CN114983951B - Gastric floating tablet composition and preparation method thereof - Google Patents
Gastric floating tablet composition and preparation method thereof Download PDFInfo
- Publication number
- CN114983951B CN114983951B CN202111596379.3A CN202111596379A CN114983951B CN 114983951 B CN114983951 B CN 114983951B CN 202111596379 A CN202111596379 A CN 202111596379A CN 114983951 B CN114983951 B CN 114983951B
- Authority
- CN
- China
- Prior art keywords
- parts
- agent
- gastric
- tablet composition
- cellulose ether
- 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.)
- Active
Links
- 230000002496 gastric effect Effects 0.000 title claims abstract description 29
- 239000007916 tablet composition Substances 0.000 title claims abstract description 25
- 238000002360 preparation method Methods 0.000 title abstract description 14
- 150000001875 compounds Chemical class 0.000 claims abstract description 28
- 229920003086 cellulose ether Polymers 0.000 claims abstract description 25
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 20
- 239000000203 mixture Substances 0.000 claims abstract description 19
- 239000004088 foaming agent Substances 0.000 claims abstract description 18
- 239000012752 auxiliary agent Substances 0.000 claims abstract description 16
- 238000004090 dissolution Methods 0.000 claims abstract description 15
- 238000002156 mixing Methods 0.000 claims abstract description 14
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims abstract description 14
- 229960001233 pregabalin Drugs 0.000 claims abstract description 13
- 238000003756 stirring Methods 0.000 claims abstract description 7
- 239000002994 raw material Substances 0.000 claims abstract description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 15
- 229920002125 Sokalan® Polymers 0.000 claims description 15
- 229960001631 carbomer Drugs 0.000 claims description 15
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 14
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
- -1 polyoxyethylene Polymers 0.000 claims description 14
- 102220310434 rs764401457 Human genes 0.000 claims description 14
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 11
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 11
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical group [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 8
- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 7
- 229940069328 povidone Drugs 0.000 claims description 7
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 4
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 4
- 239000003814 drug Substances 0.000 abstract description 32
- 229940079593 drug Drugs 0.000 abstract description 21
- 230000000694 effects Effects 0.000 abstract description 7
- 239000003826 tablet Substances 0.000 description 21
- 239000000126 substance Substances 0.000 description 10
- 239000011248 coating agent Substances 0.000 description 7
- 238000000576 coating method Methods 0.000 description 7
- 230000000052 comparative effect Effects 0.000 description 7
- 229960000913 crospovidone Drugs 0.000 description 7
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 7
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 7
- 241000219470 Mirabilis Species 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 241000222722 Leishmania <genus> Species 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 239000011148 porous material Substances 0.000 description 3
- 102220487426 Actin-related protein 2/3 complex subunit 3_K15M_mutation Human genes 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000001186 cumulative effect Effects 0.000 description 2
- 230000000857 drug effect Effects 0.000 description 2
- 150000002170 ethers Chemical class 0.000 description 2
- 210000004051 gastric juice Anatomy 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 description 2
- 229960004390 palbociclib Drugs 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- RAGOYPUPXAKGKH-XAKZXMRKSA-N posaconazole Chemical compound O=C1N([C@H]([C@H](C)O)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3C[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 RAGOYPUPXAKGKH-XAKZXMRKSA-N 0.000 description 2
- 229960001589 posaconazole Drugs 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 238000009475 tablet pressing Methods 0.000 description 2
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 description 1
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 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 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- 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 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 229920000954 Polyglycolide Polymers 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000004061 bleaching Methods 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 235000010216 calcium carbonate Nutrition 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 230000030135 gastric motility Effects 0.000 description 1
- 229940049654 glyceryl behenate Drugs 0.000 description 1
- 230000036571 hydration Effects 0.000 description 1
- 238000006703 hydration reaction Methods 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229960003943 hypromellose Drugs 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 235000014380 magnesium carbonate Nutrition 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000004633 polyglycolic acid Substances 0.000 description 1
- 239000011736 potassium bicarbonate Substances 0.000 description 1
- 229910000028 potassium bicarbonate Inorganic materials 0.000 description 1
- 235000015497 potassium bicarbonate Nutrition 0.000 description 1
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002028 premature Effects 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 229940083575 sodium dodecyl sulfate Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000013269 sustained drug release Methods 0.000 description 1
- 239000007939 sustained release tablet Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 238000012360 testing method Methods 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
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
-
- 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
Abstract
The invention relates to the technical field of medicines, in particular to a gastric floating tablet composition with IPC classification number of A61K and a preparation method thereof, wherein the gastric floating tablet composition comprises the following raw materials in parts by weight: 320-340 parts of pregabalin, 301-305 parts of nonionic cellulose ether compound, 480-500 parts of dissolution agent, 10-15 parts of foaming agent and 2.5-3.0 parts of auxiliary agent. Adding pregabalin, nonionic cellulose ether compound, dissolution agent and foaming agent into a conical mixer for mixing, adding an auxiliary agent, mixing and stirring to obtain a mixture, transferring the mixture into a rotary tablet press for tabletting, and preparing the gastric floating tablet composition, wherein the composition can enable medicines to be slowly released, give full play to medicine effects, and ensure medication safety.
Description
Technical Field
The invention relates to the technical field of medicines, and in particular relates to a gastric floating tablet composition and a preparation method thereof, wherein the IPC classification number is A61K.
Background
The density of the gastric floating tablet is usually smaller than that of gastric juice, the gastric floating tablet can be slowly released, a polymer is added into the preparation of the gastric floating tablet, buoyancy is provided by hydration swelling, absorption of the drug in the stomach can be improved, adverse reactions are reduced, and further clinical curative effects are improved, and the particle size, shape and density of tablet auxiliary materials can be optimized, so that the tablet has enough mechanical strength in the delivery process, can bear gastric movement, and further the residence time of the gastric floating tablet is prolonged.
Improving the efficacy of gastric floating tablets requires avoiding premature release of the pharmaceutically active ingredient, which is quite different from the traditional tablet form. Meanwhile, higher requirements are also put forward for production and research and development, buoyancy and mechanical strength are required to be considered, gastric motility can be born, and the retention time of the gastric floating tablets is ensured to fully exert the drug effect.
Patent CN201510162791.2 discloses a palbociclib gastric floating tablet and a preparation method thereof, wherein the preparation raw materials comprise palbociclib, hypromellose, a bleaching aid, a foaming agent, microcrystalline cellulose and magnesium stearate, the prepared gastric floating tablet can keep floating time of more than 10 hours in gastric juice, and sustained drug release is carried out in hydrochloric acid solution with pH of 1.2, but the drug release time is shorter.
Patent CN201911421021.X discloses a posaconazole gastric floating tablet and a preparation method thereof, wherein the preparation raw materials comprise posaconazole, carbomer, sodium bicarbonate, lactose, sodium dodecyl sulfate, PEG and magnesium stearate, the preparation process is simple, the cost is low, the drug compliance is strong, but the drug slow release effect is poor.
Therefore, the gastric floating tablet which has long slow release time, sufficient slow release, poor slow release effect, uniform slow release concentration and full play of drug effect is developed, and has good practical application value.
Disclosure of Invention
The first aspect of the present invention provides a gastric-floating tablet composition comprising, in parts by weight: 320-340 parts of pregabalin, 301-305 parts of nonionic cellulose ether compound, 480-500 parts of dissolution agent, 10-15 parts of foaming agent and 2.5-3.0 parts of auxiliary agent.
Preferably, the nonionic cellulose ether compound is one or a combination of several of HPMC K4M, EC, HPMC K100LV, HEC and HPMC K15M, CMC;
further preferably, the nonionic cellulose ether compound is HPMC K4M;
preferably, the dissolving agent is one or a combination of more than one of crosslinked povidone XL, glyceryl behenate, polyoxyethylene N60K, sodium carboxymethyl starch, carbomer 971P, crosslinked sodium carboxymethyl cellulose and polyglycolic acid;
further preferably, the dissolving agent is a compound of crospovidone XL, polyoxyethylene N60K and carbomer 971P, and the mass ratio of the crospovidone XL, the polyoxyethylene N60K and the carbomer 971P is 8-9:0.8-1.3:1.1 to 1.7;
preferably, the foaming agent is one or a combination of more of sodium bicarbonate, sodium carbonate, potassium bicarbonate, calcium carbonate and magnesium carbonate;
further preferably, the foaming agent is sodium bicarbonate;
preferably, the auxiliary agent is one or a combination of more of magnesium stearate, talcum powder and micro powder silica gel;
further preferably, the auxiliary agent is magnesium stearate;
the second aspect of the invention provides a method for preparing a gastric-floating tablet composition, comprising the specific steps of: adding pregabalin, nonionic cellulose ether compound, dissolving agent and foaming agent into a conical mixer, mixing, adding auxiliary agent, mixing and stirring to obtain a mixture, transferring the mixture into a rotary tablet press, and tabletting to obtain the gastric floating tablet composition.
The beneficial effects are that:
(1) The invention prepares the gastric floating tablet composition by adding pregabalin, nonionic cellulose ether compound, dissolution agent and foaming agent into a conical mixer for mixing, so that the medicine is slowly released, the medicine effect is fully exerted, and the medication safety is ensured.
(2) The applicant finds that the drug slow release property of the prepared gastric floating tablet composition can be improved by adding the nonionic cellulose ether compound, and particularly when the nonionic cellulose ether compound is HPMC K4M, the drug slow release property can be fully released, the nonionic cellulose ether compound and a dissolving agent in a system cooperate to effectively coat the active ingredients of the drug, the dissolution speed of the drug is controlled, so that the drug is fully dissolved, active groups in the nonionic cellulose ether compound and the active ingredients of the drug can be tightly adsorbed on the surfaces of the active ingredients of the drug through intermolecular acting force to form a coating structure, the dissolution speed of the drug can be controlled, the contact angle of the drug and water is reduced, the drug is easy to wet, water molecules are filled into pores of the coating structure after water absorption, the coating structure is expanded, the dissolution rate and the release rate of the prepared tablet are improved, but the surface of the coating structure may have micro-pore uneven phenomenon, so that the medicine is dissolved too fast or too slowly in a specific time, and the interaction between nonionic cellulose ether compounds and the dissolution agent in the system through strong polymer molecular chains can improve the microscopic characteristics of a coating structure formed by the nonionic cellulose ether compounds and the effective components of the medicine, so that the microscopic pores on the surface of the coating structure are more uniform, the toughness and the hardness of the coating structure are increased, the hardness of the gastric floating tablet composition prepared by the tablet pressing process is high through specific mixing and stirring, the stability and the dissolution rate of the gastric floating tablet composition are high after water is met, the medicine can be continuously and uniformly released for a long time, the medicine effect is further prolonged, the blood concentration is constantly maintained in an effective concentration range for a long time, the dissolution is sufficient, the medicine slow release property of the gastric floating tablet composition is greatly improved, fully exerts the efficacy, and is especially suitable for improving the slow release property and efficacy of the medicine of the gastric floating tablet.
(3) The invention adds pregabalin, nonionic cellulose ether compound, dissolving agent and foaming agent into a conical mixer to mix, then adds auxiliary agent, mixes and stirs to obtain a mixture, transfers the mixture into a rotary tablet press to carry out tablet pressing, and prepares the gastric floating tablet composition which can slowly release the medicine, fully exert the medicine effect and ensure the medication safety.
Drawings
FIG. 1 is a graph showing the cumulative release (%) of a gastric-floating tablet composition obtained by the preparation of commercial products and example 2, comparative example 1 and comparative example 2.
Detailed Description
Example 1
Example 1 provides a gastric-floating tablet composition comprising, in parts by weight: 335 parts of pregabalin, 305 parts of nonionic cellulose ether compound, 491 parts of dissolution agent, 12 parts of foaming agent and 2.9 parts of auxiliary agent.
The nonionic cellulose ether compound is HPMC K4M, and has viscosity of 2700-5040mPa.s and brand: the USA Mirabilis is purchased from Shanghai Senjun chemical industry formulation auxiliary material Co., ltd;
the dissolving agent is a compound of crosslinked povidone XL, polyoxyethylene N60K and carbomer 971P, and the mass ratio of the crosslinked povidone XL to the polyoxyethylene N60K to the carbomer 971P is 8.7:1.1:1.5, crospovidone XL, brand: leishmania, available from Shanghai forest chemical preparation auxiliary material Co., ltd., polyoxyethylene N60K, brand: DOW chemical, carbomer 971P, available from Shanghai Chang as a pharmaceutical adjuvant technology Co., ltd;
the foaming agent is sodium bicarbonate;
the auxiliary agent is magnesium stearate;
the second aspect of the invention provides a method for preparing a gastric-floating tablet composition, comprising the specific steps of:
adding pregabalin, nonionic cellulose ether compound, a dissolving agent and a foaming agent into a conical mixer, mixing at a mixing speed of 18r/min for 15min, adding an auxiliary agent, mixing and stirring for 5min to obtain a mixture, transferring the mixture into a rotary tablet press, and tabletting with a tabletting mold comprising: 22.0 x 10.8mm shallow arc mould, to prepare a gastric floating tablet composition.
Example 2
Example 2 provides a gastric-floating tablet composition comprising, in parts by weight: 330 parts of pregabalin, 303.8 parts of nonionic cellulose ether compound, 488.4 parts of dissolution agent, 10 parts of foaming agent and 2.8 parts of auxiliary agent.
The nonionic cellulose ether compound is HPMC K4M, and has viscosity of 2700-5040mPa.s and brand: the USA Mirabilis is purchased from Shanghai Senjun chemical industry formulation auxiliary material Co., ltd;
the dissolving agent is a compound of crosslinked povidone XL, polyoxyethylene N60K and carbomer 971P, and the mass ratio of the crosslinked povidone XL to the polyoxyethylene N60K to the carbomer 971P is 8.5:1.0:1.3, crospovidone XL, brand: leishmania, available from Shanghai forest chemical preparation auxiliary material Co., ltd., polyoxyethylene N60K, brand: DOW chemical, carbomer 971P, available from Shanghai Chang as a pharmaceutical adjuvant technology Co., ltd;
the foaming agent is sodium bicarbonate;
the auxiliary agent is magnesium stearate;
the second aspect of the invention provides a method for preparing a gastric-floating tablet composition, comprising the specific steps of:
adding pregabalin, nonionic cellulose ether compound, a dissolving agent and a foaming agent into a conical mixer, mixing at a mixing speed of 18r/min for 15min, adding an auxiliary agent, mixing and stirring for 5min to obtain a mixture, transferring the mixture into a rotary tablet press, and tabletting with a tabletting mold comprising: 22.0 x 10.8mm shallow arc mould, to prepare a gastric floating tablet composition.
Comparative example 1
The specific embodiment is the same as example 2, except that the nonionic cellulose ether compound is HPMC K100LV, the viscosity is 80-120mPa.s, and the brand: the USA Mirabilis is purchased from Shanghai Senjun chemical industry formulation auxiliary material Co.
Comparative example 2
The specific embodiment is the same as example 2, except that the nonionic cellulose ether compound is HPMC K15M, the viscosity is 13500-25200mPa.s, and the brand: the USA Mirabilis is purchased from Shanghai Senjun chemical industry formulation auxiliary material Co.
Comparative example 3
The specific embodiment is the same as example 2, and the difference is that the dissolution agent is a compound of crospovidone XL, polyoxyethylene N60K and carbomer 971P, and the mass ratio of the crospovidone XL, polyoxyethylene N60K and carbomer 971P is 3:0.8:0.5, crospovidone XL, brand: leishmania, available from Shanghai forest chemical preparation auxiliary material Co., ltd., polyoxyethylene N60K, brand: dow chemical, carbomer 971P, available from Shanghai Chang as pharmaceutical excipients technology Co.
Performance testing
The commercial Lyrica CR pregabalin sustained release tablet has the specification of 330mg and the manufacturer is: the composition of the conventional Gastria tablet, which is prepared in examples 1-2 and comparative examples 1-3, was tested for dissolution by a high performance liquid chromatograph, and the composition of the conventional Gastria tablet, which is prepared in examples 1-2 and comparative examples 1-3, was tested for cumulative release (%) of the drug over a period of 0-24 hours.
The dissolution method comprises the following steps: pulp method, pulp rotation speed: 50rpm, dissolution medium: 0.06mol/L HCl, medium volume: 900ml, medium temperature: 37 ℃, sampling point: 0. 1, 2, 4, 6, 8, 10, 12, 16, 24h.
Claims (1)
1. The gastric floating tablet composition is characterized by comprising the following raw materials in parts by weight: 320-340 parts of pregabalin, 301-305 parts of nonionic cellulose ether compound, 480-500 parts of dissolution agent, 10-15 parts of foaming agent and 2.5-3.0 parts of auxiliary agent;
the nonionic cellulose ether compound is HPMC K4M, and the viscosity is 2700-5040mPa.s;
the dissolving agent is a compound of crosslinked povidone XL, polyoxyethylene N60K and carbomer 971P, and the mass ratio of the crosslinked povidone XL to the polyoxyethylene N60K to the carbomer 971P is 8-9:0.8-1.3:1.1 to 1.7;
the foaming agent is sodium bicarbonate;
the auxiliary agent is magnesium stearate;
a method of preparing a gastric-floating tablet composition as described above comprising the steps of:
adding pregabalin, nonionic cellulose ether compound, dissolving agent and foaming agent into a conical mixer, mixing, adding auxiliary agent, mixing and stirring to obtain a mixture, transferring the mixture into a rotary tablet press, and tabletting to obtain the gastric floating tablet composition.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202111596379.3A CN114983951B (en) | 2021-12-24 | 2021-12-24 | Gastric floating tablet composition and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202111596379.3A CN114983951B (en) | 2021-12-24 | 2021-12-24 | Gastric floating tablet composition and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN114983951A CN114983951A (en) | 2022-09-02 |
| CN114983951B true CN114983951B (en) | 2023-11-07 |
Family
ID=83018297
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202111596379.3A Active CN114983951B (en) | 2021-12-24 | 2021-12-24 | Gastric floating tablet composition and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN114983951B (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104906064A (en) * | 2015-05-15 | 2015-09-16 | 中国药科大学 | Pregabalin intragastric floating sustained release tablet and preparation method thereof |
| CN112004520A (en) * | 2017-12-18 | 2020-11-27 | 特瑞斯制药公司 | Modified release drug powder compositions comprising a gastric retentive raft forming system with triggered pulsed drug release |
| CN113521025A (en) * | 2021-07-09 | 2021-10-22 | 上海博志研新药物研究有限公司 | Pharmaceutical composition of pregabalin and preparation method and application thereof |
| CN113577036A (en) * | 2021-05-31 | 2021-11-02 | 石药集团欧意药业有限公司 | Pregabalin gastric floating sustained release tablet and preparation method thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109475510B (en) * | 2016-07-17 | 2023-03-10 | Mapi医药公司 | Extended release dosage forms of pregabalin |
| WO2019238068A1 (en) * | 2018-06-13 | 2019-12-19 | 北京泰德制药股份有限公司 | Sustained-release pregabalin composition and preparation method therefor |
-
2021
- 2021-12-24 CN CN202111596379.3A patent/CN114983951B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104906064A (en) * | 2015-05-15 | 2015-09-16 | 中国药科大学 | Pregabalin intragastric floating sustained release tablet and preparation method thereof |
| CN112004520A (en) * | 2017-12-18 | 2020-11-27 | 特瑞斯制药公司 | Modified release drug powder compositions comprising a gastric retentive raft forming system with triggered pulsed drug release |
| CN113577036A (en) * | 2021-05-31 | 2021-11-02 | 石药集团欧意药业有限公司 | Pregabalin gastric floating sustained release tablet and preparation method thereof |
| CN113521025A (en) * | 2021-07-09 | 2021-10-22 | 上海博志研新药物研究有限公司 | Pharmaceutical composition of pregabalin and preparation method and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| 普瑞巴林胃滞留缓释片的制备及体外释药机理研究;史雯星;尹莉芳;祝玲;陈玉红;石心红;;海峡药学(第10期);全文 * |
| 普瑞巴林胃漂浮缓释片的处方工艺研究;翟小春;辜勇军;;中国药剂学杂志(网络版)(第03期);全文 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN114983951A (en) | 2022-09-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4842866A (en) | Slow release solid preparation | |
| US6066334A (en) | Use of redispersible polymer powders or polymer granules as binders for producing solid pharmaceutical presentations | |
| CN1635894A (en) | Dosage form for treatment of diabetes mellitus | |
| JPH10511407A (en) | Sustained release matrix for high dose poorly soluble drugs | |
| CA2746855A1 (en) | Extended-release pharmaceutical formulations | |
| EP3981399A1 (en) | Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor | |
| JPH10502056A (en) | Modifiable starch acetate compositions and methods of making and using the same | |
| US20030045580A1 (en) | Ibuprofen containing active agent preparation | |
| RU2489153C2 (en) | Pharmaceutical compositions containing prodrug of hcv polymerase inhibitor | |
| WO2013082706A1 (en) | Disintegrant-free delayed release doxylamine and pyridoxine formulation and process of manufacturing | |
| JPH0513132B2 (en) | ||
| CN114983951B (en) | Gastric floating tablet composition and preparation method thereof | |
| CN100525760C (en) | Duloxetine hydrochloride sustained release medicine | |
| CN113116836A (en) | Gliclazide sustained release tablet | |
| CN104666263B (en) | A kind of tablet containing Levetiracetam and preparation method thereof | |
| CN112168796A (en) | Controlled-release drug sustained-release preparation of biphasic sustained-release system and preparation method thereof | |
| CN107744509B (en) | Mosapride citrate tablet and preparation method thereof | |
| RU2377989C2 (en) | Trimetazidine preparation as matrix tablet of prolonged action and method for making thereof | |
| CN104758266A (en) | Felodipine sustained-release tablet and preparation technology thereof | |
| JPH02184624A (en) | Sustained release composition wherein trimebtin is base and preparation thereof | |
| CN115227660B (en) | Metformin hydrochloride sustained release tablet and preparation method thereof | |
| JPH115739A (en) | Prolonged action drug containing bezafibrate and manufacture of the same | |
| CN116898819B (en) | Pregabalin sustained release agent and preparation method thereof | |
| CN112516099B (en) | Gliclazide sustained release tablet and preparation method thereof | |
| CN116803378B (en) | Gliclazide sustained-release tablet and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |