CN102600234A - Swertia mileensis dispersible tablet and preparation method thereof - Google Patents

Abstract

The invention discloses a swertia mileensis dispersible tablet and a preparation method thereof. The preparation method is characterized by comprising the following steps: extracting swertia mileensis by adopting a carbon dioxide supercritical extraction method; drying at reduced pressure; crushing the swertia mileensis into nano-paste by using a high-energy nano-impact mill; adding a functional auxiliary material to prepare the swertia mileensis dispersible tablet. By adopting the preparation method, the contents of effective components are remarkably improved, the disintegration time is remarkably shortened, the curative effect is remarkably superior to the swertia mileensis tablet, and a positive effect is obtained.

Description

Qingyedan dispersible tablet and preparation method thereof

technical field

The invention relates to the field of traditional Chinese medicines, in particular to a Qingyedan dispersible tablet and a preparation method thereof.

Background technique

Foliage Gallbladder has the effects of clearing the liver and gallbladder, clearing heat and promoting dampness, and is used for the treatment of icteric hepatitis and viral hepatitis. The existing gallbladder preparations are prepared by traditional techniques, and there are deficiencies such as incomplete extraction of active ingredients, low content of active ingredients, slow disintegration, and low curative effect.

Contents of the invention

In order to overcome the above disadvantages, the present invention provides a Qingyedan dispersible tablet with complete extraction of active ingredients, high content of active ingredients, fast disintegration speed and high curative effect and a preparation method thereof.

Invention embodiment is as follows:

Take 1570g of Foliage gallbladder, crush it into 60 mesh coarse powder, and extract it by carbon dioxide supercritical extraction method, the extraction pressure is 20-40Mpa, the extraction temperature is 20-40°C, the separator pressure is 10-20Mpa, and the separator temperature is 40-60°C. The time is 2-4 hours, the flow rate of carbon dioxide is 20-40L per hour, and the extract is obtained; the extract is dried at 60°C-80°C under reduced pressure to obtain a dry paste; the dry paste is added with 80-120g of calcium sulfate, and crushed by a high-energy nano-impact mill Mixed dry paste powder with a particle size of 200-300nm; take the mixed dry paste powder, microcrystalline cellulose 35-45g, cross-linked polyvinylpyrrolidone 35-45g, cross-linked carmellose sodium 35-45g, hypromellose Cellulose 25-35g, micropowder silica gel 15-25g, sodium chloride 5-15g, mannitol 4-6g, lactose 4-6g, mix well, wet granulate with 50-70% ethanol, dry at 60℃～80℃, Add 7 to 9 g of sodium carboxymethyl starch and 1 to 3 g of magnesium stearate, granulate it, and press it into 1000 tablets to obtain dispersible tablets of Aoba bile.

The raw material standard mentioned in above-mentioned embodiment is as follows:

Folium Folium: A Standard of the Chinese Pharmacopoeia 2010 Edition, it is the dried whole herb of the Gentianaceae plant Folium Folium, harvested in the autumn flower and fruit period, and dried in the sun.

Calcium sulfate: Chinese Pharmacopoeia 2010 edition two standards.

Microcrystalline cellulose: Chinese Pharmacopoeia 2010 edition two standards.

Cross-linked polyvinylpyrrolidone: Chinese Pharmacopoeia 2010 edition two standards.

Croscarmellose sodium: Chinese Pharmacopoeia 2010 edition two standards.

Hypromellose: Chinese Pharmacopoeia 2010 edition two standards.

Micropowder silica gel: Chinese Pharmacopoeia 2010 edition two standards.

Sodium chloride: Chinese Pharmacopoeia 2010 edition two standards.

Mannitol: Chinese Pharmacopoeia 2010 edition two standards.

Lactose: the second standard of Chinese Pharmacopoeia 2010 edition.

Carboxymethyl starch sodium: Chinese Pharmacopoeia 2010 edition two standards.

Magnesium stearate: Chinese Pharmacopoeia 2010 edition two standards.

The raw materials used in the above Qingyedan dispersible tablets can be purchased from pharmaceutical companies, and all can be used to implement the scheme of the present invention as long as they meet the national standards.

Detailed ways

Specific embodiments of the present invention 1

Take 1570g of Foliage gallbladder, crush it into a 60-mesh coarse powder, and use carbon dioxide supercritical extraction method to extract, the extraction pressure is 20Mpa, the extraction temperature is 20°C, the separator pressure is 10Mpa, the separator temperature is 40°C, the separation time is 2 hours, and the flow of carbon dioxide per hour 20L to obtain the extract; take the extract and dry it under reduced pressure at 60°C to obtain a dry paste; add 80g of calcium sulfate to the dry paste, and use a high-energy nano-impact mill to pulverize it into a mixed dry paste powder with a particle size of 200-300nm; take the mixed dry paste powder , microcrystalline cellulose 35g, crospovidone 35g, croscarmellose sodium 35g, hypromellose 25g, micropowder silica gel 15g, sodium chloride 5g, mannitol 4g, lactose 4g, mix well, Wet granulate with 50% ethanol, dry at 60°C, add 7g of sodium carboxymethyl starch, 1g of magnesium stearate, granulate, press into 1000 pieces, and make Aoba dispersible tablets.

Specific embodiment of the present invention 2

Take 1570g of Foliage gallbladder, crush it into 60 mesh coarse powder, and extract it by carbon dioxide supercritical extraction method, the extraction pressure is 40Mpa, the extraction temperature is 40°C, the separator pressure is 20Mpa, the separator temperature is 60°C, the separation time is 4 hours, and the flow rate of carbon dioxide per hour 40L to obtain the extract; take the extract and dry it under reduced pressure at 80°C to obtain a dry paste; add 120g of calcium sulfate to the dry paste, and use a high-energy nano-impact mill to pulverize it into a mixed dry paste powder with a particle size of 200-300nm; take the mixed dry paste powder , microcrystalline cellulose 45g, crospovidone 45g, croscarmellose sodium 45g, hypromellose 35g, micropowder silica gel 25g, sodium chloride 15g, mannitol 6g, lactose 6g, mix well, Wet granulate with 70% ethanol, dry at 80°C, add 9g of sodium carboxymethyl starch, 3g of magnesium stearate, granulate, press into 1000 pieces, and make Aoba bile dispersible tablets.

Specific embodiment of the present invention 3

Take 1570g of Foliage gallbladder, crush it into 60 mesh coarse powder, and use carbon dioxide supercritical extraction method to extract, the extraction pressure is 30Mpa, the extraction temperature is 30°C, the separator pressure is 15Mpa, the separator temperature is 50°C, the separation time is 3 hours, and the flow rate of carbon dioxide per hour 30L to obtain the extract; take the extract and dry it under reduced pressure at 70°C to obtain a dry paste; add 100g of calcium sulfate to the dry paste, and use a high-energy nano-impact mill to pulverize it into a mixed dry paste powder with a particle size of 200-300nm; take the mixed dry paste powder , microcrystalline cellulose 40g, crospovidone 40g, croscarmellose sodium 40g, hypromellose 30g, micropowder silica gel 20g, sodium chloride 20g, mannitol 5g, lactose 5g, mix well, Wet granulate with 60% ethanol, dry at 70°C, add 8g of sodium carboxymethyl starch, 2g of magnesium stearate, granulate, press into 1000 pieces, and make Aoba dispersible tablets.

The above examples illustrate that both extreme conditions and optimized conditions of the embodiments of the present invention can be used to make Folium Folium dispersible tablets. Inspect the practical effect of the present invention below with the Folium Chinensis dispersible tablet that embodiment 3 makes:

Comparison of active ingredient content between Qingyedan dispersible tablets and Qingyedan tablets

1 Determination method

Take this product Qingyedan dispersible tablets or Qingyedan tablets 5g, grind finely, accurately weigh, put in a 100ml measuring bottle, add 80ml of methanol, soak for 20 minutes, ultrasonically treat (power 250W, frequency 33kHz) for 15 minutes, let cool , add methanol to the mark, shake well, filter, and take the subsequent filtrate as the test solution. Take another appropriate amount of swertiamarin reference substance, weigh it accurately, add methanol to make a solution containing 0.5mg per 1ml, and use it as the reference substance solution. Octadecylsilane bonded silica gel is used as filler, methanol-0.3% formic acid solution (25:75) is used as mobile phase, the detection wavelength is 237nm, and the number of theoretical plates is not less than 2000 based on the swertiamarin peak. Accurately draw 10ul each of the reference substance solution and the test solution respectively, inject them into a liquid chromatograph, measure them, and calculate the swertiamarin content with the peak area external standard method.

2 Comparison of content of active ingredient swertiamarin

Table 1 Comparison of swertiamarin content in Qingyedan dispersible tablets and Qingyedan tablets

The above results show that compared with Qingyedan Tablets, Qingyedan Dispersible Tablets prepared by the present invention have significant advantages such as complete extraction of active ingredients and higher content of active ingredients.

Comparison of disintegration time between Qingyedan dispersible tablets and Qingyedan tablets

1 Determination of disintegration time

Measured according to Appendix Ⅻ A of Chinese Pharmacopoeia 2010 edition.

2 Comparison of disintegration time

Table 2 Comparison table of disintegration time between Qingyedan dispersible tablets and Qingyedan tablets

The above results show that the Qingyedan dispersible tablet prepared by the present invention has significant advantages such as faster disintegration speed and higher bioavailability compared with Qingyedan tablet.

Clinical Observation of Qingyedan Dispersed Tablets and Qingyedan Tablets in Treating Acute Jaundice Hepatitis

1 case situation

According to statistics of outpatient and inpatient cases, a total of 121 cases of acute icteric hepatitis were observed, with an average age of 39 years. All patients had jaundice, 68 cases had a jaundice index between 20 and 39, and 53 cases had a jaundice index above 40. All 121 patients had elevated alanine aminotransferase.

2 treatment methods

The patients were randomly divided into two groups, the test group took Qingyedan dispersible tablets, and the control group took Qingyedan tablets.

3 Evaluating Criteria for Efficacy

Cured: the clinical symptoms disappeared, and the liver function tests were normal for two consecutive times.

Effective: the clinical symptoms basically disappeared, the liver function improved, and one or two did not return to normal.

Ineffective: no improvement in clinical symptoms, and more than two liver function tests did not return to normal.

4 Clinical observation results

Table 3 Comparison table of clinical efficacy of Qingyedan dispersible tablets and Qingyedan tablets

The above clinical curative effect observation results show that the curative effect of Qingyedan dispersible tablet prepared by the present invention is significantly higher than that of Qingyedan tablet in the treatment of acute icteric hepatitis, p<0.05.

Claims (3)

1. a Chinese medicine of treating hepatitis is characterized in that getting Herba Swertiae Mileensis 1570g, is ground into 60 order coarse powder; The employing carbon dioxide supercritical extraction method is extracted, extracting pressure 20～40Mpa, 20～40 ℃ of extraction temperature; Separator pressure 10～20Mpa, 40～60 ℃ of separator temperatures, disengaging time 2～4 hours; Carbon dioxide flow is 20～40L per hour, gets extracting solution; Get 60 ℃～80 ℃ drying under reduced pressure of extracting solution, get dry extract; Get dried cream and add calcium sulfate 80～120g, adopt the impact grinding of high energy nanometer to be ground into the mixing dried cream powder of particle diameter 200～300nm; Get the mixing dried cream powder, microcrystalline Cellulose 35～45g, crospolyvinylpyrrolidone 35～45g, cross-linking sodium carboxymethyl cellulose 35～45g; Hypromellose 25～35g, micropowder silica gel 15～25g, sodium chloride 5～15g, mannitol 4～6g; Lactose 4～6g, mix homogeneously, with 50～70% ethanol wet granulations, 60 ℃～80 ℃ dryings; Add carboxymethyl starch sodium 7～9g, magnesium stearate 1～3g, granulate is pressed into the Herba Swertiae Mileensis dispersible tablet.

2. according to claim 1 said preparation method of Chinese medicine, it is characterized in that getting Herba Swertiae Mileensis 1570g, be ground into 60 order coarse powder; The employing carbon dioxide supercritical extraction method is extracted, extracting pressure 20～40Mpa, 20～40 ℃ of extraction temperature; Separator pressure 10～20Mpa, 40～60 ℃ of separator temperatures, disengaging time 2～4 hours; Carbon dioxide flow is 20～40L per hour, gets extracting solution; Get 60 ℃～80 ℃ drying under reduced pressure of extracting solution, get dry extract; Get dried cream and add calcium sulfate 80～120g, adopt the impact grinding of high energy nanometer to be ground into the mixing dried cream powder of particle diameter 200～300nm; Get the mixing dried cream powder, microcrystalline Cellulose 35～45g, crospolyvinylpyrrolidone 35～45g, cross-linking sodium carboxymethyl cellulose 35～45g; Hypromellose 25～35g, micropowder silica gel 15～25g, sodium chloride 5～15g, mannitol 4～6g; Lactose 4～6g, mix homogeneously, with 50～70% ethanol wet granulations, 60 ℃～80 ℃ dryings; Add carboxymethyl starch sodium 7～9g, magnesium stearate 1～3g, granulate is pressed into the Herba Swertiae Mileensis dispersible tablet.

3. according to claim 1 said preparation method of Chinese medicine, it is characterized in that getting Herba Swertiae Mileensis 1570g, be ground into 60 order coarse powder; The employing carbon dioxide supercritical extraction method is extracted, extracting pressure 30Mpa, 30 ℃ of extraction temperature; Separator pressure 15Mpa, 50 ℃ of separator temperatures, disengaging time 3 hours; Carbon dioxide flow is 30L per hour, gets extracting solution; Get 70 ℃ of drying under reduced pressure of extracting solution, get dry extract; Get dried cream and add calcium sulfate 100g, adopt the impact grinding of high energy nanometer to be ground into the mixing dried cream powder of particle diameter 200～300nm; Get the mixing dried cream powder, microcrystalline Cellulose 40g, crospolyvinylpyrrolidone 40g, cross-linking sodium carboxymethyl cellulose 40g; Hypromellose 30g, micropowder silica gel 20g, sodium chloride 10g, mannitol 5g; Lactose 5g, mix homogeneously, with 60% ethanol wet granulation, 70 ℃ of dryings; Add carboxymethyl starch sodium 8g, magnesium stearate 2g, granulate is pressed into the Herba Swertiae Mileensis dispersible tablet.