CN104546760A - Thiamazole composition freeze-drying tablet and preparation method thereof - Google Patents
Thiamazole composition freeze-drying tablet and preparation method thereof Download PDFInfo
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- CN104546760A CN104546760A CN201410829202.7A CN201410829202A CN104546760A CN 104546760 A CN104546760 A CN 104546760A CN 201410829202 A CN201410829202 A CN 201410829202A CN 104546760 A CN104546760 A CN 104546760A
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Abstract
The invention provides a thiamazole composition freeze-drying tablet and a preparation method thereof, and relates to the technical field of medicines and medicine production. The thiamazole composition freeze-drying tablet comprises thiamazole, starch and cane sugar, wherein starch and cane sugar are adopted as auxiliary materials. As ordinary corn starch is subjected to heating process treatment, the adhesion and disintegration functions of starch in the tablet are improved, the formability of the tablet is improved, and the thiamazole composition freeze-drying tablet only needs two auxiliary materials, that is, starch and cane sugar. The thiamazole composition freeze-drying tablet is prepared by using a freeze-drying process that the temperature is reduced twice and risen twice, so that the formability of the tablet is relatively good, the dissolution rate of the tablet is increased, and the bioavailability of the tablet is improved; defects of ordinary thiamazole tablets are overcome, the types and the use amount of auxiliary materials in the thiamazole tablet are reduced, the tablet is high in dissolution rate and high in bioavailability, and the curative effect and security of the tablet in clinical medication are ensured.
Description
Technical field
The present invention relates to medicine and medical production technical field, be specifically related to a kind of thiamazole composition freeze-drying sheet and preparation method thereof.
Background technology
Molecular formula C
4h
6n
2s
Molecular weight 114.16
Existing clinical common dosage forms is the thiamazole sheet of synthetic.This product is antithyroid drug.Its mechanism of action suppresses thyroid endoperoxide enzyme, thus hinder the oxidation of iodide and the coupling of tyrosine in suction to thyroid, hinders the synthesis of thyroxine (T4) and trilute (T3).Animal experimental observation can suppress bone-marrow-derived lymphocyte synthetic antibody, reduces the level of thyroid stimulating antibody in blood circulation, makes Ts function recover normal.Clinical common formulations is tablet.
In common thiamazole sheet containing supplementary product kind and quantity more, generally will use filler, lubricant, disintegrating agent, adhesive, correctives etc., its disintegration time reaches 12 minutes, and bioavailability is lower.And increasing research shows that impurity in the incompatibility of the toxic and side effects of adjuvant itself, adjuvant and principal agent, adjuvant etc. all can have an impact to the safety of medicine.
Therefore, provide one can overcome above-mentioned shortcoming, select suitable adjuvant and technique, reduce supplementary product kind and consumption in thiamazole sheet, improve thiamazole sheet bioavailability, ensure that the safety of clinical application all has positive effect.
Traditional lyophilizing tablet can improve bioavailability, but still need use the adjuvant such as mannitol, gelatin.And mannitol has certain biological activity, gelatin resource-constrained and perishable.
Starch is the basic adjuvant of oral solid formulation, it is polymerized by glucose molecule, and be commonly used for adhesive, diluent and disintegrating agent in tablets, it is cheap and easy to get, to human-body safety, but being used alone starch has no report as adjuvant freeze-dry process production thiamazole lyophilizing sheet.
Summary of the invention
Technical problem to be solved by this invention is the defect overcoming prior art, and propose a kind of thiamazole composition freeze-drying sheet and preparation method thereof further, said preparation adjuvant is few, good stability, and bioavailability is high.
Technical problem to be solved by this invention realizes by the following technical solutions:
A kind of thiamazole composition freeze-drying sheet, adjuvant is done with starch and sucrose, produce with freeze-dry process, this tablet overcomes the shortcoming of above-mentioned common thiamazole sheet, decrease supplementary product kind and consumption in thiamazole sheet, this sheet dissolution is large, and bioavailability is high, ensure that curative effect and the safety of clinical application.
A kind of thiamazole composition freeze-drying sheet, is prepared from by following raw material:
A preparation method for thiamazole composition freeze-drying sheet, comprises step as follows:
A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 5.5-6.5, be then heated to 72 DEG C, be incubated 20 minutes, make the corn starch solution of 5 ~ 15% (W/V);
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100mL, stir evenly, obtain B solution;
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, is down to room temperature and obtains Semen Maydis-sucrose solution;
D, take thiamazole 50 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;
Medicinal liquid is sub-packed in drug-containing dish after measuring thiamazole content by E, medicinal liquid, each drug-containing dish dress 1.0ml;
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain thiamazole composition freeze-drying sheet.
Described starch selects corn starch, preferably the corn starch solution of 10% (W/V).
Beneficial effect of the present invention is:
The preparation method of a kind of thiamazole composition freeze-drying sheet of the present invention, heating process process is carried out to common corn starch, starch bonding in tablets, disintegration can be improved, improve the mouldability of tablet, in thiamazole composition freeze-drying sheet, dosage of sucrose is 8.5% (W/V), it is the hardness reinforcer of this tablet, and plays flavored action.Thiamazole composition freeze-drying sheet only needs starch and sucrose two kinds of adjuvants.The freeze-dry process of two liters falls in thiamazole composition freeze-drying sheet employing two, and twice cooling, twice intensification can make sheet mouldability better, and shorten the disintegration time of tablet, improve the bioavailability of tablet.
Detailed description of the invention
The technological means realized to make the present invention, creation characteristic, reaching object and effect is easy to understand, below in conjunction with specific embodiment, set forth the present invention further, but following embodiment being only the preferred embodiments of the present invention, and not all.Based on the embodiment in embodiment, those skilled in the art under the prerequisite not making creative work obtain other embodiment, all belong to the protection domain of this patent.
Embodiment 1
A, take the corn starch of 100g, the purified water adding 900ml stirs, and controls 6.5, is then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 9% (W/V) by pH adjusting agent by the pH value of solution.
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100mL, stir evenly, obtain B solution.
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after solution be down to room temperature obtain Semen Maydis-sucrose solution.
D, take thiamazole 50g, add in 1L Semen Maydis-sucrose solution, stir 30 minutes.
Medicinal liquid is sub-packed in drug-containing dish after measuring thiamazole content by E, medicinal liquid, each drug-containing dish dress 1.0ml.
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain thiamazole composition freeze-drying sheet.
Embodiment 2
A, take the corn starch of 130g, the purified water adding 900ml stirs, and controls at 5.5-7.5, is then heated to 72 DEG C, keep 120 minutes, make the corn starch solution of 13% (W/V) by pH adjusting agent by the pH value of solution.
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100mL, stir evenly, obtain B solution.
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after solution be down to room temperature obtain Semen Maydis-sucrose solution.
D, take thiamazole 50 grams (by 1000 calculations), add 1L Semen Maydis-sucrose solution, stir 30 minutes.
Medicinal liquid is sub-packed in drug-containing dish after measuring thiamazole content by E, medicinal liquid, each drug-containing dish dress 1.0ml.
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs.Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain thiamazole composition freeze-drying sheet.
Experimental data
The thiamazole composition freeze-drying sheet that above-described embodiment is obtained carries out following quality research test:
1, hardness, friability contrast test
Get thiamazole composition freeze-drying sheet prepared by above-described embodiment respectively and thiamazole ordinary tablet (commercially available) detects friability and hardness by " Chinese Pharmacopoeia " version in 2010 two annex XG inspection techniques, contrast, the results are shown in following table:
| Sample | Hardness/N | Friability |
| Embodiment 1 | 62 | <1％ |
| Embodiment 2 | 65 | <1％ |
| Ordinary tablet | 68 | <1％ |
Experimental data shows, thiamazole composition freeze-drying sheet and ordinary tablet without significant difference, meet " Chinese Pharmacopoeia " version in 2010 to the requirement of tablet on friability and hardness.
2, disintegration contrast test
Get thiamazole composition freeze-drying sheet prepared by above-described embodiment respectively and thiamazole ordinary tablet (commercially available) operates by Chinese Pharmacopoeia (2010 editions) second annex XA, its disintegration is checked.Result is as follows:
One, thiamazole ordinary tablet (commercially available)
Two, thiamazole composition freeze-drying sheet (No. 1 to No. 3 is embodiment 1, and No. 4 to No. 6 is embodiment 2)
Result judges:
Judge about the bioassay standard in disintegration of tablet time limit according to Chinese Pharmacopoeia (2010 editions) second thiamazole tablet quality standard and Chinese Pharmacopoeia (2010 editions) second annex XA, thiamazole sheet is no more than 15 minutes for qualified disintegration, actual measurement is 12 minutes, and thiamazole composition freeze-drying sheet (embodiment 1 and embodiment 2) disintegration is 6 minutes.It can thus be appreciated that thiamazole composition freeze-drying sheet disintegration is than reducing by 50% (6 minutes) thiamazole sheet (commercially available) disintegration, so thiamazole composition freeze-drying sheet absorption of human body is faster, the blood drug level peaking time is shorter than thiamazole ordinary tablet (commercially available), its bioavailability is higher, better efficacy.
More than show and describe ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what describe in above-described embodiment and description is only preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.Application claims protection domain is defined by appending claims and equivalent thereof.
Claims (2)
1. a thiamazole composition freeze-drying sheet, is characterized in that, is prepared from by following raw material:
2. a preparation method for thiamazole composition freeze-drying sheet according to claim 1, is characterized in that, comprise step as follows:
A, take the starch of component amount, add a certain amount of purified water and stir, by pH adjusting agent, the pH value of solution is controlled between 5.5-6.5, be then heated to 72 DEG C, be incubated 20 minutes, make the corn starch solution of 5 ~ 15% (W/V);
B, measure purified water 45ml, boil, add 85g sucrose, stir, after dissolving, continue to be heated to 100 DEG C, filter with purified cotton, the appropriate hot distilled water of filter is cleaned, and washing liquid and filtrate merge, and let cool, add appropriate distilled water, make full dose become 100mL, stir evenly, obtain B solution;
The solution that C, the solution and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, is down to room temperature and obtains Semen Maydis-sucrose solution;
D, take thiamazole 50 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;
Medicinal liquid is sub-packed in drug-containing dish after measuring thiamazole content by E, medicinal liquid, each drug-containing dish dress 1.0ml;
F, the drug-containing dish that medicinal liquid is housed is put into vacuum freezing drying oven, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, then be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 2 ~ 4 hours, then be warming up to 28 ~ 32 DEG C of dryings 4 ~ 6 hours gradually, whole process vacuum remains on 10 handkerchiefs; Finally the drug-containing dish lid of powder charge is covered tightly, and load aluminium foil bag and carry out sealing and obtain thiamazole composition freeze-drying sheet.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410829202.7A CN104546760A (en) | 2014-12-25 | 2014-12-25 | Thiamazole composition freeze-drying tablet and preparation method thereof |
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| CN201410829202.7A CN104546760A (en) | 2014-12-25 | 2014-12-25 | Thiamazole composition freeze-drying tablet and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61242556A (en) * | 1985-04-19 | 1986-10-28 | Hatoya Seika:Kk | Preparation of snack using fruits |
| US20020173016A1 (en) * | 2001-03-27 | 2002-11-21 | Helmut Wurst | High-throughput nucleic acid polymerase devices and methods for their use |
| CN1562004A (en) * | 2004-03-30 | 2005-01-12 | 贵州圣济堂制药有限公司 | Preparation containing methimazole and its preparing method |
-
2014
- 2014-12-25 CN CN201410829202.7A patent/CN104546760A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61242556A (en) * | 1985-04-19 | 1986-10-28 | Hatoya Seika:Kk | Preparation of snack using fruits |
| US20020173016A1 (en) * | 2001-03-27 | 2002-11-21 | Helmut Wurst | High-throughput nucleic acid polymerase devices and methods for their use |
| CN1562004A (en) * | 2004-03-30 | 2005-01-12 | 贵州圣济堂制药有限公司 | Preparation containing methimazole and its preparing method |
Non-Patent Citations (1)
| Title |
|---|
| 刘晓睿: "《口腔速溶片的研究进展》", 《中南药学》 * |
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Application publication date: 20150429 |