Do you have any doubts about the delay of tablet disintegration in rotary tablet press?
Last Update: 2019-07-12
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In the production and sales process of the tablet press, there is often contact with the rotary tablet press manufacturer of Shanghai Tianjiu machinery factory, which involves that the pressed tablet cannot be disintegrated within the specified time limit, which affects the dissolution, absorption and efficacy of the drug For the tablet disintegrated, we will share it with you 1 The influence of tablet pore state Generally, the disintegrating medium is water or artificial gastric juice, and its viscosity does not change much, so the four main factors that affect the penetration of disintegrating medium (water) into tablet are capillary quantity (porosity), capillary pore diameter (pore diameter R), surface tension γ of liquid and contact angle θ The influencing factors are: (1) the compressibility of raw and auxiliary materials When the raw and auxiliary materials with strong compressibility are compressed, they are prone to plastic deformation The porosity and pore diameter r of the tablet are smaller, so the amount and distance L of water penetration are smaller, and the disintegration of the tablet is slower The results showed that the addition of starch in some tablets could increase the porosity of the tablets, significantly enhance the water absorption of the tablets and facilitate the rapid disintegration of the tablets However, it can not be concluded that the more starch the better, because too much starch, the poor compressibility, tablets difficult to form (2) hardness of particles When the hardness of particles (or materials) is small, they are easy to be broken due to pressure, so the pore and pore diameter r of the compressed tablets are small, so the amount and distance L of water penetration are also small, and the tablets disintegrate slowly; otherwise, they disintegrate faster (3) tablet pressing force In general, the larger the pressure, the smaller the porosity and pore diameter R, the smaller the amount and distance L of water penetration, and the slower the disintegration of tablets Therefore, the pressure should be moderate, otherwise the tablet is too hard to disintegrate However, the disintegration time of some tablets decreases with the increase of pressure For example, phenacetin tablets take starch as disintegrating agent When the pressure is small, the porosity of tablets is large, and the disintegrating agent has sufficient expansion space after absorbing water, so it is difficult to play the role of disintegration When the pressure is large, the porosity is small, the disintegrating agent has sufficient expansion space after absorbing water, and the tablets have relatively large expansion and disintegration Hurry up (4) lubricants and surfactants When the contact angle θ is greater than 90 °, cos θ is negative, and the water can not penetrate into the pores of the tablet, that is, the tablet can not be wetted by water, so it is difficult to disintegrate This requires that drugs and excipients have a small contact angle θ If the contact angle θ is large, for example, hydrophobic drug aspirin, it is necessary to add an appropriate amount of surfactant to improve its wettability, reduce the contact angle θ, increase the cos θ value, so as to accelerate the disintegration of tablets Hydrophobic lubricants commonly used in tablets may also seriously affect the wettability of tablets, resulting in the increase of contact angle θ, the difficulty of water penetration, and the slow disintegration For example, the contact angle of magnesium stearate is 121 °, when it is mixed with the particles, it will be adsorbed on the surface of the particles, so that the hydrophobicity of the tablets is significantly enhanced, the water is not easy to penetrate, and the disintegration is slow, especially when the amount of magnesium stearate is large, this phenomenon is more obvious In the same way, when hydrophobic lubricant and particles are mixed for a long time and with a large mixing strength, the surface of particles is completely covered by hydrophobic lubricant Therefore, the pore wall of the tablet has a strong hydrophobicity, which significantly prolongs the disintegration time Therefore, in production practice, the variety, dosage, mixing strength and mixing time of lubricants should be strictly controlled to avoid mass waste 2 The influence of other auxiliary materials: (1) the influence of starch, starch can make insoluble or hydrophobic drugs disintegrate quickly, but it has poor effect with water-soluble drugs; (2) the adhesive has strong adhesion, and the amount is more, which can make the disintegration time limit exceed; (3) the amount of lubricant is more, which can make the disintegration time limit exceed 3 Effect of tablet storage conditions: after the tablet is stored, the disintegration time is often prolonged, which is mainly related to the temperature and humidity of the environment, that is, the tablet slowly absorbs moisture, so that the disintegrating agent cannot play its disintegration role, so the disintegration of the tablet becomes relatively slow The disintegration of sugar containing tablets was prolonged obviously after high storage temperature or humidification.
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