CN1629128A - Method for preparing leucogen materials and leucogen tablets - Google Patents
Method for preparing leucogen materials and leucogen tablets Download PDFInfo
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- CN1629128A CN1629128A CN 200410054101 CN200410054101A CN1629128A CN 1629128 A CN1629128 A CN 1629128A CN 200410054101 CN200410054101 CN 200410054101 CN 200410054101 A CN200410054101 A CN 200410054101A CN 1629128 A CN1629128 A CN 1629128A
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- Prior art keywords
- leucogen
- ethanol
- thrombocytopenia
- aplastic anemia
- dextrin
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Abstract
The invention discloses a method for preparing leucogen materials and leucogen tablets for treating thrombocytopenia and regenerative anemia, which consists of, subjecting ethyl phenylacetate, ethyl formate, ethyl ether, metallic sodium to condensation, acidifying, and cyclization to obtain the leucogen raw material, thus subjecting the leucogen raw powder, dextrin, starch, cane sugar powder, ethanol (60%) and magnesium stearate to sieving, mixing, palletizing, and stamping.
Description
The present invention relates to a kind of being used to prevents, treats the medicinal preparation for oral administration by radio exposure, the caused leukopenia of chemicals, is a kind of leucogen's raw material and leucogen's sheet for the treatment of thrombocytopenia, aplastic anemia.
Signs such as the leukopenia patient often can go out to appear tired, the dizzy tinnitus of tired god, pale complexion, palpitation and insomnia, numbness of the limbs, menoxenia and amenorrhoea, and is serious even can faint.Clinical is thrombocytopenia and aplastic anemia.
Modern medicine is mainly taked etiological treatment to thrombocytopenia and aplastic anemia, as rescues and lose blood and haemolysis, the additional hematopoiesis material that is lacked.Next is to use hematopoietic, and serious anaemia person should take the circumstances into consideration to transfuse blood.
The purpose of this invention is to provide a kind of leucogen's raw material and leucogen's sheet for the treatment of thrombocytopenia, aplastic anemia safely and effectively.
The present invention treats the principal feature of leucogen's raw material and leucogen's sheet of thrombocytopenia, aplastic anemia:
1, leucogen's raw material proterties of the present invention is a white crystalline powder.155～160 ℃ of fusing points.
2, be used for prevention, treatment by radio exposure, the caused leukopenia of chemicals.
3, the usual amounts of this product is oral 1 time, each 20mg, 3 times on the one.
The present invention realizes by following formula rate and complete processing:
1. condensation, acidifying yield 61%
Ratio of components: Phenylacetic acid ethylester: ethyl formate: ether: sodium Metal 99.5
0.8～1.2 ∶ 0.56～0.84∶1.6～2.4∶0.13～0.2
Ether is added in the retort, be chilled to 10-15 ℃, drip Phenylacetic acid ethylester and ethyl formate mixed solution, control reaction temperature 20-30 ℃, top temperature can not be above 32 ℃.Finish, continue to stir standing over night 12 hours.Add hydrochloric acid and be stirred to water layer PH1.Leave standstill branch and get oil reservoir, 110-120 ℃/30-20mm fraction is collected in underpressure distillation, gets α-formyl radical toluylic acid second fat.
2. the cyclization yield 85%
Ratio of components: α-formyl radical toluylic acid second fat: cysteine hydrochloride: ethanol: water
0.8～1.2 ∶?0.64～0.96 ∶4.8～7.2∶5.1～7.7
Water and cysteine hydrochloride are added in the retort, stir,, add sodium bicarbonate, make reaction solution PH about 7 in below 40 ℃.Drip α-formyl radical toluylic acid second fat and ethanol simultaneously.Reflux 1 hour.Crystallisation by cooling gets rid of filter, crystallization distilled water, and ethanol elder generation after scouring is again with a small amount of ether washing.Promptly get leucogen's raw material that the present invention treats thrombocytopenia, aplastic anemia after drying, drying, the pulverizing.Total recovery 52%.
3. film-making
Formula rate: the former powder 0.8kg of leucogen～1.2kg cane sugar powder 1.84kg～2.76kg
Dextrin 1.88kg～2.82kg ethanol (60%) 1.6kg～2.4kg
Starch 1.88kg～2.82kg Magnesium Stearate 0.064kg～0.096kg
A. the former powder of leucogen, dextrin, starch, cane sugar powder are crossed 80 mesh sieves separately.
B. the former powder of leucogen adds dextrin, starch, cane sugar powder and drops into stirrer and mix, and adds ethanol again and makes softwood.
C. softwood is granulated 60 ℃ of fluidized dryings on one-step-granulating method.After the cooling in 1 hour, other adds Magnesium Stearate, the whole grain of 14 mesh sieves mixing, and with 100,000 of 6mm scrobicula stamping compressing tablets, every heavy 0.1mg.Promptly get leucogen's sheet that the present invention treats thrombocytopenia, aplastic anemia.
Embodiments of the invention are as follows:
1. condensation, acidifying yield 61%
Ratio of components: Phenylacetic acid ethylester: ethyl formate: ether: sodium Metal 99.5
1 ∶ 0.7 ∶?2.0∶?0.16
The 2kg ether is added in the retort, be chilled to 10-15 ℃, drip 1kg Phenylacetic acid ethylester and 0.7kg ethyl formate mixed solution, control reaction temperature 20-30 ℃, top temperature can not be above 32 ℃.Finish, continue to stir standing over night 12 hours.Add appropriate hydrochloric acid and be stirred to water layer PH1.Leave standstill branch and get oil reservoir, 110-120 ℃/30-20mm fraction is collected in underpressure distillation, gets α-formyl radical toluylic acid second fat.
2. the cyclization yield 85%
Ratio of components: α-formyl radical toluylic acid second fat: cysteine hydrochloride: ethanol: water
1 ∶ 0.8 ∶6.08∶6.4
6.4kg water and 0.8kg cysteine hydrochloride are added in the retort, stir,, add an amount of sodium bicarbonate, make reaction solution PH about 7 in below 40 ℃.Drip 1kg α-formyl radical toluylic acid second fat and 6.08kg ethanol simultaneously.Reflux 1 hour.Crystallisation by cooling gets rid of filter, crystallization distilled water, and ethanol elder generation after scouring is again with a small amount of ether washing.Promptly get leucogen's raw material that the present invention treats thrombocytopenia, aplastic anemia after drying, drying, the pulverizing.Total recovery 52%.
3. film-making
Formula rate: the former powder 1kg of leucogen cane sugar powder 2.3kg
Dextrin 2.35kg ethanol (60%) 2kg
Starch 2.35kg Magnesium Stearate 0.08kg
A. the former powder of leucogen, dextrin, starch, cane sugar powder are crossed 80 mesh sieves separately.
B.1kg the former powder of leucogen adds 2.35kg dextrin, 2.35kg starch, 2.3kg cane sugar powder and drops into stirrer and mix, and adds 2kg ethanol again and makes softwood.
C. softwood is granulated 60 ℃ of fluidized dryings on one-step-granulating method.After the cooling in 1 hour, other adds the 0.08kg Magnesium Stearate, the whole grain of 14 mesh sieves mixing, and with 100,000 of 6mm scrobicula stamping compressing tablets, every heavy 0.1mg.Promptly get leucogen's sheet that the present invention treats thrombocytopenia, aplastic anemia.
Claims (4)
1, the present invention is a kind of leucogen's raw material for the treatment of thrombocytopenia, aplastic anemia.The present invention realizes by following formula rate and complete processing.It is characterized in that:
A. condensation, acidifying yield 61%
Ratio of components: Phenylacetic acid ethylester: ethyl formate: ether: sodium Metal 99.5
0.8～1.2∶0.56～0.84∶1.6～2.4∶0.13～0.2
Ether is added in the retort, be chilled to 10-15 ℃, drip Phenylacetic acid ethylester and ethyl formate mixed solution, control reaction temperature 20-30 ℃, top temperature can not be above 32 ℃.Finish, continue to stir standing over night 12 hours.Add hydrochloric acid and be stirred to water layer PH1.Leave standstill branch and get oil reservoir, 110-120 ℃/30-20mm fraction is collected in underpressure distillation, gets α-formyl radical toluylic acid second fat.
B. the cyclization yield 85%
Ratio of components: α-formyl radical toluylic acid second fat: cysteine hydrochloride: ethanol: water
0.8～1.2∶0.64～0.96∶4.8～7.2∶5.1～7.7
Water and cysteine hydrochloride are added in the retort, stir,, add sodium bicarbonate, make reaction solution PH about 7 in below 40 ℃.Drip α-formyl radical toluylic acid second fat and ethanol simultaneously.Reflux 1 hour.Crystallisation by cooling gets rid of filter, crystallization distilled water, and ethanol elder generation after scouring is again with a small amount of ether washing.Promptly get leucogen's raw material that the present invention treats thrombocytopenia, aplastic anemia after drying, drying, the pulverizing.Total recovery 52%.
2, formula rate and the complete processing according to best in the formula rate of leucogen's raw material of the treatment thrombocytopenia described in the claim 1, aplastic anemia and the complete processing is as follows:
A. condensation, acidifying yield 61%
Ratio of components: Phenylacetic acid ethylester: ethyl formate: ether: sodium Metal 99.5
1∶0.7∶2.0∶0.16
The 2kg ether is added in the retort, be chilled to 10-15 ℃, drip 1kg Phenylacetic acid ethylester and 0.7kg ethyl formate mixed solution, control reaction temperature 20-30 ℃, top temperature can not be above 32 ℃.Finish, continue to stir standing over night 12 hours.Add appropriate hydrochloric acid and be stirred to water layer PH1.Leave standstill branch and get oil reservoir, 110-120 ℃/30-20mm fraction is collected in underpressure distillation, gets α-formyl radical toluylic acid second fat.
B. the cyclization yield 85%
Ratio of components: α-formyl radical toluylic acid second fat: cysteine hydrochloride: ethanol: water
1∶0.8∶6.08∶6.4
6.4kg water and 0.8kg cysteine hydrochloride are added in the retort, stir,, add an amount of sodium bicarbonate, make reaction solution PH about 7 in below 40 ℃.Drip 1kg α-formyl radical toluylic acid second fat and 6.08kg ethanol simultaneously.Reflux 1 hour.Crystallisation by cooling gets rid of filter, crystallization distilled water, and ethanol elder generation after scouring is again with a small amount of ether washing.Promptly get leucogen's raw material that the present invention treats thrombocytopenia, aplastic anemia after drying, drying, the pulverizing.Total recovery 52%.
3, the present invention is a kind of leucogen's sheet for the treatment of thrombocytopenia, aplastic anemia.The present invention realizes by following formula rate and complete processing.It is characterized in that:
Formula rate: the former powder 0.8kg of leucogen～1.2kg cane sugar powder 1.84kg～2.76kg
Dextrin 1.88kg～2.82kg ethanol (60%) 1.6kg～2.4kg
Starch 1.88kg～2.82kg Magnesium Stearate 0.064kg～0.096kg
A. the former powder of leucogen, dextrin, starch, cane sugar powder are crossed 80 mesh sieves separately.
B. the former powder of leucogen adds dextrin, starch, cane sugar powder and drops into stirrer and mix, and adds ethanol again and makes softwood.
C. softwood is granulated 60 ℃ of fluidized dryings on one-step-granulating method.After the cooling in 1 hour, other adds Magnesium Stearate, the whole grain of 14 mesh sieves mixing, and with 100,000 of 6mm scrobicula stamping compressing tablets, every heavy 0.1mg.Promptly get leucogen's sheet that the present invention treats thrombocytopenia, aplastic anemia.
4, formula rate and the complete processing according to best in the formula rate of leucogen's sheet of the treatment thrombocytopenia described in the claim 3, aplastic anemia and the complete processing is as follows:
Formula rate: the former powder 1kg of leucogen cane sugar powder 2.3kg
Dextrin 2.35kg ethanol (60%) 2kg
Starch 2.35kg Magnesium Stearate 0.08kg
A. the former powder of leucogen, dextrin, starch, cane sugar powder are crossed 80 mesh sieves separately.
B.1kg the former powder of leucogen adds 2.35kg dextrin, 2.35kg starch, 2.3kg cane sugar powder and drops into stirrer and mix, and adds 2kg ethanol again and makes softwood.
C. softwood is granulated 60 ℃ of fluidized dryings on one-step-granulating method.After the cooling in 1 hour, other adds the 0.08kg Magnesium Stearate, the whole grain of 14 mesh sieves mixing, and with 100,000 of 6mm scrobicula stamping compressing tablets, every heavy 0.1mg.Promptly get leucogen's sheet that the present invention treats thrombocytopenia, aplastic anemia.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410054101 CN1629128A (en) | 2004-08-30 | 2004-08-30 | Method for preparing leucogen materials and leucogen tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410054101 CN1629128A (en) | 2004-08-30 | 2004-08-30 | Method for preparing leucogen materials and leucogen tablets |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1629128A true CN1629128A (en) | 2005-06-22 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410054101 Pending CN1629128A (en) | 2004-08-30 | 2004-08-30 | Method for preparing leucogen materials and leucogen tablets |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1302283C (en) * | 2005-07-15 | 2007-02-28 | 张宏业 | Quality inspection of Ricosi preparation |
| CN103102324A (en) * | 2011-11-14 | 2013-05-15 | 南京长澳医药科技有限公司 | Preparation method of leucongen |
| CN115872948A (en) * | 2021-12-30 | 2023-03-31 | 江苏吉贝尔药业股份有限公司 | Crystal form B of leucogen, preparation method and application thereof |
| WO2023124408A1 (en) * | 2021-12-30 | 2023-07-06 | 江苏吉贝尔药业股份有限公司 | Crystalline form of leucogen and method for preparation thereof and use thereof |
| CN116655556A (en) * | 2023-04-17 | 2023-08-29 | 常州亚邦制药有限公司 | Crystal form A of ritodrine and preparation method thereof |
-
2004
- 2004-08-30 CN CN 200410054101 patent/CN1629128A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1302283C (en) * | 2005-07-15 | 2007-02-28 | 张宏业 | Quality inspection of Ricosi preparation |
| CN103102324A (en) * | 2011-11-14 | 2013-05-15 | 南京长澳医药科技有限公司 | Preparation method of leucongen |
| CN115872948A (en) * | 2021-12-30 | 2023-03-31 | 江苏吉贝尔药业股份有限公司 | Crystal form B of leucogen, preparation method and application thereof |
| WO2023124408A1 (en) * | 2021-12-30 | 2023-07-06 | 江苏吉贝尔药业股份有限公司 | Crystalline form of leucogen and method for preparation thereof and use thereof |
| CN115872948B (en) * | 2021-12-30 | 2023-09-26 | 江苏吉贝尔药业股份有限公司 | Crystal form B of ritodrine, and preparation method and application thereof |
| CN116655556A (en) * | 2023-04-17 | 2023-08-29 | 常州亚邦制药有限公司 | Crystal form A of ritodrine and preparation method thereof |
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