CN1418637A - Silicibinin-N-methylglucamine disperser for treating hepatitis, and its prepn. method - Google Patents

Abstract

The present invention relates to a silybin meglumine dispersing tablet for curing hepatitis and its preparation method. Said invention provides its structural formula and its molecular formula, and its composition is composed of C22H39O15N and ten auxiliary materials. Said invented dispersing tablet can be mainly used for curing acute hepatitis, chronic hepatitis, initial cirrhosis, fatty liver and protecting liver for toxic hepatic damage.

Description

Silybin meglumine dispersible tablet of treatment hepatitis and preparation method thereof

Technical field

The present invention relates to pharmaceutical, particularly relate to treatment silybin meglumine dispersible tablet and preparation method thereof.

Background technology

Hepatitis is meant the liver inflammation.It comprises the hepatitis that Different types of etiopathogenises is different.But viral hepatitis is the most common in the daily life, so people abbreviate viral hepatitis as hepatitis habitually.Viral hepatitis is that common clinically a kind of liver damage is main, the infectious disease of immune dysfunction.It has the sickness rate height, and the course of disease is long, and the patient's condition repeatability is strong, and the characteristics that hazardness is bigger if do not treat effectively and timely, very easily change hepatitis interstitialis chronica and hepatocarcinoma into.At present viral hepatitis is mainly divided five kinds of first type, B-mode, third type, fourth type and hepatitis Es, finds to have own type hepatitis and hepatitis G in recent years again.Wherein first type and hepatitis E have self limiting, generally can not transfer to chronicly, and minority can develop into liver cirrhosis.Chronic hepatitis B and primary hepatoma substantial connection arranged.

According to authority statistics, China is the viral hepatitis district occurred frequently, annual about 1,200,000 examples of acute viral hepatitis that take place in the whole nation, wherein 50% be the first type, 25% is B-mode, 5% is third type, 10% is penta type, surplus 10% be own type, heptan type.About 3,200 ten thousand examples of China's chronic hepatitis patient are died from about 300,000 examples of liver patient every year, and wherein 50% is primary hepatoma, and most and second, hepatitis C are relevant.Calculate that according to existing investigation China has 1.2 hundred million people to carry hepatitis B virus, the chronic viral hepatitis B patient is about, and 3,000 ten thousand, 3,800 ten thousand people carry hepatitis C virus., almost be that national people ten have one only from the numeral of hepatitis B virus carriers.

Chronic hepatitis B is a kind of chronic, infectious disease that is caused by hepatitis B virus (HBV), and serious harm health influences quality of life.Chronic hepatitis B is a kind of commonly encountered diseases, frequently-occurring disease.HBV infects and is global distribution, and possibility world populations more than half were once infected, the new infection of annual generation 5,000 ten thousand examples, annual 1 million people's death.5% of about world population is chronic HBsAg carrier.Can be divided into according to hepatitis B surface antigen (HBsAg) carrying rate: high popular district (＞8%), in popular district (2%-7%), low popular district (＜2%).China is one of high popular district.According to statistics, the present hepatitis B virus infection rate of China overview is: anti-HBc and/or anti-HBs positive person are about 60%; Non-infection population accounts for 26%; Chronic hepatitis B reaches 2%; The male chronic asymptomatic HBsAg carrier of HBsAg is 10%; The chronic asymptomatic HBV carrier of HBsAg feminine gender is 2%.This shows that the popular situation of China's hepatitis B is very severe.

Concerning the patient, hepatitis virus is killed medicine needs taking dose bigger, and side effect is all more serious, in the water dissolving bad, thereby bioavailability of medicament is not high, effect is undesirable.How overcoming above-mentioned defective, improve effect, the reduction side effect of hepatitis B control medicine, is that contemporary pharmaceutics is badly in need of one of key technology that solves.

Summary of the invention

Purpose of the present invention provides a kind of put in the water can quickly disintegrated, the remarkable dispersible tablet of therapeutic effect, and preparation method thereof.

The object of the invention can reach by following measure: the silybin meglumine dispersible tablet of treatment hepatitis, and it is made up of principal agent and adjuvant, wherein:

One, principal agent: silybin meglumine

Chemical name: 2-(2,3-dihydro-2-(4-hydroxy 3-methoxybenzene base)-3-(hydroxymethyl)-1,4-benzo dioxin-6-yl)-2,3-dihydro-3,5,7-trihydroxy-4H-1-.alpha.-5:6-benzopyran-4-ketone

English name: Silybin Meglumine

Structural formula:

Molecular formula: C ₃₂H ₃₉O ₁₅N

Two, adjuvant: raw material is by weight percentage formed, totally ten kinds of adjuvants:

A lactose: 5-80%

B mannitol: 2.5-45%

C carboxymethyl starch sodium: 1-12%

D sodium carboxymethyl cellulose: 1-3%

E hydroxypropyl emthylcellulose: 1-3%

F microcrystalline Cellulose: 5-50%

G polyvinylpyrrolidone: 1-30%

H cetyl sulfo-sodium succinate: 0.05-1.0%

I sodium lauryl sulphate: 0.05-1.0%

J magnesium stearate: 0.5-2.0%

The method of silybin meglumine dispersible tablet: earlier the principal agent micropowder is handled (＜100 μ m), mixes pulverizing with all adjuvants except that carboxymethyl starch sodium, sieve below 30 orders, and then with the carboxymethyl starch sodium mix homogeneously, tabletting, promptly.

The present invention has following advantage compared to existing technology: dispersible tablet be meant place water fast disintegrate form the pharmaceutical preparation of even suspension.Special performances such as this dosage form has taking convenience, it is fast to absorb, bioavailability is high and untoward reaction is little have become one of contemporary pharmaceutics new technique.This dosage form is used for tablet that dosage is unfavorable for that more greatly old man or child swallow or the medicine that capsule improves, some need absorb instant effect to the irritant medicine of gastrointestinal tract, acute pain etc. and has shown bigger medication advantage.

The specific embodiment

Enumerate three embodiment below, the present invention is further specified

Embodiment 1

Earlier 100 gram principal agent silybin-N-methylglucamine places (＜100 μ m) being vulcanized sodium succinate, 0.05 with all adjuvants removing 6 gram carboxymethyl starch sodium as 54.4 gram lactose, 20 gram mannitol, 1 gram carboxymethyl cellulose sodium, 3 gram hydroxypropyl emthylcelluloses, 5 gram microcrystalline Cellulose, 10 gram polyvinylpyrrolidones, 0.05 gram cetyl restrains sodium lauryl sulphate and 0.5 and restrains magnesium stearate and mix pulverizing, cross the following sieve of 30 orders, and then with the carboxymethyl starch sodium mix homogeneously, tabletting is promptly.Ten kinds of adjuvant gross weights are 100 grams, make 1000,100 milligrams of every adjuvants, and 100 milligrams of principal agents, promptly dispersible tablet weighs 200 milligrams.Embodiment 2

Principal agent 200 gram replaces the principal agent of embodiment 1, and all the other ten kinds of supplementary product consumptions and preparation method are all with embodiment 1, and then dispersible tablet weighs 300 milligrams, 200 milligrams of every principal agents.

Embodiment 3

Principal agent 500 grams replace the principal agent of embodiment 1, and all the other are all with embodiment 1 or 2, and then dispersible tablet weighs 600 milligrams, and every contains 500 milligrams of principal agents.The embodiment of the invention contains 100 milligrams of principal agents, 200 milligrams, 500 milligrams/sheet totally three kinds of specifications, and other contains the embodiment of principal agent 50-1000 milligram/sheet, and method is the same.

Product of the present invention is mainly treated acute hepatitis, chronic hepatitis, and first cirrhosis, fatty liver protects the liver dirty during toxic hepatitis (as taking prejudicial medicine of hepatocyte or frequent heavy drinking).

Claims (2)

1, the silybin meglumine dispersible tablet of treatment hepatitis is characterized in that it is made up of principal agent and adjuvant, wherein:

One, principal agent: silybin meglumine

Chemical name: 2-(2,3-dihydro-2-(4-hydroxy 3-methoxybenzene base)-3-(hydroxymethyl)-1,4-benzo dioxin-6-yl)-2,3-dihydro-3,5,7-trihydroxy-4H-1-.alpha.-5:6-benzopyran-4-ketone

English name: Silybin Meglumine

Structural formula:

Molecular formula: C ₃₂H ₃₉O ₁₅N

Two, adjuvant: raw material is by weight percentage formed, totally ten kinds of adjuvants:

A lactose: 5-80%

B mannitol: 2.5-45%

C carboxymethyl starch sodium: 1-12%

D sodium carboxymethyl cellulose: 1-3%

E hydroxypropyl emthylcellulose: 1-3%

F microcrystalline Cellulose: 5-50%

G polyvinylpyrrolidone: 1-30%

H cetyl sulfo-sodium succinate: 0.05-1.0%

I sodium lauryl sulphate: 0.05-1.0%j magnesium stearate: 0.5-2.0%

2, the method for silybin meglumine dispersible tablet according to claim 1 is characterized in that earlier the principal agent micropowder being handled less than 100 μ m, mixes pulverizing with all adjuvants except that carboxymethyl starch sodium, cross the following sieve of 30 orders, and then with the carboxymethyl starch sodium mix homogeneously, tabletting, promptly.