CN1211432A - Anticancer oral liquid and its preparation method - Google Patents

Abstract

An anticancer oral liquid for treating lung cancer, stomach cancer, esophagus cancer, rectum cancer, colon cancer, breast cancer, nasopharyngeal cancer and lymph tumor contains such components (wt. portions) as prepared white aconite root (600-1000), oldenlandia (200-300), barbat skullcap (150-250) and astragalus root (50-200). It can control the growth of cancer, relax the pain of patient and promote appetite.

Description

A kind of antitumor oral liquid and preparation method thereof

The invention belongs to the cancer therapy drug field, particularly a kind of sick oral liquid such as pulmonary carcinoma, gastric cancer, esophageal carcinoma, rectal cancer, colon cancer, breast carcinoma, hepatocarcinoma, nasopharyngeal carcinoma, lymph tumor and preparation method thereof that is used for the treatment of.

At present, in the medicine of treatment late malignant tumour, mostly have the toxic and side effects of certain degree, therapeutic effect is also not really desirable, and tumor patient is taken the back and apparent in view reaction symptom often occurred.How to find in practice a kind of and chemotherapeutics compatible mutually can improve the medicine of body to the holding capacity of chemotherapy, be the generally problem of care of medical circle institute always.

The object of the present invention is to provide and a kind ofly can alleviate reaction symptom, alleviate patient's pain, improving appetite, sick oral liquid and preparation methoies such as the treatment gastric cancer of control tumor development, esophageal carcinoma, rectal cancer, colon cancer, pulmonary carcinoma, breast carcinoma, hepatocarcinoma, nasopharyngeal carcinoma, lymph tumor.

Technical solution of the present invention can realize according to following mode: this oral liquid, contain following component (weight ratio):

Rhizoma Typhonii 600-1000

Herba Hedyotidis Diffusae 200-300

Herba Scutellariae Barbatae 150-250

Radix Astragali 50-200 its preparation method: Rhizoma Typhonii is cut into slices, decoct with water twice, 1 hour-3 hours for the first time, 1 hour-4 hours for the second time, remerge decoction, Rhizoma Typhonii: Herba Hedyotidis Diffusae: Herba Scutellariae Barbatae: the Radix Astragali is (600-1000): (200-300): (150-250): (50-200) (weight ratio), filtering, filtrate concentrates, the weight ratio of concentrated solution and above-mentioned four flavor crude drug in whole is 1: 1,95% ethanol that adds triplication, limit add to stir makes precipitation, leaves standstill 50-80 hour, get the supernatant decompression recycling ethanol, supernatant is added water stir evenly, adjust total amount, stir evenly, filter, fill, sterilization promptly.

The present invention also can contain: Rhizoma Curcumae, Semen Persicae, Rhizoma Paridis, root of subprostrate sophora, Herba Salviae Chinensis, Scolopendra, Hirudo, Bufo siccus, Rhizoma Polygoni Cuspidati, Herba Chelidonii, Cortex Cinnamomi, Myrrha, Rhizoma Corydalis, Radix Asparagi, Rhizoma Polygonati, Radix Ginseng, Radix Glycyrrhizae, its weight ratio is: Rhizoma Typhonii: Herba Hedyotidis Diffusae: Herba Scutellariae Barbatae: Rhizoma Curcumae: Semen Persicae: Rhizoma Paridis: root of subprostrate sophora: Herba Salviae Chinensis: Scolopendra: Hirudo: Bufo siccus: Rhizoma Polygoni Cuspidati: Herba Chelidonii: Cortex Cinnamomi: Myrrha: the Radix Astragali: Rhizoma Corydalis: day each: Rhizoma Polygonati: Radix Ginseng: Radix Glycyrrhizae is: (600-1000): (200-300): (150-250): (50-150): (50-150): (50-100): (50-100): (50-100): (20-50): (20-50): (10-30): (20-50): (10-20): (10-20): (50-150): (50-200): (50-100): (50-100): (30-100): (20-50): (30-100).

The growth that the present invention can obviously suppress carcinoma alleviates the toxicity symptom of chemotherapy, alleviate patient's pain, improving appetite, tumor is dwindled gradually, diseases such as treatment pulmonary carcinoma, gastric cancer, esophageal carcinoma, rectal cancer, colon cancer, breast carcinoma, hepatocarcinoma, nasopharyngeal carcinoma, lymph tumor are had significant curative effect some patient.

Acute toxicity test

1, gastric infusion

Animal: Kunming kind white mice, body weight 21-22 restrains sex, and male and female half and half are provided by animal housing of Shenyang Pharmaceutical University.

Medicine: antitumor oral liquid is provided by Shenyang City's Chinese medicine anticancer research.

Method: can not survey animal dead dosage through giving test.Formal experiment 3; 40 male and female half and half of mice, every gives antitumor oral liquid 50ml/kg (50ml * 2g/ml=100g/kg, g/kg system amount to the crude drug amount and calculate) and all by same dosage gastric infusion, observed seven days, and mice does not have death.See attached list.

2, intraperitoneal administration

Animal: medicine is the same

Method: can not survey dead dosage through giving test.Formal experiment, 20 of mices, male and female half and half, every gives antitumor oral liquid 30ml/kg (30ml * 2g/ml=60g/kg, g/kg system folding platform crude drug amount is calculated) and all by same dosage intraperitoneal administration, observed seven days, and mice does not have death.See attached list.

Drug administration approach dosage the weight of animals (gram) number of animals (only)

Ml/kg begins the result and begins the result

Anticancer gastric infusion 50 21.2 23.6 40 40

Anticancer liquid intraperitoneal administration 30 21.4 23.3 20 20

Conclusion: show through the animal acute experiment, antitumor oral liquid, its median lethal dose(LD 50) of gastric infusion (LD50) more than 50ml/kg, its median lethal dose(LD 50) of intraperitoneal administration (LD50) more than 30ml/kg, this medicine avirulence.

The antitumor action of antitumor oral liquid

One, animal

Healthy animal, male and female all can, must be identical with sex in a collection of experiment, mice body weight 18-22 gram.Kunming kind white mice, animal housing of Shenyang Pharmaceutical University provides.The C57BL/6 mice, animal portion of Chinese Medical Sciences University provides.

Two, medicine

Antitumor oral liquid, Tang Yan army of Shenyang City's Chinese medicine anticancer research institute provides.The pyridine of 5-fluorine urea, Shanghai No. 3 Pharmaceutical Factory

Three, tumor model:

Mouse tumor sarcoma 180 (S180); The ehrlich carcinoma solid type; (EC), tumor research chamber in the court's provides.Lewis lung cancer.China medical courses in general institute institute of materia medica provides.

Four, experimental technique and therapeutic evaluation

Test used animal requirement, inoculation method, experimental design and therapeutic evaluation standard are all according to document ⁽¹⁾And with reference to relevant material ⁽²⁾Carry out.Under aseptic condition, select the good lotus tumor kind Mus of health condition, take out tumor liquid (the oncocyte number is calculated in levelling), get diluent 0.2ml, the axillary fossa that is inoculated in mice is subcutaneous.Random packet after 24 hours, some groups of administrations, negative control group and positive controls.Some days of successive administration.Kunming mouse gastric infusion 7 days, C57BL/6 mouse stomach administration 11 days.Drug withdrawal was put to death animal after 24 hours, dissects, and the record body weight, tumor is heavy, calculates tumor control rate.

The therapeutic evaluation formula:

C is that the average tumor of matched group is heavy in the formula, and T is that the average tumor of administration group is heavy.When suppression ratio＞30%, there were significant differences (P value＜0.05) and after secondary repeated experiments proof, then can evaluate this medicine has certain curative effect to tumor to learn processing by statistics.

Five; Experimental result sees Table 1; 2; 31 180 （ S180 ） （ ） （ ） ml／kg／ X±SD ％ P 40×7 10 8 22.4 23.1 0.83±0.35 47.1＜0.01 20×7 10 9 22.1 22.4 0.97±0.21 38.2＜0.01 10×7 10 9 21.8 26.7 1.15±0.33 26.7＜0.015-FUmg／kg 20×7 10 9 21.9 21.4 0.65±0.23 58.5＜0.01 20×7 20 18 21.6 24.9 1.57±0.36-- 40×7 10 10 20.1 19.9 1.14±0.28 43.8＜0.01 20×7 10 10 19.8 24.3 1.36±0.53 33.0＜0.01 10×7 10 9 19.5 24.2 1.45±0.26 28.5＜0.015-FUmg／kg 20×7 10 10 19.8 20.2 0.68±0.25 66.5 0.01 20×7 20 20 20.1 24.6 2.03±0.49-- 40×7 10 10 21.7 22.7 1.26±0.25 41.9＜0.01 20×7 10 10 21.6 24.1 1.47±0.29 32.2＜0.015-FUmg／kg 20×7 10 10 21.9 20.9 1.02±0.30 52.9＜0.01 20×7 20 18 21.7 22.6 2.17±0.46--。

2 ( EC ) ( ) ( ) ml/kg/ X±SD ％ P 40×7 10 10 19.6 23.6 1.31±0.22 47.3＜0.01 20×7 10 10 19.8 25.6 1.62±0.67 34.9＜0.05 10×7 10 10 19.7 27.2 1.96±0.26 21.2＞0.055-FUmg/kg 20×7 10 10 19.8 23.5 1.04±0.35 58.2＜0.01 20×7 20 19 9.7 28.7 2.49±0.84-- 40×7 10 19 21.6 22.9 0.95±0.24 42.4＜0.01 20×7 10 10 21.5 23.8 1.14±0.21 30.9＜0.01 10×7 10 9 21.1 23.1 1.23±0.31 22.4＜0.055-FUmg/kg 20×7 10 9 20.3 19.1 0.58±0.15 58.7＜0.01 20×7 20 19 21.6 22.9 1.65±0.53-- 40×7 10 10 21.7 22.6 1.07±0.29 41.8＜0.01 20×7 10 10 21.3 22.3 1.19±0.27 35.3＜0.015-FUmg/kg 20×7 10 10 21.5 20.8 0.92±0.18 50.0＜0.01 20×7 20 19 21.1 23.2 1.84±0.48--

3 C57BL/6 Lewis ( ) ( ) ml/kg/ X±SD ％ P 40×11 10 10 21.5 21.1 0.97±0.23 50.2＜0.01 20×11 10 10 21.6 22.2 1.18±0.24 39.4＜0.01 10×11 10 9 21.8 21.5 1.37±0.22 29.7＜0.055-FUmg/kg 15×11 10 10 21.7 20.6 0.89±0.19 54.3＜0.0120×11 20 20 20.4 22.4 1.95±0.39-- 40×11 10 9 19.8 20.3 0.97±0.17 52.9＜0.01 20×11 10 9 19.3 20.1 1.37±0.37 33.4＜0.01 10×11 10 10 19.6 24.6 1.56±0.27 24.2＜0.055-FU 15×11 10 9 19.8 19.4 0.70±0.21 66.0＜0.01mg/kg20×11 17 16 20.1 20.4 2.06±0.69-- 40×11 10 9 20.7 20.1 0.60±0.15 62.5＜0.01 20×11 10 10 20.4 20.1 0.87±0.24 45.6＜0.015-FU 15×11 10 9 20.8 19.7 0.42±0.14 73.7＜0.01mg/kg20×11 15 15 20.5 20.9 1.60±0.64--

Six, discuss

Above-mentioned result of the test shows: this medicine is selected three dosage groups, i.e. 40ml/kg, 20ml/kg and 10ml/kg for use.To the S-180 of Kunming kind white mice, the Lewis lung cancer of EC and C57BL/6 mice, its tumor control rate, except that small dose group, its suppression ratio is all greater than 30%.S-180 wherein, the suppression ratio of the heavy dose group of EC is more than 40%, and Lewis lung cancer is more than 50%.Better through the retrial repeatability.This pharmaceutical quantities difference, the drug effect difference has certain dose-effect relationship.From The acute toxicity tests, this medicine avirulence.In a word, antitumor oral liquid, as pure Chinese medicinal preparation, no acute toxicity has tangible active anticancer, and researching value is arranged.This medicine mechanism of action is remained further to be studied.

Preferred forms of the present invention: embodiment 1 is described in detail below in detail: Rhizoma Typhonii (aquatic foods) 800g Herba Hedyotidis Diffusae 250g

Herba Scutellariae Barbatae 200g Radix Astragali 100g

More than four flavors, with Rhizoma Typhonii (aquatic foods) section, add Herba Hedyotidis Diffusae, Herba Scutellariae Barbatae, the Radix Astragali, decoct twice, 2 hours for the first time, 1.5 hours for the second time, remerge decocting liquid, filter, filtrate concentrates, the weight ratio of concentrated solution and above-mentioned four flavor crude drug in whole is 1: 1, adds 95% ethanol of triplication, and the limit edged stirs and makes precipitation, left standstill 72 hours, and got the supernatant decompression recycling ethanol, supernatant is added water stir evenly, adjust total amount to 800ml, stir evenly, filtration, fill, sterilization, promptly.Embodiment 2: this product contains: Rhizoma Typhonii (aquatic foods) 800g Herba Hedyotidis Diffusae 250g

Herba Scutellariae Barbatae 200g Rhizoma Curcumae 100g Semen Persicae 100g

Rhizoma Paridis 75g root of subprostrate sophora 75g Herba Salviae Chinensis 75g

Scolopendra 27.5g Hirudo 25g Bufo siccus 20g

Rhizoma Polygoni Cuspidati 25g Herba Chelidonii 12.5g Cortex Cinnamomi 15g

Myrrha 100g Radix Astragali 100g Rhizoma Corydalis 75g

Radix Asparagi 75g Rhizoma Polygonati 50g Radix Ginseng 25g Radix Glycyrrhizae 50g

More than 20 2275g altogether simply, make 1000ml.

[method for making] above 20 simply, Rhizoma Typhonii (aquatic foods) 800g is cut into slices, Radix Ginseng 25g is cataclasm, adds other 19 flavor medicine to weight by above-mentioned, decocts with water twice, 2 hours for the first time, 1.5 hours for the second time, remerge decocting liquid, filter, filtrate concentrates, concentrated solution and above-mentioned 20 weight ratio of crude drug in whole simply is 1: 1, and the 95% ethanol limit edged that adds triplication stirs and makes precipitation, leaves standstill 72 hours, get the supernatant decompression recycling ethanol, supernatant is added water stir evenly, adjust total amount, stir evenly to 1000ml, filtration, fill, sterilization, promptly.Embodiment 3: Rhizoma Typhonii, Herba Hedyotidis Diffusae, Herba Scutellariae Barbatae, the Radix Astragali are respectively:

700g、210g、180g、80g

Preparation method is the same.

Claims (3)

1, a kind of antitumor oral liquid is characterized in that: contain following component (weight ratio):

Rhizoma Typhonii 600-1000

Herba Hedyotidis Diffusae 200-300

Herba Scutellariae Barbatae 150-250

Radix Astragali 50-200

2, antitumor oral liquid according to claim 1, it is characterized in that: also contain: Rhizoma Curcumae, Semen Persicae, Rhizoma Paridis, root of subprostrate sophora, Herba Salviae Chinensis, Scolopendra, Hirudo, Bufo siccus, Rhizoma Polygoni Cuspidati, Herba Chelidonii, Cortex Cinnamomi, Myrrha, Rhizoma Corydalis, the Radix Asparagi Rhizoma Polygonati, Radix Ginseng, Radix Glycyrrhizae, its weight ratio is: Rhizoma Typhonii: Herba Hedyotidis Diffusae: Herba Scutellariae Barbatae: Rhizoma Curcumae: Semen Persicae: Rhizoma Paridis: root of subprostrate sophora: Herba Salviae Chinensis: Scolopendra: Hirudo: Bufo siccus: Rhizoma Polygoni Cuspidati: Herba Chelidonii: Cortex Cinnamomi: Myrrha: the Radix Astragali: Rhizoma Corydalis: Radix Asparagi: Rhizoma Polygonati: Radix Ginseng: Radix Glycyrrhizae is: (600-1000): (200-300): (150-250): (50-150): (50-150): (50-100): (50-100): (50-100): (20-50): (20-50): (10-30): (20-50): (10-20): (10-20): (50-150): (50-200): (50-100): (50-100): (30-100): (20-50): (30-100)

3, according to the preparation method of the described antitumor oral liquid of claim 1, it is characterized in that: Rhizoma Typhonii is cut into slices, add Herba Hedyotidis Diffusae, Herba Scutellariae Barbatae, the Radix Astragali, decoct with water twice, 1 hour-3 hours for the first time, 1 hour-4 hours for the second time, remerge decocting liquid, wherein: Rhizoma Typhonii: Herba Hedyotidis Diffusae: Herba Scutellariae Barbatae: the Radix Astragali is (600-1000): (200-300): (150-250): (50-200) (weight ratio); Filter, filtrate concentrates, and the weight ratio of concentrated solution and above-mentioned four flavor crude drug in whole is 1: 1, adds 95% ethanol of triplication, the limit edged stirs and makes precipitation, leaves standstill 50-80 hour, gets the supernatant decompression recycling ethanol, supernatant is added water stirs evenly, adjust total amount, stir evenly, filtration, fill, sterilization promptly.