CN114917195B - Piracetam tablet and preparation method thereof - Google Patents
Piracetam tablet and preparation method thereof Download PDFInfo
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- CN114917195B CN114917195B CN202210660609.6A CN202210660609A CN114917195B CN 114917195 B CN114917195 B CN 114917195B CN 202210660609 A CN202210660609 A CN 202210660609A CN 114917195 B CN114917195 B CN 114917195B
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- piracetam
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- sorbitol
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- GMZVRMREEHBGGF-UHFFFAOYSA-N Piracetam Chemical compound NC(=O)CN1CCCC1=O GMZVRMREEHBGGF-UHFFFAOYSA-N 0.000 title claims abstract description 66
- 229960004526 piracetam Drugs 0.000 title claims abstract description 65
- 238000002360 preparation method Methods 0.000 title claims abstract description 27
- 238000000034 method Methods 0.000 claims abstract description 13
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 30
- 239000000600 sorbitol Substances 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 26
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 22
- 239000011575 calcium Substances 0.000 claims description 22
- 229910052791 calcium Inorganic materials 0.000 claims description 22
- 239000003814 drug Substances 0.000 claims description 22
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 19
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 16
- 239000002245 particle Substances 0.000 claims description 16
- 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 14
- 229940079593 drug Drugs 0.000 claims description 14
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 10
- 239000003085 diluting agent Substances 0.000 claims description 10
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 10
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 10
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 10
- 238000002156 mixing Methods 0.000 claims description 10
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 9
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 9
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 9
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 9
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 8
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 7
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 6
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims description 6
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 6
- 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 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 6
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 6
- 229940069328 povidone Drugs 0.000 claims description 6
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 6
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 6
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 5
- 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 description 5
- 229930195725 Mannitol Natural products 0.000 claims description 5
- 239000008101 lactose Substances 0.000 claims description 5
- 239000000594 mannitol Substances 0.000 claims description 5
- 235000010355 mannitol Nutrition 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 5
- 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 claims description 4
- 229920000881 Modified starch Polymers 0.000 claims description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- 239000000853 adhesive Substances 0.000 claims description 4
- 230000001070 adhesive effect Effects 0.000 claims description 4
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 4
- 235000019359 magnesium stearate Nutrition 0.000 claims description 4
- 239000000741 silica gel Substances 0.000 claims description 4
- 239000011734 sodium Substances 0.000 claims description 4
- 229910052708 sodium Inorganic materials 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 229920001353 Dextrin Polymers 0.000 claims description 3
- 239000004375 Dextrin Substances 0.000 claims description 3
- 235000019425 dextrin Nutrition 0.000 claims description 3
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 3
- 229910002027 silica gel Inorganic materials 0.000 claims description 3
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 3
- 229960002920 sorbitol Drugs 0.000 claims 4
- 229960005069 calcium Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 239000007884 disintegrant Substances 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 229940032147 starch Drugs 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 238000004090 dissolution Methods 0.000 abstract description 17
- 238000004519 manufacturing process Methods 0.000 abstract description 5
- 230000000052 comparative effect Effects 0.000 description 15
- 239000000243 solution Substances 0.000 description 7
- 206010041662 Splinter Diseases 0.000 description 6
- 238000005336 cracking Methods 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 238000005550 wet granulation Methods 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 210000004556 brain Anatomy 0.000 description 3
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 3
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 230000003925 brain function Effects 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 238000011835 investigation Methods 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 208000007125 Neurotoxicity Syndromes Diseases 0.000 description 1
- 231100000076 Toxic encephalopathy Toxicity 0.000 description 1
- 208000030886 Traumatic Brain injury Diseases 0.000 description 1
- 238000005299 abrasion Methods 0.000 description 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 1
- 229960004373 acetylcholine Drugs 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000005978 brain dysfunction Effects 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical class NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 229910021487 silica fume Inorganic materials 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Psychiatry (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a piracetam tablet and a preparation method thereof. The piracetam tablet obtained by the invention has better friability and dissolution, in particular to better initial dissolution, and the process of the piracetam tablet in the preparation process is smooth, so that the quality of the obtained product meets the standard requirement, the safety and the effectiveness of taking by patients are ensured, and the piracetam tablet is suitable for industrial mass production.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a piracetam tablet and a preparation method thereof.
Background
Piracetam tablet (Naofukang tablet) is clinically used for treating hypomnesis and light and moderate brain dysfunction caused by various reasons such as acute and chronic cerebrovascular diseases, brain trauma, various toxic encephalopathies and the like, and can also be used for treating intelligent hypoevolutism and the like of children. Piracetam is a brain metabolism improving drug, belonging to the ring-shaped derivative of gamma-aminobutyric acid. Has effects in resisting brain function injury caused by physical and chemical factors. Can promote the conversion of ADP in brain into ATP, promote the synthesis of acetylcholine and enhance the conduction of nerve excitation, and promote the metabolism in brain. Can resist brain function injury caused by physical and chemical factors.
Currently, the preparation types of piracetam include tablets, capsules, injections, freeze-dried powder injections and the like. The injection and the freeze-dried powder injection need medical staff to perform injection, and patients are inconvenient to use at home, and the clinical popularization of injection preparations is further limited. Compared with the piracetam tablet, the piracetam tablet has great advantages in clinical application. However, the content of the main drug in the piracetam tablet is large, and due to the poor compressibility of the piracetam bulk drug, phenomena such as cracking and the like often occur in the tabletting process, and the friability of the piracetam tablet is close to the upper limit of the standard, so that certain difficulty is brought to the production operation, the production quality is threatened, and the product quality is possibly disqualified if the product quality is slightly wrong.
CN111297818a discloses a high drug-loading piracetam tablet composition and a preparation method thereof, which adopts 10% -20% of high-forming microcrystalline Cellulose (CEOLUSTM) and other auxiliary materials to prepare the high drug-loading piracetam tablet, changes the compressibility of the materials, and ensures that the prepared tablet has lower friability and better hardness. However, the inventors have found that even if the compressibility is improved, the dissolution rate of the drug is inevitably reduced, and the drug efficacy is affected.
Therefore, further studies on piracetam tablets are needed to obtain a piracetam tablet with good compressibility and stable dissolution.
Disclosure of Invention
In view of the above, the invention provides a piracetam tablet, which aims to solve the problem of poor friability of the tablet caused by poor compressibility of piracetam and reduce the occurrence of cracking in the tabletting process. The piracetam tablet obtained by the invention has better friability and dissolution, in particular to the piracetam tablet which has better initial dissolution. In addition, the piracetam tablet disclosed by the invention is smooth in process in the preparation process, the quality of the obtained product meets the standard requirement, the safety and effectiveness of taking by patients are ensured, and the piracetam tablet is suitable for industrial mass production.
The invention provides a piracetam tablet, which specifically comprises piracetam, sorbitol, calcium hydrophosphate, a diluent, a disintegrating agent and a binder.
In the piracetam tablet, the problem of compressibility of the piracetam can be effectively solved by adding sorbitol and calcium hydrophosphate into the prescription, and the preparation process and the dissolution rate of the piracetam tablet can achieve satisfactory effects.
In the piracetam tablet, the mass dosage ratio of the sorbitol to the calcium hydrophosphate is 1:1-3.5.
The study on the dosage of sorbitol and calcium hydrophosphate shows that when the mass dosage ratio of sorbitol to calcium hydrophosphate is 1:1-3.5, the piracetam tablet can better meet the requirements of compression formability, preparation process and dissolution, not only ensures the dissolution of the piracetam tablet, but also can realize a smooth preparation process, and the product with qualified quality is obtained.
In the piracetam tablet, the diluent is one or more of microcrystalline cellulose, lactose, mannitol, pregelatinized starch and dextrin.
In the piracetam tablet, the disintegrating agent is one or more of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, crosslinked povidone and crosslinked sodium carboxymethyl cellulose.
In the piracetam tablet, the binder is one or more of hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose and povidone.
In the piracetam tablet, the dosage of each component is as follows in parts by mass: 200-400 parts of piracetam, 6-10 parts of sorbitol, 6-25 parts of calcium hydrophosphate, 35-70 parts of diluent, 5-15 parts of disintegrating agent and 5-15 parts of adhesive.
The piracetam tablet also comprises a lubricant. Further, the lubricant is one or more of talcum powder, magnesium stearate, sodium stearyl fumarate and micro silica gel.
The invention also provides a preparation method of the piracetam tablet, which comprises the following steps:
a. uniformly mixing piracetam, sorbitol, calcium hydrophosphate, diluent and disintegrating agent to prepare a mixture;
b. c, granulating the mixture obtained in the step a by a wet method by using an ethanol solution containing a binder to obtain drug particles;
c. tabletting the drug particles of step b.
The preparation method of the piracetam tablet comprises the steps a and/or c and the step of adding a lubricant.
Compared with the prior art, the invention has the beneficial effects that:
1. The invention can well solve the problem of poor piracetam compressibility by adding sorbitol and calcium hydrophosphate, reduce the phenomena of cracking and the like in the tabletting process, and ensure that the obtained tablet has good friability.
2. The invention not only solves the problem of poor piracetam compressibility, but also can realize good dissolution, in particular to have better initial dissolution, so that the obtained piracetam tablet can realize quick dissolution, smooth preparation process and good friability effect simultaneously, and ensures the product quality and curative effect by adding sorbitol and calcium hydrophosphate and matching with diluents, disintegrating agents and binders in the prescription of the piracetam tablet.
Detailed Description
Example 1
| Composition of the composition | Dosage (g) |
| Piracetam | 400 |
| Sorbitol | 8 |
| Dibasic calcium phosphate | 10 |
| Microcrystalline cellulose | 40 |
| Croscarmellose sodium | 7 |
| Hydroxypropyl cellulose | 8 |
The preparation method comprises the following steps:
a. uniformly mixing piracetam, sorbitol, calcium hydrophosphate, microcrystalline cellulose and croscarmellose sodium to prepare a mixture;
b. c, carrying out wet granulation on the mixture obtained in the step a by using an ethanol solution containing hydroxypropyl cellulose to obtain medicine particles;
c. tabletting the drug particles of step b.
Example 2
| Composition of the composition | Dosage (g) |
| Piracetam | 400 |
| Sorbitol | 6 |
| Dibasic calcium phosphate | 15 |
| Lactose and lactose | 45 |
| Low substituted hydroxypropyl cellulose | 10 |
| Sodium carboxymethyl cellulose | 8 |
The preparation method comprises the following steps:
a. uniformly mixing piracetam, sorbitol, calcium hydrophosphate, lactose and low-substituted hydroxypropyl cellulose to prepare a mixture;
b. c, carrying out wet granulation on the mixture obtained in the step a by using an ethanol solution containing sodium carboxymethyl cellulose to obtain medicine particles;
c. tabletting the drug particles of step b.
Example 3
| Composition of the composition | Dosage (g) |
| Piracetam | 400 |
| Sorbitol | 10 |
| Dibasic calcium phosphate | 10 |
| Pregelatinized starch | 35 |
| Crosslinked povidone | 5 |
| Hydroxypropyl methylcellulose | 6 |
The preparation method comprises the following steps:
a. uniformly mixing piracetam, sorbitol, calcium hydrophosphate, pregelatinized starch and crosslinked povidone to prepare a mixture;
b. c, carrying out wet granulation on the mixture obtained in the step a by using an ethanol solution containing hydroxypropyl methyl cellulose to obtain medicine particles;
c. tabletting the drug particles of step b.
Example 4
The preparation method comprises the following steps:
a. Uniformly mixing piracetam, sorbitol, calcium hydrophosphate, microcrystalline cellulose, dextrin and croscarmellose sodium to prepare a mixture;
b. c, carrying out wet granulation on the mixture obtained in the step a by using an ethanol solution containing povidone to obtain drug particles;
c. And d, adding sodium stearyl fumarate into the medicine particles in the step b, uniformly mixing, and tabletting.
Example 5
| Composition of the composition | Dosage (g) |
| Piracetam | 400 |
| Sorbitol | 5 |
| Dibasic calcium phosphate | 17.5 |
| Microcrystalline cellulose | 50 |
| Croscarmellose sodium | 4 |
| Sodium carboxymethyl starch | 4 |
| Hydroxypropyl cellulose | 7 |
| Magnesium stearate | 2 |
The preparation method comprises the following steps:
a. uniformly mixing piracetam, sorbitol, calcium hydrophosphate, microcrystalline cellulose, croscarmellose sodium, sodium carboxymethyl starch and magnesium stearate to prepare a mixture;
b. c, carrying out wet granulation on the mixture obtained in the step a by using an ethanol solution containing hydroxypropyl cellulose to obtain medicine particles;
c. tabletting the drug particles of step b.
Example 6
| Composition of the composition | Dosage (g) |
| Piracetam | 400 |
| Sorbitol | 8 |
| Dibasic calcium phosphate | 25 |
| Microcrystalline cellulose | 65 |
| Mannitol (mannitol) | 5 |
| Croscarmellose sodium | 8 |
| Sodium carboxymethyl cellulose | 7 |
| Hydroxypropyl methylcellulose | 15 |
| Micro powder silica gel | 2 |
| Talc powder | 2 |
The preparation method comprises the following steps:
a. Uniformly mixing piracetam, sorbitol, calcium hydrophosphate, microcrystalline cellulose, mannitol, croscarmellose sodium and micro powder silica gel to prepare a mixture;
b. C, carrying out wet granulation on the mixture obtained in the step a by using an ethanol solution containing sodium carboxymethyl cellulose and hydroxypropyl methyl cellulose to obtain medicine particles;
c. And d, adding talcum powder into the medicine particles in the step b, uniformly mixing, and tabletting.
Comparative example
The preparation method is the same as in example 1.
Investigation of Process smoothness
The processes in the preparation of examples 1 to 6 and comparative examples 1 to 6 were examined for smoothness and friability of the resulting tablets. The method comprises the following steps:
| Examples | Whether the process is smooth | Friability (%) |
| 1 | Is that | 0.14 |
| 2 | Is that | 0.17 |
| 3 | Is that | 0.18 |
| 4 | Is that | 0.20 |
| 5 | Is that | 0.13 |
| 6 | Is that | 0.22 |
| Comparative example 1 | If not, there is a splinter phenomenon | 0.91 |
| Comparative example 2 | If not, there is a splinter phenomenon | 0.87 |
| Comparative example 3 | If not, there is a splinter phenomenon | 1.34 |
| Comparative example 4 | If not, there is a splinter phenomenon | 0.98 |
| Comparative example 5 | If not, there is a splinter phenomenon | 0.75 |
| Comparative example 6 | If not, there is a splinter phenomenon | 0.72 |
Examination of the preparation processes of the above examples 1-6 and comparative examples 1-6 shows that the preparation process is smooth after sorbitol and calcium hydrophosphate are added in the examples of the invention, and no cracking phenomenon occurs, and the obtained tablet has good friability of between 0.13 and 0.22 percent, meets the standards of Chinese pharmacopoeia (the friability is less than 1 percent specified by the standards), is not easy to occur, has cracking, edge abrasion and other phenomena in the transportation process, and is suitable for industrialized mass production. And the formulas of the comparative examples 1-4 do not contain sorbitol and calcium hydrophosphate at the same time, and when the mass ratio of the sorbitol to the calcium hydrophosphate in the formulas of the comparative examples 5-6 is not 1:1-3.5, the tablet has the cracking phenomenon in the preparation process, and the friability of the obtained tablet does not meet the requirements or meets the requirements of medicine quality at the upper limit of the standard stipulated in Chinese pharmacopoeia.
Dissolution investigation
Samples prepared in examples 1 to 6 and comparative examples 1 to 6 were taken, phosphate buffer solution of pH6.8 was used as a dissolution medium, and dissolution was carried out at 50 rpm according to a dissolution rate measurement method (second method of appendix X C of 2010 edition of Chinese pharmacopoeia) and at 5, 10, 15, 20, 30 and 45min, and the following experimental results were obtained:
From the experimental results, the dissolution rate of piracetam can be improved by adding the sorbitol and the calcium hydrophosphate to be matched with the diluent, the disintegrating agent and the adhesive. In contrast, in comparative examples 1 to 3, sorbitol and calcium hydrogen phosphate were not added at the same time, and in comparative example 4, calcium phosphate was used instead of calcium hydrogen phosphate, and in comparative examples 5 to 6, the mass ratio of sorbitol to calcium hydrogen phosphate was not 1:1 to 3.5, the dissolution effect of the prepared samples was poor.
Claims (4)
1. A piracetam tablet, comprising piracetam, sorbitol, dibasic calcium phosphate, diluent, disintegrant and binder; the diluent is one or more of microcrystalline cellulose, lactose, mannitol, pregelatinized starch and dextrin; the disintegrating agent is one or more of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, crospovidone and croscarmellose sodium; the adhesive is one or more of hydroxypropyl cellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose and povidone; the weight portions of the components are as follows: 200-400 parts of piracetam, 6-10 parts of sorbitol, 6-25 parts of calcium hydrophosphate, 35-70 parts of diluent, 5-15 parts of disintegrating agent and 5-15 parts of adhesive; the mass dosage ratio of the sorbitol to the calcium hydrophosphate is 1:1-3.5; the preparation method of the tablet comprises the following steps: uniformly mixing piracetam, sorbitol, calcium hydrophosphate, diluent and disintegrating agent to prepare a mixture; b, granulating the mixture obtained in the step a by a wet method by using an ethanol solution containing a binder to obtain drug particles; tabletting the drug particles in the step b.
2. The piracetam tablet according to claim 1, characterized in that the tablet further comprises a lubricant.
3. The piracetam tablet according to claim 2, characterized in that the lubricant is one or more of talc, magnesium stearate, sodium stearyl fumarate, micro-powder silica gel.
4. The piracetam tablet according to claim 1, characterized in that step a and/or step c further comprises the step of adding a lubricant.
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| CN111297818A (en) * | 2020-04-02 | 2020-06-19 | 常州制药厂有限公司 | High-drug-loading-capacity piracetam tablet composition and preparation method thereof |
| JP2021134168A (en) * | 2020-02-27 | 2021-09-13 | 日新製薬株式会社 | Solid preparation and method for producing the same |
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| ES2380010T3 (en) * | 2007-10-16 | 2012-05-07 | Pharmathen S.A. | Enhanced pharmaceutical composition containing an anticonvulsant derived from pyrrolidone and method for its preparation |
| US8551529B2 (en) * | 2009-07-10 | 2013-10-08 | Merck Patent Gmbh | Composition for the production of tablets, and method for the production of said composition |
| WO2011003602A2 (en) * | 2009-07-10 | 2011-01-13 | Merck Patent Gmbh | Tableting agent having a low water content, and method for the production thereof |
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| CN111297818A (en) * | 2020-04-02 | 2020-06-19 | 常州制药厂有限公司 | High-drug-loading-capacity piracetam tablet composition and preparation method thereof |
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