• Korean Journal of Schizophrenia Research
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• v.21 no.2
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• pp.74-80
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• 2018

Objectives : This study investigated whether long-acting injectable (LAI) paliperidone is different from its oral form in terms of the effect on cognitive function in schizophrenia spectrum and other psychotic disorders. Methods : We reviewed the medical records of patients in Seoul National University Bundang Hospital who were diagnosed as having schizophrenia and/or other psychotic disorders based on DSM-5 from 2016 to 2017. Seven patients were treated with oral paliperidone and 11 were treated with paliperidone palmitate. All patients underwent clinical and neuropsychological assessment, including the Korean version of the MATRICS Consensus Cognitive Battery (MCCB) at their first visit or within one month of their initial treatment. MCCB was repeated within three to 12 months after the initial assessment. Results : There was no significant difference between the two groups in most cognitive domains including speed of processing, attention and vigilance, working memory, verbal learning, visual learning and reasoning and problem solving domain. However, patients treated with paliperidone palmitate showed better improvement in social cognition domain than those taking oral paliperidone. The standardized values of social cognition domain scores had significantly improved over time in patients under paliperidone palmitate, demonstrating a significant time-by-group interaction. Conclusion : Our results show that long-acting injectable paliperidone could be helpful in some aspects of improving cognitive function in schizophrenia spectrum and other psychotic disorders. Further studies with other antipsychotics are necessary to generalize the results.

• Clinical Psychopharmacology and Neuroscience
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• v.16 no.4
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• pp.361-375
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• 2018

We aimed to compare the efficacy and safety of long-acting injectable (LAI) and oral second-generation antipsychotics (SGAs) in treating schizophrenia by performing a systematic review and meta-analysis. MEDLINE, EMBASE, PsycINFO, CINAHL, and the Cochrane Library, as well as five Korean databases, were systemically searched to identify studies published from 2000 to 16 April 2015, which compared the efficacy and safety of LAI and oral SGAs. Using data from randomized controlled trials (RCTs), meta-analyses were conducted. In addition, the GRADE (the Grading of Recommendations, Assessment, Development and Evaluation) approach was applied to explicitly assess the quality of the evidence. A total of 30 studies including 17 RCTs and 13 observational studies were selected. The group treated with LAI SGAs was characterized by significantly lower relapse rates, longer times to relapse and fewer hospital days, but also by a higher occurrence of extrapyramidal syndrome and prolactin-related symptoms than that in the group treated with oral SGAs. Our findings demonstrate that there is moderate to high level of evidence suggesting that in the treatment of schizophrenia, LAI SGAs have higher efficacy and are associated with higher rates of extrapyramidal syndrome and prolactin-related symptoms. Additionally, the use of LAI SGAs should be combined with appropriate measures to reduce dopamine $D_2$ antagonism-related symptoms.

• Korean Journal of Veterinary Service
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• v.17 no.1
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• pp.54-60
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• 1994

Anaplasmosis is a tick-borne disease mainly of cattle, sheep, and goats. Anaplasmosis in goat had been reported at last year by authors. The disease brought the economic losses in the goat farm in Chonbuk province. In order to treat the disease, a long-acting formulation terramycin injectable solution was used experimental animals which indigenous goats were sick with moderate anemia. We were devided into two groups was treated with single dosage (20mg /kg of body weight). one group was treated with single injection, the other group was treated with twice of the same dosage intramusculary injection. The results indicate that the use of long-acting terramycin would minimize clinical signs of anaplasmosis infection in goat. After treament the differrences of hematological appearences and parasitaemia were observed in the effect of terramycin treatment. obviously, increased value of RBC. HB and HCT, and parasitaemia by means of Giemsa staining and acrydine orange staining was observed decreased due to treatment.

• Journal of Pharmaceutical Investigation
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• v.26 no.1
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• pp.13-22
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• 1996

Poly(D,L-lactic acid) (PLA) microspheres containing alprazolam(APZ) were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of APZ to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like APZ crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of APZ for long-acting injectable delivery system in vitro, which would aid in predicting in vitro release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

• Korean Journal of Biological Psychiatry
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• v.20 no.3
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• pp.111-117
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• 2013

Objectives We investigated the effectiveness and safety when treated in schizophrenics with paliperidone palmitate, a long acting injectable antipsychotic. Methods This was a 24-week open-label study, performed at one center in Korea. The eligible patients with schizophrenia diagnosed by Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, Text Revision (DSM-IV-TR) criteria were enrolled. Patients received long-acting paliperidone palmitate injection (234 mg, baseline; 156 mg, week 1 ; then once 4 weeks flexible dosing). Effectiveness assessments were measured by the Positive and Negative Syndrome Scale (PANSS), The Clinical Global Impression Severity Scale (CGI-S), The Personal and Social Performance (PSP) at baseline, week 1, every 4 weeks untill 24 weeks or endpoint. Safety assessments were measured by The Extrapyramidal Symptom Rating Scale (ESRS), body weight (BW) and incidence of adverse events. Oral antipsychotics were stopped or tapered off within next 14 days. Results Of 20 patients recruited, 9 patients (45%) completed the study. Paliperidone palmitate produced a significant improvement in PANSS total score from baseline to endpoint. The response rate was 75% [mean change (${\pm}SD$) $-25.9{\pm}14.4$, all p < 0.001]. The CGI-S and PSP total scores significantly improved during 24 weeks (All p < 0.001). Eighty percent of patients reported adverse events and most common adverse events (${\geq}10%$) in paliperidone palmitate were anticholinergic adverse event, extrapyramidal symptoms, weight gain, akathisia, insomnia, headache, agitation, anxiety and GI trouble. ESRS score is not statistically significant, but tends to get better at the end of the study when compared to baseline. Conclusions Our study results demonstrated maintained effectiveness and safety of paliperidone palmitate treatment in schizophrenics. And provides both clinicians and patients with a new choice of treatment that can improve the outcome of long term therapy. Their potential effectiveness and safety should be better addressed by future randomized-controlled trials.

• Journal of Pharmaceutical Investigation
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• v.36 no.3
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• pp.175-184
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• 2006

Poly(D,L-lacic acid)(PLA) microshperes containing loazepam were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of lorazepam to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like lorazepam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of lorazepam for long-acting injectable delivery system in vitro, which would aid in Predicting in vivo release Profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

• Journal of Pharmaceutical Investigation
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• v.38 no.1
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• pp.63-72
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• 2008

Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to $PLA^{\circ}{\AE}s$ with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.

• Journal of Pharmaceutical Investigation
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• v.41 no.3
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• pp.173-178
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• 2011

Injectable chitosan hydrogels have attracted great potential due to sustained-release property and safety. Here, palmityl-acylated glycol chitosan (Pal-GC) was used to generate physically cross-linked hydrogels by virtue of hydrophobic attraction of linear fatty carbons. Glycol chitosan was chemically modified with N-hydroxysuccinimide-activated palmitic acid in dimethylsulfoxide (DMSO) containing dimethylaminopyridine. Through a series of preparation steps of (i) dialysis with DMSO, (ii) addition of palmityl-acylated exendin-4 (Ex4-C16), and (iii) dialysis with water, Pal-GC was self-assembled to form physically cross-linked hydrogels entrapped with Ex4-C16. The Pal-GC derivative was analyzed by using 1H NMR, and the surface morphology of Pal-GC hydrogels formed was examined by scanning electron microscopy. Also, the hypoglycemic effect induced by Pal-GC hydrogels containing Ex4-C16 (250 nmol/kg) was evaluated in non-fasted type 2 diabetic db/db mice and compared with GC hydrogels containing native Ex4 at the same dose. Results showed that palmityl group was successfully conjugated with the amines of glycol chitosan, and that Pal-GC efficiently generated the hydrogels formation. Moreover, Pal-GC hydrogels containing Ex4-C16 was found to greatly prolong the hypoglycemia duration (~ 4 days). This was due to the dual-functions of the palmityl groups present in both GC and exendin-4 such as hydrophobic attraction and plasma albumin-binding. We consider this new type of self-assembled GC hydrogels loaded with Ex4-C16 would be a promising long-acting sustained-release system with anti-diabetic property.