Preparation of diclofenac sodium immediate-release micro-tablets by direct pressure method with DCPA/MCC

In this study, a combination of anhydrous calcium hydrogen phosphate A150 (DCPA) and microcrystalline cellulose 102 was used, without additional disintegrants, and a direct pressure method was used to prepare an immediate release microparticle with satisfactory mechanical strength and disintegration properties.

Microchip 

Microtablet is a new dosage form of modern solid medicine that has been widely used and developed in recent years

Materials and Method 

• Diclofenac sodium: API, accounting for 10%

• Anhydrous Calcium Hydrogen Phosphate (DI-CAFOS®A150): The particle size is 150μm, the porosity is about 70%, accounting for 61.

  
  

  Recommended supplier: Budenheim, F2017000063 has been activated

  
  

• Microcrystalline cellulose 102: the particle size is about 130μm, accounting for 27.

  
  

  Recommended supplier: Dongchen Pharmaceutical, F20180000805

• Sodium stearyl fumarate: lubricant, accounting for 1.

  
  

  Recommended supplier: SPI

method:The components were mixed for 15 min → sodium stearyl fumarate was mixed for 1 min → a concave punch with a diameter of 3 mm was pressed at 0.

The process of preparing microchips by the direct pressure method using the above-mentioned materials is smooth and trouble-free

(Note: The point of view here that "the difference between the actual content value and the estimated value is acceptable " comes from a German supplier, and the domestic application needs to be verified)

Mechanical properties and dissolution of diclofenac sodium microtablets:

Table 1.

Figure 1.

1.

2.

3.

5.
As shown in Figure 1, there are slight differences in the dissolution profiles of microtablets prepared at different pressures, which are related to the hardness of the microtablets and the disintegration time
.
The dissolution and drug release ratios of different microtablets were similar after 20 minutes, and all reached 80% or more after 30 minutes
.

6.
It should be noted that the microtablets do not contain typical disintegrants, only 27% of microcrystalline cellulose 102 is added, but the disintegration and dissolution can achieve the desired effect
.
This is because the porosity of the anhydrous calcium hydrogen phosphate A150 as high as 70% ensures the rapid and full disintegration of the formulation
.

 in conclusion 

• 
  In this study, a combination of anhydrous calcium hydrogen phosphate (DCPA) and microcrystalline cellulose was used without additional disintegrants.
  The direct compression method was used to prepare microtablets with satisfactory mechanical strength and disintegration properties.
  This method was used to prepare microtablets with satisfactory mechanical strength and disintegration properties.
  The microtablets can be further processed through steps such as coating
  .
  

• 
  The size of the microtablets allows the filling of hard capsules with diclofenac sodium microtablets containing 25 mg or even 50 mg doses
  .
  
  

• 
  The high porosity of anhydrous calcium hydrogen phosphate A150 enables the formulation to release about 80% of the drug within 30 minutes without disintegrating agent , which meets the requirements for disintegration of quick-release tablets
  .