CN102716129B - Application of ligustrazine to medicines for adjuvant therapy of rheumatoid diseases - Google Patents

Application of ligustrazine to medicines for adjuvant therapy of rheumatoid diseases Download PDF

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Publication number
CN102716129B
CN102716129B CN201110075776.6A CN201110075776A CN102716129B CN 102716129 B CN102716129 B CN 102716129B CN 201110075776 A CN201110075776 A CN 201110075776A CN 102716129 B CN102716129 B CN 102716129B
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ligustrazine
preparation
treatment
comprises following
application
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CN102716129A (en
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吕爱平
吕诚
姜淼
何小娟
张驰
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Institute of Basic Medical Sciences of CAMS
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Institute of Basic Medical Sciences of CAMS
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Abstract

The invention relates to an application of ligustrazine to medicines for adjuvant therapy of rheumatoid diseases. The application comprises the following ratio schemes of pharmaceutical raw materials: methotrexate 1 g and ligustrazine 4-20 g; salazosulfadimidine 2 g and ligustrazine 0.4-2.0 g; tripterygium wilfordii 1 g and ligustrazine 0.4-2.0 g; cyclophosphamide 1 g and ligustrazine 0.4-2.0 g; leflunomide 1 g and ligustrazine 4-20 g; azathioprine 2 g and ligustrazine 0.2-1.8 g; penicillamine 2.5 g and ligustrazine 0.4-2.0 g; and hydroxychloroquine 4 g and ligustrazine 0.4-2.0 g. The preparation method is that mixing and making two pharmaceutical raw materials into powder, adding routine pharmaceutic adjuvants, and making the powder with adjuvants into tablets or injections through a routine preparation technology. The application initiates a new usage of the ligustrazine in medicines and has obvious effects when cooperating with mainstream medicines for treating rheumatoid diseases, such as methotrexate, salazosulfadimidine, etc. The application contributes greatly to the treatment of stubborn rheumatoid diseases.

Description

The application of ligustrazine in adjuvant therapy rheumatoid disease medicament
Technical field
The application of the new purposes, particularly ligustrazine that the present invention relates to known substance ligustrazine in adjuvant therapy rheumatoid disease medicament.
Background technology
Atrophic diseases is the class disease that clinical onset rate is higher, hazardness is larger.Many rheumatoid disease belong to clinical difficult serious symptom, and some sick disability rate is high, and some sick oncoming force is dangerous, threat to life.And it all can fall ill in each age group crowd, and sickness rate increases with age growth.
Methotrexate, salazosulfadimidine, Radix Tripterygii Wilfordii, cyclophosphamide etc. are the main medicines for the treatment of atrophic diseases, but because rheumatoid disease belongs to clinical difficult serious symptom, a lot of pathogeny are not quite clear, even if strengthen and extend the consumption of methotrexate, salazosulfadimidine, Radix Tripterygii Wilfordii, cyclophosphamide etc. in treatment, still there is considerable patient's disease to mustn't go to effective alleviation, bring great misery to patient.
Ligustrazine has the effect of blood circulation promoting and blood stasis dispelling, antiinflammatory, antioxidation, cell proliferation for many medical personnels and patient know.But there is not yet the application of ligustrazine in adjuvant therapy rheumatoid disease field.
Ligustrazine, as not having the significant degree of association between the medicine of blood circulation promoting and blood stasis dispelling, antiinflammatory, antioxidation, cell proliferation and treatment atrophic diseases, does not have the report of this respect at present yet.
Summary of the invention
The application of the new purposes, particularly ligustrazine that the object of the present invention is to provide known substance ligustrazine in adjuvant therapy rheumatoid disease medicament.
The drug preparation technique scheme of the treatment atrophic diseases that the present invention makes is as follows:
Scheme one: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: methotrexate 1g, ligustrazine 4-20g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme two: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: salazosulfadimidine 2g, ligustrazine 0.4-2.0g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme three: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: Radix Tripterygii Wilfordii 1g, ligustrazine 0.4-2.0g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme four: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: cyclophosphamide 1g, ligustrazine 0.4-2.0g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme five: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: leflunomide 1g, ligustrazine 4-20g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme six: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: azathioprine 2g, ligustrazine 0.2-1.8g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme seven: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: penicillamine 2.5g, ligustrazine 0.4-2.0g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Scheme eight: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: oxychloroquine 4g, ligustrazine 0.4-2.0g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
specific embodiment:
Embodiment 1: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: methotrexate 1g, ligustrazine 4g, wherein preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Embodiment 2: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: methotrexate 1g, ligustrazine 12g, wherein preparation method is with embodiment 1.
Embodiment 3: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: methotrexate 1g, ligustrazine 20g, wherein preparation method is with embodiment 1.
Embodiment 4: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: salazosulfadimidine 2g, ligustrazine 0.4g, wherein preparation method is with embodiment 1.
Embodiment 5: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: salazosulfadimidine 2g, ligustrazine 1.2g, wherein preparation method is with embodiment 1.
Embodiment 6: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: salazosulfadimidine 2g, ligustrazine 2.0g, wherein preparation method is with embodiment 1.
Embodiment 7: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: Radix Tripterygii Wilfordii 1g, ligustrazine 0.4g, wherein preparation method is with embodiment 1.
Embodiment 8: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: Radix Tripterygii Wilfordii 1g, ligustrazine 1.2g, wherein preparation method is with embodiment 1.
Embodiment 9: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: Radix Tripterygii Wilfordii 1g, ligustrazine 2.0g, wherein preparation method is with embodiment 1.
Embodiment 10: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: cyclophosphamide 1g, ligustrazine 0.4g, wherein preparation method is with embodiment 1.
Embodiment 11: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: cyclophosphamide 1g, ligustrazine 1.2g, wherein preparation method is with embodiment 1.
Embodiment 12: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: cyclophosphamide 1g, ligustrazine 2.0g, wherein preparation method is with embodiment 1.
Embodiment 13: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: leflunomide 1g, ligustrazine 4g, wherein preparation method is with embodiment 1.
Embodiment 14: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: leflunomide 1g, ligustrazine 12g, wherein preparation method is with embodiment 1.
Embodiment 15: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: leflunomide 1g, ligustrazine 20g, wherein preparation method is with embodiment 1.
Embodiment 16: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: azathioprine 2g, ligustrazine 0.2g, wherein preparation method is with embodiment 1.
Embodiment 17: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: azathioprine 2g, ligustrazine 1.0g, wherein preparation method is with embodiment 1.
Embodiment 18: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: azathioprine 2g, ligustrazine 1.8g, wherein preparation method is with embodiment 1.
Embodiment 19: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: penicillamine 2.5g, ligustrazine 0.4g, wherein preparation method is with embodiment 1.
Embodiment 20: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: penicillamine 2.5g, ligustrazine 1.2g, wherein preparation method is with embodiment 1.
Embodiment 21: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: penicillamine 2.5g, ligustrazine 2.0g, wherein preparation method is with embodiment 1.
Embodiment 22: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: oxychloroquine 4g, ligustrazine 0.4g, wherein preparation method is with embodiment 1.
Embodiment 23: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: oxychloroquine 4g, ligustrazine 1.2g, wherein preparation method is with embodiment 1.
Embodiment 24: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: oxychloroquine 4g, ligustrazine 2.0g, wherein preparation method is with embodiment 1.
Embodiment 25: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: sinomenine 2g, chlorogenic acid 5g, ligustrazine is 3g, wherein preparation method is made Powdered by three kinds of medicament mixed, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
Embodiment 26: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: sinomenine 2g, chlorogenic acid 5g, ligustrazine is 5g, wherein preparation method is with embodiment 25.
Embodiment 27: the pharmaceutical preparation for the treatment of atrophic diseases, the weight proportion that comprises following medicine: sinomenine 2g, chlorogenic acid 5g, ligustrazine is 7g, wherein preparation method is with embodiment 25.
Embodiment 28: the pharmaceutical preparation for the treatment of atrophic diseases, only with ligustrazine 5g as raw material, wherein preparation method is made ligustrazine Powdered, adds conventional pharmaceutic adjuvant, adopts conventional preparation technology, makes tablet or injection.
Embodiment 29: the hybrid medicine powder that embodiment 1-28 is made, mix homogeneously with starch and dextrin, make tablet according to conventional tablet preparation method, wherein the content of each component is as follows:
Composition weight (part)
Hybrid medicine powder 25
Starch 25
Dextrin 7
Carboxymethyl starch sodium 7
Magnesium stearate 1
All the other are with embodiment 1-28.
Embodiment 30: the hybrid medicine powder that embodiment 1-28 is made, inject water, make injection according to regular injection agent preparation method, wherein the content of each component is as follows:
Composition weight (part)
Hybrid medicine powder 150
Sodium chloride 50
Water for injection 1000
Efficacy experiment:
(1) 300 rheumatoid arthritis patients are divided into A, B, C, D, E, F, G, H, I, J10 group, every group of 30 people, the oral medicament mixed powder of making by embodiment 2,5,8,11,14,17,20,23,26,28 respectively, one day twice, take continuously three months, effect is as shown in the table:
(2) get 350 of healthy normal SD rats, random choose wherein 10 as normal group, all the other rats are accepted CFA modeling, modeling is selected 290 of the obvious rats of secondary affection on the 30th day and is divided into groups, and 10 every group, is divided at random 29 groups.The hybrid medicine powder of the treatment rheumatoid arthritis being made by embodiment 1 to 28 is given 28 groups of rat feedings with the oral dose of 30mg/kg respectively, is left one group as model group.By the curative effect that checks Drug therapy rheumatoid arthritis for 1 day, 10 days, 20 days, 30 days, this experiment is similar to the experiment of the joint pathology damage that rat is carried out, and for referencial use with the comprehensive score of its joint pathology damage sxemiquantitative.Effect of drugs is as follows:
Embodiment 1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,22,23,24 contrasts with model group respectively, and the 10th day decline scope of the comprehensive score of joint pathology damage sxemiquantitative is all at 2-5%.
Embodiment 1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,22,23,24 contrasts with model group respectively, and the 20th day decline scope of the comprehensive score of joint pathology damage sxemiquantitative is all at 5-10%.
Embodiment 1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,22,23,24 contrasts with model group respectively, and the 30th day decline scope of the comprehensive score of joint pathology damage sxemiquantitative is all at 12-20%.
Embodiment 25,26,27,28 contrasts with model group respectively, and the 10th day decline scope of the comprehensive score of joint pathology damage sxemiquantitative is all at 0-5%.
Embodiment 25,26,27,28 contrasts with model group respectively, and the 20th day decline scope of the comprehensive score of joint pathology damage sxemiquantitative is all at 0-5%.
Embodiment 25,26,27,28 contrasts with model group respectively, and the 20th day decline scope of the comprehensive score of joint pathology damage sxemiquantitative is all at 0-10%.
Obtain following results in conjunction with above-mentioned result of the test:
1, use separately ligustrazine treatment rheumatoid disease effect undesirable.
2, ligustrazine coordinates the rheumatoid medicine methotrexate for the treatment of of main flow, salazosulfadimidine, Radix Tripterygii Wilfordii, cyclophosphamide, leflunomide, azathioprine, penicillamine, oxychloroquine successful.This is huge for the obstinate rheumatoid contribution for the treatment of.
3, use separately methotrexate, when salazosulfadimidine, Radix Tripterygii Wilfordii, cyclophosphamide, leflunomide, azathioprine, penicillamine, oxychloroquine are treated rheumatoid medicine, therapeutic effect statistically not as ligustrazine respectively with methotrexate, salazosulfadimidine, Radix Tripterygii Wilfordii, cyclophosphamide, leflunomide, azathioprine, penicillamine, oxychloroquine are combined the good effect of use.
4, comprehensively above-mentioned, ligustrazine has the effect of adjuvant therapy rheumatoid disease, and the application of ligustrazine in adjuvant therapy rheumatoid disease medicament has foundation.

Claims (2)

1. the application of pharmaceutical composition in preparation treatment atrophic diseases medicine, described pharmaceutical composition is: leflunomide 1g, ligustrazine 4-20g.
2. the application of pharmaceutical composition as claimed in claim 1 in preparation treatment atrophic diseases medicine, it is characterized by: preparation method is that two kinds of medicament mixed are made Powdered, add conventional pharmaceutic adjuvant, adopt conventional preparation technology, make tablet or injection.
CN201110075776.6A 2011-03-29 2011-03-29 Application of ligustrazine to medicines for adjuvant therapy of rheumatoid diseases Expired - Fee Related CN102716129B (en)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101411707A (en) * 2008-10-10 2009-04-22 西南大学 Pharmaceutical composition for treating rheumatoid arthritis

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2569836A1 (en) * 2004-06-09 2005-12-22 Shenzhen Qianrenren Sci. & Tech. Development Co., Ltd. Herbal compositions for prevention and treatment of rheumatic and inflammatory diseases and method of preparing the same

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101411707A (en) * 2008-10-10 2009-04-22 西南大学 Pharmaceutical composition for treating rheumatoid arthritis

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