Powder direct compression method

Direct powder tableting refers to a method in which a drug powder is mixed with a suitable auxiliary material and directly compressed without being granulated. The direct compression of the powder does not require the preparation of granules, which not only shortens the process, simplifies the equipment, but also facilitates the automation of continuous biomedical research. The education network collects and produces the product, and there is no moist heat process, which improves the stability of the drug, facilitates the dissolution of the drug, and improves the drug. effect. However, it is necessary to solve the problem of fluidity and compressibility of the powder. At present, it mainly starts from improving the performance of the tablet material and improving the tableting machinery.

At present, although the production of tablets in China is still widely used in wet granule tableting, the application of powder direct compression technology in domestic and foreign pharmaceutical enterprises is gradually receiving attention. Now I will introduce and summarize the characteristics and advantages of direct powder tableting technology and the key issues that need to be solved in the application.

Significantly reduce production costs
The preparation process of the tablet mainly includes several methods such as wet granulation tableting, dry granulation tableting, powder direct compression tableting and lyophilization tableting. The direct compression of the powder is carried out by separately sieving and mixing the powder of the drug with a suitable auxiliary material, and directly compressing the tablet without granulating (wet or dry particles). Because of its simple process, no need to granulate, dry, save energy and time, protect drug stability, improve drug dissolution, and high degree of industrial automation, it is increasingly used by pharmaceutical companies in various countries. According to relevant information, about 40% of the tablet varieties in foreign countries have been produced by seed production.

Compared to conventional wet granulation, the powder direct compression technology is a significant advantage in its economy. In the traditional wet granulation, factors such as the amount of binder added, the drying time of the granules, the granulation time of the granules of the granules, etc., the number of machines required for production is large, the space is large, and some factors need to rely on experience judgment, which may result in Product quality is unstable, and there are large differences between batches. The direct compression technology ziu has the obvious advantage that it reduces the cost of equipment and operation: its production process is simple, no granulation, sieving, drying, sizing and intermediate sampling testing are required, which reduces the investment in the corresponding equipment factory and Inspection cost and labor intensity, saving time and energy, and not determining the quality of the product due to the experience of the workers, so that the quality of the final product is stable, the difference between batches is small, the operability is strong, the continuous production is guaranteed, especially suitable for GMP requirements. Production management.

Greatly improve disintegration and dissolution
The tablets produced by the direct tableting technology have good disintegration performance and excellent dispersion uniformity. Therefore, the technology is widely used in some instant release and rapid disintegration tablets, and the production of domestic orally disintegrating tablets has been gradually adopted. Powder molding direct compression technology.

Why can the direct powder tableting technology improve the disintegration of tablets? Disintegration of tablets relies primarily on the disintegrating agent in the tablet to cause disintegration of the tablet by capillary action or swelling. The tablet prepared by the direct powder tableting process has a disintegrant different from the disintegrant in the wet granulation, and does not reduce the disintegration performance due to the contact with moisture in the early stage, thereby ensuring good disintegration characteristics. In addition, since the tablet is not tableted, the tablet does not shape after disintegration.

It forms a large group of particles, but forms a fine powder with a relatively large specific surface area, which can be well distributed in the body, improves the uniformity of dispersion of the tablets, and contributes to the release and absorption of the drug. Studies have shown that this technology can ensure that the tablets disintegrate completely in less than 30 seconds. At present, many dispersible tablets have been prepared using powder direct compression technology.

Powder direct compression technology also helps to improve the dissolution of drugs with low solubility. Since these drugs are greatly affected by the specific surface area and the surface properties of the finished product, the pharmaceutics method is adopted, and the hydrophilic auxiliary material is selected. After the direct compression, the drug is directly released from the powder after the drug disintegrates, and the dispersion is increased. Large, dissolution is accelerated, and relative bioavailability is improved.

The powder direct compression technology is adopted, and a hydrophilic hydrophilic auxiliary material (for example, lactose) is selected as a filler, so that the drug and the lactose powder are uniformly dispersed in water under the premise of ensuring rapid disintegration of the tablet, and then the lactose is dissolved and on the surface of the drug. Hydrogen bonding is formed by van der Waals force and water, thereby reducing the hydrophobicity of the drug and contributing to the dissolution of the drug. For example, the Yantongxikang tablets produced by wet granulation only dissolve 52% in 60 minutes, while the tablets produced by direct tablet compression can have a dissolution rate of 90% in 60 minutes.

Strong process adaptability
Compared to wet granulation, powder direct compression technology also has the advantage that it avoids the effects of heat and moisture. In actual production, certain chemically unstable drugs, such as easily hydrolyzable esters, amides, oxidizable phenolic hydroxyls, vitamin C, vitamin E, etc.; in wet granulation, many A drug that is unstable in the event of heat or light may undergo a hydrolysis reaction during the production process, or may be destroyed by heat during the drying process of the particles, or may cause photolysis of the drug due to complicated processes. For these problems, consider using a direct compression process. Since the direct direct tableting process of the powder is simple, no granulation and drying are required, thereby effectively protecting the stability of the main drug and avoiding various unstable factors caused by wet granulation, thereby ensuring the quality of the product.

In actual production, some drugs with low melting point (about 60 ° C or lower than 60 ° C), such as α-lipoic acid (melting point is 60 ° C), dry after granulation, due to the main drug is heated and melted, the particles are difficult to dry , thereby affecting the production; the pellets prepared from the ephedrine hydrochloride and diphenhydramine hydrochloride in the compound preparation Baichuanpeng tablets are not easy to dry due to the low eutectic phenomenon during drying. This problem can be solved by direct powder tableting.

In addition, some drugs that are more viscous in water, difficult to granulate, or strong in dehumidification and should not be exposed to the air for a long time, such as most traditional Chinese medicine extracts, can be directly compressed by powder to avoid stickiness and lead. The unfavorable factors brought about by the wetness, so that qualified tablets are obtained.

"Combination processing" to improve the properties of excipients
A big difference between direct compression and wet granulation is that the material required for tableting is powdery fine powder. The compressibility and fluidity of the material will determine the quality of the final product. Since the fluidity and compressibility of several drug powders cannot meet the requirements of direct compression, it is a direct and effective method to select the excipients with superior performance to increase the fluidity of the drug. The correct choice of excipients in direct compression is more stringent than wet granulation.

However, at present, there is no conventional excipient that combines the good fluidity required for direct compression and excellent compressibility, adhesion, high adhesion, and low sensitivity to lubricants. Conventional starch, dextrin, and powdered sugar are relatively poor in fluidity and compressibility. Therefore, the development of excipients suitable for direct powder tableting technology is a new topic.

Excipients that meet the above requirements can be obtained by a "combination process" method. A complex consisting of a friable lactose monohydrate and a plastic material (powdered cellulose, microcrystalline cellulose, starch), such as spray-dried lactose (Flowlac-100), modified lactose (Tablettose series) , spray-dried lactose-cellulose premix (Cellactose), only need simple physical mixing, combined with the nature of the main drug, appropriate prescription adjustment, can meet the compressibility and fluidity (can be added to the glidant) The requirements make it easier to directly compress the powder. The use of such "combination processing" products can increase the hardness of the tablet more than a simple mixture of the above two components, respectively.

Tableting equipment needs further improvement
At present, the direct compression equipment - tablet press, is constantly updated and improved. By improving the feeding device and dust removal device, the company can improve the pre-compression mechanism to help ensure the smooth progress of the entire direct compression process.

The flowability of the fine powder is not as good as that of the granules. It is easy to appear in the powder feeder or the flow is fast and slow, which causes the difference in tablet weight. The use of the oscillating feeding powder or the forced feeding device can make the powder evenly flow into the die hole; There is more air in the particles than in the particles. When the tablet is pressed, it is easy to cause the top crack, and the tableting speed is reduced, or the second compression is performed, that is, the initial compression is performed, and the second time is the final pressing of the tablet into the tablet. The problem, and because of the increased compression time, it is advantageous to discharge the air in the powder, reduce the phenomenon of splitting, and increase the hardness of the tablet; in addition, because the powder has a flying property, when the powder is directly compressed, more dust is generated, sometimes The phenomenon of powder leakage occurs, so the tablet press should have an automatic sealing device, a good dust removal device and a tight joint between the duster and the turntable.

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