CN111870606A - Aspirin composition and preparation method and application thereof - Google Patents
Aspirin composition and preparation method and application thereof Download PDFInfo
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Abstract
The invention is suitable for the technical field of medicine, and provides an aspirin composition and a preparation method and application thereof, wherein the aspirin composition comprises the following components: aspirin; an enteric coating layer comprising an enteric material for dissolution in intestinal fluid and not in the stomach; a first isolation coating layer disposed between the aspirin and the enteric coating layer; a gastro-soluble coating layer comprising a gastro-soluble material for dissolution in the stomach and insoluble in water and intestinal fluids; and a second isolating coating layer for isolating the gastric coating layer from the enteric coating layer; the second release coat layer includes an adhesive. According to the aspirin composition provided by the invention, the first isolation coating layer, the enteric coating layer, the second isolation coating layer and the gastric dissolution coating layer are sequentially coated on the outer side of aspirin, so that a medicament can be not dissolved out under the conditions of oral cavity and gastric juice and can be quickly dissolved out under the intestinal tract condition, and thus, an oral preparation suitable for children is prepared, and the problem of irritation of aspirin to stomach is solved.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to an aspirin composition as well as a preparation method and application thereof.
Background
Congenital heart diseases are the most common congenital malformations, account for about 28% of various congenital malformations and account for 0.4% -1% of life infants, which means that 15-20 ten thousand congenital heart disease patients are newly increased every year in China. Children with 1/3 children were killed with serious complications within 1 year after birth without immediate treatment. Most children need surgical treatment to correct deformity. At present, most children patients can recover to normal conditions like normal people if timely surgical treatment is carried out. But no matter the intervention treatment or the surgical treatment, the infant has potential thrombus after the operation. Therefore, aspirin is needed to prevent thrombus formation after operation. After operation, the children need to take small dose of aspirin from half a year to life, and cannot stop taking the aspirin automatically. Kawasaki disease is an acute febrile eruptive pediatric disease with systemic vasculitis as the main pathological feature. Kawasaki disease has become the most important cause of acquired heart disease in children at present. Kawasaki disease is mostly seen in children under 5 years old, the most serious complication is coronary artery thrombotic occlusion, and aspirin is the first choice medicine for the anti-platelet treatment of children suffering from the Kawasaki disease.
The above two diseases are both administrated by common tablets or enteric-coated tablets. The tablet is difficult for children to swallow, and the compliance of children patients is extremely poor. The tablets are also broken or ground for administration, the administration dose is inaccurate, and the broken or ground administration destroys the enteric coating, so that the sperelin stimulates the stomach, and the stomach of a child patient is greatly damaged after long-term administration. Dispersible tablets also have the problems of indistinguishable doses and gastric irritation.
The children require good compliance of children patients, the oral administration is convenient, and the dosage can be accurately adjusted according to different ages. Suitable for children, such as oral liquid, granule, and suspension. Oral liquid is the best choice, but aspirin cannot be made into oral liquid because it is unstable in water and easily degrades in water.
In addition, aspirin has strong stimulation to the stomach, which can cause erosion, bleeding, ulcer and the like of the gastric mucosa. Most patients take aspirin with a medium dose for a plurality of days, and the fecal occult blood test is positive; the incidence rate of ulcer diseases is high when the medicine is taken for a long time. Aspirin can permeate the sebaceous protein membrane layer on gastric mucosa to destroy the protective effect of the lipoprotein membrane, so that gastric acid can be reversibly diffused into tissues to damage cells, and capillaries are damaged to cause bleeding. As a preventive agent for thrombus, it is required to be taken for a long period of time. Therefore, it is required that aspirin is not dissolved in the oral cavity and in an aqueous solution (children's medicine is usually taken with a water suspension), is not dissolved in a gastric juice (gastric irritation is avoided), and is rapidly dissolved in an intestinal tract (rapid onset of action) when the aspirin is orally administered.
However, the intestinal conditions, the aqueous solution conditions and the oral conditions are very similar, and the pH value is 6.5-7.5. If the drug is not dissolved in water or in the oral cavity, it is difficult to achieve dissolution of the drug in intestinal conditions, and thus the conventional enteric preparation cannot achieve the purpose.
Therefore, how to develop a novel aspirin preparation which is convenient for children to administer and can avoid the gastric irritation to children patients is an urgent technical problem to be solved.
Disclosure of Invention
An object of an embodiment of the present invention is to provide an aspirin composition, which aims to solve the problems set forth in the background art.
The embodiment of the invention is realized in such a way that the aspirin composition comprises the following components:
aspirin;
an enteric coating layer comprising an enteric material for dissolution in intestinal fluid and not in the stomach;
a first isolation coating layer disposed between the aspirin and the enteric coating layer; the first release coating layer comprises a binder;
a gastro-soluble coating layer comprising a gastro-soluble material for dissolution in the stomach and insoluble in water and intestinal fluids; and
a second isolating coating layer for isolating the gastric coating layer from the enteric coating layer; the second release coat layer includes an adhesive.
In a preferred embodiment of the present invention, the enteric material is at least one of an acrylic resin enteric material, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, and polyvinyl alcohol phthalate.
In another preferred embodiment of the present invention, the binder is at least one of hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, xanthan gum and acacia gum.
In another preferred embodiment of the present invention, the gastric soluble material is an acrylic gastric soluble material.
Another object of an embodiment of the present invention is to provide a method for preparing the aspirin composition, which includes the following steps:
taking aspirin as a raw material medicine;
preparing a first isolation coating solution from an adhesive;
coating the raw material medicine by using first isolation coating liquid to form a first isolation coating layer to obtain a material A;
preparing enteric coating solution from enteric materials;
coating the material A with an enteric coating solution to form an enteric coating layer to obtain a material B;
preparing a second isolation coating solution by using an adhesive;
coating the material B with a second isolation coating solution to form a second isolation coating layer to obtain a material C;
preparing gastric-soluble coating liquid from gastric-soluble materials;
and (3) coating the material C with a gastric-soluble coating solution to form a gastric-soluble coating layer to obtain the aspirin composition.
As another preferred scheme of the embodiment of the invention:
the first isolation coating liquid comprises the following components in percentage by mass: 2-25% of adhesive, 1-20% of anti-sticking agent and the balance of solvent, wherein the sum of the mass percentages of the components is 100%;
the enteric coating solution comprises the following components in percentage by mass: 10-55% of enteric material, 1-10% of plasticizer, 1-10% of anti-sticking agent, 0-0.8% of surfactant and the balance of solvent, wherein the sum of the mass percentages of the components is 100%;
the second isolation coating liquid comprises the following components in percentage by mass: 5-20% of adhesive, and the balance of solvent, wherein the sum of the mass percentages of the components is 100%;
the gastric coating solution comprises the following components in percentage by mass: 5-10% of gastric soluble material, 0.5-8% of plasticizer, 2-5% of anti-sticking agent, 0-0.5% of surfactant and the balance of solvent, wherein the sum of the mass percentages of the components is 100%.
As another preferred scheme of the embodiment of the invention:
the solvent is at least one of water, ethanol, acetone and isopropanol;
the anti-sticking agent is silicon dioxide and/or talcum powder;
the plasticizer is citric acid ester and/or phthalic acid ester;
the surfactant is sodium dodecyl sulfate and/or tween.
As another preferred scheme of the embodiment of the invention:
the weight of the first isolation coating layer is 5-15% of the weight of the raw material medicine;
the weight of the enteric coating layer is 12 to 30 percent of the weight of the material A;
the weight of the second isolation coating layer is 5-15% of the weight of the material B;
the weight of the gastric-soluble coating layer is 7-25% of the weight of the material C.
Another object of the embodiments of the present invention is to provide an aspirin composition prepared by the above preparation method.
Another object of the embodiments of the present invention is to provide an application of the aspirin composition in preparing a medicine for preventing children thrombus.
According to the aspirin composition provided by the embodiment of the invention, the first isolation coating layer, the enteric coating layer, the second isolation coating layer and the gastric dissolution coating layer are sequentially coated outside aspirin, so that a medicament can not be dissolved out under the conditions of oral cavity and gastric juice and can be quickly dissolved out under the condition of intestinal tract, and the problem of irritation of aspirin to stomach can be solved.
In addition, the aspirin composition prepared by the embodiment of the invention can be prepared into granules or dry suspensions, is more suitable for children to take compared with common tablets, solves the problem that children take medicine and swallow difficultly, and can accurately divide the dose according to the age of children so as to solve the problem that children take medicine and accurately divide the dose.
Drawings
FIG. 1 is a graph showing the dissolution profiles of aspirin compositions prepared in example 1 of the present invention in various media.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is described in further detail below with reference to the accompanying drawings and embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.
Example 1
This embodiment provides an aspirin composition, the preparation method of which includes the steps of:
s1, taking aspirin as a raw material medicine; wherein, the particle size of 80% of the raw material medicine can be controlled between 80-100 meshes.
S2, 50g of hydroxypropyl cellulose (HPC-SL) was added to a mixed solvent of 50g of water and 400g of ethanol with stirring, and after stirring was continued until the solution became clear, 50g of talc was added thereto and stirred to prepare a suspension, thereby obtaining a first barrier coating solution for use.
S3, placing 1000g of the raw material medicines (the raw material medicines in the S1 step) in a fluidized bed, coating the raw material medicines with 550g of first isolation coating liquid, and drying until the moisture content is lower than 2% to obtain a material A; wherein the coating treatment conditions in this step are as follows: the material temperature is 32 ℃, the air inlet temperature is 60 ℃, the air outlet temperature is 30 ℃, and the air inlet volume is 1m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 1.5 bar.
S4, adding 9g of triethyl citrate and 40g of talcum powder into 186g of water, carrying out high-speed shearing for 10min, adding 265g of acrylic resin enteric material and stirring at the same time to obtain the enteric coating solution for later use. As the acrylic resin enteric material, commercially available Equidz L30D-55 (30% aqueous dispersion) can be specifically used.
S5, placing 1000g of the material A in a fluidized bed, heating to 40 ℃, preheating for 5min, then coating the material A with 491g of enteric coating solution, and drying until the water content is lower than 2% to obtain a material B; wherein the coating treatment conditions in this step are as follows: the material temperature is 40 ℃, the air inlet temperature is 60 ℃, the air outlet temperature is 35 ℃, and the air inlet volume is 1m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 1.5 bar.
S6, adding 80g of hydroxypropyl cellulose (HPC-SL) into 600g of water while stirring, and continuously stirring until the solution is clear to obtain a second isolation coating solution for later use.
S7, placing 1000g of the material B in a fluidized bed, heating to 40 ℃, preheating for 5min, coating the material B with 680g of second isolation coating liquid, and drying until the moisture content is lower than 2% to obtain a material C; wherein the coating treatment conditions in this step are as follows: the material temperature is 39 ℃, the air inlet temperature is 60 ℃, the air outlet temperature is 35 ℃, and the air inlet volume is 1m3Min/kg, liquid supply speed of 10g/min/kg, atomization pressureIt was 1.5 bar.
S8, slowly adding 100g of acrylic resin gastric-soluble material into a mixed solvent of 50g of water and 850g of acetone, and stirring for 40min to obtain a solution A; then, adding 15g of triethyl citrate and 50g of talcum powder into 650g of acetone, and stirring for 120min to obtain a solution B; and then, uniformly mixing the solution A and the solution B to obtain gastric-soluble coating liquid for later use. The acrylic resin gastric soluble material can be commercially available Esterqi E100.
S9, placing 1000g of the material C in a fluidized bed, heating to 35 ℃, preheating for 5min, coating the material C with 1715g of gastric-soluble coating liquid, and drying until the water content is lower than 2% to obtain the aspirin composition; wherein the coating treatment conditions in this step are as follows: the material temperature is 30 ℃, the air inlet temperature is 55 ℃, the air outlet temperature is 40 ℃, and the air inlet volume is 1m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 1.5 bar.
Example 2
This embodiment provides an aspirin composition, the preparation method of which includes the steps of:
s1, taking aspirin as a raw material medicine; wherein, the particle size of 80% of the raw material medicine can be controlled between 80-100 meshes.
S2, adding 50g of polyvinylpyrrolidone (K30) into 500g of ethanol while stirring, continuously stirring until the solution is clear, and adding 50g of talcum powder to prepare a suspension to obtain a first isolation coating solution for later use.
S3, placing 1000g of the raw material medicines into a fluidized bed, coating the raw material medicines with 600g of first isolation coating liquid, and drying until the water content is lower than 2% to obtain a material A; wherein the coating treatment conditions in this step are as follows: the material temperature is 30 ℃, the air inlet temperature is 50 ℃, the air outlet temperature is 25 ℃, and the air inlet quantity is 0.5m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 0.5 bar.
S4, adding 10.8g of triethyl citrate and 48g of talcum powder into 223g of water, carrying out high-speed shearing for 10min, adding 318g of acrylic resin enteric material, and stirring while adding to obtain the enteric coating solution for later use. As the acrylic resin enteric material, commercially available Equidz L30D-55 (30% aqueous dispersion) can be specifically used.
S5, placing 1000g of the material A in a fluidized bed, heating to 40 ℃, preheating for 5min, then coating the material A with 599.8g of enteric coating solution, and drying until the water content is lower than 2% to obtain a material B; wherein the coating treatment conditions in this step are as follows: the material temperature is 38 ℃, the air inlet temperature is 55 ℃, the air outlet temperature is 30 ℃, and the air inlet quantity is 0.5m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 0.5 bar.
S6, adding 60g of hydroxypropyl cellulose (HPC-SL) into 600g of water while stirring, and continuously stirring until the solution is clear to obtain a second isolation coating solution for later use.
S7, placing 1000g of the material B in a fluidized bed, heating to 40 ℃, preheating for 5min, coating the material B with 660g of second isolation coating liquid, and drying until the moisture content is lower than 2% to obtain a material C; wherein the coating treatment conditions in this step are as follows: the material temperature is 38 ℃, the air inlet temperature is 55 ℃, the air outlet temperature is 30 ℃, and the air inlet quantity is 0.5m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 0.5 bar.
S8, slowly adding 100g of acrylic resin gastric-soluble material into a mixed solvent of 50g of water and 850g of acetone, and stirring for 40min to obtain a solution A; then, adding 15g of triethyl citrate and 50g of talcum powder into 650g of acetone, and stirring for 120min to obtain a solution B; and then, uniformly mixing the solution A and the solution B to obtain gastric-soluble coating liquid for later use. The acrylic resin gastric soluble material can be commercially available Esterqi E100.
S9, placing 1000g of the material C in a fluidized bed, heating to 35 ℃, preheating for 5min, coating the material C with 1715g of gastric-soluble coating liquid, and drying until the water content is lower than 2% to obtain the aspirin composition; wherein the coating treatment conditions in this step are as follows: the material temperature is 26Air inlet temperature of 50 ℃, air outlet temperature of 25 ℃ and air inlet quantity of 0.5m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 0.5 bar.
Example 3
This embodiment provides an aspirin composition, the preparation method of which includes the steps of:
s1, taking aspirin as a raw material medicine; wherein, the particle size of 80% of the raw material medicine can be controlled between 80-100 meshes.
S2, 20g of hydroxypropyl methyl cellulose is added into a mixed solvent of 280g of water and 300g of ethanol while stirring, stirring is continued until the solution is clear, and then 50g of silicon dioxide and 50g of talcum powder are added and mixed to prepare a suspension, so that a first isolation coating solution is obtained for later use.
S3, placing 1000g of the raw material medicines into a fluidized bed, coating the raw material medicines with 648g of first isolation coating liquid, and drying until the water content is lower than 2% to obtain a material A; wherein the coating treatment conditions in this step are as follows: the material temperature is 35 ℃, the air inlet temperature is 65 ℃, the air outlet temperature is 40 ℃, and the air inlet volume is 1.8m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 2.0 bar.
S4, adding 10g of phthalate and 10g of silicon dioxide into a mixed solvent of 200g of water and 230g of ethanol, carrying out high-speed shearing for 10min, adding 500g of acrylic resin enteric material and 50g of hydroxypropyl methyl cellulose phthalate while stirring to obtain the enteric coating solution for later use. As the acrylic resin enteric material, commercially available Equidz L30D-55 (30% aqueous dispersion) can be specifically used.
S5, placing 1000g of the material A in a fluidized bed, heating to 40 ℃, preheating for 5min, then coating the material A with 1000g of enteric coating liquid, and drying until the water content is lower than 2% to obtain a material B; wherein the coating treatment conditions in this step are as follows: the material temperature is 40 ℃, the air inlet temperature is 65 ℃, the air outlet temperature is 40 ℃, and the air inlet volume is 1.8m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 2.0 bar.
S6, adding 50g of xanthan gum into 950g of water while stirring, and continuously stirring until the solution is clear to obtain a second isolation coating solution for later use.
S7, placing 1000g of the material B in a fluidized bed, heating to 40 ℃, preheating for 5min, coating the material B with 1000g of second isolation coating liquid, and drying until the moisture content is lower than 2% to obtain a material C; wherein the coating treatment conditions in this step are as follows: the material temperature is 40 ℃, the air inlet temperature is 65 ℃, the air outlet temperature is 40 ℃, and the air inlet volume is 1.8m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 2.0 bar.
S8, slowly adding 100g of acrylic resin gastric-soluble material into a mixed solvent of 200g of water, 600g of acetone and 200g of isopropanol, and stirring for 40min to obtain a solution A; then, 10g of phthalate and 100g of silicon dioxide are added into 790g of isopropanol and stirred for 120min to obtain a solution B; and then, uniformly mixing the solution A and the solution B to obtain gastric-soluble coating liquid for later use. The acrylic resin gastric soluble material can be commercially available Esterqi E100.
S9, placing 1000g of the material C in a fluidized bed, heating to 35 ℃, preheating for 5min, coating the material C with 900g of gastric-soluble coating liquid, and drying until the water content is lower than 2% to obtain the aspirin composition; wherein the coating treatment conditions in this step are as follows: the material temperature is 32 ℃, the air inlet temperature is 60 ℃, the air outlet temperature is 50 ℃, and the air inlet volume is 1.8m3Min/kg, liquid supply speed of 10g/min/kg, and atomization pressure of 2.5 bar.
Example 4
This embodiment provides an aspirin composition, the preparation method of which includes the steps of:
s1, taking aspirin as a raw material medicine; wherein, the particle size of 80% of the raw material medicine can be controlled between 80-100 meshes.
S2, adding 150g of hydroxypropyl methyl cellulose, 50g of polyvinylpyrrolidone and 50g of acacia gum into 740g of water while stirring, continuously stirring until the solution is clear, adding 10g of silicon dioxide, and uniformly mixing to obtain a first isolation coating solution for later use.
S3, placing 1000g of the raw material medicines into a fluidized bed, coating the raw material medicines with 650g of first isolation coating liquid, and drying until the water content is lower than 2% to obtain a material A; wherein the coating treatment conditions in this step were the same as in example 1.
S4, adding 50g of triethyl citrate, 50g of phthalate and 100g of silicon dioxide into 692g of water, shearing at high speed for 10min, adding 50g of cellulose acetate phthalate, 50g of polyvinyl alcohol phthalate, 4g of sodium dodecyl sulfate and 4g of Tween, stirring while adding to obtain the enteric coating solution for later use.
S5, placing 1000g of the material A in a fluidized bed, heating to 40 ℃, preheating for 5min, then coating the material A with 1000g of enteric coating liquid, and drying until the water content is lower than 2% to obtain a material B; wherein the coating treatment conditions in this step were the same as in example 1.
S6, adding 100g of hydroxypropyl methylcellulose, 50g of xanthan gum and 50g of arabic gum into 800g of water while stirring, and continuously stirring until the solution is clear to obtain a second isolation coating solution for later use.
S7, placing 1000g of the material B in a fluidized bed, heating to 40 ℃, preheating for 5min, coating the material B with 800g of second isolation coating liquid, and drying until the moisture content is lower than 2% to obtain a material C; wherein the coating treatment conditions in this step were the same as in example 1.
S8, slowly adding 200g of acrylic resin gastric-soluble material and 10g of sodium dodecyl sulfate into a mixed solvent of 100g of water and 900g of acetone, and stirring for 40min to obtain a solution A; then, 160g of triethyl citrate and 40g of silicon dioxide are added into 590g of acetone and stirred for 120min to obtain a solution B; and then, uniformly mixing the solution A and the solution B to obtain gastric-soluble coating liquid for later use. The acrylic resin gastric soluble material can be commercially available Esterqi E100.
S9, placing 1000g of the material C in a fluidized bed, heating to 35 ℃, preheating for 5min, coating the material C with 1300g of gastric-soluble coating liquid, and drying until the water content is lower than 2% to obtain the aspirin composition; wherein the coating treatment conditions in this step were the same as in example 1.
Example 5
This embodiment provides an aspirin composition, the preparation method of which includes the steps of:
s1, taking aspirin as a raw material medicine; wherein, the particle size of 80% of the raw material medicine can be controlled between 80-100 meshes.
S2, adding 100g of hydroxypropyl cellulose and 35g of polyvinylpyrrolidone into a mixed solvent of 350g of water and 360g of ethanol while stirring, continuously stirring until the solution is clear, adding 155g of talcum powder, and uniformly mixing to obtain a first isolation coating solution for later use.
S3, placing 1000g of the raw material medicines into a fluidized bed, coating the raw material medicines with 400g of first isolation coating liquid, and drying until the water content is lower than 2% to obtain a material A; wherein the coating treatment conditions in this step were the same as in example 1.
S4, adding 55g of phthalate and 55g of talcum powder into 535g of water, carrying out high-speed shearing for 10min, then adding 200g of acrylic resin enteric material, 50g of hydroxypropyl methyl cellulose phthalate, 100g of cellulose acetate phthalate and 5g of sodium dodecyl sulfate while stirring to obtain the enteric coating solution for later use. As the acrylic resin enteric material, commercially available Equidz L30D-55 (30% aqueous dispersion) can be specifically used.
S5, placing 1000g of the material A in a fluidized bed, heating to 40 ℃, preheating for 5min, then coating the material A with 700g of enteric coating solution, and drying until the water content is lower than 2% to obtain a material B; wherein the coating treatment conditions in this step were the same as in example 1.
S6, adding 120g of hydroxypropyl methyl cellulose into 880g of water while stirring, and continuously stirring until the solution is clear to obtain a second isolation coating solution for later use.
S7, placing 1000g of the material B in a fluidized bed, heating to 40 ℃, preheating for 5min, coating the material B with 1000g of second isolation coating liquid, and drying until the moisture content is lower than 2% to obtain a material C; wherein the coating treatment conditions in this step were the same as in example 1.
S8, slowly adding 150g of acrylic resin gastric-soluble material and 5g of Tween into a mixed solvent of 100g of water and 900g of acetone, and stirring for 40min to obtain a solution A; then, 80g of phthalate and 70g of talcum powder are added into 695g of acetone and stirred for 120min to obtain a solution B; and then, uniformly mixing the solution A and the solution B to obtain gastric-soluble coating liquid for later use. The acrylic resin gastric soluble material can be commercially available Esterqi E100.
S9, placing 1000g of the material C in a fluidized bed, heating to 35 ℃, preheating for 5min, coating the material C with 1100g of gastric-soluble coating liquid, and drying until the water content is lower than 2% to obtain the aspirin composition; wherein the coating treatment conditions in this step were the same as in example 1.
Experimental example:
the aspirin composition prepared in the above example 1 was placed in different media for dissolution measurement, and the specific dissolution conditions were as follows: under the condition that the rotating speed is 50rpm, completing the aspirin composition in 500mL of aqueous medium within 30min, then adding hydrochloric acid to adjust the pH to 1.2, the volume to 600mL, and in acid medium for 90min, and then adjusting the pH to 6.8, the volume to 900 mL; the dissolution behavior of the sample was measured, and the measurement results are shown in FIG. 1.
As can be seen from FIG. 1, the aspirin composition prepared in example 1 dissolved out in an aqueous medium (solution preparation conditions) for 30min, and the dissolution rate was less than 10%; dissolving in gastric juice (pH 1.2) for 120min to obtain a dissolution amount of less than 10%; the dissolution rate in intestinal tract (pH 6.8) is more than 80% within 30 min.
The above-mentioned embodiments only express several embodiments of the present invention, and the description thereof is more specific and detailed, but not construed as limiting the scope of the present invention. It should be noted that, for a person skilled in the art, several variations and modifications can be made without departing from the inventive concept, which falls within the scope of the present invention. Therefore, the protection scope of the present patent shall be subject to the appended claims.
Claims (10)
1. An aspirin composition comprising aspirin, further comprising:
an enteric coating layer comprising an enteric material for dissolution in intestinal fluid and not in the stomach;
a first isolation coating layer disposed between the aspirin and the enteric coating layer; the first release coating layer comprises a binder;
a gastro-soluble coating layer comprising a gastro-soluble material for dissolution in the stomach and insoluble in water and intestinal fluids; and
a second isolating coating layer for isolating the gastric coating layer from the enteric coating layer; the second release coat layer includes an adhesive.
2. An aspirin composition according to claim 1, wherein the enteric material is at least one of acrylic resin based enteric material, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, polyvinyl alcohol phthalate.
3. An aspirin composition in accordance with claim 1, wherein the binding agent is at least one of hydroxypropylmethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, xanthan gum, gum arabic.
4. An aspirin composition in accordance with claim 1, wherein said gastric soluble material is an acrylic gastric soluble material.
5. A process for preparing an aspirin composition as claimed in any one of claims 1-4, comprising the steps of:
taking aspirin as a raw material medicine;
preparing a first isolation coating solution from an adhesive;
coating the raw material medicine by using first isolation coating liquid to form a first isolation coating layer to obtain a material A;
preparing enteric coating solution from enteric materials;
coating the material A with an enteric coating solution to form an enteric coating layer to obtain a material B;
preparing a second isolation coating solution by using an adhesive;
coating the material B with a second isolation coating solution to form a second isolation coating layer to obtain a material C;
preparing gastric-soluble coating liquid from gastric-soluble materials;
and (3) coating the material C with a gastric-soluble coating solution to form a gastric-soluble coating layer to obtain the aspirin composition.
6. A process for preparing an aspirin composition in accordance with claim 5, wherein:
the first isolation coating liquid comprises the following components in percentage by mass: 2-25% of adhesive, 1-20% of anti-sticking agent and the balance of solvent, wherein the sum of the mass percentages of the components is 100%;
the enteric coating solution comprises the following components in percentage by mass: 10-55% of enteric material, 1-10% of plasticizer, 1-10% of anti-sticking agent, 0-0.8% of surfactant and the balance of solvent, wherein the sum of the mass percentages of the components is 100%;
the second isolation coating liquid comprises the following components in percentage by mass: 5-20% of adhesive, and the balance of solvent, wherein the sum of the mass percentages of the components is 100%;
the gastric coating solution comprises the following components in percentage by mass: 5-10% of gastric soluble material, 0.5-8% of plasticizer, 2-5% of anti-sticking agent, 0-0.5% of surfactant and the balance of solvent, wherein the sum of the mass percentages of the components is 100%.
7. A process for preparing an aspirin composition in accordance with claim 6, wherein:
the solvent is at least one of water, ethanol, acetone and isopropanol;
the anti-sticking agent is silicon dioxide and/or talcum powder;
the plasticizer is citric acid ester and/or phthalic acid ester;
the surfactant is sodium dodecyl sulfate and/or tween.
8. A process for preparing an aspirin composition in accordance with claim 5, wherein:
the weight of the first isolation coating layer is 5-15% of the weight of the raw material medicine;
the weight of the enteric coating layer is 12 to 30 percent of the weight of the material A;
the weight of the second isolation coating layer is 5-15% of the weight of the material B;
the weight of the gastric-soluble coating layer is 7-25% of the weight of the material C.
9. An aspirin composition produced by the production method according to any one of claims 5 to 8.
10. Use of the aspirin composition according to any one of claims 1 to 4 and claim 9 in the preparation of a medicament for the prophylaxis of thrombosis in children.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669918A (en) * | 2008-09-11 | 2010-03-17 | 北京科信必成医药科技发展有限公司 | Aspirin double-releasing preparation and preparation method thereof |
| CN102641254A (en) * | 2012-05-07 | 2012-08-22 | 山东新华制药股份有限公司 | Preparation method of aspirin enteric-coated sustained-release preparation |
| CN104800183A (en) * | 2015-04-14 | 2015-07-29 | 南京多宝生物科技有限公司 | Aspirin enteric-coated tablet as well as preparation method and application thereof |
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2020
- 2020-08-04 CN CN202010770610.5A patent/CN111870606A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669918A (en) * | 2008-09-11 | 2010-03-17 | 北京科信必成医药科技发展有限公司 | Aspirin double-releasing preparation and preparation method thereof |
| CN102641254A (en) * | 2012-05-07 | 2012-08-22 | 山东新华制药股份有限公司 | Preparation method of aspirin enteric-coated sustained-release preparation |
| CN104800183A (en) * | 2015-04-14 | 2015-07-29 | 南京多宝生物科技有限公司 | Aspirin enteric-coated tablet as well as preparation method and application thereof |
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