Xinhua News Agency, Beijing (Reporter Zhang Zhaohui) — On October 12, Qilu Pharmaceutical's official WeChat account announced that the long-acting microcrystal formulation, Paliperidone Palmitate Injection, has been approved for marketing and is deemed to have passed the consistency evaluation. The drug is used for the treatment of acute and maintenance phases of schizophrenia and is China’s first domestically produced monthly-administration long-acting microcrystal formulation to be approved for marketing.
Palmitate paliperidone is a prodrug of paliperidone, which forms a drug reservoir at the injection site after intramuscular injection, allowing for the slow release of the drug. The free drug palmitate paliperidone released from the reservoir is rapidly hydrolyzed by esterases into the highly active paliperidone, which simultaneously antagonizes central dopamine 2 (D2) receptors and serotonin 2 (5HT2A) receptors, thereby exerting therapeutic effects on schizophrenia.
As a novel atypical antipsychotic long-acting injectable microcrystal drug, paliperidone palmitate injection utilizes nano-grinding technology to precisely control the particle size distribution of the drug, overcoming the time-lag barrier in drug release without the need for oral supplementation. Compared with traditional antipsychotic drugs, this product requires administration only once a month, offering distinct advantages in terms of clinical medication management convenience, preventing missed doses by patients, effectively reducing relapse and rehospitalization rates, and alleviating the burden on families and society.
As a special and complex formulation, the long-acting microcrystal formulation presents extremely high technical barriers in terms of preparation technology, quality control, and production equipment. Although the patent for paliperidone palmitate injection expired many years ago after being on the Chinese market for over a decade, there has been no generic version launched in China, and internationally, generics are also scarce.
Proofread by Baoqing Liu