CN110302434A - A kind of Lipiodol embolizatim agent and preparation method thereof for being easy to inject - Google Patents
A kind of Lipiodol embolizatim agent and preparation method thereof for being easy to inject Download PDFInfo
- Publication number
- CN110302434A CN110302434A CN201910632632.2A CN201910632632A CN110302434A CN 110302434 A CN110302434 A CN 110302434A CN 201910632632 A CN201910632632 A CN 201910632632A CN 110302434 A CN110302434 A CN 110302434A
- Authority
- CN
- China
- Prior art keywords
- oil
- suppository
- injection
- emulsifier
- water
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L31/00—Materials for other surgical articles, e.g. stents, stent-grafts, shunts, surgical drapes, guide wires, materials for adhesion prevention, occluding devices, surgical gloves, tissue fixation devices
- A61L31/005—Ingredients of undetermined constitution or reaction products thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L31/00—Materials for other surgical articles, e.g. stents, stent-grafts, shunts, surgical drapes, guide wires, materials for adhesion prevention, occluding devices, surgical gloves, tissue fixation devices
- A61L31/14—Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
- A61L31/16—Biologically active materials, e.g. therapeutic substances
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L31/00—Materials for other surgical articles, e.g. stents, stent-grafts, shunts, surgical drapes, guide wires, materials for adhesion prevention, occluding devices, surgical gloves, tissue fixation devices
- A61L31/14—Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
- A61L31/18—Materials at least partially X-ray or laser opaque
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
- A61L2300/20—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials
- A61L2300/216—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials with other specific functional groups, e.g. aldehydes, ketones, phenols, quaternary phosphonium groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
- A61L2300/40—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
- A61L2300/416—Anti-neoplastic or anti-proliferative or anti-restenosis or anti-angiogenic agents, e.g. paclitaxel, sirolimus
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
- A61L2300/60—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a special physical form
- A61L2300/602—Type of release, e.g. controlled, sustained, slow
Abstract
Invention belongs to medical diagnosis and interventional therapy field, is related to a kind of Lipiodol embolizatim agent being easy to inject, high drug load and preparation method thereof.The suppository is existing when Lipiodol embolizatim in clinical application to propose, the mixture being made of iodized oil, oil for injection, emulsifier and antineoplastic there is embolism, development and chemotherapy aiming at the problem that be not easy to inject and be not easy to carry medicine.The suppository significantly reduces the viscosity of iodized oil, is conducive to inject, the partial size of gained emulsion droplet can be controlled by adjusting the ratio of emulsifier after emulsification and structure is more stable by introducing the lower oil for injection of viscosity and emulsifier.The suppository not only can use oil for injection and emulsifier carrys out solubilized oil-soluble anti-tumor drug, but also can be prepared simple and easy to do by forming the method for W/O lotion come solubilized water-soluble antineoplastic.
Description
Technical field
The invention belongs to medical diagnosis and interventional therapy field, are related to a kind of iodized oil being easy to inject, high drug load
Suppository and preparation method thereof.
Background technique
Malignant tumour is to cause the second largest cause of disease of human death, seriously threatens the health of the mankind, wherein dying of pernicious swollen
First five cancer of tumor is successively are as follows: gastric cancer, liver cancer, lung cancer, the cancer of the esophagus and colorectal cancer.The main method for the treatment of malignant tumor at present
There are operative treatment, radiochemotherapy, chemotherapy and interventional therapy.Transcatheter arterial em-bolization (TCAE), which has been proved to be, to be controlled
Embolism materials are passed through the supply of conduit Selective implantation to a certain diseased organ by the effective ways for treating the No operation of solid tumor
It is intravascular, make corresponding vascular occlusion, interrupts blood supply and achieve the purpose that treatment.Current existing intervention material has: graininess
Embolism materials, such as gelatin, albumin and microballoon；Liquid embolism materials, such as dehydrated alcohol, lipiodol；Large-scale embolism materials, such as spiral shell
Circle, Detachable baloon.The malignant tumour arteries embolism of clinical application at present is mainly biodegradable material, as iodized oil,
Gelatin.
Iodized oil is a kind of organic iodine injection, has viscosity, due to that can develop under X-ray, be otherwise known as positive bolt
Suppository is often used as hepatic artery embolism agent use in the interventional therapy of clinical liver cancer.On the other hand, iodized oil is to malignant tumour
Tissue affinity is high, has targeting, these features is clinically utilized, after iodized oil is mixed with anticarcinogen such as 5 FU 5 fluorouracil
Emulsion is made, for the interventional therapy of the diseases such as late tumor, iodized oil blocks cancer cell blood supply, 5- fluorine urine using viscosity
Pyrimidine is killed after then diffusing to tumour cell.But that there are chemotherapeutics is insoluble or insufficient for this emulsification method
Defect causes curative effect to reduce.Simultaneously lipiodol due to viscosity it is too big, cause to be not easy to inject in surgical procedure.
Summary of the invention
The purpose of the present invention is provide one aiming at the problem that iodized oil in process of clinical application injects difficulty and is not easy to carry medicine
Kind be easy to inject with the suppository of high drug load and preparation method thereof.The suppository is iodized oil, oil for injection, emulsifier and resists
The mixture of tumour medicine composition, has the function of embolism, development and chemotherapy.Wherein iodized oil has developing function, oil for injection
Play the role of solubilized chemotherapeutics with emulsifier and reduce viscosity, while the suppository also has slow-release function.
The present invention is achieved by the following technical solutions:
It is easy to inject and the Lipiodol embolizatim agent of high drug load the present invention provides a kind of, the suppository is by iodized oil, note
It penetrates with oil, emulsifier and antineoplastic composition.
The iodized oil is commercially available CT radiography iodate fat injection, 200~1000mgmL containing iodine-1。
The oil for injection is to meet grease as defined in injection in pharmacopeia, including one of following material or their group
It closes: ethyl oleate, middle chain (C6-10) fatty glyceride, isopropyl myristate, soybean oil, sesame oil, tea oil, olive oil, castor
Sesame oil, peanut oil, cotton seed oil.
The emulsifier includes surfactant and cosurfactant.
The surfactant includes one of following material or their combination: soybean lecithin, egg yolk lecithin, brain
Phosphatide, PLURONICS F87, Brij 35, Myrj51, Myrj53, Cremophor RH40, Cremophor EL, 80 and of Tween
Tween 85。
The cosurfactant includes one of following material or their combination: ethyl alcohol, 1,2- propylene glycol, glycerol,
Polyethylene glycol 400, ethylene glycol monomethyl ether.
The anti-tumor drug is water-soluble antitumor medicine or oil-soluble dissolubility antineoplastic.
The water-soluble antitumor medicine includes one of following drug or their combination: doxorubicin hydrochloride, Ji Xita
Guest, cis-platinum, 5 FU 5 fluorouracil, cytarabine, carboplatin, mitomycin, Kato moor glycosides, bleomycin A5.
The oil-soluble antineoplastic includes one of following drug or their combination: adriamycin, Carmustine, camplotheca acuminata
Alkali, taxol, vincristine, elemene, docetaxel, Fotemustine.
The mass fraction of each component is respectively as follows: iodized oil 30~50%, oil for injection 0~39%, cream in the suppository
Agent 0~49%, water for injection 5~19%, water-soluble antitumor medicine 0.1~10%.
The mass fraction of each component is respectively as follows: iodized oil 30~60%, oil for injection 0~49%, cream in the suppository
Agent 0~49%, oil-soluble antineoplastic 0.1~10%.
The preparation method of the suppository the following steps are included:
For water-soluble anti-tumor medicine:
(1) by water-soluble antitumor medicine dissolution with appropriate water for injection in, as water phase；
(2) by iodized oil, oil for injection and emulsifier mix after, be placed under blender and stir, revolving speed be 500~
5000rpm·min-1, mixing time is 20~60min, as oily phase；
(3) water phase in step 1 is added in the oily phase in step 2 (volume ratio 1: 5~20), is placed under blender and stirs
It mixes, revolving speed is 500~5000rpmmin-1, mixing time is 20~60min, and temperature is 20~50 DEG C to get required embolism
Agent；
For oil-soluble anti-tumor drug:
(1) it adds drug in oil for injection, is placed under blender and stirs, revolving speed is 100~1000rpmmin-1,
Mixing time is 20~120min；
(2) oil solution in step 1 is mixed with iodized oil and emulsifier, is placed under blender and stirs, revolving speed be 500~
5000rpm·min-1, mixing time is 20~60min, and temperature is 20~50 DEG C to get required suppository.
The suppository forms partial size as 0.1~900 μm of emulsion droplet when extension rate is 5~100 times in vitro.
The beneficial effects of the present invention are:
(1) present invention solves the problems, such as that iodized oil load medicine is difficult, can be significant by introducing oil for injection and emulsifier
Increase the solubility of oil-soluble antineoplastic, and water-soluble anti-tumor medicine then passes through W/O emulsion form and increases its drugloading rate.Together
When the present invention obtained by suppository have the effect of be sustained.
(2) present invention significantly reduces the viscosity of iodized oil by the lower oil for injection of introducing viscosity and emulsifier,
Be conducive to inject, the partial size of gained emulsion droplet is controlled by adjusting the ratio of emulsifier after emulsification, stable structure.
Detailed description of the invention
Fig. 1 is grain size distribution after 15 times of the dilution agent of embolism containing antineoplastic of embodiment
Fig. 2 is CT development figure after the intervention of 1 suppository containing antineoplastic of embodiment
Fig. 3 is grain size distribution after 25 times of the dilution agent of embolism containing antineoplastic of embodiment
Fig. 4 is CT development figure after the intervention of 2 suppository containing antineoplastic of embodiment
Specific embodiment
Embodiment 1: the preparation of suppository containing antineoplastic
(1) taxol 20mg is taken to be added in 150mg 1,2-PD, temperature is heated to 40 DEG C, magnetic agitation 20min.
(2) it takes iodized oil 500mg and Cremophor RH40 330mg loaded in bottle, is placed on magnetic stirring apparatus and stirs
It mixes, mixing speed 1200rpmmin-1, mixing time 40min.
(3) liquid in step 1 and 2 is mixed to be placed on magnetic stirring apparatus and is stirred, mixing speed is
1000rpm·min-1, mixing time 45min, temperature maintains 40 DEG C.Faint yellow uniform solution is finally obtained, it is as required
Suppository.By preoperative 5~10 times of the water for injection dilution of the suppository, the emulsion droplet (such as Fig. 1) that partial size is 5~110 μm is obtained, easily
In injecting.Transcatheter arterial em-bolization is carried out to liver cancer patient, discovery development effect is obvious (such as Fig. 2).
Embodiment 2: the preparation of suppository containing antineoplastic
(1) it takes Carmustine 30mg to be added in 150mg medium-chain fatty glyceride, is placed on magnetic stirring apparatus and stirs,
Revolving speed is 600rpmmin-1, time 50min, temperature is 45 DEG C.
(2) iodized oil 400mg, 400 120mg of Cremophor RH40 300mg and PEG are taken, is added in bottle, sets
In being stirred on magnetic stirring apparatus, revolving speed 1000rpmmin-1, mixing time 45min.
(3) it after mixing the liquid in step 1 and 2, is stirred on magnetic stirring apparatus, revolving speed 800rpmmin-1, stir
Mixing the time is 60min, obtains faint yellow uniform liquid, as required suppository.By the preoperative water for injection dilution 5 of the suppository
~10 times, the emulsion droplet (such as Fig. 3) that partial size is 50~400 μm is obtained, is easy to inject.Liver cancer patient is carried out through transcatheter arterial embolization
Art, discovery development effect are obvious (such as Fig. 4).
Embodiment 3: the preparation of suppository containing antineoplastic
(1) it takes ethyl oleate 450mg, docetaxel 30mg loaded in bottle, is preheated to 45 DEG C, bottle is placed in magnetic force
It is stirred on blender, revolving speed 500rpmmin-1, mixing time 30min is completely dissolved in docetaxel in ethyl oleate.
(2) it takes iodized oil 520mg to be added in above-mentioned ethyl oleate, is placed on magnetic stirring apparatus and stirs, revolving speed is
800rpm·min-1, mixing time 45min obtains showing slightly flaxen uniform oil solution.The oil solution is required embolism
Agent, since ethyl oleate viscosity is lower, the viscosity of the mixed solution is substantially reduced compared with iodized oil.Before the surgery by the suppository
The droplet that partial size is 100~300 μm is formed after artificial emulsification, is used for embolism parteriole tip.
Embodiment 4: the preparation of suppository containing antineoplastic
(1) 5 FU 5 fluorouracil 30mg is taken to be dissolved in 150mg water for injection as water phase.
(2) iodized oil 350mg, ethyl oleate 250mg, Cremophor RH40 150mg and 1,2- propylene glycol 70mg dress are taken
In bottle, magnetic agitation, revolving speed 800rpmmin are carried out at 35 DEG C-1, mixing time 1h finally obtains uniform liquid
Body, as oily phase.
(3) above-mentioned water phase is slowly added into oily phase, while is stirred on magnetic stirring apparatus, revolving speed is
1000rpm·min-1, mixing time 45min, temperature is 25 DEG C.The W/O emulsion being evenly distributed is finally obtained, as gained bolt
Suppository.The mixed liquor is diluted 5~10 times with water for injection in the preoperative, obtains the W/O/W emulsion droplet that partial size is 5~50 μm.It is postoperative
5 FU 5 fluorouracil is slowly released into blood across oil reservoir, realizes the purpose of sustained release.
Embodiment 5: the preparation of suppository containing antineoplastic
(1) doxorubicin hydrochloride 30mg is taken to be dissolved in 150mg water for injection as water phase.
(2) take iodized oil 450mg, medium-chain fatty glyceride 150mg, Tween 80 170mg and glycerol 50mg loaded on small
In bottle, magnetic agitation, revolving speed 1000rpmmin are carried out at 35 DEG C-1, mixing time 1h finally obtains uniform liquid,
As oily phase.
(3) above-mentioned water phase is slowly added into oily phase, while is stirred on magnetic stirring apparatus, revolving speed is
1000rpm·min-1, mixing time 45min, temperature is 25 DEG C.The W/O emulsion being evenly distributed is finally obtained, as gained bolt
Suppository.The mixed liquor is diluted 5~10 times with water for injection in the preoperative, obtains the W/O/W emulsion droplet that partial size is 20~100 μm.Art
Doxorubicin hydrochloride is slowly released into blood across oil reservoir afterwards, realizes the purpose of sustained release.
Embodiment 6: the preparation of suppository containing antineoplastic
(1) cis-platinum 50mg is taken to be dissolved in 150mg water for injection as water phase.
(2) iodized oil 500mg, Cremophor EL 120mg, Cremophor RH40 100mg and PEG 400 are taken
80mg carries out magnetic agitation, revolving speed 1000rpmmin loaded in bottle at 35 DEG C-1, mixing time 1h finally obtains
Uniform liquid, as oily phase.
(3) above-mentioned water phase is slowly added into oily phase, while is stirred on magnetic stirring apparatus, revolving speed is
1000rpm·min-1, mixing time 45min, temperature is 25 DEG C.The W/O emulsion being evenly distributed is finally obtained, as gained bolt
Suppository.The mixed liquor is diluted 5~10 times with water for injection in the preoperative, obtains the W/O/W emulsion droplet that partial size is 0.5~20 μm.Art
Cis-platinum is slowly released into blood across oil reservoir afterwards, realizes the purpose of sustained release.
Embodiment 7: the preparation of suppository containing antineoplastic
(1) it takes elemene 30mg to be added in 150mg soybean oil, is placed on magnetic stirring apparatus and stirs, revolving speed is
600rpm·min-1, time 50min, temperature is 45 DEG C.
(2) iodized oil 450mg, Tween 80 300mg and glycerol 70mg are taken, is added in bottle, is placed in magnetic stirring apparatus
Upper stirring, revolving speed 1200rpmmin-1, mixing time 35min.
(3) it after mixing the liquid in step 1 and 2, is stirred on magnetic stirring apparatus, revolving speed 800rpmmin-1, stir
Mixing the time is 60min, obtains faint yellow uniform liquid, as required suppository.By the preoperative water for injection dilution 5 of the suppository
~10 times, the emulsion droplet that partial size is 80~500 μm is obtained, is easy to inject.Transcatheter arterial em-bolization, discovery are carried out to liver cancer patient
Development effect is obvious.
Embodiment 8: the preparation of suppository containing antineoplastic
(1) it takes vincristine 15mg to be added in 55mg castor oil and 80mg ethyl oleate, is placed on magnetic stirring apparatus and stirs,
Revolving speed is 600rpmmin-1, time 55min, temperature is 45 DEG C.
(2) 35 100mg of iodized oil 350mg, Brij, 400 200mg of Myrj53 200mg and PEG are taken, bottle is added to
In, it is placed on magnetic stirring apparatus and stirs, revolving speed 1000rpmmin-1, mixing time 45min.
(3) it after mixing the liquid in step 1 and 2, is stirred on magnetic stirring apparatus, revolving speed 800rpmmin-1, stir
Mixing the time is 60min, obtains faint yellow uniform liquid, as required suppository.By the preoperative water for injection dilution 5 of the suppository
~10 times, obtain the emulsion droplet that partial size is 200~800 μm.
Embodiment 9: the preparation of suppository containing antineoplastic
(1) it takes adriamycin 80mg to be added in 100mg medium-chain fatty glyceride and 200mg ethyl oleate, is placed in magnetic force and stirs
It mixes and is stirred on device, revolving speed 600rpmmin-1, time 55min, temperature is 45 DEG C.
(2) iodized oil 300mg, PLURONICS F87 50mg, Tween 400 70mg of 80 200mg and PEG are taken, is added to
In bottle, it is placed on magnetic stirring apparatus and stirs, revolving speed 1000rpmmin-1, mixing time 45min.
(3) it after mixing the liquid in step 1 and 2, is stirred on magnetic stirring apparatus, revolving speed 1000rpmmin-1, stir
Mixing the time is 40min, obtains faint yellow uniform liquid, as required suppository.By the preoperative water for injection dilution 5 of the suppository
~10 times, obtain the emulsion droplet that partial size is 0.5~20 μm.
Embodiment 10: the preparation of suppository containing antineoplastic
(1) it takes Fotemustine 50mg to be added in 250mg medium-chain fatty glyceride, is placed on magnetic stirring apparatus and stirs, turn
Speed is 800rpmmin-1, time 55min, temperature is 35 DEG C.
(2) iodized oil 400mg, soybean lecithin 30mg, PLURONICS F87 50mg, Tween 85 200mg and PEG are taken
400 20mg, are added in bottle, are placed on magnetic stirring apparatus and stir, revolving speed 1000rpmmin-1, mixing time is
45min。
(3) it after mixing the liquid in step 1 and 2, is stirred on magnetic stirring apparatus, revolving speed 1000rpmmin-1, stir
Mixing the time is 40min, obtains faint yellow uniform liquid, as required suppository.By the preoperative water for injection dilution 5 of the suppository
~10 times, obtain the emulsion droplet that partial size is 2~200 μm.
Embodiment 11: the preparation of suppository containing antineoplastic
(1) 5 FU 5 fluorouracil 50mg is taken to be dissolved in 150mg water for injection as water phase.
(2) iodized oil 450mg, ethyl oleate 200mg, Tween 80 100mg and ethyl alcohol 20mg is taken to be loaded in bottle,
Magnetic agitation, revolving speed 1000rpmmin are carried out at 45 DEG C-1, mixing time 1h finally obtains uniform liquid, as oil
Phase.
(3) above-mentioned water phase is slowly added into oily phase, while is stirred on magnetic stirring apparatus, revolving speed is
1000rpm·min-1, mixing time 45min, temperature is 25 DEG C.The W/O emulsion being evenly distributed is finally obtained, as gained bolt
Suppository.The mixed liquor is diluted 5~10 times with water for injection in the preoperative, obtains the W/O/W emulsion droplet that partial size is 50~600 μm.Art
Cis-platinum is slowly released into blood across oil reservoir afterwards, realizes the purpose of sustained release.
Claims (10)
- It is easy to inject and the Lipiodol embolizatim agent of high drug load 1. a kind of, it is characterised in that by iodized oil, oil for injection, emulsifier It is formed with anti-tumor drug, the iodized oil is commercially available CT radiography iodate fat injection, 200~1000mgmL containing iodine-1, The oil for injection is to meet one of grease as defined in injection, including following material or their combination in pharmacopeia: oleic acid second Ester, middle chain (C6-10) fatty glyceride, isopropyl myristate, soybean oil, sesame oil, tea oil, olive oil, castor oil, peanut Oil, cotton seed oil, the emulsifier include surfactant and cosurfactant.
- 2. suppository according to claim 1, it is characterised in that the surfactant include one of following material or Their combination: soybean lecithin, egg yolk lecithin, cephalin, PLURONICS F87, Brij 35, Myrj51, Myrj53, Cremophor RH40, Cremophor EL, Tween 80 and Tween 85.
- 3. suppository according to claim 1, it is characterised in that the cosurfactant include one of following material or Person's their combination: ethyl alcohol, 1,2- propylene glycol, glycerol, polyethylene glycol 400, ethylene glycol monomethyl ether.
- 4. suppository according to claim 1, it is characterised in that the anti-tumor drug is water-soluble antitumor medicine or oil Dissolubility antineoplastic.
- 5. suppository according to claim 4, it is characterised in that the water-soluble antitumor medicine includes one of following drug Or their combination: doxorubicin hydrochloride, gemcitabine, cis-platinum, 5 FU 5 fluorouracil, cytarabine, carboplatin, mitomycin, Kato moors glycosides, bleomycin A5.
- 6. suppository according to claim 4, it is characterised in that the oil-soluble antineoplastic includes one of following drug Or their combination: adriamycin, Carmustine, camptothecine, taxol, vincristine, elemene, docetaxel, Fu Mosi Spit of fland.
- 7. suppository according to claim 1, it is characterised in that the mass fraction of each component is respectively as follows: in the suppository Iodized oil 30~50%, oil for injection 0~39%, emulsifier 0~49%, water for injection 5~19%, water-soluble antitumor medicine 0.1~10%.
- 8. suppository according to claim 1, it is characterised in that the mass fraction of each component is respectively as follows: in the suppository Iodized oil 30~60%, oil for injection 0~49%, emulsifier 0~49%, oil-soluble antineoplastic 0.1~10%.
- 9. the preparation method of suppository according to claim 1, it is characterised in that the preparation method packet of the suppository Include following steps:For water-soluble anti-tumor medicine:(1) by water-soluble antitumor medicine dissolution with appropriate water for injection in, as water phase；(2) it after mixing iodized oil, oil for injection and emulsifier, is placed under blender and stirs, revolving speed is 500~5000rpm min-1, mixing time is 20~60min, as oily phase；(3) water phase in step 1 being added in the oily phase in step 2, volume ratio 1: 5~20 is placed under blender and stirs, Revolving speed is 500~5000rpmmin-1, mixing time is 20~60min, and temperature is 20~50 DEG C to get required suppository；For oil-soluble anti-tumor drug:(1) it adds drug in oil for injection, is placed under blender and stirs, revolving speed is 100~1000rpmmin-1, stirring Time is 20~120min；(2) oil solution in step 1 is mixed with iodized oil and emulsifier, is placed under blender and stirs, revolving speed be 500~ 5000rpm·min-1, mixing time is 20~60min, and temperature is 20~50 DEG C to get required suppository.
- 10. suppository according to claim 1, it is characterised in that extension rate is 5~100 to the suppository in vitro Times when, forming partial size is 0.1~900 μm of emulsion droplet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910632632.2A CN110302434A (en) | 2019-07-14 | 2019-07-14 | A kind of Lipiodol embolizatim agent and preparation method thereof for being easy to inject |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910632632.2A CN110302434A (en) | 2019-07-14 | 2019-07-14 | A kind of Lipiodol embolizatim agent and preparation method thereof for being easy to inject |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110302434A true CN110302434A (en) | 2019-10-08 |
Family
ID=68081321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910632632.2A Pending CN110302434A (en) | 2019-07-14 | 2019-07-14 | A kind of Lipiodol embolizatim agent and preparation method thereof for being easy to inject |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN110302434A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112245384A (en) * | 2020-11-03 | 2021-01-22 | 贵州医科大学 | Iodized oil suppository containing adriamycin and preparation method thereof |
| CN112933250A (en) * | 2020-12-17 | 2021-06-11 | 太阳雨林（厦门）生物医药有限公司 | Iodized oil emulsion or drug-loaded iodized oil emulsion and preparation method and application thereof |
| CN112933246A (en) * | 2020-12-17 | 2021-06-11 | 太阳雨林（厦门）生物医药有限公司 | Developable oil preparation and preparation method thereof |
Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6042322A (en) * | 1983-08-19 | 1985-03-06 | Nippon Kayaku Co Ltd | Novel emulsified preparation |
| JPH03287542A (en) * | 1990-04-04 | 1991-12-18 | Natl Sci Council | Anticancer emulsion having improved stability and sustained release action for chemical target treatment method and preparation thereof |
| WO1997036576A1 (en) * | 1996-04-01 | 1997-10-09 | Korea Institute Of Science And Technology | Preparation method of emulsion for chemoembolization |
| CN1547469A (en) * | 2001-09-13 | 2004-11-17 | 韩国科学技术研究院 | Paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof |
| CN1555253A (en) * | 2001-09-13 | 2004-12-15 | ������ѧ�����о�Ժ | Oily composition of taxol,preparation for chemical therapeutic embolism and their producing method |
| CN1671370A (en) * | 2002-07-20 | 2005-09-21 | 韩国科学技术研究院 | Composition for solubilization of paclitaxel and preparation method thereof |
| CN101618022A (en) * | 2009-07-29 | 2010-01-06 | 中国人民解放军第三军医大学第二附属医院 | Improved method for preparing artery embolic agent |
| CN109821055A (en) * | 2019-02-01 | 2019-05-31 | 厦门大学 | A kind of drug-lipiodol solvent and preparation method thereof |
| CN111298189A (en) * | 2018-12-11 | 2020-06-19 | 陈传果 | Iodized oil suppository easy to inject and preparation method thereof |
-
2019
- 2019-07-14 CN CN201910632632.2A patent/CN110302434A/en active Pending
Patent Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6042322A (en) * | 1983-08-19 | 1985-03-06 | Nippon Kayaku Co Ltd | Novel emulsified preparation |
| JPH03287542A (en) * | 1990-04-04 | 1991-12-18 | Natl Sci Council | Anticancer emulsion having improved stability and sustained release action for chemical target treatment method and preparation thereof |
| WO1997036576A1 (en) * | 1996-04-01 | 1997-10-09 | Korea Institute Of Science And Technology | Preparation method of emulsion for chemoembolization |
| CN1547469A (en) * | 2001-09-13 | 2004-11-17 | 韩国科学技术研究院 | Paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof |
| CN1555253A (en) * | 2001-09-13 | 2004-12-15 | ������ѧ�����о�Ժ | Oily composition of taxol,preparation for chemical therapeutic embolism and their producing method |
| CN1671370A (en) * | 2002-07-20 | 2005-09-21 | 韩国科学技术研究院 | Composition for solubilization of paclitaxel and preparation method thereof |
| CN101618022A (en) * | 2009-07-29 | 2010-01-06 | 中国人民解放军第三军医大学第二附属医院 | Improved method for preparing artery embolic agent |
| CN111298189A (en) * | 2018-12-11 | 2020-06-19 | 陈传果 | Iodized oil suppository easy to inject and preparation method thereof |
| CN109821055A (en) * | 2019-02-01 | 2019-05-31 | 厦门大学 | A kind of drug-lipiodol solvent and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 任慧等: "《微纳米含能材料》", 30 April 2015, 北京理工大学出版社 * |
| 余元勋等: "《中国分子肝癌学》", 30 April 2016, 安徽科学技术出版社 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112245384A (en) * | 2020-11-03 | 2021-01-22 | 贵州医科大学 | Iodized oil suppository containing adriamycin and preparation method thereof |
| CN112933250A (en) * | 2020-12-17 | 2021-06-11 | 太阳雨林（厦门）生物医药有限公司 | Iodized oil emulsion or drug-loaded iodized oil emulsion and preparation method and application thereof |
| CN112933246A (en) * | 2020-12-17 | 2021-06-11 | 太阳雨林（厦门）生物医药有限公司 | Developable oil preparation and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN110302434A (en) | A kind of Lipiodol embolizatim agent and preparation method thereof for being easy to inject | |
| CN101022786B (en) | Self emulsifying compositions for delivering lipophilic coenzyme Q10 and other dietary ingredients | |
| CN109310643A (en) | The dutasteride and Tadalafei compound formulation of ester derivant containing glycerine fatty acid or methyl glycol fatty acid ester derivative and the oral capsule preparation comprising it | |
| JP2020128404A5 (en) | ||
| CN108815160A (en) | A kind of rapamycin liposome nano granule and preparation method thereof | |
| CN108136217A (en) | For treating the preparation of carcinoma of urinary bladder | |
| CN103536574A (en) | Coenzyme Q10 soft capsule and preparation method thereof | |
| CN107812008A (en) | A kind of preparation method of near-infrared fluorescence imaging small molecule anti-cancer Nano medication | |
| WO2020073559A1 (en) | Flurbiprofen axetil emulsion for injection and preparation method therefor | |
| CN106074377A (en) | A kind of stable vitamin K2submicron emulsion and preparation method thereof | |
| CN109663145A (en) | A kind of lipiodol targeted drug compound | |
| CN101524329B (en) | Bicyclo-ethanol submicron emulsion and preparation method thereof | |
| JP2022508807A (en) | Intratumor injection product | |
| CN102526065A (en) | Compound injection preparation for treating cardiovascular and cerebrovascular diseases and preparation method thereof | |
| CN101601649B (en) | Ubenimex fat emulsion injection and preparation method thereof | |
| CN111298189A (en) | Iodized oil suppository easy to inject and preparation method thereof | |
| CN101810577B (en) | Gossypol intravenous injection fatty emulsion for curing tumors | |
| CN110302154A (en) | A kind of 2,4- dinitrophenol Fat Emulsion and its preparation method and application | |
| JPH0518806B2 (en) | ||
| CN1990032B (en) | Composite intravenous injection emulsion of glossy ganoderma spore oil and coix seed oil and method for making same | |
| CN100408033C (en) | Fat emulsion of biobalide B and preparation method | |
| CN104125825B (en) | For diagnose and treat hormone dependent cancer and synthesize steroid hormone organ cancer preparation | |
| KR20190096244A (en) | Composition for Hepatic Arterial Embolization Comprising Microbubbles Carrying a Water-soluble Anticancer Agent and Method for Preparing Thereof | |
| CN104306372B (en) | A kind of butylphenyl phthaleine preparation compositions and preparation method thereof and purposes | |
| CN101632635A (en) | Antitumor emulsion and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20191008 |