CN103054881A - Traditional Chinese medicine active component compound preparation for treating lung cancer and preparation method thereof - Google Patents
Traditional Chinese medicine active component compound preparation for treating lung cancer and preparation method thereof Download PDFInfo
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- CN103054881A CN103054881A CN2013100282516A CN201310028251A CN103054881A CN 103054881 A CN103054881 A CN 103054881A CN 2013100282516 A CN2013100282516 A CN 2013100282516A CN 201310028251 A CN201310028251 A CN 201310028251A CN 103054881 A CN103054881 A CN 103054881A
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Abstract
The invention discloses a traditional Chinese medicine active component compound preparation for treating lung cancer and a preparation method thereof. The compound preparation is a traditional Chinese medicine active component compound prepared from taxol, cinobufagin and triptolide according to a certain weight ratio. The preparation method comprises the steps of preparing a lipidosome by adopting an ethanol injection method or preparing a pill by taking polyethylene glycol as a substrate, thereby obtaining the traditional Chinese medicine active component preparation. The dosage forms of the compound preparation are compound lipidosomes and compound pills; found from animal internal anticancer pharmacological experiments, the traditional Chinese medicine active component compound preparation has obvious inhibition effect on development of lung cancer; and the anticancer activity of the compound preparation is obviously higher than that of a chemotherapeutic drug, namely 5-fluorouracil.
Description
Technical field
The present invention relates to technical field of Chinese medicines, specifically relate to a kind of active ingredient of Chinese herbs compound preparation for the treatment of pulmonary carcinoma and preparation method thereof.
Background technology
Cancer is the formidable enemy of harm humans health.The annual new cases of cancer of China has 1,600,000 people approximately, and that dies from cancer every year has 1,300,000 people approximately, rises year by year because of the dead number of cancer in the whole nation, and China is the zone occurred frequently of the cancers such as pulmonary carcinoma, breast carcinoma, hepatocarcinoma, and cancer mortality is high.
There is no at present the most of cancer patients of effective cured substance.Though chemotherapeutics has certain curative effect to cancer, toxic and side effects is large, and Chinese patent medicine is generally lower to the curative effect of cancer, and curative effect is all undesirable.
The inventor is through the arduous Sirikaya of having studied decades, the Herba Phyllanthi Urinariae, Ramulus et folium taxi cuspidatae, the anticancer active substance of the Chinese medicines such as dry maxima skin, therefrom extract multiple anti-cancer active compound, show through anticancer experimentation, to human breast carcinoma, pulmonary carcinoma, the cancerous cell such as hepatocarcinoma and zoografting carcinoma all have significant inside and outside anticancer therapy effect, and (patent No. is respectively: ZL02148474.0 to have applied for obtaining 7 antineoplastic product invention patent certificates, ZL02148475.9, ZL03112707.X, ZL200410041122.1, ZL200610085781.4, ZL200610085781.4, ZL200810124588.6).On the basis of above-mentioned research, the inventor studies again and has invented a kind of active anticancer height, the wide anticarcinogen of anticancer spectrum.
Summary of the invention
1, goal of the invention: the purpose of this invention is to provide a kind of active anticancer height, the wide anticarcinogen of anticancer spectrum, a kind of active ingredient of Chinese herbs compound preparation for the treatment of breast carcinoma and pulmonary carcinoma that specifically prepares as raw material take paclitaxel, cinobufagin, triptolide and preparation method thereof.
2, technical scheme:
A kind of active ingredient of Chinese herbs compound preparation for the treatment of pulmonary carcinoma is characterized in that by the active ingredient of Chinese herbs of following weight portion proportioning made: 1～3 part of paclitaxel, 1～3 part of cinobufagin, 1～3 part of triptolide.
Each active ingredient of Chinese herbs brief introduction is as follows:
Paclitaxel (Paclitaxe, Taxol, TAX), (claiming again: taxol, Paclitaxe, Paclitaxe), molecular formula: C
47H
51NO
14, chemical structural formula:
Cinobufagin (Cinobufagin, CBG), (claiming again: cinobufacin, cinobufagin), molecular formula: C
26H
34O
6, chemical structural formula:
Triptolide (triptolide, TL), (claim again: Radix Tripterygii Wilfordii lactone alcohol),, molecular formula: C
20H
24O
6, chemical structural formula:
Described active ingredient of Chinese herbs compound preparation, the dosage form that it is characterized in that this compound preparation is compound recipe liposome and compound dripping pill.
The preparation method of the compound recipe liposome of active ingredient of Chinese herbs compound preparation of the present invention is: material and the proportioning of (1) compound recipe liposome preparation are: lecithin respectively with mPEG2000-DSPE(amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine) mass ratio is 10:1～1.2, with the mass ratio of cholesterol be 10:1～1.2, with the mass ratio of active ingredient of Chinese herbs compound medicine be 30:0.8～1; (2) preparation method of compound recipe liposome is: adopt the alcohol injection preparation: get the PBS buffer of pH7.4 in eggplant type bottle, in 50～55 ℃ of preheating 30～35min of water bath with thermostatic control; Get lecithin, cholesterol, Chinese medicine dispelling toxins and dredging collaterals composition compound medicine and mPEG2000-DSPE in beaker, add an amount of dehydrated alcohol and make its dissolving, all be injected into rapidly in the eggplant type bottle that buffer solution is housed of constant temperature preheating after the dissolving until medicine, obtain the milky liposome turbid liquor, continue to stir aquation 1～1.2h, evacuation is except ethanol, and 800P crosses 10～12 circulations of high pressure dispersing emulsification machine, namely gets Chinese medicine dispelling toxins and dredging collaterals composition compound recipe liposome.
The preparation method of the compound dripping pill of active ingredient of Chinese herbs compound preparation of the present invention is: the material of (1) compound dripping pill preparation and proportioning, condition are: polyethylene glycol 6000 (PEG6000) is substrate, liquid Paraffin is coolant, the ratio of active ingredient of Chinese herbs compound medicine and substrate is 1:2～3, fluid temperature is 80～85 ℃, and chilling temperature is 10～15 ℃; (2) the compound dripping pill preparation method is: polyethylene glycol 6000 is put in the water-bath after the heat fused ratio in medicine and substrate add Chinese medicine dispelling toxins and dredging collaterals composition compound medicine and stir, put in the drop pill preparation facilities, insulation splashes into that dripping becomes ball in the liquid Paraffin coolant, and the condensed fluid of the drop pill that makes being removed the surface namely gets the active ingredient of Chinese herbs compound dripping pill.
The application of active ingredient of Chinese herbs compound preparation of the present invention in preparation treatment lung-cancer medicament.
Active ingredient of Chinese herbs compound preparation of the present invention has obvious inhibitory action to the growth of pulmonary carcinoma in vivo, and its active anticancer is apparently higher than the chemotherapeutic 5-fluorouracil.
3, beneficial effect:
Active ingredient of Chinese herbs compound preparation of the present invention is tested through Anticancer in animal body, growth to pulmonary carcinoma has obvious inhibitory action, the active ingredient of Chinese herbs compound preparation of 9mg/kg dosage can significantly suppress the growth (P＜0.01) of mice Lewis lung carcinoma, and its tumour inhibiting rate is 72.84%; Its active anticancer to pulmonary carcinoma is higher than chemotherapeutic 5-fluorouracil (5-Fu), also is higher than the single composition (paclitaxel single, cinobufagin single, triptolide single) of prescription.Can be used for treating pulmonary carcinoma.
A kind of active ingredient of Chinese herbs compound preparation of the present invention is the active ingredient of Chinese herbs compound anti-cancer medicine for preparing as raw material take paclitaxel, cinobufagin, triptolide.Animal vivo antitumor experimental result shows that the active ingredient of Chinese herbs compound preparation has very high active anticancer to the growth of pulmonary carcinoma, and its vivo antitumor activity is higher than chemotherapeutic 5-fluorouracil (5-Fu), also is higher than the single composition of prescription.This provides very promising efficient preliminary election medicine for improving anticancer clinical efficacy, and also the mechanism for Study of Traditional Chinese Medicine active component compatibility provides good component prescription.
The specific embodiment
Embodiment 1: the active ingredient of Chinese herbs compound preparation, and made by paclitaxel 1 part (10mg), cinobufagin 1 part (10mg) and triptolide 1 part (10mg), wherein the preparation method of liposome is as follows:
(1) active ingredient of Chinese herbs compound recipe liposome prepares material and proportioning is: lecithin respectively with mPEG2000-DSPE(amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine) mass ratio is 10: 1, with the mass ratio of cholesterol be 10: 1, with the mass ratio of active ingredient of Chinese herbs compound medicine be 30: 1;
(2) active ingredient of Chinese herbs compound recipe method for preparing lipidosome is: adopt the alcohol injection preparation, precision is measured the PBS buffer 90mL of pH7.4 in eggplant type bottle, in 50 ℃ of preheating 30min of water bath with thermostatic control; Lecithin 900mg, cholesterol 90mg, active ingredient of Chinese herbs compound medicine 30mg and mPEG2000-DSPE90mg are accurately weighed in beaker, add an amount of dehydrated alcohol and make its dissolving, all be injected into rapidly in the eggplant type bottle that buffer solution is housed of constant temperature preheating after the dissolving until medicine, obtain the milky liposome turbid liquor, continue to stir aquation 1h, evacuation is except ethanol, and 800P crosses 10 circulations of high pressure dispersing emulsification machine, namely gets active ingredient of Chinese herbs compound recipe liposome.
Wherein the preparation method of compound dripping pill is as follows:
(1) the active ingredient of Chinese herbs compound dripping pill prepares material and proportioning, condition is: polyethylene glycol 6000 (PEG6000) is substrate, liquid Paraffin is coolant, the ratio of active ingredient of Chinese herbs compound medicine and substrate is 1:2, and fluid temperature is 85 ℃, and chilling temperature is 12～14 ℃;
(2) active ingredient of Chinese herbs compound dripping pill preparation method is: the polyethylene glycol 6000 of 60mg is put in the water-bath after the heat fused ratio in compound medicine and substrate 1:2 add active ingredient of Chinese herbs compound medicine 30mg and stir, put in the drop pill preparation facilities, insulation splashes into that dripping becomes ball in the liquid Paraffin coolant, and the condensed fluid of the drop pill that makes being removed the surface namely gets the active ingredient of Chinese herbs compound dripping pill.
Embodiment 2: the active ingredient of Chinese herbs compound preparation, and made by paclitaxel 2 parts (20mg), cinobufagin 2 parts (20mg) and triptolide 2 parts (20mg), wherein the preparation method of liposome is as follows:
(1) active ingredient of Chinese herbs compound recipe liposome prepares material and proportioning is: lecithin respectively with mPEG2000-DSPE
(amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine) mass ratio is 10: 1, with the mass ratio of cholesterol be 10: 1, with the mass ratio of active ingredient of Chinese herbs compound medicine be 30: 1;
(2) active ingredient of Chinese herbs compound recipe method for preparing lipidosome is: adopt the alcohol injection preparation, precision is measured the PBS buffer 180mL of pH7.4 in eggplant type bottle, in 50 ℃ of preheating 30min of water bath with thermostatic control; Lecithin 1800mg, cholesterol 180mg, active ingredient of Chinese herbs compound medicine 60mg and mPEG2000-DSPE180mg are accurately weighed in beaker, add an amount of dehydrated alcohol and make its dissolving, all be injected into rapidly in the eggplant type bottle that buffer solution is housed of constant temperature preheating after the dissolving until medicine, obtain the milky liposome turbid liquor, continue to stir aquation 1h, evacuation is except ethanol, and 800P crosses 12 circulations of high pressure dispersing emulsification machine, namely gets active ingredient of Chinese herbs compound recipe liposome.
Wherein the preparation method of compound dripping pill is as follows:
(1) the active ingredient of Chinese herbs compound dripping pill prepares material and proportioning, condition is: polyethylene glycol 6000 (PEG6000) is substrate, liquid Paraffin is coolant, the ratio of active ingredient of Chinese herbs compound medicine and substrate is 1:2, and fluid temperature is 85 ℃, and chilling temperature is 12～14 ℃;
(2) active ingredient of Chinese herbs compound dripping pill preparation method is: the polyethylene glycol 6000 of 120mg is put in the water-bath after the heat fused ratio in compound medicine and substrate 1:2 add active ingredient of Chinese herbs compound medicine 60mg and stir, put in the drop pill preparation facilities, insulation splashes into that dripping becomes ball in the liquid Paraffin coolant, and the condensed fluid of the drop pill that makes being removed the surface namely gets the active ingredient of Chinese herbs compound dripping pill.
Embodiment 3: the active ingredient of Chinese herbs compound preparation, and made by paclitaxel 3 parts (30mg), cinobufagin 3 parts (30mg) and triptolide 3 parts (30mg), wherein the preparation method of liposome is as follows:
(1) active ingredient of Chinese herbs compound recipe liposome prepares material and proportioning is: lecithin respectively with mPEG2000-DSPE(amphipathic ethylene glycol 2000-distearyl phospholipid ethanolamine) mass ratio is 10: 1.2, with the mass ratio of cholesterol be 10: 1.2, with the mass ratio of active ingredient of Chinese herbs compound medicine be 30: 0.8;
(2) active ingredient of Chinese herbs compound recipe method for preparing lipidosome is: adopt the alcohol injection preparation, precision is measured the PBS buffer 270mL of pH7.4 in eggplant type bottle, in 50 ℃ of preheating 30min of water bath with thermostatic control; Lecithin 2700mg, cholesterol 324mg, active ingredient of Chinese herbs compound medicine 90mg and mPEG2000-DSPE324mg are accurately weighed in beaker, add an amount of dehydrated alcohol and make its dissolving, all be injected into rapidly in the eggplant type bottle that buffer solution is housed of constant temperature preheating after the dissolving until medicine, obtain the milky liposome turbid liquor, continue to stir aquation 1h, evacuation is except ethanol, and 800P crosses 12 circulations of high pressure dispersing emulsification machine, namely gets active ingredient of Chinese herbs compound recipe liposome.
Wherein the preparation method of compound dripping pill is as follows:
(1) the active ingredient of Chinese herbs compound dripping pill prepares material and proportioning, condition is: polyethylene glycol 6000 (PEG6000) is substrate, liquid Paraffin is coolant, the ratio of active ingredient of Chinese herbs compound medicine and substrate is 1:2, and fluid temperature is 85 ℃, and chilling temperature is 12～14 ℃;
(2) active ingredient of Chinese herbs compound dripping pill preparation method is: the polyethylene glycol 6000 of 180mg is put in the water-bath after the heat fused ratio in compound medicine and substrate 1:2 add active ingredient of Chinese herbs compound medicine 90mg and stir, put in the drop pill preparation facilities, insulation splashes into that dripping becomes ball in the liquid Paraffin coolant, and the condensed fluid of the drop pill that makes being removed the surface namely gets the active ingredient of Chinese herbs compound dripping pill.
Embodiment 4: the active ingredient of Chinese herbs compound preparation is to the inhibitory action of Lewis lung carcinoma
1, laboratory animal and tumor strain
Male and healthy C57BL/6 mice, body weight 18-22g, Mus 6-8 in age week is available from zoopery center, this school; Lewis cells of lung cancer is available from zoopery center, institute of oncology, Jiangsu Province.
1, modeling and experimental technique
70 of C57BL/6 mices stay 10 negative matched groups in proportion at random, and all the other 60 are carried out modeling.Prepare the Lewis lung cancer tumor-bearing mice, peel off the tumor tissue of growth animated period, choose well-grown lump 1.5mm
3About, in tumor (g): normal saline (ml) is ratio homogenate in 1: 3, transferring cell number is 2 * 10
6/ ml.Choose healthy mice, every right side of mice axillary fossa subcutaneous vaccination 0.2ml under aseptic condition.Whole seeded process must be carried out with the sterile working in aseptic cover, finishes inoculation in the 1h.
Be divided at random 6 groups after the inoculation, 10 every group, be respectively tumor model matched group, active ingredient of Chinese herbs compound recipe and 4 test group of composition single thereof, 5-fu positive controls, other adds negative control group, totally 6 groups.Behind the inoculation oncocyte 24h, test group lumbar injection active ingredient of Chinese herbs compound recipe, paclitaxel single, cinobufagin single, triptolide single, dosage is 9mg/kg, negative control group and tumor model matched group equal-volume injectable drug solvent, the 5-FU matched group is take normal saline as solvent, dosage is 20mg/kg, each treated animal all by 0.2ml at lumbar injection, successive administration 10d.Next day after the last administration, carry out following observation:
Completely peel off the tumor piece, and the calculating tumor control rate of weighing, tumor control rate=(matched group tumor weight-treatment group tumor weight)/matched group tumor weight * 100%.
3, experimental result:
The active ingredient of Chinese herbs compound recipe is to the inhibitory action of mice Lewis lung carcinoma: 9mg/kg active ingredient of Chinese herbs compound recipe can significantly suppress the growth (P＜0.01) of mice Lewis lung carcinoma, its anti-lung cancer activity is higher than chemotherapeutic 5-fluorouracil (5-Fu), also be higher than the single composition (paclitaxel single, cinobufagin single, triptolide single) of prescription, see Table 1.
Table 1 active ingredient of Chinese herbs compound recipe is to mice Lewis lung carcinoma Lewis exercising result
Claims (3)
1. active ingredient of Chinese herbs compound preparation for the treatment of pulmonary carcinoma is characterized in that it is made by the weight proportion of following traditional Chinese medicines active component:
1～3 part of paclitaxel, 1～3 part of cinobufagin, 1～3 part of triptolide.
2. active ingredient of Chinese herbs compound preparation according to claim 1 is characterized in that being that the dosage form of this compound preparation is compound recipe liposome and compound dripping pill.
3. the application of active ingredient of Chinese herbs compound preparation as claimed in claim 1 in preparation treatment lung-cancer medicament.
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018210224A1 (en) * | 2017-05-15 | 2018-11-22 | 王晓辉 | Applications of triptolide and derivative thereof in preparing medicament for treating and/or preventing lung-damaging diseases |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2018210224A1 (en) * | 2017-05-15 | 2018-11-22 | 王晓辉 | Applications of triptolide and derivative thereof in preparing medicament for treating and/or preventing lung-damaging diseases |
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