Tablet disintegration delay how to solve PHARMA manufacturers

In the process of production and sales of rotary tablet presses, PHARMA Machinery Manufacturing Factory often contacts with manufacturers of rotary tablet presses. It involves that the tablet cannot be completely disintegrated within the specified time limit, which affects dissolution, drug absorption and curative effect. For the disintegration of the tablet, our PHARMA editor will share with you. If you have other needs, please contact us

1 Effect of tablet pore state. The disintegration medium is generally water or artificial gastric juice, and its viscosity does not change much. Therefore, the four main factors affecting the penetration of the disintegration medium (water) into the tablet are capillary number (porosity), capillary pore size (pore size R), and liquid surface tension γ and contact angle θ. Influencing factors are: (1) Compressibility of raw materials. Highly compressible raw materials are prone to plastic deformation when compressed. The porosity and pore diameter r of the tablet are smaller, so the amount of water penetration and the distance L are smaller, and the disintegration of the tablet is slower. The results show that adding starch to some tablets can increase the porosity of the tablet, increase the water absorption rate of the tablet, and facilitate the rapid disintegration of the tablet. But we cannot infer that more starch is better. Tablets are difficult to shape due to excess starch and poor compressibility. (2) Particle hardness. When the hardness of the particle (or material) is small, it is easy to break due to the effect of pressure, so the pore size and pore size r of the compressed tablet are small, the water penetration amount and the penetration distance L are small, and the tablet disintegration is slow; faster. (3) PRESSURE. Generally speaking, the higher the pressure, the smaller the porosity and pore size R, the smaller the water penetration and penetration distance L, and the slower the disintegration speed of the tablet. Therefore, the pressure should be moderate, otherwise the tablet is too difficult to disintegrate. However, some tablets showed shorter disintegration times as the pressure was increased. If the pressure is low, the porosity of phenacetin tablets is large, and the disintegrating agent has enough expansion space after absorbing water, so it is difficult to disintegrate. When the pressure increases, the porosity is small, the disintegrant has enough expansion space after absorbing water, and the disintegration of the tablet is relatively small. (4) Lubricants and surfactants. When the contact angle θ is greater than 90°, the cosθ is negative, and water cannot penetrate into the pores of the tablet, that is, the tablet cannot be wetted by water, so it is difficult to disintegrate. This requires that the drug and excipients have a small contact angle θ. If the contact angle θ is large, such as the hydrophobic drug aspirin, it is necessary to add an appropriate amount of surfactant to improve its wettability, reduce the contact angle θ, and increase the cosθ value, thereby accelerating the disintegration of the tablet. Hydrophobic lubricants commonly used in tablets can also seriously affect the wettability of tablets, increasing the contact angle θ, making it difficult for water to penetrate, resulting in slow disintegration. For example, when magnesium stearate is mixed with granules, the contact angle is 121°, which will be adsorbed on the surface of granules, so that the hydrophobicity of the tablet is significantly enhanced, and the water is not easy to penetrate and disintegrate slowly, especially when the amount of magnesium stearate is large. Similarly, when the hydrophobic lubricant is mixed with the particles for a long time and with high mixing intensity, the surface of the particles is completely covered by the hydrophobic lubricant. Therefore, the pore wall of the tablet has strong hydrophobicity, which prolongs the disintegration time significantly. Therefore, in production practice, the type, dosage, stirring intensity and stirring time of the lubricant should be strictly controlled to avoid a lot of waste.

2 The influence of other excipients: (1) The influence of starch Starch can quickly disintegrate insoluble or hydrophobic drugs, but the effect with water-soluble drugs is poor; (2) Adhesives have strong adhesion and bond If the amount of lubricant is large, the disintegration time will exceed the limit; (3) if the amount of lubricant is large, the disintegration time will exceed the limit.