Introduction

Paliperidone palmitate injection is a long-acting aqueous suspension for intramuscular injection. It is a long-acting injection form of the second-generation antipsychotic drug paliperidone.

Paliperidone palmitate suspension prepared by ATS

Preparation method:
(1) Pre-dispersion: Weigh the polysorbate and add it to 1/3-1/2 of the water, stir evenly, then add citric acid, polyethylene glycol, disodium hydrogen phosphate, sodium dihydrogen phosphate and hydroxide in sequence. After removing the sodium, add the remaining water, cut, and set aside;
(2) Mixing: Weigh the raw material paliperidone palmitate, add the solution prepared in step (1), and cut until the raw material and solution are fully mixed;
(3) Homogenization: Add the pre-dispersed solution in step (2) into a homogenizer, control the temperature with a chiller, homogenize 7 times, take a sample to detect the particle size, and obtain the paliperidone palmitate preparation.

Preparation difficulties:
This sample is a sterile preparation. The original research requires small particle size, and it is difficult to achieve the target particle size.

Solution:
ATS can customize online sterilization equipment according to needs, and cooperate with the sterile environment to achieve full aseptic operation. Special processes can be designed to achieve the required particle size.

Result:

The results of different processing times

compare results

Summarize:
In the preparation process of paliperidone palmitate injection, the use of a ball mill to grind and disperse the materials can also achieve the effect of reducing the particle size and dispersing uniformly. The effect will be better if the beads are small and the time is long; but the use of a high-pressure homogenizer can achieve uniform dispersion. quality, the particle size reduction effect is more obvious, and the particle size distribution span is small, and it is evenly dispersed, very close to the original research.