CN101019860A - Compound prepn of artemisinin derivative and histamine H2 receptor agonist - Google Patents
Compound prepn of artemisinin derivative and histamine H2 receptor agonist Download PDFInfo
- Publication number
- CN101019860A CN101019860A CN 200710065695 CN200710065695A CN101019860A CN 101019860 A CN101019860 A CN 101019860A CN 200710065695 CN200710065695 CN 200710065695 CN 200710065695 A CN200710065695 A CN 200710065695A CN 101019860 A CN101019860 A CN 101019860A
- Authority
- CN
- China
- Prior art keywords
- weight ratio
- cimetidine
- histamine
- ranitidine
- compound
- Prior art date
- 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.)
- Pending
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
The present invention relates to medicine preparation, and is especially medicine composition of artemisinin derivative and histamine H2 receptor agonist. The medicine composition consists of dihydro artemisinin and cimetidine in the weight ratio of 1 to (1-30); dihydro artemisinin and ranitidine in the weight ratio of 1 to (1-25); artemether or other artemisinin derivative and cimetidine in the weight ratio of 1 to (1.5-20); or artemether or other artemisinin derivative and ranitidine in the weight ratio of 1 to (1.5-15). The medicine composition may be prepared into tablet, capsule, suppository, oral liquid or injection. The present invention has reduced artemisinin derivative consumption, raised blood medicine concentration, low cost and other advantages.
Description
Affiliated technical field
The invention belongs to the pharmaceutical product that contains organic effective ingredient, particularly the artemisinin compound pharmaceutical product.
Background technology
Arteannuin (Artemisnin) is the malaria effective ingredient that extracts from the feverfew Herba Artemisiae annuae, its derivant comprises Artemether, arteether, artesunate and dihydroarteannuin, metabolism is very fast in vivo, T1/2 is very short, for example: artesunate for Injection, the very fast decline of blood drug level after the intravenous injection, T1/2 is about 30 minutes; The blood plasma T1/2 of dihydroarteannuin sheet is 1.57 hours; Artesunate tablet blood plasma T1/2 is about 30 minutes.Because metabolism is all fast with drainage, single with arteannuin antimalarial treatment pernicious malaria, the effective blood drug concentration weak point of holding time is unfavorable for thoroughly killing plasmodium, cause the palindromia rate higher, clinically by strengthening reasonable administration time, the repetitively administered of initial dose, use 5 days or the course of treatment on the 7th.Yet the big plasmodium that may make of dosage produces drug resistance to anti-malaria medicaments, and World Health Organization (WHO) proposes: the treatment malaria, and doctor's clinical application should be used the Artequick preparation; Drugmaker is preferably with compound medicines, but not folk prescription medicine form is produced arteannuin.Cimetidine, ranitidine, famotidine and nizatidine are histamine H2 receptor antagonist class medicine, are widely used in the treatment ulcer of upper digestive tract.As bisfentidine, it can with the H2 receptors bind of a plurality of tissues of human body, sealing histamine, has androgen antagonist, antiviral, immunomodulating, suppress physiological effecies such as prostaglandin release, especially, to extensively distributing in the human body and participating in the Cytochrome P450 of degraded the 1st phase reaction in the medicine liver, histamine H2 receptor antagonist can be by suppressing the biotransformation metabolic function of Cytochrome P450, prolong drug metabolism time in vivo, improve blood drug level, thereby strengthen medicine in the intravital effect of host.
China is taking its place in the front ranks of the world aspect the development of Artequick.More satisfactory with artemisine and mefloquine, malaridine, LUMEFANTRINE or NAPHTHOQUINE PHOSPHATE and mefloquine combined therapy subtertian malaria; Artemisine and primaquine share and can effect a radical cure tertian malaria; Artemisine and trimethoprim share and can reduce recent resume combustion of malaria or recurrence.For observing cimetidine to the active influence of artesunate anti schistosoma, Zhou Ying etc. share in mouse test in the dosage of 1: 1 ratio, each 100mg/kg with cimetidine and artesunate injection and have obtained better drug effect.(unming Medical College's journal 2006 (6) 43-46) great dosage of this article helps observing animal tissue's experimental result, and the artesunate injection therapeutic dose that is applicable to human body only is 1.2mg/kg-1.5mg/kg, and experiment only relates to the compatibility experiment of cimetidine and two kinds of folk prescriptions of artesunate, do not propose medicaments compound, do not use other drug yet.
Summary of the invention
Render a service, prevent to develop immunity to drugs in order to strengthen artemisinin-based drug medicine malaria, the present invention is directed to the short shortcoming of metabolic half life of artemisinin-based drug, the compound medicine of a kind of artemisine and histamine H2 receptor antagonist is provided, with reduce arteannuin or ex hoc genus anne drug dose, increase arteannuin ex hoc genus anne the concentration of medicine in blood plasma, improve efficacy of drugs, and the Drug resistance that reduces and prevent plasmodium to produce.
Pharmaceutical composition of the present invention is combined to form with histamine H2 receptor antagonist cimetidine, ranitidine, famotidine or a kind of of nizatidine by selection in dihydroarteannuin, Artemether, arteannuin, arteether or the artesunate is a kind of, and the weight ratio of the former with the latter is 1: (1.5-35).
The weight ratio of described dihydroarteannuin and cimetidine is 1: (3-30), and the weight ratio of dihydroarteannuin and ranitidine is 1: (1-25).
One of described Artemether, arteether or artesunate are 1 with the weight ratio of cimetidine: (2-16), and the weight ratio of one of Artemether, arteether or artesunate and ranitidine is 1: (1.5-12).
The weight ratio of described dihydroarteannuin and cimetidine further is selected from 1: (12-16), and the weight ratio of dihydroarteannuin and ranitidine further is selected from 1: (3-7).
One of described Artemether, arteether or artesunate further are selected from 1 with the weight ratio of cimetidine: (5-10), and the weight ratio of one of Artemether, arteether or artesunate and ranitidine further is selected from 1: (1.5-8).
Histamine H2 receptor antagonist of the present invention can gastric acid inhibitory secretion, it makes up with artemisinin-based drug, can improve and keep the blood level of artemisine, the half-life of prolong drug in blood plasma, is convenient to medicine and gives full play to and kill plasmodial effectiveness.
According to existing pharmacological action theory, observe and analyze through the actual effect of folk prescription, theoretical reasoning and calculating, and reasonable compound recipe, we determine for certain, pharmaceutical composition provided by the invention can be realized described medical usage, promptly reduce dihydroarteannuin or ex hoc genus anne drug dose, increase dihydroarteannuin ex hoc genus anne the concentration of medicine in blood plasma, improve efficacy of drugs, reduce the palindromia rate, thereby play the bad result that the prevention excess dosage uses arteannuin to develop immunity to drugs.Therefore, the present invention have improve the artemisinin-based drug effect, fast alleviate clinical symptoms, curative effect height, reduced the advantage of medicine cost.
The specific embodiment
The present invention further specifies by following embodiment:
Embodiment 1:
Arteannuin and cimetidine are with weight ratio combination in 1: 3.
Embodiment 2:
Dihydroarteannuin and cimetidine are with weight ratio combination in 1: 5.
Embodiment 3:
Dihydroarteannuin and cimetidine are with weight ratio combination in 1: 10.
Embodiment 4:
Dihydroarteannuin and cimetidine are with weight ratio combination in 1: 14.
Embodiment 5:
Dihydroarteannuin and cimetidine are with weight ratio combination in 1: 27.
Embodiment 6:
Selection is a kind of in ranitidine, famotidine or the nizatidine makes up with weight ratio with dihydroarteannuin at 1: 1.5.
Embodiment 7:
Selection is a kind of in ranitidine, famotidine or the nizatidine makes up with weight ratio with dihydroarteannuin at 1: 5.
Embodiment 8:
Selection is a kind of in ranitidine, famotidine or the nizatidine makes up with weight ratio with dihydroarteannuin at 1: 20.
Embodiment 9:
Artemether and cimetidine are with weight ratio combination in 1: 2.
Embodiment 10:
Artesunate and cimetidine are with weight ratio combination in 1.5: 8.
Embodiment 11:
Arteether and cimetidine are with weight ratio combination in 1: 10.
Embodiment 12:
Arteether and cimetidine are with weight ratio combination in 1: 16.
Embodiment 13:
Selection is a kind of in ranitidine, famotidine or the nizatidine makes up with weight ratio with Artemether at 1: 1.5.
Embodiment 14:
Selection is a kind of in ranitidine hydrochloride, famotidine or the nizatidine makes up with weight ratio with artesunate at 1: 3.
Embodiment 15:
Selection is a kind of in ranitidine hydrochloride, famotidine or the nizatidine makes up with weight ratio with artesunate at 1: 10.
Embodiment 16:
Selection is a kind of in ranitidine, famotidine or the nizatidine makes up with weight ratio with Artemether at 1: 5.
More than the compositions of each embodiment can make tablet, capsule, suppository, oral liquid or injection.
Dosage and usage:
Oral 200-400mg/ time, 1-2 time/day.Injection slowly instils after diluting with normal saline or 5% glucose injection 20-500ml.
Claims (6)
1. the compound of artemisinin derivative and histamine H2 receptor antagonist, it is characterized in that this pharmaceutical composition is combined to form with cimetidine, ranitidine, famotidine or a kind of of nizatidine by selection in dihydroarteannuin, Artemether, arteannuin, arteether or the artesunate is a kind of, the weight ratio of the former with the latter is 1: (1.5-35).
2. according to the compound of described artemisinin derivative of claim 1 and histamine H2 receptor antagonist, the weight ratio that it is characterized in that dihydroarteannuin and cimetidine is 1: (1-30), and the weight ratio of dihydroarteannuin and ranitidine is 1: (1-25).
3. according to the compound of described artemisinin derivative of claim 1 and histamine H2 receptor antagonist, it is characterized in that one of Artemether, arteether or artesunate and the weight ratio of cimetidine are 1: (1.5-20), and the weight ratio of one of Artemether, arteether or artesunate and ranitidine is 1: (1.5-15).
4. according to the compound of described artemisinin derivative of claim 2 and histamine H2 receptor antagonist, the weight ratio that it is characterized in that dihydroarteannuin and cimetidine further is 1: (12-16), and the weight ratio of dihydroarteannuin and ranitidine further is 1: (3-7).
5. according to the compound of described artemisinin derivative of claim 3 and histamine H2 receptor antagonist, it is characterized in that one of Artemether, arteether or artesunate and the weight ratio of cimetidine further are 1: (5-10), and the weight ratio of one of Artemether, arteether or artesunate and ranitidine further is 1: (1.5-8).
6. according to the compound of claim 1,2,3,4,5 or 6 described artemisinin derivatives and histamine H2 receptor antagonist, the dosage form that it is characterized in that this pharmaceutical composition is tablet, capsule, suppository, oral liquid or injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710065695 CN101019860A (en) | 2007-03-02 | 2007-03-02 | Compound prepn of artemisinin derivative and histamine H2 receptor agonist |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710065695 CN101019860A (en) | 2007-03-02 | 2007-03-02 | Compound prepn of artemisinin derivative and histamine H2 receptor agonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101019860A true CN101019860A (en) | 2007-08-22 |
Family
ID=38707786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200710065695 Pending CN101019860A (en) | 2007-03-02 | 2007-03-02 | Compound prepn of artemisinin derivative and histamine H2 receptor agonist |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101019860A (en) |
-
2007
- 2007-03-02 CN CN 200710065695 patent/CN101019860A/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20190151398A1 (en) | Pharmaceutical Composition Comprising Cannabidiol (CBD) and Lecithin | |
| JP6446552B2 (en) | Compositions used for weight and body fat reduction and their pharmaceuticals and uses | |
| AU2011324137B2 (en) | A combination composition | |
| JP6511492B2 (en) | Treatment of symptoms related to female gastroparesis | |
| CN102008482A (en) | Compound preparation containing valsartan for treating hypertension | |
| WO2005084392A2 (en) | 4-methylpyrazole formulations for inhibiting ethanol intolerance | |
| CN102008712A (en) | Trandolapril-containing compound preparation for curing hypertension | |
| CN102283928A (en) | Technology for preparing novel integrated dosage form of Ermiao powder and production method thereof | |
| CN101019860A (en) | Compound prepn of artemisinin derivative and histamine H2 receptor agonist | |
| US20100255088A1 (en) | Method for delivering a combination of resveratrol and aspirin for use in treatment and prevention of vascular disease | |
| WO2015041723A1 (en) | Artemisinin-based combination therapy for treating viral mediated disease | |
| CN102100768A (en) | Preparation technique for ephedra decoction in novel formed formulation and production method thereof | |
| CN1287808C (en) | Ginkgo leaf extract composition | |
| CN101327215B (en) | Medicament composition containing protoberberine type alkaloids | |
| CN110179860A (en) | A kind of drug of anti-epileptic, preparation method and the usage | |
| CN110279691A (en) | A kind of surgical postoperative nursing analgesic and application thereof | |
| CN107252426A (en) | Application of the dexchlorpheniramine in anti-motion sickness field | |
| CN102283832B (en) | Medicinal composition for preventing or treating hypertensive obese patient and application thereof | |
| CN100998587A (en) | Application of 5-hydroxy furfurol for preparing medicine | |
| CN102000052B (en) | Application of taxol and taxol derivatives to pharmacy | |
| CN117243947A (en) | Application of daphnetin and combination containing daphnetin in preparation of diabetes complication medicaments | |
| CN102895244A (en) | Pharmaceutical composition | |
| CN104721220B (en) | A kind of pharmaceutical composition and its application, preparation | |
| CN1985843B (en) | Malaria treating medicine | |
| CN103768048B (en) | Silybin meglumine tablets and effect for reducing fat thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Open date: 20070822 |