CN111150710B - Medicament composition of high-load lubricant and preparation method thereof - Google Patents

Medicament composition of high-load lubricant and preparation method thereof Download PDF

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CN111150710B
CN111150710B CN202010072048.9A CN202010072048A CN111150710B CN 111150710 B CN111150710 B CN 111150710B CN 202010072048 A CN202010072048 A CN 202010072048A CN 111150710 B CN111150710 B CN 111150710B
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pharmaceutical composition
lubricant
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alkanoic acid
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CN111150710A (en
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于广华
刘宇
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

The invention provides a medicament composition of a high-load lubricant and a preparation method thereof, wherein the medicament composition of the high-load lubricant comprises the following components in parts by weight: 50-150 percent of at least one aryl alkanoic acid non-steroidal anti-inflammatory drug, 120-350 percent of at least one filling agent, 10-30 percent of at least one disintegrating agent and 4-10 percent of at least one binding agent, wherein the medicament composition also comprises a lubricating agent, and the mass percent of the lubricating agent in the medicament composition is 2.3-4 percent; the lubricant is a mixture of pregelatinized starch and sodium stearate in a weight ratio of 1-1.3: 1; according to the high-load lubricant pharmaceutical composition, sodium stearate and pregelatinized starch are selected as the lubricant, and the dosage of the lubricant is screened, so that the dissolution and disintegration of the pharmaceutical composition meet the regulations, the tensile strength of the pharmaceutical composition is remarkably improved, and the compression formability of the pharmaceutical composition is further improved.

Description

Medicament composition of high-load lubricant and preparation method thereof
Technical Field
The invention belongs to the field of pharmaceutical preparations containing organic active ingredients, and particularly relates to a pharmaceutical composition of a high-load lubricant and a preparation method thereof.
Background
Nonsteroidal anti-inflammatory Drugs (NSAIDs) are a class of anti-inflammatory Drugs that do not contain a steroidal structure and are classified by their chemical structure into salicylates such as aspirin and benorilate, acetanilides such as acetaminophen, pyrazolones such as antipyrine, 3, 5-pyrazolidinediones such as phenylbutazone, arylalkanoic acids such as indomethacin, sulindac, diclofenac sodium, ibuprofen and naproxen, anthranilic acids such as clofenamic acid, 1, 2-benzothiazines such as piroxicam, meloxicam and the like, and others such as nimesulide. The non-steroidal anti-inflammatory drug has the effects of resisting inflammation, rheumatism, pain, defervescence, anticoagulation and the like, and is widely used for clinically relieving osteoarthritis, rheumatoid arthritis, various fever and various pain symptoms.
Most of tablets marketed as aryl alkanoic acid non-steroidal anti-inflammatory drugs use stearate such as magnesium stearate as a lubricant for a formulation system. However, in the known formulation system, the loading ratio of the stearate is not preferably more than 1%, and if the loading ratio is too high, disintegration or delayed dissolution will result. In order to ensure that the disintegration and dissolution of the aryl alkanoic acid non-steroidal anti-inflammatory drug meet the requirements, the dosage of a stearate lubricant is strictly limited, and then in the preparation process of the aryl alkanoic acid non-steroidal anti-inflammatory drug tablet, the dosage of the stearate is too low to ensure good lubricating property and anti-adhesion property, so that the prepared aryl alkanoic acid non-steroidal anti-inflammatory drug tablet has low tensile strength, and the compression formability of the tablet is further influenced.
Disclosure of Invention
In order to solve the problems in the prior art, the invention provides a medicament composition of a high-load lubricant and a preparation method thereof.
One technical scheme of the invention provides a medicament composition of a high-load lubricant, which comprises the following components in parts by weight:
Figure BDA0002377545560000021
the medicament composition also comprises a lubricant, and the mass percentage of the lubricant in the medicament composition is 2.3-4%;
the lubricant is a mixture of pregelatinized starch and sodium stearate in a weight ratio of 1-1.3: 1;
the aryl alkanoic acid non-steroidal anti-inflammatory drug is selected from ibuprofen, sulindac, indomethacin or naproxen.
In a further improved scheme, the particle size distribution D of the aryl alkanoic acid nonsteroidal anti-inflammatory drug9040-60 μm, particle size distribution D of the filler75Is 40-60 μm.
In a further development, the filler is selected from mannitol, lactose, microcrystalline cellulose or corn starch, preferably mannitol.
In a further improved scheme, the disintegrant is selected from sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose or crospovidone, preferably crospovidone.
In a further improvement, the binder is selected from hydroxypropyl cellulose, sodium carboxymethyl cellulose or methyl cellulose, preferably hydroxypropyl cellulose.
In a further improved scheme, the medicament composition also comprises 3.6-4 parts by weight of starch slurry with the water content of 40-45%.
In another aspect, the present invention provides a method for preparing a lubricant-highly loaded pharmaceutical composition, comprising the steps of:
dissolving the adhesive in water to prepare a soft material;
mixing aryl alkanoic acid non-steroidal anti-inflammatory drug, filler, disintegrating agent and soft material, granulating, drying, grading, and making into granule;
the granules and the pregelatinized starch are uniformly mixed, and then are uniformly mixed with the sodium stearate, and finally the high-load lubricant pharmaceutical composition is obtained by tabletting.
In a further improved scheme, the granulation is the granulation by sieving with a 60-mesh sieve to obtain the material with the bulk density of 150-180kg/m3The coarse particles of (3).
In a further improvement, the whole granules are sieved by 80-mesh and 120-mesh sieves, and granules between 80 meshes and 120 meshes are collected.
In a further improved scheme, the aryl alkanoic acid non-steroidal anti-inflammatory drug, the filling agent, the disintegrating agent and the soft material are uniformly mixed, granulated, dried and granulated to obtain granules: uniformly mixing the aryl alkanoic acid non-steroidal anti-inflammatory drug and the starch slurry to prepare a mixture; the filling agent, the disintegrating agent and the soft material are mixed evenly and then mixed with the mixture evenly.
The invention provides a medicament composition with a high-load lubricant and a preparation method thereof.
Detailed Description
Examples 1 to 6 and comparative examples 1 to 5 provide a lubricant-loaded pharmaceutical composition, preferably a tablet, comprising the components and amounts of the examples and comparative examples of the lubricant-loaded pharmaceutical composition shown in table 1.
TABLE 1 Components and amounts of highly lubricant-loaded pharmaceutical compositions of the examples and comparative examples
Figure BDA0002377545560000041
Figure BDA0002377545560000051
The preparation process of the tablets provided in the above examples and comparative examples is as follows:
dissolving an adhesive in water to prepare a soft material with the mass fraction of 2%;
uniformly mixing the aryl alkanoic acid non-steroidal anti-inflammatory drug, the filling agent and the disintegrating agent with the soft material, granulating, drying and finishing granules;
mixing the granules with lubricant, and tabletting.
Experiment 1 tensile strength test of the pharmaceutical composition provided in each example and comparative example
The tensile strength of the tablets provided in examples 1 to 6 and comparative examples 1 to 5 was measured, and the results are shown in Table 2.
The Tensile strength (Ts) is expressed as a breaking force per unit area, and is calculated as follows:
Ts＝2F/(π·D·L)
wherein F-the force required to break the tablet radially, kN;
d-diameter of the tablet, m;
l-thickness of the tablet, m.
TABLE 2 tensile Strength test results of tablets of examples and comparative examples
Tablet formulation Tensile Strength (kPa)
Example 1 2.53
Example 2 2.61
Example 3 2.60
Example 4 2.09
Example 5 2.28
Example 6 2.16
Comparative example 1 1.25
Comparative example 2 1.79
Comparative example 3 2.05
Comparative example 4 1.57
Comparative example 5 2.46
As can be seen from the table, the tablets provided in examples 1 and 6 both have a tensile strength greater than 2kPa, which suggests that the selection of sodium stearate and pregelatinized starch as the mixed lubricant can improve the tensile strength of the aryl alkanoic acid based nsaid, but not all of the tensile strengths can be significantly improved, and the tensile strengths of different aryl alkanoic acid based nsaids vary in magnitude; comparative example 1, which did not contain pregelatinized starch in the lubricant, had a significantly reduced tablet tensile strength compared to example 3; comparative examples 2 and 3 compared to example 3, when the amount of pregelatinized starch was too low or too high, the tensile strength of the tablet was significantly affected; comparative example 4 has a significantly reduced tensile strength when the amount of sodium stearate used is low, compared to example 3; comparative example 5 has no effect on tensile strength when the amount of sodium stearate is high, compared with example 3.
Experiment 2 dissolution and disintegration experiments of examples and comparative examples
The dissolution rates and disintegrations of the tablets of examples 1 to 6 and comparative examples 1 to 5 were measured, and the results are shown in Table 3.
The disintegration degree is detected according to a method of Chinese pharmacopoeia 2010 edition: taking 6 tablets, respectively placing the tablets in glass tubes of hanging baskets, starting a disintegration tester for inspection, and calculating the average disintegration of the 6 tablets.
The dissolution rate is detected according to a method of 2010 version Chinese pharmacopoeia: measuring 900mL of degassed solvent, injecting into each operation container, heating to maintain the temperature of the solvent at 37 + -0.5 deg.C, and regulating rotation speed to stabilize the solvent. Taking 6 test samples, respectively putting into 6 rotating baskets, lowering the rotating baskets into a container, immediately starting to time to 20min, sucking a proper amount of solution at a specified sampling point, immediately filtering through a microporous membrane with the diameter of not more than 0.8 μm, and finishing the filtering within 30s from sampling to filtering. The filtrate was taken, measured by a predetermined method in the photographic section, and the dissolution index amount of each tablet was calculated and the average value was calculated.
Table 3 dissolution and disintegration test results of each example and comparative example (n ═ 6)
Sample (I) Average degree of disintegration (min) Average dissolution index (%)
Example 1 9.5±0.82 85.4±1.2
Example 2 9.3±0.51 86.3±0.9
Example 3 9.9±0.43 85.9±1.0
Example 4 12.6±1.2 72.2±1.2
Example 5 11.1±0.92 76.1±0.8
Example 6 13.8±1.0 75.6±0.7
Comparative example 1 35.3±5.6 54.7±1.4
Comparative example 2 20.4±4.7 67.3±1.0
Comparative example 3 12.3±3.5 76.4±0.8
Comparative example 4 11.9±2.1 80.3±1.3
Comparative example 5 28.7±3.8 60.9±1.1
As can be seen from the table, the disintegration and dissolution rates of examples 1 to 6 both conform to the regulations of pharmacopoeia, but different aryl alkanoic acid nonsteroidal anti-inflammatory drugs have different disintegration and dissolution rates, wherein the disintegration and dissolution rate of sulindac tablets are better than those of other aryl alkanoic acid nonsteroidal anti-inflammatory drugs; comparative example 1 compared to example 3, when pregelatinized starch was not present in the tablet and the amount of sodium stearate exceeded 1%, the disintegration and dissolution of the tablet was retarded; comparative example 2 compared to example 3, when the amount of pregelatinized starch is too low, the disintegration and dissolution of the tablet will also be affected, making the degree of disintegration not in compliance with pharmacopoeia standards; comparative example 3 when the amount of pregelatinized starch was too high, the dissolution rate and dissolution rate were not much affected, but the dissolution rate and disintegration rate of the tablet were slightly decreased, as compared with example 3; comparative example 4 compared with example 3, when the amount of sodium stearate is 1%, there is no influence on the disintegration and dissolution of the tablet; comparative example 5 when the amount of sodium stearate used was too high as compared with example 3, even the pregelatinized starch was contained, resulting in delayed dissolution and disintegration of the tablet.
Stearate such as sodium stearate is a common tablet lubricant, and when the dosage exceeds 1%, the dissolution and disintegration of the tablet are affected, but when the dosage is less than 1%, the tensile strength of the tablet is affected, and in order to balance the relationship between the tensile strength of the tablet and the dissolution and disintegration, a proper lubricant needs to be selected.
Examples 7 to 9 and comparative examples 6 to 8 provide a lubricant-highly loaded pharmaceutical composition, preferably a tablet, the components and amounts of the lubricant-highly loaded pharmaceutical composition of each example and comparative example are shown in table 3.
TABLE 3 Components and amounts of highly lubricant-loaded pharmaceutical compositions of the examples and comparative examples
Figure BDA0002377545560000081
Figure BDA0002377545560000091
The preparation process of the tablets provided in the above examples and comparative examples is as follows:
sieving the aryl alkanoic acid non-steroidal anti-inflammatory drug and the filler respectively to prepare the aryl alkanoic acid non-steroidal anti-inflammatory drug and the filler with the particle size distribution meeting the requirement;
dissolving an adhesive in water to prepare a soft material with the mass fraction of 2%;
uniformly mixing the prepared aryl alkanoic acid non-steroidal anti-inflammatory drug, the filler and the disintegrant with the soft material, granulating, drying and finishing;
mixing the granules with lubricant, and tabletting.
Experiment 3 friability test results
The friability of examples 7-9 and comparative examples 6-8 was measured and the results are shown in Table 4.
The friability is detected according to the method of 2010 version of Chinese pharmacopoeia: taking several tablets with weight of 0.65g or less to make the total weight of the tablets about 0.65 g; taking 10 tablets when the weight of the tablets is more than 0.65 g. The powder that has fallen off is blown off with a blower, precisely weighed, placed in a cylinder and rotated 100 times. Taking out, removing powder by the same method, precisely weighing, reducing weight not more than 1%, and not detecting fracture, crack and crushed sheet.
TABLE 4 friability test results for each example and control
Figure BDA0002377545560000092
Figure BDA0002377545560000101
As can be seen from the table, the friability of examples 7, 8 and 9, and comparative example 7 all met the criteria, and the friability of comparative example 6 and comparative example 8 did not meet the criteria; although the friability of comparative example 7 was acceptable, the materials were not easily mixed.
In order to improve the dissolution rate of the poorly soluble drug, the particle size of the active ingredient is generally limited, and generally, the smaller the particle size (1-20 μm), the better the dissolution, the easier the mixing; however, in the present invention, by reasonably limiting the particle size distribution of the active ingredient and the filler, when the particle size of the filler having a particle size distribution of 75% is equal to that of the active ingredient having a particle size distribution of 90%, and the particle size of the filler having a particle size range of 40 to 60 μm is large, the dissolution of the tablet is not affected, the raw materials are more easily mixed, and the friability of the tablet is not affected.
Examples 10 to 11 and comparative examples 9 to 13 provide lubricant-loaded pharmaceutical compositions, preferably tablets, comprising the ingredients and amounts of the examples and comparative examples of the lubricant-loaded pharmaceutical compositions shown in table 5.
TABLE 5 Components and amounts of highly lubricant-loaded pharmaceutical compositions of the examples and comparative examples
Figure BDA0002377545560000102
The preparation process of the tablets provided in the above examples and comparative examples is as follows:
dissolving an adhesive in water to prepare a soft material with the mass fraction of 1.4%;
uniformly mixing the aryl alkanoic acid non-steroidal anti-inflammatory drug and the starch slurry to prepare a mixture; mixing the filler, disintegrant and soft material, mixing with the mixture, sieving with 60 mesh sieve, and granulating to obtain the final product with bulk density of 160kg/m3Sieving the coarse particles with 80-mesh and 120-mesh sieves to complete the particles, and collecting the particles between 80-mesh and 120-mesh sieves;
mixing the granules with pregelatinized starch, mixing with sodium stearate, and tabletting to obtain tablet.
Comparative example 11 dosage of 1000 tablets of sulindac:
Figure BDA0002377545560000111
the preparation process comprises the following steps:
dissolving 7.8g of hydroxypropyl cellulose in water to prepare a soft material with the mass fraction of 2%;
uniformly mixing 100g of sulindac with starch slurry with the water content of 45% to obtain a mixture; mixing 263.3g mannitol, 12.8g crospovidone and soft material, mixing with the mixture, sieving with 60 mesh sieve, and granulating to obtain granules with bulk density of 150kg/m3Sieving the coarse particles with 80-mesh and 120-mesh sieves to complete the particles, and collecting the particles between 80-mesh and 120-mesh sieves;
the granules were mixed with 6.6g of pregelatinized starch, then with 5.5g of sodium stearate, and tabletted to obtain tablets.
Comparative example 12 dosage of prescription of 1000 tablets of sulindac:
Figure BDA0002377545560000121
the preparation process comprises the following steps:
dissolving 7.8g of hydroxypropyl cellulose in water to prepare a soft material with the mass fraction of 1%;
uniformly mixing 100g of sulindac with starch slurry with the water content of 45% to obtain a mixture; mixing 263.3g mannitol, 12.8g crospovidone and soft material, mixing with the mixture, sieving with 60 mesh sieve, and granulating to obtain granules with bulk density of 150kg/m3Sieving the coarse particles with 80-mesh and 120-mesh sieves to complete the particles, and collecting the particles between 80-mesh and 120-mesh sieves;
the granules were mixed with 6.6g of pregelatinized starch, then with 5.5g of sodium stearate, and tabletted to obtain tablets.
Comparative example 13 prescription dosage of 1000 tablets of sulindac:
Figure BDA0002377545560000131
the preparation process comprises the following steps:
dissolving 7.8g of hydroxypropyl cellulose in water to prepare a soft material with the mass fraction of 1.4%;
uniformly mixing 100g of sulindac, starch slurry with the water content of 45%, 263.3g of mannitol, 12.8g of crospovidone and soft materials, sieving with a 60-mesh sieve for granulation, and sieving with a 80-mesh sieve for granulation;
the granules were mixed with 6.6g of pregelatinized starch, then with 5.5g of sodium stearate, and tabletted to obtain tablets.
Experiment 4 piece weight difference and whether sticking experiment is carried out
The differences in sheet weight and the sticking of examples 3, 10 to 11 and comparative examples 9 to 13 were examined, and the results are shown in Table 6.
The difference of tablet weight is determined according to the Chinese pharmacopoeia
Average weight (g) of tablets Tablet difference limit (%)
＜0.30g ±7.5
≥0.30g ±5.0
The tablet weight difference detection method comprises the following steps: and taking 20 tablets, precisely weighing the weight of each tablet, calculating the average weight of each tablet, comparing the weight of each tablet with the average weight of each tablet, wherein the number of the tablets exceeding the difference limit in the table is not more than 2, and is not 1 time of the number of the tablets exceeding the limit of 1, otherwise, judging the tablets to be unqualified.
TABLE 6 sheet weight difference and sticking test results of examples and comparative examples
Sample (I) Tablet difference (%) Whether sticking occurs or not
Example 3 ±4.25 Sticking punch
Example 10 ±1.12 Without sticking
Example 11 ±0.98 Without stickingPunching machine
Comparative example 9 ±1.05 Sticking punch
Comparative example 10 ±3.47 Without sticking
Comparative example 11 ±1.15 Sticking punch
Comparative example 12 ±2.90 Without sticking
Comparative example 13 ±2.04 Without sticking
As can be seen from the table, the tablet of example 3 meets the pharmacopoeial standards, but has a sticking phenomenon; the tablet difference of the tablets provided in example 10 and example 11 meets pharmacopeia standards, but is obviously better than that of example 3, and no sticking phenomenon occurs; the tablet differences of the comparative examples 9 and 11 are in accordance with the standard and have no significant difference with the example 10, but the sticking phenomenon occurs in the tabletting process, and the sticking phenomenon does not occur in the tabletting process of the comparative examples 10, 12 and 13, but the tablet difference is different with the example 10.
In the preparation process of the tablet, the mass fraction of the binder is usually 2-10%, and when starch slurry is used as the binder, the common concentration of the starch slurry is 8-20%; however, through experiments, the mass fraction of the adhesive is controlled to be 1.4-1.5%, and when the water content in the starch slurry is 40-45%, the sticking phenomenon of tablets can be avoided, and the difference of tablet weights can be obviously reduced.

Claims (10)

1. The medicament composition is characterized by comprising the following components in parts by weight:
at least one kind of aryl alkanoic acid as non-steroidal anti-inflammatory drug 50-150
At least one filler 120-350
At least one disintegrating agent 10-30
At least one binder 4-10
The medicament composition also comprises a lubricant, wherein the lubricant accounts for 2.3-3.2% of the mass of the medicament composition;
the lubricant is a mixture of pregelatinized starch and sodium stearate in a weight ratio of 1-1.3: 1;
the aryl alkanoic acid non-steroidal anti-inflammatory drug is selected from ibuprofen, sulindac, indomethacin or naproxen;
the particle size distribution D90 of the aryl alkanoic acid non-steroidal anti-inflammatory drug is 40-60 mu m, and the particle size distribution D75 of the filler is 40-60 mu m;
the medicament composition also comprises 3.6 to 4 weight parts of starch slurry with the water content of 40 to 45 percent.
2. The pharmaceutical composition of claim 1, wherein the filler is selected from the group consisting of mannitol, lactose, microcrystalline cellulose, and corn starch.
3. The pharmaceutical composition of claim 2, wherein the bulking agent is mannitol.
4. The pharmaceutical composition of claim 1, wherein the disintegrant is selected from sodium carboxymethyl starch, low substituted hydroxypropyl cellulose, or crospovidone.
5. The pharmaceutical composition of claim 4, wherein the disintegrant is crospovidone.
6. The pharmaceutical composition of claim 1, wherein the binder is selected from the group consisting of hydroxypropyl cellulose, sodium carboxymethyl cellulose, and methyl cellulose.
7. The pharmaceutical composition of claim 1, wherein the binder is hydroxypropylcellulose.
8. A method of preparing the pharmaceutical composition of claim 1, comprising the steps of:
dissolving the adhesive in water to prepare a soft material;
mixing aryl alkanoic acid non-steroidal anti-inflammatory drug, filler, disintegrating agent and soft material, granulating, drying, grading, and making into granule;
the granules and the pregelatinized starch are uniformly mixed, and then are uniformly mixed with the sodium stearate, and the tablet is pressed to obtain the medicament composition.
9. The method for preparing the pharmaceutical composition of claim 8, wherein the granulation is 60 mesh granulation to obtain a bulk density of 150-3The coarse particles of (3).
10. The method of preparing a pharmaceutical composition according to claim 8, wherein the whole granules are sieved through 80 mesh and 120 mesh sieves, and the granules between 80 mesh and 120 mesh are collected.
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