CN116473935B - Glipizide controlled-release tablet - Google Patents
Glipizide controlled-release tablet Download PDFInfo
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- CN116473935B CN116473935B CN202310453002.5A CN202310453002A CN116473935B CN 116473935 B CN116473935 B CN 116473935B CN 202310453002 A CN202310453002 A CN 202310453002A CN 116473935 B CN116473935 B CN 116473935B
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- China
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- glipizide
- tablet
- release
- semipermeable membrane
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- ZJJXGWJIGJFDTL-UHFFFAOYSA-N glipizide Chemical compound C1=NC(C)=CN=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZJJXGWJIGJFDTL-UHFFFAOYSA-N 0.000 title claims abstract description 48
- 229960001381 glipizide Drugs 0.000 title claims abstract description 47
- 238000013270 controlled release Methods 0.000 title claims abstract description 31
- FLKPEMZONWLCSK-UHFFFAOYSA-N diethyl phthalate Chemical compound CCOC(=O)C1=CC=CC=C1C(=O)OCC FLKPEMZONWLCSK-UHFFFAOYSA-N 0.000 claims abstract description 32
- 239000003814 drug Substances 0.000 claims abstract description 31
- 239000012528 membrane Substances 0.000 claims abstract description 20
- 229940079593 drug Drugs 0.000 claims abstract description 17
- 239000000314 lubricant Substances 0.000 claims abstract description 17
- 239000004372 Polyvinyl alcohol Substances 0.000 claims abstract description 16
- 229920002451 polyvinyl alcohol Polymers 0.000 claims abstract description 16
- 230000003204 osmotic effect Effects 0.000 claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 10
- 239000004094 surface-active agent Substances 0.000 claims abstract description 8
- 239000013543 active substance Substances 0.000 claims abstract description 7
- 229940068918 polyethylene glycol 400 Drugs 0.000 claims abstract description 7
- 239000003961 penetration enhancing agent Substances 0.000 claims abstract description 4
- 239000011248 coating agent Substances 0.000 claims description 37
- 238000000576 coating method Methods 0.000 claims description 37
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 28
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 15
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 15
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 15
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 14
- 229930195725 Mannitol Natural products 0.000 claims description 14
- 235000019359 magnesium stearate Nutrition 0.000 claims description 14
- 239000000594 mannitol Substances 0.000 claims description 14
- 235000010355 mannitol Nutrition 0.000 claims description 14
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 13
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 13
- 239000004203 carnauba wax Substances 0.000 claims description 13
- 235000013869 carnauba wax Nutrition 0.000 claims description 13
- 238000002156 mixing Methods 0.000 claims description 13
- -1 polyoxyethylene Polymers 0.000 claims description 13
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 13
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 12
- 238000001035 drying Methods 0.000 claims description 12
- OVARTBFNCCXQKS-UHFFFAOYSA-N propan-2-one;hydrate Chemical compound O.CC(C)=O OVARTBFNCCXQKS-UHFFFAOYSA-N 0.000 claims description 12
- 235000010413 sodium alginate Nutrition 0.000 claims description 12
- 239000000661 sodium alginate Substances 0.000 claims description 12
- 229940005550 sodium alginate Drugs 0.000 claims description 12
- 239000007779 soft material Substances 0.000 claims description 12
- 239000002904 solvent Substances 0.000 claims description 12
- 238000005507 spraying Methods 0.000 claims description 12
- QQGISFDJEJMKIL-JAIQZWGSSA-N (5z)-5-[[3-(hydroxymethyl)thiophen-2-yl]methylidene]-10-methoxy-2,2,4-trimethyl-1h-chromeno[3,4-f]quinolin-9-ol Chemical group C1=CC=2NC(C)(C)C=C(C)C=2C2=C1C=1C(OC)=C(O)C=CC=1O\C2=C/C=1SC=CC=1CO QQGISFDJEJMKIL-JAIQZWGSSA-N 0.000 claims description 10
- 239000011230 binding agent Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000853 adhesive Substances 0.000 abstract description 15
- 230000001070 adhesive effect Effects 0.000 abstract description 15
- 238000009776 industrial production Methods 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 2
- 239000007788 liquid Substances 0.000 description 22
- 230000032683 aging Effects 0.000 description 11
- 238000005553 drilling Methods 0.000 description 11
- 239000002202 Polyethylene glycol Substances 0.000 description 10
- 229920001223 polyethylene glycol Polymers 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 9
- 230000001133 acceleration Effects 0.000 description 6
- 230000007774 longterm Effects 0.000 description 6
- 238000000338 in vitro Methods 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000008363 phosphate buffer Substances 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
- 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 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000000691 measurement method Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 238000012795 verification Methods 0.000 description 2
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920003086 cellulose ether Polymers 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 235000001727 glucose Nutrition 0.000 description 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000003914 insulin secretion Effects 0.000 description 1
- 238000011031 large-scale manufacturing process Methods 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 229910000402 monopotassium phosphate Inorganic materials 0.000 description 1
- 235000019796 monopotassium phosphate Nutrition 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000003538 oral antidiabetic agent Substances 0.000 description 1
- 229940127209 oral hypoglycaemic agent Drugs 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 150000004804 polysaccharides Chemical class 0.000 description 1
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 1
- LWIHDJKSTIGBAC-UHFFFAOYSA-K potassium phosphate Substances [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 230000001502 supplementing effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 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
- A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
-
- A—HUMAN NECESSITIES
- 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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- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明属于药物制剂领域，具体涉及所述格列吡嗪控释片中，包含片芯、半透膜和释药孔，所述片芯包括：格列吡嗪、促渗剂、渗透压活性剂、表面活性剂、阻滞剂、粘合剂、润滑剂；半透膜为聚乙烯醇、邻苯二甲酸二乙酯、聚乙二醇400，均具有较好的释放效果，同时该控释片性能稳定，能够长时间存放，且制备工艺简单，适于工业化生产。The invention belongs to the field of pharmaceutical preparations, and specifically relates to a glipizide controlled-release tablet, which comprises a tablet core, a semipermeable membrane and a drug release hole. The tablet core comprises: glipizide, a penetration enhancer, an osmotic pressure active agent, a surfactant, a blocker, an adhesive, and a lubricant; the semipermeable membrane is polyvinyl alcohol, diethyl phthalate, and polyethylene glycol 400, all of which have good release effects. At the same time, the controlled-release tablet has stable performance, can be stored for a long time, and has a simple preparation process, and is suitable for industrial production.
Description
Technical Field
The invention relates to the field of pharmaceutical preparations, in particular to a glipizide controlled release tablet and a preparation method thereof.
Background
Glipizide is an oral hypoglycemic agent, and can promote glucose-stimulated insulin secretion. Controlled release tablets, currently marketed under the trade name GLUCOTROL XL, comprise an "active" layer of a drug and a "booster" layer comprising a pharmacologically inert (but osmotically active) ingredient. The formulation has water-soluble Polymer Ethylene Oxide (PEO) as a matrix material, and the carrier has good miscibility with water. However, due to the low melting point of PEO, which is only 63-67 ℃, the thermal stability is poor, which is not conducive to the preparation and storage of large-scale production, and many attempts have been made by those skilled in the art to improve the quality of glipizide controlled-release tablets. If CN110368372a discloses a double-chamber osmotic pump type glipizide controlled release tablet, CN104414992B discloses a glipizide osmotic pump controlled release tablet, CN103565774B discloses a glipizide controlled release composition, the manufacturing cost is higher, the controlled release effect is not ideal, the release speed is too fast, not lasting, the release is incomplete, or the preparation is unstable and cannot be stored for a long time, and the preparation process of the preparation is complex, which is not beneficial to industrialized mass production.
Disclosure of Invention
The invention aims at solving the technical problems and provides a glipizide controlled-release tablet which is mild and durable in release, basically can be completely released in 24 hours, and meanwhile, has stable performance, can be stored for a long time, is simple in preparation process and is suitable for industrial production.
In order to solve the technical problems, the invention adopts the following technical scheme:
The glipizide controlled release tablet comprises a tablet core, a semipermeable membrane and drug release holes, wherein the tablet core is composed of the following auxiliary materials of glipizide, a permeation promoter, an osmotic pressure active agent, a surfactant, a retarder, an adhesive and a lubricant, and the semipermeable membrane is composed of the following auxiliary materials of polyvinyl alcohol, diethyl phthalate and polyethylene glycol 400.
The glipizide controlled release tablet comprises, by weight, 5 parts of glipizide, 10-20 parts of a permeation promoter, 2-3 parts of an osmotic pressure active agent, 3-5 parts of a surfactant, 1-2 parts of a retarder, 0.2-0.4 part of an adhesive and 0.1-0.2 part of a lubricant.
The glipizide controlled release tablet comprises, by weight, 10-20 parts of polyvinyl alcohol, 5-10 parts of diethyl phthalate and 1-2 parts of polyethylene glycol 400.
The penetration enhancer is selected from one or more of hydroxypropyl methylcellulose, hydroxyethyl cellulose, methylcellulose, non-cellulose polysaccharide, polyvinylpyrrolidone, hydroxypropyl cellulose, carboxymethyl cellulose and its salts, alginic acid and its salts, polyoxyethylene and hydroxymethyl cellulose.
The glipizide controlled release tablet is characterized in that the osmotic pressure active agent is one or more of mannitol, xylitol, glucose, sorbitol, fructose and sucrose, and the surfactant is sodium dodecyl sulfate.
The glipizide controlled release tablet is characterized in that the retarder is one or more of beeswax, carnauba wax, hydrogenated vegetable oil and stearyl alcohol, the adhesive is one or more of cellulose ether, polyvinylpyrrolidone and hydroxypropyl methyl cellulose succinate, and the lubricant is one or more of stearic acid, magnesium stearate and calcium stearate.
The glipizide controlled release tablet comprises, by weight, 5 parts of glipizide, 5-10 parts of sodium alginate, 5-10 parts of polyoxyethylene, 2-3 parts of mannitol, 3-5 parts of sodium dodecyl sulfate, 1-2 parts of carnauba wax, 0.2-0.4 part of polyvinylpyrrolidone and 0.1-0.2 part of magnesium stearate.
The glipizide controlled release tablet comprises, by weight, 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol.
The glipizide controlled release tablet comprises, by weight, 5 parts of glipizide, 5 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate.
The preparation method of the glipizide controlled release tablet comprises the following steps:
(1) Uniformly mixing glipizide, a permeation promoter, an osmotic pressure active agent, a surfactant and a retarder, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as coating solvent, adding polyvinyl alcohol, diethyl phthalate and polyethylene glycol 400 to prepare semipermeable membrane coating liquid, spraying the coating liquid onto the drug tablet core obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
The invention controls the rate of water entering the tablet core through the membrane control coating system, after the water enters the tablet core, the osmotic pressure promoter absorbs water to enable the osmotic pressure in the tablet core to be higher than the external medium environment, thereby generating osmotic pressure difference, further promoting the penetration of the water, the permeation promoter absorbs water to expand, and the medicine forming suspension is pushed out from the medicine release hole, so as to control the medicine release. Meanwhile, the glipizide controlled release tablet provided by the invention is mild and durable in release, basically can be completely released in 24 hours, is stable in performance, can be stored for a long time, is simple in preparation process, and is suitable for industrial production.
Detailed Description
The advantages of the invention will be further illustrated by the following examples, it being understood that the examples of the invention are given by way of illustration only and not by way of limitation, and thus, simple modifications of the invention which are intended to fall within the scope of the invention as claimed.
Example 1
(1) Taking 5 parts of glipizide, 5 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 2
(1) Taking 5 parts of glipizide, 10 parts of sodium alginate, 5 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 3
(1) Taking 5 parts of glipizide, 10 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 4
(1) Taking 5 parts of glipizide, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 5
(1) Taking 5 parts of glipizide, 10 parts of sodium alginate, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 6
(1) Taking 5 parts of glipizide, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 7
(1) Taking 5 parts of glipizide, 5 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 8
(1) Taking 5 parts of glipizide, 5 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as a coating solvent, adding 15 parts of polyvinyl alcohol, 8 parts of diethyl phthalate and 400 parts of polyethylene glycol to prepare a semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet cores obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Example 9
(1) Taking 5 parts of glipizide, 5 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as coating solvent, adding 15 parts of polyvinyl alcohol and 400 parts of polyethylene glycol to prepare semipermeable membrane coating liquid, and spraying the coating liquid onto the drug tablet core obtained in the step (1) to form a coated tablet;
(3) Aging the coated tablet, and performing laser drilling.
Example 10
(1) Taking 5 parts of glipizide, 5 parts of sodium alginate, 10 parts of polyoxyethylene, 2 parts of mannitol, 4 parts of sodium dodecyl sulfate, 1 part of carnauba wax, 0.3 part of polyvinylpyrrolidone and 0.1 part of magnesium stearate, uniformly mixing, adding an adhesive to prepare a soft material, drying, granulating, adding a lubricant to mix, and tabletting to obtain a medicine tablet core;
(2) Using acetone-water solution as coating solvent, adding diethyl phthalate 8 parts and polyethylene glycol 400 parts to prepare semipermeable membrane coating liquid, spraying the coating liquid onto the drug tablet core obtained in the step (1) to form coated tablets;
(3) Aging the coated tablet, and performing laser drilling.
Verification example 1 evaluation of in vitro Release degree
The conditions for the release measurement were C18 column, mobile phase, phosphate buffer (13.8 g of sodium dihydrogen phosphate was dissolved in water and diluted to 1000mL, pH was adjusted to 6.0 with 2mol/L sodium hydroxide), methanol (55:45), and detection wavelength: 225nm. The release rate was measured by a standard curve method, according to the release rate measurement method (second part of Chinese pharmacopoeia, appendix XD first method), by using a dissolution rate measurement method second method device, using phosphate buffer (taking 6.8g of monopotassium phosphate, adding an appropriate amount of water for dissolution, adding 190mL of 0.2mol/L sodium hydroxide solution, adding about to 900mL of water, adjusting pH to 7.5 with 0.2mol/L sodium hydroxide solution, adding 1000mL of water, mixing uniformly), taking 900mL of solution as dissolution medium at a rotation speed of 50 revolutions, taking 9mL of solution respectively in 2,4, 8, 12, 16, 20 and 24 hours according to the law, and immediately supplementing 9mL of phosphate buffer preheated to 37C, filtering, and measuring the release rate, as shown in Table 1.
TABLE 1 degree of Release in vitro (%)
| Group of | 2h | 4h | 8h | 12h | 16h | 20h | 24h |
| Example 1 | 39.5 | 75.2 | 95.4 | 96.1 | 98.2 | 99.3 | 99.9 |
| Example 2 | 27.8 | 56.4 | 72.8 | 87.5 | 91.4 | 96.8 | 97.3 |
| Example 3 | 32.8 | 61.4 | 85.6 | 89.8 | 94.5 | 97.4 | 98.2 |
| Example 4 | 19.7 | 45.7 | 65.5 | 76.5 | 78.5 | 82.4 | 90.1 |
| Example 5 | 26.5 | 38.5 | 55.6 | 69.4 | 73.5 | 83.8 | 92.3 |
| Example 6 | 29.4 | 45.8 | 50.9 | 56.7 | 68.7 | 79.5 | 89.2 |
| Example 7 | 36.6 | 45.8 | 55.8 | 66.9 | 78.4 | 89.2 | 93.5 |
| Example 8 | 49.5 | 95.2 | 99.4 | 99.3 | 99.2 | 99.5 | 99.1 |
| Example 9 | 34.8 | 64.7 | 75.5 | 86.9 | 91.3 | 94.6 | 95.8 |
| Example 10 | 31.3 | 55.8 | 68.9 | 76.8 | 81.3 | 90.3 | 94.9 |
As can be seen from Table 1, the split components, proportions and contents of example 1 were selected, and the release rate of the obtained glipizide controlled-release tablet was mild and durable, and the release rate was the highest. Examples 2 to 5, which are prepared by changing the ratio of sodium alginate to polyoxyethylene, release slowly and lack permeation enhancers, or examples 6 to 8, which lack surfactants and retarders, release slowly or too quickly, and the prescription of the semipermeable membrane can also affect the release, so that only auxiliary materials with specific ratios can produce beneficial effects. Verification example 2 Release stability study
The samples of example 1 and example 2 were subjected to acceleration (40 ℃ C./relative humidity RH 75%) and long-term (25 ℃ C./relative humidity RH 65%) conditions for the next month, and the release rate in vitro was examined for the trend of change in the release rate according to the release rate evaluation method described above, and the release conditions are shown in Table 2.
TABLE 2 degree of Release in vitro (%)
| Group of | 2h | 4h | 8h | 12h | 16h | 20h | 24h |
| Example 1 | 39.5 | 75.2 | 95.4 | 96.1 | 98.2 | 99.3 | 99.9 |
| Example 1 (acceleration) | 37.8 | 74.3 | 94.5 | 97.2 | 98.9 | 99.5 | 99.3 |
| Example 1 (Long term) | 39.8 | 70.5 | 93.8 | 98.2 | 98.9 | 99.8 | 99.7 |
| Example 2 | 27.8 | 56.4 | 72.8 | 87.5 | 91.4 | 96.8 | 97.3 |
| Example 2 (acceleration) | 29.5 | 59.7 | 75.9 | 80.4 | 86.7 | 90.7 | 90.5 |
| Example 2 (Long term) | 30.6 | 45.5 | 65.7 | 76.8 | 78.9 | 89.3 | 91.3 |
As can be seen from table 2, the release trend of the glipizide controlled-release tablet of example 1 of the present invention was not significantly changed when compared with the release of the glipizide controlled-release tablet under the acceleration condition and the long-term condition under the condition of 0 month, and thus it can be seen that the glipizide controlled-release tablet of example 1 of the present invention has good stability and does not significantly change under the acceleration condition and the long-term storage condition. However, the release condition of the glipizide controlled-release tablet in example 2 under the acceleration condition and the long-term condition is compared with that of the glipizide controlled-release tablet under the condition of 0 month, which shows that the prescription proportion of example 1 is more reasonable.
Although the present invention has been described in detail with reference to the foregoing embodiments, it should be understood by those skilled in the art that the foregoing embodiments may be modified or equivalents to some of the features thereof, and that the modifications or substitutions do not depart from the spirit of the embodiments of the present invention.
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| WO2004098572A1 (en) * | 2003-05-06 | 2004-11-18 | Ranbaxy Laboratories Limited | Biphasic release of glipizide from monocompartment osmotic dosage form |
| CN104414992A (en) * | 2013-08-22 | 2015-03-18 | 合肥华方医药科技有限公司 | Glipizide osmotic pump controlled release tablet |
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| WO2003103637A2 (en) * | 2002-01-10 | 2003-12-18 | Ranbaxy Laboratories Limited | Modified release, multiple unit drug delivery systems |
| CN103565772A (en) * | 2012-08-10 | 2014-02-12 | 石药集团中奇制药技术（石家庄）有限公司 | Glipizide controlled release composition and preparation method thereof |
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| WO2004098572A1 (en) * | 2003-05-06 | 2004-11-18 | Ranbaxy Laboratories Limited | Biphasic release of glipizide from monocompartment osmotic dosage form |
| CN104414992A (en) * | 2013-08-22 | 2015-03-18 | 合肥华方医药科技有限公司 | Glipizide osmotic pump controlled release tablet |
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