Sugar coating composition

Abstract

The invention discloses a sugar coating composition. The invention provides a sugar coating composition which comprises the following components in parts by mass: 40-60 parts of cane sugar, 0.2-1 part of povidone, 4-7 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talcum powder and 0.5-2 parts of titanium dioxide. The sugar coating composition is easy and convenient to operate, and the dissolution rate can be adjusted according to the drug activity requirement.

Description

Technical Field

[0001] The present invention relates to a sugar coating composition. Background Art

[0002] Coating refers to a coating layer made of suitable materials on the surface of a preparation. Sugar coating uses a large amount of syrup and talcum powder to coat the tablets to achieve the basic functions of improving appearance and masking taste. In the 1930s, the technological exploration of film coating began. Although film coating technology has gradually replaced sugar coating technology, the appearance of sugar-coated tablets, such as smoothness, is still better than that of film-coated tablets. Some original research products abroad are also sugar-coated tablets.

[0003] The traditional syrup coating process adds a variety of excipients that have nothing to do with drug treatment, mainly talcum powder, sucrose, and gelatin, to the surface of the drug tablet core, making the finished product extra weight up to 50-100%. The syrup preparation and coating process is complicated, and the coating operation mostly relies on the operator's experience and touch to control the coating quality.

[0004] Coating steps: 1) Isolation layer (3-5 layers, 30 minutes per layer): mainly ethanol solution of polymer materials such as corn protein, shellac, cellulose acetate phthalate (CAP); 2) Powder coating layer (15-18 layers, 20-30 minutes per layer): mainly syrup and talcum powder; 3) Sugar coating layer (10-15 layers, 15-20 minutes per layer): mainly syrup; 4) Colored sugar coating layer (8-15 layers, 15-20 minutes per layer): mainly pigment syrup. During the coating process, the coating materials are weighed and the slurry is prepared according to different needs, and the slurry needs to be prepared and used immediately, so the slurry preparation operation is cumbersome, time-consuming and labor-intensive.

[0005] The traditional operation of powder coating is to "sprinkle slurry once, sprinkle powder once" until the edges and corners of the tablet disappear. However, with this coating method, the syrup attached to the tablet adheres to too little talcum powder at one time, resulting in many coating layers, long time, high energy consumption, and large dust, which is easy to cause environmental pollution and material loss. At the same time, the amount of talcum powder thrown is also difficult to control. Summary of the invention

[0006] The technical problem to be solved by the present invention is that the existing sugar coating compositions are few in variety, the operation process relies on hand feeling, and the dissolution rate cannot be freely adjusted. To this end, the present invention provides a sugar coating composition, which has one or more of the following advantages: 1) It is easy to operate, and the time is shorter and the efficiency is higher than that of traditional syrup coating technology. 2) The dissolution rate can be adjusted according to the demand for active ingredients of the drug.

[0007] The present invention provides a sugar coating composition 1, which comprises the following components in parts by mass: 40-60 parts of sucrose, 0.2-1 parts of povidone, 4-7 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talc and 0.5-2 parts of titanium dioxide.

[0008] In a certain scheme, some technical features are described below, and the remaining features are as described in any of the above schemes (hereinafter referred to as "a certain scheme")

[0009] In one embodiment, the sugar coating composition 1 is composed of 40-60 parts of sucrose, 0.2-1 parts of povidone, 4-7 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talc and 0.5-2 parts of titanium dioxide, in parts by mass.

[0010] In one embodiment, the sucrose is 56 parts;

[0011] In one embodiment, the povidone may be povidone K90 or povidone K30, preferably povidone K90, more preferably povidone with an average molecular weight of 3.8×10 4 Povidone K90.

[0012] In a certain embodiment, the povidone K90 is:

[0013]

[0014] In a certain embodiment, based on 56 parts of sucrose, the amount of povidone is 0.2 to 1 part, for example, 0.53 part.

[0015] In one embodiment, the polyethylene glycol may be polyethylene glycol 6000 or polyethylene glycol 4000, preferably polyethylene glycol 6000, more preferably polyethylene glycol 6000 with an average molecular weight of 5400 to 7800, such as polyethylene glycol 6000 with an average molecular weight of 7389 or polyethylene glycol 6000 with an average molecular weight of 7402.

[0016] In a certain embodiment, the polyethylene glycol 6000 is:

[0017]

[0018] In a certain embodiment, based on 56 parts of sucrose, the polyethylene glycol is 4 to 7 parts, for example 6.17 parts.

[0019] In one embodiment, the calcium carbonate is preferably light calcium carbonate.

[0020] In one embodiment, based on 56 parts of sucrose, the calcium carbonate is 20 to 30 parts, for example, 24.15 parts.

[0021] In a certain embodiment, based on 56 parts of sucrose, the talc powder is 10 to 20 parts, for example, 11.77 parts.

[0022] In a certain embodiment, based on 56 parts of sucrose, the titanium dioxide is 0.5 to 2 parts, for example 0.68 parts.

[0023] In one embodiment, the sugar coating composition 1 is composed of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, and 0.68 parts of titanium dioxide, in parts by mass.

[0024] In one embodiment, the sugar coating composition 1 is composed of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, and 0.71 parts of titanium dioxide, by mass.

[0025] In a certain embodiment, the sugar coating composition 1 may further include a pigment.

[0026] In one embodiment, the sugar coating composition 1 is composed of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, 0.68 parts of titanium dioxide and pigment, by mass.

[0027] In one embodiment, the sugar coating composition 1 is composed of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, 0.71 parts of titanium dioxide and pigment, by mass.

[0028] The present invention provides a sugar coating composition 2, which includes water and materials, wherein the mass ratio of the water to the materials is (5-8):10; the materials include the following components in parts by mass: 40-60 parts of sucrose, 0.2-1 parts of povidone, 4-6 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talc, and 0.5-2 parts of titanium dioxide.

[0029] In a certain embodiment, the actual solid content of the sugar coating composition 2 can be 44.4% to 67.3%, preferably 44.4%, 57.9%, 63.6%, 66.7% or 67.3%, where the solid content refers to the mass percentage of the material in the sugar coating composition 2.

[0030] In one embodiment, the viscosity of the sugar coating composition 2 may be 75 mPa·s to 210 mPa·s.

[0031] In one embodiment, the viscosity of the sugar coating composition 2 is 75 mPa·s, 116 mPa·s or 210 mPa·s.

[0032] In one embodiment, the water is purified water.

[0033] In one embodiment, the mass ratio of the water to the material may be (5.5-7.6):10, preferably 7.5:10, 6.1:10, 5.5:10, 7.6:10, 6.3:10, 4.8:10 or 8.2:10;

[0034] In a certain embodiment, the material consists of 40-60 parts of sucrose, 0.2-1 parts of povidone, 4-7 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talc and 0.5-2 parts of titanium dioxide, calculated by weight.

[0035] In one embodiment, the sucrose is 56 parts;

[0036] In one embodiment, the povidone may be povidone K90 or povidone K30, and povidone K90 is selected, and more preferably, the povidone with an average molecular weight of 3.8×10 4 Povidone K90.

[0037] In a certain embodiment, the povidone K90 is:

[0038]

[0039] In a certain embodiment, based on 56 parts of sucrose, the amount of povidone is 0.2 to 1 part, for example, 0.53 part or 0.55 part.

[0040] In one embodiment, the polyethylene glycol may be polyethylene glycol 6000 or polyethylene glycol 4000, preferably polyethylene glycol 6000, more preferably polyethylene glycol 6000 with an average molecular weight of 5400 to 7800, such as polyethylene glycol 6000 with an average molecular weight of 7389 or polyethylene glycol 6000 with an average molecular weight of 7402.

[0041] In a certain embodiment, the polyethylene glycol 6000 is:

[0042]

[0043] In a certain embodiment, based on 56 parts of sucrose, the polyethylene glycol is 4 to 7 parts, for example, 6.17 parts or 6.41 parts.

[0044] In one embodiment, the calcium carbonate is preferably light calcium carbonate.

[0045] In one embodiment, based on 56 parts of sucrose, the calcium carbonate is 20 to 30 parts, for example, 24.15 parts or 25.15 parts.

[0046] In a certain embodiment, based on 56 parts of sucrose, the talc powder is 10 to 20 parts, for example, 11.77 parts or 12.25 parts.

[0047] In a certain embodiment, based on 56 parts of sucrose, the titanium dioxide is 0.5 to 2 parts, for example, 0.68 parts or 0.71 parts.

[0048] In one embodiment, the material is composed of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, and 0.68 parts of titanium dioxide, in parts by mass.

[0049] In one embodiment, the material is composed of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, and 0.71 parts of titanium dioxide, in parts by mass.

[0050] In a certain embodiment, the sugar coating composition 2 is composed of water and a material; the mass ratio of the water to the material is 7.5:10; the material, by mass, is composed of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, and 0.68 parts of titanium dioxide.

[0051] In a certain embodiment, the sugar coating composition 2 is composed of water and a material; the mass ratio of the water to the material is 7.6:10; the material, by mass, is composed of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, and 0.71 parts of titanium dioxide.

[0052] In a certain embodiment, the material may further include a pigment.

[0053] In a certain embodiment, the sugar coating composition 2 is composed of water and a material; the mass ratio of the water to the material is 7.5:10; the material, by mass, is composed of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, 0.68 parts of titanium dioxide and a pigment.

[0054] In a certain embodiment, the sugar coating composition 2 is composed of water and a material; the mass ratio of the water to the material is 7.6:10; the material, in parts by mass, is composed of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, 0.71 parts of titanium dioxide and a pigment.

[0055] The present invention also provides a method for preparing the sugar coating composition 2, which comprises the following steps:

[0056] (1) mixing solution A with material II to obtain mixture B; the material II is composed of calcium carbonate, talcum powder, and titanium dioxide; the solution A is a mixture of sucrose, povidone K90, polyethylene glycol 6000, and water;

[0057] (2) The mixture B is passed through a sieve of 80-200 mesh; preferably the sieve is 120 mesh; and the sugar coating composition 2 is obtained.

[0058] In one embodiment, the solution A is prepared by the following method: dissolving the sucrose, the povidone and the polyethylene glycol in water at 60-80°C, heating the solution to 100°C and maintaining the temperature at 100°C for ≤20 min to obtain solution A.

[0059] The present invention also provides a method for preparing a sugar-coated tablet, which uses the above-mentioned sugar-coated composition 2 and comprises the following steps:

[0060] S1: spraying; the spraying refers to spraying the tablet core in the coating machine using a coating machine spray gun; the spraying slurry is the above-mentioned sugar coating composition 2;

[0061] S2: loose tablets; the loose tablets refer to the coating machine rotating after the spraying, waiting for the coated tablets to change from the sticky state just after the coating liquid is added to the loose state;

[0062] S3: Drying: The drying refers to the air intake, exhaust and heating of the coated tablets after the tablets are scattered; the air intake temperature of the drying is 15.0-60.0°C, and the air intake volume of the drying is 1800±300 / m 3 / h, the drying fan frequency is 15-30 / Hz;

[0063] S4: cooling; the cooling refers to blowing cold air into the coating machine to cool the coated tablets after the drying;

[0064] S5: Repeat the above steps S1-S4 until the coating is completed.

[0065] The coating is completed when the weight of every 50 coated tablets reaches 6950 mg. The number of coating layers of the coated tablets is 55 to 60 layers.

[0066] In one embodiment, the spraying time is 80±30s; the spraying amount is 0.3-0.8kg of the slurry for every 30-50kg of the tablet core.

[0067] In one embodiment, the drying air inlet temperature is 15.0-60.0°C, and the drying air inlet volume is 1800±300 / m 3 / h, and the drying fan frequency is 15-30 / Hz.

[0068] In one embodiment, in S5, coating is completed until the weight of every 50 coated tablets reaches 6950 mg, and the number of coating layers of the coated tablets is 55 to 60 layers.

[0069] The present invention provides a sugar-coated tablet, which consists of a tablet core and a sugar coating, wherein the sugar coating covers the tablet core;

[0070] The sugar coating is the sugar coating composition 1 mentioned above;

[0071] Alternatively, the sugar coating is obtained by coating the sugar coating composition 2 mentioned above.

[0072] In one embodiment, the coating is the preparation method of the above-mentioned sugar-coated tablet.

[0073] In one embodiment, the core comprises an active ingredient.

[0074] In one embodiment, the sugar-coated tablets are smooth, round and shiny coated tablets.

[0075] In a certain embodiment, the mass ratio of the tablet core to the sugar coating is 1:(0.6-0.9), preferably 1:0.8.

[0076] The reagents or raw materials used in the present invention are all commercially available.

[0077] The positive and progressive effects of the present invention are: the present invention relates to a sugar coating premix combination, which can achieve 1) adjusting the dissolution rate by adjusting the concentration of the coating solution according to the demand for active ingredients of the drug; 2) improving the coating efficiency. Compared with the traditional coating process, the composition is easy to weigh, easy to adjust the ratio concentration with purified water, and the slurry preparation process is simple; combined with the current coating machine technology, the whole stage from slurry preparation to coating can be mechanized, intelligently controlled in real time, reducing pollution and occupational exposure, with high coating efficiency and easier industrialization. BRIEF DESCRIPTION OF THE DRAWINGS

[0078] Figure 1 The tablet core containing no active substance in Example 3

[0079] Figure 2 The finished product of the coated tablet of Group F in Example 3

[0080] Figure 3 The finished product of the coated tablet of Group G in Example 3 DETAILED DESCRIPTION

[0081] The present invention is further described below by way of examples, but the present invention is not limited to the scope of the examples. The experimental methods in the following examples without specifying specific conditions are carried out according to conventional methods and conditions, or selected according to the product specifications.

[0082] The active ingredient of the WSC tablet core in the embodiment is estradiol valerate, and the physicochemical properties of estradiol valerate are as follows.

[0083]

[0084] Preparation process of WSC tablet core in the embodiment: 1 part of active ingredient, 56 parts of lactose, 16 parts of corn starch, 2.4 parts of povidone K25 are prepared into a 15% povidone K25 aqueous solution, 2.40 parts of talcum powder, and 0.2 parts of magnesium stearate. After adding the active ingredient, lactose, and corn starch to a wet granulation pot and mixing evenly, 15% povidone K25 aqueous solution is added to prepare a soft material, and granules are obtained after shearing, drying, and granulation. Talc powder and magnesium stearate are added, mixed evenly, and pressed into deep concave tablets with a diameter of 6 mm and a hardness of 20 to 40N.

[0085] The WSC core is a WSC tablet core prepared by wet granulation and tableting. It is composed of active ingredients and traditional wet granulation excipients corn starch, lactose, and adhesive povidone. The production process includes wet granulation, fluidized bed drying, granulation, and tableting. The active ingredient of the tablet core is a low-solubility drug with a high pKa value. The choice of dissolution medium pH is almost unrestricted, and there is no dissolution in dissolution media with different pH. After adding an appropriate amount of SDS to each medium, it has a higher solubility in a high pH environment, and a slightly lower solubility in an acidic environment, with a certain pH dependence.

[0086] The physical and chemical properties of some materials used in this experiment are shown in the following table:

[0087] Polyethylene glycol 6000

[0088]

[0089] Povidone K90

[0090]

[0091] The dissolution test method of the following embodiments and comparative examples is as follows

[0092]

[0093] Embodiment 1

[0094] The present invention uses WSC tablet cores containing the active ingredient for coating, and adds different weights of purified water to prepare sugar coating solutions of different concentrations:

[0095]

[0096] Preparation process:

[0097] (1) Preparation of coating solution: fully stir the soluble film-forming material I in purified water at 60-80°C, heat to boiling after dissolving, keep boiling for 10 minutes, then add the insoluble weight-increasing material II and stir for 30 minutes, pass through a 120-mesh sieve to obtain a coating solution;

[0098] (2) Preheating of tablet cores (6 mm in diameter and 3.1 mm in thickness): When the inlet air temperature is ≥ 60°C, turn off the heating and wait until the tablet bed temperature drops to ≤ 40°C. Then, place 420,000 tablet cores into the preheated coating pan and preheat for 10 min.

[0099] Comparison of viscosity of sugar coating compositions

[0100] Group Actual solid content of suspension syrup (%) Suspension syrup viscosity (mPa·s) Group A 57.9 75 Group B 63.6 116 Group C 67.3 210

[0101] (3) Coating step:

[0102] ① Use the coating machine spray gun for spraying. Before the formal coating, the spray gun will be tested to ensure that the amount of slurry added by the spray gun in 60 seconds is within 417g±10%. Add 0.3-0.8kg of sugar coating composition to 30-50kg tablet cores for coating. During the formal coating, the spraying time is controlled, and the spraying time is 80±30s. Starting from 50s, as the number of coating layers increases, the slurry adding time is gradually increased, and the maximum does not exceed 110s;

[0103] ② There is no air passing through the coating pot (turn off the air inlet and exhaust buttons), and only the coating pot rotates until the tablets change from the sticky state just after adding the coating liquid to the loose and non-sticky state;

[0104] ③ After the tablets are spread out, open the air intake, exhaust and heating to allow hot air to enter the coating pot to dry the coated tablets. The air intake temperature is controlled at 15.0-60.0℃ and the air intake volume is controlled at 1800±300 / m 3 / h, the fan frequency is controlled at 15~30 / Hz, and after drying to the exhaust air temperature ≥45.0℃, the heating is turned off and cooling begins;

[0105] ④ After turning off the heating button, the incoming air is no longer heated, and the original heated hot air is changed to cold air after surface cooling and dehumidification and blown into the pot to achieve cooling. Cooling conditions: Each layer needs to be cooled. When the heating and drying reaches the exhaust air temperature ≥45℃, turn off the heating and start cooling. After cooling to the exhaust air temperature ≤38.0℃, proceed to the next layer of spraying;

[0106] ⑤ When the weight of 50 coated tablets reaches the target tablet weight of the preparation (6950 mg), the coating is completed. Generally, the number of coating layers is 55 to 60.

[0107] Appearance of coated tablets obtained according to the coating preparation process (white or off-white, smooth, round, and shiny coated tablets)

[0108] The weight gain of coated tablets in groups A, B and C was 80%.

[0109] (4) After reaching the weight gain, the tablets are put into a polishing machine for polishing to obtain the finished coated tablets.

[0110] Dissolution curve comparison

[0111]

[0112] According to the dissolution curve detection method of the standard medium (aqueous medium) of the preparation, the dissolution curve detection of the coated tablets of Group A, Group B and Group C of the embodiment of the present invention was carried out. The results are shown in the following table.

[0113]

[0114] From the results in the above table, it can be seen that by adjusting the ratio of purified water to sugar coating premix composition, WSC coated tablets with the same coating weight gain exhibit different dissolution rates, and the 60 min dissolution rates are all ≥90%.

[0115] The product prepared by the sugar coating premix adopted in the embodiment of the present invention can achieve different dissolution requirements under the same coating weight gain conditions by adjusting the ratio of the purified water:sugar coating premix composition.

[0116] Embodiment 2

[0117] The present invention uses WSC tablet cores containing the active ingredient for coating, and compares the preparation using sugar coating premix (Example 2 and traditional sugar coating process) (Comparative Example 1-Traditional sugar coating process) Comparative Example 1 uses the same batch of WSC tablet cores as Group D and Group E, and is coated according to the traditional "one layer of syrup, one layer of talcum powder" process. ) Preparation of coated tablets Coating time difference:

[0118]

[0119] Preparation process:

[0120] (1) Preparation of coating solution: fully stir the soluble film-forming material I in purified water at 60-80°C, heat to boiling after dissolving, keep boiling for 10 minutes, then add the insoluble weight-increasing material II and stir for 30 minutes, pass through a 120-mesh sieve to obtain a coating solution;

[0121] (2) Tablet core preheating: Add 360,000 tablet cores into the preheated coating pan and preheat for 10 minutes;

[0122] (3) Coating step:

[0123] ① Use the coating machine spray gun for spraying. Before the formal coating, the spray gun will be tested to ensure that the amount of slurry added by the spray gun in 60 seconds is within 417g±10%. Add 0.3-0.8kg of sugar coating composition to 30-50kg tablet cores for coating. During the formal coating, the spraying time is controlled, and the spraying time is 80±30s. Starting from 50s, as the number of coating layers increases, the slurry adding time is gradually increased, and the maximum does not exceed 110s;

[0124] ② There is no air passing through the coating pot (turn off the air inlet and exhaust buttons), and only the coating pot rotates until the tablets change from the sticky state just after adding the coating liquid to the loose and non-sticky state;

[0125] ③ After the tablets are scattered, open the air inlet, exhaust and heating, let the hot air enter the coating pot to dry the coated tablets, control the air inlet temperature at 15.0~60.0℃, the air volume at 1800±300 / m3 / h, and the fan frequency at 15~30 / Hz. After drying to the exhaust temperature ≥45.0℃, turn off the heating and start cooling;

[0126] ④ After turning off the heating button, the incoming air is no longer heated, and the original heated hot air is changed to cold air after surface cooling and dehumidification and blown into the pot to achieve cooling. Cooling conditions: Each layer needs to be cooled. When the heating and drying reaches the exhaust air temperature ≥45℃, turn off the heating and start cooling. After cooling to the exhaust air temperature ≤38.0℃, proceed to the next layer of spraying;

[0127] ⑤ When the weight of 50 coated tablets reaches the target tablet weight of the preparation (6950 mg), the coating is completed. Generally, the number of coating layers is 55 to 60.

[0128] Both groups D and E gained 80% of their weight.

[0129] (4) After reaching the weight gain, polishing agent is added and polishing is performed to obtain the finished coated tablet.

[0130] Embodiment 3

[0131] The present invention uses blank tablet cores without raw materials (diameter 6mm, deep concave tablets, such as Figure 1 The coating is performed as shown in the figure, and the mass ratio of water to the sugar coating composition is determined to be within (5-8):10. The viscosity of the prepared syrup meets the spraying requirements, and the prepared coated tablets have a smooth, round and shiny appearance.

[0132]

[0133] Preparation process:

[0134] (1) Preparation of coating solution: fully stir the soluble film-forming material I in purified water at 60-80°C, heat to boiling after dissolving, keep boiling for 10 minutes, then add the insoluble weight-increasing material II and stir for 30 minutes, pass through a 120-mesh sieve to obtain a coating solution;

[0135] (2) Tablet core preheating: Add 420,000 tablet cores into the preheated coating pan and preheat for 10 minutes;

[0136] (3) Coating step:

[0137] ① Use the coating machine spray gun for spraying. Before the formal coating, the spray gun will be tested to ensure that the amount of slurry added by the spray gun in 60 seconds is within 417g±10%. Add 0.3-0.8kg of sugar coating composition to 30-50kg tablet cores for coating. During the formal coating, the spraying time is controlled, and the spraying time is 80±30s. Starting from 50s, as the number of coating layers increases, the slurry adding time is gradually increased, and the maximum does not exceed 110s;

[0138] ② There is no air passing through the coating pot (turn off the air inlet and exhaust buttons), and only the coating pot rotates until the tablets change from the sticky state just after adding the coating liquid to the loose and non-sticky state;

[0139] ③ After the tablets are scattered, open the air inlet, exhaust and heating, let the hot air enter the coating pot to dry the coated tablets, control the air inlet temperature at 15.0~60.0℃, the air volume at 1800±300 / m3 / h, and the fan frequency at 15~30 / Hz. After drying to the exhaust temperature ≥45.0℃, turn off the heating and start cooling;

[0140] ④ After turning off the heating button, the incoming air is no longer heated, and the original heated hot air is changed to cold air after surface cooling and dehumidification and blown into the pot to achieve cooling. Cooling conditions: Each layer needs to be cooled. When the heating and drying reaches the exhaust air temperature ≥45℃, turn off the heating and start cooling. After cooling to the exhaust air temperature ≤38.0℃, proceed to the next layer of spraying;

[0141] ⑤ When the weight of 50 coated tablets reaches the target tablet weight of the preparation (6950 mg), the coating is completed. Generally, the number of coating layers is 55 to 60.

[0142] Both groups F and G gained 80% of their weight.

[0143] (4) After reaching the weight gain, polishing agent is added and polishing is performed to obtain the finished coated tablets. Figure 2 As shown, the finished product of Group G coated tablets is as follows Figure 3 shown.

[0144] Comparative Example 1 - Traditional Sugar Coating Process

[0145] The comparative example used the same batch of WSC tablets as those in groups D and E, and coated them according to the traditional "one layer of syrup and one layer of talcum powder" process.

[0146] Preparation process:

[0147] (1) Slurry preparation

[0148] Preparation of monosaccharide syrup: Weigh 18 kg of boiling water, slowly add 42 kg of sucrose while stirring, heat until the solution boils again and keep boiling for 10 minutes, the concentration is about 70%.

[0149] Preparation of gelatin slurry: Take 2kg of gelatin and put it in a stainless steel container. Add 10 times the amount of distilled water and soak it for more than 12 hours to allow the gelatin to swell completely. Heat in a water bath to dissolve and set aside. The concentration of the gelatin slurry is 10 and it needs to be freshly prepared.

[0150] Preparation of 2% gelatin syrup: Add 35kg of monosaccharide syrup solution to 5kg and 10% gelatin slurry, heat to boiling, filter and set aside.

[0151] (2) Coating

[0152] Isolation layer: Use 10-15% gelatin slurry to coat 3-5 layers, drying temperature is 40℃-50℃, air volume is 1500-2000m 3 / h.

[0153] Powder coating: Use 2% gelatin syrup and talcum powder, coat with one layer of gelatin syrup and one layer of talcum powder, 15 to 18 layers, drying temperature is 40℃ to 55℃, air volume is 1500 to 2000m 3 / h.

[0154] Single syrup layer: Use 10 to 15 layers of single syrup, drying temperature is 30℃ to 40℃, air volume is 1200 to 1500m 3 / h.

[0155] After reaching the weight gain, polishing agent is added and polishing is performed to obtain the finished coated tablets.

[0156] Coating efficiency comparison:

[0157]

[0158] *The slurry preparation time and coating time are both included in the coating working hours.

[0159] Dissolution curve comparison:

[0160]

[0161] Comparing the process of Group D and Group E of the embodiment of the present invention with the comparative example, the embodiment of the present invention adopts the sugar coating premix composition to prepare the coating liquid, which is simple to weigh, convenient and rapid; and during use, talcum powder is added to the coating liquid as an insoluble weight-increasing material, without dust pollution, low energy consumption, simple process operation, and can realize full mechanization to replace manual coating, and the addition amount is easy to control, which is easier to realize industrialization.

Claims

1. A sugar coating composition, comprising the following components, by mass: 40-60 parts of sucrose, 0.2-1 parts of povidone, 4-7 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talc and 0.5-2 parts of titanium dioxide.

2. The sugar coating composition according to claim 1, characterized in that: It meets one or more of the following conditions: (1) The povidone is povidone K90 or povidone K30, preferably povidone K90, more preferably povidone with an average molecular weight of 3.8×10 4 Povidone K90; (2) based on 56 parts of the sucrose, 0.2 to 1 part of the povidone, for example 0.53 part; (3) The polyethylene glycol is polyethylene glycol 6000 or polyethylene glycol 4000, preferably polyethylene glycol 6000, more preferably polyethylene glycol 6000 with an average molecular weight of 5400 to 7800, such as polyethylene glycol 6000 with an average molecular weight of 7389 or polyethylene glycol 6000 with an average molecular weight of 7402; (4) based on 56 parts of the sucrose, 4 to 7 parts of the polyethylene glycol, for example 6.17 parts; (5) The calcium carbonate is preferably light calcium carbonate; (6) Based on 56 parts of the sucrose, the calcium carbonate comprises 20 to 30 parts, for example, 24.15 parts; (7) Based on 56 parts of the sucrose, the talc powder comprises 10 to 20 parts, for example, 11.77 parts; (8) Based on 56 parts of sucrose, 0.5 to 2 parts of titanium dioxide, for example 0.68 parts; (9) the sucrose is 56 parts; (10) The sugar coating composition further includes a pigment; (11) The sugar coating composition is composed, by weight, of 40-60 parts of sucrose, 0.2-1 parts of povidone, 4-7 parts of polyethylene glycol, 20-30 parts of calcium carbonate, 10-20 parts of talc and 0.5-2 parts of titanium dioxide.

3. The sugar coating composition according to claim 2, characterized in that: It meets one or more of the following conditions: (1) The polyvidone K90 is: (2) The polyethylene glycol 6000 is:

4. The sugar coating composition according to claim 1, characterized in that: The sugar coating composition is any combination of the following: Combination 1, by mass: the sugar coating composition consists of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, and 0.68 parts of titanium dioxide; Combination 2, by mass: the sugar coating composition consists of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, and 0.71 parts of titanium dioxide; Combination 3, by mass: the sugar coating composition consists of 56 parts of sucrose, 0.53 parts of povidone K90, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, 0.68 parts of titanium dioxide and pigment; Combination 4, by mass: the sugar coating composition consists of 56 parts of sucrose, 0.55 parts of povidone K90, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, 0.71 parts of titanium dioxide and pigment.

5. A sugar coating composition 2, comprising water and a material, wherein the mass ratio of the water to the material is (5-8):10; the material is the sugar coating composition according to any one of claims 1-4.

6. The sugar coating composition 2 according to claim 5, characterized in that: It meets one or more of the following conditions: (1) The actual solid content of the sugar coating composition 2 is 44.4% to 67.3%, preferably 44.4%, 57.9%, 63.6%, 66.7% or 67.3%, wherein the solid content refers to the mass percentage of the material in the sugar coating composition 2; (2) The viscosity of the sugar coating composition 2 is 75 mPa·s to 210 mPa·s, for example, 75 mPa·s, 116 mPa·s or 210 mPa·s; (3) The water is purified water; (4) The mass ratio of the water to the material is 5.5 to 7.6:10, preferably 7.5:10, 6.1:10, 5.5:10, 7.6:10, 6.3:10, 4.8:10 or 8.2:

10.

7. The sugar coating composition 2 according to claim 5, characterized in that: The sugar coating composition 2 is any combination of the following: Combination 1, the sugar coating composition 2 is composed of water and materials; the mass ratio of the water to the materials is 7.5:10; the materials, by mass, are composed of 56 parts of sucrose, 0.53 parts of povidone K900, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, and 0.68 parts of titanium dioxide; Combination 2, the sugar coating composition 2 is composed of water and materials; the mass ratio of the water to the materials is 7.6:10; the materials, by mass, are composed of 56 parts of sucrose, 0.55 parts of povidone K900, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, and 0.71 parts of titanium dioxide; Combination 3, the sugar coating composition 2 is composed of water and materials; the mass ratio of the water to the materials is 7.5:10; the materials, by mass, are composed of 56 parts of sucrose, 0.53 parts of povidone K900, 6.17 parts of polyethylene glycol 6000, 24.15 parts of light calcium carbonate, 11.77 parts of talc, 0.68 parts of titanium dioxide and pigment; Combination 4, the sugar coating composition 2 is composed of water and materials; the mass ratio of the water to the material is 7.6:10; the material, in parts by mass, is composed of 56 parts of sucrose, 0.55 parts of povidone K900, 6.41 parts of polyethylene glycol 6000, 25.15 parts of light calcium carbonate, 12.25 parts of talc, 0.71 parts of titanium dioxide and pigment.

8. A method for preparing the sugar coating composition 2 as claimed in any one of claims 5 to 7, comprising the following steps: S1: mixing solution A with material II to obtain mixture B; the material II consists of the calcium carbonate, the talc and the titanium dioxide; the solution A is a mixture of the sucrose, the povidone, the polyethylene glycol and the water; S2: the mixture B is passed through a 80-200 mesh sieve; the sieve is preferably 120 mesh; and the sugar coating composition 2 is obtained; Preferably, the solution A is prepared by the following method: dissolving the sucrose, the povidone and the polyethylene glycol in water at 60-80°C, heating to 100°C, and maintaining 100°C ≤ 20 min to obtain solution A.

9. A method for preparing a sugar-coated tablet, comprising the following steps: S1: spraying; the spraying refers to spraying the tablet core in the coating machine using a coating machine spray gun; the slurry for spraying is the sugar coating composition 2 according to any one of claims 5 to 7; for example, the time of spraying The time is 80±30s; the amount of spraying is Add 0.3-0.8 kg of the slurry to 30-50 kg of the tablet core; S2: loose tablets; the loose tablets refer to the coating machine rotating after the spraying, waiting for the coated tablets to change from the sticky state just after the coating liquid is added to the loose state; S3: Drying: The drying refers to the air intake, exhaust and heating of the coated tablets after the tablets are scattered; for example, the air intake temperature of the drying is 15.0-60.0°C, and the air intake volume of the drying is 1800±300 / m 3 / h, the drying fan frequency is 15-30 / Hz; S4: cooling; the cooling refers to blowing cold air into the coating machine to cool the coated tablets after the drying; S5: Repeat steps S1-S4 until the coating is completed; for example, until the weight of every 50 coated tablets reaches 6950 mg, the coating is finished, and the number of coating layers of the coated tablets is 55 to 60 layers.

10. A sugar-coated tablet, comprising a tablet core and a sugar coating, wherein the sugar coating covers the tablet core; the sugar coating is the sugar coating composition according to any one of claims 1 to 4; Alternatively, the sugar coating is obtained by coating the sugar coating composition 2 according to any one of claims 5 to 7; For example, the tablet core comprises an active ingredient; For example, the mass ratio of the tablet core to the sugar coating is 1:(0.6-0.9), preferably 1:0.8.

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