title: Injectable long-term control-released in situ gels of hydrochloric thiothixene for the treatment of schizophrenia: preparation, in vitro and in vivo evaluation.
abstract: Hydrochloric thiothixene (HT) is an antipsychotic drug used in the treatment of various psychoses including schizophrenia, mania, polar disorder, and in behavior disturbances. However, because the psychotics often could not control their behaviors, the independent administration of antipsychotic drug based on medical order was difficult. The omissions of the administration often brought an unsatisfactory therapeutic efficacy. A novel injectable long-term control-released in situ gel of HT for the treatment of schizophrenia was developed based on biodegradable material polylactic acid (PLA). The optimum formulation of the injectable PLA-based HT in situ gel containing 15% (w/w) HT and 45% (w/w) PLA with benzyl benzoate was used as a gelling solvent. The results of the in vitro and in vivo studies showed that this in situ gel had a long-term period of drug release for several weeks and a good histocompatibility without any remarkable inflammatory reactions.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Che
authors.initials: C
authors.lastname: Xin
authors.affiliation: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Wang
authors.initials: W
authors.lastname: Lihong
authors.affiliation: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Li
authors.initials: L
authors.lastname: Qiuyuan
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address: xhm_79@yahoo.com.cn.
authors.forename: Liu
authors.initials: L
authors.lastname: Hongzhuo
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D001565:Benzoates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005782:Gels; D006801:Humans; D007273:Injections, Intramuscular; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D011091:Polyesters; D011108:Polymers / Q000737:chemistry*; D017208:Rats, Wistar; D012559:Schizophrenia / Q000188:drug therapy*; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013888:Thiothixene / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D014150:Antipsychotic Agents; D001565:Benzoates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005782:Gels; D011091:Polyesters; D011108:Polymers; D019344:Lactic Acid; C033616:poly(lactide); D013888:Thiothixene; C006723:benzyl benzoate
keywords: Biodegradable; Control-released; Hydrochloric thiothixene; In situ gel; Injectable; PLA; Schizophrenia