CN102793659B - Aspirin suppository and preparation method thereof - Google Patents
Aspirin suppository and preparation method thereof Download PDFInfo
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- CN102793659B CN102793659B CN 201210291131 CN201210291131A CN102793659B CN 102793659 B CN102793659 B CN 102793659B CN 201210291131 CN201210291131 CN 201210291131 CN 201210291131 A CN201210291131 A CN 201210291131A CN 102793659 B CN102793659 B CN 102793659B
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Abstract
The invention provides an aspirin suppository suitable for cavitary drug delivery and a preparation method thereof. The suppository is prepared from the following raw materials by weight part: 10-20 of aspirin, 7-12 of sodium carboxymethylcellulose, 14-28 of an oleaginous matrix (such as coconut oil ester, Litsea cubeba oil, palmitate, propylene glycol stearate and the like), 35-95 of a water soluble matrix (such as glycerol, gelatin, polyethylene glycol and the like), and 5-10 of a hardening agent (such as white wax, stearic acid, carnauba wax and the like). The drug provided in the invention can be absorbed directly from an intestinal canal, so that the destruction of a liver first-pass effect during oral administration can be avoided. The drug has the advantages of uniform dispersion, stable dissolution rate, and bioavailability improvement, thus being an effective way of administration.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, specifically, relate to a kind of Asupirin and preparation method thereof.
Background technology
Aspirin is the salicylic acid antipyretic analgesic, by optionally making cyclooxygenase acetylation in the cell, suppresses the activity of cyclooxygenase.It is synthetic to influence hypothalamic cells pyrexin prostaglandin, the normal reaction that makes heat center recover regulate body temperature, and aspirin also has the platelet aggregation of inhibition effect in addition.It is applicable to the heating that flu causes; Alleviate mild to moderate pain; Prevent and treat arterial thrombus and myocardial infarction.
Existing market aspirin solid preparation has tablet, capsule, and these all are oral formulations, and are all lower at dissolution in vitro, and blood drug level and bioavailability are also lower; Aspirin has local irritation, it is more obvious when concentration is higher, common oral preparation oral be quick disintegrate, local concentration is higher and produce gastrointestinal is stimulated, can cause nauseating, vomiting, epigastric discomfort or untoward reaction such as severe pain, bronchospasm anaphylaxis, liver is also had certain toxicity.In addition aspirin is made the therapeutical effect that common preparation can not be given full play to this medicine, for the patient, do not reached the curative effect of obvious aspirin with other medicine.
Summary of the invention
The present invention is intended to overcome the existing defective that aspirin oral formulations dissolution in vitro is low, bioavailability is low, and a kind of Asupirin that is suitable for cavity/canal drug administration and preparation method thereof is provided.
In order to realize the object of the invention, a kind of Asupirin of the present invention is made by the raw material of following weight portion: aspirin 10～20, sodium carboxymethyl cellulose 7～12, greasing base 14～28, water-soluble base 35～95, sclerosing agent 5～10.Preferred Asupirin is made by the raw material of following weight portion: aspirin 10～16, sodium carboxymethyl cellulose 8～11, greasing base 15～25, water-soluble base 35～85, sclerosing agent 5～10.Wherein, greasing base is one or more in cocos nucifera oil ester, Fructus Litseae grease, cetylate, the propylene glycol stearate etc.; Water-soluble base is one or more in glycerol, gelatin, cetomacrogol 1000, the Macrogol 4000 etc.; Sclerosing agent is one or more in white beeswax, stearic acid, the Brazil wax etc.
The preparation method of above-mentioned Asupirin comprises step: (1) crosses the pulverizing of 80～100 mesh sieves and mixing with aspirin and sodium carboxymethyl cellulose; (2) with water-soluble base fusion in 60-90 ℃ of water-bath; (3) make its fusing with stirring in greasing base and the sclerosing agent adding (2); (4) with stirring in (1) adding (3), make paste; Treat that (5) (4) temperature drops to below 40 ℃, pour mould into, cooling.
The invention has the advantages that:
(1) the present invention is by making aspirin and suitable substrate the suppository of cavity/canal drug administration, can reduce or avoid to need to adopt with patient's (as alleviating mild to moderate pain, preventing and treating arterial thrombus and myocardial infarction etc.) of aspirin for treatment for a long time some untoward reaction of oral aspirin.
(2) because aspirin is slightly soluble in water and fusing point height, therefore in prescription, select greasing base and sclerosing agent to make paste, this product has the fusing point than fever under the dry storage condition, can keep stable and not melt when transportation or lay up period variations in temperature; Because the humidity of intracavity moisturizes suppository and its fusing point is reduced, medicine can effectively discharge in body cavity when inserting rectum.
(3) Asupirin makes medicine not be subjected to the destruction of gastrointestinal pH or enzyme, medicine absorbs from rectum, the destruction that is subjected to the liver first-pass effect in the time of can avoiding oral, suppository in vivo can biodegradation, noresidue and toxic and side effects, can also reduce medicine to toxicity and the side effect of liver, the safety that has improved medicine.
(4) medicine directly disturbs from rectum absorptance oral absorption and lacks, and the action time of suppository is longer than general oral tablet, is a kind of effective route of administration to the patient with vomiting.
(5) dispersion of medicine, dissolution rate is stable, has improved the effectiveness of bioavailability and medicine.
(6) can reduce the purpose that dust from flying reaches the healthy and production environment of protection operator in the preparation process.
The specific embodiment
Following examples are used for explanation the present invention, but are not used for limiting the scope of the invention.If do not specialize the conventional means that used technological means is well known to those skilled in the art among the embodiment, the raw materials used commercial goods that is.
The preparation of embodiment 1 Asupirin
(1) 150g aspirin and 100g sodium carboxymethyl cellulose sieve were pulverized 100 orders and mix homogeneously.
(2) with 500g polyethylene glycols (300g cetomacrogol 1000 and 200g Macrogol 4000) 85 ℃ of water-bath fusions.
(3) propylene glycol stearate and stearic acid are added in (2), stir.
(4) with stirring in (1) adding (3), make the paste charges of suppository.
Treat that (5) (4) temperature drops to below 40 ℃, pour in the mould, behind the cooling curing, with the part that cutter is pruned and overflowed, open the bolt mould, release.
The preparation of embodiment 2 Asupirins
(1) 300g aspirin and 200g sodium carboxymethyl cellulose sieve were pulverized 100 orders and mix homogeneously.
(2) with Macrogol 4000 and each 400g of glycerol 85 ℃ of water-bath fusions.
(3) cocos nucifera oil ester and stearic acid and Brazil wax are added in (2), stir.
(4) with stirring in (1) adding (3), make the paste charges of suppository.
Treat that (5) (4) temperature drops to below 40 ℃, pour in the mould, behind the cooling curing, with the part that cutter is pruned and overflowed, open the bolt mould, release.
The preparation of embodiment 3 Asupirins
(1) 150g aspirin and 110g sodium carboxymethyl cellulose sieve were pulverized 100 orders and mix homogeneously.
(2) with 400g cetomacrogol 1000 and 300g gelatin 85 ℃ of water-bath fusions.
(3) Fructus Litseae grease and stearic acid are added in (2), stir.
(4) with stirring in (1) adding (3), make the paste charges of suppository.
Treat that (5) (4) temperature drops to below 40 ℃, pour in the mould, behind the cooling curing, with the part that cutter is pruned and overflowed, open the bolt mould, release.
The preparation of embodiment 4 Asupirins
(1) 200g aspirin and 120g sodium carboxymethyl cellulose sieve were pulverized 100 orders and mix homogeneously.
(2) with 750g polyethylene glycols (300g cetomacrogol 1000 and 450g Macrogol 4000) 85 ℃ of water-bath fusions.
(3) cetylate and stearic acid are added in (2), stir.
(4) with stirring in (1) adding (3), make the paste charges of suppository.
Treat that (5) (4) temperature drops to below 40 ℃, pour in the mould, behind the cooling curing, with the part that cutter is pruned and overflowed, open the bolt mould, release.
The preparation of embodiment 5 Asupirins
(1) 200g aspirin and 100g sodium carboxymethyl cellulose sieve were pulverized 100 orders and mix homogeneously.
(2) with 400g polyethylene glycols (each 200g of cetomacrogol 1000 and Macrogol 4000) 85 ℃ of water-bath fusions.
(3) propylene glycol stearate and stearic acid are added in (2), stir.
(4) with stirring in (1) adding (3), make the paste charges of suppository.
Treat that (5) (4) temperature drops to below 40 ℃, pour in the mould, behind the cooling curing, with the part that cutter is pruned and overflowed, open the bolt mould, release.
The preparation of embodiment 6 Asupirins
(1) 180g aspirin and 90g sodium carboxymethyl cellulose sieve were pulverized 100 orders and mix homogeneously.
(2) with 600g polyethylene glycols (each 300g of cetomacrogol 1000 and Macrogol 4000) 85 ℃ of water-bath fusions.
(3) propylene glycol stearate and stearic acid are added in (2), stir.
(4) with stirring in (1) adding (3), make the paste charges of suppository.
Treat that (5) (4) temperature drops to below 40 ℃, pour in the mould, behind the cooling curing, with the part that cutter is pruned and overflowed, open the bolt mould, release.
The dissolution experiment of embodiment 7 Asupirins
To aspirin tablet (Bengbu FengYuan TuShan Pharmaceutical Co., Ltd, lot number 110504), Aspirin Enteric-coated Tablets (Bengbu FengYuan TuShan Pharmaceutical Co., Ltd, lot number: 110112) and the Asupirin of embodiment 1～6 preparation carry out in-vitro evaluation, the result is as shown in table 1.
Dissolution (%) contrast of table 1 different dosage form product
Wherein, dissolution medium is used the simulated intestinal fluid of high pH instead more earlier with the simulated gastric fluid of low pH, changes with pH in the analogue body; The temperature of stripping is about 37 ℃ with body temperature.
The stability experiment of embodiment 8 Asupirins
(1) hot test
Test sample (Asupirin of embodiment 1～6 preparation) opening is placed suitable clean container, placed 10 days under 40 ℃ of temperature, respectively at sampling in the 0th, 5 and 10 day, detect by stable high spot reviews project, the weight of test sample before and after accurately weighing is tested simultaneously is with the situation (table 2-4) of investigating test sample air slaking weightlessness.
The situation of the 0th day test sample air slaking weightlessness of table 2
The situation of the 5th day test sample air slaking weightlessness of table 3
The situation of the 10th day test sample air slaking weightlessness of table 4
(2) high humility test
Test sample (Asupirin of embodiment 1～6 preparation) opening is placed the constant humidity hermetic container, under 25 ℃, relative humidity 90% ± 5% condition, placed 10 days, respectively at sampling in the 0th, 5 and 10 day, detect by stable high spot reviews project, the weight of test sample before and after accurately weighing is tested simultaneously is with the situation (table 5-7) of investigating test sample moisture absorption weightening finish.
The situation of table 5 test sample moisture absorption in the 0th day weightening finish
The situation of table 6 test sample moisture absorption in the 5th day weightening finish
The situation of table 7 test sample moisture absorption in the 10th day weightening finish
(3) strong illumination test
Test sample (Asupirin of embodiment 1～6 preparation) opening is put in being placed on the light kitchen, be to place under (4500 ± 500) lx condition 10 days in illumination, respectively at sampling in the 0th, 5 and 10 day, detect by stable high spot reviews project, with the cosmetic variation (table 8-10) of investigating test sample.
The situation of the 0th day test sample cosmetic variation of table 8
The situation of the 5th day test sample cosmetic variation of table 9
The situation of the 10th day test sample cosmetic variation of table 10
Above embodiment shows that fully the Asupirin of the present invention's preparation has stability preferably, and dissolution rate is stable.
Though above the present invention is described in detail with a general description of the specific embodiments, on basis of the present invention, can make some modifications or improvements it, this will be apparent to those skilled in the art.Therefore, these modifications or improvements all belong to the scope of protection of present invention without departing from theon the basis of the spirit of the present invention.
Claims (3)
1. an Asupirin is characterized in that, is made by the raw material of following weight portion: aspirin 10～20, sodium carboxymethyl cellulose 7～12, greasing base 14～28, water-soluble base 35～95, sclerosing agent 5～10;
Wherein, greasing base is one or more in cocos nucifera oil ester, Fructus Litseae grease, cetylate, the propylene glycol stearate; Water-soluble base is one or more in glycerol, gelatin, cetomacrogol 1000, the Macrogol 4000; Sclerosing agent is one or more in white beeswax, stearic acid, the Brazil wax.
2. Asupirin according to claim 1 is characterized in that, is made by the raw material of following weight portion: aspirin 10～16, sodium carboxymethyl cellulose 8～11, greasing base 15～20, water-soluble base 35～85, sclerosing agent 5～8.
3. the preparation method of claim 1 or 2 described Asupirins is characterized in that, comprises step:
(1) aspirin and sodium carboxymethyl cellulose are crossed the pulverizing of 80～100 mesh sieves and mixing;
(2) with water-soluble base fusion in 60-90 ℃ of water-bath;
(3) make its fusing with stirring in greasing base and the sclerosing agent adding (2);
(4) with stirring in (1) adding (3), make paste;
Treat that (5) (4) temperature drops to below 40 ℃, pour mould into, cooling.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210291131 CN102793659B (en) | 2012-08-15 | 2012-08-15 | Aspirin suppository and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210291131 CN102793659B (en) | 2012-08-15 | 2012-08-15 | Aspirin suppository and preparation method thereof |
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| CN102793659A CN102793659A (en) | 2012-11-28 |
| CN102793659B true CN102793659B (en) | 2013-09-04 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1102096A (en) * | 1993-10-30 | 1995-05-03 | 文士元 | Anti-inflammatory antipyretic suppository for animals |
| CN102018660A (en) * | 2010-12-03 | 2011-04-20 | 蚌埠丰原涂山制药有限公司 | Naftopidil suppository and preparation method thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6197327B1 (en) * | 1997-06-11 | 2001-03-06 | Umd, Inc. | Device and method for treatment of dysmenorrhea |
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- 2012-08-15 CN CN 201210291131 patent/CN102793659B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1102096A (en) * | 1993-10-30 | 1995-05-03 | 文士元 | Anti-inflammatory antipyretic suppository for animals |
| CN102018660A (en) * | 2010-12-03 | 2011-04-20 | 蚌埠丰原涂山制药有限公司 | Naftopidil suppository and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 郭剑伟 等.阿司匹林栓剂制备工艺改进.《大理学院学报》.2006,第5卷(第4期),9-10页. |
| 阿司匹林栓剂制备工艺改进;郭剑伟 等;《大理学院学报》;20060430;第5卷(第4期);9-10页 * |
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