Paliperidone palmitate is an atypical long acting antipsychotics，which
can fast onset in acute phase and continuously improve the symptoms in
maintenance phase． It has the solid efficacy and convenient
ad[1]ministration，which offer a new option for schizophrenia treatment
and will help patients to adhere the treatment and prevent relapse． As
the sole long acting antipsychotics with monthly injection，it was
approved by CFDA in 2011 and indicated for the acute and maintenance
treatment of schizophrenia．
ChEBI: 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate is a fatty acid ester obtained by the formal condensation of the carboxy group of hexadecanoic acid with the hydroxy group of 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one. It is a member of 1,2-benzoxazoles, a heteroarylpiperidine, an organofluorine compound, a pyridopyrimidine and a fatty acid ester.
The review of the literature also underlined that paliperidone palmitate
is well tolerated, compared with placebo. Frequency and severity of
side-effects such as extrapyramidal symptoms, hyperprolactinemia and
weight gain, was similar or less than those found in treatment with
other atypical antipsychotics, including long-acting ones.
Aseptic air-flow mill was used to control the crushing pressure of 3~5bar, and the sterile paliperidone palmitate was crushed to the effective particle size of 2~15μm. Weighed 12g of sodium carboxymethyl cellulose, placed in about 500ml of injectable water, dissolved, dissolved; and then took 15g of injectable polysorbate 80, 40g of mannitol, 0.9g of sodium dihydrogen phosphate, stirred to dissolve, and then adjust the pH value to 7.0 by using 0.5 M sodium hydroxide solution to adjust the pH to 7.0. Weigh 312g of micronized sterile papanicolone palmitate was added to the above solution, stirred and sheared until uniformly dispersed, replenished with water for injection, and the volume of the material was fixed to 1000 ml, to obtain the aseptic papanicolone palmitate suspension with an effective particle size in the range of 2~15μm.
