CN104434834A - Mebendazole composition chewable tablet and preparation method thereof - Google Patents
Mebendazole composition chewable tablet and preparation method thereof Download PDFInfo
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- CN104434834A CN104434834A CN201410736768.5A CN201410736768A CN104434834A CN 104434834 A CN104434834 A CN 104434834A CN 201410736768 A CN201410736768 A CN 201410736768A CN 104434834 A CN104434834 A CN 104434834A
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Abstract
The invention provides a mebendazole composition chewable tablet and a preparation method thereof, and relates to the technical field of medicine production. The mebendazole composition chewable tablet consists of mebendazole, starch and sucrose. The tablet disclosed by the invention is capable of overcoming the shortcomings of a normal chewable tablet, and reducing the variety and dosage of accessories in the mebendazole chewable tablet; and the medicine preparation is excellent in performance, high in bioavailability, good in stability, high in patient acceptability and free from grittiness, and has important clinical application value.
Description
Technical field
The present invention relates to medicine and medical production technical field, be specifically related to a kind of mebendazole compositions chewable tablet and preparation method thereof.
Background technology
Tablet quality is stable, taking convenience, is basic, the most the most frequently used a kind of dosage form.But for the patient of child, old man and dysphagia, conventional tablet often takes difficulty, and Long-term taking medicine even can make it produce psychological phenomenon of refusing to take medicine, and chewable tablet then can remedy such and insufficient.Chewable tablet is the tablet under a class can chew posterior phraynx in oral cavity, and size is general identical with conventional tablet, can make difform Special-shaped sheet as required.Tablet is convenient to swallow after chewing, and coat tablets is long-pending to be increased, and can promote medicine dissolving in vivo, absorption.For the medicine of difficult disintegrate, make chewable tablet and can accelerate its disintegrate, improve drug effect.Chewable tablet taking convenience, even if also can medication on time under the condition of hydropenia, be specially adapted to the patient that children's, old man, dysphagia or gastrointestinal function are poor, can reduces medicine and bear gastrointestinal.Therefore, chewable tablet application is extensively got up gradually.
Mebendazole is a wide spectrum anthelmintic, in body or in vitro tests all prove directly to suppress nematicide to the absorption of glucose, cause glycogen depletion, make it survive, there is the effect killed larva significantly, suppress ovulation development, but do not affect blood in human body in sugar level.Can be used for the intestinal parasitical diseases such as control ancylostome, ascarid, pinworm, whipworm, excrement class loop line worm.Its chemical structural formula formula is as follows:
C
16H
13N
3O
3259.30
The pharmaceutical preparation of the mebendazole gone on the market has conventional tablet, ball, chewable tablet, emulsifiable paste, wherein mebendazole chewable tablet supplementary product kind and quantity more, generally to use filler, lubricant, disintegrating agent, adhesive, correctives etc., and at least will use 4 kinds of adjuvants.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, select suitable adjuvant and technique, reduce supplementary product kind and the consumption of mebendazole chewable tablet, improve bioavailability and the stability of mebendazole chewable tablet, for ensureing that the safety of clinical application has positive effect.
Starch is polymerized by glucose molecule, it is the basic adjuvant of oral solid formulation, be usually used in chewable tablet, making adhesive, diluent and disintegrating agent, and starch all extracts from the natural materials such as Semen Maydis, Maninot esculenta crantz., safe and reliable, cheap and easy to get, but being used alone starch has no report as adjuvant for the production of chewable tablet.
Summary of the invention
Technical problem to be solved by this invention is the defect overcoming prior art, and propose a kind of mebendazole compositions chewable tablet 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 mebendazole compositions chewable tablet, comprise mebendazole, starch, sucrose, this tablet overcomes the shortcoming of above-mentioned common chewable tablet, decrease supplementary product kind and consumption in mebendazole chewable tablet, this pharmaceutical preparation function admirable, bioavailability is high, have good stability, patient acceptance is high, without sand type, has important clinical value.
A kind of mebendazole compositions chewable tablet, is prepared from by following raw material:
A preparation method for mebendazole compositions chewable tablet, 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 4 ~ 9, be then heated to 72 DEG C, be incubated 120 minutes, make the gelatinizing 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 medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid;
D, take mebendazole 100 grams, add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 25 ~ 35 minutes;
E, the medicinal liquid sampling and measuring mebendazole content that step D is obtained;
After mebendazole content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made;
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, 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 below 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 mebendazole compositions chewable tablet.
The preparation method of a kind of mebendazole compositions chewable tablet of the present invention, in described steps A, pH adjusting agent is sodium hydroxide or hydrochloric acid, preferably controls 6.5 by the pH value of solution; Mixing time preferably 30 minutes in step C; Preferably be warming up to 0 DEG C gradually again in step F, keep 3 hours, then be warming up to 30 DEG C of dryings 5 hours gradually; Described starch selects corn starch.
Beneficial effect of the present invention is:
The preparation method of a kind of mebendazole compositions chewable tablet of the present invention, it adopts unique processing step, carries out special process process, can improve the bonding of starch in chewable tablet, disintegration to common corn starch, improves the molding of chewable tablet.And dosage of sucrose is 8.5% (W/V) in mebendazole compositions chewable tablet, it is the hardness reinforcer of this tablet, and plays flavored action.Mebendazole compositions chewable tablet only needs starch and sucrose two kinds of adjuvants, reduces the kind of required adjuvant; Because the technique of two liters falls in freeze-dry process employing two, twice cooling, twice intensification can make chewable tablet mouldability better, and improve stability and the dissolution of product, improve quality and the bioavailability of product.Therefore the preparation method of a kind of mebendazole compositions chewable tablet provided by the invention has easy to operate, and prescription is simple, and technique is unique, the feature that product stability, safety are high.
Accompanying drawing explanation
Fig. 1 is the dissolution correlation curve figure of mebendazole 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.
Mebendazole content is for 100mg/ sheet.
Embodiment 1
Prescription: 1000 amounts
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 gelatinizing corn starch solution of about 10% (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 medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid.
D, take mebendazole 100g (by 1000 calculations), add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 30 minutes.
E, the medicinal liquid sampling and measuring mebendazole content that step D is obtained.
After mebendazole content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made.
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 3 hours, then be warming up to 30 DEG C of dryings 5 hours gradually, whole process vacuum remains on below 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 a kind of mebendazole compositions chewable tablet.
Embodiment 2
Prescription: 1000 amounts
A, take the corn starch of 150g, the purified water adding 900ml stirs, and controls 6.5, is then heated to 72 DEG C, keep 120 minutes, make the gelatinizing corn starch solution of about 5 ~ 15% (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 medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid.
D, take mebendazole 100g (by 1000 calculations), add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 30 minutes.
E, the medicinal liquid sampling and measuring mebendazole content that step D is obtained.
After mebendazole content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made.
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, be cooled to subzero 45 DEG C, keep 2 hours, evacuation, then 0 DEG C is warming up to gradually, keep 2 hours, be cooled to subzero 45 DEG C, keep 2 hours, be warming up to 0 DEG C gradually again, keep 3 hours, then be warming up to 30 DEG C of dryings 5 hours gradually, whole process vacuum remains on below 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 a kind of mebendazole compositions chewable tablet.
Experimental data
The mebendazole compositions chewable tablet that above-described embodiment is obtained carries out following quality research test:
1, hardness, friability, mouthfeel contrast test
The mebendazole compositions chewable tablet prepared according to above-described embodiment and commercially available mebendazole chewable tablet (commercially available) detect friability and hardness by " Chinese Pharmacopoeia " version in 2010 two annex X G inspection techniques, contrast, the results are shown in following table:
Experimental data shows, the more commercially available mebendazole chewable tablet of mebendazole compositions chewable tablet on friability and hardness without significant difference, meet " Chinese Pharmacopoeia " version in 2010 to the requirement of chewable tablet, and mouthfeel is greatly improved, make it the demand more meeting patient.
2, dissolution contrast test
Get mebendazole chewable tablet (commercially available) respectively and mebendazole compositions chewable tablet (is prepared to No. 3 for embodiment 1 for No. 1, prepare to No. 6 for embodiment 2 for No. 4) each 6, respectively according to dissolution method (" Chinese Pharmacopoeia " version in 2010 two annex X C second methods), with the 0.1mol/L hydrochloric acid solution 900ml of 1% sodium lauryl sulphate for dissolution medium, rotating speed is 75r/min, operates in accordance with the law.
Sample respectively at 5min, 15min, 30min, 50min, 80min, 120min, get dissolution fluid appropriate, filter, precision measures subsequent filtrate, as need testing solution.Another precision takes mebendazole reference substance 25mg, puts in 50ml measuring bottle, and add formic acid 10ml and make dissolving, with methanol dilution to scale, shake up, precision measures 5ml, puts in 25ml measuring bottle, is diluted to scale with dissolution medium, shake up, in contrast product solution.According to " Chinese Pharmacopoeia " version in 2010 two annex IV D high performance liquid chromatography, be filler with amino chemically bonded silica; (sodium lauryl sulphate 3.0g and sodium hydroxide 8g is got with acetonitrile-0.15% sodium dodecyl sulfate solution, be dissolved in water and be diluted to 2000ml, add phosphoric acid 20ml, and adjust ph to 2.5) (30:70) be mobile phase, determined wavelength is 254nm.Precision measures need testing solution and each 10 μ l of reference substance solution, respectively injection liquid chromatography, record chromatogram, and by external standard method with the stripping quantity of the every sheet of calculated by peak area, investigate stripping curve, result is as follows.
Mebendazole compositions chewable tablet (No. 1 to No. 3 is embodiment 1, and No. 4 to No. 6 is embodiment 2)
Mebendazole chewable tablet (commercially available)
Respectively with catch cropping Dissolution profiles during average dissolution pair, as Fig. 1.
As stated above to the mebendazole compositions chewable tablet comparative determination of mebendazole compositions chewable tablet of the present invention and commercial reference preparation, the dissolution of mebendazole compositions chewable tablet when 30min (86.3%) of the present invention is suitable with mebendazole chewable tablet (commercially available) dissolution when 120min (85.4%), and the dissolution of mebendazole compositions chewable tablet when 120min (93.8%) of the present invention comparatively mebendazole chewable tablet (commercially available) dissolution when 120min (85.4%) is higher, comparatively mebendazole chewable tablet (commercially available) dissolution time is shorter to show mebendazole compositions chewable tablet of the present invention, dissolution is higher, further show that mebendazole compositions chewable tablet bioavailability of the present invention is better than mebendazole chewable tablet (commercially available).
2, stability study
Sample source: self-control
Sample lot number: 20130901 (embodiments 1), 20130902 (embodiments 2)
Investigation project: character, content, related substance, hardness, dissolution
Investigation method: according to " Chinese Pharmacopoeia " version in 2010 two annex XIX C crude drug and pharmaceutical preparation stability test guideline, investigate the accelerated stability (January, February, March, June) of this product and long-time stability (March, June, JIUYUE, December), result of the test is as following table:
As can be seen from the above table, in acceleration 6 months, all there is not significant change in long-term 12 months, show that this product has good stability in mebendazole compositions chewable tablet indices of the present invention.
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 mebendazole compositions chewable tablet, is characterized in that, is prepared from by following raw material:
2. a preparation method for mebendazole compositions chewable tablet 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 4 ~ 9, be then heated to 72 DEG C, be incubated 120 minutes, make the gelatinizing 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 medicinal liquid and the step B that steps A are obtained obtain mixes, and fully stirs 30 minutes, after medicinal liquid be down to room temperature obtain gelatinizing Semen Maydis-sucrose system medicinal liquid;
D, take mebendazole 100 grams, add 1L gelatinizing Semen Maydis-sucrose system medicinal liquid, stir 25 ~ 35 minutes;
E, the medicinal liquid sampling and measuring mebendazole content that step D is obtained;
After mebendazole content measured by F, medicinal liquid, be sub-packed in drug-containing dish by loading amount by medicinal liquid, each drug-containing dish fills about 1.0ml, then utilizes drug-containing dish lid malcompression state to cover drug-containing dish, and drug-containing dish is the cylindric medicine carrying packaging that plastics or other materials are made;
G, the drug-containing dish that medicinal liquid is housed is put into freeze drying box, 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 below 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 mebendazole compositions chewable tablet.
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111494327A (en) * | 2020-06-23 | 2020-08-07 | 瑞阳制药有限公司 | Preparation method of mebendazole chewable tablet |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111494327A (en) * | 2020-06-23 | 2020-08-07 | 瑞阳制药有限公司 | Preparation method of mebendazole chewable tablet |
| CN111494327B (en) * | 2020-06-23 | 2023-09-05 | 瑞阳制药股份有限公司 | Preparation method of mebendazole chewable tablet |
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Application publication date: 20150325 |