CN115707454A - Valsartan orally disintegrating tablet - Google Patents
Valsartan orally disintegrating tablet Download PDFInfo
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- CN115707454A CN115707454A CN202110946363.4A CN202110946363A CN115707454A CN 115707454 A CN115707454 A CN 115707454A CN 202110946363 A CN202110946363 A CN 202110946363A CN 115707454 A CN115707454 A CN 115707454A
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- Prior art keywords
- valsartan
- orally disintegrating
- mixing
- disintegrating tablet
- flavoring agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Links
- 239000004072 C09CA03 - Valsartan Substances 0.000 title claims abstract description 32
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 title claims abstract description 32
- 229960004699 valsartan Drugs 0.000 title claims abstract description 32
- 239000006191 orally-disintegrating tablet Substances 0.000 title claims abstract description 16
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims abstract description 30
- 238000002360 preparation method Methods 0.000 claims abstract description 15
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims abstract description 12
- 235000013599 spices Nutrition 0.000 claims abstract description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 8
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 5
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims abstract description 5
- 229960000913 crospovidone Drugs 0.000 claims abstract description 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 5
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims abstract description 5
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims abstract description 5
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims abstract description 4
- 108010011485 Aspartame Proteins 0.000 claims abstract description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 4
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims abstract description 4
- 239000000605 aspartame Substances 0.000 claims abstract description 4
- 235000010357 aspartame Nutrition 0.000 claims abstract description 4
- 229960003438 aspartame Drugs 0.000 claims abstract description 4
- 229960004106 citric acid Drugs 0.000 claims abstract description 4
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims abstract description 4
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 4
- 229940085605 saccharin sodium Drugs 0.000 claims abstract description 4
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 3
- 229960001375 lactose Drugs 0.000 claims abstract description 3
- 239000008101 lactose Substances 0.000 claims abstract description 3
- 239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 3
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 3
- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 3
- 239000000796 flavoring agent Substances 0.000 claims description 35
- 235000013355 food flavoring agent Nutrition 0.000 claims description 34
- 238000002156 mixing Methods 0.000 claims description 32
- 239000012071 phase Substances 0.000 claims description 25
- 239000000945 filler Substances 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 14
- 239000007884 disintegrant Substances 0.000 claims description 13
- 239000008384 inner phase Substances 0.000 claims description 13
- 239000000314 lubricant Substances 0.000 claims description 13
- 239000003826 tablet Substances 0.000 claims description 11
- 239000000853 adhesive Substances 0.000 claims description 10
- 230000001070 adhesive effect Effects 0.000 claims description 10
- 239000008187 granular material Substances 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 8
- 238000001694 spray drying Methods 0.000 claims description 8
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 2
- 229960001021 lactose monohydrate Drugs 0.000 claims description 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 2
- 239000002304 perfume Substances 0.000 claims description 2
- 239000000463 material Substances 0.000 abstract description 7
- 239000003814 drug Substances 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 5
- 238000007908 dry granulation Methods 0.000 abstract description 3
- 238000000034 method Methods 0.000 abstract description 3
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 abstract description 2
- 235000015165 citric acid Nutrition 0.000 abstract description 2
- 229940071676 hydroxypropylcellulose Drugs 0.000 abstract description 2
- 229940057948 magnesium stearate Drugs 0.000 abstract description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 abstract 1
- 239000007935 oral tablet Substances 0.000 abstract 1
- 229940096978 oral tablet Drugs 0.000 abstract 1
- 235000013772 propylene glycol Nutrition 0.000 abstract 1
- 239000002245 particle Substances 0.000 description 7
- 230000000052 comparative effect Effects 0.000 description 4
- 239000011230 binding agent Substances 0.000 description 3
- 230000036772 blood pressure Effects 0.000 description 3
- 239000005541 ACE inhibitor Substances 0.000 description 2
- 102000005862 Angiotensin II Human genes 0.000 description 2
- 101800000733 Angiotensin-2 Proteins 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 description 2
- 229950006323 angiotensin ii Drugs 0.000 description 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 208000028185 Angioedema Diseases 0.000 description 1
- 102000008873 Angiotensin II receptor Human genes 0.000 description 1
- 108050000824 Angiotensin II receptor Proteins 0.000 description 1
- 101800004538 Bradykinin Proteins 0.000 description 1
- 102400000967 Bradykinin Human genes 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 description 1
- 208000025047 Non-histaminic angioedema Diseases 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 description 1
- 229940126317 angiotensin II receptor antagonist Drugs 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000003276 anti-hypertensive effect Effects 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 229940127088 antihypertensive drug Drugs 0.000 description 1
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 description 1
- 230000000537 coughlike effect Effects 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 208000017574 dry cough Diseases 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000004880 explosion Methods 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 239000002085 irritant Substances 0.000 description 1
- 231100000021 irritant Toxicity 0.000 description 1
- 210000000867 larynx Anatomy 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 239000008385 outer phase Substances 0.000 description 1
- 210000003800 pharynx Anatomy 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the technical field of medicines, and particularly relates to a valsartan orally disintegrating tablet and a preparation method thereof. The valsartan orally disintegrating tablet of the invention is an orally rapidly disintegrating preparation. The formula contains 20-38.10% of valsartan, and the balance of auxiliary materials, wherein the auxiliary materials comprise hydroxypropyl cellulose, microcrystalline cellulose, crospovidone, saccharin sodium, colloidal silicon dioxide, magnesium stearate, lactose, aspartame, citric acid, spice, propylene glycol and the like. The valsartan orally disintegrating tablet provided by the invention adopts a dry granulation process, overcomes the hygroscopicity and viscosity of valsartan, improves the compressibility and fluidity of the material, and improves the stability of the valsartan orally disintegrating tablet. Compared with other conventional oral preparations, the oral tablet prepared by the invention has the characteristics of convenient taking, rapid disintegration, good taste and the like.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to a valsartan orally disintegrating tablet and a preparation method thereof.
Background
20. ACE inhibitors developed in the 80 th century are very effective antihypertensive drugs, but have untoward effects which cannot be overcome, such as non-dose-related irritant dry cough (5-20%), fatal angioneurotic edema of pharynx, larynx, respiratory tract, lung and the like. Valsartan selectively binds AT as a subtype of angiotensin II receptor 1 The receptor, competitively antagonizes angiotensin II as a pressor system at the receptor level. The antihypertensive effect is exerted by antagonizing angiotensin II which is a pressure-increasing system. Has a brand-new blood pressure reducing mechanism and has no effect of promoting the generation of bradykinin and P substances, so that an angiotensin II receptor antagonist can not cause cough like an ACE inhibitor; and hypertensionPatients take valsartan without affecting heart rate when blood pressure drops. Therefore, valsartan is widely applied to the field of hypertension treatment, and brings good news and hope for a large number of patients. The valsartan orally disintegrating tablet shows better blood pressure control rate for treating severe hypertension and reduces adverse reactions. Particularly, the orally disintegrating tablet preparation with high efficiency and high bioavailability provides convenience for the elderly, infants and children or patients with drug swallowing disorder or inconvenient water intake, has good taste, and improves the compliance of the patients in medication. The dry granulation process adopted by the invention is an environment-friendly granulation process, and has the advantages of energy saving, no pollution, no explosion prevention problem of solvent granulation and no environment protection problem of exhaust emission pollution; it omits the drying procedure; saves a large amount of energy and greatly reduces the cost of dry granulation.
Disclosure of Invention
The invention aims to provide an oral solid preparation which can be rapidly disintegrated and released in an oral cavity without drinking water and has good taste and a preparation method thereof. The valsartan oral disintegrating tablet provided by the invention is characterized in that: the percentage proportion of each component is as follows:
valsartan 20 to 38.10 percent
44.9 to 67 percent of filler
10 to 25 percent of disintegrating agent
Adhesive 2~5%
Lubricant 1~3%
3 percent of flavoring agent
In the invention, the disintegrant is one or more of crospovidone, low-substituted hydroxypropyl cellulose, croscarmellose sodium and the like, and preferably is crospovidone.
In the invention, the adhesive is one or more of hydroxypropyl cellulose and hydroxypropyl methylcellulose, and preferably, the hydroxypropyl cellulose is selected.
In the invention, the flavoring agent is selected from saccharin sodium, aspartame, citric acid and spice, and the lubricant is selected from colloidal silicon dioxide and magnesium stearate.
In the present invention, the amount of lactose used cannot exceed 80% of the total amount of filler.
The invention relates to a preparation method of valsartan orally disintegrating tablets, which comprises the following specific steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the inner phase is a part of flavoring agent, filler, adhesive and disintegrating agent;
(2) Granulating the uniformly mixed inner phase obtained in the step (1) in a dry granulator, wherein a screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the external phase comprises the remaining flavoring agent, disintegrant, and glidant and lubricant;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Detailed Description
The invention is further described below by way of examples: the selected auxiliary materials all meet the medicinal requirements, and a large number of tests summarize to obtain results, and the medicament comprises the following components: contains valsartan 20-38.10% and auxiliary materials including hydroxypropyl cellulose, microcrystalline cellulose, crospovidone, saccharin sodium, colloidal silicon dioxide, magnesium stearate, lactose monohydrate, aspartame, citric acid, perfume, propylene glycol, etc. The valsartan orally disintegrating tablet comprises a main drug and auxiliary materials, wherein the auxiliary materials comprise a filling agent, a disintegrating agent, a lubricating agent, an adhesive and a flavoring agent, and the weight percentages of the components are as follows:
example 1
The prescription composition is as follows:
the preparation process comprises the following steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the internal phase is partially corrected
Flavoring agents, fillers, binders, and disintegrants;
(2) Granulating the uniformly mixed inner phase in the step (1) in a dry granulator; wherein the screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the external phase comprises the remaining flavoring agent, disintegrant, and glidant and lubricant;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Example 2
The prescription composition is as follows:
the preparation process comprises the following steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the inner phase is a part of flavoring agent, filler, adhesive and disintegrating agent;
(2) Granulating the uniformly mixed inner phase in the step (1) in a dry granulator; wherein the screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the outer phase includes the remaining flavor, disintegrant, and glidant and lubricant;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Example 3
The prescription composition is as follows:
the preparation process comprises the following steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the internal phase is partially corrected
Flavoring agents, fillers, binders, and disintegrants;
(2) Granulating the uniformly mixed inner phase in the step (1) in a dry granulator; wherein the screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the external phase comprises the remaining flavoring agent, disintegrant, and glidant and lubricant;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Example 4
The prescription composition is as follows:
the preparation process comprises the following steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the internal phase is partially corrected
Flavoring agents, fillers, binders, and disintegrants;
(2) Granulating the uniformly mixed inner phase in the step (1) in a dry granulator; wherein the screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the external phase comprises the rest corrective, disintegrant,
And glidants and lubricants;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Comparative example 1
The prescription composition is as follows:
the preparation process comprises the following steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the inner phase is a part of flavoring agent, filler, adhesive and disintegrating agent;
(2) Granulating the uniformly mixed inner phase in the step (1) in a dry granulator; wherein the screen mesh is 24 meshes;
(3) Spray-drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the external phase comprises the remaining flavoring agent, disintegrant, and glidant and lubricant;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Comparative example 2
The prescription composition is as follows:
the preparation process comprises the following steps:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the inner phase is a part of flavoring agent, filler, adhesive and disintegrating agent;
(2) Granulating the uniformly mixed inner phase in the step (1) in a dry granulator; wherein the screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the particles obtained in (3) with an external phase; the external phase comprises the remaining flavoring agent, disintegrant, and glidant and lubricant;
(5) Finally, the mixture in (4) is tabletted with a 7mm flat die to obtain tablets of the desired hardness.
The disintegration time and the taste of the tablets of the examples and the comparative examples of the invention are examined, and the results are shown in the following table;
test results of valsartan orally disintegrating tablet examples are shown in the table:
as can be seen from the table, examples 1, 2, 3 and 4 had good flowability and compressibility, moderate tablet hardness, short disintegration time and good taste. Comparative examples 1 and 2 had poor flowability and compressibility, slow disintegration time, and poor mouth feel.
Claims (4)
1. The valsartan orally disintegrating tablet is characterized in that: the components have the following weight percentages:
valsartan 20 to 38.10 percent
44.9 to 67 percent of filler
10 to 25 percent of disintegrating agent
Adhesive 2~5%
Lubricant 1~3%
3% of flavoring agent.
2. The valsartan orally disintegrating tablet according to claim 1, characterized in that: the filler is selected from microcrystalline cellulose, lactose monohydrate; the disintegrant is selected from crospovidone, croscarmellose sodium, and low substituted hydroxypropyl cellulose; the adhesive is selected from hydroxypropyl cellulose and hydroxypropyl methyl cellulose; the correctant is selected from saccharin sodium, aspartame, citric acid, and perfume, and the lubricant is selected from colloidal silicon dioxide and magnesium stearate.
3. The valsartan orally disintegrating tablet according to claim 1, characterized in that the amount of lactose does not exceed 80% of the total amount of filler.
4. The preparation method of valsartan orally disintegrating tablets according to claim 1, characterized by the specific steps of:
(1) Mixing valsartan and the internal phase in a three-dimensional mixer for 3min, and uniformly mixing; the inner phase is a part of flavoring agent, filler, adhesive and disintegrating agent;
(2) Granulating the uniformly mixed inner phase obtained in the step (1) in a dry granulator, wherein a screen mesh is 24 meshes;
(3) Spray drying and mixing the granules obtained in the step (2) with a flavoring agent in a multifunctional fluidized bed, wherein the flavoring agent is a spice dissolved in propylene glycol at a certain concentration;
(4) Mixing the granulate obtained in (3) with an external phase comprising the remaining flavouring agents, disintegrants, and glidants and lubricants;
(5) Finally, the mixture in (4) is pressed into tablets with the required hardness by a flat die with the diameter of 7 mm.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110946363.4A CN115707454A (en) | 2021-08-18 | 2021-08-18 | Valsartan orally disintegrating tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110946363.4A CN115707454A (en) | 2021-08-18 | 2021-08-18 | Valsartan orally disintegrating tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN115707454A true CN115707454A (en) | 2023-02-21 |
Family
ID=85212267
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202110946363.4A Pending CN115707454A (en) | 2021-08-18 | 2021-08-18 | Valsartan orally disintegrating tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN115707454A (en) |
-
2021
- 2021-08-18 CN CN202110946363.4A patent/CN115707454A/en active Pending
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