CN1465344A - Medicine composition for treating myocardial ischemia, angina pectoris and cardiac infarction - Google Patents

Medicine composition for treating myocardial ischemia, angina pectoris and cardiac infarction Download PDF

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Publication number
CN1465344A
CN1465344A CNA021121591A CN02112159A CN1465344A CN 1465344 A CN1465344 A CN 1465344A CN A021121591 A CNA021121591 A CN A021121591A CN 02112159 A CN02112159 A CN 02112159A CN 1465344 A CN1465344 A CN 1465344A
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Prior art keywords
angina pectoris
myocardial ischemia
myocardial infarction
diosgenin
medicine composition
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CNA021121591A
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CN1187055C (en
Inventor
刘忠荣
黄璜
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Chengdu Diao Pharmaceutical Group Co Ltd
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Chengdu Diao Pharmaceutical Group Co Ltd
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Abstract

The present invention discloses a medicine composition composed of diosgenin as active component and medicinal auxiliary material, and can obtain good therapeutic effect for curing the diseases of myocardial ischemia, angina pectoris and myocardiac infarction, etc.

Description

Pharmaceutical composition with treatment myocardial ischemia, angina pectoris and myocardial infarction function
Technical field
The invention belongs to the pharmaceutical chemistry technical field.Be specifically related to a kind of pharmaceutical composition with treatment myocardial ischemia, angina pectoris and myocardial infarction function.
Background technology
Dioscin treatment myocardial ischemia, angina pectoris early have report, and the medicine of existing dioscin composition, and listing is applied to clinical for many years as DIAOXINXUE KANG JIAONANG.But the hydrolyzate diosgenin of dioscin does not appear in the newspapers to the therapeutical effect of myocardial ischemia, angina pectoris aspect, this research by a series of evidences diosgenin effect in this regard.
Summary of the invention
Technical problem to be solved by this invention is the new function of the pharmaceutical composition of research and development diosgenin.
The invention provides a kind of pharmaceutical composition with treatment myocardial ischemia, angina pectoris and myocardial infarction function, said composition is to form as active ingredient and pharmaceutic adjuvant with the chemical compound diosgenin of following formula [I].
Figure A0211215900031
The result of the relevant pharmacodynamics test of pharmaceutical composition of the present invention (No. 1, buchu) is as follows:
Buchu No. 1 (diosgenin) is to the influence of myocardial infarction due to the rat heart muscle ischemia
Summary:
This test is with myocardial infarction model due to the rat heart muscle ischemia, and nitro blue tetrazolium (N-BT) is a stain, observes No. 1 influence to the myocardial infarction degree of buchu.Result of the test confirms that buchu can obviously alleviate the myocardial infarction degree No. 1, and infarct size is dwindled, infarct weight saving, and infarct accounts for heart and ventricle percentage ratio reduces, and with model group notable difference is arranged relatively.
Test material:
25 of animal Wistar kind rats, male, body weight 280-310g, Institute of Experimental Animals, Chinese Academy of Medical Sciences provides, the quality certification number: SCXK11-00-0006 number.
Medicine:
No. 1 powder of buchu, Chengdu Diao Pharmaceutical Group Co., Ltd provides; Pure Oleum Arachidis hypogaeae semen, suburb, northeast, Beijing oils and fats storage refinery produces date of manufacture 2001.01.09.
Instrument:
Dual-trace recorder (Japanese photoelectricity Recticorder); Ecg amplifier (Japanese photoelectricity ECG Amplifier, AC-601G); Respirator (SC-3 type, Shanghai Medical Equipment Factory); Multi-media color pathology picture and text analytical systems (MPIAS-500).
Test method:
Animal is divided into 3 groups at random, 5 every group; (normal saline, 3ml), buchu No. 1 0.9,0.45g/kg organize (being respectively maximum dosage-feeding 1/20,1/40) to model group.No. 1 medicine is molten to desired concn with Oleum Arachidis hypogaeae semen, and the administration volume is 3ml/kg, and route of administration is a duodenum.
Animal faces upward the position and fixes with urethanes (Urathan) intraperitoneal anesthesia (1000mg/kg), amplifies along (Japanese wide ECG Amplifier AC-601G) connects dual-trace recorder (Japanese photoelectricity Recticorder) monitoring standard II lead electrocardiogram with electrocardio; Tracheostomize inserts tracheal intubation, meets respirator (SC-3 type, Shanghai Medical Equipment Factory) pedestrian worker and breathes (32 times/minute, breathed ratio 1: 3); Open breast, disconnected 3-5 rib is opened pericardium, exposes heart, in left anterior descending coronary artery root threading (No. 0 stitching thread), is equipped with ligation and uses; Separate 12 intestinal and prepare administration; Stablized behind the threading 10 minutes, ligation (no ST section and T ripple changer eliminate) feeds and is subjected to close abdomen behind the reagent thing; Sew up thoracic wall, recover autonomous respiration.
Ligation finishes test after 3 hours, 5 of the following crosscuts of heart ligature, and multi-media color pathology map analysis system (MPIAS-500) is adopted in N-BT dyeing, with fixedly image distance measurement normal myocardium and infarcted myocardium area, observation myocardial infarction degree; The result carries out statistical procedures (t check).
Result of the test:
1. No. 1 influence of buchu to the myocardial infarction degree
Dosage normal myocardium area infarcted myocardium area infarct weight infarct accounts for infarct and accounts for grouping n
Kg mm 2Mm 2G ventricle % heart % model 5 323.41 ± 21.79 103.06 ± 10.51 0.278 ± 0.027 31.8 ± 2.1 27.1 ± 1.8 ground No. 15 0.9g 317.72 difficult to understand ± No. 15 0.45g 326.78 ± 11.85 96.51 ± 14.08 0.260 ± 0.047 29.5 ± 4.4 25.0 ± 3.8 difficult to understand, 10.18 81.59 ± 8.62**, 0.212 ± 0.021**, 25.8 ± 3.4**, 21.6 ± 2.6** ground
*: compare P<0.05, P<0.01 with model group
Result of the test confirms that the model group infarct accounts for ventricle and heart percentage ratio is respectively 31.8 and 27.1%; No. 1 0.9g/kg group of buchu myocardial infarction degree obviously alleviates, and infarct size reduces, infarct weight saving, and infarct accounts for ventricle and heart percentage ratio reduces, and with model group significant difference (P<0.01) is arranged more all.
Conclusion:
This experiment is observed drug effect with myocardial infarction model due to the rat heart muscle ischemia.Laboratory observation arrives, and myocardium continuous ischemia causes myocardial infarction to take place, and N-BT dyeing back heart infarction speckle is obvious, accounts for 31.8% of the ventricle gross area.
Buchu obviously alleviates the myocardial infarction degree No. 1, and the heart infarction area dwindles, and infarct weight saving has clear and definite protective effect to myocardial ischemia.
Our experiments show that pharmaceutical composition of the present invention has the coronary artery dilator blood vessel, increase coronary flow, reduce coronary resistance, improve the work done of left chamber, adjust cardiovascular compliance, be used to prepare the pharmaceutical preparation for the treatment of myocardial ischemia, angina pectoris and myocardial infarction function clinically.
Therefore, with this chemical compound is effective medicinal ingredient, after auxiliary and/or adding ingredient mixes by acceptable in the pharmaceutical methods of present various routines and technological requirement and the pharmacy, promptly can make the medicine of the several formulations forms such as corresponding oral type preparation, buccal lozenge, injection-type preparation of diseases such as being used for the treatment of myocardial ischemia, angina pectoris and myocardial infarction.Wherein said injection-type preparation can include injection and different dosage forms such as powder pin.
The specific embodiment
Embodiment 1
Irritate stomach with (1) 0.14g/kg agent and 0.28g/kg dosage and give dog, respectively behind the medicine prodrug 15,30,45,60,90,120 minutes the record experimental index, the result shows: administration (1) back 30-60 minute, coronary flow obviously increases, increasing degree is (P<0.05-0.01) about 20%, reduce from 30 minutes coronary resistances, amplitude shows that (1) can obviously treat myocardial ischemia, angina pectoris and myocardial infarction about 15%.
Embodiment 2
Make injection with (1) and give dog by 0.07g/kg and 0.14g/kg intravenous injection, respectively behind the medicine prodrug 1,3,5,10,15,30,60,90 minute the record experimental index, the result shows: administration (1) back 3-60 minute, coronary flow obviously increases, increasing degree is (P<0.01) about 30%, and coronary resistance reduces, and amplitude is about 20%, left side chamber work done obviously increases (P<0.05), shows that (1) can obviously treat myocardial ischemia, angina pectoris and myocardial infarction.Embodiment 3
Add 100mg starch with (1) 100mg and incapsulate, by one time two, one day three times, take a week after, the patient obviously feels remissions such as cardiopalmus, the heart is tired, nervous, above-mentioned symptom almost disappears after one month.

Claims (3)

1. the pharmaceutical composition with treatment myocardial ischemia, angina pectoris and myocardial infarction function is characterized in that said composition is to form as active ingredient and pharmaceutic adjuvant with the chemical compound diosgenin of following formula [I].
Figure A0211215900021
2. preparation of drug combination method with treatment myocardial ischemia, angina pectoris and myocardial infarction function as claimed in claim 1 is characterized in that this method is that the chemical compound diosgenin of formula [I] is made oral, buccal lozenge, ejection preparation or external type preparation according to a conventional method as active ingredient and pharmaceutic adjuvant.
3. the chemical compound diosgenin with formula [I] as claimed in claim 1 has application in the pharmaceutical composition of treatment myocardial ischemia, angina pectoris and myocardial infarction function in preparation.
CNB021121591A 2002-06-21 2002-06-21 Medicine composition for treating myocardial ischemia, angina pectoris and cardiac infarction Expired - Lifetime CN1187055C (en)

Priority Applications (1)

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CN1187055C CN1187055C (en) 2005-02-02

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006107902A3 (en) * 2005-04-01 2006-11-30 Samaritan Pharmaceuticals Inc Use of spirostenols to treat mitochondrial disorders
WO2007003957A3 (en) * 2005-07-06 2007-05-31 Btg Int Ltd Steroidal glycoside compounds as core 2 glcnac- t inhibitors
US7906493B2 (en) 2003-12-22 2011-03-15 Btg International Limited Core 2 GlcNAc-T inhibitors

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7906493B2 (en) 2003-12-22 2011-03-15 Btg International Limited Core 2 GlcNAc-T inhibitors
WO2006107902A3 (en) * 2005-04-01 2006-11-30 Samaritan Pharmaceuticals Inc Use of spirostenols to treat mitochondrial disorders
WO2007003957A3 (en) * 2005-07-06 2007-05-31 Btg Int Ltd Steroidal glycoside compounds as core 2 glcnac- t inhibitors

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