CN101607068A - A kind of treatment hepatocarcinoma Chinese medicine precursor liposome injection and preparation technology thereof - Google Patents
A kind of treatment hepatocarcinoma Chinese medicine precursor liposome injection and preparation technology thereof Download PDFInfo
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- CN101607068A CN101607068A CNA2009100233299A CN200910023329A CN101607068A CN 101607068 A CN101607068 A CN 101607068A CN A2009100233299 A CNA2009100233299 A CN A2009100233299A CN 200910023329 A CN200910023329 A CN 200910023329A CN 101607068 A CN101607068 A CN 101607068A
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Abstract
The present invention proposes a kind of Chinese medicine precursor liposome injection and preparation technology thereof who treats hepatocarcinoma, belongs to Chinese medicine preparation technology field.Prescription is made up of Semen zanthoxyli oil and Oleum Curcumae 2 flavor medical materials, and its weight ratio is: 16～25 parts of Semen zanthoxyli oils, 4～6 parts of Oleum Curcumae.Preparation method: the Semen zanthoxyli oil medical material mixes the back according to the pro-liposome method by a certain percentage with Oleum Curcumae, is that preparing carriers becomes pro-liposome with the sorbitol.Add the jolting of injection water before the use, hydration forms liposome turbid liquor, intravenous drip administration.This product is novel pure compound Chinese medicinal preparation, not only strengthens drug targeting, improves bioavailability; Increase medicine stability simultaneously, cover bad smell; And be beneficial to storage and transport.Raw material sources are abundant, and cost is low; Preparation technology is simple, is easy to enlarge produce.
Description
Affiliated technical field
The invention belongs to Chinese medicine and field of pharmaceutical preparations thereof, specifically is a kind of novel form and preparation technology thereof who is used for the treatment of the herbal mixture of hepatocarcinoma.
Background technology
Hepatocarcinoma is clinical common malignancy, and sickness rate occupies the 3rd in tumor, and poor prognosis.5-fluorouracil and amycin etc. are treatment hepatocarcinoma chemotherapeutics commonly used, but these medicines have very strong toxic and side effects.Exploitation has, and PTS efficient, low toxicity becomes the task of top priority.But in the research and development of cancer therapy drug, the multidrug resistance of cancerous cell is to influence the key issue that chemotherapy of tumors carries out.Studies confirm that, the herbal pharmacology action range, side effect is little, can be applicable to reverse multidrug resistance
[1 ~ 3]And Chinese medical and herbal therapy has positive effect to tumor disease in the body resistance strengthening and constitution consolidating, human body immunity improving function and resistance against diseases, has bigger potentiality.
Modern Chinese medicine studies confirm that alpha-linolenic acid has the generation of inhibition cancer and the effect of transfer; Especially hepatoma carcinoma cell had stronger lethal effect.Semen zanthoxyli oil is the dry mature seed of rutaceae Pericarpium Zanthoxyli, is the standard Chinese medicine that " Shandong Province's Chinese crude drug standard " nineteen ninety-five version is recorded.Early-stage Study confirms, extracts the Semen zanthoxyli oil core oil that obtains in the Semen zanthoxyli oil and contains a large amount of unsaturated fatty acids, and wherein alpha-linolenic acid content has potential resisting liver cancer activity up to more than 35%.
Oleum Curcumae is the volatile oil that Rhizoma Zingiberis Recens tannin plant temperature Rhizoma Curcumae, Guangxi zedoary and RADIX CURCUMAE rhizome extract, and is light brown or dark-brown supernatant liquid; Gas is special, mildly bitter flavor and suffering; Crude drug records in version " Chinese pharmacopoeia in 2005.Contain multiple anticancer active ingredient in the Oleum Curcumae, as curcumenol, curzerenone, beta-elemene etc.Its main effect of modern study is antiviral and antitumor.Oleum Curcumae not only has direct killing effect to tumor, can also strengthen the immunogenicity of tumor cell.Because of its toxicity is bigger, the clinical auxiliary treatment that are used for tumor more.
Our preliminary pharmacological tests confirms that Semen zanthoxyli oil core oil has better effects with the treatment that the compatibility of Oleum Curcumae is used hepatocarcinoma, not only can effectively suppress the formation of hepatocarcinoma, and reduce the consumption of Oleum Curcumae, and toxic and side effects is very little.
Summary of the invention
Because Semen zanthoxyli oil core oil is the oils composition with Oleum Curcumae, less stable, and have special odor.The objective of the invention is provides scientific formulation, preparation technology's pure Chinese medicinal preparation pro-liposome easy, evident in efficacy to liver cancer patient.Said preparation has better targeting at the focus zone, can be by number of ways administrations such as oral, injections; And the increase medicine stability is covered the adverse drug abnormal smells from the patient.
In order to realize the foregoing invention purpose, fabricating technology route of the present invention is that supercritical fluid extraction extracts the Semen zanthoxyli oil core oil in the Semen zanthoxyli oil, press by the raw material that is equipped with pro-liposome after 4: 1 the mixed by the pro-liposome legal system with Oleum Curcumae, form the suspension of liposome with preceding hydration jolting.
Specific embodiments
1, pro-liposome prescription and preparation technology thereof
16～25 parts of [prescription] Semen zanthoxyli oils, 4～6 parts of Oleum Curcumae, phosphatidase 12～4 part, 0.5～1 part in cholesterol, 0.1～0.5 part of VE oil, 8～10 parts of sorbitol
[preparation technology] takes by weighing in mixture, lecithin, cholesterol, VE oil, the ether that is dissolved in 5 times of amounts or the chloroform-ether (1: 1) of Semen zanthoxyli oil core oil and Oleum Curcumae by recipe quantity, forms clear and bright lipoids solution.Other took by weighing the sorbitol of 100 mesh sieves, placed eggplant-shape bottle preheating 30min, and gradation adds above-mentioned lipoids solution then, and reduction vaporization volatilizes solvent to free from extraneous odour in water bath with thermostatic control.The product that will make place the vacuum desiccator dried overnight, cross 40 mesh sieves, are packed as 1000 in the 5ml cillin bottle (1g/ props up), sterilization, and 4 ℃ keep in Dark Place.
2, operation instruction
[function with cure mainly] circulation of qi promoting removing blood stasis; The removing food stagnancy pain relieving; Inducing diuresis to remove edema.Cure mainly hepatocarcinoma.
[usage and consumption] with before adding the jolting of injection water, hydration forms liposome turbid liquor, intravenous drip administration.Each 1, every day 1 time.
[untoward reaction] forbids this product allergy sufferers; Contraindication in pregnancy.
[storage] shading is put shady and cool dry place and is preserved.
3, technical characterictic and innovation
The present invention has designed the Chinese medicine precursor liposome injection and the preparation technology thereof of treatment hepatocarcinoma.Prescription Chinese medicine component is low-polarity component, the higher entrapment that is easy to get in preparation process, and easy to leak not.Granule or powder that pro-liposome is generally dry, has the good flow performance add the hydration of water shake well before the use, form the suspension of liposome.This dosage form not only has the basic characteristics of liposome, as better targeting is arranged at cancerous cell, improves bioavailability, reduces drug toxicity, covers adverse drug abnormal smells from the patient etc.; Solved problems such as the stability of conventional liposome and high temperature sterilize simultaneously, be beneficial to and preserve and transportation.Our province abounds with Pericarpium Zanthoxyli, and Rhizoma Curcumae also has ample resources at our province, and crude drug source is abundant; The pro-liposome production technology is easy, and cost is low, is easy to preserve, and is convenient to promote the use of.
Claims (3)
1, the herbal mixture injection of treatment hepatocarcinoma is proposed.This prescription is made up of 2 flavor Chinese medicines, and wherein Semen zanthoxyli oil is the extract of the medical material Semen zanthoxyli that records in " Shandong Province's Chinese crude drug standard "; Oleum Curcumae belongs to version " the standard medical material that one one of Chinese pharmacopoeia is recorded in 2005.Adjuvant in the prescription all meets the version " regulation under the Chinese pharmacopoeia corresponding entry in 2005.It is composed as follows to write out a prescription: Semen zanthoxyli oil, Oleum Curcumae, lecithin, cholesterol, VE oil, sorbitol.
2, the drug prescription of treatment hepatocarcinoma as claimed in claim 1 is prepared into pro-liposome with it.It is characterized in that taking by weighing respectively, make dry powder according to the preparation technology of pro-liposome according to prescription Chinese medicine and specific proportioning; Add the jolting of injection water before the use, hydration forms liposome turbid liquor, intravenous drip administration.The prescription of this crude drug: 16～25 parts of Semen zanthoxyli oils, 4～6 parts of Oleum Curcumae, 2～4 parts in lecithin, 0.5～1 part in cholesterol, 0.1～0.5 part of VE oil, 8～10 parts of sorbitol.Its preparation technology and method are:
(1) get 16～25 parts of Semen zanthoxyli oil core oil, 4～6 parts of Oleum Curcumae, 2～4 parts in lecithin, 0.5～1 part in cholesterol, 0.1～0.5 part of VE oil is dissolved in the ether or chloroform-ether (1: 1) of 5 times of amounts, forms clear and bright lipoids solution.Other took by weighing 8～10 parts of the sorbitol of 100 mesh sieves, placed eggplant-shape bottle preheating 30min, and gradation adds in the above-mentioned lipoids solution then, and reduction vaporization volatilizes solvent to free from extraneous odour in water bath with thermostatic control.The product that will make place the vacuum desiccator dried overnight, cross 40 mesh sieves, be sub-packed in (1g/ props up) in the 5ml cillin bottle, and sterilization, 4 ℃ keep in Dark Place.
(2) add the jolting of injection water before the use, hydration forms liposome turbid liquor, intravenous drip administration.
3, require 1-2 that prescription is prepared into pro-liposome by aforesaid right, in the regulation Semen zanthoxyli oil core oil, alpha-linolenic acid content is not less than 35%.The liposome particle diameter of making by claim 2 is about 100nm, and envelop rate is more than 75%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2009100233299A CN101607068A (en) | 2009-07-15 | 2009-07-15 | A kind of treatment hepatocarcinoma Chinese medicine precursor liposome injection and preparation technology thereof |
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| CNA2009100233299A CN101607068A (en) | 2009-07-15 | 2009-07-15 | A kind of treatment hepatocarcinoma Chinese medicine precursor liposome injection and preparation technology thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20101872A1 (en) * | 2010-10-13 | 2012-04-14 | Vincenzo Cinosi | USE OF PHOSPHATIDYLCOLINE IN THE TREATMENT OF CANCER |
| WO2015124616A1 (en) * | 2014-02-20 | 2015-08-27 | Indena S.P.A. | Compositions containing extracts of curcuma longa and echinacea angustifolia which are useful to reduce peripheral inflammation and pain |
| WO2016003383A1 (en) | 2014-07-01 | 2016-01-07 | Tunca Berrin | Use of the extract obtained from the olea europaea leaves in the treatment of glioblastoma |
-
2009
- 2009-07-15 CN CNA2009100233299A patent/CN101607068A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20101872A1 (en) * | 2010-10-13 | 2012-04-14 | Vincenzo Cinosi | USE OF PHOSPHATIDYLCOLINE IN THE TREATMENT OF CANCER |
| WO2012049647A1 (en) * | 2010-10-13 | 2012-04-19 | Vincenzo Cinosi | Phosphatidylcholine in the treatment ophosphatidylcholinef tumours |
| WO2015124616A1 (en) * | 2014-02-20 | 2015-08-27 | Indena S.P.A. | Compositions containing extracts of curcuma longa and echinacea angustifolia which are useful to reduce peripheral inflammation and pain |
| CN106029082A (en) * | 2014-02-20 | 2016-10-12 | 因德纳有限公司 | Compositions containing extracts of curcuma longa and echinacea angustifolia which are useful to reduce peripheral inflammation and pain |
| US10286028B2 (en) | 2014-02-20 | 2019-05-14 | Indena S.P.A. | Compositions containing extracts of Curcuma longa and Echinacea angustifolia which are useful to reduce peripheral inflammation and pain |
| AU2015220913B2 (en) * | 2014-02-20 | 2020-04-09 | Indena S.P.A. | Compositions containing extracts of Curcuma Longa and Echinacea angustifolia which are useful to reduce peripheral inflammation and pain |
| WO2016003383A1 (en) | 2014-07-01 | 2016-01-07 | Tunca Berrin | Use of the extract obtained from the olea europaea leaves in the treatment of glioblastoma |
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Open date: 20091223 |