CN113081983A - Lurasidone sublingual tablet and preparation method thereof - Google Patents
Lurasidone sublingual tablet and preparation method thereof Download PDFInfo
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- CN113081983A CN113081983A CN202110419896.7A CN202110419896A CN113081983A CN 113081983 A CN113081983 A CN 113081983A CN 202110419896 A CN202110419896 A CN 202110419896A CN 113081983 A CN113081983 A CN 113081983A
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- lurasidone
- parts
- sublingual tablet
- salt
- sorbitol
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- 229960001432 lurasidone Drugs 0.000 title claims abstract description 43
- PQXKDMSYBGKCJA-CVTJIBDQSA-N lurasidone Chemical compound C1=CC=C2C(N3CCN(CC3)C[C@@H]3CCCC[C@H]3CN3C(=O)[C@@H]4[C@H]5CC[C@H](C5)[C@@H]4C3=O)=NSC2=C1 PQXKDMSYBGKCJA-CVTJIBDQSA-N 0.000 title claims abstract description 43
- 239000006190 sub-lingual tablet Substances 0.000 title claims abstract description 42
- 229940098466 sublingual tablet Drugs 0.000 title claims abstract description 34
- 238000002360 preparation method Methods 0.000 title abstract description 19
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 32
- 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 abstract description 20
- 229930195725 Mannitol Natural products 0.000 claims abstract description 19
- 239000000594 mannitol Substances 0.000 claims abstract description 19
- 235000010355 mannitol Nutrition 0.000 claims abstract description 19
- 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 abstract description 18
- 239000000600 sorbitol Substances 0.000 claims abstract description 18
- 235000010356 sorbitol Nutrition 0.000 claims abstract description 18
- 108010011485 Aspartame Proteins 0.000 claims abstract description 16
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 16
- 239000000605 aspartame Substances 0.000 claims abstract description 16
- 235000010357 aspartame Nutrition 0.000 claims abstract description 16
- 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 16
- 229960003438 aspartame Drugs 0.000 claims abstract description 16
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 16
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 16
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 16
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims abstract description 14
- 229960000913 crospovidone Drugs 0.000 claims abstract description 14
- NEKCRUIRPWNMLK-SCIYSFAVSA-N lurasidone hydrochloride Chemical compound Cl.C1=CC=C2C(N3CCN(CC3)C[C@@H]3CCCC[C@H]3CN3C(=O)[C@@H]4[C@H]5CC[C@H](C5)[C@@H]4C3=O)=NSC2=C1 NEKCRUIRPWNMLK-SCIYSFAVSA-N 0.000 claims abstract description 14
- 229960002863 lurasidone hydrochloride Drugs 0.000 claims abstract description 14
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims abstract description 14
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 239000002994 raw material Substances 0.000 claims abstract description 6
- 239000002245 particle Substances 0.000 claims abstract description 5
- 239000000463 material Substances 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 6
- 239000011812 mixed powder Substances 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- 238000005303 weighing Methods 0.000 claims description 2
- 238000003825 pressing Methods 0.000 claims 1
- 238000004090 dissolution Methods 0.000 abstract description 6
- 239000003814 drug Substances 0.000 abstract description 6
- 238000010521 absorption reaction Methods 0.000 abstract description 4
- 239000012528 membrane Substances 0.000 abstract description 4
- 238000000338 in vitro Methods 0.000 abstract 1
- 239000003826 tablet Substances 0.000 description 8
- 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 description 7
- 210000000214 mouth Anatomy 0.000 description 6
- 229940071676 hydroxypropylcellulose Drugs 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 229960002920 sorbitol Drugs 0.000 description 5
- 229940079593 drug Drugs 0.000 description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 4
- 201000000980 schizophrenia Diseases 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000011156 evaluation Methods 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- 210000004379 membrane Anatomy 0.000 description 3
- 230000003340 mental effect Effects 0.000 description 3
- 210000002200 mouth mucosa Anatomy 0.000 description 3
- 239000008055 phosphate buffer solution Substances 0.000 description 3
- 230000007423 decrease Effects 0.000 description 2
- 230000007547 defect Effects 0.000 description 2
- 208000020016 psychiatric disease Diseases 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 description 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 description 1
- 102000004980 Dopamine D2 Receptors Human genes 0.000 description 1
- 108090001111 Dopamine D2 Receptors Proteins 0.000 description 1
- 208000028017 Psychotic disease Diseases 0.000 description 1
- 208000003443 Unconsciousness Diseases 0.000 description 1
- 230000000561 anti-psychotic effect Effects 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 230000008451 emotion Effects 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 238000009776 industrial production Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 230000008447 perception Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 208000024891 symptom Diseases 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
- A61K9/2004—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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- 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
-
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
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- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
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Abstract
The invention discloses a sublingual tablet containing lurasidone hydrochloride or salt thereof and a preparation method thereof. The sublingual tablet is prepared from the following raw materials in parts by mass: 4-8 parts of lurasidone or salt thereof, 2-6 parts of sorbitol, 4-8 parts of mannitol, 0.5-1.5 parts of crospovidone, 0.1-0.5 part of hydroxypropyl cellulose, 0.1-0.2 part of aspartame and 0.1-0.2 part of magnesium stearate, wherein the particle size range of the lurasidone or salt thereof is 0.1-10 mu m. The sublingual tablet has the advantages of convenient preparation process, high medicine content, high disintegration speed, good permeable membrane absorption, good in-vitro dissolution and mouthfeel, and can provide a preparation containing lurasidone or salt thereof, which is convenient to take, quick to absorb and high in bioavailability for patients.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and particularly relates to a lurasidone sublingual tablet and a preparation method thereof.
Background
Schizophrenia (schizophrenia) is a common mental disease whose etiology is not completely clarified, and the disease mostly occurs in young and old years, and is often disordered in aspects of perception, thinking, emotion, behavior and the like, and is generally disordered in unconsciousness and intelligence. The disease course is prolonged, the disease attacks are repeated, partial patients suffer from mental activity decline and social function defects of different degrees, the mental activity decline accounts for more than half of patients in the psychiatric department, about half of patients finally suffer from mental disabilities, and serious burden is brought to the society, patients and family members.
Lurasidone hydrochloride is a novel antipsychotic drug with dual action developed by the pharmaceutical company Sumitomo, Japan. It has a high affinity for both the 5-HT2A receptor and the dopamine D2 receptor. Has obvious curative effect on positive and negative symptoms of psychosis patient.
Lurasidone (Lurasidone) is a novel atypical anti-schizophrenia drug approved by the Food and Drug Administration (FDA) in 28 u.s.u.s.a.in 2010 for sale under the trade name Latudao.
The structural formula of lurasidone hydrochloride is as follows:
the pKa value of the oral cavity is 1.2, the pH value of the normal oral cavity is 6.6-7.1, and the oral cavity can absorb the medicine without adding a buffering agent.
The lurasidone common tablet has the following defects that the lurasidone common tablet needs to be swallowed by water, the disintegration speed is slow, and the onset time is longer. However, patients with schizophrenia have difficulty in swallowing, have poor compliance, and cannot achieve the effect of drug therapy, so that a novel tablet which can be disintegrated without water in the oral cavity or swallowed and can be absorbed well through a film under the tongue needs to be developed.
Disclosure of Invention
The invention aims to provide a lurasidone sublingual tablet convenient for oral administration. The lurasidone sublingual tablet is simple and convenient to take, can be disintegrated quickly, can be swallowed directly without water, is absorbed quickly, and is convenient for patients with mental diseases to take.
The lurasidone sublingual tablet provided by the invention is prepared from the following raw materials in parts by mass: 4-8 parts of lurasidone or salt thereof, 2-6 parts of sorbitol, 4-8 parts of mannitol, 0.5-1.5 parts of crospovidone, 0.1-0.5 part of hydroxypropyl cellulose, 0.1-0.2 part of aspartame and 0.1-0.2 part of magnesium stearate.
Preferably, the particle size range of the lurasidone or the salt thereof is 0.1-10 mu m.
Preferably, the lurasidone or the salt thereof is lurasidone hydrochloride.
Preferably, sorbitol and crospovidone which are auxiliary materials in the invention are sieved by a 100-mesh sieve before use.
Preferably, the auxiliary material mannitol in the invention is spray-dried mannitol.
Further, the lurasidone sublingual tablet is prepared from the following raw materials in parts by mass: 4 parts of lurasidone hydrochloride, 4 parts of sorbitol, 7.5 parts of mannitol, 1.2 parts of crospovidone, 0.2 part of hydroxypropyl cellulose, 0.1 part of aspartame and 0.1 part of magnesium stearate.
The invention also provides a preparation method of the lurasidone sublingual tablet.
The preparation method of the lurasidone sublingual tablet provided by the invention comprises the following steps:
1) weighing the raw and auxiliary materials according to the mass ratio;
2) and (3) uniformly mixing the lurasidone or the salt thereof with sorbitol, crospovidone and hydroxypropyl cellulose, adding mannitol and aspartame into the obtained mixed powder, uniformly mixing, adding magnesium stearate, and tabletting to obtain the sublingual tablet.
Preferably, the tabletting in the step 2) is powder direct compression.
The sublingual tablet of the invention has the advantages of few auxiliary material types, higher drug content, high disintegration speed and good permeable membrane absorption, and can be effectively used for sublingual administration: in addition, after the raw materials and the auxiliary materials are compatible, special dispersion technology treatment is not needed, so that the forming process is simpler and more convenient, the production cost is lower, and the industrial production is facilitated.
Detailed Description
The present invention will be further illustrated with reference to the following specific examples, but the present invention is not limited to the following examples. The method is a conventional method unless otherwise specified. The starting materials are commercially available from the open literature unless otherwise specified.
Example 1 preparation of Lurasidone Sublingual tablets
[ prescription composition ]
| Components | Dosage is g/1000 tablets |
| Lurasidone hydrochloride | 40 |
| Sorbitol | 20 |
| Spray-dried mannitol | 80 |
| Cross-linked polyvidone | 5 |
| Hydroxypropyl cellulose | 3 |
| Aspartame | 1 |
| Magnesium stearate | 1 |
Wherein the particle size range of the lurasidone hydrochloride is 0.1-1 mu m.
[ PREPARATION METHOD ]
Mixing the lurasidone and sorbitol, crospovidone and hydroxypropyl cellulose which are sieved by a 100-mesh sieve uniformly, adding spray-dried mannitol and aspartame, mixing uniformly, adding magnesium stearate, and tabletting to obtain the sublingual tablet.
Example 2 preparation of Lurasidone Sublingual tablets
[ prescription composition ]
| Components | Dosage is g/1000 tablets |
| Lurasidone hydrochloride | 40 |
| Sorbitol | 40 |
| Spray-dried mannitol | 60 |
| Cross-linked polyvidone | 10 |
| Hydroxypropyl cellulose | 2 |
| Aspartame | 1 |
| Magnesium stearate | 1 |
Wherein the particle size range of the lurasidone hydrochloride is 0.1-1 mu m.
[ PREPARATION METHOD ]
Mixing the lurasidone and sorbitol, crospovidone and hydroxypropyl cellulose which are sieved by a 100-mesh sieve uniformly, adding spray-dried mannitol and aspartame, mixing uniformly, adding magnesium stearate, and tabletting to obtain the sublingual tablet.
Example 3 preparation of Lurasidone Sublingual tablets
[ prescription composition ]
| Components | Dosage is g/1000 tablets |
| Lurasidone hydrochloride | 80 |
| Sorbitol | 20 |
| Mannitol | 80 |
| Cross-linked polyvidone | 15 |
| Hydroxypropyl cellulose | 5 |
| Aspartame | 2 |
| Magnesium stearate | 2 |
[ PREPARATION METHOD ]
Mixing the lurasidone and sorbitol, crospovidone and hydroxypropyl cellulose which are sieved by a 100-mesh sieve uniformly, adding spray-dried mannitol and aspartame, mixing uniformly, adding magnesium stearate, and tabletting to obtain the sublingual tablet.
Example 4 preparation of Lurasidone Sublingual tablets
[ prescription composition ]
[ PREPARATION METHOD ]
Mixing the lurasidone and sorbitol, crospovidone and hydroxypropyl cellulose which are sieved by a 100-mesh sieve uniformly, adding spray-dried mannitol and aspartame, mixing uniformly, adding magnesium stearate, and tabletting to obtain the sublingual tablet.
Example 5 preparation of Lurasidone Sublingual tablets
[ prescription composition ]
| Components | Dosage is g/1000 tablets |
| Lurasidone hydrochloride | 40 |
| Sorbitol | 40 |
| Spray-dried mannitol | 75 |
| Cross-linked polyvidone | 12 |
| Hydroxypropyl cellulose | 2 |
| Aspartame | 1 |
| Magnesium stearate | 1 |
[ PREPARATION METHOD ]
Mixing the lurasidone and sorbitol, crospovidone and hydroxypropyl cellulose which are sieved by a 100-mesh sieve uniformly, adding spray-dried mannitol and aspartame, mixing uniformly, adding magnesium stearate, and tabletting to obtain the sublingual tablet.
EXAMPLE 6 evaluation of the Effect of sublingual tablets
The method for evaluating the mouthfeel and detecting the irritation, disintegration time and dissolution rate of the oral mucosa comprises the following steps:
evaluation of oral mucosa irritation:
the mouth feel test was conducted on 20 volunteer subjects aged 20-25 years, randomly divided into 5 groups of 4 persons, each of 4 lurasidone sublingual tablets of examples 1-5, respectively, randomly taken. The results are shown in Table 1
TABLE 1 evaluation results of oral mucosa irritation of Lurasidone Sublingual tablets
Disintegration time limit:
referring to the general rule of the fourth part of the 'Chinese pharmacopoeia' 2015 edition < 0921: the disintegration time limit detection method > determines the disintegration condition of the lurasidone sublingual tablet:
| group of | Disintegration time (S) | Phenomenon of disintegration |
| Example 1 | 75 | Rapidly disintegrating |
| Example 2 | 98 | Rapidly disintegrating |
| Example 3 | 122 | Rapidly expanding and disintegrating |
| Example 4 | 103 | Rapidly expanding and disintegrating |
| Example 5 | 54 | Rapidly expanding and disintegrating |
Dissolution rate:
adopts the technical proposal that the fourth part <0931 of the 'Chinese pharmacopoeia' 2015 edition: dissolution and release rate measurement method > in the second method, 50rpm/min, dissolution was measured in water, a ph3.8 phosphate buffer solution, a ph4.0 phosphate buffer solution, and a ph6.8 phosphate buffer solution, respectively (n ═ 12).
The test result shows that:
the lurasidone sublingual tablet provided by the invention has the characteristics of high solubility and strong stability through screening, and the absorption percentage of the outer permeable membrane of the lurasidone sublingual tablet is obviously higher than that of a common tablet sold in the market.
In conclusion, the screened sublingual tablet has the advantages of few auxiliary material types, good taste, small stimulation to oral cavity, high disintegration speed and good permeable membrane absorption, and can be effectively used for oral/sublingual administration. The lurasidone sublingual tablet provided by the invention has similar dissolution behavior and effective storage period with the commercially available preparation.
Claims (8)
1. The lurasidone sublingual tablet is prepared from the following raw materials in parts by mass: 4-8 parts of lurasidone or salt thereof, 2-6 parts of sorbitol, 4-8 parts of mannitol, 0.5-1.5 parts of crospovidone, 0.1-0.5 part of hydroxypropyl cellulose, 0.1-0.2 part of aspartame and 0.1-0.2 part of magnesium stearate.
2. The sublingual tablet of claim 1, wherein: the particle size range of the lurasidone or the salt thereof is 0.1-10 mu m.
3. The sublingual tablet according to claim 1 or 2, wherein: the lurasidone or the salt thereof is lurasidone hydrochloride.
4. The sublingual tablet according to any one of claims 1-3, wherein: the sorbitol and the crospovidone are sieved by a 100-mesh sieve before use.
5. The sublingual tablet according to any one of claims 1 to 4, wherein: the mannitol is spray-dried mannitol.
6. The sublingual tablet according to any one of claims 1-5, wherein: the lurasidone sublingual tablet is prepared from the following raw materials in parts by mass: 4 parts of lurasidone hydrochloride, 4 parts of sorbitol, 7.5 parts of mannitol, 1.2 parts of crospovidone, 0.2 part of hydroxypropyl cellulose, 0.1 part of aspartame and 0.1 part of magnesium stearate.
7. A method for preparing the lurasidone sublingual tablet as claimed in any one of claims 1 to 6, comprising the steps of
1) Weighing the raw and auxiliary materials according to the mass ratio of the lurasidone sublingual tablet in any one of claims 1-6;
2) and uniformly mixing the lurasidone hydrochloride, the sorbitol, the crospovidone and the hydroxypropyl cellulose, adding the mannitol and the aspartame into the obtained mixed powder, uniformly mixing, adding the magnesium stearate, and tabletting to obtain the sublingual tablet.
8. The method of claim 7, wherein: in the step 2), the tabletting is powder direct pressing.
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| CN113081983B CN113081983B (en) | 2022-09-06 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023080854A1 (en) * | 2021-11-03 | 2023-05-11 | Santa Farma Ilac Sanayii A.S. | Lurasidone hydrochloride compositions |
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| CN107007565A (en) * | 2017-03-17 | 2017-08-04 | 万全万特制药江苏有限公司 | A kind of Lurasidone HCl oral disintegrating tablet and preparation method thereof |
| CN107137364A (en) * | 2016-03-01 | 2017-09-08 | 天津市汉康医药生物技术有限公司 | A kind of Lurasidone sublingual tablet and its production and use |
| EP3318279A1 (en) * | 2016-11-02 | 2018-05-09 | Sanovel Ilac Sanayi ve Ticaret A.S. | Solid oral pharmaceutical compositions of lurasidone hydrochloride |
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Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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