CN117530917B - Bupleurum root suppository - Google Patents
Bupleurum root suppository Download PDFInfo
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- CN117530917B CN117530917B CN202410028326.9A CN202410028326A CN117530917B CN 117530917 B CN117530917 B CN 117530917B CN 202410028326 A CN202410028326 A CN 202410028326A CN 117530917 B CN117530917 B CN 117530917B
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- China
- Prior art keywords
- polyoxyethylene ether
- castor oil
- polysorbate
- bupleurum
- parts
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- 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.)
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- 241000202726 Bupleurum Species 0.000 title claims abstract description 51
- 239000000829 suppository Substances 0.000 title claims abstract description 45
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 79
- 239000003814 drug Substances 0.000 claims abstract description 61
- 239000004359 castor oil Substances 0.000 claims abstract description 57
- 235000019438 castor oil Nutrition 0.000 claims abstract description 57
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims abstract description 57
- 229920000056 polyoxyethylene ether Polymers 0.000 claims abstract description 56
- 229940051841 polyoxyethylene ether Drugs 0.000 claims abstract description 55
- 229940079593 drug Drugs 0.000 claims abstract description 47
- 229920001577 copolymer Polymers 0.000 claims abstract description 35
- 229920000136 polysorbate Polymers 0.000 claims abstract description 27
- 229950008882 polysorbate Drugs 0.000 claims abstract description 27
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims abstract description 26
- 229940083466 soybean lecithin Drugs 0.000 claims abstract description 26
- 239000000341 volatile oil Substances 0.000 claims abstract description 23
- 239000002202 Polyethylene glycol Substances 0.000 claims abstract description 20
- 229920001223 polyethylene glycol Polymers 0.000 claims abstract description 20
- 235000011187 glycerol Nutrition 0.000 claims description 31
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 23
- 229940068918 polyethylene glycol 400 Drugs 0.000 claims description 16
- 229920001213 Polysorbate 20 Polymers 0.000 claims description 14
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 14
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 14
- 229940068977 polysorbate 20 Drugs 0.000 claims description 14
- 229940110456 cocoa butter Drugs 0.000 claims description 12
- 235000019868 cocoa butter Nutrition 0.000 claims description 12
- 240000007817 Olea europaea Species 0.000 claims description 11
- 229920001219 Polysorbate 40 Polymers 0.000 claims description 9
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 claims description 9
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 claims description 9
- 229940101027 polysorbate 40 Drugs 0.000 claims description 9
- 101001109993 Artemia salina 60S acidic ribosomal protein P2 Proteins 0.000 claims description 8
- 239000011248 coating agent Substances 0.000 claims description 2
- 238000000576 coating method Methods 0.000 claims description 2
- 239000002585 base Substances 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 abstract description 30
- 239000008280 blood Substances 0.000 abstract description 5
- 210000004369 blood Anatomy 0.000 abstract description 5
- 206010034912 Phobia Diseases 0.000 abstract description 2
- 208000019899 phobic disease Diseases 0.000 abstract description 2
- 208000019505 Deglutition disease Diseases 0.000 abstract 1
- 238000012360 testing method Methods 0.000 description 31
- 239000000203 mixture Substances 0.000 description 20
- 238000009472 formulation Methods 0.000 description 17
- 230000000694 effects Effects 0.000 description 13
- BAPJBEWLBFYGME-UHFFFAOYSA-N Methyl acrylate Chemical compound COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 description 8
- 238000002844 melting Methods 0.000 description 8
- 230000008018 melting Effects 0.000 description 8
- 239000000047 product Substances 0.000 description 8
- 238000003756 stirring Methods 0.000 description 8
- 230000001186 cumulative effect Effects 0.000 description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 238000011835 investigation Methods 0.000 description 5
- JQWAHKMIYCERGA-UHFFFAOYSA-N (2-nonanoyloxy-3-octadeca-9,12-dienoyloxypropoxy)-[2-(trimethylazaniumyl)ethyl]phosphinate Chemical compound CCCCCCCCC(=O)OC(COP([O-])(=O)CC[N+](C)(C)C)COC(=O)CCCCCCCC=CCC=CCCCCC JQWAHKMIYCERGA-UHFFFAOYSA-N 0.000 description 4
- 241000283973 Oryctolagus cuniculus Species 0.000 description 4
- 230000009286 beneficial effect Effects 0.000 description 4
- 239000013642 negative control Substances 0.000 description 4
- 239000013641 positive control Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000002511 suppository base Substances 0.000 description 4
- PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 description 3
- 208000031636 Body Temperature Changes Diseases 0.000 description 3
- 230000036760 body temperature Effects 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 238000000465 moulding Methods 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 239000008347 soybean phospholipid Substances 0.000 description 3
- 206010037660 Pyrexia Diseases 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 210000000436 anus Anatomy 0.000 description 2
- 230000001627 detrimental effect Effects 0.000 description 2
- 238000004945 emulsification Methods 0.000 description 2
- 235000019197 fats Nutrition 0.000 description 2
- 239000012467 final product Substances 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000007689 inspection Methods 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 229940068968 polysorbate 80 Drugs 0.000 description 2
- 238000013112 stability test Methods 0.000 description 2
- 241000207836 Olea <angiosperm> Species 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 241000779819 Syncarpia glomulifera Species 0.000 description 1
- 230000001133 acceleration Effects 0.000 description 1
- 230000001754 anti-pyretic effect Effects 0.000 description 1
- 235000014121 butter Nutrition 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical class [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 125000002091 cationic group Chemical group 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 description 1
- 201000009240 nasopharyngitis Diseases 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000001739 pinus spp. Substances 0.000 description 1
- -1 polyoxyethylene Polymers 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000007493 shaping process Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 229940036248 turpentine Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
- A61K9/025—Suppositories; Bougies; Bases therefor; Ovules characterised by shape or structure, e.g. hollow layered, coated
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
- A61K36/233—Bupleurum
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61K9/0031—Rectum, anus
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Alternative & Traditional Medicine (AREA)
- Pain & Pain Management (AREA)
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- Medicinal Preparation (AREA)
Abstract
Embodiments of the present application provide bupleurum root suppositories, including: the drug core and the quick release layer, wherein the quick release layer is wrapped on the surface of the drug core; the drug core and the quick release layer together comprise: the bupleurum volatile oil is 1 part by mass and the suppository soft base is 6-15 parts by mass; the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate are 1-2; the total mass part of the methyl acrylate-dimethyl acrylic acid carbamate copolymer, the soybean lecithin and the glycerol is 0.5-1. The application can quickly release part of active ingredients in a short time, slowly release the rest of active ingredients, and can quickly and continuously maintain the blood concentration. Because bupleurum suppositories of the present application do not need to be orally taken, are friendly to people with drug phobia and dysphagia.
Description
Technical Field
The application relates to the field of medicines, in particular to bupleurum root suppositories.
Background
Common cold fever is a clinical common disorder, and according to data, children under 6 years old are shown to have an average of 6-8 times per year, and older children and adults have an average of 2-4 times per year.
The bupleurum root is used as a common medicine for treating cold and fever, and the currently developed medicine formulation mainly comprises injection, dripping pill, medicinal granules, tablets and the like. However, the injection is inconvenient to use, and the oral dosage form is unfavorable for the people with difficult oral administration, so that a new bupleurum dosage form is needed.
Disclosure of Invention
In view of the above, the present application provides bupleurum suppositories to at least partially solve the above problems.
In order to achieve the above purpose, the present application is realized by the following technical scheme:
the bupleurum root suppository of the application comprises: the quick-release coating is wrapped on the surface of the drug core;
the drug core and the immediate release layer together comprise:
the bupleurum volatile oil is 1 part by mass and the suppository soft base is 6-15 parts by mass;
the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate are 1-2;
the total mass part of the methyl acrylate-dimethyl acrylic acid carbamate copolymer, the soybean lecithin and the glycerol is 0.5-1.
For the mass parts of the suppository soft base, 6 to 15 parts means any value ranging from 6 parts to 15 parts, for example, 6 parts, 7 parts, 7.5 parts, 8 parts, 9 parts, 9.5 parts, 10 parts, 11 parts, 12 parts, 12.5 parts, 13 parts, 14 parts and 15 parts.
For the total mass parts of polyethylene glycol, castor oil polyoxyethylene ether and polysorbate, 1 to 2 parts means any value ranging from 1 part to 2 parts, for example, 1 part, 1.2 parts, 1.4 parts, 1.5 parts, 1.6 parts, 1.7 parts, 1.8 parts, 1.9 parts and 2 parts.
For the total mass parts of methyl acrylate-urethane dimethacrylate copolymer, soybean lecithin and glycerin, 0.5-1 part means any value ranging from 0.5 part to 1 part, for example, 0.5 part, 0.6 part, 0.7 part, 0.8 part, 0.9 part and 1 part.
Preferably, when the polyethylene glycol is polyethylene glycol 400, the mass ratio of the polyethylene glycol 400 to the castor oil polyoxyethylene ether in the drug core and the quick release layer is 1:1, and the mass ratio of the castor oil polyoxyethylene ether to the polysorbate is 1:0.25-0.8.
Specifically, when the polyethylene glycol is polyethylene glycol 400, the mass ratio of castor oil polyoxyethylene ether to polysorbate in the drug core and the immediate release layer is any value ranging from 1:0.25 to 1:0.8, such as 1:0.25, 1:0.3, 1:0.35, 1:0.4, 1:0.45, 1:0.5, 1:0.55, 1:0.6, 1:0.65, 1:0.7, 1:0.75, and 1:0.8.
Preferably, when the polysorbate is polysorbate 20, the mass ratio of the castor oil polyoxyethylene ether in the drug core and the quick release layer to the polysorbate 20 is 1:0.3-0.5.
For the mass ratio of castor oil polyoxyethylene ether and polysorbate 20, 1:0.3-0.5 refers to any value in the range of 1:0.3 to 1:0.5, such as 1:0.3, 1:0.32, 1:0.34, 1:0.36, 1:0.38, 1:0.4, 1:0.42, 1:0.44, 1:0.46, 1:0.48, and 1:0.5.
It is understood that when the polysorbate is polysorbate 20, the ratio of the total parts by mass of polyethylene glycol 400, castor oil polyoxyethylene ether and polysorbate 20 in the drug core and immediate release layer to the total parts by mass of polyethylene glycol 400, castor oil polyoxyethylene ether and polysorbate 20 in the immediate release layer is 1.5:1.
Preferably, when the polysorbate is polysorbate 40, the mass ratio of the castor oil polyoxyethylene ether in the drug core and the quick release layer to the polysorbate 40 is 1:0.5-0.8.
For the mass ratio of castor oil polyoxyethylene ether and polysorbate 40, 1:0.5-0.8 refers to any value in the range of 1:0.5 to 1:0.8, such as 1:0.5, 1:0.55, 1:0.6, 1:0.65, 1:0.7, 1:0.75, and 1:0.8.
It will be appreciated that when the polysorbate is polysorbate 40, the ratio of the total parts by mass of polyethylene glycol 400, castor oil polyoxyethylene ether and polysorbate 40 in the drug core and immediate release layer to the total parts by mass of polyethylene glycol 400, castor oil polyoxyethylene ether and polysorbate 40 in the immediate release layer is 1.5:1.
Preferably, in the drug core, the total mass parts of the methyl acrylate-dimethacrylate copolymer, the soybean lecithin and the glycerin are 0.425-0.95.
For the total mass parts of methyl acrylate-urethane dimethacrylate copolymer, soybean lecithin and glycerin, 0.425-0.95 means any value ranging from 0.425 parts to 0.95 parts, such as 0.425 parts, 0.43 parts, 0.45 parts, 0.47 parts, 0.5 parts, 0.52 parts, 0.55 parts, 0.58 parts, 0.6 parts, 0.62 parts, 0.64 parts, 0.66 parts, 0.68 parts, 0.7 parts, 0.72 parts, 0.74 parts, 0.76 parts, 0.78 parts, 0.8 parts, 0.82 parts, 0.84 parts, 0.85 parts, 0.86 parts, 0.87 parts, 0.88 parts, 0.89 parts, 0.9 parts, 0.91 parts, 0.92 parts, 0.93 parts, 0.94 parts and 0.95 parts.
The ratio of the total mass parts of the methyl acrylate-dimethacrylate copolymer, the soybean lecithin and the glycerin in the drug core to the total mass parts of the methyl acrylate-dimethacrylate copolymer, the soybean lecithin and the glycerin in the quick release layer is 7.5-11:1.
For the ratio of the total mass parts of methyl acrylate-urethane dimethacrylate copolymer, soy lecithin and glycerin in the drug core and immediate release layer, 7.5-11:1 refers to any value in the range of 7.5:1 to 11:1, such as 7.5:1, 7.6:1, 7.8:1, 8:1, 8.2:1, 8.4:1, 8.6:1, 8.8:1, 9:1, 9.2:1, 9.4:1, 9.6:1, 9.8:1, 10:1, 10.2:1, 10.4:1, 10.6:1, 10.8:1 and 11:1.
Preferably, when the suppository base includes cocoa butter and olive, the mass ratio of the cocoa butter to the olive in the drug core and the immediate release layer is 1:0.5-2.
For the mass ratio of cocoa butter to olive butter, 1:0.5-2 refers to any value in the range of 1:0.5 to 1:2, such as 1:0.5, 1:0.6, 1:0.7, 1:0.8, 1:0.9, 1:1, 1:1.1, 1:1.2, 1:1.3, 1:1.4, 1:1.5, 1:1.6, 1:1.7, 1:1.8, 1:1.9, and 1:2.
Preferably, the ratio of the total mass of cocoa butter and olive in the core to the total mass of cocoa butter and olive of the immediate release layer is 3:1.
Preferably, the ratio of the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate in the drug core to the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate in the quick release layer is 1.5:1.
Specifically, the castor oil polyoxyethylene ether of the present application includes: at least one of castor oil polyoxyethylene ether EL10, castor oil polyoxyethylene ether EL12 and castor oil polyoxyethylene ether EL 20. It is understood that the castor oil polyoxyethylene ether may be castor oil polyoxyethylene ether EL10, castor oil polyoxyethylene ether EL12, or a mixture of castor oil polyoxyethylene ether EL10 and castor oil polyoxyethylene ether EL20, or a mixture of castor oil polyoxyethylene ether EL12 and castor oil polyoxyethylene ether EL 20.
Preferably, in the drug core and the immediate release layer,
the mass ratio of the methyl acrylate-dimethacrylate copolymer to the soybean lecithin is 1:0.5;
the mass ratio of the methyl acrylate-dimethyl acrylic acid carbamate copolymer to the glycerol is 1:0.5-1.5.
For the mass ratio of methyl acrylate-urethane dimethacrylate copolymer to glycerol, 1:0.5-1.5 refers to any value in the range of 1:0.5 to 1:1.5, such as 1:0.5, 1:0.6, 1:0.7, 1:0.8, 1:0.9, 1:1, 1:1.1, 1:1.2, 1:1.3, 1:1.4 and 1:1.5.
Preferably, the bupleurum volatile oil in the medicine core is 0.85-0.9 parts by mass.
For the parts by mass of bupleurum volatile oil, 0.85-0.9 means any value in the range of 0.85 to 0.9, such as 0.85, 0.86, 0.87, 0.88, 0.89 and 0.9.
The bupleurum volatile oil of 1 part by mass is extracted from bupleurum crude drug of 7.5-12.5 g. For the amount of bupleurum crude drug, 7.5-12.5g refers to any value in the range of 7.5g to 12.5g, such as 7.5g, 7.6g, 7.7g, 7.8g, 8g, 8.2g, 8.4g, 8.6g, 8.8g, 9g, 9.2g, 9.5g, 9.8g, 10g, 10.2g, 10.5g, 10.7g, 11g, 11.2g, 11.5g, 11.8g, 12g, 12.3g and 12.5g.
The preparation method of the bupleurum suppository comprises the following steps:
preparing a medicine core: uniformly stirring the cocoa butter and olive fat in the drug core; sequentially adding bupleuri radix volatile oil, and stirring; sequentially adding polyethylene glycol 400, castor oil polyoxyethylene ether and polysorbate, and stirring uniformly; and finally adding methyl acrylate-dimethacrylate copolymer, soybean lecithin and glycerin, and stirring uniformly to obtain the final product.
Preparing a quick release layer: uniformly stirring cocoa butter and olive fat in the dosage of the quick release layer; sequentially adding bupleuri radix volatile oil, and stirring; sequentially adding polyethylene glycol 400, castor oil polyoxyethylene ether and polysorbate, and stirring uniformly; and finally adding methyl acrylate-dimethacrylate copolymer, soybean lecithin and glycerin, and stirring uniformly to obtain the final product.
The medicine core and the quick release layer are put into a mould to prepare the suppository.
The bupleurum root suppository is solid at normal temperature. The bupleurum suppository can be used by, but is not limited to, inserting the bupleurum suppository into anus through an appliance so as to soften and dissolve under the action of body temperature.
According to the technical scheme, the bupleurum root suppository is provided, and consists of a medicine core and a quick-release layer wrapped on the surface of the medicine core, wherein the medicine core and the quick-release layer both contain bupleurum root volatile oil. After the bupleurum suppository is inserted into anus, the quick-release layer of the bupleurum suppository can be quickly dissolved and release bupleurum volatile oil in a short time under the action of body temperature. Simultaneously, the medicine core of the bupleurum suppository is gradually softened, dissolved and slowly released with bupleurum volatile oil in the medicine core. The bupleurum volatile oil is released by combining quick release and slow release, so that the bupleurum suppository can reach the blood concentration in a short time, the blood concentration is stable, the peak valley phenomenon is avoided or reduced, and the toxic and side effects are reduced. In addition, the bupleurum root suppository does not need to be orally taken, so that the oral administration difficulty or the compliance of people with drug phobia can be improved.
Drawings
In order to more clearly illustrate the embodiments of the present application or the technical solutions in the prior art, the drawings that are required in the embodiments or the description of the prior art will be briefly described, and it is obvious that the drawings in the following description are some embodiments of the present application, and other drawings may be obtained according to these drawings without inventive effort for a person skilled in the art.
FIG. 1 is a graph showing the results of examining the amount of bupleurum volatile oil used in test example 3 of the present application;
FIG. 2 is a view showing the results of examining the amounts and types of soft base suppositories provided in test example 4 of the present application;
FIG. 3 is a view showing the results of examining the amounts and types of polyethylene glycol and polysorbate used in test example 5 of the present application;
FIG. 4 is a view showing the results of examining the amounts and types of polyoxyethylene castor oil provided in test example 6 of the present application;
FIG. 5 is a view showing the results of examining a methyl acrylate-urethane dimethacrylate copolymer provided in test example 7 of the present application;
FIG. 6 is a view showing the results of examining the amounts and types of soybean lecithin and glycerin provided in test example 8 of the present application;
fig. 7 shows the body temperature change at different time points of the test subjects provided in test example 9 of the present application.
Description of the embodiments
In order to better understand the technical solutions in the embodiments of the present application, the following description will clearly and completely describe the technical solutions in the embodiments of the present application with reference to the drawings in the embodiments of the present application, and it is obvious that the described embodiments are only some embodiments of the present application, but not all embodiments. All other embodiments obtained by a person of ordinary skill in the art based on the embodiments provided herein shall fall within the scope of the embodiments of the present application.
The present application is further described below with reference to specific examples.
Example 1: prescription information
The individual prescription information is shown in table 1. Wherein the polysorbate in prescription 1, prescription 2 and prescription 3 is polysorbate 20; the polysorbate in recipe 4 and recipe 5 was polysorbate 40. The castor oil polyoxyethylene ether in the prescription 1 and the prescription 3 is castor oil polyoxyethylene ether EL12; the castor oil polyoxyethylene ether in the prescription 2 and the prescription 4 is castor oil polyoxyethylene ether EL 10; the castor oil polyoxyethylene ether in the formula 5 is castor oil polyoxyethylene ether EL 20.
Table 1 prescription summary table
Example 2: quality inspection
The samples of each formulation in example 1 were examined for accelerated stability test, weight difference, melting time limit, and in vitro dissolution, and the examination results are shown in table 2.
Table 2 quality inspection results
As can be seen from Table 2, the weight difference of the samples of formulas 1 to 5 is not more than 10, so that the amounts of the active components of the samples of formulas 1 to 5 are more uniform, which is beneficial to ensuring the consistency of the drug effect.
The melting time limit of the quick-release layer of the samples in the prescription 1-5 is 5-8min, and each sample can quickly release the active ingredients in the quick-release layer. The melting time limit of the medicine core of each prescription sample is 105-120min, and the result shows that each sample can slowly release the active ingredients in the medicine core. Thus, a part of active ingredients are released quickly through the drug core, and another part of active ingredients are released through the drug core, so that the drug can be quickly removed, and the blood concentration can be maintained for a long time.
For the in vitro dissolution test, the cumulative release of each prescription sample is within the range of 95% -99% as can be seen from table 2, and the results show that each sample can well release active ingredients, thereby being beneficial to improving the utilization rate of the active ingredients.
In addition, the content detection result of the 6-month accelerated stability test of each prescription sample is in the range of 98% -101%, so that the stability of the sample can be indicated to be good.
The use amount and the type of each component in the prescription are examined, wherein the prescription 1 in the example 1 is a comparative prescription, and specific examination results are shown in examples 3 to 9.
Example 3: investigation of the amount of active substance
The amount of bupleurum volatile oil is examined, and specific information is shown in table 3.
Table 3 investigation of the amount of bupleurum volatile oil
As can be seen from Table 3, the total amounts of active ingredients in the samples of recipe 1, recipe 1-1 and recipe 1-2 are the same. The above formulation differs in that the amounts of active ingredient in the immediate release layer and the drug core are different.
As can be seen from FIG. 1, the samples of the formulations 1-2, which did not release the active ingredient rapidly in a short time, failed to achieve the immediate release effect, because the immediate release layer was not added with bupleurum volatile oil.
Compared with the dosage of bupleurum volatile oil in the sample of the prescription 1, the dosage of bupleurum volatile oil in the quick-release layer in the sample of the prescription 1-1 is more, and the dosage of bupleurum volatile oil in the drug core is less. As can be seen from FIG. 1, the samples of formulation 1-1, although capable of rapidly releasing the active ingredient in a short time, had poor slow release due to the low amount of bupleurum volatile oil in the core.
As can be seen from fig. 1, the formulation 1 sample is capable of rapidly releasing a small amount of active ingredient in a short time, reaching an effective concentration in a short time. And then slowly releasing a relatively large amount of the active ingredient so as to maintain the blood concentration in the human body within a stable range for a relatively long time.
Example 4: examination of suppository Soft base
The amount and type of the soft base of the suppository were examined in this example, and specific information is shown in Table 4.
TABLE 4 examination of the amount and types of Soft base of suppositories
As can be seen from Table 4, the amount of soft base suppository in formulas 1-4 is relatively small, and the amount of soft base suppository in formulas 1-5 is relatively large. The amount of the suppository base used in prescription 1 and prescriptions 1-3 is the same, but the composition of the soft base is different.
The samples of formulas 1-4 were not easily made into suppositories during preparation, and were poorly formable. Resulting in a short period of active ingredient release when examined for the melting time limit, as shown in fig. 2.
The samples of formulas 1-5 are well formed in the preparation process, but the melting time limit of the samples is longer than 300 minutes, and the requirement that the active ingredients are released in a short time cannot be met, as shown in figure 2.
The stearates and hydrogenated vegetable oils of formulas 1-3 are all commonly used components in suppository base. As shown in FIG. 2, although the melting time period of the samples of formulas 1-3 is relatively good, the variance of the melting time period is large, indicating that the active ingredients in the system are not uniformly mixed, which can easily lead to inaccurate control of drug release.
In conclusion, the soft base of the suppositories with different components and different dosages has great influence on the melting time limit and the formability of the bupleurum suppositories. The cocoa butter and olives of the present application, when present in a range of amounts, aid in the shaping of the suppository and the release of the active ingredient.
Example 5: investigation of polyethylene glycol and Polysorbate
The amounts and types of polyethylene glycol and polysorbate were examined in this example, and specific information is shown in Table 5.
TABLE 5 investigation of polyethylene glycol and Polysorbate
As can be seen from table 5 and fig. 3:
the amounts of polyethylene glycol 400 and polysorbate 20 used in the samples of formulas 1-7 were relatively low compared to formula 1. The cumulative release of the active ingredient in the formulation is low, and the results indicate that the low amounts of polyethylene glycol 400 and polysorbate 20 result in poor emulsification of the matrix, which is detrimental to rapid release of the active ingredient in the immediate release layer.
The amounts of polyethylene glycol 400 and polysorbate 20 used in the samples of formulas 1-8 were relatively high compared to formula 1. The samples of the formulas 1-8 can release a large amount of active ingredients in a short time, and have good quick release effect, but poor subsequent slow release effect.
In comparison to formulation 1, samples of formulations 1-6 used polyethylene glycol 2000 and polysorbate 80, and the other components and amounts were the same as those of formulation 1. However, the cumulative release of the sample still does not reach 80% at 12h, and the release requirement cannot be met. The results show that the emulsification effect of polyethylene glycol 2000 and polysorbate 80 is less than that of polyethylene glycol 400 and polysorbate 20, and the release of the active ingredients is not facilitated.
The use of a certain amount of polyethylene glycol 400 and polysorbate 20 in the sample of formulation 1 can provide a cumulative release of about 50% of the active ingredient at 3 hours, followed by a release of about 50% of the active ingredient within 9 hours, to achieve a combined immediate release and sustained release effect.
In summary, the amounts and types of polyethylene glycol and polysorbate may affect the emulsifying effect of the matrix on the suppository base, and thus the release effect of the active ingredient.
Example 6: examination of Castor oil Polyoxyethylene Ether
The amount and type of the castor oil polyoxyethylene ether were examined in this example, and specific information is shown in table 6.
TABLE 6 examination of castor oil polyoxyethylene ethers
As is clear from Table 6, the samples of the formulations 1 to 10 were not added with castor oil polyoxyethylene ether EL 12. As can be seen from FIG. 4, the cumulative release of the sample at 12 hours still does not reach 80%, and the release effect is poor.
The castor oil polyoxyethylene ether EL12 was used in the samples of formulas 1-11 in a smaller amount than the sample of formula 1. As can be seen from fig. 4, the samples of formulas 1-11 have a relatively better release effect than the samples of formulas 1-10, indicating that castor oil polyoxyethylene ether EL12 is beneficial for releasing the active ingredient; the cumulative release of the samples of prescription 1-11 is still much lower than that of the sample of prescription 1.
Compared with the sample of the prescription 1, the dosage of the castor oil polyoxyethylene ether EL12 in the sample of the prescription 1-12 is more. As can be seen from fig. 4, the samples of formulas 1 to 12 have a cumulative release rate of about 80% at 3 hours, and the release effect is remarkable, but the release time is short because the active ingredient is released too fast.
The castor oil polyoxyethylene ether EL 90 was used in the samples of the formulations 1 to 9, and the other components and amounts were the same as those of the sample of the formulation 1. As can be seen from FIG. 4, the release effect of the samples of formulations 1-9 is better than that of formulations 1-12, and a large amount of active substances can be released in a short time, but the slow release time is shorter and the slow release effect is worse.
The sample of formulation 1 was able to release a small amount of active ingredient quickly followed by a large amount of active ingredient slowly to maintain a good release rate.
Example 7: examination of methyl acrylate-urethane dimethacrylate copolymer
The methyl acrylate-urethane dimethacrylate copolymer of this example was examined, and specific information is shown in Table 7.
TABLE 7 examination of methyl acrylate-dimethacrylate copolymers
No methyl acrylate-urethane dimethacrylate copolymer was added to both the drug core and the immediate release layer of samples of formulas 1-14. As can be seen from FIG. 5, the contents of the samples of formulas 1-14 were significantly reduced after the accelerated test, and the product stability was poor.
The drug core and immediate release layer of the samples of formulas 1-16 used relatively more methyl acrylate-urethane dimethacrylate copolymer than the sample of formula 1. As can be seen from FIG. 5, the samples of formulas 1-16 showed less variation in content after the accelerated test, indicating good product stability. However, the content of the sample in recipe 1 was comparable to that in the samples in recipes 1 to 16, and the difference between the two recipes was only that the amount of methyl acrylate-urethane dimethacrylate copolymer was used, which means that the use of a larger amount of methyl acrylate-urethane dimethacrylate copolymer did not make the sample more stable, and that the amount of methyl acrylate-urethane dimethacrylate copolymer in the sample in recipe 1 was already able to provide a good stabilizing effect for the product.
As can be seen from the comparison of the 6-month acceleration test results of the samples of the formulas 1-14 and 1-16, the addition of the methyl acrylate-dimethacrylate copolymer to the bupleurum suppository type is beneficial to improving the stability of the samples.
The drug core of the samples of the prescriptions 1-15 uses methyl acrylate-dimethyl acrylic acid urethane copolymer, the immediate release layer uses methyl acrylate, and the two components are used in a smaller amount, and the other components and the amounts are the same as the sample of the prescriptions 1. As can be seen from FIG. 5, the reduction in the contents of the samples of formulas 1-15 after the accelerated test is more pronounced, the contents of the samples of formulas 1-15 are slightly higher than the contents of the samples of formulas 1-14, and the contents of the samples of formulas 1-15 are lower than the contents of the sample of formula 1. This indicates that the methyl acrylate-urethane dimethacrylate copolymer and methyl acrylate help to improve product stability, but the effect of improving stability is not obvious, and is not as good as that of the sample of formula 1, indicating that the use of a certain amount of methyl acrylate-urethane dimethacrylate copolymer in both the immediate release layer and the drug core helps to improve the stability of the sample.
The drug core and immediate release layer in the samples of formulas 1-13 were each methyl acrylate, the other components and amounts were the same as in the sample of formula 1. As can be seen from FIG. 5, the contents of the samples of formulas 1-13 were also reduced after the accelerated test, indicating that the methyl acrylate was not as stable as the methyl acrylate-urethane dimethacrylate copolymer.
Example 8: investigation of soybean lecithin and Glycerol
The amounts and types of soybean lecithin and glycerin were examined in this example, and specific information is shown in Table 8.
TABLE 8 examination of soybean lecithin and glycerin
The samples of formulas 1-19 were less soy lecithin and glycerol than formula 1. As can be seen from FIG. 6, the samples of formulas 1-19 were significantly reduced in content after accelerated testing, indicating that the low amounts of soy lecithin and glycerol are detrimental to product stability.
Compared with prescription 1, the soybean lecithin and glycerin in the samples of prescriptions 1-20 are used in a larger amount. As can be seen from FIG. 6, the variation of the sample contents of the prescriptions 1-20 is small after the accelerated test, which indicates that the dosage is favorable for the stability of the product. The difference between the prescription 1-20 samples and the prescription 1 sample is that the soybean lecithin and the glycerol are used in a large amount, but the content change of the prescription 1-20 samples and the prescription 1 samples is smaller, which shows that the soybean lecithin and the glycerol are used in a large amount, so that the samples are not more stable, and the soybean lecithin and the glycerol in the prescription 1 can meet the stability of the samples.
Glycerin was used in the drug core of samples 1-18 and egg yolk lecithin was used in the immediate release layer. As can be seen from FIG. 6, the content of samples 1 to 18 was significantly reduced after the accelerated test, indicating that the stability of the products using egg yolk lecithin and glycerol was poor.
The drug core and the quick release layer of the sample in the prescription 1-17 both use egg yolk lecithin and propylene glycol, and other components and the dosage are the same as those of the sample in the prescription 1, and as can be seen from fig. 6, the content of the sample in the prescription 1-17 is obviously reduced after the accelerated test, which shows that the combination of the egg yolk lecithin and the propylene glycol is better than the combination of the soybean lecithin and the glycerol, and the stability of the product cannot be better ensured.
Example 9: evaluation of pharmacodynamics
Test object: healthy, adult rabbits were selected, from which a group of rabbits was randomly drawn as a blank control group.
Constructing a heating model: turpentine was injected subcutaneously into the backs of rabbits except the blank group. When the temperature detected by the thermometer exceeds 40.5 ℃, the molding was successful.
Grouping: the rabbits with similar temperature (+ -0.5 ℃) after successful molding are divided into a test group, a positive control group, a negative control group and a molding group at random and equal quantity.
The specific test: the test group was given the sample of formula 1, the commercial bupleurum particles were given to the cationic control group, the blank suppositories except for the active ingredient in formula 1 were given to the negative control group, and the blank group and the model group were not given any drug.
The rectal temperatures of the test, positive control, negative control and blank test subjects were measured half an hour after administration, followed by measuring the rectal temperatures of the above test subjects in each group every 3 hours. The body temperature change at different time points for each group of subjects is shown in figure 7.
As can be seen from fig. 7, the rectal temperature of the test group and the test subjects of the positive control group was significantly reduced after the first administration compared with the rectal temperature before the administration, and the rectal temperature of the test group was gradually stabilized and tended to be normal body temperature within 3 to 12 hours after the administration, but the body temperature change of the test group was more remarkable than that of the test subjects of the positive control group. The subjects in the negative control group showed a small range of change in rectal temperature after the first administration and rectal temperature before the administration, indicating that the blank suppository had no antipyretic effect. The range of rectal temperature change of the test subjects in the blank control group is smaller, which indicates that the physical state of each group of test subjects is good.
It should also be noted that the term "comprises," "comprising," or any other variation thereof is intended to cover a non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements does not include only those elements but may include other elements not expressly listed or inherent to such process, method, article, or apparatus. Without further limitation, an element defined by the phrase "comprising at least one of the elements" does not exclude the presence of additional identical elements in a process, method, article or apparatus that comprises the element.
In this specification, each embodiment is described in a progressive manner, and identical and similar parts of each embodiment are all referred to each other, and each embodiment mainly describes differences from other embodiments.
Finally, it should be noted that the foregoing description is only an example of the present application, and is merely for illustrating the technical solution of the present invention, not for limiting the present application. Various modifications and changes may be made to the present application by those skilled in the art. Any modifications, equivalent substitutions, improvements, etc. which are within the spirit and principles of the present application are intended to be included within the scope of the claims of the present application.
Claims (7)
1. Bupleurum root suppository, which is characterized by comprising: the quick-release coating is wrapped on the surface of the drug core;
the medicine core comprises bupleuri radix volatile oil, suppository soft base, polyethylene glycol, castor oil polyoxyethylene ether, polysorbate, methyl acrylate-dimethacrylate copolymer, soybean lecithin and glycerol;
the quick release layer comprises bupleurum volatile oil, suppository soft base, polyethylene glycol, castor oil polyoxyethylene ether, polysorbate, methyl acrylate-dimethacrylate urethane copolymer, soybean lecithin and glycerol;
the drug core and the quick release layer comprise the following components in parts by mass:
the bupleurum volatile oil is 1 part by mass and the suppository soft base is 6-15 parts by mass;
the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate are 1-2;
0.5-1 parts by mass of methyl acrylate-dimethacrylate urethane copolymer, soybean lecithin and glycerin;
in the drug core, the total mass parts of the methyl acrylate-dimethyl acrylic acid carbamate copolymer, the soybean lecithin and the glycerin are 0.425-0.95;
the suppository soft base is cocoa butter and olive, and the mass ratio of the cocoa butter to the olive in the drug core and the quick release layer is 1:0.5-2;
the weight portion of the bupleurum volatile oil in the medicine core is 0.85 to 0.9;
wherein,
the polyethylene glycol is polyethylene glycol 400;
the castor oil polyoxyethylene ether is selected from castor oil polyoxyethylene ether EL10, castor oil polyoxyethylene ether EL12 and castor oil polyoxyethylene ether EL20;
the polysorbate is selected from polysorbate 20 and polysorbate 40.
2. The bupleurum suppository of claim 1,
the mass ratio of the polyethylene glycol 400 to the castor oil polyoxyethylene ether in the drug core and the quick release layer is 1:1, and the mass ratio of the castor oil polyoxyethylene ether to the polysorbate is 1:0.25-0.8.
3. The bupleurum suppository of claim 2,
the mass ratio of the castor oil polyoxyethylene ether to the polysorbate 20 in the drug core and the quick release layer is 1:0.3-0.5.
4. The bupleurum suppository of claim 2,
the mass ratio of the castor oil polyoxyethylene ether to the polysorbate 40 in the drug core and the quick release layer is 1:0.5-0.8.
5. The bupleurum suppository of claim 1,
the ratio of the total mass parts of the methyl acrylate-dimethacrylate copolymer, the soybean lecithin and the glycerin in the drug core to the total mass parts of the methyl acrylate-dimethacrylate copolymer, the soybean lecithin and the glycerin in the quick release layer is 7.5-11:1.
6. The bupleurum suppository of claim 1,
the ratio of the total mass of cocoa butter and olive in the core to the total mass of cocoa butter and olive in the immediate release layer is 3:1.
7. The bupleurum suppository of claim 1,
the ratio of the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate in the drug core to the total mass parts of the polyethylene glycol, the castor oil polyoxyethylene ether and the polysorbate in the quick release layer is 1.5:1;
and/or the number of the groups of groups,
in the drug core and the immediate release layer,
the mass ratio of the methyl acrylate-dimethacrylate copolymer to the soybean lecithin is 1:0.5;
the mass ratio of the methyl acrylate-dimethyl acrylic acid carbamate copolymer to the glycerol is 1:0.5-1.5.
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