CN104434774A - Hydrocortisone composition freeze-dried tablet and preparation method thereof - Google Patents
Hydrocortisone composition freeze-dried tablet and preparation method thereof Download PDFInfo
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- CN104434774A CN104434774A CN201410736810.3A CN201410736810A CN104434774A CN 104434774 A CN104434774 A CN 104434774A CN 201410736810 A CN201410736810 A CN 201410736810A CN 104434774 A CN104434774 A CN 104434774A
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Abstract
The invention provides a hydrocortisone composition freeze-dried tablet and a preparation method thereof, and relates to the technical field of medicines and medicine production. The hydrocortisone composition freeze-dried tablet is made of hydrocortisone, starch and cane sugar, starch and cane sugar are used as auxiliary materials, the bonding and disintegration functions of the starch in the tablet are improved as ordinary corn starch is subjected to heating process treatment, the forming property of the tablet is improved, and the hydrocortisone composition freeze-dried tablet only needs two auxiliary materials, namely, starch and cane sugar. According to the hydrocortisone composition freeze-dried tablet, a freeze-drying process, namely twice raising of temperature and twice reduction of temperature, is adopted, so that the forming property of the tablet is relatively good, the dissolution rate of the tablet is increased, and the biological availability of the tablet is improved; by adopting the tablet, the defects of ordinary hydrocortisone tablets are overcome, the types and the use amount of the auxiliary materials in the hydrocortisone tablet are reduced, the dissolution rate is large, the bioavailability is high, and the treatment effect and the security in clinical administration are ensured.
Description
Technical field
The present invention relates to medicine and medical production technical field, be specifically related to a kind of hydrocortisone composition freeze-drying sheet and preparation method thereof.
Background technology
Hydrocortisone is synthetic is also naturally occurring glucocorticoid, be mainly used in the replacement therapy of adrenocortical insufficiency and the treatment of congenital adrenal function hypertrophy disease, also can be used for rheumatoid arthritis, rheumatic fever, gout, bronchial asthma, anaphylactic disease, and can be used for severe infections and shock treatment etc.
Molecular weight: 362.47
In common hydrocortisone sheet containing supplementary product kind and quantity more, generally to use filler, lubricant, disintegrating agent, adhesive, correctives etc., according to Chinese Pharmacopoeia (2010 editions) second hydrocortisone tablet quality standard, the dissolution of hydrocortisone sheet reached more than 70% for qualified 30 minutes time, 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 hydrocortisone sheet, improve dissolution and the bioavailability of hydrocortisone sheet, ensure that the safety of clinical application all has positive effect.
Traditional lyophilizing tablet can improve dissolution and 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 hydrocortisone 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 hydrocortisone 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 hydrocortisone composition freeze-drying sheet, adjuvant is done with starch and sucrose, produce with freeze-dry process, this tablet overcomes the shortcoming of above-mentioned conventional hydrogenation cortisone sheet, decrease supplementary product kind and consumption in hydrocortisone sheet, this sheet dissolution is large, and bioavailability is high, ensure that curative effect and the safety of clinical application.
A kind of hydrocortisone composition freeze-drying sheet, is prepared from by following raw material:
A preparation method for hydrocortisone 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 5-7.5, 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 hydrocortisone 10 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;
Medicinal liquid is sub-packed in drug-containing dish after measuring hydrocortisone 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 hydrocortisone 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 hydrocortisone 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 hydrocortisone composition freeze-drying sheet, dosage of sucrose is 8.5% (W/V), it is the hardness reinforcer of this tablet, and plays flavored action.Hydrocortisone composition freeze-drying sheet only needs starch and sucrose two kinds of adjuvants.The freeze-dry process of two liters falls in hydrocortisone composition freeze-drying sheet employing two, and twice cooling, twice intensification can make sheet mouldability better, which increase the dissolution of tablet, thus improve the bioavailability of tablet.
Accompanying drawing explanation
Fig. 1 is the dissolution correlation curve figure of hydrocortisone in experiment.
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 at 5-7.5, 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 hydrocortisone 10g, add in 1L Semen Maydis-sucrose solution, stir 30 minutes.
Medicinal liquid is sub-packed in drug-containing dish after measuring hydrocortisone 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 hydrocortisone composition freeze-drying sheet.
Embodiment 2
A, take the corn starch of 130g, the purified water adding 900ml stirs, and controls at 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 hydrocortisone 10 grams (by 1000 calculations), add 1L Semen Maydis-sucrose solution, stir 30 minutes.
Medicinal liquid is sub-packed in drug-containing dish after measuring hydrocortisone 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 hydrocortisone composition freeze-drying sheet.
Experimental data
The hydrocortisone composition freeze-drying sheet that above-described embodiment is obtained carries out following quality research test:
1, hardness, friability contrast test
Get hydrocortisone composition freeze-drying sheet prepared by above-described embodiment respectively and hydrocortisone ordinary tablet (commercially available) detects friability and hardness by " Chinese Pharmacopoeia " version in 2010 two annex X G inspection techniques, carry out comparative study, the results are shown in following table:
Sample | Hardness/N | Friability |
Execute example 1 | 67.5 | <1% |
Execute example 2 | 66.3 | <1% |
Ordinary tablet (commercially available) | 69.5 | <1% |
Experimental data shows, hydrocortisone composition freeze-drying sheet and ordinary tablet (commercially available) without significant difference, meet " Chinese Pharmacopoeia " version in 2010 to the requirement of tablet on friability and hardness.
2, dissolution contrast test
(No. 1 to No. 3 is embodiment 1 to get hydrocortisone sheet (commercially available) and each 6 of hydrocortisone composition freeze-drying sheet, No. 4 to No. 6 is embodiment 2), press Chinese Pharmacopoeia (2010 editions) second dissolution method annex X C second method respectively, according to dissolution method (annex X C second method), with water 900ml for dissolution medium, rotating speed is 50 turns per minute, operate in accordance with the law, respectively through 10min, 20min, 25min, 30min, during 60min, get solution to filter, precision measures subsequent filtrate 5ml and puts in 10ml measuring bottle, be diluted with water to scale, shake up.According to ultraviolet visible spectrophotometry (annex IV A), measuring absorbance at the wavelength place of 248nm, is the stripping quantity of the every sheet of 449.3 calculating by the absorptance of C21H3005.Result is as follows:
One, hydrocortisone sheet (commercially available)
Two, hydrocortisone lyophilizing sheet (No. 1 to No. 3 is embodiment 1, and No. 4 to No. 6 is embodiment 2)
Respectively with catch cropping Dissolution profiles during average dissolution pair, as Fig. 1.
Four, result judges
Judge according to Chinese Pharmacopoeia (2010 editions) second hydrocortisone tablet quality standard, the dissolution of hydrocortisone sheet (commercially available) reached more than 70% for qualified 30 minutes time, actual measurement is 73.4%, and hydrocortisone lyophilizing sheet dissolution 20 minutes time reaches 72.5%.It can thus be appreciated that the time that hydrocortisone lyophilizing sheet dissolution reaches 70% is than the time decreasing about 10 minutes of hydrocortisone sheet (commercially available).So the hydrocortisone lyophilizing sheet blood drug level peaking time is shorter than hydrocortisone sheet (commercially available), and 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 hydrocortisone composition freeze-drying sheet, is characterized in that, is prepared from by following raw material:
2. a preparation method for hydrocortisone 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 5-7.5, 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 hydrocortisone 10 grams, add in 1L Semen Maydis-sucrose solution, stir 25 ~ 35 minutes;
Medicinal liquid is sub-packed in drug-containing dish after measuring hydrocortisone 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 hydrocortisone composition freeze-drying sheet.
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Citations (2)
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 |
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Patent Citations (2)
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 |
Non-Patent Citations (2)
Title |
---|
刘晓睿等: "口腔速溶片的研究进展", 《中南药学》, vol. 2, no. 05, 20 October 2004 (2004-10-20), pages 296 - 297 * |
刘阳等: "氢化可的松片含量测定方法的研究", 《现代医药卫生》, vol. 27, no. 10, 31 December 2011 (2011-12-31), pages 1586 * |
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Application publication date: 20150325 |