Tablet coating component, preparation method and application

Abstract

The invention relates to the field of pharmacy, in particular to a tablet coating component, a preparation method and application. The modified montmorillonite cellulose acetate composite material is prepared from the following components in parts by weight: 70 parts of a modified montmorillonite cellulose acetate composite, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methyl cellulose, 10 parts of polyethylene glycol and 3 parts of maleic anhydride. The modified montmorillonite cellulose acetate compound is prepared from modified montmorillonite and cellulose acetate. According to the invention, montmorillonite is modified by hexadecyl trimethyl ammonium bromide, and then is compounded with cellulose acetate, so that the mechanical strength of the coating is improved, and the problem that the mechanical strength of the coating is different when hydroxypropyl methyl cellulose is used is solved. The tablet coating is suitable for coating of various medicines, can be used for oral medicines, can also be used for medicines of other administration routes, and has a wide application prospect.

Description

Technical Field

[0001] The present invention relates to the field of pharmaceuticals, and particularly to a tablet coating composition, a preparation method and an application thereof. Background Art

[0002] In the professional and crucial field of pharmaceutical preparation packaging, the term "coating" plays a pivotal role. Specifically, it refers to a highly technical process. The origin of this process can be traced back to the UK. At its inception, the main purpose was to color the pharmaceutical agents to improve the appearance of the agents and visually identify the differences between different drugs.

[0003] The coating film, as a key product in the drug coating process, is defined as a protective layer that covers the surface of the drug and is mainly composed of polymer materials to form a film on the tablet. This coating film is a new type of pharmaceutical tablet packaging material and exhibits many incomparable advantages in the modern pharmaceutical industry. The coating film can endow the drug with sustained and controlled release functions. By precisely controlling the drug release rate and time, the drug can be continuously and stably released in the body, thereby maintaining an effective blood drug concentration, prolonging the action time of the drug, improving the efficacy of the drug, reducing the number of drug administrations, and bringing a more convenient medication experience for patients. Summary of the Invention

[0004] Aiming at the problems existing in the prior art, the present invention provides a tablet coating composition, a preparation method and an application thereof.

[0005] The present invention is achieved by the following technical solutions: A tablet coating is composed of the following components by weight: 70-100 parts of a modified montmorillonite cellulose acetate composite, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The modified montmorillonite cellulose acetate composite is prepared from modified montmorillonite and cellulose acetate.

[0006] Preferably, the weight of the modified montmorillonite cellulose acetate composite is 70-90 parts.

[0007] Furthermore, the preparation method of the modified montmorillonite cellulose acetate composite is as follows: Step S1: Add cetyltrimethylammonium bromide modified montmorillonite to acetone, stir and sonicate for 2 h to obtain a cetyltrimethylammonium bromide modified montmorillonite dispersion; Step S2: Add polyethylene glycol and cellulose acetate to acetone; Step S3: The cetyltrimethylammonium bromide modified montmorillonite dispersion obtained in Step S1 is added to the solution obtained in Step S2, stirred and sonicated for 4 h; then, after evaporating the excess solvent at 40 °C, vacuum drying is carried out. In the above steps, the mass ratio of cellulose acetate: polyethylene glycol: cetyltrimethylammonium bromide modified montmorillonite is 100:20:1 - 5.

[0008] Further, the mass ratio of cellulose acetate: polyethylene glycol: cetyltrimethylammonium bromide modified montmorillonite is 100:20:1.

[0009] Further, the preparation method of the cetyltrimethylammonium bromide modified montmorillonite is as follows: Montmorillonite is dispersed in distilled water and stirred for 24 h; then it is heated to 80 °C and maintained, and then a cetyltrimethylammonium bromide solution is slowly added and stirred for 24 h; then the precipitate is filtered, and the obtained precipitate is washed with distilled water to remove the unreacted cetyltrimethylammonium bromide, and then the precipitate is vacuum dried at 60 °C.

[0010] The present invention also provides a preparation method of a tablet coating: The following steps are included: The modified montmorillonite cellulose acetate composite, polylactic acid, PVP and hydroxypropyl methylcellulose are first dried in an oven at 50 °C for 4 h to remove moisture, and then blended evenly, heated, melted, extruded, granulated, and dried to obtain a tablet coating. Preferably, the melting and extrusion temperature is controlled at 160 - 185 °C.

[0011] Further, the present invention also provides an application of the tablet coating in pharmaceuticals.

[0012] Compared with the prior art, the present invention has the following advantages and beneficial effects: In the present invention, montmorillonite is modified by cetyltrimethylammonium bromide and then compounded with cellulose acetate to improve the mechanical strength of the coating, solving the problem of different mechanical strengths of the coating when using hydroxypropyl methylcellulose. This tablet coating is suitable for coating a variety of drugs. Specific Embodiments

[0013] To make the purpose, technical solutions and advantages of the present invention clearer and more understandable, the present invention will be further described in detail below in conjunction with embodiments. The illustrative embodiments and descriptions of the present invention are only used to explain the present invention and do not limit the present invention.

[0014] In the present invention, PVP is polyvinylpyrrolidone with an Mw of about 55000; montmorillonite is purchased from sigma and not further processed; polyethylene glycol has an Mn of 400; hydroxypropyl methylcellulose has an Mn of 10000.

[0015] Example 1 A tablet coating consists of the following components by weight: 70 parts of modified montmorillonite cellulose acetate complex, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The preparation method of the tablet coating is as follows: First, dry the modified montmorillonite cellulose acetate complex, polylactic acid, PVP, and hydroxypropyl methylcellulose in an oven at 50 °C for 4 h to remove moisture, then mix them evenly, heat at 160 °C, melt and extrude, granulate, and dry to obtain the tablet coating.

[0016] Among them, the preparation method of the modified montmorillonite cellulose acetate complex is as follows: Step S1: Add 1 g of cetyltrimethylammonium bromide modified montmorillonite to 10 mL of acetone, stir and sonicate for 2 h to obtain a cetyltrimethylammonium bromide modified montmorillonite dispersion; Step S2: Add 20 g of polyethylene glycol and 100 g of cellulose acetate to 200 mL of acetone; Step S3: Add the cetyltrimethylammonium bromide modified montmorillonite dispersion obtained in Step S1 to the solution obtained in Step S2, stir and sonicate for 4 h; then evaporate the excess solvent at 40 °C and then vacuum dry; In the above steps, the mass ratio of cellulose acetate: polyethylene glycol: cetyltrimethylammonium bromide modified montmorillonite is 100:20:1.

[0017] Among them, the preparation method of the cetyltrimethylammonium bromide modified montmorillonite is as follows: Disperse 10 g of montmorillonite in 100 mL of distilled water, stir for 24 h; then heat to 80 °C and keep it, then slowly add the cetyltrimethylammonium bromide solution and stir for 24 h, where the cetyltrimethylammonium bromide solution is 7.3 g / 150 mL and the solvent is water; then filter to obtain a precipitate, wash the obtained precipitate with distilled water to remove the unreacted cetyltrimethylammonium bromide, and then vacuum dry the precipitate at 60 °C.

[0018] Example 2 A tablet coating consists of the following components by weight: 80 parts of modified montmorillonite cellulose acetate complex, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The preparation method of the tablet coating is as follows: First, dry the modified montmorillonite cellulose acetate complex, polylactic acid, PVP, and hydroxypropyl methylcellulose in an oven at 50 °C for 4 h to remove moisture, then mix them evenly, heat at 160 °C, melt and extrude, granulate, and dry to obtain the tablet coating.

[0019] Among them, the preparation method of the modified montmorillonite cellulose acetate complex is the same as that in Example 1.

[0020] Example 3 A tablet coating consists of the following components by weight: 90 parts of modified montmorillonite cellulose acetate complex, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The preparation method of the tablet coating is as follows: The modified montmorillonite cellulose acetate complex, polylactic acid, PVP, and hydroxypropyl methylcellulose are first dried in an oven at 50 °C for 4 h to remove moisture, then blended evenly, heated at 160 °C, melt-extruded, granulated, and dried to obtain the tablet coating.

[0021] Among them, the preparation method of the modified montmorillonite cellulose acetate complex is the same as that in Example 1.

[0022] Example 4 A tablet coating consists of the following components by weight: 100 parts of modified montmorillonite cellulose acetate complex, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The preparation method of the tablet coating is as follows: The modified montmorillonite cellulose acetate complex, polylactic acid, PVP, and hydroxypropyl methylcellulose are first dried in an oven at 50 °C for 4 h to remove moisture, then blended evenly, heated at 160 °C, melt-extruded, granulated, and dried to obtain the tablet coating.

[0023] Among them, the preparation method of the modified montmorillonite cellulose acetate complex is the same as that in Example 1.

[0024] Comparative Example 1 A tablet coating consists of the following components by weight: 100 parts of cellulose acetate, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The preparation method of the tablet coating is as follows: The cellulose acetate, polylactic acid, PVP, and hydroxypropyl methylcellulose are first dried in an oven at 50 °C for 4 h to remove moisture, then blended evenly, heated at 160 °C, melt-extruded, granulated, and dried to obtain the tablet coating.

[0025] Test Example 1 Test the tensile strength and elongation at break of the prepared coating material. Cut the film material into a size of 10.0 mm in length and 6.0 mm in width. Check the integrity of the free film before measurement, and measure the average film thickness at different parts with a thickness gauge. Cut the free film into an oval shape with a length of 10.0 mm and a width of 6.0 mm, clamp both ends on the fixture of an electronic universal testing machine, and perform the test at a tensile speed of 5 mm / min, record the force-displacement values, and calculate the mechanical property parameters according to the following formula: Tensile strength = breaking load / (film thickness × film width); Elongation at break = (Length at break - Initial length) / Initial length.

[0026] Table 1 Mechanical Property Tests

[0027] Test Example 2 The coating materials obtained from each example and comparative example were coated to obtain potassium chloride sustained-release tablets, and sustained-release tests and dissolution tests were carried out: The second method device in General Rule 0931 of the Fourth Edition of the Chinese Pharmacopoeia 2015 was used, the rotation speed was 50 r / min, the medium was a hydrochloric acid solution with pH 1.2 as the dissolution medium, the medium volume was 900 mL, and dissolution tests were carried out. The detection method was flame atomic absorption spectrometry.

[0028] Table 2 Sustained-Release Performance Tests

[0029] It can be seen from Table 1 and Table 2 that the tensile strengths of Examples 1-4 are all higher than that of Comparative Example 1, and they have better tensile resistance. The elongation at break of Examples 1-4 is also higher than that of Comparative Example 1, indicating that the materials of the examples can withstand greater deformation before fracture, and have better flexibility and ductility. The drug sustained-release time of Examples 1-4 is longer than that of Comparative Example 1, which means that the materials of the examples can release drugs more slowly and lastingly in terms of drug release, which is beneficial to the long-term effect of drugs. In summary, the materials of the examples are significantly superior to the comparative example (29.7 MPa, 44%) in terms of tensile strength (47.3 - 56.3 MPa), elongation at break (57 - 71%) and drug sustained-release time, and among them, Example 3 (56.3 MPa, 71%) has the best comprehensive performance.

[0030] The specific embodiments described above further elaborate on the purpose, technical solutions and beneficial effects of the present invention. It should be understood that the above are only specific embodiments of the present invention and are not used to limit the protection scope of the present invention. Any modifications, equivalent replacements, improvements, etc. made within the spirit and principle of the present invention shall be included within the protection scope of the present invention.

Claims

1. A tablet coating, characterized in that: The composition is composed of the following components by weight: 70-100 parts of modified montmorillonite cellulose acetate composite, 20 parts of polylactic acid, 10 parts of PVP, 25 parts of hydroxypropyl methylcellulose, 10 parts of polyethylene glycol, and 3 parts of maleic anhydride; The modified montmorillonite-cellulose acetate composite is prepared from modified montmorillonite and cellulose acetate.

2. The tablet coating according to claim 1, characterized in that The weight portion of the modified montmorillonite cellulose acetate composite is 70 to 90 parts.

3. The tablet coating according to claim 2, characterized in that The weight portion of the modified montmorillonite cellulose acetate composite is 90 parts.

4. The tablet coating according to claim 1, characterized in that The preparation method of the modified montmorillonite cellulose acetate composite is as follows: Step S1: adding hexadecyltrimethylammonium bromide modified montmorillonite into acetone, stirring and ultrasonicating for 2 hours to obtain a hexadecyltrimethylammonium bromide modified montmorillonite dispersion; Step S2: adding polyethylene glycol and cellulose acetate into acetone; Step S3: adding the hexadecyltrimethylammonium bromide modified montmorillonite dispersion obtained in step S1 to the solution obtained in step S2, stirring and ultrasonicating for 4 hours; then evaporating the excess solvent at 40° C., and then vacuum drying; In the above steps, the mass ratio of cellulose acetate: polyethylene glycol: hexadecyltrimethylammonium bromide modified montmorillonite is 100:20:1-5.

5. The tablet coating according to claim 4, characterized in that The preparation method of the hexadecyltrimethylammonium bromide modified montmorillonite is: Disperse montmorillonite in distilled water and stir for 24 hours; then heat to 80°C and maintain the temperature, then slowly add hexadecyltrimethylammonium bromide solution and stir for 24 hours; then filter to obtain a precipitate, wash the obtained precipitate with distilled water to remove unreacted hexadecyltrimethylammonium bromide, and then vacuum dry the precipitate at 60°C.

6. The method for preparing a tablet coating according to any one of claims 1 to 5, characterized in that: The following steps are involved: The modified montmorillonite cellulose acetate complex, polylactic acid, PVP and hydroxypropyl methylcellulose are first dried in an oven at 50° C. for 4 hours to remove moisture, then blended evenly, heated, melted, extruded, granulated and dried to obtain a tablet coating.

7. The method for preparing a tablet coating according to claim 6, characterized in that: The melt extrusion temperature is controlled at 160-185°C.

8. Use of the tablet coating according to any one of claims 1 to 5 in medicines.

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