Application method of powder direct compression and its precautions

The application method of powder direct compression and its precautions have obvious advantages due to the direct compression of powder. For example, the process is relatively simple, no granulation, drying, product disintegration or dissolution is fast, and the quality of the finished product is stable. % of the tablet varieties have been produced using this process.

First, the application
1. Drugs used for moisture, heat, discoloration and decomposition Many drugs are unstable to humidity and heat. For example, cefixime is wet, heat is prone to discoloration, and potency is reduced. Vitamin C is reductive and easily oxidized by air. As a result, the color turns yellow and the content decreases, especially when it is affected by moisture, temperature, metal ions, etc., which is more likely to cause deterioration of the drug; the aminophylline is easily decomposed and discolored by moisture and heat, releasing a strong ammonia odor; rifampicin is wet, The heat is also unstable, the content is decreased, and the dissolution is unqualified; vitamins B1, B2, and B6 are unstable to wet, hot, and metal ions. If these drugs are granulated by conventional wet granulation, the drug will contact the solvent in the adhesive during the production process and be dried at a high temperature, which will have an impact on the quality of the product. The tablet is directly compressed, and the prepared tablet has a smooth surface, no lobes and sticking, and the difference in tablet weight is small, and the time limit for disintegration is short. After accelerated experiment and sample retention, there is no change in the quality indexes of the tablets. .

2, for esters, amides and other easily hydrolyzed drugs because of the easy hydrolysis of meclofenoxate, using the conventional wet granulation process, due to the addition of binders in the production process, containing water, under dry high temperature conditions, drugs Accelerated decomposition, which affects the quality of the drug, not only reduces the content of the drug, but also increases the degradation products, resulting in reduced efficacy and increased side effects. It is produced by direct powder tableting process, avoiding contact with water, and optional wetted excipients to further ensure the stability of the drug during storage.

3. The dissolution rate of a drug with low solubility or small hydrophobicity is greatly affected by its specific surface area and the surface properties of the finished product. By pharmacy method, hydrophilic adjuvant is selected, and the powder is directly compressed. After the drug disintegrates, the drug is directly released from the powder, the dispersion is increased, the dissolution is accelerated, and the relative bioavailability is improved.

4. The melting point of the compound drug cyclomandelin for low melting point and eutectic melting is 50 ° C ~ 62 ° C. Conventional wet granulation can cause the drug to melt and affect the quality; the compound preparation of ephedrine hydrochloride and diphenhydramine hydrochloride, When wet granulation is dry, the two can be eutectic and not easy to dry. The powder direct compression process can effectively solve the above problems.

Second, matters needing attention
1. The properties of the drug and the auxiliary materials should be similar. When the powder is directly compressed, the physical properties such as bulk density, particle size and particle size distribution of the drug and the auxiliary material are similar, so as to facilitate uniform mixing, especially the specification is small, and the content uniformity needs to be determined. For drugs, various excipients must be carefully selected.

2, insoluble lubricants must be added to the insoluble lubricant for direct compression of the powder must be added at the end, that is, the raw materials and other auxiliary materials are mixed evenly, then add insoluble lubricants, and control the mixing time, otherwise it will be serious Affects disintegration or dissolution. In addition, when pregelatinized starch, microcrystalline cellulose, etc. are used as auxiliary materials, if the amount of magnesium stearate is large and the mixing time is long, the tablet has a softening phenomenon, so the general dosage should be below 0.75%, and The mixing time, speed and intensity are verified.

3. The content measurement after mixing is the same as the conventional wet granulation production process. After mixing the raw materials of the direct compression of the powder, the content is determined to ensure that the quality of the intermediate product and the finished product meets the prescribed standards.

4. Sufficient test amplification after small test In general, unqualified tablets pressed by powder direct compression process should not be reworked. Since the tablet is re-pulverized after rework, the compressibility of the material after pulverization is remarkably lowered, so that it is not suitable for direct compression. Therefore, from small test to large production, it must be piloted and fully verified, and the pilot should use the same type of equipment as the large production in the future, so that the determined parameters can guide the large production.

5, the use of microcrystalline cellulose when the tablet hardness and friability is unqualified, microcrystalline cellulose can be added, the amount can be as high as 65%; can also be used to first press into a large piece, then broken into particles, and then tablet The method can get satisfactory results.

6. Handling the abnormal conditions in the tablet in time. During the tableting process, samples should be taken in time according to the standard operating procedures. Observe the appearance of the tablet and measure the difference in weight, hardness, friability, disintegration time, thickness and other quality indicators. And observe the operation of the equipment, the abnormal situation should be reported in a timely manner and take emergency measures, detailed records of abnormal phenomena and processing results, detailed analysis to ensure product quality.

With the introduction of new foreign pharmaceutical excipients, the continuous development and listing of new varieties of domestic pharmaceutical excipients, the continuous updating, improvement and improvement of tableting equipment, the application of powder direct compression method in China will gradually increase. The instrument used above is recommended for use with Tianjin Gangdong DF-4 tablet press.

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