CN1762364A - Formula of blood brain barrier-passing quickly highly-efficient anti-cancer medicine and its preparation process - Google Patents
Formula of blood brain barrier-passing quickly highly-efficient anti-cancer medicine and its preparation process Download PDFInfo
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- CN1762364A CN1762364A CN 200410155390 CN200410155390A CN1762364A CN 1762364 A CN1762364 A CN 1762364A CN 200410155390 CN200410155390 CN 200410155390 CN 200410155390 A CN200410155390 A CN 200410155390A CN 1762364 A CN1762364 A CN 1762364A
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Abstract
The invention discloses a formula of blood brain barrier-passing quickly highly-efficient anti-cancer medicine and its preparation process, which consists of the steps of proportioning cisplatin, borneol and other medicaments, dissolving with right base and carrying out high speed shearing and ultramicro emulsification, melting with dissolved base at a predetermined temperature proportionally, finally obtaining the drop pill preparation.
Description
Technical field
The present invention relates to a kind of prescription and manufacture method of passing through blood brain barrier high resistance cancer drug rapidly, specifically is the preparation and the technology manufacture method thereof of main component with cisplatin and Borneolum Syntheticum.
Background technology
At present, tumor oneself become cause China human mortality important sick and one of plant.According to the Ministry of Public Health statistics, China increased tumour patient 2,000,000 people every year newly in recent years, dead more than 130 ten thousand people, and present national tumor patient sum is about about 4,500,000 people.So numerous tumor patients has formed a huge antitumor drug market.
The medicine of this prescription form and main effect etc. as follows: 1. cisplatin molecular formula: PtCl
2(NH
3)
2This product chemical name is: (Z)-two hydrazine dichloride platinum.It is the metal complex of platinum, and effect is like alkylating agent, and main action target spot is DNA, acts on interlinkage in DNA interchain and the chain, forms DDP～DNA complex, disturbs dna replication dna, or combines with nucleoprotein and plasmosin.Non-specific medicine of genus cycle.Cisplatin is a kind of highly anticancer active medicine that has clinically, and the brain cancer is had curative effect preferably.2. Borneolum Syntheticum is a Chinese medicine commonly used simply, has the effect of " fragrance is walked to scurry, and priming is up ".[Compendium of Materia Medica] early has the statement of its treatment " headache " function.
Cisplatin intravenous injection, artery administration or intracavitary administration absorb all extremely rapid.Be distributed widely in liver, kidney, prostate, bladder, ovary after the injection, also can reach breast, abdominal cavity, seldom pass through blood brain barrier.For treating a line medication of multiple solid tumor.Be treatment SCLC or NSCLC one line scheme with VP-16 associating (EP scheme), combined with MMC, IFO (IMP scheme), or scheme such as NVB is a treatment NSCLC common scheme at present, combined chemotherapy based on DDP also is the main therapeutic scheme of advanced ovarian cancer, osteosarcoma and neuroblastoma, effective with couplings such as ADM, CTX to multi-section position squamous cell carcinoma, transitional cell carcinoma, as incidence, cervix uteri, esophagus and urological cancer etc." PVB " (DDP, VLB, BLM) can treat non-spermatogonium carcinoma of testis of most of IV phase, remission rate 50%～80%.In addition, this product is a radiotherapeutic sensitizer, is widely used at present the local radiotherapy of inoperable NSCLC of IV phase abroad, can improve curative effect and improves life cycle.
The cisplatin of market upper vein injection now is difficult to directly enter cerebral tissue, is because the protective effect of blood brain barrier.Modern pharmacological research shows: Borneolum Syntheticum absorbs rapidly through mesentery, and administration can be passed through blood brain barrier in 5 minutes, and it is long to accumulate the time at brain, measures also quite high.
The experiment proved that: Borneolum Syntheticum can promote that cisplatin passes through blood brain barrier.Short saturating with Borneolum Syntheticum, after the administration 35 minutes to 48 hours, the concentration of cisplatin in rat brain was more stable, and this is highly beneficial to the antitumaous effect of performance cisplatin in brain.
This kind medicine is the preparation that utilizes solid dispersion technology to be prepared from, utilize water-solubility carrier to improve the dissolubility and the dissolution rate of medicine, improve the infiltration rate and the absorbtivity of medicine, thereby improve bioavailability, improve the curative effect of medicine, very effective to clinical patients such as cancer pains.
Summary of the invention
The object of the present invention is to provide a kind of taking convenience, newtype drug evident in efficacy, can effectively pass through blood brain barrier, give full play to the antitumaous effect of cisplatin in brain.
Solution of the present invention is: adopting solid dispersion technology, producing little, quick-acting, the pharmaceutical dosage form efficiently of dosage.
Said preparation is the product of solid dispersion technology, is characterized in: adopt fusion method to make medicine be scattered in the physiology inertia with molecularity and in the carrier soluble in water, form disperse system.(3～4um) is also little, thereby improved surface area greatly, and its bioavailability is much higher than the medicine of general dosage form than micronized particles for drug particle (0.001-0.1um).After entering the intestines and stomach, water-solubility carrier dissolves rapidly, because particle is little, the solid dispersion dissolution velocity is fast, can be absorbed by cell rapidly to enter blood circulation, thereby reach efficient and quick-acting effects.Particularly contain a large amount of volatilization zest compositions in the effective site, adopt solid dispersion technology more can fully contain, make it bring into play effect to a greater extent.
Medicine of the present invention is formed (consumption is a weight portion) by following component:
Cisplatin 2-25 part
Borneolum Syntheticum 1-15 part
Substrate 20-100 part
The ratio range of the component preferred weight of medicine of the present invention is:
Cisplatin 5-15 part
Borneolum Syntheticum 3-8 part
Substrate 20-100 part
The optimum weight proportioning of medicine of the present invention is:
10 parts of cisplatin
5 parts of Borneolum Syntheticums
35 parts of substrate
The method of said components being made medicine of the present invention is:
Choose medicine material according to national standard;
Choose Borneolum Syntheticum by [pharmacopeia] standard;
Choose substrate by national standard.
Illustrate:
Medicine of the present invention meets the national drug standard;
Borneolum Syntheticum of the present invention is the synthetic product that meet the state-promulgated pharmacopoeia standard.
Substrate of the present invention is pharmacopeia designated country standard substance.
With said medicine, Borneolum Syntheticum powder is broken into fine powder or is the moistening or dissolving of solvent with the dehydrated alcohol, then medicine and molten matrix is uniformly dispersed, and is no more than 1um through high speed shear ultra micro emulsifying to particle diameter, joins then in the fluid reservoir and is incubated 85 ℃.
With the water dropper valve open of fluid reservoir, and suitably regulate vacuum equipment.Water dropper apart from the coolant fluid identity distance from being not more than 50cm.The cooling column height is not less than 50cm, and coolant temperature is controlled at about 10 ℃; Drop splashes in the coolant by preset frequency, and medicine drips slowly and sinks, and relies on the tension force of self to be shrunk to ball gradually.After becoming ball, clean surperficial silicone oil or liquid paraffin, drying at room temperature or blowing dry and finished product.
An important feature of the present invention is that medicine and substrate are uniformly dispersed, and makes drug absorption quick, and drug effect is multiplied.
Another important feature of the present invention is the high speed shear ultra micro emulsification technology by uniqueness, and effective ingredient is organically combined.
The specific embodiment
10 parts of cisplatin
5 parts of Borneolum Syntheticums
35 parts of substrate
Embodiment: (1000 of drop pill, every 50mg)
Make 1000 altogether, every heavy 50mg
Preparation method: join respectively in the molten matrix by said components medicine Borneolum Syntheticum, after the emulsifying of high speed shear ultra micro, inject 85 ℃ of fluid reservoirs and be incubated.With coolant cools to the 10 ℃ system of dripping, water dropper to the distance of coolant liquid level is 5cm in cooling column, opens and by-pass cock, and medicinal liquid is splashed in the coolant according to certain frequency, and messenger drug drips slowly and sinks, and relies on self tension force to be shrunk to ball gradually.After becoming ball, clean the coolant on surface, drying at room temperature or blowing dry and finished product.
Claims (9)
1. prescription that can have highly anticancer active medicine rapidly by blood brain barrier is characterized in that it is made up of following components in weight percentage:
Cisplatin 2-25 part Borneolum Syntheticum 1-15 part substrate 20-100 part
2. a kind of prescription that can have highly anticancer active medicine rapidly by blood brain barrier according to claim 1 is characterized in that wherein the weight proportion of each component is:
Cisplatin 5-15 part Borneolum Syntheticum 3-8 part substrate 20-100 part
3. a kind of prescription that can have highly anticancer active medicine rapidly by blood brain barrier according to claim 1 is characterized in that wherein the weight proportion of each component is:
35 parts of 5 parts of substrate of 10 parts of Borneolum Syntheticums of cisplatin
4. according to claim 1,2 or 3 described a kind of prescriptions that can have highly anticancer active medicine rapidly by blood brain barrier, it is characterized in that described preparation is the drop pill on the pharmaceutics.
5. make that claim 4 is described a kind ofly to have the manufacture method of highly anticancer active medicine rapidly by blood brain barrier for one kind, it is characterized in that:
(1) chooses the cisplatin raw material according to national standard;
(2) choose Borneolum Syntheticum by [pharmacopeia] standard;
(3) choose substrate by national standard;
Said medicine in any one described ratio of claim 1-3, and is no more than 1um through high speed shear ultra micro emulsifying to particle diameter, substrate is heated to 85 ℃ of fusings; Then medicine is successively joined in the substrate, inject fluid reservoir and insulation, open and by-pass cock, adjust vacuum and pressure apparatus, splash at regular time and quantity in 5-15 ℃ the coolant, under capillary effect, be shrunk to drop pill naturally at 85 ℃.
6. according to claim 5 a kind ofly can have the manufacture method of highly anticancer active medicine rapidly by blood brain barrier, it is characterized in that:
Cisplatin qualitative, quantitative wherein; Borneolum Syntheticum powder is broken into fine powder or the moistening or dissolving with solvent ethanol.Be no more than 1um through high speed shear ultra micro emulsifying to particle diameter.
7. according to claim 5 a kind ofly can have the manufacture method of highly anticancer active medicine rapidly by blood brain barrier, it is characterized in that:
Two kinds of medicines will add 85 ℃ of fully substrate high speed shearing ultra micro emulsifyings of fusing of temperature respectively sequentially successively.
8. substrate according to claim 5 includes but not limited to Polyethylene Glycol 12000, polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, Macrogol 600, PEG400, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
9. coolant according to claim 5 includes but not limited to dimethicone, liquid paraffin, plant wet goods.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410155390 CN1762364A (en) | 2004-10-21 | 2004-10-21 | Formula of blood brain barrier-passing quickly highly-efficient anti-cancer medicine and its preparation process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410155390 CN1762364A (en) | 2004-10-21 | 2004-10-21 | Formula of blood brain barrier-passing quickly highly-efficient anti-cancer medicine and its preparation process |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1762364A true CN1762364A (en) | 2006-04-26 |
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ID=36746822
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410155390 Pending CN1762364A (en) | 2004-10-21 | 2004-10-21 | Formula of blood brain barrier-passing quickly highly-efficient anti-cancer medicine and its preparation process |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103006622A (en) * | 2011-09-21 | 2013-04-03 | 成都中医药大学 | New borneol use and lung cancer treatment drug composition |
-
2004
- 2004-10-21 CN CN 200410155390 patent/CN1762364A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103006622A (en) * | 2011-09-21 | 2013-04-03 | 成都中医药大学 | New borneol use and lung cancer treatment drug composition |
| CN103006622B (en) * | 2011-09-21 | 2015-07-22 | 成都中医药大学 | New borneol use and lung cancer treatment drug composition |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |