CN101543628A - Medicament and preparation thereof for treating hyperlipemia and atherosclerosis - Google Patents
Medicament and preparation thereof for treating hyperlipemia and atherosclerosis Download PDFInfo
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- CN101543628A CN101543628A CN200810102655A CN200810102655A CN101543628A CN 101543628 A CN101543628 A CN 101543628A CN 200810102655 A CN200810102655 A CN 200810102655A CN 200810102655 A CN200810102655 A CN 200810102655A CN 101543628 A CN101543628 A CN 101543628A
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Abstract
The invention relates to a medicament for treating hyperlipemia and atherosclerosis. The medicament contains a lipid-regulating active ingredient A and a lipid-regulating active ingredient B, wherein the lipid-regulating active ingredient A is one or more of nicotinic acid, clofibrate, phenoxy acetic acid and HMG-CoA reductase inhibitor, and the lipid-regulating active ingredient B is one kind or more kinds in long-chain fatty alcohol. The invention also relates to the application of the medicament for treating hyperlipemia or treating atherosclerosis. The medicament greatly reduces the dosage of statins with the curative effect not lower than that of the statins which is singly used, thereby reducing the side effect of the statins, reducing the drug cost and saving the drug expense for the patients.
Description
Technical field
The present invention relates to a kind of compound medicinal formulation and application thereof, relate in particular to a kind of compound medicinal formulation and application thereof for the treatment of hyperlipemia and atherosclerosis, belong to field of medicaments.
Background technology
Hyperlipemia is to cause atherosclerotic main cause.Fat-reducing medicament commonly used at present is by adjusting the disorder of blood plasma lipide or lipoprotein, treatment hyperlipemia and the effect of generation arteriosclerosis, wherein the novel and effective medicine is 3-hydroxyl-3-first glutaryl coenzyme A (HMG-CoA) reductase inhibitor, i.e. statins the most.Statins does not have serious adverse reaction when general dosage short-term is used, minority shows slight gastrointestinal reaction, headache or erythra; But prolonged application (more than 4 weeks) is seen hepar damnification more, and therefore, the patient can not tolerate, and how must suspend after taking for 4 weeks and to use this medicine, in order to liver function recovery.In addition, statins can also cause myalgia and raise with creatine phosphokinase, and particularly rhabdomyolysis and renal failure takes place has higher fatality rate, and the sthene (cerivastatin) of visiing several years ago promptly is that example is levied.Heavy dose of life-time service statins also can cause cataract.And for the hyperlipemia patient, generally all are long-term prescriptions, and the price of statins is again the most expensive in all lipid lowerers, has therefore brought very big financial burden to the patient.
Summary of the invention
The object of the present invention is to provide a kind of curative effect to be not less than statins, but side effect is little, the treatment hyperlipemia that price is low and the compound medicinal formulation of atherosclerosis.
For achieving the above object, the present invention is surprised to find that, the long chain alkanol class, particularly be rich in the myricin of the pure and mild triacontanol of octacosane, with the blood lipid regulation medicine, especially during 3-hydroxyl-3-first glutaryl coenzyme A (HMG-CoA) reductase inhibitor drug combination, under the situation that drug effect does not reduce, can significantly reduce the dosage of 3-hydroxyl-blood lipid regulation medicines such as 3-first glutaryl coenzyme A (HMG-CoA) reductase inhibitor, thereby reduce the clinical adverse of blood lipid regulation medicine.Technical solution of the present invention is as follows:
The invention provides a kind of blood lipid regulation or antiatherogenic medicine, it is characterized in that: described medicine contains to be transferred the fat active components A and transfers fat active component B, described accent fat active components A is selected from one or more of nicotinic acid class, clofibrate, phenoxy acetic acid class, HMG-CoA reductase inhibitor apoplexy due to endogenous wind, and described accent fat active component B is selected from one or more in the long-chain fatty alcohol.
Above-mentioned described medicine, wherein said accent fat active component B be selected from carbon number 16～36, more preferably carbon number 24～34, in the long-chain fatty alcohol that selects carbon number 28-32 one or more are arranged most.As one of preferred version of the present invention, wherein said accent fat active component B is a myricin.
The above-mentioned described medicine of the present invention, wherein said accent fat active components A, be preferably one or more of HMG-CoA reductase inhibitor apoplexy due to endogenous wind, preferred especially described accent fat active components A is lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin or its pharmaceutical salts.
Medicine of the present invention can be adjusted the wherein dosage of blood lipid regulation composition according to the clinical application situation, and per unit preparation for example can contain that to transfer the fat active components A be 1～20mg, and transferring fat active component B is 5～200mg.
As an embodiment of the present invention, in the wherein said medicine, the per unit preparation contains HMG-CoA reductase inhibitor 1～20mg, myricin 5～200mg.More preferably, in the wherein said medicine, the per unit preparation contains lovastatin, simvastatin, pravastatin or its pharmaceutical salts 1～20mg, myricin 5～200mg.Wherein, in the more preferably described medicine, contain lovastatin or its pharmaceutical salts 5-10mg in the per unit preparation, contain myricin 50～100mg; Perhaps contain pravastatin or its pharmaceutical salts 2-5mg in the per unit preparation, contain myricin 20～100mg; Perhaps contain simvastatin or its pharmaceutical salts 2-5mg in the per unit preparation, contain myricin 20～100mg.
The above-mentioned described medicine of the present invention, wherein said myricin, be by Cera Flava through conventional method extract obtain contain the total alkanol of octacosanol to n-Dotriacontanol, its main component is the pure and mild triacontanol of octacosane, content is respectively 60%-70% and 10%-20%.
The above-mentioned described medicine of the present invention can add suitable pharmaceutical necessities as required in case of necessity, makes suitable preparation and is used for clinical.For example, this area routine techniques be can use, capsule, tablet or granule etc. made.
The above-mentioned described medicine of the present invention the results showed to have the blood lipid regulation effect, is used for the treatment of hyperlipemia and atherosclerosis etc.
Medicine of the present invention, with different adjustment blood fat active component drug combination, especially HMG-CoA reductase inhibitor statins and myricin coupling are used, statins has potent effect for reducing fat, and the octacosanol that contains in the myricin has stronger effect for reducing blood fat, in addition, it is auxilliary mutually old mutually that myricin also has effects such as the cardiovascular function of adjusting, integration metabolic process, control atherosclerosis, complement one another, make the two use in conjunction, the performance synergism reaches 1 and adds 1 greater than 2 compound recipe effect.Simultaneously, the time-concentration relationship of statins and the time-concentration relationship of myricin can cooperatively interact, and both are administration on the 1st 3 times, make both reach the blood drug level peak simultaneously, can not cause the mutual interference of administration phase simultaneously again.
Especially, statinses such as life-time service lovastatin can cause extensive untoward reaction, and myricin is proved to be without any toxicity and shows.The present invention is surprised to find that, the untoward reaction of can cancelling out each other of HMG-CoA reductase inhibitor statins and myricin.For example, generally all can cause changes of liver function after statins is taken, show as the transaminase and raise, and the Main Ingredients and Appearance octacosanol in the myricin have direct liver protection, thereby can comprehensively prevent the generation of poisoning.The present invention is by drug combination, and under the unabated situation of drug effect, the dosage of statins can turn down 1/3, and the serious adverse reaction of its rhabdomyolysis is alleviated, and incidence rate reduces, and accomplishes more safe and effective.
When the dosage of the used statins of compound medicinal formulation of treatment hyperlipemia of the present invention and atherosclerosis has only independent use statins 2/3rds of dosage, but curative effect is not less than independent use statins, greatly reduces the side effect that independent use statins is produced.Because of having reduced the consumption of statins, thereby reduce drug price, alleviated patient's financial burden.
The specific embodiment
Further explain and describe content of the present invention by the following examples, but do not constitute limiting the scope of the invention.
Example 1: capsule
Medicine is formed:
Preparation method:
Take by weighing hypromellose and in purified water, dissolve, add an amount of ethanol, be diluted to 2% hypromellose, 30% alcoholic solution, standby; After starch, cross-linking sodium carboxymethyl cellulose, sodium bicarbonate crossed 100 mesh sieves respectively, it was standby to take by weighing recipe quantity; After getting pravastatin, myricin and crossing 120 mesh sieves, take by weighing recipe quantity,,, granulate, dry under 60 ℃ of conditions, add magnesium stearate mixing fill capsule behind the granulate promptly with 20 mesh sieves with 2% hypromellose, 30% alcoholic solution system soft material with above-mentioned auxiliary materials and mixing.
Example 2: tablet
Medicine is formed:
Preparation method:
Take by weighing hypromellose and in purified water, dissolve, add an amount of ethanol, be diluted to 50% alcoholic solution of 2%PVC, standby; After lactose, microcrystalline Cellulose crossed 100 mesh sieves respectively, it was standby to take by weighing recipe quantity; After simvastatin, the myricin that takes by weighing recipe quantity again crossed 200 mesh sieves, with after the above-mentioned auxiliary materials and mixing with the 50% alcoholic solution system soft material of 2%PVC, the granulation after drying, add the recipe quantity magnesium stearate, mix homogeneously is selected ф 6mm shallow concave punch for use, regulate pressure, tabletting promptly.
Embodiment 3 drug efficacy studies
1, experiment is prepared
1.1 normal feedstuff prescription (%) flour 53, rice flour 1918, Semen Maydis powder 718, Testa Tritici 310, yeast 415, casein 110, whole milk powder 415, analysis for soybean powder 310, bone meal 112, cod-liver oil 112, salt 110.
1.2 high lipid food prescription (%) normal feedstuff 79, cholesterol 1, yolk powder 10, Adeps Sus domestica 10.
1.3 experimental drug: myricin is available from White Cloud Mountain, Guangzhou pharmaceutical factory, and main component is the pure and mild triacontanol of octacosane, and content is respectively 65% and 15%.
2, laboratory animal grouping and experiment flow
Choose 90 of SD male rats, body weight 200～230g studies the effect of the compound medicinal formulation blood lipid regulation of treatment hyperlipemia of the present invention and atherosclerosis.Animal is divided into 9 groups at random, wherein take respectively and contain lovastatin and myricin is low by the compound medicinal formulation of 1:10 weight ratio for 6 groups, in, high dose group (is equivalent to lovastatin dosage 5mg/kg, 10mg/kg, 15mg/kg), it is low by the compound medicinal formulation of 1:10 weight ratio to contain pravastatin and myricin, in, high dose group (is equivalent to pravastatin dosage 2.5mg/kg, 5mg/kg, 10mg/kg), all the other 3 groups positive lovastatin matched groups (15mg/kg), normal feedstuff group (normal control) and high lipid food pathological model group, each group is all irritated stomach and is given distilled water or relative medicine, experimental session is except that normal physiological saline group is fed with normal diet, and other each groups are all fed with high lipid food.After the administration 21 days, each treated animal is plucked eyeball and is got blood, and separation of serum is measured blood lipid level (TC, TG, HDL-C, LDL-C).With SPSS12 data are carried out the variance analysis statistics, experimental result as shown in Table 1 and Table 2.
The influence of table 1 pair rat blood serum T-CHOL, content of triglyceride
n＝10，mean±SD
Compare with high lipid food pathological model group,
△ △ △P＜0.001; Compare with positive lovastatin matched group
* *P＜0.001
The influence of table 2 pair rat blood serum low-density lipoprotein cholesterol, high density finger protein cholesterol level
n＝10，mean±SD
Compare with high lipid food pathological model group,
△P＜0.05,
△ △ △P＜0.001; Compare with positive lovastatin matched group
*P＜0.05,
* *P＜0.001
By the experimental result of table 1 and table 2 as seen, drug administration group of the present invention is compared with model control group, basic, normal, high dosage group and positive controls all improve the effect of Serum HDL-C, significantly reduce serum TC, TG, LDL-C level, and the highly significant significant difference is arranged.Serum HDL-C can be quickened in the blood plasma cholesterol and triglyceride and transport to liver, thereby reduces cholesterol and content of triglyceride in the blood.The effect of compound medicinal formulation blood lipid regulation of the present invention has obvious dose dependent, and is the most obvious with the high dose group effect, and action intensity is all above positive controls, thereby the odds ratio list that makes HDL-C/LDL-C greatly increases during with statins.
The present invention is described according to preferred embodiment.Should be understood that the description of front and embodiment are just to illustrating the present invention.Under prerequisite without departing from the spirit and scope of the present invention, those skilled in the art can design multiple alternative of the present invention and improvement project, and it all should be understood to be within protection scope of the present invention.
Claims (10)
1. a blood lipid regulation or antiatherogenic medicine, it is characterized in that: described medicine contains to be transferred the fat active components A and transfers fat active component B, described accent fat active components A is selected from one or more of nicotinic acid class, clofibrate, phenoxy acetic acid class, HMG-CoA reductase inhibitor apoplexy due to endogenous wind, and described accent fat active component B is selected from one or more in the long-chain fatty alcohol.
2. medicine according to claim 1, wherein said accent fat active component B are selected from carbon number 16～36, more preferably one or more in carbon number 24～34 long-chain fatty alcohols.
3. medicine according to claim 1 and 2, wherein said accent fat active component B is a myricin.
4. according to the described medicine of claim 1-3, wherein said accent fat active components A is one or more of HMG-CoA reductase inhibitor apoplexy due to endogenous wind, and preferred described accent fat active components A is lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin or its pharmaceutical salts.
5. according to the described medicine of claim 1-4, in the wherein said medicine, it is 1～20mg that the per unit preparation contains accent fat active components A, and transferring fat active component B is 5～200mg.
6. medicine according to claim 5, in the wherein said medicine, the per unit preparation contains HMG-CoA reductase inhibitor 1～20mg, myricin 5～200mg.
7. medicine according to claim 6, in the wherein said medicine, the per unit preparation contains lovastatin, simvastatin, pravastatin or its pharmaceutical salts 1～20mg, myricin 5～200mg.
8. according to the described medicine of claim 1-7, in the wherein said medicine, the main component of myricin is the pure and mild triacontanol of octacosane, and content is respectively 60%-70% and 10%-20%.
9. according to any described medicine of claim 1-8, it is characterized in that described medicine is capsule, tablet or granule.
10. use in the medicine of preparation treatment hyperlipemia and/or atherosclerosis according to any described medicine of claim 1-8.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810102655A CN101543628A (en) | 2008-03-25 | 2008-03-25 | Medicament and preparation thereof for treating hyperlipemia and atherosclerosis |
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| CN200810102655A CN101543628A (en) | 2008-03-25 | 2008-03-25 | Medicament and preparation thereof for treating hyperlipemia and atherosclerosis |
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| CN200810102655A Pending CN101543628A (en) | 2008-03-25 | 2008-03-25 | Medicament and preparation thereof for treating hyperlipemia and atherosclerosis |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110693916A (en) * | 2019-09-23 | 2020-01-17 | 北京量化健康科技有限公司 | Application of blautia in preparation of product for enhancing efficacy of hypolipidemic drug for treating hyperlipidemia |
| CN114903862A (en) * | 2022-06-15 | 2022-08-16 | 湖北中古生物制药有限公司 | Policosanol atorvastatin calcium compound preparation and preparation method thereof |
-
2008
- 2008-03-25 CN CN200810102655A patent/CN101543628A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110693916A (en) * | 2019-09-23 | 2020-01-17 | 北京量化健康科技有限公司 | Application of blautia in preparation of product for enhancing efficacy of hypolipidemic drug for treating hyperlipidemia |
| CN110693916B (en) * | 2019-09-23 | 2021-08-24 | 北京量化健康科技有限公司 | Application of blautia in preparation of product for enhancing efficacy of hypolipidemic drug for treating hyperlipidemia |
| CN114903862A (en) * | 2022-06-15 | 2022-08-16 | 湖北中古生物制药有限公司 | Policosanol atorvastatin calcium compound preparation and preparation method thereof |
| CN114903862B (en) * | 2022-06-15 | 2023-08-22 | 湖北中古生物制药有限公司 | Polypolicosanol atorvastatin calcium compound preparation and preparation method thereof |
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Open date: 20090930 |