CN108008097A - A kind of method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree - Google Patents
A kind of method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree Download PDFInfo
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- CN108008097A CN108008097A CN201711229745.5A CN201711229745A CN108008097A CN 108008097 A CN108008097 A CN 108008097A CN 201711229745 A CN201711229745 A CN 201711229745A CN 108008097 A CN108008097 A CN 108008097A
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- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/15—Medicinal preparations ; Physical properties thereof, e.g. dissolubility
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Abstract
The invention belongs to Pharmaceutical Analysis technical field, more particularly to a kind of method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree.The present invention provides it is a kind of can between quantitative assessment pharmaceutical preparation dissolution rate similarity degree method, this method grows the projective module of reference preparation stripping curve vector by calculating test sample preparation stripping curve vector, quotient is done with reference preparation stripping curve vector mould length, dissolution projects similar factors P between drawing two kinds of reference preparations, made the difference with P values and 100%, its order of magnitude can be used as two kinds of preparation stripping curve similarity degree judgment criteria of evaluation.A kind of method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree provided by the invention can evaluate the similarity degree of two kinds of preparation stripping curves from quantitative angle, as a result from the influence of final stripping quantity and last sample point.
Description
Technical field
It is more particularly to a kind of using sciagraphy evaluation pharmaceutical preparation dissolution rate phase the invention belongs to Pharmaceutical Analysis technical field
Like the method for degree.
Background technology
The In Vitro Dissolution degrees of data of solid pharmaceutical preparation be a kind of pharmaceutical preparation different cultivars of evaluation, different manufacturers product,
The significant data of quality between different batches.There is different requirement standards to different preparations in pharmacopoeia of each country.In Vitro Dissolution
Certain correlation is presented with vivo biodistribution availability to a certain extent in degree, often can also estimate from its In Vitro Dissolution degrees of data
Count its pharmacokinetics and the characteristic of drug bioavailability.U.S. FDA thinks some medicines to be tried with dissolution in vitro
Test and tested instead of vivo biodistribution availability.Its condition is that dissolution in vitro is related to vivo biodistribution availability：1. indicate dose
Dissolution percentage is related to body absorption percentage.2. dissolution rate and amount and pharmacokinetic parameter tmax, cmax, Ka, AUC
It is related.3. dissolution rate and amount are related to pharmacological action.4. averagely dissolution in vitro is related to average residence time.In Vitro Dissolution
Degree has the characteristics that easy, controllable, accurate, easy repeat compared with being tested with vivo biodistribution availability.Therefore mouths of the FDA in 1999
Similarity estimate is recommended in oral solid bioavailability of drugs and bioequivalence Guide to research and evaluates its dissolution rate, with true
Determine Counterfeit Item and compare the dissolution rate difference of medicine, and assert the similar factors f2 of test drug>50 be equivalent.
The paper of entitled " the statistical evaluation analysis of the dissolution in vitro of solid pharmaceutical preparation " that Xia Jinhui etc. is delivered is public
Open using f2 factorization methods to evaluate similarity degree between the stripping curve of different batches pharmaceutical preparation.Though the method has, calculating is simple,
Without fitted model parameters, the advantages that can directly calculating dissolution data, but final stripping quantity and last sample point
F2 values, and the stripping curve similarity degree between the reflection preparation without standard measure can be significantly affected, and judging result false sun is occurred
Property.
The content of the invention
In order to overcome in the prior art evaluate pharmaceutical preparation between dissolution rate similarity degree method existing for deficiency, the present invention
Provide it is a kind of can between quantitative assessment pharmaceutical preparation dissolution rate similarity degree method, this method is by calculating test sample system
Agent stripping curve vector grows the projective module of reference preparation stripping curve vector, and business is with reference preparation stripping curve vector mould length
Value, draws dissolution projection similar factors P between two kinds of reference preparations, is made the difference with P values and 100%, its order of magnitude can conduct
Evaluate two kinds of preparation stripping curve similarity degree judgment criteria.Absolute value is smaller, then shows the similar journey of two kinds of preparation stripping curves
Degree is higher.
The present invention provides a kind of method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, including following step
Suddenly：
The stripping curve data preparation of test sample preparation into test sample stripping curve vector, is shown in formula 1 by S1, every in vector
Dimension represents each data point on the stripping curve of test sample preparation,
The stripping curve data preparation of reference preparation into reference preparation stripping curve vector, is shown in formula 2 by S2, every in vector
Dimension represents each data point on the stripping curve of reference preparation,
S3 projects similar factors P by the dissolution that formula 3 calculates between the two,
S4 calculates the absolute difference of P and 100%, sees formula 4,
| p-100% | formula 4.
Wherein, | p-100% | judge the similarity degree between two kinds of stripping curves, absolute value is smaller, then show both it
Between it is more similar, conversely, absolute value is bigger, then show more dissimilar between the two.
Compared with prior art, the method provided by the invention using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree
Beneficial effect includes：The similarity degree of two kinds of preparation stripping curves can be evaluated from quantitative angle, as a result from final dissolution
The influence of amount and last sample point.
Brief description of the drawings
Fig. 1 is principle of the invention ideograph.
Fig. 2 is the present invention and f2 factorization method result of calculation comparison diagrams.
Embodiment
Embodiment one, a kind of method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree
The stripping curve data preparation of test sample preparation into test sample stripping curve vector, is shown in formula 1 by S1, every in vector
Dimension represents each data point on the stripping curve of test sample preparation,
The stripping curve data preparation of reference preparation into reference preparation stripping curve vector, is shown in formula 2 by S2, every in vector
Dimension represents each data point on the stripping curve of reference preparation,
S3 projects similar factors P by the dissolution that formula 3 calculates between the two,
S4 calculates the absolute difference of P and 100%, sees formula 4, judges the similarity degree between two kinds of stripping curves,
| p-100% | formula 4.
Embodiment two, the present invention and f2 factorization methods result of calculation contrast
There is provided respectively with f2 factorization methods with the embodiment of the present invention one similar using sciagraphy evaluation pharmaceutical preparation dissolution rate
The method of degree is evaluated, for convenience of description problem, and the data value in this example is assumed average, wherein, test sample 1 to 3
It is different difference lies in last point, for observing influence of the last stripping quantity to two methods result of calculation.Most volume data and meter
Calculation the results are shown in Table 1 (wherein the unit at time point is h), and Fig. 2 is shown in the stripping curve contrast of test sample and reference.
The data value and two methods result of calculation of 1 reference of table and four kinds of test sample stripping curve different time points
As shown in Table 1, when last stripping quantity is relatively low, f2 factor pair difference stripping curves discrimination declines, in table 1,
Test sample 1 to 3, with the increase of last stripping quantity, f2 values decline therewith, and fall is only 5%, and p value change is very bright
It is aobvious, fall 10%.In addition, test sample 4 is substantially dissimilar with reference preparation, but f2 values are really more than 50, false positive occur,
And p value is 175.3%, hence it is evident that higher than other batches.
Embodiment three, the discussion to limit value of the present invention
Entitled " the statistical evaluation analysis of the dissolution in vitro of solid pharmaceutical preparation " that this example application Xia Jinhui etc. is delivered
Paper in test data, come inquire into projection quantitative similarity method limit value requirement.Table 2 is test data and calculating in document
End value.
Data and the result of calculation with two methods in 2 document of table
| 1 | 2 | 3 | 4 | 6 | 8 | 12 | f | P | |
| Reference | 25.40% | 42.20% | 65.30% | 78.30% | 81.30% | 93.40% | 93.40% | 100.0 | 100.00% |
| Test sample 1 | 15.70% | 30.90% | 53.50% | 64.90% | 72.10% | 80.60% | 87.70% | 49.5 | 115.8% |
| Test sample 2 | 30.10% | 46.70% | 68.20% | 81.20% | 85.10% | 90.50% | 99.50% | 69.1 | 97.9% |
| Test sample 3 | 27.60% | 43.10% | 64.20% | 81.20% | 82.90% | 90.60% | 97.10% | 81.6 | 98.2% |
As shown in Table 2, when f values are more than 50, p value is all sufficiently close to 100%, in test sample 1, f 49.5, and p value is
115.8%, it is possible to consider that limit value is set between 85.0%~115.0%, both when the stripping curve of two kinds of preparations projects phase
Fall like angle value between 85.0%~115.0%, it is believed that both stripping curves are similar.
In conclusion assay method provided by the invention is realized from quantitative angle two kinds of preparation stripping curves of evaluation
Similarity degree, as a result from the influence of final stripping quantity and last sample point, and calculating process is simple, easy-to-understand, can use
In different preparation medicine stripping curve similarity evaluations.
Above content is that a further detailed description of the present invention in conjunction with specific preferred embodiments, it is impossible to is assert
The specific implementation of the present invention is confined to these explanations.For general technical staff of the technical field of the invention,
On the premise of not departing from present inventive concept, some simple deduction or replace can also be made, should all be considered as belonging to the present invention's
Protection domain.
Claims (6)
- A kind of 1. method using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, it is characterised in that：Comprise the following steps：The stripping curve data preparation of test sample preparation into test sample stripping curve vector, is shown in formula 1 by S1, every one-dimensional in vector Degree represents each data point on the stripping curve of test sample preparation,The stripping curve data preparation of reference preparation into reference preparation stripping curve vector, is shown in formula 2 by S2, every one-dimensional in vector Degree represents each data point on the stripping curve of reference preparation,S3 projects similar factors P by the dissolution that formula 3 calculates between the two,S4 calculates the absolute difference of P and 100%, sees formula 4, judges the similarity degree between two kinds of stripping curves,| p-100% | formula 4.
- 2. the method according to claim 1 using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, its feature exists In：Stripping curve in the step S1 includes the drug-eluting curve of ordinary preparation and the insoluble drug release song of sustained-release preparation Line.
- 3. the method according to claim 1 using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, its feature exists In：Preparation in the step S1 and step S2 is solid pharmaceutical preparation, liquid preparation or special preparation.
- 4. the method according to claim 3 using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, its feature exists In,The solid pharmaceutical preparation is powder, granule, tablet, capsule, pill or film.
- 5. the method according to claim 3 using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, its feature exists In：The liquid preparation is injection, soft capsule, ointment, suppository or aerosol.
- 6. the method according to claim 3 using sciagraphy evaluation pharmaceutical preparation dissolution rate similarity degree, its feature exists In：The special preparation is microcapsules, microspheres agent or Liposomal agents.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101271092A (en) * | 2007-03-19 | 2008-09-24 | 沈阳药科大学 | Chinese medicine color spectrum fingerprint pattern characteristic digitalization and full-qualitative full-quantitative quality control method |
| CN104330495A (en) * | 2014-11-04 | 2015-02-04 | 天津医药集团津康制药有限公司 | Method for determining similarity of dissolution curves of cefdinir dry suspension |
| CN106645481A (en) * | 2016-12-23 | 2017-05-10 | 东药集团沈阳施德药业有限公司 | Method for testing dissolution curve of quick release dosage form drug-amoxicillin and clavulanate potassium dispersible tablet |
-
2017
- 2017-11-29 CN CN201711229745.5A patent/CN108008097A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101271092A (en) * | 2007-03-19 | 2008-09-24 | 沈阳药科大学 | Chinese medicine color spectrum fingerprint pattern characteristic digitalization and full-qualitative full-quantitative quality control method |
| CN104330495A (en) * | 2014-11-04 | 2015-02-04 | 天津医药集团津康制药有限公司 | Method for determining similarity of dissolution curves of cefdinir dry suspension |
| CN106645481A (en) * | 2016-12-23 | 2017-05-10 | 东药集团沈阳施德药业有限公司 | Method for testing dissolution curve of quick release dosage form drug-amoxicillin and clavulanate potassium dispersible tablet |
Non-Patent Citations (4)
| Title |
|---|
| 刘清飞 等: "缓控释制剂释放度相似性评价方法的应用进展", 《中国药学杂志》 * |
| 夏锦辉 等: "固体药物制剂的体外溶出度的统计学评价分析", 《中国药学杂志》 * |
| 王昕 等: "溶出曲线相似性的两种评价方法", 《天津药学》 * |
| 陈贤春 等: "关于溶出曲线比较和评价方法", 《中国医院药学杂志》 * |
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