Deferiprone composition and preparation method thereof
By employing dry granulation and coating techniques for deferoxone compositions, the delayed efficacy of deferoxone formulations when taken after meals and the problems of sticking and adhering to the walls during the preparation process were solved, achieving rapid dissolution and improved uniformity, thereby enhancing the bioavailability of the drug.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-12-12
- Publication Date
- 2026-03-10
AI Technical Summary
Existing deferoxone formulations have a prolonged time to peak concentration and a lower serum peak concentration when taken after meals, which affects efficacy. Furthermore, the small particle size of the raw materials leads to problems with tableting and capsule filling.
By using a combination of deferoxone, polyoxyethylene stearate, colloidal silica, fillers, and lubricants, tablets or capsules are prepared through dry granulation and coating technology, which improves solubility and dissolution rate and solves the problems of sticking to the punch and the wall.
It shortens the time to peak concentration after meals, increases peak serum concentration, enhances drug efficacy, and improves the formability and uniformity of the formulation, avoiding problems with tableting and filling.
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Abstract
Description
TECHNICAL FIELD
[0001] The present application belongs to the technical field of pharmaceutical preparations, and particularly relates to a deferasirox composition and a preparation method thereof. BACKGROUND
[0002] Deferasirox is used for treating iron overload in thalassemia patients who are intolerant or unwilling to accept existing chelator treatment. Thalassemia is a common clinical genetic hemolysis in children, and the treatment method is that the children need long-term quantitative blood transfusion to ensure the concentration of hemoglobin in the body, so as to ensure the normal life of the children. However, long-term high-dose blood transfusion therapy can lead to accumulation of iron content in the body, and excessive iron can damage the liver, heart and various endocrine organs of the patient. If iron ion removal is not performed, the children will eventually still be in danger of life due to iron overload in the body. Deferasirox is a liposoluble iron chelator approved by the European Union, which can remove excess iron from the body by combining with iron, effectively promote iron excretion, and prevent the accumulation of serum iron load in blood transfusion-dependent thalassemia patients. Deferasirox has the functions of iron chelator and protective agent. Deferasirox is a deferoxamine used in clinical practice after iron removal, and is also the first oral iron chelator, which can effectively promote iron excretion and prevent the accumulation of serum iron load in blood transfusion-dependent thalassemia patients. In vivo and in vitro studies have shown that deferasirox can remove intracellular iron, reticuloendothelial system iron, transferrin-bound iron, and iron stored in the form of ferritin and hemosiderin.
[0003] The existing deferasirox preparations mainly include tablets and oral solutions. The deferasirox tablets can be quickly absorbed after oral administration, especially when administered on an empty stomach, the peak concentration can be reached within 45-60 min. However, when administered after a meal, the peak time is prolonged to 2 h. Although the postprandial administration does not reduce the total amount of absorption, the serum peak concentration after the postprandial administration is lower than that of the fasting administration. The half-life of deferasirox is 2-3 h, and the inactivation is mainly through glucuronidation metabolism, and the total dose of 75%-90% is excreted with urine within 24 h after administration, in the form of original form, glucuronidation metabolites and iron-deferasirox complex. Studies have shown that in people with renal dysfunction, the renal clearance rate of deferasirox decreases, but the systemic clearance rate does not decrease. Since deferasirox is administered after a meal, the peak time is prolonged to 2 h, and the serum peak concentration is lower than that of the fasting administration, which leads to slow drug onset and even reduced drug efficacy. Therefore, it is necessary to reduce the loss of first-pass effect and food interference, so that the drug can quickly pass through the stomach into the intestine for absorption, reduce the opportunity of being degraded or combined with food in the stomach, and thus increase the amount of drug entering the systemic circulation. Moreover, when preparing tablets, due to the small particle size of the deferasirox raw material, sticking and punching problems easily occur during tabletting, which affects the surface density and uniformity of the tablets. When preparing capsules, the particles are easily stuck to the capsule shell, which reduces the production efficiency. SUMMARY
[0004] In view of this, the present application provides a deferasirox composition and a preparation method thereof, which is prepared by granulating deferasirox, polyoxyethylene stearate and other excipients, and then into tablets or capsules, thereby improving the drug dissolution rate and solving the tablet sticking and bumping problem caused by the small particle size of the deferasirox raw material.
[0005] To solve the above technical problems, the present application provides a deferasirox composition, which comprises, by weight fraction: 50-70 parts of deferasirox, 0.1-2 parts of polyoxyethylene stearate, 0.1-2 parts of colloidal silicon dioxide, 25-40 parts of a filler and 0.1-2 parts of a lubricant.
[0006] The deferasirox composition provided by the present application contains non-ionic surfactant polyoxyethylene stearate, which contains both lipophilic and hydrophilic ends. The lipophilic end molecular chain can wrap the deferasirox molecules to form micelles, and has a low critical micelle concentration. The hydrophilic end molecular chain can disperse the micelles in the aqueous medium, thereby increasing the solubility of the deferasirox liposoluble molecules in gastric juice and intestinal juice. The deferasirox composition provided by the present application significantly improves the dissolution and dissolution of deferasirox, shortens the peak time when taken after meals, increases the serum peak concentration, and enhances the drug efficacy.
[0007] In combination with the first aspect, the deferasirox composition comprises, by weight fraction: 50-60 parts of deferasirox, 0.1-1.5 parts of polyoxyethylene stearate, 0.1-1 parts of colloidal silicon dioxide, 28-35 parts of a filler and 0.5-1.5 parts of a lubricant.
[0008] In combination with the first aspect, the deferasirox composition comprises, by weight fraction: 50 parts of deferasirox, 0.2 parts of polyoxyethylene stearate, 0.1 parts of colloidal silicon dioxide, 29 parts of a filler and 0.9 parts of a lubricant.
[0009] In combination with the first aspect, the filler is selected from at least one of microcrystalline cellulose, corn starch, calcium hydrogen phosphate and lactose.
[0010] The above-mentioned filler not only adjusts the weight or dosage of the tablet or capsule, but more importantly, improves the compression molding property of the drug and improves the content uniformity.
[0011] In combination with the first aspect, the lubricant is selected from at least one of calcium stearate, sodium stearyl fumarate, stearic acid and magnesium stearate.
[0012] The above-mentioned lubricant can reduce the friction between the material and the mold wall to ensure uniform pressure distribution during tabletting and tablet pushing, and the tablet can be smoothly pushed out of the mold hole.
[0013] In combination with the first aspect, the dosage form of the deferasirox composition is a tablet or a capsule, and can also be other pharmaceutically acceptable dosage forms, such as granules or suspensions.
[0014] In combination with the first aspect, the deferasirox composition is in the form of a tablet, and the preparation method comprises the following steps: The prescription amount of the deferasirox, the filler, the polyoxyethylene stearate and the colloidal silicon dioxide are mixed and dry granulated, and the obtained granules are mixed with the lubricant to obtain deferasirox granules; the deferasirox granules are compressed to obtain a tablet core; and the tablet core is coated to obtain a deferasirox tablet.
[0015] In combination with the first aspect, in the dry granulation step, the screw feeding speed is 19-25 rpm, the pressure roller pressure is 10-40 bar, the pressure roller gap is 0.8-1.5 mm, the aperture of the crushing screen is 0.7-0.9 mm, and the crushing speed is 90-110 rpm.
[0016] In combination with the first aspect, the hardness of the tablet core is 90-150 N; the concentration of the coating liquid used for coating is 10%-15%, and the coating layer weight gain is 1%-3%.
[0017] Preferably, the coating material used comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, polyethylene glycol and titanium dioxide, etc.
[0018] In combination with the first aspect, the deferasirox composition is in the form of a capsule, and the preparation method comprises the following steps: The prescription amount of the deferasirox, the filler, the polyoxyethylene stearate and the colloidal silicon dioxide are mixed and dry granulated, and the obtained granules are mixed with the lubricant to obtain deferasirox granules; the deferasirox granules are compressed to obtain a tablet core; and the tablet core is coated to obtain a deferasirox tablet.
[0019] Preferably, the material of the capsule shell can be gelatin, plant cellulose and derivatives thereof.
[0020] The deferasirox composition provided by the application contains polyoxyethylene stearate, the polyoxyethylene stearate and the deferasirox are fully combined through dry granulation, and then film coating or capsule shell filling is performed, so that the preparation process is simple, the dissolution rate of the preparation is improved, and the in vivo absorption of the drug after meal is improved. At the same time, the polyoxyethylene stearate can also adhere to the surface of the deferasirox granules to form a "lubricating film", so that the flow resistance of the deferasirox granules is reduced, the problems of sticking and wall sticking during tablet compression and capsule filling are avoided, and the weight difference of the preparation is qualified. DETAILED DESCRIPTION
[0021] In order to make the objects, technical solutions and advantages of the present application clearer, the present application will be further described in detail below with specific examples. It should be understood that the specific examples described herein are only used to explain the present application and not to limit the present application.
[0022] Those skilled in the art can understand that, unless otherwise defined, all terms (including technical terms and scientific terms) used herein have the same meaning as commonly understood by those skilled in the art to which the present application belongs. It should also be understood that terms such as those defined in general dictionaries should be understood as having meanings consistent with those in the context of the prior art, and should not be interpreted in an idealized or overly formal sense unless specifically defined.
[0023] The raw reagents and equipment used in the present application are all conventional commercially available ordinary reagents and ordinary equipment unless otherwise specified. The deferasirox, polyoxyethylene stearate, sodium dodecyl sulfate, polysorbate 80, soybean phospholipid and α-cyclodextrin used in the following examples and comparative examples are all used after being sieved through a 100-mesh sieve.
[0024] Deferasirox is a yellow needle-shaped crystal, which is soluble in alcohol and ether solvents and slightly soluble in water. After oral administration of deferasirox, it is quickly absorbed after digestion. When administered on an empty stomach, the peak concentration can be reached in 45-60 min, but when taken after a meal, the peak time is prolonged to 2 h. Although taking with food (i.e. after a meal) does not reduce the total amount of absorption, the serum peak concentration after a meal is lower than that of fasting, which affects the onset speed of the drug. Moreover, the particle size of deferasirox raw material is small, which is prone to sticking and bumping problems during the preparation of the preparation, affecting the weight of the preparation and reducing the qualified rate of the finished product.
[0025] Therefore, the present application provides a deferasirox composition, which contains polyoxyethylene stearate. The polyoxyethylene stearate and deferasirox are fully combined by dry granulation, and then tablets are prepared by compression and coating or capsules are prepared by loading into a capsule shell. The preparation process is simple, the dissolution rate of the preparation is improved, which is helpful for the rapid in vivo absorption of the drug after oral administration after a meal. At the same time, the polyoxyethylene stearate can also adhere to the surface of the deferasirox particles to form a "lubricating film", which reduces the flow resistance of the deferasirox particles, avoids the problems of sticking and bumping during tabletting and capsule filling, and ensures the weight difference of the preparation to be qualified.
[0026] Example 1 The present example provides a deferasirox tablet, which comprises: deferasirox 500 g, microcrystalline cellulose 290 g, polyoxyethylene stearate 2 g, colloidal silicon dioxide 1 g, and magnesium stearate 9 g.
[0027] The deferasirox tablet is prepared according to the following method: The sieved deferasirox and polyoxyethylene stearate, and microcrystalline cellulose and colloidal silicon dioxide are weighed according to the set prescription and added into a dry granulator for dry granulation, with the screw feeding speed set to 23 rpm, the compression roller pressure set to 20 bar, the compression roller gap set to 1.0 mm, the crushing screen mesh size set to 0.8 mm, and the crushing speed set to 100 rpm. The magnesium stearate is weighed according to the set prescription and mixed with the granules after sizing in a three-dimensional mixer until uniform, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0028] The deferasirox granules are compressed into tablets, with the tablet core hardness controlled to be 90-150 N.
[0029] A coating liquid (the coating liquid contains hydroxypropyl methyl cellulose, polyethylene glycol and titanium dioxide) with a concentration of 12% is prepared and used for coating, with the coating layer weight gain set to 2%, to obtain 1000 deferasirox tablets.
[0030] Example 2 This example provides a deferasirox tablet, with the components including: deferasirox 500 g, microcrystalline cellulose 290 g, polyoxyethylene stearate 2 g, colloidal silicon dioxide 1 g, and magnesium stearate 9 g.
[0031] The deferasirox tablet is prepared according to the following method: The sieved deferasirox and polyoxyethylene stearate, and microcrystalline cellulose and colloidal silicon dioxide are weighed according to the set prescription and added into a dry granulator for dry granulation, with the screw feeding speed set to 20 rpm, the compression roller pressure set to 15 bar, the compression roller gap set to 1.3 mm, the crushing screen mesh size set to 0.8 mm, and the crushing speed set to 90 rpm. The magnesium stearate is weighed according to the set prescription and mixed with the granules after sizing in a three-dimensional mixer until uniform, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0032] The deferasirox granules are compressed into tablets, with the tablet core hardness controlled to be 90-150 N.
[0033] A coating liquid (the coating liquid contains hydroxypropyl methyl cellulose, polyethylene glycol and titanium dioxide) with a concentration of 10% is prepared and used for coating, with the coating layer weight gain set to 1%, to obtain 1000 deferasirox tablets.
[0034] Example 3 This example provides a deferasirox tablet, with the components including: deferasirox 500 g, corn starch 290 g, polyoxyethylene stearate 2 g, colloidal silicon dioxide 1 g, and sodium stearyl fumarate 9 g.
[0035] The deferasirox tablet is prepared according to the following method: The sieved deferasirox and polyoxyethylene stearate, and corn starch and colloidal silicon dioxide are weighed according to the set prescription and added into a dry granulator for dry granulation, with the screw feeding speed set to 23 rpm, the compression roller pressure set to 25 bar, the compression roller gap set to 1.2 mm, the crushing screen mesh size set to 0.9 mm, and the crushing speed set to 100 rpm. The sodium stearyl fumarate is weighed according to the set prescription and mixed with the granules after sizing in a three-dimensional mixer until uniform, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0036] The deferasirox granules are compressed into tablets, with the tablet core hardness controlled to 90-150 N.
[0037] A coating liquid (the coating liquid contains hydroxypropyl methyl cellulose, polyethylene glycol, and titanium dioxide) with a concentration of 15% is prepared and used for coating, with the coating layer weight gain set to 3%, to obtain 1000 deferasirox tablets.
[0038] Example 4 This example provides a deferasirox capsule, with the components including: deferasirox 500 g, microcrystalline cellulose 290 g, polyoxyethylene stearate 2 g, colloidal silicon dioxide 1 g, and magnesium stearate 9 g.
[0039] The deferasirox capsule is prepared according to the following method: The sieved deferasirox and polyoxyethylene stearate, and microcrystalline cellulose and colloidal silicon dioxide are weighed according to the set prescription and added into a dry granulator for dry granulation, with the screw feeding speed set to 23 rpm, the compression roller pressure set to 20 bar, the compression roller gap set to 1.0 mm, the crushing screen mesh size set to 0.8 mm, and the crushing speed set to 100 rpm. The sodium stearyl fumarate is weighed according to the set prescription and mixed with the granules after sizing in a three-dimensional mixer until uniform, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0040] The deferasirox granules are filled into capsule shells (the capsule shells contain gelatin) according to the amount, to obtain 1000 deferasirox capsules.
[0041] Comparative Example 1 This comparative example provides a deferasirox tablet, with the components including: deferasirox 500 g, microcrystalline cellulose 290 g, colloidal silicon dioxide 1 g, and magnesium stearate 9 g.
[0042] The deferasirox tablet is prepared according to the following method: The sieved deferasirox, microcrystalline cellulose and colloidal silicon dioxide were weighed according to the set prescription and added into a dry granulator for dry granulation, with the screw feeding speed set to 23 rpm, the compression roller pressure set to 20 bar, the compression roller gap set to 1.0 mm, the crushing screen mesh size set to 0.8 mm, and the crushing speed set to 100 rpm. The magnesium stearate was weighed according to the set prescription and mixed with the granules after the granulation in a three-dimensional mixer until uniform, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0043] The deferasirox granules were compressed into tablets, with the tablet core hardness controlled to be 90-150 N.
[0044] A coating liquid with a concentration of 12% (the coating liquid comprising hydroxypropyl methyl cellulose, polyethylene glycol and titanium dioxide) was prepared and used for coating, with the coating layer weight gain set to 2%, to obtain 1000 deferasirox tablets.
[0045] This comparative example is different from Example 1 in that no polyoxyethylene stearate was added.
[0046] Comparative Example 2 This comparative example provides a deferasirox tablet, with the components comprising: deferasirox 500 g, microcrystalline cellulose 290 g, sodium dodecyl sulfate 2 g, colloidal silicon dioxide 1 g, magnesium stearate 9 g.
[0047] The deferasirox tablet was prepared according to the following method: The sieved deferasirox and sodium dodecyl sulfate, and the microcrystalline cellulose and colloidal silicon dioxide were weighed according to the set prescription and added into a dry granulator for dry granulation, with the screw feeding speed set to 23 rpm, the compression roller pressure set to 20 bar, the compression roller gap set to 1.0 mm, the crushing screen mesh size set to 0.8 mm, and the crushing speed set to 100 rpm. The magnesium stearate was weighed according to the set prescription and mixed with the granules after the granulation in a three-dimensional mixer until uniform, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0048] The deferasirox granules were compressed into tablets, with the tablet core hardness controlled to be 90-150 N.
[0049] A coating liquid with a concentration of 12% (the coating liquid comprising hydroxypropyl methyl cellulose, polyethylene glycol and titanium dioxide) was prepared and used for coating, with the coating layer weight gain set to 2%, to obtain 1000 deferasirox tablets.
[0050] This comparative example is different from Example 1 in that the polyoxyethylene stearate was replaced with an equal amount of sodium dodecyl sulfate.
[0051] Comparative Example 3 The comparative example provides a deferasirox tablet, and the components include: deferasirox 500 g, microcrystalline cellulose 290 g, Polysorbate 80 802 g, colloidal silicon dioxide 1 g, magnesium stearate 9 g.
[0052] The deferasirox tablet is prepared according to the following method: The sieved deferasirox and soybean phospholipid, and the microcrystalline cellulose and colloidal silicon dioxide are weighed according to the set prescription and added to a dry granulator for dry granulation, and the screw feeding speed is set to 23 rpm, the pressure roller pressure is set to 20 bar, the pressure roller gap is set to 1.0 mm, the crushing screen mesh size is set to 0.8 mm, and the crushing speed is set to 100 rpm. The magnesium stearate is weighed according to the set prescription and mixed with the granules after granulation in a three-dimensional mixer to obtain deferasirox granules.
[0053] The deferasirox granules are compressed into tablets, and the tablet core hardness is controlled to be 90-150 N.
[0054] A coating liquid with a concentration of 12% (the coating liquid contains hydroxypropyl methyl cellulose, polyethylene glycol and titanium dioxide) is prepared and used for coating, and the coating layer weight gain is 2%, to obtain 1000 deferasirox tablets.
[0055] The difference between the comparative example and example 1 is that the polysorbate 80 is replaced by an equal amount of polyoxyethylene stearate.
[0056] Comparative example 4 The comparative example provides a deferasirox tablet, and the components include: deferasirox 500 g, microcrystalline cellulose 290 g, Soybean phospholipid 2 g, colloidal silicon dioxide 1 g, magnesium stearate 9 g.
[0057] The deferasirox tablet is prepared according to the following method: The sieved deferasirox and soybean phospholipid, and the microcrystalline cellulose and colloidal silicon dioxide are weighed according to the set prescription and added to a dry granulator for dry granulation, and the screw feeding speed is set to 23 rpm, the pressure roller pressure is set to 20 bar, the pressure roller gap is set to 1.0 mm, the crushing screen mesh size is set to 0.8 mm, and the crushing speed is set to 100 rpm. The magnesium stearate is weighed according to the set prescription and mixed with the granules after granulation in a three-dimensional mixer to obtain deferasirox granules.
[0058] The deferasirox granules are compressed into tablets, and the tablet core hardness is controlled to be 90-150 N.
[0059] A coating liquid with a concentration of 12% (the coating liquid contains hydroxypropyl methyl cellulose, polyethylene glycol and titanium dioxide) is prepared and used for coating, and the coating layer weight gain is 2%, to obtain 1000 deferasirox tablets.
[0060] The difference between this comparative example and Example 1 is that the polyoxyethylene stearate is replaced by an equal amount of soybean phospholipid.
[0061] Comparative Example 5 This comparative example provides a deferasirox tablet, the components of which include: deferasirox 500 g, microcrystalline cellulose 290 g, α-cyclodextrin 2 g, colloidal silicon dioxide 1 g, magnesium stearate 9 g.
[0062] The deferasirox tablet is prepared according to the following method: The deferasirox and α-cyclodextrin after sieving, and the microcrystalline cellulose and colloidal silicon dioxide are weighed according to the set prescription and added to a dry granulator for dry granulation, with the screw feeding speed set to 23 rpm, the compression roller pressure set to 20 bar, the compression roller gap set to 1.0 mm, and the crushing screen mesh size set to 0.8 mm and the crushing speed set to 100 rpm. The magnesium stearate is weighed according to the set prescription and mixed with the granules after sizing in a three-dimensional mixer for uniform mixing, with the mixing speed set to 10 rpm and the mixing time set to 5 minutes, to obtain deferasirox granules.
[0063] The deferasirox granules are compressed into tablets, with the tablet core hardness controlled at 90-150 N.
[0064] A coating liquid with a concentration of 12% (the coating liquid contains hydroxypropylmethyl cellulose, polyethylene glycol, and titanium dioxide) is prepared for coating, with the coating layer weight gain set to 2%, to obtain 1000 deferasirox tablets.
[0065] The difference between this comparative example and Example 1 is that the polyoxyethylene stearate is replaced by an equal amount of α-cyclodextrin.
[0066] Test Example 1 The hardness test and appearance comparison of the deferasirox compositions obtained in Examples 1-4 and Comparative Examples 1-5 are shown in Table 1.
[0067] Table 1
[0068] As can be seen from Table 1, the addition of polyoxyethylene stearate can make the tablet surface smooth and neat, and the deferasirox capsule surface clean, smooth, and with a qualified loading amount.
[0069] Test Example 2 The deferasirox tablets obtained in Examples 1-3 and Comparative Examples 1-5 are tested for disintegration time according to the Disintegration Time Test Method in the Fourth Part of the Chinese Pharmacopoeia 2025, with the results shown in Table 2.
[0070] Table 2
[0071] As can be seen from Table 2, compared with no addition of polyoxyethylene stearic acid ester and addition of other surfactants, the polyoxyethylene stearic acid ester can significantly shorten the disintegration time of the deferasirox composition.
[0072] Test Example 3 The dissolution rates of the deferasirox compositions of Example 1, Example 4 and Comparative Examples 1-5 were determined by using the dissolution curves of artificial postprandial gastric juice and intestinal juice as indexes, respectively, and the results are shown in Table 3 and Table 4, respectively.
[0073] Table 3 Results of artificial postprandial gastric juice dissolution curves
[0074] Table 4 Results of artificial postprandial intestinal juice dissolution curves
[0075] As can be seen from Table 3 and Table 4, compared with no addition of polyoxyethylene stearic acid ester and addition of other surfactants, after the addition of polyoxyethylene stearic acid ester, the dissolution curves of the deferasirox compositions of Example 1 and Example 4 in the artificial postprandial gastric juice and the artificial postprandial intestinal juice are obviously superior to those of Comparative Examples 1-5, which indicates that the deferasirox composition provided by the present application can be dissolved more quickly and at the same time solves the problems of sticking and walling in the processes of tabletting and capsule shell filling.
[0076] The above description is merely preferred specific embodiments of the present application, but the protection scope of the present application is not limited thereto, and any person skilled in the art can make equivalent replacements or changes to the technical solutions and the inventive concept of the present application within the technical scope disclosed by the present application, which should be covered within the protection scope of the present application.
Claims
1. A deferiprone composition, characterized in that, The deferiprone composition comprises 50-70 parts by weight of deferiprone, 0.1-2 parts by weight of polyoxyethylene stearate, 0.1-2 parts by weight of colloidal silicon dioxide, 25-40 parts by weight of a filler and 0.1-2 parts by weight of a lubricant.
2. The deferiprone composition of claim 1, wherein, The deferiprone composition comprises 50-60 parts by weight of deferiprone, 0.1-1.5 parts by weight of polyoxyethylene stearate, 0.1-1 parts by weight of colloidal silicon dioxide, 28-35 parts by weight of a filler and 0.5-1.5 parts by weight of a lubricant.
3. The deferiprone composition of claim 2, wherein, The deferiprone composition comprises 50 parts by weight of deferiprone, 0.2 parts by weight of polyoxyethylene stearate, 0.1 parts by weight of colloidal silicon dioxide, 29 parts by weight of a filler and 0.9 parts by weight of a lubricant.
4. The deferiprone composition according to any one of claims 1 to 3, wherein The filler is at least one selected from the group consisting of microcrystalline cellulose, corn starch, calcium hydrogen phosphate and lactose.
5. The deferiprone composition according to any one of claims 1 to 3, wherein The lubricant is at least one selected from the group consisting of calcium stearate, sodium stearyl fumarate, stearic acid and magnesium stearate.
6. The deferiprone composition according to any one of claims 1 to 3, wherein The deferiprone composition is in the form of tablets, capsules, granules or suspensions.
7. The deferiprone composition of claim 6, wherein the composition is a tablet. The deferiprone composition is in the form of tablets, and the preparation method comprises the following steps: mixing the prescription amount of deferiprone, filler, polyoxyethylene stearate and colloidal silicon dioxide, and then performing dry granulation, mixing the obtained granules with the lubricant to obtain deferiprone granules; compressing the deferiprone granules to obtain tablet cores; coating the tablet cores to obtain deferiprone tablets.
8. The deferiprone composition of claim 7, wherein, In the dry granulation step, the screw feeding speed is 19-25 rpm, the pressure roller pressure is 10-40 bar, the pressure roller gap is 0.8-1.5 mm, the aperture of the pulverizing screen is 0.7-0.9 mm, and the pulverizing speed is 90-110 rpm.
9. The deferiprone composition of claim 7, wherein, The hardness of the tablet core is 90-150 N, and the coating layer weight gain is 1%-3%.
10. The deferiprone composition of claim 6, wherein, The deferiprone composition is in the form of capsules, and the preparation method comprises the following steps: mixing the prescription amount of deferiprone, filler, polyoxyethylene stearate and colloidal silicon dioxide, and then performing dry granulation, mixing the obtained granules with the lubricant to obtain deferiprone granules; filling the deferiprone granules into capsule shells to obtain deferiprone capsules.