NL2030846B1 - Pharmaceutical composition for preventing atherosclerosis and application thereof - Google Patents
Pharmaceutical composition for preventing atherosclerosis and application thereof Download PDFInfo
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- NL2030846B1 NL2030846B1 NL2030846A NL2030846A NL2030846B1 NL 2030846 B1 NL2030846 B1 NL 2030846B1 NL 2030846 A NL2030846 A NL 2030846A NL 2030846 A NL2030846 A NL 2030846A NL 2030846 B1 NL2030846 B1 NL 2030846B1
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- pharmaceutical composition
- parts
- humulene
- cinnamate
- atherosclerosis
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- 201000001320 Atherosclerosis Diseases 0.000 title claims abstract description 62
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 55
- CCRCUPLGCSFEDV-UHFFFAOYSA-N cinnamic acid methyl ester Natural products COC(=O)C=CC1=CC=CC=C1 CCRCUPLGCSFEDV-UHFFFAOYSA-N 0.000 claims abstract description 36
- CCRCUPLGCSFEDV-BQYQJAHWSA-N methyl trans-cinnamate Chemical compound COC(=O)\C=C\C1=CC=CC=C1 CCRCUPLGCSFEDV-BQYQJAHWSA-N 0.000 claims abstract description 36
- BWXDHBQGBNPJMN-UHFFFAOYSA-N Lupeol palmitate Natural products C12CCC3C4C(C(C)=C)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(OC(=O)CCCCCCCCCCCCCCC)C1(C)C BWXDHBQGBNPJMN-UHFFFAOYSA-N 0.000 claims abstract description 35
- BWXDHBQGBNPJMN-VBHWJLTNSA-N [(1r,3ar,5ar,5br,7ar,9s,11ar,11br,13ar,13br)-3a,5a,5b,8,8,11a-hexamethyl-1-prop-1-en-2-yl-1,2,3,4,5,6,7,7a,9,10,11,11b,12,13,13a,13b-hexadecahydrocyclopenta[a]chrysen-9-yl] hexadecanoate Chemical compound C([C@@]1(C)CC[C@H]([C@@H]1[C@H]1CC[C@H]23)C(C)=C)C[C@@]1(C)[C@]3(C)CC[C@@H]1[C@]2(C)CC[C@H](OC(=O)CCCCCCCCCCCCCCC)C1(C)C BWXDHBQGBNPJMN-VBHWJLTNSA-N 0.000 claims abstract description 35
- 239000002994 raw material Substances 0.000 claims abstract description 28
- 239000003814 drug Substances 0.000 claims description 15
- HAVYZKHVTLAPDZ-RCHZWEEESA-N beta-Humulene Natural products C\C1=C\CC(C)(C)\C=C\CC(=C)CCC1 HAVYZKHVTLAPDZ-RCHZWEEESA-N 0.000 claims 5
- HAVYZKHVTLAPDZ-PRUKLFJYSA-N β-humulene Chemical compound C\C1=C\CC(C)(C)\C=C/CC(=C)CCC1 HAVYZKHVTLAPDZ-PRUKLFJYSA-N 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 15
- 230000007774 longterm Effects 0.000 abstract description 4
- 238000003908 quality control method Methods 0.000 abstract description 4
- 241000700159 Rattus Species 0.000 description 33
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 13
- 210000002376 aorta thoracic Anatomy 0.000 description 12
- FAMPSKZZVDUYOS-UHFFFAOYSA-N alpha-Caryophyllene Natural products CC1=CCC(C)(C)C=CCC(C)=CCC1 FAMPSKZZVDUYOS-UHFFFAOYSA-N 0.000 description 10
- 102000007330 LDL Lipoproteins Human genes 0.000 description 9
- 108010007622 LDL Lipoproteins Proteins 0.000 description 9
- 229940079593 drug Drugs 0.000 description 9
- BXWQUXUDAGDUOS-UHFFFAOYSA-N gamma-humulene Natural products CC1=CCCC(C)(C)C=CC(=C)CCC1 BXWQUXUDAGDUOS-UHFFFAOYSA-N 0.000 description 9
- QBNFBHXQESNSNP-UHFFFAOYSA-N humulene Natural products CC1=CC=CC(C)(C)CC=C(/C)CCC1 QBNFBHXQESNSNP-UHFFFAOYSA-N 0.000 description 9
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 9
- 239000000203 mixture Substances 0.000 description 8
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 description 6
- 210000004618 arterial endothelial cell Anatomy 0.000 description 5
- 239000000969 carrier Substances 0.000 description 5
- 210000004026 tunica intima Anatomy 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- 230000003143 atherosclerotic effect Effects 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- 230000000007 visual effect Effects 0.000 description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 238000000386 microscopy Methods 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 208000037260 Atherosclerotic Plaque Diseases 0.000 description 1
- -1 B-humulene Chemical compound 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 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
- 208000017170 Lipid metabolism disease Diseases 0.000 description 1
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 108010009736 Protein Hydrolysates Proteins 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- 229930006000 Sucrose Natural products 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
- 208000007536 Thrombosis Diseases 0.000 description 1
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- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 235000010419 agar Nutrition 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 230000036770 blood supply Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
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- 230000004064 dysfunction Effects 0.000 description 1
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- 238000002474 experimental method Methods 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- UHUSDOQQWJGJQS-UHFFFAOYSA-N glycerol 1,2-dioctadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(CO)OC(=O)CCCCCCCCCCCCCCCCC UHUSDOQQWJGJQS-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- 235000009200 high fat diet Nutrition 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229960004844 lovastatin Drugs 0.000 description 1
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 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
- 239000001814 pectin Substances 0.000 description 1
- 235000010987 pectin Nutrition 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
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- 238000012453 sprague-dawley rat model Methods 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- A61K31/01—Hydrocarbons
- A61K31/015—Hydrocarbons carbocyclic
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
Abstract
The present disclosure belongs to a pharmaceutical composition for preventing atherosclerosis and an application thereof. The pharmaceutical composition is prepared from the following raw materials: lupeol palmitate, B-humulene and methyl trans- cinnamate. The present disclosure has the advantages of being capable of effectively preventing atherosclerosis, obvious in effect, stable in quality control and suitable for long-term administration of patients.
Description
PHARMACEUTICAL COMPOSITION FOR PREVENTING
ATHEROSCLEROSIS AND APPLICATION THEREOF
[DI] The present disclosure belongs to the technical field of medicines, and particularly relates to a pharmaceutical composition for preventing atherosclerosis and an application thereof.
[02] Atherosclerosis is a type of arterial sclerosis, which mainly occurs in the intima of large and medium arteries, and contains yellow atheromatous plaque substances such as cholesterol and glucolipid. The disease is mostly caused by lipid metabolism disorders and neurovascular dysfunction, often leading to thrombosis and blood supply disorder, etc. Atherosclerosis is more common in men over the age of 40 and postmenopausal women. The disease is often accompanied by hypertension, hypercholesterolemia or diabetes, and it is a common and frequently-occurring disease, with a high mortality and disability rate, which seriously endangers the life and health of humans. It is common in mental workers and is one of the main causes of death in the elderly.
[03] At present, there is no better drug to prevent the occurrence and development of atherosclerosis. Generally it is prevented by a reasonable diet, exercise, and rest, but the effect is not ideal.
[04] The present disclosure aims to overcome the defects in the prior art and provide a pharmaceutical composition for preventing atherosclerosis, which is stable in quality control, safe, effective, natural, non-toxic and suitable for long-term administration, and an application thereof.
[05] The object of the present disclosure is realized as follows: a pharmaceutical composition is prepared from the following raw materials: lupeol palmitate, B-humulene and methyl trans-cinnamate.
[06] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1-100 parts of lupeol palmitate, 8-100 parts of B- humulene and 10-100 parts of methyl trans-cinnamate.
[07] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1-80 parts of lupeol palmitate, 8-80 parts of B-
S humulene and 10-80 parts of methyl trans-cinnamate.
[08] The pharmaceutical composition for preventing atherosclerosis 1s prepared from the following raw materials: 1-50 parts of lupeol palmitate, 8-50 parts of B- humulene and 10-50 parts of methyl trans-cinnamate.
[09] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1 part of lupeol palmitate, 8 parts of B-humulene and parts of methyl trans-cinnamate.
[10] The present disclosure provides an application of a pharmaceutical composition in preparing a medicament for preventing atherosclerosis.
[11] Lupeol palmitate, B-humulene and methyl trans-cinnamate in the present 15 disclosure can be directly available from the market and can also be obtained by extracting plants.
[12] The raw materials are crushed, sieved, mixed and encapsulated or pressed into tablets respectively according to parts by weight, or are mixed with a pharmaceutically acceptable carrier or diluent and then encapsulated or pressed into tablets. 13] The present disclosure also provides a method for taking the pharmaceutical composition. The dosage of the pharmaceutical composition is 10-15 mg/time for adults, 3 times a day, and the effect of preventing the clinical symptoms of atherosclerosis can be achieved. Particularly, special groups such as pregnant women, etc. need to follow the doctor's advices when taking the pharmaceutical composition, and no special adverse reaction is found at present.
[14] The molecular formula of lupeol palmitate is CisHsoO2, and the molecular weight is 268.2641, and the molecular structure is as follows:
J. a
[15] The molecular formula of B-humulene is CisHas, and the molecular weight 1s 204.36, and the molecular structure is as follows:
J
\ \
[16]
[17] The molecular formula of methyl trans-cinnamate is C10H1002, the molecular weight is 162.19, and the molecular structure is as follows:
[18] \ ) AY
[19] Studies have shown that the composition composed of lupeol palmitate, B- humulene and methyl trans-cinnamate can prevent increase of serum cholesterol, triglyceride and low-density lipoprotein, the formation of arterial plaques, damage of the arterial intima and damage of arterial endothelial cells in the atherosclerosis model rats.
The determination of the contents of serum cholesterol, triglyceride and low-density lipoprotein of the rat finds that the contents of serum cholesterol, triglyceride and low- density lipoprotein of the atherosclerosis model rat are obviously increased, and the composition can effectively prevent increase of the contents of serum cholesterol, triglyceride and low-density lipoprotein in atherosclerosis model rats. The visual observation on the thoracic aorta of the rat finds that the arterial plaques of the atherosclerosis model rats are obvious, and the composition can effectively prevent formation of the arterial plaques of the atherosclerosis model rats. Light microscopy on the thoracic aorta of the rats finds that the damage of the arterial intima of the atherosclerosis model rats is obvious, and the composition can effectively prevent damage of the arterial intima of the atherosclerosis model rats. Light microscopy on the thoracic aorta of the rat finds that the damage of the arterial endothelial cells of the atherosclerosis model rats is obvious, and the composition can effectively prevent damage of the arterial endothelial cells of the atherosclerosis model rats.
[20] The present disclosure is capable of effectively preventing atherosclerosis, obvious in effect, stable in quality control and suitable for long-term administration of patients.
[21] Lupeol palmitate, B-humulene and methyl trans-cinnamate are all from natural medicine extract components. Compared with a traditional Chinese medicine, the pharmaceutical composition has the characteristic of controllable quality. Animal experiments and clinical trials find that the pharmaceutical composition has the characteristics of obviously inhibiting blood fat rise of high fat diet rats and effectively preventing atherosclerosis, and has the advantages of being capable of effectively preventing atherosclerosis, obvious in effect, stable in quality control and suitable for long-term administration of patients.
[22] FIG. 1 shows the effect of a pharmaceutical composition of the present disclosure on thoracic aorta morphology of an atherosclerosis model rat (by visual observation).
[23] FIG. 2 shows the effect of a pharmaceutical composition of the present disclosure on thoracic aorta morphology of an atherosclerosis model rat (by a light microscope 400x}.
[24] FIG. 3 shows the effect of a pharmaceutical composition of the present disclosure on thoracic aorta morphology of an atherosclerosis model rat (by an electron microscope 8000x).
[25] The present disclosure provides a pharmaceutical composition for preventing atherosclerosis and an application thereof. The pharmaceutical composition is prepared from the following raw materials: lupeol palmitate, B-humulene and methyl trans- cinnamate. 5 [26] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1-100 parts of lupeol palmitate, 8-100 parts of B- humulene and 10-100 parts of methyl trans-cinnamate.
[27] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1-80 parts of lupeol palmitate, 8-80 parts of B- humulene and 10-80 parts of methyl trans-cinnamate.
[28] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1-50 parts of lupeol palmitate, 8-50 parts of B- humulene and 10-50 parts of methyl trans-cinnamate.
[29] The pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1 part of lupeol palmitate, 8 parts of B-humulene and 15 parts of methyl trans-cinnamate.
[30] The present disclosure provides an application of a pharmaceutical composition in preparing a medicament for preventing atherosclerosis.
[31] In order to explain the present disclosure more clearly, the present disclosure will be described in conjunction with specific embodiments. The embodiments are as follows:
[32] Example 1
[33] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 101 parts of lupeol palmitate, 1 part of B-humulene and 105 parts of methyl trans-cinnamate.
[34] Example 2
[35] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 0.8 part of lupeol palmitate, 102 parts of B-humulene and 9 parts of methyl trans-cinnamate.
[36] Example 3
[37] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 103 parts of lupeol palmitate, 6 parts of B-humulene and 104 parts of methyl trans-cinnamate.
[38] Example 4
[39] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1 part of lupeol palmitate, 8 parts of B-humulene and 10 parts of methyl trans-cinnamate.
[40] Example 5
[41] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 100 parts of lupeol palmitate, 100 parts of B-humulene and 100 parts of methyl trans-cinnamate.
[42] Example 6
[43] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 50.5 parts of lupeol palmitate, 54 parts of B-humulene and 55 parts of methyl trans-cinnamate.
[44] Example 7
[45] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 80 parts of lupeol palmitate, 80 parts of B-humulene and 80 parts of methyl trans-cinnamate.
[46] Example 8
[47] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 40.5 parts of lupeol palmitate, 44 parts of B-humulene and 45parts of methyl trans-cinnamate.
[48] Example 9
[49] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 5Oparts of lupeol palmitate, 50 parts of B-humulene and 50 parts of methyl trans-cinnamate.
[50] Example 10
[51] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 25.5 parts of lupeol palmitate, 29 parts of B-humulene and 30 parts of methyl trans-cinnamate.
[52] Example 11
[83] A pharmaceutical composition for preventing atherosclerosis is prepared from the following raw materials: 1 part of lupeol palmitate, 8 parts of B-humulene and 15 parts of methyl trans-cinnamate.
[54] The above embodiments are only examples for clearly illustrating the present disclosure, and are not intended to limit the embodiments. For those skilled in the art, changes or modifications in other different forms can also be made on the basis of the above description. It is unnecessary and impossible to list all the embodiments herein, and the obvious changes or modifications derived therefrom still fall within the protection scope as claimed by the appended claims of the present disclosure.
[55] According to the present disclosure, lupeol palmitate, B-humulene and methyl trans-cinnamate could be prepared into various forms of medicaments, such as a hydrosolvent, powder and a mixture; when the hydrosolvent needed to be prepared, the following medicines were weighed by weight: 10 mg of lupeol palmitate, 80 mg of B- humulene and 150 mg of methyl trans-cinnamate, and the medicines were mixed, dissolved in tri-distilled water and aliquoted. When the powder needed to be prepared, the following medicines were weighed by weight: 1 g of lupeol palmitate, 8 g of B- humulene and 15 g of methyl trans-cinnamate, and the medicines were mixed and aliquoted. When the mixture needed to be prepared, the following medicines were weighed by weight: 1 g of lupeol palmitate, 8 g of B-humulene and 15 g of methyl trans- cinnamate, and the medicines were mixed, aliquoted and filled into capsules.
[56] Test Example: the serum cholesterol, triglyceride, low-density lipoprotein content, thoracic aorta macroscopic, light microscope and electron microscope shapes of the thoracic aorta in atherosclerotic model rats were detected.
[57] 1. Drugs: Lupinyl palmitate, B-humulene, and methyl trans-cinnamate were purchased from Shanghai Kexing Trading Co, Ltd, and lovastatin tablets were purchased from Beijing WINSUNNY Pharmaceutical Co., Ltd.
[58] 2. Animals: Sprague-Dawley (SD) rats, 6 weeks old, male, 180-220 g, clean grade, provided by Henan Provincial Laboratory Animal Center.
[59] 3. Experimental grouping: the rats were acclimatized in the laboratory for 1 week, and there was no abnormality in activity, eating and feces. The 40 rats were randomly divided into 4 groups according to the random number table: (1) normal control group; (2) model control group; (3) lovastatin group (100 mg/kg), (4) the present disclosure group (5 mg/kg).
[60] 4. Test contents: serum cholesterol, triglyceride, low-density lipoprotein content, thoracic aorta macroscopic, light microscope, and electron microscope shapes.
[61] 5. Statistical method: All data were expressed as mean + standard deviation (X +s). Differences between groups were compared using ANOVA and Newman-Student multiple comparisons; t-test was performed by SPSS 13.0 statistical software, and two- sided P<0.05 was considered significant differences.
[62] 6. Results
[63] 6.1 Effect of the pharmaceutical composition on the contents of serum cholesterol, triglyceride and low-density lipoprotein of an atherosclerosis model rat: the test result showed that the contents of serum cholesterol, triglyceride and low-density lipoprotein of a model control group rat were significantly higher than those of a normal control group (P < 0.05), and the contents of serum cholesterol, triglyceride and low- density lipoprotein of the group rat were significantly lower than those of the model control group (P <0.05). (Results were shown in Table 1).
[64] Table 1 Effect on blood fat of atherosclerosis model rats (n =10, *+s)
Rl oe . == ae CL —. Low-density hipoprotem
Group Cholesterol iumoVL} Triglyceride (pmol/L) ir = {pmol/L}
Normal . i 31 1720 dE 31 SH 724005" 1124004” 0.170.035 control group model control 34 13 18440136 0.2440.06% group
Lovastati x x - = vasta 0.5520.09 0.87+0.06 0.2520.06 group
The present disclosure 0.5340.06° 0.924,13" 0244006 group
[65] Note: *P<0.05 compared with the model control group, #P<0.05 compared with the lovastatin group.
[66] 6.2 FIG. 1 showed the effect of the pharmaceutical composition of the present disclosure (visual observation) on the thoracic aorta morphology of the atherosclerosis model rats. As shown from the figure, the atherosclerosis model rats had obvious arterial plaques. The pharmaceutical composition could effectively prevent the formation of the arterial plaque of the atherosclerosis model rats. As shown in FIG. 1, 1 represented the normal control group, 2 represented the model control group, 3 represented the lovastatin group and 4 represented the present disclosure group.
[67] 6.3 FIG. 2 showed the effect of the pharmaceutical composition of the present disclosure on the thoracic aorta morphology of the atherosclerosis model rats (light microscope 400%). As shown from the figure, the atherosclerosis model rats had obvious damage to the arterial intima, and the pharmaceutical composition could effectively prevent the arterial intima damage of the atherosclerotic rats. As shown in FIG. 2, 1 represented the normal control group, 2 represented the model control group, 3 represented the lovastatin group and 4 represented the present disclosure group.
[68] 6.4 FIG. 3 showed the effect of the pharmaceutical composition of the present disclosure on the thoracic aorta morphology of the atherosclerosis model rats (electron microscope 800*). As shown from the figure, the atherosclerosis model rats had obvious damage to the arterial endothelial cells, and the pharmaceutical composition could effectively prevent the damage to the arterial endothelial cells of the atherosclerotic rats.
As shown in FIG. 3, 1 represented the normal control group, 2 represented the model control group, 3 represented the lovastatin group and 4 represented the present disclosure group.
[69] The form and characteristics of the pharmaceutically acceptable carriers or diluents described herein were determined by the amount of active ingredient to be mixed therewith, route of administration, in vivo processes (including absorption, distribution, metabolism, excretion) and other known variables. These carriers must be “acceptable”, i.e. they should be compatible with other ingredients of the preparation,
without affecting the effect of the preparation and without harming the recipient of the preparation. For example, the pharmaceutical carrier used could be solid or liquid.
Examples of solid carriers were lactose, carclazyte, sucrose, talc, gelatin, agar, pectin, gum arabic, magnesium stearate, stearic acid, polyethylene glycol, polyvinylpyrrolidone, collagen hydrolysate, etc. Examples of liquid carriers were phosphate buffer solutions, syrups, emulsions, wetting agents, sterile solutions, etc.
Similarly, the carrier or diluent could include a time-delayed material known in the art, for example, glycerol monostearate or glycerol distearate alone or a mixture with wax.
A wide range of pharmaceutical forms could be used. Thus, if solid carriers were used, the preparation could be in the form of tablets, in the form of powder or granules placed in hard gelatin capsules, in the form of lozenges or sugar ingots. The amount of solid carrier could vary significantly, but preferably from about 50 mg to about 1g. When liquid carriers were used, the preparation could be in the form of syrups, emulsions, soft gelatin capsules.
Claims (6)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NL2030846A NL2030846B1 (en) | 2022-02-08 | 2022-02-08 | Pharmaceutical composition for preventing atherosclerosis and application thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NL2030846A NL2030846B1 (en) | 2022-02-08 | 2022-02-08 | Pharmaceutical composition for preventing atherosclerosis and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NL2030846B1 true NL2030846B1 (en) | 2023-08-14 |
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ID=87654390
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|---|---|---|---|
| NL2030846A NL2030846B1 (en) | 2022-02-08 | 2022-02-08 | Pharmaceutical composition for preventing atherosclerosis and application thereof |
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2022
- 2022-02-08 NL NL2030846A patent/NL2030846B1/en active
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