CN1286122A - Radioactive Re labelled glucosan medicines and preparing process thereof - Google Patents
Radioactive Re labelled glucosan medicines and preparing process thereof Download PDFInfo
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- CN1286122A CN1286122A CN 99116812 CN99116812A CN1286122A CN 1286122 A CN1286122 A CN 1286122A CN 99116812 CN99116812 CN 99116812 CN 99116812 A CN99116812 A CN 99116812A CN 1286122 A CN1286122 A CN 1286122A
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- glucosan
- rhenium
- radioactive
- marked
- solution
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Abstract
A radioactive Re labelled glucosan medicine contains radioactive Re labelled glucosan as active component and medicinal auxiliary, and features that it can be automatically directed to target position, such as lymphatic system, using it for anticancer radiotherapy. The preparing and labelling process is disclosed.
Description
The present invention relates to radioactive label medicament and preparation technology, be specifically related to radioactive rhenium marked glucosan preparation technology.
Lymphosarcoma and other lymph tumors are brought very big harm to health, and the medicine of developing this type of disease is the difficult problem of still needing and solving.
The objective of the invention is to develop and automatic guide to be positioned lymphoid radiation treatment medicine.
The invention provides a kind of radioactive rhenium marked glucosan medicament, this medicament is by forming as active ingredient and pharmaceutic adjuvant with radioactive rhenium marked glucosan.
Another object of the present invention provides a kind of radioactive rhenium marked glucosan medicaments preparation technology, and this technology comprises the following steps:
(1) the refining glucosan of classification:
Get it filled and use glucosan, add 2-10 times of water, heating for dissolving adds ethanol in solution, and it is 30～50% solution that preparation contains concentration of alcohol, removes the excessive or too small glucosan of molecular weight, collects the glucosan of mean molecule quantity 9～140,000, the dry crude product that gets; Crude product is added 2～10 times of water dissolutioies, activated carbon adsorption impurity, filter, in solution, add ethanol, to contain concentration of alcohol be 30～50% solution in preparation, collects the glucosan of mean molecule quantity 9～110,000, dryly must make with extra care glucosan, beta-dextran content is measured with the optical rotation method by the pharmacopeia appendix, and molecular weight is measured with the Ubbelohde viscometer method;
(2) preparation glucosan lyophilized formulations:
Prescription: medicinal glucose
90-14010～30g
Reducing agent is an amount of
Right amount of auxiliary materials
Water 1000ml
Take by weighing glucosan by formula proportion, Reducing agent and other pharmaceutic adjuvants, add water for injection to desired volume, stir into solution, filter, regulate pH to 2～7 through sintered filter funnel, under aseptic technique, divide in the penicillin bottle of packing into, every bottled 1～2ml carries out lyophilization, fills nitrogen, jumps a queue to roll the cap seal dress and make the glucosan lyophilized formulations;
(3) the radioactive rhenium marked glucosan injection of preparation
The glucosan lyophilized formulations that above-mentioned steps is made, inject radioactive rhenium hydrochlorate leacheate 1～5ml (5-30mCi), place in 20～100 ℃ of water-baths jolting continuously 5～30 minutes, sampling is carried out ply of paper and is analysed, with methanol or normal saline ascending development, take out airing after, the chromatography paper slip is cut into 10 five equilibriums, measure radioactivity with # type γ calculating instrument respectively, the Rf=0 of the rhenium-glucosan of labelling, free-rhenium ion ReO
4Rf=0.75 about, require rhenium mark rate 〉=90%, promptly get rhenium-glucosan injection.
The glucosan that foregoing invention method (1) step obtains the experiment proved that to be following array structure:
Glu represents glucosyl group in the formula
(1 → 6) expression 1,6 chain or (1 → 3) expression 1,3 chain.
The described radioactive rhenium of the inventive method is
186Rhenium or
188Rhenium, Reducing agent are vitamin C, CuCl
2, SnCl
2, sodium sulfite, sodium thiosulfate or tartaric acid etc.Pharmaceutic adjuvant is sucrose, glucose, mannitol, sorbitol, lactose, sodium alginate or carboxymethyl cellulose etc.
Radioactive rhenium marked glucosan injection with the inventive method makes shows that through animal experiment this medicine can automatic guide be positioned positions, target area such as lymphsystem, can be used as the directed new drug preparation of antitumor internal radiotherapy.
Radioactive rhenium marked glucosan medicament animal test results of the present invention is as follows:
Get 3 groups of 9 branches of 1.8～2kg rabbit, after in tame rabbit hind leg interdigit, respectively injecting 0.1ml188Re-glucosan (1mCi) injection, put to death in 30 minutes, 60 minutes, 120 minutes, dissect the Qu lymphonodi poplitei, the heart, kidney,spleen,liver, blood, each 1g of muscle, place in the small test tube respectively, test tube is put respectively in people # or the r type enumerator, measured placement property intensity, be converted into every gram internal organs activity Yu lymphonodi poplitei activity ratio.
The injection of table one rabbit
188Bio distribution in the different time body behind the Re-glucosan
Conclusion: show from last table data
188The quantity that Re-Dx concentrates at lymph node is higher than its hetero-organization, explanation far away
188The fairly obvious ground of Re-Dx can automatic guide location lymphsystem, can reach the effect of radiation internal-radiation therapy to the lymphsystem of pathological changes.
The inventive method is simple, is suitable for a large amount of preparations.
Example 1,
Get 100 the gram in molecular weight glucosan (pharmacopeia specification) add 5000 ml waters, heating for dissolving becomes weak solution, in this solution, add medicinal alcohol, it is mixed with to contain ethanol be 42% solution, room temperature staticly settles, and filters inappropriate glucosan, then mother solution reuse ethanol is adjusted to and contains ethanol 44% solution, room temperature staticly settles, and removes the upper strata mother solution, takes out moist precipitate and dewaters with dehydrated alcohol.The precipitation sucking filtration promptly gets crude product in 95 ℃ of dryings, and dissolving crude product is made 2% dextran solution in water, add active carbon, boils, and filters, and mother solution adds ethanol again and is adjusted to the solution that contains ethanol 42%, precipitation, and dry elaboration promptly gets glucosan 90.
Example 2,
Pharmaceutical formulation
Refining glucosan
9030g
SnCl
2 35mg
Sorbitol 30g
H
2O 1000ml
Above-mentioned prescription is mixed with solution filters with No. five sintered glass funnels, every bottle of 1ml of bacteria-free filtrate packing penicillin bottle carried out aseptic lyophilization after 35 hours, filled nitrogen, jumped a queue, and rolled lid, made dried frozen aquatic products.
Example 3,
Get above-mentioned bottled glucosan
90Dried frozen aquatic products, every bottle of injection
186Rhenate (Na
186ReO
4) leacheate 1～5ml, and radioactive intensity (5～30mci), be placed in the 40-100 ℃ of water-bath, jolting was carried out ply of paper and is analysed the certification mark rate after 30 minutes continuously.With syringe about 10 microlitres of sampling, put on chromatographic paper, use normal saline, ascending development takes out airing, keeps flat, and with gammacamera or SPECT instrument, detects speckle on the chromatographic paper.Require the mark rate of the radioactive rhenium of glucosan to reach 90%, promptly
186Rhenium-glucosan
90Injection.
Example 4, get above-mentioned bottled pharmaceutical formulation sterilization filtrate 1ml, every bottle of injection produces Na by generator
188ReO
4 -Physiological water leacheate 1-5ml, activity (5-30mCi) is placed on bottle in 90 ℃ of water-baths, shake up, about 20 minutes,, put on chromatographic paper with syringe about 10 microlitres of sampling, use normal saline, ascending development takes out airing, keeps flat, with gammacamera or SPECT instrument, detect speckle on the chromatographic paper.Draw mark rate, require to reach about 90, promptly get can be used for clinical
188Rhenium-glucosan
90(
188Re-Dx
90) injection.
Example 5,
Identical with example 1 described operation, as long as replace 44% ethanol described in the example 1 with ethanol 40% solution, the result get final product glucosan 140 products.
Example 6,
Get glucosan
140The substitution of refined glucosan
90, other is operated with example 2.
Claims (4)
1, a kind of radioactive rhenium marked glucosan medicament is characterized in that this medicament is by forming as active ingredient and pharmaceutic adjuvant with radioactive rhenium marked glucosan.
2, a kind of a kind of radioactive rhenium marked glucosan medicaments preparation method as claimed in claim 1 is characterized in that this method comprises the following steps:
(1) the refining glucosan of classification:
Get it filled and use glucosan, add 2-10 times of water, heating for dissolving adds ethanol in solution, and it is 30～50% solution that preparation contains concentration of alcohol, removes the excessive or too small glucosan of molecular weight, collects the glucosan of mean molecule quantity 9～140,000, the dry crude product that gets; Crude product is added 2～10 times of water dissolutioies, and activated carbon adsorption impurity filters, and adds ethanol in solution, and it is 30～50% solution that preparation contains concentration of alcohol, collects the glucosan of mean molecule quantity 9～110,000, dryly must make with extra care glucosan
90-glucosan
140, beta-dextran content is measured with the optical rotation method by the pharmacopeia appendix, and molecular weight is measured with the Ubbelohde viscometer method;
(2) preparation glucosan lyophilized formulations:
Prescription: medicinal glucose
90-14010～30g
Reducing agent is an amount of
Right amount of auxiliary materials
Water 1000ml
Take by weighing glucosan by formula proportion, Reducing agent and other pharmaceutic adjuvants, add water for injection to desired volume, stir into solution, filter, regulate pH to 2～7 through sintered filter funnel, under aseptic technique, divide in the penicillin bottle of packing into, every bottled 1～2ml carries out lyophilization, fills nitrogen, jumps a queue to roll the cap seal dress and make the glucosan lyophilized formulations;
(3) the radioactive rhenium marked glucosan injection of preparation
The glucosan lyophilized formulations that above-mentioned steps is made, inject radioactive rhenium hydrochlorate leacheate 1～5ml (5-30mCi), place in 20～100 ℃ of water-baths jolting continuously 5～30 minutes, sampling is carried out ply of paper and is analysed, with methanol or normal saline ascending development, take out airing after, the chromatography paper slip is cut into 10 five equilibriums, measure radioactivity, the Rf=0 of the rhenium-glucosan of labelling, free rhenium ion ReO with # type γ calculating instrument respectively
4Rf=0.75 about, require rhenium mark rate 〉=90%, promptly get rhenium-glucosan injection.
3, a kind of radioactive rhenium marked glucosan medicament according to claim 1 and 2, wherein said radioactive rhenium is
186Rhenium or
188Rhenium, Reducing agent are SnCl
2, CuCl
2Or vitamin
C, sodium sulfite, pharmaceutic adjuvant are glucose, mannitol, sucrose, lactose.
4, a kind of radioactive rhenium marked glucosan medicament as claimed in claim 1 or 2 is used for the purposes of lymphatic disease.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 99116812 CN1286122A (en) | 1999-08-26 | 1999-08-26 | Radioactive Re labelled glucosan medicines and preparing process thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 99116812 CN1286122A (en) | 1999-08-26 | 1999-08-26 | Radioactive Re labelled glucosan medicines and preparing process thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1286122A true CN1286122A (en) | 2001-03-07 |
Family
ID=5279487
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 99116812 Pending CN1286122A (en) | 1999-08-26 | 1999-08-26 | Radioactive Re labelled glucosan medicines and preparing process thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1286122A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101020697B (en) * | 2006-11-10 | 2012-09-05 | 北京师范大学 | Glucose derivative complex marked with 99mTc, 188 Re or 186Re and its preparation process |
| CN101066982B (en) * | 2007-03-06 | 2012-09-05 | 北京师范大学 | Amino acid-glucose derivative 99m TC compound and its prepn process |
-
1999
- 1999-08-26 CN CN 99116812 patent/CN1286122A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101020697B (en) * | 2006-11-10 | 2012-09-05 | 北京师范大学 | Glucose derivative complex marked with 99mTc, 188 Re or 186Re and its preparation process |
| CN101066982B (en) * | 2007-03-06 | 2012-09-05 | 北京师范大学 | Amino acid-glucose derivative 99m TC compound and its prepn process |
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| PB01 | Publication | ||
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| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |