CN110025589A - A kind of sodium ferulate controlled release tablet and preparation method thereof - Google Patents
A kind of sodium ferulate controlled release tablet and preparation method thereof Download PDFInfo
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- CN110025589A CN110025589A CN201910038532.7A CN201910038532A CN110025589A CN 110025589 A CN110025589 A CN 110025589A CN 201910038532 A CN201910038532 A CN 201910038532A CN 110025589 A CN110025589 A CN 110025589A
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- Prior art keywords
- controlled release
- sodium ferulate
- parts
- release tablet
- sodium
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- NCTHNHPAQAVBEB-WGCWOXMQSA-M sodium ferulate Chemical compound [Na+].COC1=CC(\C=C\C([O-])=O)=CC=C1O NCTHNHPAQAVBEB-WGCWOXMQSA-M 0.000 title claims abstract description 42
- 238000013270 controlled release Methods 0.000 title claims abstract description 35
- 238000002360 preparation method Methods 0.000 title abstract description 13
- 239000000463 material Substances 0.000 claims abstract description 28
- 239000003814 drug Substances 0.000 claims abstract description 18
- 238000002156 mixing Methods 0.000 claims abstract description 16
- 239000011248 coating agent Substances 0.000 claims abstract description 13
- 238000000576 coating method Methods 0.000 claims abstract description 13
- 239000002994 raw material Substances 0.000 claims abstract description 7
- 238000004080 punching Methods 0.000 claims abstract description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 24
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 18
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 18
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 15
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 12
- 238000001035 drying Methods 0.000 claims description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 9
- 239000008187 granular material Substances 0.000 claims description 9
- 235000019359 magnesium stearate Nutrition 0.000 claims description 9
- 229940057838 polyethylene glycol 4000 Drugs 0.000 claims description 9
- 239000011780 sodium chloride Substances 0.000 claims description 9
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 6
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims description 6
- 239000000853 adhesive Substances 0.000 claims description 6
- 230000001070 adhesive effect Effects 0.000 claims description 6
- 229920002301 cellulose acetate Polymers 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 235000019441 ethanol Nutrition 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 230000003204 osmotic effect Effects 0.000 claims description 6
- 239000004014 plasticizer Substances 0.000 claims description 6
- 239000007779 soft material Substances 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- 239000000080 wetting agent Substances 0.000 claims description 6
- 239000004480 active ingredient Substances 0.000 claims description 5
- 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 claims description 5
- 238000000034 method Methods 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 3
- 239000001856 Ethyl cellulose Substances 0.000 claims description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 3
- 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 3
- 239000002202 Polyethylene glycol Substances 0.000 claims description 3
- MUXFZBHBYYYLTH-UHFFFAOYSA-N Zaltoprofen Chemical compound O=C1CC2=CC(C(C(O)=O)C)=CC=C2SC2=CC=CC=C21 MUXFZBHBYYYLTH-UHFFFAOYSA-N 0.000 claims description 3
- 238000005553 drilling Methods 0.000 claims description 3
- 229920001249 ethyl cellulose Polymers 0.000 claims description 3
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- 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 3
- 239000008101 lactose Substances 0.000 claims description 3
- 239000001103 potassium chloride Substances 0.000 claims description 3
- 235000011164 potassium chloride Nutrition 0.000 claims description 3
- 238000003825 pressing Methods 0.000 claims description 3
- 238000003756 stirring Methods 0.000 claims description 3
- 230000002829 reductive effect Effects 0.000 abstract description 7
- 239000008280 blood Substances 0.000 abstract description 6
- 210000004369 blood Anatomy 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 6
- 206010067484 Adverse reaction Diseases 0.000 abstract description 3
- 230000006838 adverse reaction Effects 0.000 abstract description 3
- 230000009286 beneficial effect Effects 0.000 abstract description 2
- 231100000331 toxic Toxicity 0.000 abstract description 2
- 230000002588 toxic effect Effects 0.000 abstract description 2
- 229940079593 drug Drugs 0.000 abstract 2
- 230000000857 drug effect Effects 0.000 abstract 1
- 238000007711 solidification Methods 0.000 abstract 1
- 230000008023 solidification Effects 0.000 abstract 1
- 238000002347 injection Methods 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- KSEBMYQBYZTDHS-UHFFFAOYSA-N 3-(4-hydroxy-3-methoxyphenyl)prop-2-enoic acid Chemical compound COC1=CC(C=CC(O)=O)=CC=C1O KSEBMYQBYZTDHS-UHFFFAOYSA-N 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 210000003989 endothelium vascular Anatomy 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- KSEBMYQBYZTDHS-HWKANZROSA-M (E)-Ferulic acid Natural products COC1=CC(\C=C\C([O-])=O)=CC=C1O KSEBMYQBYZTDHS-HWKANZROSA-M 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 102000002045 Endothelin Human genes 0.000 description 1
- 108050009340 Endothelin Proteins 0.000 description 1
- 208000022461 Glomerular disease Diseases 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 208000005392 Spasm Diseases 0.000 description 1
- 208000001407 Vascular Headaches Diseases 0.000 description 1
- 206010047115 Vasculitis Diseases 0.000 description 1
- 206010047139 Vasoconstriction Diseases 0.000 description 1
- 238000009098 adjuvant therapy Methods 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 230000023555 blood coagulation Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 230000000295 complement effect Effects 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 201000009101 diabetic angiopathy Diseases 0.000 description 1
- 201000002249 diabetic peripheral angiopathy Diseases 0.000 description 1
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 description 1
- 230000002851 endotheliumprotective effect Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 235000001785 ferulic acid Nutrition 0.000 description 1
- 229940114124 ferulic acid Drugs 0.000 description 1
- KSEBMYQBYZTDHS-HWKANZROSA-N ferulic acid Chemical compound COC1=CC(\C=C\C(O)=O)=CC=C1O KSEBMYQBYZTDHS-HWKANZROSA-N 0.000 description 1
- 231100000852 glomerular disease Toxicity 0.000 description 1
- XLYOFNOQVPJJNP-ZSJDYOACSA-N heavy water Substances [2H]O[2H] XLYOFNOQVPJJNP-ZSJDYOACSA-N 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000003859 lipid peroxidation Effects 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 231100000572 poisoning Toxicity 0.000 description 1
- 230000000607 poisoning effect Effects 0.000 description 1
- 239000003223 protective agent Substances 0.000 description 1
- 208000002815 pulmonary hypertension Diseases 0.000 description 1
- 230000033904 relaxation of vascular smooth muscle Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000816 toxic dose Toxicity 0.000 description 1
- QURCVMIEKCOAJU-UHFFFAOYSA-N trans-isoferulic acid Natural products COC1=CC=C(C=CC(O)=O)C=C1O QURCVMIEKCOAJU-UHFFFAOYSA-N 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
Classifications
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
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- 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
- A61P25/06—Antimigraine agents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- Veterinary Medicine (AREA)
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- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
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- Vascular Medicine (AREA)
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- Pulmonology (AREA)
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Abstract
The invention discloses a kind of sodium ferulate controlled release tablets, are made of sodium ferulate, controlled-release material, pharmaceutically acceptable auxiliary material, component is according to the mass fraction are as follows: 12-15 parts of sodium ferulate, 7-12 parts of controlled-release material, auxiliary material 73-81 parts pharmaceutically acceptable；The invention also discloses a kind of preparation methods of sodium ferulate controlled release tablet, include the following steps: raw material preparation, mixing, coating, dry solidification, punching；The beneficial effects of the present invention are: blood concentration is steady, peak valley phenomenon is avoided or reduced, toxic side effect is favorably reduced；The accumulated dose for reducing medication, can reach maximum drug effect with minimum dose；Administration number of times is reduced, patient's Compliance is improved；Advantageously reduce the adverse reaction of drug.
Description
Technical Field
The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a sodium ferulate controlled release tablet and a preparation method thereof.
Background
Sodium ferulate is sodium ferulate extracted from rhizoma Ligustici Chuanxiong and radix Angelicae sinensis, and has chemical name of 3-methoxy-4 hydroxy cinnamic acid sodium salt dihydrate, and molecular formula C10H9NaO4·2H2O; ferulic acid is a vascular endothelium protective agent, can remove free radicals, prevent and treat lipid peroxidation injury, antagonize vasoconstriction, pressure rise and vascular smooth muscle cell proliferation caused by endothelin, and relieve vascular endothelium injury; increase NO synthesis, relaxation of vascular smooth muscle; inhibiting platelet aggregation, resisting blood coagulation, and improving hemorheology. It also has effects in inhibiting cholesterol synthesis, reducing blood lipid, influencing complement, enhancing immunity, and relieving pain and spasm. It is mainly used for the adjuvant treatment of vascular diseases such as atherosclerosis, coronary heart disease, cerebrovascular disease, glomerular disease, pulmonary hypertension, diabetic angiopathy, and vasculitis, and also can be used for the treatment of migraine and vascular headache.
At present, sodium ferulate preparations for clinical application comprise common tablets, liquid injection preparations, freeze-dried powder injection and the like.
The existing sodium ferulate preparation has the following defects:
1. the common tablet has low bioavailability and large side effect on the digestive tract, needs to be taken three times a day and has poor compliance after long-term taking;
2. although the liquid injection preparation and the freeze-dried powder injection avoid the side effect of the digestive tract, the phenomenon of peak valley of the blood concentration still exists, and when the blood concentration is at the peak, the blood concentration can be higher than the minimum toxic concentration of the medicine in a short time, so adverse reactions and even poisoning are easily caused; at "trough" levels, the plasma concentration is likely to be below therapeutic levels and not effective.
Disclosure of Invention
The invention aims to provide a sodium ferulate controlled release tablet and a preparation method thereof, which aim to solve the problems in the background technology.
In order to achieve the purpose, the invention provides the following technical scheme: a sodium ferulate controlled release tablet comprises sodium ferulate, a controlled release material and pharmaceutically acceptable auxiliary materials, and comprises the following components in parts by mass: 12-15 parts of sodium ferulate, 7-12 parts of controlled release materials and 73-81 parts of pharmaceutically acceptable auxiliary materials.
In a preferred embodiment of the present invention, the controlled-release material is one or both of cellulose acetate and ethyl cellulose.
As a preferred technical scheme of the invention, the pharmaceutically acceptable auxiliary materials comprise osmotic pressure active ingredients, an adhesive, a plasticizer, a pore-forming agent, a lubricant and a wetting agent.
As a preferable technical scheme of the invention, the osmotic pressure active ingredient is one or more of sodium chloride, potassium chloride and lactose.
As a preferable technical scheme of the invention, the adhesive is one or more of hydroxypropyl methylcellulose, polyethylene glycol 4000, ethanol and water.
In a preferred embodiment of the present invention, the plasticizer is one or two of polyethylene glycol 4000 and polyethylene oxide.
As a preferable technical scheme of the invention, the pore-forming agent is one or two of polyethylene glycol 4000 and talcum powder.
In a preferred embodiment of the present invention, the lubricant is one or both of magnesium stearate and talc.
As a preferable technical scheme of the invention, the wetting agent is one or more of chloroform, acetone, methanol, ethanol and water.
The invention also discloses a preparation method of the sodium ferulate controlled release tablet, which comprises the following steps:
the method comprises the following steps: preparing raw materials: the weight portions are as follows: 12-15 parts of sodium ferulate, 7-12 parts of controlled release material and 73-81 parts of pharmaceutically acceptable auxiliary materials;
step two: mixing: uniformly mixing a sodium ferulate raw material medicine, 60-mesh-screened polyethylene oxide (PEON N-10) and sodium chloride, adding absolute ethyl alcohol to prepare a soft material, granulating by using a 18-mesh sieve, drying at 40 ℃, taking out, adding magnesium stearate, uniformly mixing to obtain medicine-containing layer granules, uniformly mixing 60-mesh-screened polyethylene oxide (PEO WSR303) and sodium chloride, adding absolute ethyl alcohol to prepare a soft material, granulating by using a 18-mesh sieve, drying at 40 ℃, taking out, adding magnesium stearate, uniformly mixing to obtain pushing layer granules, and pressing the medicine-containing layer and the pushing layer granules into a double-layer tablet core;
step three: coating: adding cellulose acetate into acetone, stirring to dissolve to obtain coating solution, placing the pressed double-layer tablet core into a coating pan, and coating;
step four: drying and curing: drying the coated product at 40 deg.C, and curing;
step five: punching: a small hole of 100-60 microns is punched in the center of the medicine-containing layer of the coated tablet by a laser-beam drilling machine.
Compared with the prior art, the invention has the beneficial effects that:
(1) the blood concentration is stable, the peak valley phenomenon is avoided or reduced, and the toxic and side effects are favorably reduced;
(2) the total dosage of the medicine is reduced, and the maximum medicine effect can be achieved by using the minimum dosage;
(3) the frequency of administration is reduced, and the administration compliance of a patient is improved;
(4) is favorable for reducing the adverse reaction of the medicine.
Drawings
FIG. 1 is a flow chart of a preparation method of the present invention;
FIG. 2 is a release profile of the release of sodium ferulate tablets of the present invention;
Detailed Description
A sodium ferulate controlled release tablet comprises sodium ferulate, a controlled release material and pharmaceutically acceptable auxiliary materials, and comprises the following components in parts by mass: 12-15 parts of sodium ferulate, 7-12 parts of controlled release material and 73-81 parts of pharmaceutically acceptable auxiliary materials; the controlled release material is one or two of cellulose acetate and ethyl cellulose; the pharmaceutically acceptable auxiliary materials comprise osmotic pressure active ingredients, adhesives, plasticizers, pore-forming agents, lubricants and wetting agents; wherein,
the osmotic pressure active ingredient is one or more of sodium chloride, potassium chloride and lactose;
the adhesive is one or more of hydroxypropyl methylcellulose, polyethylene glycol 4000, ethanol and water;
the plasticizer is one or two of polyethylene glycol 4000 and polyethylene oxide;
the pore-forming agent is one or two of polyethylene glycol 4000 and talcum powder;
the lubricant is one or two of magnesium stearate and talcum powder;
the wetting agent is one or more of chloroform, acetone, methanol, ethanol and water;
a preparation method of sodium ferulate controlled release tablet comprises the following steps:
the method comprises the following steps: preparing raw materials: the weight portions are as follows: 12-15 parts of sodium ferulate, 7-12 parts of controlled release material and 73-81 parts of pharmaceutically acceptable auxiliary materials;
step two: mixing: uniformly mixing a sodium ferulate raw material medicine, 60-mesh-screened polyethylene oxide (PEON N-10) and sodium chloride, adding absolute ethyl alcohol to prepare a soft material, granulating by using a 18-mesh sieve, drying at 40 ℃, taking out, adding magnesium stearate, uniformly mixing to obtain medicine-containing layer granules, uniformly mixing 60-mesh-screened polyethylene oxide (PEO WSR303) and sodium chloride, adding absolute ethyl alcohol to prepare a soft material, granulating by using a 18-mesh sieve, drying at 40 ℃, taking out, adding magnesium stearate, uniformly mixing to obtain pushing layer granules, and pressing the medicine-containing layer and the pushing layer granules into a double-layer tablet core;
step three: coating: adding cellulose acetate into acetone, stirring to dissolve to obtain coating solution, placing the pressed double-layer tablet core into a coating pan, and coating;
step four: drying and curing: drying the coated product at 40 deg.C, and curing;
step five: punching: a small hole of 100-60 microns is punched in the center of the medicine-containing layer of the coated tablet by a laser-beam drilling machine.
Example 1
| Time (h) | Example 1 degree of Release (%) | Sodium ferulate tablet Release (%) |
| 1 | 4.3 | 37.6 |
| 2 | 8.1 | 68.5 |
| 4 | 16.6 | 94.5 |
| 8 | 32.5 | 97.9 |
| 16 | 65.2 | 98.8 |
| 24 | 99.3 | 99.5 |
Degree of release in example 1 at various times, and table of sodium ferulate tablet release
Note: compared with the 0 month release curve, the accelerated release curve of 6 months has no difference, and the stability of the release degree is good
Release stability data sheet
Examples 2 to 6
Examples 2 to 6 degrees of Release (%)
Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that changes, modifications, substitutions and alterations can be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.
Claims (10)
1. The sodium ferulate controlled release tablet is characterized by comprising sodium ferulate, a controlled release material and pharmaceutically acceptable auxiliary materials, wherein the sodium ferulate controlled release tablet comprises the following components in parts by mass: 12-15 parts of sodium ferulate, 7-12 parts of controlled release materials and 73-81 parts of pharmaceutically acceptable auxiliary materials.
2. The sodium ferulate controlled release tablet of claim 1, wherein: the controlled release material is one or two of cellulose acetate and ethyl cellulose.
3. The sodium ferulate controlled release tablet of claim 1, wherein: the pharmaceutically acceptable auxiliary materials comprise osmotic pressure active ingredients, adhesives, plasticizers, pore-forming agents, lubricants and wetting agents.
4. The sodium ferulate controlled release tablet of claim 3, wherein: the osmotic pressure active component is one or more of sodium chloride, potassium chloride and lactose.
5. The sodium ferulate controlled release tablet of claim 3, wherein: the adhesive is one or more of hydroxypropyl methylcellulose, polyethylene glycol 4000, ethanol and water.
6. The sodium ferulate controlled release tablet of claim 3, wherein: the plasticizer is one or two of polyethylene glycol 4000 and polyethylene oxide.
7. The sodium ferulate controlled release tablet of claim 3, wherein: the pore-forming agent is one or two of polyethylene glycol 4000 and talcum powder.
8. The sodium ferulate controlled release tablet of claim 3, wherein: the lubricant is one or two of magnesium stearate and talcum powder.
9. The sodium ferulate controlled release tablet of claim 3, wherein: the wetting agent is one or more of chloroform, acetone, methanol, ethanol and water.
10. The method for preparing sodium ferulate controlled release tablet of claim 1, which is characterized by the following steps: the method comprises the following steps:
the method comprises the following steps: preparing raw materials: the weight portions are as follows: 12-15 parts of sodium ferulate, 7-12 parts of controlled release material and 73-81 parts of pharmaceutically acceptable auxiliary materials;
step two: mixing: uniformly mixing a sodium ferulate raw material medicine, 60-mesh-screened polyethylene oxide (PEON N-10) and sodium chloride, adding absolute ethyl alcohol to prepare a soft material, granulating by using a 18-mesh sieve, drying at 40 ℃, taking out, adding magnesium stearate, uniformly mixing to obtain medicine-containing layer granules, uniformly mixing 60-mesh-screened polyethylene oxide (PEO WSR303) and sodium chloride, adding absolute ethyl alcohol to prepare a soft material, granulating by using a 18-mesh sieve, drying at 40 ℃, taking out, adding magnesium stearate, uniformly mixing to obtain pushing layer granules, and pressing the medicine-containing layer and the pushing layer granules into a double-layer tablet core;
step three: coating: adding cellulose acetate into acetone, stirring to dissolve to obtain coating solution, placing the pressed double-layer tablet core into a coating pan, and coating;
step four: drying and curing: drying the coated product at 40 deg.C, and curing;
step five: punching: a small hole of 100-60 microns is punched in the center of the medicine-containing layer of the coated tablet by a laser-beam drilling machine.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1522693A (en) * | 2003-09-08 | 2004-08-25 | 天津太平洋制药有限公司 | Sodium ferulic acid osmosis pump controlled release formulation and its preparation method |
| CN101627977A (en) * | 2008-07-17 | 2010-01-20 | 北京科信必成医药科技发展有限公司 | Double-layer osmotic pump controlled-release medicinal composition of barnidipine or physiologically acceptable salt of barnidipine |
| CN102091053A (en) * | 2009-12-14 | 2011-06-15 | 常州善美药物研究开发中心有限公司 | Particle composite controlled-release tablets |
-
2019
- 2019-01-16 CN CN201910038532.7A patent/CN110025589A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1522693A (en) * | 2003-09-08 | 2004-08-25 | 天津太平洋制药有限公司 | Sodium ferulic acid osmosis pump controlled release formulation and its preparation method |
| CN101627977A (en) * | 2008-07-17 | 2010-01-20 | 北京科信必成医药科技发展有限公司 | Double-layer osmotic pump controlled-release medicinal composition of barnidipine or physiologically acceptable salt of barnidipine |
| CN102091053A (en) * | 2009-12-14 | 2011-06-15 | 常州善美药物研究开发中心有限公司 | Particle composite controlled-release tablets |
Non-Patent Citations (3)
| Title |
|---|
| LILI HE等: "A novel controlled porosity osmotic pump system for sodium ferulate", 《PHARMAZIE》 * |
| 张强等: "《药剂学》", 30 January 2005, 北京大学医学出版社 * |
| 胡容峰: "《工业药剂学》", 31 August 2010, 中国中医药出版社 * |
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Application publication date: 20190719 |