CN104666276A - Preparation method of 5-Fu magnetic microcapsule - Google Patents
Preparation method of 5-Fu magnetic microcapsule Download PDFInfo
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- CN104666276A CN104666276A CN201310621215.0A CN201310621215A CN104666276A CN 104666276 A CN104666276 A CN 104666276A CN 201310621215 A CN201310621215 A CN 201310621215A CN 104666276 A CN104666276 A CN 104666276A
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- fluorine
- urine pyridine
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Abstract
The invention provides a preparation method of a 5-Fu magnetic microcapsule. According to the characteristics that 5-Fu plasma is short in half-life period, frequent dosage is needed, and the serious toxic and side effects such as myelosuppression and gastrointestinal toxicity are generated, 5-Fu is prepared into the magnetic microcapsule, releasing of medicines in a human body is delayed, the medicine action time is prolonged, the microcapsule is made to have the good targeting and biocompatibility, and the toxic and side effect is reduced. The preparation method is simple, practicable and suitable for scale production of an enterprise.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule.
Background technology
5-fluorine phonetic urine pyridine (5-Fu) is a kind of antimetabolic antineoplastic agent, can suppress thymidylate synthase, blocks deoxyribonucleotides nucleotide and converts thymidylic acid to, and interference DNA synthesis, also has certain inhibitory action to the synthesis of RNA.Short according to 5-fluorine phonetic urine pyridine plasma half-life, need frequent drug administration, produce serious toxic and side effects, as bone marrow depression, gastrointestinal toxicity etc., phonetic for 5-fluorine urine pyridine is prepared into magnetic microcapsule by spy, delay medicine release in vivo, prolong drug action time, make it that there is good targeting and biocompatibility, reduce toxic and side effects.Specifically, (1) magnetic target preparation is jointly wrapped in high molecular polymer carrier medicine and microgranule ferromagnetic material.Displacement and location focus on the drug-supplying system of target site in vivo to adopt external magnetic field guide drugs.Magnetic microcapsule is under enough externally-applied magnetic field effects. can guide carrying medicament in vivo displacement, locate, concentrate, thus improve the targeting of antitumor drug, and reduce the toxic and side effects of antitumor drug significantly, and thus medicine magnetic microcapsule formulation has become the ideal candidate of target medicine carrier. and be a kind of novel targeted drug-supplying system.(2) adopt ferroso-ferric oxide to be magnetic core, to human non-toxic, harmless, and magnetic responsiveness is good, is medical magnetic microgranule ideal at present, has a wide range of applications in clinical and biomedicine field.
Summary of the invention
The preparation method of the 5-fluorine phonetic urine pyridine magnetic microcapsule that the present invention aims to provide a kind of anti-tumor target tropism and medicine stability is high, slow release is controlled, drug treating time is long, toxicity is low.
For achieving the above object, the preparation method of a kind of 5-of the present invention fluorine phonetic urine pyridine magnetic microcapsule, specific embodiments is:
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, it is characterized in that, this preparation method comprises the following steps:
(1) preparation of magnetic material ferroso-ferric oxide: get Iron dichloride tetrahydrate and ferric chloride hexahydrate is appropriate, add 100mL distilled water, heating in water bath is to 50-60 DEG C, under 400-500r/min condition, slowly add sodium hydroxide solution regulate pH=10-13, reaction 20-40min, filters, carries out Magneto separate, the ferroso-ferric oxide obtained is cleaned, dries;
(2) emulsion method prepares the phonetic urine pyridine-gelatin-sodium alginate magnetic microcapsule of 5-fluorine:
1. precision takes ferroso-ferric oxide fine powder (cross 200 mesh sieves) and adds 50mL in right amount containing in the gelatin-sodium alginate soln of the phonetic urine pyridine of 5-fluorine, is uniformly mixed under 60 DEG C of conditions;
2. separately get sorbester p17, liquid paraffin mix homogeneously, under 60 DEG C of conditions, add Tween 80,500-600r/min stirs 5min;
3. will 1. slowly add 2., continue to stir;
4. cool the temperature to 40 DEG C, adjust ph, add glutaraldehyde, continue to stir;
5. 4000 r/min centrifugalize 20 min, precipitate uses distilled water, washed with diethylether for several times respectively, and drying under reduced pressure at 35 DEG C, to obtain final product.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, is characterized in that Iron dichloride tetrahydrate and ferric chloride hexahydrate mol ratio are 1:1.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, is characterized in that step (1) pH value of solution=12.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, is characterized in that in the gelatin-sodium alginate soln of step (2) 1. 5-fluorine phonetic urine pyridine, the phonetic urine pyridine of 5-fluorine is 1%.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, it is characterized in that (2) 3. mixing time be 20-40 min.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, it is characterized in that (2) 4. adjust ph to 5.0, mixing time is 1.5-3 h.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, it is characterized in that (2) 3. mixing time be 30 min, make water-in-oil emulsion.
The preparation method of a kind of 5-fluorine of the present invention phonetic urine pyridine magnetic microcapsule, it is characterized in that (2) 4. mixing time be 2 h.
The preparation method of a kind of 5-of the present invention fluorine phonetic urine pyridine magnetic microcapsule, has the following advantages:
1. technique is simple, easy to operate, is applicable to suitability for industrialized production;
2. it is high that the 5-fluorine phonetic urine pyridine magnetic microcapsule prepared by has anti-tumor target tropism, and medicine stability is good, and toxic and side effects is low, has the medical and prospect of marketing.
Detailed description of the invention
Embodiment is only that the present invention will be described further below, does not limit the present invention in any form.
Embodiment
(1) preparation of magnetic material ferroso-ferric oxide
Get Iron dichloride tetrahydrate and ferric chloride hexahydrate appropriate (mol ratio is 1:1), add 100mL distilled water, heating in water bath is to 60 DEG C, under 500r/min condition, slowly add sodium hydroxide solution regulate pH=12, reaction 40min, filters, carries out Magneto separate, the ferroso-ferric oxide obtained is cleaned, dries.Yield 65%.
(2) emulsion method prepares the phonetic urine pyridine-gelatin-sodium alginate magnetic microcapsule of 5-fluorine
1. precision takes 0.5g ferroso-ferric oxide fine powder (cross 200 mesh sieves) and adds 50mL containing in the gelatin-sodium alginate soln of the phonetic urine pyridine of 1%5-fluorine, is uniformly mixed under 60 DEG C of conditions.
2. separately get 1g sorbester p17,50g liquid paraffin mix homogeneously, add 0.5g Tween 80 under 60 DEG C of conditions, 600r/min stirs 5min.
3. will 1. slowly add 2., continue to stir 30min, make water-in-oil emulsion.
4. cool the temperature to 40 DEG C, adjust ph to 5.0, add 5 mL glutaraldehydes, continue to stir 2h.
5. 4000 r/min centrifugalize 20 min, precipitate uses distilled water, washed with diethylether for several times respectively, and drying under reduced pressure at 35 DEG C, to obtain final product.
Claims (8)
1. a preparation method for 5-fluorine phonetic urine pyridine magnetic microcapsule, it is characterized in that, this preparation method comprises the following steps:
(1) preparation of magnetic material ferroso-ferric oxide: get Iron dichloride tetrahydrate and ferric chloride hexahydrate is appropriate, add 100mL distilled water, heating in water bath is to 50-60 DEG C, under 400-500r/min condition, slowly add sodium hydroxide solution regulate pH=10-13, reaction 20-40min, filters, carries out Magneto separate, the ferroso-ferric oxide obtained is cleaned, dries;
(2) emulsion method prepares the phonetic urine pyridine-gelatin-sodium alginate magnetic microcapsule of 5-fluorine:
1. precision takes ferroso-ferric oxide fine powder (cross 200 mesh sieves) and adds 50mL in right amount containing in the gelatin-sodium alginate soln of the phonetic urine pyridine of 5-fluorine, is uniformly mixed under 60 DEG C of conditions;
2. separately get sorbester p17, liquid paraffin mix homogeneously, under 60 DEG C of conditions, add Tween 80,500-600r/min stirs 5min;
3. will 1. slowly add 2., continue to stir;
4. cool the temperature to 40 DEG C, adjust ph, add glutaraldehyde, continue to stir;
5. 4000 r/min centrifugalize 20 min, precipitate uses distilled water, washed with diethylether for several times respectively, and drying under reduced pressure at 35 DEG C, to obtain final product.
2. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 1, is characterized in that Iron dichloride tetrahydrate and ferric chloride hexahydrate mol ratio are 1:1.
3. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 1, is characterized in that step (1) pH value of solution=12.
4. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 1, is characterized in that in the gelatin-sodium alginate soln of step (2) 1. 5-fluorine phonetic urine pyridine, the phonetic urine pyridine of 5-fluorine is 1%.
5. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 1, it is characterized in that (2) 3. mixing time be 20-40 min.
6. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 1, it is characterized in that (2) 4. adjust ph to 5.0, mixing time is 1.5-3 h.
7. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 5, it is characterized in that (2) 3. mixing time be 30 min, make water-in-oil emulsion.
8. the preparation method of a kind of 5-fluorine phonetic urine pyridine magnetic microcapsule according to claim 6, it is characterized in that (2) 4. mixing time be 2 h.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310621215.0A CN104666276A (en) | 2013-11-29 | 2013-11-29 | Preparation method of 5-Fu magnetic microcapsule |
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| CN201310621215.0A CN104666276A (en) | 2013-11-29 | 2013-11-29 | Preparation method of 5-Fu magnetic microcapsule |
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| CN104666276A true CN104666276A (en) | 2015-06-03 |
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| CN201310621215.0A Pending CN104666276A (en) | 2013-11-29 | 2013-11-29 | Preparation method of 5-Fu magnetic microcapsule |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107260703A (en) * | 2017-05-02 | 2017-10-20 | 北京理工大学 | A kind of internal magnetic guiding delivering method of salmonella |
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2013
- 2013-11-29 CN CN201310621215.0A patent/CN104666276A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107260703A (en) * | 2017-05-02 | 2017-10-20 | 北京理工大学 | A kind of internal magnetic guiding delivering method of salmonella |
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Application publication date: 20150603 |