting agent is citric acid, and the lubricant is sodium stearyl fumarate and magnesium stearate.
9. The preparation method of vardenafil hydrochloride orally disintegrating tablet as claimed in any one of claims 1 to 8, wherein the orally disintegrating tablet is prepared by dry mixing and direct compression process, comprising the following steps:
(1) sieving the main drug, the filler, the disintegrant, the glidant and the sweetener together to obtain first mixed powder;
(2) sieving the flavoring agent and the pH regulator to obtain second mixed powder;
(3) mixing the first mixed powder prepared in the step (1) and the second mixed powder prepared in the step (2), and sieving to obtain third mixed powder;
(4) mixing and sieving the third mixed powder prepared in the step (3) to obtain fourth mixed powder;
(5) mixing the fourth mixed powder prepared in the step (4) to obtain fifth mixed powder;
(6) sieving the lubricant to obtain sixth mixed powder;
(7) mixing the fifth mixed powder prepared in the step (5) and the sixth mixed powder prepared in the step (6) to obtain seventh mixed powder;
(8) and (4) tabletting the seventh mixed powder prepared in the step (7) by using a punch to obtain the orally disintegrating tablet.
10. The method of manufacturing according to claim 9, characterized by one or more of the following 1) to 5):
in the step (1), the sieving is to pass through a 30-40-mesh sieve;
in the step (2), the sieving is to pass through a sieve of 50-60 meshes;
in the step (3), the sieving is to pass through a 30-40-mesh sieve;
in the step (4), the sieving is to pass through a 30-40-mesh sieve;
in the step (6), the sieving is to pass through a sieve of 50-60 meshes.
CN201910759120.2A 2019-08-16 2019-08-16 Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof Pending CN110840851A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111346062A (en) * 2020-03-11 2020-06-30 左人杰 Orally disintegrating tablet with composite calcium salt for improving stability of main drug and preparation method thereof
CN115737581A (en) * 2022-12-13 2023-03-07 上海普康药业有限公司 Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof

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Publication number Priority date Publication date Assignee Title
CN1984661A (en) * 2004-05-11 2007-06-20 拜耳医药保健股份公司 Controlled-release formulations containing vardenafil
CN101141950A (en) * 2005-03-01 2008-03-12 拜耳医药保健股份公司 Pharmaceutical forms with improved pharmacokinetic properties
CN108272765A (en) * 2018-04-26 2018-07-13 江西杏林白马药业有限公司 Pharmaceutical composition, oral disintegrating tablet and its preparation, the application of hydrochloric Vardenafil

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
CN1984661A (en) * 2004-05-11 2007-06-20 拜耳医药保健股份公司 Controlled-release formulations containing vardenafil
CN101141950A (en) * 2005-03-01 2008-03-12 拜耳医药保健股份公司 Pharmaceutical forms with improved pharmacokinetic properties
CN108272765A (en) * 2018-04-26 2018-07-13 江西杏林白马药业有限公司 Pharmaceutical composition, oral disintegrating tablet and its preparation, the application of hydrochloric Vardenafil

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111346062A (en) * 2020-03-11 2020-06-30 左人杰 Orally disintegrating tablet with composite calcium salt for improving stability of main drug and preparation method thereof
CN115737581A (en) * 2022-12-13 2023-03-07 上海普康药业有限公司 Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof
CN115737581B (en) * 2022-12-13 2024-03-12 上海普康药业有限公司 Vardenafil hydrochloride orally disintegrating tablet and preparation method thereof

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