CN1865998A - Apparatus and method for in vitro disintegration time limit determination of orally disintegrating tablet - Google Patents
Apparatus and method for in vitro disintegration time limit determination of orally disintegrating tablet Download PDFInfo
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- CN1865998A CN1865998A CN 200510070950 CN200510070950A CN1865998A CN 1865998 A CN1865998 A CN 1865998A CN 200510070950 CN200510070950 CN 200510070950 CN 200510070950 A CN200510070950 A CN 200510070950A CN 1865998 A CN1865998 A CN 1865998A
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Abstract
The related test device to test the disintegration time in vitro of oral disintegration material can simulate mouth physiological environment well, and can ensure the time within one minute.
Description
Technical field
The present invention relates to a kind of experimental provision and method, be used to measure the external disintegration time limited of oral disnitegration tablet, can simulate the physiological environment in oral cavity preferably, set up the external disintegration time mensuration method that meets this product galenic pharmacy feature, and guarantee that disintegration time limited is in 1 minute.
Background technology
Oral disnitegration tablet (Orally disintegrating tablets is called for short oral disintegrating tablet below) preparation need not be obeyed water in the oral cavity, also need not to chew, and places on the tongue, after rapid dissolving of chance saliva or the disintegration, borrows swallowing act to go into the stomach onset.This formulation provides a kind of new instructions of taking, makes things convenient for part crowd medication, as the patient's medication under old man, children, dysphagia or the inconvenient environment of fetching water.There are some years in oral disintegrating tablet on the market abroad, technology of preparing mainly contains desivac, compression moulding, direct compression process, wet method pressed disc method and wet granule compression tablet method, but still not having unified standard method at present in the world comes the speed of quantitative this series products of investigation to collapse characteristic, multiple different technologies has caused the difference of product property, make the hardness of product less as freeze drying technology, friability is higher; Wet granulation technique makes the hardness of product bigger, and the Orally disintegrating time is longer than the freeze drying technology product.Some ordinary tablet, especially some dispersing tablet also can reach the requirement of oral disintegrating tablet simultaneously, and all these factors have all limited and adopted unified standard to investigate the possibility that its external speed collapses characteristic.
The implication of " Orally disintegrating " should be that intra-oral disintegration on a kind of subjective significance The is below certain particle size, in the hope of there not being the sensation of grit or solid, objectively and do not require the absolute or all dissolvings of medicine.Some gross reference mark of disintegration time mensuration are: disintegration time in one minute, the first-selected water of medium, consumption should be less than 2ml, temperature is preferably 37 ℃, adopts static method, and granularity control project (should less than the 0.71mm of dispersing tablet) should be arranged.Present external disintegration experiment: all adopt the oar method to measure as the Japan and the U.S., but owing to tablet contacts with volume water, characteristic that can't fine simulation oral disnitegration tablet; Other have method put on the microslide and scrape in a tablet, a spot of water, the 1min and sieve as adopting (＜0.71mm), this method is suitable for freeze-drying prods, because of the sheet of this series products heavy generally on the low side, density is also little, when being used for bigger other technical products of hardness, solution thickness, the dynamic process that scrapes may make sheet in the heart do not collapse part disintegration or dissolving, thereby can't accurately judge disintegration time limited; And detection method disintegration time limited of the routine in the pharmacopeia appendix can't be distinguished oral disintegrating tablet and ordinary tablet, and lacks the inside and outside correlativity.
In view of above all present situations, we have designed a covering device in the laboratory, and purpose is to set up the stronger disintegration inspection technique of specificity, is used for investigating oral disintegrating tablet and collapses characteristic in external speed.
Description of drawings
Fig. 1 is external disintegration time limited of a detection method installation drawing
Experiment at normal temperatures, wherein 1 is rubber hose (the about 3mm of internal diameter), and 2 is constant flow pump, and 3 is cillin bottle (capacity 6ml), and 4 and 6 is glass funnel, 5 is the funnel trough (bottom is put tested) that 40 eye mesh screens are converted into.H is the distance between the foot of funnel 6 and tested, requires the cell body that h highly locates in the funnel trough 5 long-pending less than 2ml.Fill the purified water of 2ml in the cillin bottle, be full of purified water (being about 5ml) in the rubber hose, an end places the cillin bottle bottom, and the other end places the foot of funnel 6.This device feature 1 internal diameter can be 2-5mm, and parts 2 can be other current velocity controller, and parts 6 can be other any device that contains distance between water pipe and the funnel trough that is used for fixing.
Fig. 2 is t disintegration time limited (sec) of six kinds of self-control oral disintegrating tablets and the relation curve of constant flow pump flow velocity index
The technical measures that carry out an invention
1. the actual conditions of this experiment
Adopt the flow velocity v of the Shanghai Hu Xi analytical instrument BT-100 of factory type constant flow pump control water, the volume that 1cm highly locates in the funnel trough 5 is about 1-2ml, therefore fixing h=1cm.
2. the purpose of experimental design and parameter setting foundation
But the physiological environment in this experimental provision best simulation oral cavity, tested is in static relatively, as to be fixed on funnel trough 5 bottom, water dropwise touches its surface, the continuous circulating analog of water the behavior of saliva in the oral cavity, relying on the trace of water to flow and taking away the sheet surface has been 40 eye mesh screens of 0.45mm by the part of water disintegration or dissolving and by the aperture, has controlled the granule size after the disintegration.Because the interaction force between water and screen cloth, the part water droplet possibly can't dropwise see through screen cloth, the water yield is rich long-pending around causing tested, the maximum height value that water can arrive in the funnel trough 5 is h, when arriving the h height, water company in water and the groove in the flexible pipe, the water that powerful action of gravity meeting is highly located h all falls, the circulation that guarantees water is continuous, uninterrupted, and the water yield around tested is less than 2ml all the time in the process.
3. disintegration time mensuration method, it comprises the following steps
First step: be ready to disintegration time mensuration device as claimed in claim 1;
Second step: tablet to be determined is placed on the funnel trough, and funnel trough places on the glass funnel, and insert in the cillin bottle lower end of fixing glass funnel;
Third step: fill in the cillin bottle low amounts of water (≤2ml), an end that contains water pipe places the cillin bottle bottom, the other end places the funnel trough top, should make its cell body apart from groove Chinese medicine tablet height place long-pending less than 2ml;
The 4th step: control contains the flow velocity of water in the water pipe, picks up counting with first moment that contacts tested of dripping, and stops timing during all by screen cloth to tablet, and the time that stopwatch shows is the disintegration time of slice, thin piece.
4. the standard of disintegration time limited
During sheet weight≤300mg, when the constant flow pump flow is about 16g/min (being that the flow velocity index is 1.2), disintegration time limited＜1min; When sheet weighs between 300-600mg, when the constant flow pump flow is about 43g/min (being that the flow velocity index is 2.8), disintegration time limited＜1min; During sheet weight＞600mg, must investigate separately.
Embodiment
The present invention is described in further detail below in conjunction with embodiment.
Specify the present invention in conjunction with the embodiments, but be not limited to following embodiment.
Respectively with oral disintegrating tablet, dispersing tablet and ordinary tablet as tested, its sheet is heavy, hardness, Orally disintegrating time limit, see Table 1 by 2000 editions pharmacopeia appendix XA check results disintegration time limited; By measuring the flow size in the special time under the constant flow pump different in flow rate index, obtain and the corresponding flow size of index (g/min), investigation constant flow pump different in flow rate v the results are shown in Table 2 to the influence in three kinds of disintegration of tablet time limits.Wherein t disintegration time limited (sec) of 6 kinds of self-control oral disintegrating tablets sees Fig. 2 with the relation curve of flow velocity v.Compared the disintegration time mensuration result of normal temperature and 37 ℃ of following 6 kinds of oral disintegrating tablets, seen Table 3, found basic indifference, so simplify experimental provision, need not heat temperature controlling instruments, normal temperature test down gets final product.
Every conventional parameter value (n=6) of three kinds of tablets of table 1
| Parameter | Sheet heavy (mg) | Sheet footpath (mm), the sheet type | Hardness (N) | Mouth collapses the time limit (sec) | Disintegration time limited (sec) among the ChP appendix XA |
| Oral disintegrating tablet 1 oral disintegrating tablet 2 oral disintegrating tablets 3 oral disintegrating tablets 4 oral disintegrating tablets 5 oral disintegrating tablets 6 comparison film dispersing tablet ordinary tablets 1 ordinary tablet 2 ordinary tablets 3 ordinary tablets 4 | 150 150 150 500 600 600 620 174 150 150 150 150 | 7, disk 7, disk 7, disk 11, disk 7 * 17 capsule shape sheets 7 * 17 capsule shape sheets 13, disk 8, disk 7, disk 7, disk 7, disk 7, disk | 33 37 25 35 169 131 7 23 105 96 100 100 | 33 40 56 46 54 55 32 91 63 65 ＞300 ＞600 | 33 29 19 46 33 32 - 27 29 64 165 349 |
Annotate: oral disintegrating tablet 1 is a risperidone orally disintegrating tablets, oral disintegrating tablet 2 is the Zaleplon oral-cavity disintegrated tablet, oral disintegrating tablet 3 is an oral loratadine disintegrating tablet, oral disintegrating tablet 4 is the Fluoxetine hydrochloride oral disnitegration tablet, oral disintegrating tablet 5 is a fexofenadine hydrochloride orally disintegrating tablet, oral disintegrating tablet 6 is the racecadotril oral disnitegration tablet, and comparison film is external oral disnitegration tablet (trade name Triaminic_Softchews
TM); Dispersing tablet is the racecadotril dispersing tablet; Ordinary tablet 1-4 is blank, surveys (down together) by 2000 editions different requirement preparation disintegration time limited "-" expressions of pharmacopeia appendix XA method
The disintegration time limited of the following three kinds of tablets of table 2 different in flow rate (sec, n=6)
| Constant flow pump flow velocity index | Flow velocity v (g/min) | Oral disintegrating tablet 1 | Oral disintegrating tablet 2 | Oral disintegrating tablet 3 | Oral disintegrating tablet 4 | Oral disintegrating tablet 5 | Oral disintegrating tablet 6 | Comparison film | Dispersing tablet | Ordinary tablet 1 |
| 0.6 0.8 1.0 1.2 1.4 1.6 1.8 2.0 2.2 2.4 2.6 2.8 3.0 | 5.4 8.8 12.3 16.0 18.4 22.1 25.6 29.0 32.5 36.3 39.5 43.0 46.0 | 87 59 46 42 - - - 31 - - - 20 - | 101 65 49 44 - - - 36 - - - 18 - | 114 61 43 37 - - - 32 - - - 21 - | 357 225 147 107 112 86 73 65 47 44 49 48 41 | 426 248 208 180 129 107 92 90 78 77 70 50 53 | 330 243 216 156 115 105 102 78 68 63 60 58 50 | 165 - - 57 - - - 43 - - - - - | ＞300 261 204 155 150 158 106 90 - - - 50 - | ＞300 ＞300 ＞300 ＞300 190 170 150 135 - - - 85 - |
Annotate: experiment is a limit time with 300sec, and constant flow pump flow velocity index is 0.8,1.0,1.2 o'clock, and dispersing tablet also leaves 2-3 fritter residue on screen cloth; Index is 0.6 o'clock, and dispersing tablet shape on screen cloth has one deck binding; When index was 0.6-1.2, ordinary tablet 1 shape on screen cloth had one deck binding
The disintegration time limited of oral disintegrating tablet under table 3 different temperatures (sec, n=6)
| Oral disintegrating tablet 1 | Oral disintegrating tablet 2 | Oral disintegrating tablet 3 | Oral disintegrating tablet 4 | Oral disintegrating tablet 5 | Oral disintegrating tablet 6 | |
| 20 ℃ of normal temperature | 42 | 44 | 37 | 48 | 50 | 58 |
| 37℃ | 42 | 43 | 38 | 46 | 50 | 57 |
As can be seen from Table 2, sheet is heavily to there being certain influence disintegration time limited, and especially influence is bigger when hanging down flow velocity.Selecting to detect the fastest ordinary tablet 1 disintegration time limited that obtains by 2000 editions pharmacopeia appendix XA in four kinds of ordinary tablets contrasts, though the sheet weight average of dispersing tablet and ordinary tablet is less than 300mg, but the disintegration time limited of six kinds of oral disintegrating tablets is almost all less than dispersing tablet and ordinary tablet under identical flow velocity, self-control the most large stretch of of oral disintegrating tablet heavily is 600mg in the experiment, with 300mg is separation, when sheet heavily is lower than it (oral disintegrating tablet 1-3), the constant flow pump index is 1.2 can distinguish oral disintegrating tablet, dispersing tablet and ordinary tablet preferably; When sheet heavily is higher than 300mg (oral disintegrating tablet 4-6), the constant flow pump index is 2.8 can make disintegration time limited less than 1min, and ordinary tablet disintegration time limited of the heavy 150mg of sheet this moment is still greater than 1min, so can infer that sheet heavily is higher than the ordinary tablet of 300mg disintegration time limited can be longer, simultaneously value disintegration time limited under the dispersing tablet different in flow rate of 174mg also can release the dispersing tablet that sheet heavily is higher than 300mg disintegration time limited can be greater than 1min.As can be seen from Figure 2, after flow velocity increases to certain value, be subjected to the disintegration time limited of oral disintegrating tablet the influence of flow velocity very little.
Consider of the influence of factors such as different technologies, sheet weight, shape, hardness to oral disintegrating tablet, so tentative standard is: during sheet weight≤300mg, when the constant flow pump flow is about 16g/min (being that the flow velocity index is 1.2), disintegration time limited＜1min; When sheet weighs between 300-600mg, when the constant flow pump flow is about 43g/min (being that the flow velocity index is 2.8), disintegration time limited＜1mim; During sheet weight＞600mg, must investigate separately.
Claims (7)
1. experimental provision that is used to measure the external disintegration time limited of oral disnitegration tablet, what it is characterized in that this device comprises an adjustable flow velocity contains water pipe, at least one glass funnel, funnel trough, the cillin bottle that screen cloth is converted into.
2. the assay method of a specificity is stronger oral disnitegration tablet external disintegration time limited is characterized in that it comprises the following steps: first step: be ready to disintegration time mensuration device as claimed in claim 1;
Second step: tablet to be determined is placed on the funnel trough, and funnel trough places on the glass funnel, and insert in the cillin bottle lower end of fixing glass funnel;
Third step: fill in the cillin bottle low amounts of water (≤2ml), an end that contains water pipe places the cillin bottle bottom, the other end places the funnel trough top, should make its cell body apart from groove Chinese medicine tablet height place long-pending less than 2ml;
The 4th step: control contains the flow velocity of water in the water pipe, picks up counting with first moment that contacts tested of dripping, and stops timing during all by screen cloth to tablet, and the time that stopwatch shows is the disintegration time of slice, thin piece.
3. the external disintegration time mensuration device of oral disnitegration tablet as claimed in claim 1 contains that adjustable flow velocity parts are constant flow pump in the water pipe.
4. the external disintegration time mensuration device of oral disnitegration tablet as claimed in claim 1, moisture bore is 2-5mm, preferred moisture bore is 3mm.
5. the external disintegration time mensuration device of oral disnitegration tablet as claimed in claim 1, the aperture of screen cloth should be less than 0.71mm in the funnel trough, preferred aperture 0.45mm.
6. the external disintegration time mensuration device of oral disnitegration tablet as claimed in claim 1 can contain one again and be used for fixing glass funnel or other any stationary installation that contains distance between water pipe and the funnel trough.
7. adopt the described assay method of claim 2, the standard of disintegration time limited can be decided to be: when tested weight≤300mg, contain when flow is about 16g/min in the water pipe disintegration time limited＜1min; When sheet weighs between 300-600mg, contain when flow is about 43g/min in the water pipe disintegration time limited＜1min; During sheet weight＞600mg, must investigate separately.
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| CN 200510070950 CN1865998A (en) | 2005-05-19 | 2005-05-19 | Apparatus and method for in vitro disintegration time limit determination of orally disintegrating tablet |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104422756A (en) * | 2013-09-09 | 2015-03-18 | 北京量子高科制药科技有限公司 | Disintegration time limit determination device for rapid disintegration preparation |
| CN104807726A (en) * | 2014-01-23 | 2015-07-29 | 成都中医药大学附属医院 | Detection method for dipping dispersion time limit of pressed traditional Chinese medicine decoction pieces |
| AU2015299033B2 (en) * | 2014-08-06 | 2020-08-13 | Hexal Ag | Method and device for determining the disintegration time of film-shaped pharmaceutical dosage forms |
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2005
- 2005-05-19 CN CN 200510070950 patent/CN1865998A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104422756A (en) * | 2013-09-09 | 2015-03-18 | 北京量子高科制药科技有限公司 | Disintegration time limit determination device for rapid disintegration preparation |
| CN104807726A (en) * | 2014-01-23 | 2015-07-29 | 成都中医药大学附属医院 | Detection method for dipping dispersion time limit of pressed traditional Chinese medicine decoction pieces |
| CN104807726B (en) * | 2014-01-23 | 2018-03-02 | 成都中医药大学附属医院 | Suppress the detection method that prepared slices of Chinese crude drugs leaching dissipates the time limit |
| AU2015299033B2 (en) * | 2014-08-06 | 2020-08-13 | Hexal Ag | Method and device for determining the disintegration time of film-shaped pharmaceutical dosage forms |
| AU2015299033B8 (en) * | 2014-08-06 | 2021-01-28 | Hexal Ag | Method and device for determining the disintegration time of film-shaped pharmaceutical dosage forms |
| AU2015299033A8 (en) * | 2014-08-06 | 2021-01-28 | Hexal Ag | Method and device for determining the disintegration time of film-shaped pharmaceutical dosage forms |
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