CN111773194B - Canagliflozin tablet and preparation method thereof - Google Patents
Canagliflozin tablet and preparation method thereof Download PDFInfo
- Publication number
- CN111773194B CN111773194B CN201910271445.6A CN201910271445A CN111773194B CN 111773194 B CN111773194 B CN 111773194B CN 201910271445 A CN201910271445 A CN 201910271445A CN 111773194 B CN111773194 B CN 111773194B
- Authority
- CN
- China
- Prior art keywords
- canagliflozin
- tablet
- granulating
- polyvinylpyrrolidone
- prescription
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Images
Classifications
-
- 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
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides a canagliflozin tablet and a preparation method thereof, wherein the canagliflozin tablet is prepared from the following raw and auxiliary materials in percentage by weight: 50-60% of canagliflozin, 32-40% of filler, 5-7% of disintegrating agent, 1-3% of adhesive and 0.5-1% of lubricant. The preparation method adopts a wet granulation process, has simple preparation process, easy operation and good reproducibility, is suitable for industrialized mass production, and the obtained canagliflozin tablet has fast dissolution and good stability of each batch.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and in particular relates to a canagliflozin tablet and a preparation method thereof.
Background
Type II diabetes mellitus, also known as non-insulin dependent diabetes mellitus, accounts for about 90% of the total number of patients with diabetes mellitus, and most of the diabetes mellitus occurs slowly after the age of 35 years, and is hidden. The main causes are overweight or obesity, hypophysical activity and stress (stress, fatigue, mental irritation, trauma, surgery, etc.), resulting in insulin secretion defects, which in turn lead to a gradual decrease in the body's sensitivity to insulin, and an increase in blood glucose, which in turn leads to the occurrence of type II diabetes.
Canagliflozin is a sodium glucose cotransporter 2 (SGLT-2) inhibitor, so that glucose in a renal tubule cannot be successfully reabsorbed into blood and discharged along with urine, thereby reducing the blood concentration, and the Canagliflozin is suitable for assisting diet and exercise therapy to improve the blood glucose control of type II diabetics. Canagliflozin tablet (Canagliflozin, trade name:
) The product is jointly developed by the American Qianssen pharmaceutical (Janssen) and the Mitsubishi field limit pharmaceutical (Mitsubishi Tanabe Pharma), and is approved by the FDA for marketing in 29 of 2013, 11 and 15 of 2013, EMA for marketing in 09 of 2017, and CFDA for marketing.
WO2008/069327A1 discloses crystalline hemihydrate of a compound of formula (I) and a process for its preparation. The document further mentions that amorphous Canaglifflozin has stability problems; WO 2011/142478 discloses a tablet and improves properties of the tablet, such as hardness, friability, by adjusting excipients; WO2011/143296 discloses a formulation of the hemihydrate Canaglifloz, the excipients comprising diluents, disintegrants, binders and lubricants. CN108078945 discloses adjuvants in the composition; none of the above prior art documents discloses stability data for the compositions. US20120115799, US20130338087 and US2015000524 disclose commercial canagliflozin compositions of invitana. Compositions disclose canagliflozin hemihydrate and also microcrystalline cellulose and lactose or silicified microcrystalline cellulose and lactose as diluents in equal proportions and exhibit good bioavailability. The stability of the formulation and the associated properties of particle flowability and friability were not investigated.
The chemical name of the canagliflozin purification is (1S) -1, 5-dehydration-1- [3- [ [5- (4-fluorophenyl) -2-thienyl ]]Methyl group]-4-methylphenyl]D-glucitol of formula C 24 H 25 FO 5 S, the relative molecular weight is: 444.5, the result formula is shown as (I).
The canagliflozin has poor water solubility, is almost insoluble in aqueous media with the pH of 1.0-8.0, and the related data and the related patent report that the crystal forms of the canagliflozin comprise a hemihydrate crystal form I, an amorphous form II, a monohydrate and a plurality of anhydrous crystal forms, wherein the hemihydrate crystal form is the most stable. The oral absolute bioavailability of canagliflozin published in the FDA specification is 65%. According to the rule of exemption guidance of bioequivalence test of human body, the canagliflozin is judged to be a low-solubility and low-permeability drug, belonging to the BCS IV drug of the biological pharmaceutical classification system. Therefore, the improvement of the in vitro dissolution rate of the preparation is the key of the curative effect, and the current technology which needs to be improved is to design a prescription and/or a preparation process in the preparation process so as to achieve the purpose of improving the dissolution rate of the canagliflozin.
Disclosure of Invention
The invention aims to overcome the defects of the prior art and provide the preparation method for the canagliflozin tablet which has good dissolution performance and high stability and is easy for industrial production.
Specifically, the invention is realized by the following technical scheme:
the tablet core consists of the canagliflozin and pharmaceutic adjuvant, wherein the pharmaceutic adjuvant is at least one of a filler, a disintegrating agent, an adhesive and a lubricant: the filler is one or more of anhydrous lactose, microcrystalline cellulose, mannitol and pregelatinized starch; the disintegrating agent is as follows: one or more of croscarmellose sodium, sodium carboxymethyl starch, hydroxypropyl cellulose, and crospovidone; the adhesive is as follows: one or more of hydroxypropyl cellulose, methylcellulose, sodium carboxymethylcellulose, and polyvinylpyrrolidone; the lubricant is as follows: one or more of magnesium stearate, talcum powder and micro powder silica gel.
The filler is preferably a mixture of microcrystalline cellulose and anhydrous lactose, the disintegrant is preferably croscarmellose sodium, the binder is preferably polyvinylpyrrolidone, and the lubricant is preferably magnesium stearate.
Preferably, the microcrystalline cellulose to anhydrous lactose ratio is 1:1-1:3, preferably 1:1.
preferably, the polyvinylpyrrolidone is 5-15% aqueous solution, preferably 7-10% aqueous solution, more preferably 7% aqueous solution, in g/mL.
The canagliflozin tablet is prepared from the following raw and auxiliary materials in percentage by weight: 50-60% of canagliflozin, 32-40% of filler, 5-7% of disintegrating agent, 1-3% of adhesive and 0.5-1% of lubricant.
The specific prescription is as follows: 50-60% of canagliflozin, 16-20% of microcrystalline cellulose, 16-20% of anhydrous lactose, 5-7% of croscarmellose sodium, 1-3% of polyvinylpyrrolidone and 0.5-1% of magnesium stearate;
preferably: 51 to 52 percent of canagliflozin, 19 to 20 percent of microcrystalline cellulose, 19 to 20 percent of anhydrous lactose, 6 to 6.5 percent of croscarmellose sodium, 2 to 2.5 percent of polyvinylpyrrolidone and 0.6 to 0.8 percent of magnesium stearate;
further preferred is: the novel medicine composition comprises 51.515% of canagliflozin, 19.697% of microcrystalline cellulose, 19.697% of anhydrous lactose, 6.061% of croscarmellose sodium, 2.273% of polyvinylpyrrolidone and 0.757% of magnesium stearate.
The specific prescription of the canagliflozin tablet is as follows:
| specification of specification | 0.1g | 0.3g |
| Name of the name | Quality (part/tablet) | Quality (part/tablet) |
| Canagliflozin | 68 | 204 |
| Anhydrous lactose | 26 | 78 |
| Microcrystalline cellulose | 26 | 78 |
| Croscarmellose sodium | 8 | 24 |
| Polyvinylpyrrolidone | 3 | 9 |
| Magnesium stearate | 1 | 3 |
Because the canagliflozin is stable to moisture, a wet granulation method is adopted to prepare the canagliflozin tablet. In addition, in the research process, it is found that the dissolution performance of the preparation is not affected by different raw material granularity, and related documents mention that the canagliflozin granularity has no influence on in vivo effects, and the granularity is controlled to ensure the consistency of the preparation process of the finished product. So in order to ensure the smooth production process of the preparation and obtain qualified products, the granularity of the canagliflozin is less than or equal to 50 μm and less than or equal to d (0.9).
It is another object of the present invention to provide a method of preparing a canagliflozin tablet in accordance with the foregoing. The preparation method comprises the following steps:
(1) Adding the adhesive into water, stirring and dissolving;
(2) Stirring and mixing the rest raw materials and auxiliary materials;
(3) Adding the adhesive into the step (2), stirring, granulating, drying and tabletting;
(4) Optionally, a coating step is also included.
The preferable scheme is as follows:
(1) Adding the adhesive into water, stirring and dissolving;
(2) Adding the prescription amount of microcrystalline cellulose, canagliflozin, a disintegrating agent and anhydrous lactose into a whole grain wet mixing granulator, and stirring and mixing;
(3) Adding a binder to the wet mix granulator of (2);
(4) Wet granulating the wet granules in the step (3);
(5) Wet granules obtained in the step (4) are subjected to wet granulation and then added into a boiling granulator for drying;
(6) Optionally, adding the intermediate obtained in the step (5) into a granulator for granulating;
(7) Adding the intermediate obtained in the step (6) into a hopper mixer, and adding a lubricant for mixing;
(8) Adding the intermediate obtained in the step (7) into a tablet press to be pressed into tablets, and preparing tablet cores;
(9) Optionally, film coating the tablet cores of step (8) with a film coating.
Wherein, the weight gain of the coating is 2.0-2.5%.
The further preferable scheme is as follows:
(1) And sieving microcrystalline cellulose and anhydrous lactose respectively for standby.
(2) Adding polyvinylpyrrolidone into water, stirring and dissolving until the polyvinylpyrrolidone is clear and transparent;
(3) Adding the prescription amount of microcrystalline cellulose, canagliflozin, croscarmellose sodium and anhydrous lactose into a whole grain wet mixing granulator, and stirring and mixing;
(4) Adding a binder to the wet granulator of (3);
(5) Wet granulating the wet granules in the step (4), and granulating at a low speed: the rotation speed of the stirring paddle is 120rpm, the rotation speed of the granulating knife is 1200rpm, and the granulating is 120s; granulating at a high speed: the rotation speed of the stirring paddle is 175rpm, the rotation speed of the granulating knife is 1800rpm, and the granulating is carried out for 60 seconds;
(6) Wet granules obtained in the step (5) are subjected to wet granulation and then added into a boiling granulator for drying, wherein the drying temperature is 45 ℃, and the moisture is controlled to be less than or equal to 4.00%;
(7) Adding the intermediate obtained in the step (6) into a granulator for granulating, wherein the rotating speed of the granulator is 300-450 rpm;
(8) Adding the intermediate obtained in the step (7) into a hopper mixer, and adding magnesium stearate for mixing;
(9) Adding the intermediate obtained in the step (8) into a tablet press for tabletting, wherein the hardness of the tablet is controlled as follows: 0.1g specification: 9.00-14.00 kgf,0.3g specification: 11.00 to 17.00kgf;
(10) Optionally, adding the intermediate obtained in the step (9) into a coating machine for coating, and controlling the coating weight gain to be 2.0% -2.5%.
Preferably, the disintegrant is added by internal addition.
Wherein the coating consists of a water-soluble coating material and a coating solvent, wherein the water-soluble coating material is selected from the group consisting of opadry and polyvinylpyrrolidone; the coating solvent is selected from ethanol, water or a mixture of water and ethanol.
Wherein the water-soluble coating material is preferably Opadry, and the coating solvent is preferably water.
The proportion of the coating powder is 1% -3%, preferably 2% -3%, and more preferably 2% -2.5%.
Drawings
FIG. 1 is a dissolution profile of the tablet of example 1 in water containing 3% SDS.
FIG. 2 is a graph showing the dissolution profile of the tablets of example 2 in water containing 3% SDS.
FIG. 3 is a dissolution profile of the tablet of example 3 in water containing 3% SDS.
FIG. 4 is a dissolution profile of the tablet of example 4 in water containing 3% SDS.
FIG. 5 is a dissolution profile of the tablet of example 5 in water containing 3% SDS.
FIG. 6 is a dissolution profile of the tablet of example 6 in water containing 3% SDS.
Detailed Description
The present invention will be described in detail with reference to the following examples for further illustration of the invention, but the scope of the invention is not limited to the examples.
The medium from which the composition of the present invention is eluted is an aqueous solution containing 3.0% SDS.
EXAMPLE 1 investigation of filler proportions
TABLE 1
Conclusion:
investigation of filler proportion: from the data, the proportion of microcrystalline cellulose is increased, so that the bulk density of the granule intermediate is increased, the granule compressibility is improved, the repose angle and the friability of the tablet are not obviously different, but the dissolution is slow, and the proportion of anhydrous lactose to microcrystalline cellulose is 1:1, can be dissolved out rapidly.
EXAMPLE 2 examination of disintegrant usage and addition mode
TABLE 2
Conclusion:
investigation of the amount of disintegrant and the mode of addition: in the prescription research, the accumulated dissolution rate is taken as a main investigation index, and the result shows that the dosage and the adding mode of the disintegrating agent have influence on the dissolution of the tablet, wherein the dissolution can be realized rapidly by adding about 6% of the disintegrating agent.
EXAMPLE 3 investigation of adhesive species
TABLE 3 Table 3
Conclusion:
investigation of adhesive types: the influence of two adhesives, namely polyvinylpyrrolidone and hypromellose, on the dissolution and friability of the tablet, the compressibility and flowability of the granule and the like is examined in comparison. The results show that the dissolution effect is better using polyvinylpyrrolidone as binder.
EXAMPLE 4 concentration and mode of addition of polyvinylpyrrolidone
TABLE 4 Table 4
Conclusion:
examination of the manner of adding polyvinylpyrrolidone and the concentration of its aqueous solution based on example 3 revealed that the dissolution rate of the tablet slightly decreased when the concentration of the binder polyvinylpyrrolidone increased; and when polyvinylpyrrolidone is added in an internal manner, dissolution is poor and the fluidity of the particles becomes poor. In summary, polyvinylpyrrolidone is selected to be added as an aqueous solution.
EXAMPLE 5 prescription validation
TABLE 5
The operation steps are as follows:
(1) Sieving microcrystalline cellulose and anhydrous lactose with 60 sieves respectively for standby;
(2) Adding polyvinylpyrrolidone into water, stirring and dissolving until the polyvinylpyrrolidone is clear and transparent, wherein the concentration is 7%;
(3) Adding the prescription amount of microcrystalline cellulose, canagliflozin, croscarmellose sodium and anhydrous lactose into a whole grain wet mixing granulator, and mixing for 900s at the stirring paddle rotating speed of 120 rpm;
(4) Adding 7% adhesive into the wet granulator in the step (3), wherein the rotation speed of a stirring paddle is 10rpm, and the rotation speed of a peristaltic pump is 500rpm;
(5) Wet granulating the wet granules in the step (4), and granulating at a low speed: the rotation speed of the stirring paddle is 120rpm, the rotation speed of the granulating knife is 1200rpm, and the granulating is 120s; granulating at a high speed: the rotation speed of the stirring paddle is 175rpm, the rotation speed of the granulating knife is 1800rpm, and the granulating is carried out for 60 seconds;
(6) Wet granules obtained in the step (5) are subjected to wet granulation and then added into a boiling granulator for drying, wherein the drying temperature is 45 ℃, and the moisture is controlled to be less than or equal to 4.00%;
(7) Adding the intermediate obtained in the step (6) into a granulator for granulating, wherein the rotating speed of the granulator is 300-450 rpm;
(8) Adding the intermediate obtained in the step (7) into a hopper mixer, adding magnesium stearate for mixing, and mixing for 10min at the rotating speed of 15 rpm;
(9) Adding the intermediate obtained in the step (8) into a tablet press for tabletting, wherein the hardness of the tablet is controlled as follows: 0.1g of 9.00-14.00 kgf,0.3g of 11.00-17.00 kgf;
(10) Optionally, adding the intermediate obtained in the step (9) into a coating machine for coating, and controlling the coating weight gain to be 2.0% -2.5%. Conclusion: as shown by the results, the two specifications of tablets have better fluidity, smaller friability and quicker dissolution, and achieve ideal effects.
Example 6 coated weight gain investigation of Canagliflozin tablet
TABLE 6
The recipe and procedure were in accordance with the 0.3g specification in example 5.
Conclusion:
the dissolution curve is used as an investigation index to screen the coating weight gain of 2.0%, 2.5%, 3.0% and 4.0%. The results show that: the coating weight gain is increased, the falling-off time of the coating film is prolonged, the dissolution rate is reduced, and the inspection results of the conjugated plain tablet and the four weight gain coated tablets show that the coating film is fine and attractive when the coating weight gain is 2.0-2.5%, and the dissolution is faster, so that the coating weight gain of 0.3g and 0.1g is 2.0-2.5%.
Example 7 stability test of canagliflozin tablet:
(1) Respectively placing the samples at high temperature 60 deg.C and 25 deg.C/RH 90%, and irradiating with light (total illuminance not less than 1.2X10) 6 Lux hr) stripUnder the test piece, sampling is carried out at 5d and 10d respectively, detection is carried out, and compared with 0d, the test result is as follows:
TABLE 7
(2) Samples were placed at 40 ℃ ± 2 ℃/RH75% ± 5% for sampling at 1M, 2M, 3M, 6M, respectively, and compared to 0M results, the test results were as follows:
TABLE 8
(2) Samples were placed at 30 ℃ ± 2 ℃/RH 65% ± 5% for sampling at 3M, 6M, 9M, respectively, and compared to 0M results, the test results were as follows:
TABLE 9
Conclusion:
the results show that the related substances, dissolution and content results of the pharmaceutical composition disclosed by the invention are not obviously changed compared with those of 0d in the processes of influencing factors, accelerating and long-term stability test. Therefore, the canagliflozin tablet provided by the invention and the preparation method thereof are proved to be relatively stable.
The above examples are preferred embodiments of the present invention, but the embodiments of the present invention are not limited to the above examples, and any other changes, substitutions, combinations, simplifications, modifications, etc. that do not depart from the spirit and principle of the present invention should be made in the same way as the above examples, and are included in the scope of the present invention.
Claims (6)
1. The canagliflozin tablet is characterized by being prepared from the following raw and auxiliary materials in percentage by weight:
the polyvinylpyrrolidone is 5-15% aqueous solution;
(1) Sieving microcrystalline cellulose and anhydrous lactose respectively for standby;
(2) Adding polyvinylpyrrolidone into water, stirring and dissolving until the polyvinylpyrrolidone is clear and transparent;
(3) Adding the prescription amount of microcrystalline cellulose, canagliflozin, croscarmellose sodium and anhydrous lactose into a whole grain wet mixing granulator, and stirring and mixing;
(4) Adding the polyvinylpyrrolidone in (2) into the wet mixing granulator in (3);
(5) Wet granulating the wet granules in the step (4), and granulating at a low speed: the rotation speed of the stirring paddle is 120rpm, the rotation speed of the granulating knife is 1200rpm, and the granulating is 120s; granulating at a high speed: the rotation speed of the stirring paddle is 175rpm, the rotation speed of the granulating knife is 1800rpm, and the granulating is carried out for 60 seconds;
(6) Wet granules obtained in the step (5) are subjected to wet granulation and then added into a boiling granulator for drying, wherein the drying temperature is 45 ℃, and the moisture is controlled to be less than or equal to 4.00%;
(7) Adding the intermediate obtained in the step (6) into a granulator for granulating, wherein the rotating speed of the granulator is 300-450 rpm;
(8) Adding the intermediate obtained in the step (7) into a hopper mixer, and adding magnesium stearate for mixing;
(9) Adding the intermediate obtained in the step (8) into a tablet press for tabletting, wherein the hardness of the tablet is controlled as follows: 0.1g of the specification 9.00-14.00 kgf,0.3g of the specification: 11.00 to 17.00kgf;
(10) And (3) adding the intermediate obtained in the step (9) into a coating machine for coating, and controlling the coating weight gain to be 2.0% -2.5%.
2. The canagliflozin tablet of claim 1, wherein the polyvinylpyrrolidone is a 7-10% aqueous solution.
3. The canagliflozin tablet of claim 1, wherein the polyvinylpyrrolidone is a 7% aqueous solution.
4. The canagliflozin tablet according to claim 1, characterized in that the microcrystalline cellulose to anhydrous lactose ratio is 1:1.
5. the canagliflozin tablet of claim 1, wherein the prescription of the canagliflozin tablet is selected from a 0.1g specification prescription or a 0.3g specification prescription,
the prescription of 0.1g specification is:
the prescription of 0.3g specification is:
6. the canagliflozin tablet of any one of claims 1-5, wherein the canagliflozin particle size is d (0.9) 50 μm or less.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910271445.6A CN111773194B (en) | 2019-04-04 | 2019-04-04 | Canagliflozin tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910271445.6A CN111773194B (en) | 2019-04-04 | 2019-04-04 | Canagliflozin tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111773194A CN111773194A (en) | 2020-10-16 |
| CN111773194B true CN111773194B (en) | 2023-06-30 |
Family
ID=72755490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910271445.6A Active CN111773194B (en) | 2019-04-04 | 2019-04-04 | Canagliflozin tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN111773194B (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112190559B (en) * | 2020-11-06 | 2022-02-11 | 北京斯利安药业有限公司 | Controlled-release folic acid tablet and preparation method thereof |
| CN112741814A (en) * | 2021-02-08 | 2021-05-04 | 浙江诺得药业有限公司 | Canagliflozin tablet and preparation method thereof |
| CN114081866A (en) * | 2021-11-08 | 2022-02-25 | 则正(上海)生物科技有限公司 | Method for evaluating internal and external correlation of glipizide tablets |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120115799A1 (en) * | 2010-05-11 | 2012-05-10 | Wenhua Wang | Pharmaceutical formulations |
| CN103655539A (en) * | 2013-12-13 | 2014-03-26 | 重庆医药工业研究院有限责任公司 | Oral solid preparation of canagliflozin and preparation method thereof |
| CN105769803A (en) * | 2014-12-16 | 2016-07-20 | 康普药业股份有限公司 | Medicinal composition for treating 2-diabetes mellitus and preparation method of medicinal composition |
| CN106243097A (en) * | 2016-08-03 | 2016-12-21 | 上海延安药业有限公司 | Canagliflozin crude drug and preparation |
| CN106421794A (en) * | 2016-09-27 | 2017-02-22 | 黑龙江珍宝岛药业股份有限公司 | Drug compound for treating type II diabetes and preparation method thereof |
| US20170258761A1 (en) * | 2014-08-29 | 2017-09-14 | Sandoz Ag | Pharmaceutical Compositions Comprising Canagliflozin |
| CN108078945A (en) * | 2018-01-12 | 2018-05-29 | 杭州中美华东制药有限公司 | Canagliflozin pharmaceutical composition |
-
2019
- 2019-04-04 CN CN201910271445.6A patent/CN111773194B/en active Active
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120115799A1 (en) * | 2010-05-11 | 2012-05-10 | Wenhua Wang | Pharmaceutical formulations |
| CN103655539A (en) * | 2013-12-13 | 2014-03-26 | 重庆医药工业研究院有限责任公司 | Oral solid preparation of canagliflozin and preparation method thereof |
| US20170258761A1 (en) * | 2014-08-29 | 2017-09-14 | Sandoz Ag | Pharmaceutical Compositions Comprising Canagliflozin |
| CN105769803A (en) * | 2014-12-16 | 2016-07-20 | 康普药业股份有限公司 | Medicinal composition for treating 2-diabetes mellitus and preparation method of medicinal composition |
| CN106243097A (en) * | 2016-08-03 | 2016-12-21 | 上海延安药业有限公司 | Canagliflozin crude drug and preparation |
| CN106421794A (en) * | 2016-09-27 | 2017-02-22 | 黑龙江珍宝岛药业股份有限公司 | Drug compound for treating type II diabetes and preparation method thereof |
| CN108078945A (en) * | 2018-01-12 | 2018-05-29 | 杭州中美华东制药有限公司 | Canagliflozin pharmaceutical composition |
Also Published As
| Publication number | Publication date |
|---|---|
| CN111773194A (en) | 2020-10-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN111773194B (en) | Canagliflozin tablet and preparation method thereof | |
| CN105233300B (en) | A kind of stable vildagliptin composition and preparation method thereof | |
| JP7007300B2 (en) | New crystalline form of dapagliflozin and its manufacturing method and application | |
| CN107432869A (en) | Include net double-layer tablets of Metformin hydrochloride and En Gelie and preparation method thereof | |
| CN113616624B (en) | Empagliflozin metformin sustained release preparation and preparation method thereof | |
| CN102755301B (en) | Glimepiride tablet and preparation method thereof | |
| EP4082532A1 (en) | Complex formulation comprising sitagliptin and dapagliflozin, and preparation method therefor | |
| CN103251593B (en) | Repaglinide/metformin composition | |
| CN103251594B (en) | Repaglinide/metformin combo tablet | |
| CN105853386B (en) | Tablet containing dapagliflozin propylene glycol hydrate and preparation method thereof | |
| JP2022544167A (en) | Pharmaceutical composition containing nitroxoline, nitroxoline oral solid tablet, method of preparation thereof, and use thereof | |
| CN100577157C (en) | Dispersant tablet containing hypolipidemic component and preparation method thereof | |
| KR20230131253A (en) | Solid tablet dosage form of ridinilazole | |
| CN103070829A (en) | Medicine composition including pramipexole and active ingredients of medicinal salt and preparation method thereof | |
| CN108078945B (en) | Canagliflozin pharmaceutical composition | |
| CN113398097A (en) | Dapagliflozin metformin sustained release preparation and preparation method thereof | |
| CN106580909B (en) | Solid pharmaceutical composition containing sarpogrelate hydrochloride | |
| CN101721414B (en) | Composition containing pioglitazone hydrochloride and metformin hydrochloride and preparation thereof | |
| CN104523653B (en) | Acarbose capsules agent pharmaceutical composition | |
| CN102512388B (en) | Glimepiride orally disintegrating medicine composition | |
| CN112535674B (en) | Letrozole tablet and preparation method thereof | |
| CN116440103A (en) | Saxagliptin metformin sustained release preparation and preparation method thereof | |
| EP4162929A1 (en) | Composite formulation comprising sitagliptin and dapagliflozin and preparation method therefor | |
| CN107213119B (en) | Tamibarotene oral solid preparation, preparation method and application thereof | |
| CN117462506A (en) | Preparation method of dapagliflozin tablet |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |