CN1907360A - Medicinal compositions comprising biphenyldicarboxylate - Google Patents

Abstract

Disclosed is a synergic medicinal composition containing biphenyldicarboxylate and Chinese medicinal extracts, and its use in preparing medicament for the subsidiary treatment of hepatitis.

Description

A kind of Pharmaceutical composition that contains bifendate

Invention field

The present invention relates to the Pharmaceutical composition formed by bifendate and Chinese medicine extract, and the purposes of said composition in the medicine of preparation adjuvant treating hepatitis.

Background technology

Hepatitis has multiple sorting technique clinically, classifies as (1) nosetiology: viral hepatitis can be divided into five types is first, second, third, fourth, penta.(2) clinical classification can be divided into following a few type: 1. acute anicteric hepatitis, this is a modal type in the viral hepatitis, see with B-mode, third type, hepatitis D more, general this type of hepatitis clinical symptoms is less, and transaminase's elevated levels is lower, and Histological change is light, mortality rate is lower, but the course of disease can be delayed the long period, and " three is slow " characteristics are arranged, and morbidity is slow, recovery is slow, delay also slow (referring to the long meaning slowly); 2. acute icterohepatitis is less relatively compared with anicteric hepatitis, and the state of an illness is a self limiting often, and how good prognosis is, but minority can develop into hepatitis gravis; 3. chronic hepatitis: relevant experts in 1994 propose the name and the suggestion of chronic hepatitis again, with the cause of disease is the diagnosis name that chronic hepatitis is determined on the basis, simultaneously ordered grade scale, formulated standard by stages according to degree of hepatic fibrosis again according to the downright bad order of severity of hepatitis inflammation; 4. hepatitis gravis can be divided into acute heavy type, severe subacute and chronic heavy type again; 5. cholestatic hepatitis.

Wherein hepatitis B is caused by hepatitis B virus, serves as main a kind of infectious disease that also can cause multiple organ injury with the liver inflammatory lesion.China is the most popular country of hepatitis B, reaches more than 35% some local crowd infection rate, and be the most serious infectious disease of current harm people ' s health.According to investigations, China's hepatitis B patient is about 2,700 ten thousand, and annual New Development patient about 9,000,000.

The hepatitis B clinical manifestation is various, easily develops into chronic hepatitis and liver cirrhosis, and a few peoples finally develop into hepatocarcinoma.Hepatic fibrosis is the total pathological change of many chronic hepatopathy evolutions, and the damage of chronic, persistence is the prerequisite that hepatic fibrosis forms.Cause the factor of hepatic injury a lot,, hepatitis B, liver cirrhosis, take some drugs for a long time and can cause acute and chronic liver injury generally because of factors such as medicine, a large amount of ethanol, allergy cause acute liver damage.By reducing detrimental effect to liver function, can adjuvant treating hepatitis.

The medicine that is used for the treatment of the acute and chronic hepatic injury at present, commonly used have bifendate, a diammonium glycyrrhizinate etc.These chemicalses generally have certain side effect, and cause that therapeutic effect at a specified future date is poor, problem such as Strain produces after drug resistance phenomenon, the drug withdrawal relapse rate height.

The curative effect of Chinese medicine hepatitis B is proved by a large amount of clinical trials.Chinese medicine all can be brought into play curative effect preferably at aspects such as antiviral, adjusting immunity of organisms, protection hepatocyte.But Chinese medicine preparation ubiquity onset at present is slow, needs problems such as life-time service.

Therefore, Western medicine and Chinese Medicine and Clavicular need be got up, i.e. synergism is played in Chinese medicine and western medicine combination, solves the problem that above-mentioned Western medicine and Chinese medicine exist in auxiliary treatment all kinds hepatitis separately, produces synergistic therapeutic effect simultaneously.

Summary of the invention

One object of the present invention is to provide the Pharmaceutical composition of being made up of bifendate and a kind of Chinese medicine extract, and wherein the Chinese medicine extract of said composition prepares (for example claim 4) according to the method among the Chinese patent CN1193766C, and is as follows:

After Fructus Gardeniae is pulverized, the water extraction 3 times that adds 5 times of amounts respectively, merge extractive liquid, filters, and adds the concentrated hydrochloric acid of medical material amount 1% (M/V), stir slightly, leave standstill, after waiting to separate out gelatinous precipitate, the centrifugal supernatant of telling, cross the macroporous adsorptive resins of having handled well, after upper prop finishes, water fully be eluted to effluent clarification and color light after, add 95% ethanol elution, collect eluent, cross the neutral alumina post that is equivalent to 0.3 times of amount of medical material, 95% ethanol elution is collected eluent, be concentrated into driedly, promptly get light yellow to the off-white color Fructus Gardeniae extract.

One object of the present invention is to provide the purposes of above-mentioned Pharmaceutical composition in preparation auxiliary treatment all kinds hepatitis medicament.

This Chinese medicine the water extracted immersing paste is called " the described Chinese medicine extract of this paper (or above) " hereinafter.

Above-mentioned composition and mixing acceptable accessories can be made acceptable forms clinically, as tablet, capsule, granule, oral liquid, subcutaneous administration preparation, suppository etc.

Pharmacological research

The main pharmacodynamics of Pharmaceutical composition of the present invention studies confirm that it has strong transaminase lowering effect, i.e. function for protecting liver and reducing enzyme activity.

Edit with reference to Zhang Juntian, " modern pharmacology test method " (volume two), combined publication society of China Concord Medical Science University of Beijing Medical University, the 1397-1398 page or leaf, disclosed method in " first segment chmice acute chemical liver injury model ", set up the acute chemical liver injury model of mouse carbon tetrachloride, carry out the pharmacodynamics test of Pharmaceutical composition anti-liver injury of the present invention.

The test grouping:

1 normal control group: animal does not do any processing, and normal physiological saline is irritated stomach;

2 model control group: after the animal model modeling success, normal physiological saline is irritated stomach;

2 pure Chinese drug-treated group: the water extracted immersing paste 1.07g/kg body weight as indicated above

3 bifendate groups: the 10mg/kg body weight is irritated stomach

4 compositions groups: 10mg/kg body weight bifendate+the water extracted immersing paste 1.07g/kg body weight mentioned above is irritated stomach.

Following table has shown the influence of each group to Mouse Liver function leading indicator GOT, GPT.

Group	Number of animals	GOT (active unit)	GPT (active unit)
				The normal control group	10	20.78±16.75	48.31±17.35
Model control group	10	250.76±76.58	306.25±59.47
				Pure Chinese drug-treated group	10	174.22±59.45	227.25±51.78
The bifendate group	10	101.89±34.89	207.85±35.98
				The compositions group	10	71.32±19.32	97.23±39.12

This table shows that all there is significant difference (P＜0.05) in each group (pure Chinese drug-treated group, bifendate group, compositions group) of treatment with model control group, and all there are significant difference (P＜0.05) in compositions group and pure Chinese drug-treated group, compositions group and bifendate group.Show that there are cooperative effect in bifendate and described Chinese medicinal components in the compositions group.

The pharmaceutics test

Can produce the tablet that contains following component in a conventional manner:

Component Mg/ sheet

Pharmaceutical composition 200-1000 of the present invention

Corn starch 125.0

Pulvis Talci 75.0

Magnesium stearate 1.0

Wherein compositions is made up of with weight ratio bifendate and Chinese medicine extract mentioned above at 1: 107.

Can produce the capsule that contains following component in a conventional manner:

Component Mg/ sheet

Pharmaceutical composition 200-1000 of the present invention

Lactose 10.0

Corn starch 20.0

Talcum 5.0

Wherein compositions is made up of with weight ratio bifendate and Chinese medicine extract mentioned above at 1: 107.

Claims (2)

1 one kinds of Pharmaceutical compositions, it is made up of with weight ratio bifendate and Chinese medicine extract at 1: 107, and described Chinese medicine extract prepares by following method:

After Fructus Gardeniae is pulverized, the water extraction 3 times that adds 5 times of amounts respectively, merge extractive liquid, filters, and adds the concentrated hydrochloric acid of medical material amount 1% (M/V), stir slightly, leave standstill, after waiting to separate out gelatinous precipitate, the centrifugal supernatant of telling, cross the macroporous adsorptive resins of having handled well, after upper prop finishes, water fully be eluted to effluent clarification and color light after, add 95% ethanol elution, collect eluent, cross the neutral alumina post that is equivalent to 0.3 times of amount of medical material, 95% ethanol elution is collected eluent, be concentrated into driedly, promptly get light yellow to the off-white color Fructus Gardeniae extract.

2 compositionss as claimed in claim 1 using in the medicine of preparation adjuvant treating hepatitis.