CN103271927A - Technique of three-stage dilution method for improving content uniformity of oral contraceptive - Google Patents
Technique of three-stage dilution method for improving content uniformity of oral contraceptive Download PDFInfo
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- CN103271927A CN103271927A CN2013102104053A CN201310210405A CN103271927A CN 103271927 A CN103271927 A CN 103271927A CN 2013102104053 A CN2013102104053 A CN 2013102104053A CN 201310210405 A CN201310210405 A CN 201310210405A CN 103271927 A CN103271927 A CN 103271927A
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Abstract
The invention discloses a technique of a three-stage dilution method for improving content uniformity of oral contraceptive, and the technique is as follows: active prescription medicines are dissolved in a solvent mixture of which the weight is 5-200 times the weight of the active medicines; the active medicines are progestational hormone and estrogen; the solvent mixture is chloroform or other solvent mixtures; and the active medicines are completely dissolved in the solvent mixture into a solution at molecular distribution state, so that the influences caused by size of medicine particles in mixing of solid medicines to the content uniformity are avoided. The technique disclosed by the invention has the advantage of improving the uniformity of main medicines of the oral contraceptive.
Description
Technical field
The present invention relates to a kind of technology of three grades of dilution methods, refer in particular to and improve the formulation and technology that the oral contraceptive drug content reaches the improvement desogestrel stability of uniformity requirement.
Background technology
The compound medicine that oral contraceptive is made up of progestogen and estrogen, development have experienced so far for several times and have updated.Current, in the best oral contraceptive of developed country's medical market sales volume, contain the estrogen combination of third generation progestogen (as norgestimate) and low dosage more efficiently.The corresponding minimizing of estrogenic use amount, the tablet that its content is minimum only is the 0.02mg/ sheet, thereby it has higher effect and lower toxic and side effects.Since in the oral contraceptive of new generation active ingredient progestogen and estrogenic content low especially (estrogenic content have only for sheet heavy 0.03%), easily cause the drug content inequality in product development and the industrialization process, make the effectiveness of clinical medicine and safety inconsistent.The content homogeneity question has increased the difficulty of the especially big production of this product development, because the scrappage of drug content inequality is higher, the oral contraceptive that therefore up to the present contains third generation progestogen only has few in number listing a company abroad in process of production.The inhomogeneity requirement of oral contraceptive content must not surpass 5% of labelled amount for the active constituents of medicine content difference.
Summary of the invention
The objective of the invention is in order to overcome above deficiency, provide a kind of in order to improve the formulation and technology that the oral contraceptive drug content reaches the improvement desogestrel stability of uniformity requirement.
Purpose of the present invention is achieved through the following technical solutions: a kind of technology of improving three grades of dilution methods of oral contraceptive content uniformity, it is characterized in that, and may further comprise the steps:
A, the prescription active medicine is dissolved in this active medicine weight 5-200 solvent mixture doubly, described active medicine is progestogen and estrogen, the solvent mixture is chloroform or other solvent mixture, make active medicine all dissolvings in the solvent mixture, the solution that is the molecular distribution state is eliminated solid drugs mixing Chinese medicine granular size to the inhomogeneity influence of content;
B, in fluidised bed granulator, add this batch prescription with 10%-40% pharmaceutic adjuvant of gross weight, in fluid bed, be " boiling " shape with the pressure-air messenger drug that purifies and heated with adjuvant, simultaneously the active agent solution among the processing step A is sprayed on the pharmaceutic adjuvant of " boiling " shape, after medicine has sprayed, continue to use the pressure-air that purifies and heated to containing the granules of accessories drying of active medicine, it is mixed to finish one-level simultaneously in fluidised bed granulator;
C, the granules of accessories that contains active medicine that drying is crossed are taken out from fluidised bed granulator, add blender, add 10%-40% pharmaceutic adjuvant of this batch prescription gross weight in addition simultaneously again, and mixed 5-15 minute, it was mixed to finish secondary;
D, the pharmaceutic adjuvant of remaining 80%-20% this batch prescription consumption and lubricant are added in the blender of processing step C, continued mixed 5-15 minute, finish three grades mixed;
E, carry out tabletting finishing three grades of mixed whole batch mixings among the processing step D, final tablet coating, and packing are finished the production process of product.
The present invention compared with prior art has the following advantages:
Improve the uniformity of this oral contraceptive principal agent, made every batch of content with every medicine Chinese medicine identical, guaranteed safety and clinical effective concordance of drug use.
The specific embodiment:
In order to deepen the understanding of the present invention, the invention will be further described below in conjunction with embodiment, and this embodiment only is used for explaining the present invention, does not constitute the restriction to protection domain of the present invention.
Embodiment: progestogen and estrogen are 1,000,000 norethindrone and ethinylestradiol tablet prescription, and lubricant is magnesium stearate, and each material consumption is as follows:
| Composition | Criticize consumption (kilogram) | Percentage by weight |
| Norethindrone | 1.000 | 1.000% |
| Ethinylestradiol | 0.035 | 0.035% |
| Chloroform (volatilizing in the process) | 12.000 | 0.000% |
| Pharmaceutic adjuvant | 98.465 | 98.465% |
| Magnesium stearate | 0.500 | 0.500% |
| The batch gross weight | 100.000 | 100.000% |
A, 1 kilogram norethindrone and 35 gram ethinylestradiols are dissolved in 12 kilograms the chloroform, make all dissolvings in solvent of norethindrone and ethinylestradiol;
B, in fluidised bed granulator, add 20 kilograms of pharmaceutic adjuvants of this batch prescription consumption, in fluid bed, be " boiling " shape with the pressure-air messenger drug that purifies and heated with adjuvant, be sprayed on the pharmaceutic adjuvant of " boiling " shape containing norethindrone and the ethinylestradiol drug solution speed by the 100-300 gram/minute among the processing step A simultaneously, after medicine has sprayed, continue to use the pressure-air that purifies and heated to containing the granules of accessories drying of active medicine, it is mixed to finish one-level;
C, the granule of from step B drying being crossed that contains norethindrone and ethinylestradiol take out from fluid bed, add blender, add the other 30 kilograms pharmaceutic adjuvant of this batch prescription consumption simultaneously, and mixed 10 minutes, it was mixed to finish secondary;
D. the magnesium stearate of remaining 48.465 kilograms pharmaceutic adjuvant and 0.5 kilogram is added in the same blender from step C, mixed 10 minutes, finish three grades mixed;
E, the whole batch mixing of finishing among the processing step D is carried out tabletting, sheet heavily is 100 mg, and final tablet carries out coating, and packing, finishes the production process of product.
Claims (1)
1. a technology of improving three grades of dilution methods of oral contraceptive content uniformity is characterized in that, may further comprise the steps:
A, the prescription active medicine is dissolved in this active medicine weight 5-200 solvent mixture doubly, described active medicine is progestogen and estrogen, the solvent mixture is chloroform or other solvent mixture, make active medicine all dissolvings in the solvent mixture, the solution that is the molecular distribution state is eliminated solid drugs mixing Chinese medicine granular size to the inhomogeneity influence of content;
B, in fluidised bed granulator, add this batch prescription with 10%-40% pharmaceutic adjuvant of gross weight, in fluid bed, be " boiling " shape with the pressure-air messenger drug that purifies and heated with adjuvant, simultaneously the active agent solution among the processing step A is sprayed on the pharmaceutic adjuvant of " boiling " shape, after medicine has sprayed, continue to use the pressure-air that purifies and heated to containing the granules of accessories drying of active medicine, it is mixed to finish one-level simultaneously in fluidised bed granulator;
C, the granules of accessories that contains active medicine that drying is crossed are taken out from fluidised bed granulator, add blender, add 10%-40% pharmaceutic adjuvant of this batch prescription gross weight in addition simultaneously again, and mixed 5-15 minute, it was mixed to finish secondary;
D, the pharmaceutic adjuvant of remaining 80%-20% this batch prescription consumption and lubricant are added in the blender of processing step C, continued mixed 5-15 minute, finish three grades mixed;
E, carry out tabletting finishing three grades of mixed whole batch mixings among the processing step D, final tablet coating, and packing are finished the production process of product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102104053A CN103271927A (en) | 2013-05-31 | 2013-05-31 | Technique of three-stage dilution method for improving content uniformity of oral contraceptive |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102104053A CN103271927A (en) | 2013-05-31 | 2013-05-31 | Technique of three-stage dilution method for improving content uniformity of oral contraceptive |
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| Publication Number | Publication Date |
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| CN103271927A true CN103271927A (en) | 2013-09-04 |
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| CN2013102104053A Pending CN103271927A (en) | 2013-05-31 | 2013-05-31 | Technique of three-stage dilution method for improving content uniformity of oral contraceptive |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114259498A (en) * | 2021-12-02 | 2022-04-01 | 南通联亚药业有限公司 | Pharmaceutical composition containing desogestrel and ethinylestradiol, and preparation method and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1104487A (en) * | 1992-09-04 | 1995-07-05 | 阿克佐公司 | Pharmaceutical granulate |
-
2013
- 2013-05-31 CN CN2013102104053A patent/CN103271927A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1104487A (en) * | 1992-09-04 | 1995-07-05 | 阿克佐公司 | Pharmaceutical granulate |
Non-Patent Citations (1)
| Title |
|---|
| 奚念朱: "《药剂学》", 30 April 1996 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114259498A (en) * | 2021-12-02 | 2022-04-01 | 南通联亚药业有限公司 | Pharmaceutical composition containing desogestrel and ethinylestradiol, and preparation method and application thereof |
| CN114259498B (en) * | 2021-12-02 | 2023-04-28 | 南通联亚药业股份有限公司 | Pharmaceutical composition containing desogestrel and ethinyl estradiol as well as preparation method and application thereof |
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Application publication date: 20130904 |