WO2003057229A1

WO2003057229A1 - Antiviral and antipyretic formulation and the preparation method thereof

Info

Publication number: WO2003057229A1
Application number: PCT/CN2003/000025
Authority: WO
Inventors: Wenhan Ma
Original assignee: Wenhan Ma
Priority date: 2002-01-14
Filing date: 2003-01-14
Publication date: 2003-07-17
Also published as: CN1148220C; CN1564692A; AU2003203326A1; CN1363366A; CN1233400C

Abstract

The present invention relates to a pharmaceutical composition, more particularly, an antiviral and antipyretic formulation which is prepared with vegetal Chinese medicinal herbs, and the preparation method thereof. The formulation is primarily produced with raw materials as follows: isatis leaf (Isatidis Folium) 10-60g, scutellaria (Scutellariae Radix) 120-250g, lonicera (Lonicerae Flos) 120-250g, synthetic bovine bezoar (Bovis Bezoar Syntheticum) 1-3g, forsythia (Forsythiae Fructus) 60-150g, bamboo leaf (Lophatheri Folium) 20-80g, arctium (Arctii Fructus) 20-80g, and mint (Menthae Herba) 20-80g, by weight. Additionally, correctives, suitable adjuvants, and pH modifiers which can adjust pH to 6.5-7 are added to therein. The invention formulation has strong antiviral effect and a wide spectrum of antiviral; can rapidly and effectively cure virus influenza, upper respiratory tract infection caused by common cold, and pulmonary infection; can also effectively treat herpes zoster, parotitis and viral conjunctivitis. Moreover, it has antibacterial, antiphlogistic, antipyretic and increasing immunity effect, and excellent safety property.

Description

W 03 0 An antiviral antipyretic preparation and its preparation method TECHNICAL FIELD The present invention relates to a pharmaceutical composition, in particular to an antiviral antipyretic drug made from plant Chinese herbal medicine. BACKGROUND In general, colds are classified into common colds and influenza, which are a kind of respiratory infectious diseases that seriously endanger human health. It has a high incidence and a wide range of effects. It can often cause sinusitis, pharyngitis, bronchi, pneumonia, and asthma. It is also one of the main causes of death in elderly and pediatric patients. At present, in the clinical treatment of colds, symptomatic treatments such as antibacterial, anti-inflammatory, anti-allergic, antipyretic and analgesic or antiviral treatment are usually used. Antibacterials are commonly used for injection drugs such as penicillin; antiallergic drugs are commonly used for chlorpheniramine; antipyretic and analgesic, drugs such as aspirin and paracetamol are commonly used. Antivirals are commonly used in medicines such as Virin and Banlangen granules. According to the different types of colds, traditional Chinese medicine is usually treated with Xinwenjie table and Xinliangjie table, such as decoction and proprietary Chinese medicine. The efficacy of the above drugs is generally 3 to 4 days or longer before they can reduce fever, the effect is slow, and the treatment cycle is long. SUMMARY OF THE INVENTION The purpose of the present invention is to overcome the deficiencies in the background art and provide an antiviral antipyretic drug that can have a significant curative effect against viral respiratory infections in the short term. '

The invention is implemented as follows:

The present invention is made of raw materials composed of the following weights: 10 ~ 60 grams of big green leaves, 120 ~ 250 grams of Scutellaria baicalensis, 120 ~ 250 grams of honeysuckle, 1 ~ 3 grams of artificial bezoar, 60 ~ 150 grams of acacia, 20 bamboo leaves ~ 80 grams, bovine seeds 20 ~ 80 grams, mint 20 ~ 80 grams; and adding flavoring agent and appropriate amount of auxiliary materials; and pH adjuster, so that the pH value is between 6.5 ~ 7.

Wherein, the big green leaves can also be used isatis indigotica; the artificial bezoar can also be used bezoar; the light bamboo leaves can also be used bamboo leaves or houttuynia; the ox seeds can also be used hundred or mountain beans; Mint oil can also be used as the mint, and the green acacia can also be used amaranth or houttuynia cordata. It is also possible to implement the invention T CN03 / 00025 efficacy.

The flavoring agent is selected from glycyrrhizin or crude licorice extract and at least one of the following raw materials: stevioside, aspartame, cyclamate, protein sugar, and the like.

The auxiliary material is selected from at least one of the following raw materials: starch, cellulose, lactose, dextrin, xylitol, carboxymethyl cellulose, microcrystalline cellulose, micronized silica gel, sucrose, glucose, and the like.

The pH regulator can be selected from one of the following raw materials: NaHC03, sodium citrate, sodium carbonate.

The present invention is a symptom of wind-heat type or mild-disease-healthy diseases such as those caused by influenza and common cold caused by influenza virus infection, tonsillitis, tracheitis, shingles and mumps, and viral ophthalmic conjunctivitis. The effect is remarkable. Symptoms include fever, chills, headache, general soreness, weakness, sore throat, nasal congestion, runny nose, nasal swelling and pain, exhaled burning sensation, cough, chest pain, no sputum or less sputum and coughing, etc .; or see fever, parotid pain Pain and swelling; or see shingles, severe pain, and insomnia in the ribs and head; or see redness of ocular conjunctivitis infection.

Efficacy of the present invention-Most patients with tonsillitis and pharyngitis can take their medicine for one day and then return to normal body temperature to achieve the basic cure (that is, no longer take the medicine and the symptoms gradually disappear).

Patients with bronchitis and bronchial pneumonia can take control of the virus for 2 days, their virus can be controlled, their temperature will return to normal, and other symptoms will basically disappear within 3 days. For patients with virus and bacterial infection, the drug can be used to control the virus first, and then treated with antibiotics. Most of them can return to normal within 3 days. Compared with antibiotics alone, the course of disease can be greatly shortened.

Patients with shingles and mumps can control the virus after taking the medicine for two days, so that the disease tends to heal.

The invention also has good curative effect on viral ocular conjunctivitis.

Part of the in vitro antiviral experiment of the antiviral antipyretic preparation of the present invention was performed in June 2001 by the Institute of Chinese Materia Medica, China Academy of Chinese Medicine. The conclusion is: "The experimental results show that antiviral antipyretic granules have different degrees of inhibition on Ard-3, Ard-7, parainfluenza-1, RSV, HSV-K and HSV-2 in an in vitro cell culture system. The effective concentration range is 0.19 ~ 1.56mg / ml, the IC is between 0.252 ~ 0. 282, and the TI is between 5.0 ~ 6.3. Compared with the control (ribavirin), there is a significant difference, P <0.01. Implementation of the invention Best way Example 1: The present invention is a pharmaceutical preparation made of the following weight ratio raw materials:

10 grams of big green leaves, 120 grams of Scutellaria baicalensis, 120 grams of honeysuckle, 1 gram of artificial bezoar, 60 grams of acacia, 20 grams of light bamboo leaves, 20 grams of ox seeds, 20 grams of mint; and 4 grams of licorice extract, stevia 2.1 grams of glucosides; and appropriate amounts of excipients: starch, lactose, microcrystalline cellulose; and pH regulator: NaHC03, and the pH value is between 6.5 ~ 7.

The preparation method includes the following steps:

1. Extract large green leaves three times with 70% ethanol 8 times, 6-8 hours each time, combine the extracts, and then filter to obtain the filtrate.

2. Distill peppermint to extract volatile oil, and add oil and cyclodextrin to wrap it.

3. Scutellaria baicalensis was boiled to extract the acid precipitation method to extract baicalin.

4. Blend honeysuckle, acacia, ox, and light bamboo leaves, add 10 times the amount of water and extract twice; 8 times the amount of water for the third extraction, the time is 2 hours, 2 hours, 1 hour (available in the multifunctional extractor) Inside) ;

5. Combine the extracts under reduced pressure and concentrate to a concentration of 1: 1 or 1: 0.5; add ethanol: 65% ~ 70%, and let stand for 48 hours;

6. Filter the supernatant again; concentrate to a moderately added flavoring agent to dissolve it; and then spray-dried or vacuum-dried to dry powder;

7. Add excipients, peppermint oil inclusions, artificial bezoar, baicalin and PG regulator, and mix well;

8. Wet material is made with 90 ~ 85% ethanol as the binder; granulated by granulation mechanism; dried at 60 ° C, thousands of products are collected after 24 to 36 hours and granulated; or granulated by dry method Take whole grains.

9, and then packed by a packaging machine, the drug specifications are: 10 grams per pack of sugar (about 9 grams of crude drugs), 4 grams per pack (about 9 grams of crude drugs) of sugar-free granules; boxing; quality inspection; Can be finished products. Example 2: The present invention is a pharmaceutical preparation made of the following raw materials with the following weight ratios: 60 grams of Daqingye, 250 grams of Scutellaria baicalensis, 250 grams of honeysuckle, 3 grams of artificial bezoar, 150 grams of acacia, 80 grams of light bamboo leaves, ox seed 80g, mint 80g; and added flavoring agent: 4 ~ 5g of licorice extract, stevia 5 to 7 grams of glucosides; and appropriate amounts of excipients: starch, carboxymethyl cellulose, microcrystalline cellulose, lactose; and a pH regulator: NaHC03, so that the pH value is between 6.5 to 7.

Its production process is the same as in Example 1.

Example 3: The present invention is a pharmaceutical preparation of the best range formula made from the following weight parts of raw materials-Daqingye 10 ~ 30 grams, Scutellaria baicalensis 120 ~ 200 grams, honeysuckle 120 ~ 200 grams, artificial bezoar 1 ~ 1.5 grams, 60 ~ 120 grams of acacia, 20 ~ 40 grams of light bamboo leaves, 20 ~ 40 grams of beef seeds, 20 ~ 40 grams of mint; and added flavoring agents: 2 ~ 5 grams of licorice extract, 2 ~ 4 grams of stevioside ; A suitable amount of auxiliary materials: starch, lactose, xylitol, carboxymethyl cellulose, microcrystalline cellulose; and a pH regulator: NaHC03, so that the pH value is between 6.5 ~ 7.

Its production process is the same as in Example 1.

The usage of this medicine is-adult (based on 60 kg body weight) 2 packets each time, 3 times a day. Take after warm water dissolves. Body-3 packs for patients weighing 75 kg or more. Pediatric weight reduction. Generally, half a packet is served below 15 kg; 1 packet is served per 15 to 30 kg; 1.5 to 2 packets are served per 30 kg or more. Precautions:

1. This medicine should not be taken at the same time as macrolide drugs (such as Lijunsha, erythromycin), so as not to reduce the efficacy;

2. After taking the medicine, patients should keep warm, rest, and avoid being affected by cold;

3. If the high fever patients still feel cold and sweat-free after taking the medicine for 1 ~ 2 hours, they can take further protective measures or add sweat medicine (such as aspirin). Industrial Applicability The invention has the advantages of: strong antiviral effect and broad antiviral spectrum; quick effect and good curative effect on upper respiratory tract infection and lung infection caused by viral influenza and common cold; on shingles, mumps, Viral ocular conjunctivitis also has very good effects. It also has antibacterial, anti-inflammatory, antipyretic, and immune-enhancing effects; and has good safety.

The analysis of the curative effect of the antiviral antipyretic preparation of the present invention (treatment group) and the application of "Shuanghuanglian Oral Liquid", and a comparison of the two are shown in Tables 1 to 3. Efficacy analysis of antiviral antipyretic granules

Effect of Shuanghuanglian Oral Liquid

Comparison of treatment group and control group Classification Total number of cases with significant curative effect Mean time of treatment with significant curative effect Treatment group 104 103 99% 1. 18 days Control group 104 95 91% 3. 57 days

Claims

Rights request

1. An antiviral antipyretic preparation, which is characterized in that it is made of the following raw materials: Daqingye 10 ~ 60 grams, Scutellaria baicalensis 120 ~ 250 grams, honeysuckle 120 ~ 250 grams, artificial bezoar 1 ~ 3 grams, 60 ~ 150 grams of acacia, 20 ~ 80 grams of light bamboo leaves, 20 ~ 80 grams of beef seeds, 20 ~ 80 grams of mint; and added flavoring agents; and appropriate amount of auxiliary materials; and pH adjuster, so that the pH value is 6.5 ~ Between 7.

2. The antiviral antipyretic preparation according to claim 1, characterized in that the artificial bezoar can also be selected from bezoar.

3. The antiviral antipyretic preparation according to claim 1, wherein the light bamboo leaves can also be selected from bamboo leaves or houttuynia cordata.

4. The antiviral antipyretic preparation according to claim 1, characterized in that the bovine seeds can also be selected from Baibei or Mangosteen.

5. The antiviral antipyretic preparation according to claim 1, wherein the peppermint is also selected from peppermint oil.

6. The antiviral antipyretic preparation according to claim 1, characterized in that the big green leaf can also be isatis root.

7. The antiviral antipyretic preparation according to claim 1, characterized in that: said Atractylodes spp. Can also be selected from A. spp. Or Houttuynia cordata.

8. The antiviral antipyretic preparation according to claim 1, characterized in that: said flavoring agent is licorice extract or crude licorice extract and at least one of the following raw materials: stevioside, Aspartame, cyclamate, meringue.

9. The antiviral antipyretic preparation according to claim 1, characterized in that: as the auxiliary material, at least one of the following raw materials can be selected: starch, cellulose, lactose, dextrin, xylitol, carboxymethyl Cellulose, microcrystalline cellulose, micronized silica gel, sucrose, glucose.

10. The antiviral antipyretic preparation according to claim 1, wherein the pH adjuster can be selected from one of the following raw materials: NaHC0 ₃ , sodium citrate, and sodium carbonate.

11. The antiviral antipyretic preparation according to claim 1, characterized in that: it is a pharmaceutical preparation with an optimal range formula made of the following raw materials in parts by weight:

Large green leaves 10 ~ 30 grams, Scutellaria baicalensis 120 ~ 200 grams, honeysuckle 120 200 grams, artificial bezoar 1 ~ 1.5 grams, Qingqiao 60 ~: 120 grams, light bamboo leaves 20 ~ 40 grams, ox seeds 20 ~ 40 grams, mint 20- 40 grams; and added flavoring agent: 2 ~ 5 grams of licorice extract, 2 ~ 4 grams of stevioside; proper amount of excipients: starch, lactose, xylitol, carboxymethyl cellulose, microcrystalline cellulose; and pH adjustment Agent: NaHC03, make the pH value at 6.5 ~

12. A method for preparing an antiviral antipyretic preparation, which is characterized in that it comprises the following steps: a), leaching large green leaves three times with 70% ethanol 8 times, each time 6-8 hours, combined leaching The liquid was extracted and then filtered to obtain a filtrate.

b) Distill the volatile oil from the peppermint and wrap it with β-cyclodextrin.

c). Scutellaria baicalensis was boiled to extract acid precipitation method to extract baicalin.

d) Mix honeysuckle flower, Acacia chinensis, ox seed, light bamboo leaves, add 10 times the amount of water, and extract twice; 8 times the amount of water, extract for the third time, 2 hours, 2 hours, 1 hour;

e) The combined extracts are concentrated under reduced pressure and concentrated to a concentration of 1: 1 or 1: 0.5; ethanol is added: 65% ~ 70%, and the precipitate is allowed to stand for 48 hours;

f), and then filtering the supernatant; concentrating to a moderately added flavoring agent to dissolve; and then spray-drying or vacuum drying to dry powder;

g), adding excipients, peppermint oil inclusions, artificial bezoar, baicalin and pH regulator, and mixing well;

h). Wet material is made with 90 ~ 85% ethanol as binder; granulated by granulation mechanism; dried at 60 ° C, dried product is collected and granulated after 24 ~ 36 hours; or granulated by dry method Machine-made granules, collect whole grains.

i), and then packed by a packaging machine, the specifications of the medicine are: 10 grams per pack of sugar granules, of which about 9 grams of raw medicine; 4 grams per pack of sugar-free granules, of which, about 9 grams of raw medicine; boxing; Quality inspection; finished products can be shipped.