CN105106128A - Antipyretic, analgesic and anti-inflammatory aspirin composite dry suspension - Google Patents
Antipyretic, analgesic and anti-inflammatory aspirin composite dry suspension Download PDFInfo
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- CN105106128A CN105106128A CN201510506148.7A CN201510506148A CN105106128A CN 105106128 A CN105106128 A CN 105106128A CN 201510506148 A CN201510506148 A CN 201510506148A CN 105106128 A CN105106128 A CN 105106128A
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Abstract
The invention relates to an antipyretic, analgesic and anti-inflammatory aspirin composite dry suspension and belongs to the technical field of medicine. The suspension is made from aspirin, lactose, saccharose, carbomer, guar gum, vanillin and 95% ethyl alcohol. The aspirin is a new crystal form compound, an X-ray powder diffraction pattern of the aspirin measured by using Cu-ka ray is shown in figure 1, the aspirin is different from those reported in the prior art, and experiments show that the suspension prepared with the aspirin, the new crystal form compound, is good in stability and high in bioavailability and has low content of free salicylic acid, the content of free salicylic acid has no evident increase over storage time, and gastrointestinal adverse reaction to the suspension is greatly decreased.
Description
Technical field
The invention belongs to medical art, relate to a kind of antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension.
Background technology
Aspirin (aspirin), have another name called aspirin, one of three large classical medicines in history, as the time-honored antipyretic analgesic of one, its effectiveness is obviously cheap, so far remain most widely used antipyretic-antalgic anti-inflammatory agent, and be the standard preparation comparing and evaluate other drug.Since the sixties in 20th century, pharmacological research shows, aspirin persistency deactivation COX-1 is active, suppress platelet function, without dosage dependent interaction, extremely low concentration (nmol/L) can reach inhibitory action rapidly, namely has clear and definite blood coagulation resisting function, thus can as the medicine of pre-preventing thrombosis." Chinese Consensus of experts " suggestion aspirin prolonged application dosage in primary prevention is 75-100mg/ day, and is 75-150mg/ day at the prolonged application dosage of secondary prevention.
Mainly there is two problems in the Genprin of existing use: facile hydrolysis produces salicylic acid and causes gastrointestinal hemorrhage.Salicylic acid is the hydrolyzate of aspirin, is the principal element that aspirin causes digestive tract to stimulate simultaneously, and the height of its content is one of important indicator evaluating Genprin quality.In pharmacopeia, in regulation aspirin, salicylic content must not more than 1.5%.
The maximum toxic and side effects of aspirin is exactly very easily cause rotten to the corn, hemorrhage and ulcer of gastrointestinal tract mucosa etc.Except analgesia, antipyretic except, all need Long-term taking medicine when aspirin is used for the treatment of the diseases such as rheumatic fever, arthritis, antithrombotic, further increase the incidence rate of toxic and side effects.Although people have carried out improving dosage form, as added suppository, avoid medicine and gastrointestinal tract to touch, medication is extremely inconvenient; And for example make enteric coated preparation, although decrease the incidence rate of toxic and side effects to a certain extent, have part Seepage can occur under one's belt, stimulation can be caused to stomach like this, damage is caused to gastric mucosa; If the content of free salicylic acid is high in preparation, salicylism can be caused to react, still do not tackle the problem at its root.
Therefore, reduce free water poplar acid content in Genprin to have very important significance.
Summary of the invention
Goal of the invention of the present invention is to provide a kind of antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension.
In order to complete object of the present invention, the technical scheme of employing is:
The present invention relates to a kind of antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension, described compositions dry suspension is made up of aspirin, lactose, sucrose, carbomer, guar gum, vanillin, 95% ethanol; Described aspirin is crystal, and the X-ray powder diffraction pattern that the measurement of use Cu-K alpha ray obtains as shown in Figure 1.
First optimal technical scheme of the present invention is: with parts by weight, and described compositions dry suspension is made up of the aspirin of 0.5-1.5 weight portion, the lactose of 5-5.8 weight portion, the sucrose of 2-4 weight portion, the carbomer of 0.5-0.7 weight portion, the guar gum of 0.3-0.5 weight portion, the vanillin of 0.3-0.5 weight portion, 95% ethanol of 1.5-2.5 weight portion.
Second optimal technical scheme of the present invention is: with parts by weight, and described compositions dry suspension is made up of the aspirin of 1 weight portion, the lactose of 5.4 weight portions, the sucrose of 3 weight portions, the carbomer of 0.6 weight portion, the guar gum of 0.4 weight portion, the vanillin of 0.4 weight portion, 95% ethanol of 2 weight portions.
3rd optimal technical scheme of the present invention is: the preparation method of described compositions dry suspension comprises the following steps:
1) supplementary material process: aspirin raw material is crossed 100 mesh sieves;
2) weigh: weigh according to prescription amount;
3) mixing granulation: the aspirin of prescription amount, lactose, sucrose, carbomer, guar gum are added in wet mixing pelletizer, open stirring motor and be dry mixed 10 minutes, add prescription amount wetting agent 95% ethanol, wet mixing 240-280 soft material second, selects 16 order stainless steel meshs to be arranged in spinning comminutor and granulates;
4) dry granulate: regulate boiling drier inlet temperature 55-60 DEG C, wet granular is placed in boiling drier and carries out drying, be dried to moisture < 3.6%, by 18 order granulate in granule oscillating granulator after drying;
5) always mix: the vanillin of the dry granule after granulate and prescription amount is joined in three-dimensional motion mixer, motor rotation frequency 200r/min is set, open mixer and mix 10 minutes;
6) pack: granule is joined particles packing machine intermediate package, control content uniformity and meet inner quality standard.
4th optimal technical scheme of the present invention is: the preparation method of the crystal of described aspirin comprises the following steps:
Get aspirin crude drug, the volume adding 30 DEG C is that in the mixed solvent of the ethanol of aspirin weight 8 times, cyclohexane extraction, N-methylacetamide, ethanol, cyclohexane extraction, N-methylacetamide volume ratio are 3:1:1, obtain solution; Then in the horizontal direction of the liquid level of gained solution, apply the stationary magnetic field that magnetic field intensity is 0.9T, and under the condition of this stationary magnetic field, drip volume in solution be aspirin weight 10 times of deionized waters; After being added dropwise to complete, be cooled to-10 DEG C, leave standstill 3 hours, filter, washing, vacuum drying, obtains described aspirin crystal.
Below technical scheme of the present invention is made further explanation:
The present invention is by the precise controlling to crystallization condition, and prepared a kind of aspirin novel crystal forms unlike the prior art, the X-ray powder diffraction pattern of this aspirin crystal unlike the prior art.Simultaneously due to the ins and outs of this crystal formation, find through test, dry suspension prepared by this aspirin crystal compound, good stability, bioavailability is high, not only there is lower free salicylic acid content, and along with period of storage its free salicylic acid content of prolongation increase not obvious, greatly reduce medicine gastrointestinal side effect.
Accompanying drawing explanation
Fig. 1 is the X-ray powder diffraction that the aspirin crystal of the embodiment of the present invention 1 preparation uses the measurement of Cu-K alpha ray to obtain.
Detailed description of the invention
Below by specific embodiment, summary of the invention of the present invention is described in further detail, but does not therefore limit content of the present invention.
embodiment 1:the preparation of aspirin crystal
Get aspirin crude drug, the volume adding 30 DEG C is that in the mixed solvent of the ethanol of aspirin weight 8 times, cyclohexane extraction, N-methylacetamide, ethanol, cyclohexane extraction, N-methylacetamide volume ratio are 3:1:1, obtain solution; Then in the horizontal direction of the liquid level of gained solution, apply the stationary magnetic field that magnetic field intensity is 0.9T, and under the condition of this stationary magnetic field, drip volume in solution be aspirin weight 10 times of deionized waters; After being added dropwise to complete, be cooled to-10 DEG C, leave standstill 3 hours, filter, washing, vacuum drying, obtains described aspirin crystal.
As shown in Figure 1, its purity of high-performance liquid chromatogram determination is 99.9% to the X-ray powder diffraction pattern that the aspirin crystal prepared uses the measurement of Cu-K alpha ray to obtain.
embodiment 2:the preparation of aspirin dry suspension
Prescription: with parts by weight, the aspirin crystal-form compound 0.5 part that the embodiment of the present invention 1 is obtained, lactose 5 parts, sucrose 2 parts, carbomer 0.5 part, guar gum 0.3 part, vanillin 0.3 part, 95% ethanol 1.5 parts.
Preparation method:
1) supplementary material process: aspirin raw material is crossed 100 mesh sieves;
2) weigh: weigh according to prescription amount;
3) mixing granulation: the aspirin of prescription amount, lactose, sucrose, carbomer, guar gum are added in wet mixing pelletizer, open stirring motor and be dry mixed 10 minutes, add prescription amount wetting agent 95% ethanol, wet mixing 240-280 soft material second, selects 16 order stainless steel meshs to be arranged in spinning comminutor and granulates;
4) dry granulate: regulate boiling drier inlet temperature 55-60 DEG C, wet granular is placed in boiling drier and carries out drying, be dried to moisture < 3.6%, by 18 order granulate in granule oscillating granulator after drying;
5) always mix: the vanillin of the dry granule after granulate and prescription amount is joined in three-dimensional motion mixer, motor rotation frequency 200r/min is set, open mixer and mix 10 minutes;
6) pack: granule is joined particles packing machine intermediate package, control content uniformity and meet inner quality standard.
embodiment 3:the preparation of aspirin dry suspension
Prescription: with parts by weight, the aspirin crystal-form compound 1 part that the embodiment of the present invention 1 is obtained, lactose 5.4 parts, sucrose 3 parts, carbomer 0.6 part, guar gum 0.4 part, vanillin 0.4 part, 95% ethanol 2 parts.
Preparation method:
1) supplementary material process: aspirin raw material is crossed 100 mesh sieves;
2) weigh: weigh according to prescription amount;
3) mixing granulation: the aspirin of prescription amount, lactose, sucrose, carbomer, guar gum are added in wet mixing pelletizer, open stirring motor and be dry mixed 10 minutes, add prescription amount wetting agent 95% ethanol, wet mixing 240-280 soft material second, selects 16 order stainless steel meshs to be arranged in spinning comminutor and granulates;
4) dry granulate: regulate boiling drier inlet temperature 55-60 DEG C, wet granular is placed in boiling drier and carries out drying, be dried to moisture < 3.6%, by 18 order granulate in granule oscillating granulator after drying;
5) always mix: the vanillin of the dry granule after granulate and prescription amount is joined in three-dimensional motion mixer, motor rotation frequency 200r/min is set, open mixer and mix 10 minutes;
6) pack: granule is joined particles packing machine intermediate package, control content uniformity and meet inner quality standard.
embodiment 4:the preparation of aspirin dry suspension
Prescription: with parts by weight, the aspirin crystal-form compound 1.5 parts that the embodiment of the present invention 1 is obtained, lactose 5.8 parts, sucrose 4 parts, carbomer 0.7 part, guar gum 0.5 part, vanillin 0.5 part, 95% ethanol 2.5 parts.
Preparation method:
1) supplementary material process: aspirin raw material is crossed 100 mesh sieves;
2) weigh: weigh according to prescription amount;
3) mixing granulation: the aspirin of prescription amount, lactose, sucrose, carbomer, guar gum are added in wet mixing pelletizer, open stirring motor and be dry mixed 10 minutes, add prescription amount wetting agent 95% ethanol, wet mixing 240-280 soft material second, selects 16 order stainless steel meshs to be arranged in spinning comminutor and granulates;
4) dry granulate: regulate boiling drier inlet temperature 55-60 DEG C, wet granular is placed in boiling drier and carries out drying, be dried to moisture < 3.6%, by 18 order granulate in granule oscillating granulator after drying;
5) always mix: the vanillin of the dry granule after granulate and prescription amount is joined in three-dimensional motion mixer, motor rotation frequency 200r/min is set, open mixer and mix 10 minutes;
6) pack: granule is joined particles packing machine intermediate package, control content uniformity and meet inner quality standard.
[test example]aspirin dry suspension free salicylic acid assay is tested
Dry suspension prepared by difference Example 3 and commercially available enteric coated capsule sample appropriate (being about equivalent to aspirin 0.lg), wear into fine powder, accurately weighed, put in 100ml measuring bottle, the methanol solution jolting adding 1% glacial acetic acid makes aspirin dissolve, and is diluted to scale, shakes up, filter membrane filters, and gets subsequent filtrate as need testing solution (facing by brand-new); Get salicylic acid reference substance and be about 15mg, accurately weighed, put in 50ml measuring bottle, add the dissolve with methanol solution of 1% glacial acetic acid and be diluted to scale, shake up, precision measures 5ml, puts in 100ml measuring bottle, be diluted to scale with the methanol solution of 1% glacial acetic acid, shake up, in contrast product solution.Measure according to the method under aspirin free salicylic acid item, by external standard method with calculated by peak area, 0.5% of labelled amount must not be crossed.
The measurement result (0 day) of table 1 aspirin free salicylic acid
Free salicylic acid measurement result (6 months, 40 DEG C of 75%RH) after table 2 accelerated test
As can be seen from the result of the test of table 1 and table 2, the aspirin dry suspension prepared of the embodiment of the present invention 3 before acceleration after free salicylic acid substantially constant; And free salicylic acid increases obviously in commercially available enteric coated capsule.
Identical test is carried out to other embodiments, has obtained analog result.
Claims (5)
1. an antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension, is characterized in that: described compositions dry suspension is made up of aspirin, lactose, sucrose, carbomer, guar gum, vanillin, 95% ethanol; Described aspirin is crystal, and the X-ray powder diffraction pattern that the measurement of use Cu-K alpha ray obtains as shown in Figure 1.
2. antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension according to claim 1, it is characterized in that: with parts by weight, described compositions dry suspension is made up of the aspirin of 0.5-1.5 weight portion, the lactose of 5-5.8 weight portion, the sucrose of 2-4 weight portion, the carbomer of 0.5-0.7 weight portion, the guar gum of 0.3-0.5 weight portion, the vanillin of 0.3-0.5 weight portion, 95% ethanol of 1.5-2.5 weight portion.
3. antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension according to claim 2, it is characterized in that: with parts by weight, described compositions dry suspension is made up of the aspirin of 1 weight portion, the lactose of 5.4 weight portions, the sucrose of 3 weight portions, the carbomer of 0.6 weight portion, the guar gum of 0.4 weight portion, the vanillin of 0.4 weight portion, 95% ethanol of 2 weight portions.
4., according to the arbitrary described antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension of claim 1-3, it is characterized in that, the preparation method of described compositions dry suspension comprises the following steps:
1) supplementary material process: aspirin raw material is crossed 100 mesh sieves;
2) weigh: weigh according to prescription amount;
3) mixing granulation: the aspirin of prescription amount, lactose, sucrose, carbomer, guar gum are added in wet mixing pelletizer, open stirring motor and be dry mixed 10 minutes, add prescription amount wetting agent 95% ethanol, wet mixing 240-280 soft material second, selects 16 order stainless steel meshs to be arranged in spinning comminutor and granulates;
4) dry granulate: regulate boiling drier inlet temperature 55-60 DEG C, wet granular is placed in boiling drier and carries out drying, be dried to moisture < 3.6%, by 18 order granulate in granule oscillating granulator after drying;
5) always mix: the vanillin of the dry granule after granulate and prescription amount is joined in three-dimensional motion mixer, motor rotation frequency 200r/min is set, open mixer and mix 10 minutes;
6) pack: granule is joined particles packing machine intermediate package, control content uniformity and meet inner quality standard.
5. antipyretic-antalgic anti-inflammatory agent aspirin composition dry suspension according to claim 1, it is characterized in that, the preparation method of the crystal of described aspirin comprises the following steps:
Get aspirin crude drug, the volume adding 30 DEG C is that in the mixed solvent of the ethanol of aspirin weight 8 times, cyclohexane extraction, N-methylacetamide, ethanol, cyclohexane extraction, N-methylacetamide volume ratio are 3:1:1, obtain solution; Then in the horizontal direction of the liquid level of gained solution, apply the stationary magnetic field that magnetic field intensity is 0.9T, and under the condition of this stationary magnetic field, drip volume in solution be aspirin weight 10 times of deionized waters; After being added dropwise to complete, be cooled to-10 DEG C, leave standstill 3 hours, filter, washing, vacuum drying, obtains described aspirin crystal.
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| CN201510506148.7A CN105106128A (en) | 2015-08-18 | 2015-08-18 | Antipyretic, analgesic and anti-inflammatory aspirin composite dry suspension |
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| CN201510506148.7A CN105106128A (en) | 2015-08-18 | 2015-08-18 | Antipyretic, analgesic and anti-inflammatory aspirin composite dry suspension |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104151163A (en) * | 2014-07-14 | 2014-11-19 | 西安交通大学 | Crystal form of aspirin as well as preparation method and application thereof |
| CN104337820A (en) * | 2013-07-25 | 2015-02-11 | 青岛康地恩动物药业有限公司 | Suspension containing acetylsalicylic acid and methylprednisolone, and preparation method thereof |
| CN104761449A (en) * | 2015-04-30 | 2015-07-08 | 苗怡文 | Antipyretic, analgesic and anti-inflammatory medicine compound and preparation method thereof |
| CN104825472A (en) * | 2015-05-03 | 2015-08-12 | 苗怡文 | Fever/pain relieving and anti-inflammatory pharmaceutical composition and preparation method thereof |
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2015
- 2015-08-18 CN CN201510506148.7A patent/CN105106128A/en not_active Withdrawn
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104337820A (en) * | 2013-07-25 | 2015-02-11 | 青岛康地恩动物药业有限公司 | Suspension containing acetylsalicylic acid and methylprednisolone, and preparation method thereof |
| CN104151163A (en) * | 2014-07-14 | 2014-11-19 | 西安交通大学 | Crystal form of aspirin as well as preparation method and application thereof |
| CN104761449A (en) * | 2015-04-30 | 2015-07-08 | 苗怡文 | Antipyretic, analgesic and anti-inflammatory medicine compound and preparation method thereof |
| CN104825472A (en) * | 2015-05-03 | 2015-08-12 | 苗怡文 | Fever/pain relieving and anti-inflammatory pharmaceutical composition and preparation method thereof |
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Application publication date: 20151202 |
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