CN101288648A - Easy-to-administrate oxiracetam granular formulation and preparation method - Google Patents
Easy-to-administrate oxiracetam granular formulation and preparation method Download PDFInfo
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- CN101288648A CN101288648A CNA2008100550716A CN200810055071A CN101288648A CN 101288648 A CN101288648 A CN 101288648A CN A2008100550716 A CNA2008100550716 A CN A2008100550716A CN 200810055071 A CN200810055071 A CN 200810055071A CN 101288648 A CN101288648 A CN 101288648A
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Abstract
The invention relates to an easy-to-take oxiracetam particle preparation and a preparation method, which pertains to the technical field of medicine and is used for solving the problems of stability and inconvenient administration. The preparation comprises oxiracetam nano-particles and pharmaceutical excipients, the mix ratio by weight units of the main drug oxiracetam and the pharmaceutical excipients after the improvement is 1.195: 1, the pharmaceutical excipients are composed of mannitol, asipatan, sunset yellow and powdered fragrances, and the mix ratio by weight units of the ingredients of the pharmaceutical excipients is 440: 5: 0.2: 1. The selection of the excipients in a formula of the preparation of the invention, the mix ratio of the main drug and the excipients and the mix ratio relationship among the excipients are accurate and reasonable, thus being characterized by easy water solubility, better smell and convenient administration, more particularly, the administration by the patients with difficult swallow of other oral preparations or the patients with senile dementia who are not cooperative for injection drug delivery. The preparation has stable quality and easy preservation, thus being applicable to the patients for long-term administration. The oxiracetam particle preparation of the invention has simple preparation process, lower production cost and easy implementation.
Description
Technical field
The present invention relates to a kind of pharmaceutical preparation and preparation method, particularly a kind of oxiracetam granular preparation of being convenient to take that is used for the treatment of central nervous system disease belongs to medical technical field.
Background technology
Oxiracetam (oxiracetam) is a kind of synthetic hydroxy-amino-butyric acid (GABOB) cyclic derivatives; act on the central nervous system; mainly be distributed in cerebral cortex, Hippocampus, functional rehabilitation, the memory that improves the disturbance of intelligence patient and the learning functionality of activation, protection or promotion neurocyte arranged.The oxiracetam indication is the commonly encountered diseases among the old people, mainly show as the energy poor concentration, the forfeiture computing capability, the language performance difficulty, the severe patient loss of memory be can't take care of oneself, and can not control emotion etc., the neurologic impairment that brain injury is caused, intelligence infringement syndrome, amnestic syndrome, personality changes, disturbance of consciousness, daily life or social function are impaired etc. definite curative effect.The suitable crowd of oxiracetam mostly is dementia and amentia patient, and symptoms such as cough and choke often easily take place with dysphagia, when feed such patient, and this type of patient of order needs long-term prescription.In clinical use often relevant for taking the feedback information that the cough and choke incident takes place behind the oxiracetam capsule, therefore, the dosage form design of oxiracetam has very important significance with the improvement tool, have only a kind of dosage form of capsule and present stage is used for clinical oxiracetam oral formulations, can't satisfy most patients' clinical demand.In addition, for the medicine that this class of oxiracetam need be taken for a long time, how making it at the medium-term and long-term steady quality that keeps of natural environment, also is the major issue that needs concern and solve.
Summary of the invention
Technical problem to be solved by this invention is that the defective that overcomes prior art provides a kind of oxiracetam granular preparation and preparation method that can prevent effectively that the generation of cough and choke incident, steady quality, production cost are low, be convenient to take.
The alleged problem of the present invention is solved by following technical scheme:
A kind of oxiracetam granular preparation of being convenient to take, it comprises oxiracetam principal agent and pharmaceutic adjuvant, its special feature is: described principal agent oxiracetam and pharmaceutic adjuvant unit are by weight counted 1.195: 1, described pharmaceutic adjuvant is made up of mannitol, Aspartane, sunset yellow and powdered flavor, and the above-mentioned pharmaceutic adjuvant ratio of unit meter by weight is 440: 5: 0.2: 1.
The above-mentioned oxiracetam granular preparation of being convenient to take adds weight concentration and is 15% PVP aqueous solution in the described granular preparation, addition so that the material moistening be as the criterion.
The above-mentioned oxiracetam granular preparation of being convenient to take, it comprises oxiracetam principal agent and pharmaceutic adjuvant, described principal agent and pharmaceutic adjuvant unit are by weight counted:
Oxiracetam 200～1600;
Mannitol 165～1320;
Aspartame 1.875～15;
Sunset yellow 0.075～0.6;
Powdered flavor 0.375～3;
The 15%PVP aqueous solution is an amount of.
The above-mentioned oxiracetam granular preparation of being convenient to take, described each components contents unit is by weight counted:
Oxiracetam 800;
Mannitol 660;
Aspartame 7.5;
Sunset yellow 0.3;
Powdered flavor 1.5;
The 15%PVP aqueous solution is an amount of.
The preparation method of the above-mentioned oxiracetam granular preparation of being convenient to take, it carries out as follows:
A, cross behind 80 mesh sieves principal agent oxiracetam standby;
B, take by weighing the sunset yellow of formula ratio, being dissolved in weight concentration is as binding agent in the 15%PVP aqueous solution;
C, the mannitol that takes by weighing formula ratio, Aspartane and the oxiracetam mix homogeneously of crossing through a step process add the above-mentioned binding agent system soft material that makes, and granulate with 20 mesh sieves, behind the airpillow-dry, make dried granule with 18 mesh sieve granulate;
D, the powdered flavor that takes by weighing formula ratio and above-mentioned dried granule mixing.
The present invention is directed to existing oxiracetam preparation dosage form single, be not suitable for the problem that patient colony takes and improve, its main feature is as follows: 1. the proportion relation between the proportioning of the selection of adjuvant, principal agent and adjuvant and adjuvant and the adjuvant is accurately reasonable in the pharmaceutical formulation, oxiracetam granular preparation according to this proportioning preparation is soluble in water, smell distinguish the flavor of better, taking convenience, especially for swallowing other peroral dosage forms difficulty or mismatching the patients of senile dementia of drug administration by injection, this dosage form can improve patient's compliance, be easy to administration, and can reach ideal safety; 2. the granular preparation steady quality is easy to preserve, and is applicable to that the patient takes for a long time.Result of the test shows: placed under 60 ℃ of high temperature, illumination 4500 ± 500lx, high humidity 92.5% and high humidity 75% condition 10 days, except that high humidity environment makes product slightly the moisture absorption, other mass parameter has no significant change.By the simulation commercially available back sample has been carried out accelerated test and long term test investigation, results sample is investigated through 6 months accelerated test and 6 months long-time stability, and every investigation project is all in the scope of quality standard regulation; 3. preparation technology is easy, and production cost is lower, is convenient to implement.
The specific embodiment
The present invention mostly is dementia and amentia patient according to the suitable crowd of oxiracetam, and the problem that such patient often with dysphagia, when feed symptoms such as cough and choke takes place easily designed a kind ofly can avoid effectively that cough and choke, patient's compliance are strong, steady quality, oxiracetam granular preparation that production cost is low.As everyone knows, the proportioning in the preparation prescription between the proportioning of the selection of adjuvant, principal agent and adjuvant and adjuvant and the adjuvant directly affects the quality of preparation, wants to solve the practical problem in the production, must find out the technical scheme that is fit to practical application.The present invention is by the mass data of collection and treatment in the actual production process, through repetition test, constantly getting rid of predetermined scheme, re-establishing selection and the best proportioning between each adjuvant of determining principal agent and adjuvant, adjuvant in new departure process is 1.195: 1, and wherein pharmaceutic adjuvant is mainly by mannitol: Aspartane: sunset yellow: powdered flavor unit proportioning is by weight counted 440: 5: 0.2: 1 forms.Adopt this proportioning, can make oxiracetam granular preparation preparation technology of the present invention easy, cost is lower, steady quality, soluble in water, smell distinguish the flavor of better, taking convenience, especially for swallowing other peroral dosage forms difficulty or mismatching the patients of senile dementia of drug administration by injection, this dosage form can improve patient's compliance, is easy to administration, and can reach ideal safety.
Oxiracetam granular preparation of the present invention has good quality stability, and the stability test result who carries out according to " chemicals stability study technological guidance principle " related request is as follows:
1. influence factor's test: get the oxiracetam granular preparation, remove unlap, put illumination 4500 ± 500lx, 60 ℃ of high temperature, placed 10 days under the condition of high humidity RH75 ± 5%, high humidity RH92.5 ± 2.5%, respectively at the 5th day and sampling in the 10th day, detect by above-mentioned investigation project, test and the results are shown in Table 1.
Table 1 influence factor result of the test
The result shows, the oxiracetam granule is slightly moisture absorption weightening finish under high humidity 92.5% and 75% condition, increased weight 1.4% and 0.9% in 5 days respectively, the moisture absorption weightening finish that increased this product under 2.1% and 1.5%, two condition in 10 days does not respectively all surpass the weightening finish 5.0% of stipulating in the pharmaceutical preparation stability guideline.Placed under 60 ℃ of high temperature, illumination 4500 ± 500lx, high humidity 92.5% and high humidity 75% condition condition 10 days, except that high humidity environment makes product slightly the moisture absorption, other mass parameter has no significant change, and is all up to specification.Test the investigation result according to the influence factor, the oxiracetam granule should be preserved at the hermetically drying place, can adopt the compound membrane bag packing.
2. accelerated tests: get three lot number oxiracetam granular preparation test samples, under the composite film packaging condition, placed 6 months in 40 ℃ ± 2 ℃ of temperature, relative humidity 75% ± 5%, respectively at 0,1,2,3,6 sampling at the end of month, detect by aforementioned stable investigation project, result of the test sees Table 2.
Table 2 accelerated test result
By data in the table 2 as seen, three batches of test samples are investigated through six months accelerated test, and every detection index all in the scope of quality standard regulation, illustrates oxiracetam granular preparation steady quality.
3. long-term stable experiment
Get three lot number oxiracetam granular preparation test samples, under the compound membrane bag terms of packing, place in 25 ℃ ± 2 ℃ of temperature, relative humidity 60% ± 10%, respectively at 0,3,6,9,12,18,24 sampling at the end of month, detect by the study on the stability project, result of the test sees Table 3.
Table 3 long-term stable experiment result
By data in the table 3 as seen, the three batches of test samples are investigated through 6 months long term test, and every detection index has no significant change and all in the scope that quality standard is stipulated, oxiracetam granular preparation steady quality of the present invention is described.
Below provide several specific embodiments:
Embodiment 1.
The oxiracetam granular preparation, each components contents is counted by gram in 1000 bags:
Oxiracetam 200g
Mannitol 165g
Aspartame 1.875g
Sunset yellow 0.075g
Powdered flavor 0.375g
The 15%PVP aqueous solution is an amount of
Embodiment 2.
The oxiracetam granular preparation, each components contents is counted by gram in 1000 bags:
Oxiracetam 400g
Mannitol 330g
Aspartame 3.75g
Sunset yellow 0.15g
Powdered flavor 0.75g
The 15%PVP aqueous solution is an amount of
Embodiment 3.
The oxiracetam granular preparation, each components contents is counted by gram in 1000 bags:
Oxiracetam 800g
Mannitol 660g
Aspartame 7.5g
Sunset yellow 0.3g
Powdered flavor 1.5g
The 15%PVP aqueous solution is an amount of
Embodiment 4
The oxiracetam granular preparation, each components contents is counted by gram in 1000 bags:
Oxiracetam 1200g
Mannitol 990g
Aspartame 11.25g
Sunset yellow 0.45g
Powdered flavor 2.25g
The 15%PVP aqueous solution is an amount of
Embodiment 5.
The oxiracetam granular preparation, each components contents is counted by gram in 1000 bags:
Oxiracetam 1600g
Mannitol 1320g
Aspartame 15g
Sunset yellow 0.6g
Powdered flavor 3g
The 15%PVP aqueous solution is an amount of.
The raw material material of embodiment 1～5 prescription is operated according to the following steps:
A, cross behind 80 mesh sieves oxiracetam standby;
B, take by weighing the sunset yellow of formula ratio, be dissolved in the 15%PVP aqueous solution as binding agent;
The oxiracetam mix homogeneously of c, the mannitol that takes by weighing formula ratio, Aspartane and treated mistake adds the binding agent system soft material that makes, and granulates with 20 mesh sieves, behind the airpillow-dry, makes dried granule with 18 mesh sieve granulate;
D, the powdered flavor that takes by weighing formula ratio and dried granule mixing promptly prepare oxiracetam granular preparation of the present invention.
Oxiracetam granular preparation of the present invention, clinical memory and the disturbance of intelligence that is applicable to that diseases such as light moderate vascular dementia, alzheimer disease and cerebral trauma cause.Each one bag,, can take every day 1～3 time according to different specifications.As specification is the oxiracetam granular preparation of 0.8g/ bag, but takes every day 2 times, and taking convenience has improved patient's compliance.
Claims (5)
1. oxiracetam granular preparation of being convenient to take, it comprises oxiracetam principal agent and pharmaceutic adjuvant, it is characterized in that: described principal agent oxiracetam and pharmaceutic adjuvant unit proportioning are by weight counted 1.195: 1, described pharmaceutic adjuvant is made up of mannitol, Aspartane, sunset yellow and powdered flavor, and above-mentioned pharmaceutic adjuvant unit proportioning is by weight counted 440: 5: 0.2: 1.
2. the oxiracetam granular preparation of being convenient to take according to claim 1 is characterized in that: add weight concentration in the described granular preparation and be 15% PVP aqueous solution, addition so that the material moistening be as the criterion.
3. the oxiracetam granular preparation of being convenient to take according to claim 2 is characterized in that: described each component unit is by weight counted:
Oxiracetam 200～1600
Mannitol 165～1320
Aspartame 1.875～15
Sunset yellow 0.075～0.6
Powdered flavor 0.375～3
The 15%PVP aqueous solution is an amount of.
4, the oxiracetam granular preparation of being convenient to take according to claim 3 is characterized in that, described each components contents unit is by weight counted:
Oxiracetam 800
Mannitol 660
Aspartame 7.5
Sunset yellow 0.3
Powdered flavor 1.5
The 15%PVP aqueous solution is an amount of.
5. preparation method as the oxiracetam granular preparation being convenient to take as described in the claim 1,2,3 or 4, it is characterized in that: it carries out as follows:
A, cross behind 80 mesh sieves principal agent oxiracetam standby;
B, take by weighing the sunset yellow of formula ratio, be dissolved in the 15%PVP aqueous solution as binding agent;
C, the mannitol that takes by weighing formula ratio, Aspartane and the oxiracetam mix homogeneously of crossing through a step process add the above-mentioned binding agent system soft material that makes, and granulate with 20 mesh sieves, behind the airpillow-dry, make dried granule with 18 mesh sieve granulate;
D, the powdered flavor that takes by weighing formula ratio and above-mentioned dried granule mixing.
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106606484A (en) * | 2015-10-27 | 2017-05-03 | 重庆润泽医药有限公司 | L-oxiracetam particles with high dissolution and dispersion speed and preparation method thereof |
| CN106619526A (en) * | 2015-10-27 | 2017-05-10 | 重庆润泽医药有限公司 | Good-stability (S)-4-hydroxy-2 oxo-1-pyrrolidine acetamide granule and preparation method thereof |
| CN106619524A (en) * | 2015-10-27 | 2017-05-10 | 重庆润泽医药有限公司 | Good-stability sinistral oxiracetam and preparation method thereof |
| CN106943377A (en) * | 2016-06-15 | 2017-07-14 | 重庆润泽医药有限公司 | A kind of levo-oxiracetam particle and preparation method thereof |
| CN106943376A (en) * | 2016-06-15 | 2017-07-14 | 重庆润泽医药有限公司 | A kind of levo-oxiracetam particle and preparation method thereof |
| CN107510678A (en) * | 2016-06-15 | 2017-12-26 | 重庆润泽医药有限公司 | One kind leaches fireballing levo-oxiracetam particle and preparation method thereof |
| CN107510672A (en) * | 2016-06-15 | 2017-12-26 | 重庆润泽医药有限公司 | Good oxo-1-pyrrolidine ethanamide particle of (S) -4- hydroxyls -2 of a kind of stability and preparation method thereof |
| CN109692167A (en) * | 2017-10-23 | 2019-04-30 | 重庆润泽医药有限公司 | The pharmaceutical composition and preparation method thereof for treating cognition dysfunction |
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2008
- 2008-06-16 CN CN2008100550716A patent/CN101288648B/en active Active
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106606484A (en) * | 2015-10-27 | 2017-05-03 | 重庆润泽医药有限公司 | L-oxiracetam particles with high dissolution and dispersion speed and preparation method thereof |
| CN106619526A (en) * | 2015-10-27 | 2017-05-10 | 重庆润泽医药有限公司 | Good-stability (S)-4-hydroxy-2 oxo-1-pyrrolidine acetamide granule and preparation method thereof |
| CN106619524A (en) * | 2015-10-27 | 2017-05-10 | 重庆润泽医药有限公司 | Good-stability sinistral oxiracetam and preparation method thereof |
| CN106943377A (en) * | 2016-06-15 | 2017-07-14 | 重庆润泽医药有限公司 | A kind of levo-oxiracetam particle and preparation method thereof |
| CN106943376A (en) * | 2016-06-15 | 2017-07-14 | 重庆润泽医药有限公司 | A kind of levo-oxiracetam particle and preparation method thereof |
| CN107510678A (en) * | 2016-06-15 | 2017-12-26 | 重庆润泽医药有限公司 | One kind leaches fireballing levo-oxiracetam particle and preparation method thereof |
| CN107510672A (en) * | 2016-06-15 | 2017-12-26 | 重庆润泽医药有限公司 | Good oxo-1-pyrrolidine ethanamide particle of (S) -4- hydroxyls -2 of a kind of stability and preparation method thereof |
| CN106943376B (en) * | 2016-06-15 | 2018-10-23 | 重庆润泽医药有限公司 | A kind of levo-oxiracetam particle and preparation method thereof |
| CN109692167A (en) * | 2017-10-23 | 2019-04-30 | 重庆润泽医药有限公司 | The pharmaceutical composition and preparation method thereof for treating cognition dysfunction |
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| CN101288648B (en) | 2010-11-17 |
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