CN114917194A - Miazeping tablet raw material medicine, preparation and preparation method thereof - Google Patents
Miazeping tablet raw material medicine, preparation and preparation method thereof Download PDFInfo
- Publication number
- CN114917194A CN114917194A CN202210473658.9A CN202210473658A CN114917194A CN 114917194 A CN114917194 A CN 114917194A CN 202210473658 A CN202210473658 A CN 202210473658A CN 114917194 A CN114917194 A CN 114917194A
- Authority
- CN
- China
- Prior art keywords
- mirtazapine
- tablet
- mannitol
- malic acid
- crospovidone
- 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.)
- Pending
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- 239000003814 drug Substances 0.000 title claims abstract description 43
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 239000002994 raw material Substances 0.000 title claims description 36
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims abstract description 45
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims abstract description 45
- 239000001630 malic acid Substances 0.000 claims abstract description 45
- 235000011090 malic acid Nutrition 0.000 claims abstract description 45
- 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 41
- 229930195725 Mannitol Natural products 0.000 claims abstract description 41
- 239000000594 mannitol Substances 0.000 claims abstract description 41
- 235000010355 mannitol Nutrition 0.000 claims abstract description 41
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims abstract description 35
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims abstract description 35
- RONZAEMNMFQXRA-UHFFFAOYSA-N mirtazapine Chemical compound C1C2=CC=CN=C2N2CCN(C)CC2C2=CC=CC=C21 RONZAEMNMFQXRA-UHFFFAOYSA-N 0.000 claims abstract description 33
- 229960001785 mirtazapine Drugs 0.000 claims abstract description 33
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims abstract description 30
- 229960000913 crospovidone Drugs 0.000 claims abstract description 30
- 239000004375 Dextrin Substances 0.000 claims abstract description 28
- 229920001353 Dextrin Polymers 0.000 claims abstract description 28
- 235000019425 dextrin Nutrition 0.000 claims abstract description 28
- 229920000881 Modified starch Polymers 0.000 claims abstract description 26
- 239000000203 mixture Substances 0.000 claims abstract description 26
- 229940079593 drug Drugs 0.000 claims abstract description 24
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 24
- 239000000314 lubricant Substances 0.000 claims abstract description 22
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 18
- 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 abstract description 16
- 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 16
- 239000008101 lactose Substances 0.000 claims abstract description 16
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 15
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims abstract description 11
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 10
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 10
- 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 abstract description 10
- 229920000609 methyl cellulose Polymers 0.000 claims abstract description 10
- 239000001923 methylcellulose Substances 0.000 claims abstract description 10
- 235000010981 methylcellulose Nutrition 0.000 claims abstract description 10
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 9
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims abstract description 4
- 235000013539 calcium stearate Nutrition 0.000 claims abstract description 4
- 239000008116 calcium stearate Substances 0.000 claims abstract description 4
- 239000000741 silica gel Substances 0.000 claims abstract description 4
- 229910002027 silica gel Inorganic materials 0.000 claims abstract description 4
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims abstract description 4
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 3
- 238000002156 mixing Methods 0.000 claims description 19
- 239000000796 flavoring agent Substances 0.000 claims description 12
- 235000013355 food flavoring agent Nutrition 0.000 claims description 12
- 235000003599 food sweetener Nutrition 0.000 claims description 12
- 239000003765 sweetening agent Substances 0.000 claims description 12
- 238000003756 stirring Methods 0.000 claims description 9
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 7
- 238000007873 sieving Methods 0.000 claims description 7
- 239000004615 ingredient Substances 0.000 claims description 5
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 claims description 5
- 229940088679 drug related substance Drugs 0.000 claims 6
- 239000008186 active pharmaceutical agent Substances 0.000 claims 5
- 238000009472 formulation Methods 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 abstract description 23
- 238000010521 absorption reaction Methods 0.000 abstract description 12
- 239000002253 acid Substances 0.000 abstract description 7
- 230000001154 acute effect Effects 0.000 abstract description 3
- 206010040007 Sense of oppression Diseases 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 description 23
- 241000220225 Malus Species 0.000 description 21
- 235000021016 apples Nutrition 0.000 description 18
- 230000000694 effects Effects 0.000 description 18
- 239000003205 fragrance Substances 0.000 description 16
- 230000009286 beneficial effect Effects 0.000 description 11
- 210000004556 brain Anatomy 0.000 description 10
- 239000003795 chemical substances by application Substances 0.000 description 10
- 239000003085 diluting agent Substances 0.000 description 10
- 238000000034 method Methods 0.000 description 10
- 239000000243 solution Substances 0.000 description 9
- 206010019233 Headaches Diseases 0.000 description 5
- 239000003153 chemical reaction reagent Substances 0.000 description 5
- 239000010419 fine particle Substances 0.000 description 5
- 231100000869 headache Toxicity 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 210000003205 muscle Anatomy 0.000 description 5
- 239000002245 particle Substances 0.000 description 5
- 239000000546 pharmaceutical excipient Substances 0.000 description 5
- 230000002040 relaxant effect Effects 0.000 description 5
- 239000007787 solid Substances 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 4
- 235000005979 Citrus limon Nutrition 0.000 description 2
- 244000131522 Citrus pyriformis Species 0.000 description 2
- 239000004376 Sucralose Substances 0.000 description 2
- 230000000903 blocking effect Effects 0.000 description 2
- 238000007922 dissolution test Methods 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 235000019204 saccharin Nutrition 0.000 description 2
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 2
- 229940081974 saccharin Drugs 0.000 description 2
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 2
- 239000007909 solid dosage form Substances 0.000 description 2
- 235000019408 sucralose Nutrition 0.000 description 2
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical group O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 2
- 102000056834 5-HT2 Serotonin Receptors Human genes 0.000 description 1
- 108091005479 5-HT2 receptors Proteins 0.000 description 1
- 102000035037 5-HT3 receptors Human genes 0.000 description 1
- 108091005477 5-HT3 receptors Proteins 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 208000007415 Anhedonia Diseases 0.000 description 1
- UDIPTWFVPPPURJ-UHFFFAOYSA-M Cyclamate Chemical group [Na+].[O-]S(=O)(=O)NC1CCCCC1 UDIPTWFVPPPURJ-UHFFFAOYSA-M 0.000 description 1
- 102000014630 G protein-coupled serotonin receptor activity proteins Human genes 0.000 description 1
- 239000003929 acidic solution Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000001800 adrenalinergic effect Effects 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 210000000748 cardiovascular system Anatomy 0.000 description 1
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 230000007830 nerve conduction Effects 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 230000003518 presynaptic effect Effects 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 229960001462 sodium cyclamate Drugs 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 230000004580 weight loss Effects 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61K9/2068—Compounds of unknown constitution, e.g. material from plants or animals
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/24—Antidepressants
Abstract
The invention provides a mirtazapine bulk drug, a preparation and a preparation method thereof, belonging to the technical field of mirtazapine drugs, wherein mannitol, malic acid, crospovidone and dextrin are added into the bulk drug, and the bulk drug comprises mirtazapine, lactose, mannitol, malic acid, water-soluble components, crospovidone, pregelatinized starch, a lubricant and dextrin; the lubricant is magnesium stearate, calcium stearate, sodium stearate, silica gel, colloidal silicon dioxide or the combination of the magnesium stearate, the calcium stearate, the sodium stearate, the silica gel and the colloidal silicon dioxide; the water-soluble component adopts hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose or the combination thereof; can play and alleviate patient's head confusion and oppression sense, the cubic or slice malic acid can be dissolved in water fast after getting into the stomach in addition, forms weak acid environment, can dissolve mannitol and other mixtures fast, and the human absorption of being convenient for can realize quick by the human absorption, helps the acute patient of quality.
Description
Technical Field
The invention relates to the technical field of mirtazapine medicines, and in particular relates to a mirtazapine bulk drug, a preparation and a preparation method thereof.
Background
Mirtazapine, an active ingredient of mirtazapine, acts as a centrally acting presynaptic alpha 2 receptor antagonist, in combination with potentiating adrenergic nerve conduction; it functions to modulate 5-hydroxytryptamine by interacting with the central 5-hydroxytryptamine receptor (5-HT2, 5-HT 3); both enantiomers of mirtazapine have antidepressant activity, the levorotatory form blocking the alpha 2 and 5-HT2 receptors and the dextrorotatory form blocking the 5-HT3 receptor; the anti-histamine receptor (H1) properties of mirtazapine act as a sedative; the composition has good tolerance, almost no anticholinergic effect, and therapeutic dose has no influence on cardiovascular system, and can be used for treating symptoms such as anhedonia, psychomotor inhibition, sleep disorder and weight loss.
The mirtazapine is usually prepared into a medicine which is orally administered in the form of a conventional tablet, pill or capsule, but the tablet or pill is long in absorption time of a patient, and needs to exert a drug effect urgently when the special mood of a depression patient is difficult to control, so that a drug composition is highly expected to have quick and continuous onset time, continuous activity and good bioavailability.
Disclosure of Invention
Aiming at the problems in the prior art, the invention provides a Miazepint bulk drug, a preparation and a preparation method thereof. The invention has fragrant smell, rapid decomposition and absorption and good adaptability to acute patients.
The technical scheme of the invention is as follows:
a raw material medicine of the Miazepin tablet is added with mannitol, malic acid, crospovidone and dextrin.
Preferably, the bulk drug comprises mirtazapine, lactose, mannitol, malic acid, water-soluble components, crospovidone, pregelatinized starch, a lubricant, and dextrin.
Preferably, the lubricant employs magnesium stearate, calcium stearate, sodium stearate, silica gel, colloidal silicon dioxide, or a combination thereof.
Preferably, the water-soluble component employs hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, or a combination thereof.
Preferably, the raw material medicine comprises the following components in parts by weight:
preferably, the raw material medicine comprises the following components in parts by weight:
sweetening agents and flavoring agents are added into the raw material medicines.
A preparation method of a Miazepini tablet raw material medicine mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, crospovidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1, then mixing the mixture with mirtazapine and mannitol again, adding the crospovidone after 10-15 minutes, adding the colloidal silicon dioxide after 18-20 minutes, and continuing to mix for 10-13 minutes;
s3, tabletting the mixture finally mixed in the S2 by using a tabletting machine.
Preferably, a drum mixer is used for stirring and mixing the raw materials in the step S2.
The raw material medicaments of the preparation component comprise mirtazapine, lactose, mannitol, malic acid, a water-soluble component, crospovidone, pregelatinized starch, a lubricant and dextrin.
The beneficial technical effects of the invention are as follows:
the mixture of mannitol and malic acid can be quickly dissolved in water and decomposed when entering the stomach, so that the quick absorption by the body is facilitated, the malic acid naturally emits the fragrance of apples, the disordered and oppressive feeling of the head of a patient can be relieved, in addition, the blocky or flaky malic acid can be quickly dissolved in water after entering the stomach, a weak acid environment is formed, the mannitol and other mixtures can be quickly dissolved, the absorption by the human body is facilitated, the quick absorption by the human body can be realized, and the acute attack patient is facilitated.
Detailed Description
The present invention is described in detail below. It should be apparent that the described embodiments are only some embodiments of the present invention, and not all embodiments. All other embodiments, which can be obtained by a person skilled in the art without making any creative effort based on the embodiments in the present invention, belong to the protection scope of the present invention.
Example 1:
a Miazepin tablet is prepared by adding mannitol, malic acid, crospovidone, dextrin, mirtazapine, lactose, mannitol, malic acid, water-soluble component, crospovidone, pregelatinized starch, lubricant, and dextrin into raw materials.
Dextrin and mannitol can be used as excipient of tablets, mannitol can also be used as diluent of medicines and solid and liquid, can be rapidly dissolved in water and decomposed when entering the stomach, is beneficial to rapid absorption of the body, malic acid naturally emits the fragrance of apples, the fragrance of apples enables the body of a person to relax, the effect of relaxing the patient can be achieved when the fragrance of apples is transmitted to the brain nervous system, the disordered and the oppressive feeling of the head and the brain of the patient can be relieved, the taste of apples can relieve the headache of a subject, the muscle of the head and the neck of the person can be relaxed, the pressure can be relieved, and the effect of refreshing and restoring consciousness can be achieved; in addition, the malic acid block or tablet can be quickly dissolved in water after entering the stomach to form a weak acid environment, and can quickly dissolve mannitol and other mixtures, so that the malic acid block or tablet can be conveniently absorbed by a human body; the crospovidone is insoluble in water and common reagents, can be quickly sorted in the stomach environment of a malic acid solution, improves the release speed of the effective ingredients of the tablet, and is added with some lubricants when being mixed for use, so that the surface of the tablet is ensured to be smooth and the particle friction is reduced in the tabletting process; the pregelatinized starch is beneficial to tablet forming, a diluent and a disintegrating agent in the tabletting process, has a self-lubricating effect, and is added with magnesium stearate as a lubricant when being combined with other auxiliary materials, and the pregelatinized starch combined with the malic acid acidic solution can be used as the disintegrating agent and can be rapidly cracked into fine particles in the stomach, so that functional components are rapidly dissolved and absorbed;
the raw material medicaments comprise the following components in parts by weight:
in specific implementation, in order to improve the edible mouthfeel and taste, a sweetening agent and a flavoring agent are added into the raw material medicines.
The sweetener can be sucralose, and the flavoring agent can be orange water.
A preparation method of a Miazepini tablet raw material medicine mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, polyvinylpolypyrrolidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1 by using a roller stirrer, then mixing the mixture with mirtazapine and mannitol again, adding the crospovidone after 13 minutes, adding the colloidal silicon dioxide after 20 minutes, and continuing to mix for 13 minutes;
s3, tabletting and forming the mixture after the final mixing in the S2 by using a tabletting machine.
Example 2:
a Miazepin tablet is prepared by adding mannitol, malic acid, crospovidone, dextrin, mirtazapine, lactose, mannitol, malic acid, water-soluble component, crospovidone, pregelatinized starch, lubricant, and dextrin into raw materials.
Dextrin and mannitol can be used as excipients of tablets, mannitol can also be used as diluents of medicines and solid and liquid, can be quickly dissolved in water and decomposed when entering the stomach, is beneficial to quick absorption of the body, malic acid naturally emits the fragrance of apples, the fragrance of apples enables the body of a person to relax, the effect of relaxing patients can be achieved when the apple fragrance is transmitted to the brain nervous system, the disordered and oppressive feeling of the brains of the patients can be relieved, the taste of apples can relieve the headache of a subject, the muscles of the head and the neck of the person can be relaxed, the pressure can be relieved, and the effect of refreshing and restoring consciousness can be achieved; in addition, the malic acid block or tablet can be quickly dissolved in water after entering the stomach to form a weak acid environment, and can quickly dissolve mannitol and other mixtures, so that the malic acid block or tablet can be conveniently absorbed by a human body; the crospovidone is insoluble in water and common reagents, can be quickly sorted in the stomach environment of a malic acid solution, improves the release speed of the effective ingredients of the tablet, and is added with some lubricants when being mixed for use, so that the surface of the tablet is ensured to be smooth and the particle friction is reduced in the tabletting process; the pregelatinized starch is beneficial to tablet forming, a diluent and a disintegrating agent in the tabletting process, has self-lubricating effect, and is added with magnesium stearate as a lubricant when being combined with other auxiliary materials, and the pregelatinized starch combined with the malic acid solution can be used as the disintegrating agent and can be rapidly cracked into fine particles in the stomach, so that functional components are rapidly dissolved and absorbed;
the raw material medicaments comprise the following components in parts by weight:
in specific implementation, in order to improve the edible mouthfeel and taste, a sweetening agent and a flavoring agent are added into the raw material medicines.
The sweetener can be sodium cyclamate, and the flavoring agent can be orange water.
A preparation method of a Miazepini tablet raw material medicine mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, polyvinylpolypyrrolidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1 by using a drum stirrer, then mixing the mixture with mirtazapine and mannitol again, adding the crospovidone after 12 minutes, adding the colloidal silicon dioxide after 19 minutes and continuing to mix for 11 minutes;
s3, tabletting and forming the mixture after the final mixing in the S2 by using a tabletting machine.
Example 3:
a Miazepin tablet is prepared from mannitol, malic acid, polyvinylpolypyrrolidone, dextrin, mirtazapine, lactose, mannitol, malic acid, water-soluble component, polyvinylpolypyrrolidone, pregelatinized starch, lubricant, and dextrin.
Dextrin and mannitol can be used as excipient of tablets, mannitol can also be used as diluent of medicines and solid and liquid, can be rapidly dissolved in water and decomposed when entering the stomach, is beneficial to rapid absorption of the body, malic acid naturally emits the fragrance of apples, the fragrance of apples enables the body of a person to relax, the effect of relaxing the patient can be achieved when the fragrance of apples is transmitted to the brain nervous system, the disordered and the oppressive feeling of the head and the brain of the patient can be relieved, the taste of apples can relieve the headache of a subject, the muscle of the head and the neck of the person can be relaxed, the pressure can be relieved, and the effect of refreshing and restoring consciousness can be achieved; in addition, the malic acid block or tablet can be quickly dissolved in water after entering the stomach to form a weak acid environment, and can quickly dissolve mannitol and other mixtures, so that the malic acid block or tablet can be conveniently absorbed by a human body; the crospovidone is insoluble in water and common reagents, can be quickly sorted in the stomach environment of a malic acid solution, improves the release speed of the effective components of the tablet, and is added with some lubricants when being mixed for use, so that the surface of the tablet is ensured to be smooth and the particle friction is reduced in the tabletting process; the pregelatinized starch is beneficial to tablet forming, a diluent and a disintegrating agent in the tabletting process, has self-lubricating effect, and is added with magnesium stearate as a lubricant when being combined with other auxiliary materials, and the pregelatinized starch combined with the malic acid solution can be used as the disintegrating agent and can be rapidly cracked into fine particles in the stomach, so that functional components are rapidly dissolved and absorbed;
the raw material medicaments comprise the following components in parts by weight:
in specific implementation, in order to improve the edible mouthfeel and taste, a sweetening agent and a flavoring agent are added into the raw material medicines.
Sweetening agent can adopt saccharin and the like, and flavoring agent can adopt lemon water, but is not limited to.
A preparation method of a Miazepini tablet raw material medicine mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, crospovidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1 by using a roller stirrer, then mixing the mixture with mirtazapine and mannitol again, adding the crospovidone after 15 minutes, adding the colloidal silicon dioxide after 18 minutes, and continuing to mix for 10 minutes;
s3, tabletting the mixture finally mixed in the S2 by using a tabletting machine.
Example 4:
a Miazepin tablet is prepared by adding mannitol, malic acid, crospovidone, dextrin, mirtazapine, lactose, mannitol, malic acid, water-soluble component, crospovidone, pregelatinized starch, lubricant, and dextrin into raw materials.
Dextrin and mannitol can be used as excipients of tablets, mannitol can also be used as diluents of medicines and solid and liquid, can be quickly dissolved in water and decomposed when entering the stomach, is beneficial to quick absorption of the body, malic acid naturally emits the fragrance of apples, the fragrance of apples enables the body of a person to relax, the effect of relaxing patients can be achieved when the apple fragrance is transmitted to the brain nervous system, the disordered and oppressive feeling of the brains of the patients can be relieved, the taste of apples can relieve the headache of a subject, the muscles of the head and the neck of the person can be relaxed, the pressure can be relieved, and the effect of refreshing and restoring consciousness can be achieved; in addition, after entering the stomach, the malic acid blocks or tablets can be quickly dissolved in water to form a weak acid environment, and can quickly dissolve mannitol and other mixtures, so that the malic acid blocks or tablets can be conveniently absorbed by a human body; the crospovidone is insoluble in water and common reagents, can be quickly sorted in the stomach environment of a malic acid solution, improves the release speed of the effective ingredients of the tablet, and is added with some lubricants when being mixed for use, so that the surface of the tablet is ensured to be smooth and the particle friction is reduced in the tabletting process; the pregelatinized starch is beneficial to tablet forming, a diluent and a disintegrating agent in the tabletting process, has self-lubricating effect, and is added with magnesium stearate as a lubricant when being combined with other auxiliary materials, and the pregelatinized starch combined with the malic acid solution can be used as the disintegrating agent and can be rapidly cracked into fine particles in the stomach, so that functional components are rapidly dissolved and absorbed;
the raw material medicaments comprise the following components in parts by weight:
in specific implementation, in order to improve the edible mouthfeel and taste, a sweetening agent and a flavoring agent are added into the raw material medicines.
Sweetening agent can adopt saccharin and the like, and flavoring agent can adopt lemon water, but is not limited to.
A preparation method of a Miazepini tablet raw material medicine mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, crospovidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1 by using a drum stirrer, then mixing the mixture with mirtazapine and mannitol again, adding crospovidone after 15 minutes, adding colloidal silicon dioxide after 20 minutes and continuing to mix for 13 minutes;
s3, tabletting the mixture finally mixed in the S2 by using a tabletting machine.
Example 5:
a Miazepin tablet is prepared by adding mannitol, malic acid, crospovidone, dextrin, mirtazapine, lactose, mannitol, malic acid, water-soluble component, crospovidone, pregelatinized starch, lubricant, and dextrin into raw materials.
Dextrin and mannitol can be used as excipients of tablets, mannitol can also be used as diluents of medicines and solid and liquid, can be quickly dissolved in water and decomposed when entering the stomach, is beneficial to quick absorption of the body, malic acid naturally emits the fragrance of apples, the fragrance of apples enables the body of a person to relax, the effect of relaxing patients can be achieved when the apple fragrance is transmitted to the brain nervous system, the disordered and oppressive feeling of the brains of the patients can be relieved, the taste of apples can relieve the headache of a subject, the muscles of the head and the neck of the person can be relaxed, the pressure can be relieved, and the effect of refreshing and restoring consciousness can be achieved; in addition, after entering the stomach, the malic acid blocks or tablets can be quickly dissolved in water to form a weak acid environment, and can quickly dissolve mannitol and other mixtures, so that the malic acid blocks or tablets can be conveniently absorbed by a human body; the crospovidone is insoluble in water and common reagents, can be quickly sorted in the stomach environment of a malic acid solution, improves the release speed of the effective ingredients of the tablet, and is added with some lubricants when being mixed for use, so that the surface of the tablet is ensured to be smooth and the particle friction is reduced in the tabletting process; the pregelatinized starch is beneficial to tablet forming, a diluent and a disintegrating agent in the tabletting process, has self-lubricating effect, and is added with magnesium stearate as a lubricant when being combined with other auxiliary materials, and the pregelatinized starch combined with the malic acid solution can be used as the disintegrating agent and can be rapidly cracked into fine particles in the stomach, so that functional components are rapidly dissolved and absorbed;
the raw material medicaments comprise the following components in parts by weight:
in specific implementation, in order to improve the edible mouthfeel and taste, a sweetening agent and a flavoring agent are added into the raw material medicines.
The sweetener can be sucralose, and the flavoring agent can be orange water.
A preparation method of a Miazepini tablet raw material medicine mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, crospovidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1 by using a drum stirrer, then mixing the mixture with mirtazapine and mannitol again, adding the crospovidone after 12 minutes, adding the colloidal silicon dioxide after 19 minutes, and continuing to mix for 12 minutes;
s3, tabletting the mixture finally mixed in the S2 by using a tabletting machine.
Test example:
dissolution rate experimental analysis;
in the dissolution test, the solid dosage form is selected to have the dissolution rate of more than 75 percent in 5 minutes in 900mL of 0.1mol/L hydrochloric acid medium with the paddle speed of 50 r/min.
In the dissolution test, the solid dosage form is selected to have the dissolution rate of more than 95 percent in a hydrochloric acid medium of 900mL and 0.1mol/L with the paddle speed of 50r/min within 10 minutes.
The specific experimental results are shown in table 1 below:
TABLE 1
| 3 minutes | 5 minutes | 8 minutes | 10 minutes | |
| Example 1 | Dissolution rate of 60.5% | Dissolution rate of 82% | Dissolution rate of 90% | Dissolution rate of 97.2% |
| Example 2 | Dissolution rate of 70.7% | Dissolution rate of 88.9% | Dissolution rate of 92.5% | 99.3% dissolution |
| Example 3 | Dissolution rate of 65.4% | Dissolution rate of 84.6% | Dissolution rate of 94.3% | Dissolution rate of 97.5% |
| Example 4 | 66.33% dissolution rate | Dissolution rate of 87.25% | Dissolution rate of 95% | Dissolution rate of 98% |
| Example 5 | 66.52% dissolution rate | Dissolution rate of 84.33% | Dissolution rate of 93.5% | Dissolution rate of 97.7% |
While the embodiments of the present invention have been disclosed above, it is not limited to the applications listed in the description and embodiments, but is fully applicable to various fields suitable for the present invention, and it will be apparent to those skilled in the art that various changes, modifications, substitutions and alterations can be made in the embodiments without departing from the principle and spirit of the present invention, and therefore the present invention is not limited to the specific details without departing from the general concept defined in the claims and the scope of equivalents thereof.
Claims (8)
1. The miazinping tablet raw material medicine is characterized in that the raw material medicine comprises mirtazapine, lactose, mannitol, malic acid, water-soluble components, crospovidone, pregelatinized starch, a lubricant and dextrin; the preparation method of the bulk drug mainly comprises the following steps:
s1, sieving lactose, methylcellulose, hydroxypropyl methylcellulose, polyvinylpolypyrrolidone, pregelatinized starch and dextrin for later use;
s2, stirring and mixing the raw materials in the step S1, then mixing the mixture with mirtazapine and mannitol again, adding the crospovidone after 10-15 minutes, adding the colloidal silicon dioxide after 18-20 minutes, and continuing to mix for 10-13 minutes;
s3, tabletting and forming the mixture after the final mixing in the S2 by using a tabletting machine.
2. The mirtazapine tablet drug substance of claim 1, wherein the lubricant is magnesium stearate, calcium stearate, sodium stearate, silica gel, colloidal silicon dioxide or a combination thereof.
3. The mirtazapine tablet drug substance of claim 1, wherein the water soluble component is hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose or a combination thereof.
4. The mirtazapine tablet bulk drug of claim 1, which is characterized by consisting of the following components in parts by weight:
5. the mirtazapine tablet bulk drug of claim 4, which is characterized by consisting of the following components in parts by weight:
6. the mirtazapine tablet drug substance of claim 1, wherein a sweetener and a flavoring agent are added to the drug substance.
7. The mirtazapine tablet drug substance of claim 1, wherein the stirring and mixing of the ingredients in step S2 is performed by a drum mixer.
8. A mirtazapine formulation, wherein the formulation components are mirtazapine tablet drug substances as defined in claim 1.
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070298107A1 (en) * | 2003-11-25 | 2007-12-27 | Aurobindo Pharma Ltd. | Pharmaceutical Compositions of Mirtazapine |
| US7838029B1 (en) * | 2003-07-31 | 2010-11-23 | Watson Laboratories, Inc. | Mirtazapine solid dosage forms |
| KR20110056071A (en) * | 2009-11-20 | 2011-05-26 | 고려제약주식회사 | Composition for oral disitegrating tablets comprising olanzapine, and tablets manufactured therefrom |
| US20110257159A1 (en) * | 2010-04-15 | 2011-10-20 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Orally disintegrating tablet formulations of mirtazapine and process for preparing the same |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7838029B1 (en) * | 2003-07-31 | 2010-11-23 | Watson Laboratories, Inc. | Mirtazapine solid dosage forms |
| US20070298107A1 (en) * | 2003-11-25 | 2007-12-27 | Aurobindo Pharma Ltd. | Pharmaceutical Compositions of Mirtazapine |
| KR20110056071A (en) * | 2009-11-20 | 2011-05-26 | 고려제약주식회사 | Composition for oral disitegrating tablets comprising olanzapine, and tablets manufactured therefrom |
| US20110257159A1 (en) * | 2010-04-15 | 2011-10-20 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Orally disintegrating tablet formulations of mirtazapine and process for preparing the same |
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