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- Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 3² Factorial Design. [Journal Article]
- PPharmaceutics 2018 Nov 20; 10(4)
- Major depressive disorder (MDD) is one of the main contributors to disability and suicide mortality globally. Paroxetine hydrochloride (PHH) is the most potent antidepressant used for MDD treatment. …
Major depressive disorder (MDD) is one of the main contributors to disability and suicide mortality globally. Paroxetine hydrochloride (PHH) is the most potent antidepressant used for MDD treatment. Due to its reduced side effects PAXIL® CR is a widely-used controlled-release formulation of PHH. However, the complicated double-layer production of PAXIL® CR faces the risk of layer separation. In this study, PHH enteric coating single layer controlled-release tablets (PHH-EC-SLTs) were designed as a simplified substitution of PAXIL® CR through a rational formulation screening. The optimized PHH-EC-SLTs showed similar release behaviors in vitro to PAXIL® CR and the release profiles corresponded to a zero-order release model (R² = 0.9958). Polymer matrix erosion was the main release mechanism, according to the fitting exponents n > 1 in the Korsmeyer-Pappas model. Crucial pharmacokinetic parameters including peak-reaching time (Tmax), peak concentration (Cmax) and the area under the blood level-time curve (AUC0-48) of PHH-EC-SLTs and PAXIL® CR had no significant difference (p > 0.05) and the relative bioavailability (F = 97.97%) of PHH-EC-SLTs demonstrated their similar pharmacokinetic profiles in vivo. In view of avoiding layer separation risk and simplifying the preparation processing, the self-made PHH-EC-SLTs could be considered as a safe and economic alternative to PAXIL® CR.
- Drugs and Lactation Database (LactMed): Paroxetine [BOOK]
- BOOKNational Library of Medicine (US): Bethesda (MD)
- Because of the low levels of paroxetine in breastmilk, amounts ingested by the infant are small and paroxetine has not been detected in the serum of most infants tested. Occasional mild side effects …
Because of the low levels of paroxetine in breastmilk, amounts ingested by the infant are small and paroxetine has not been detected in the serum of most infants tested. Occasional mild side effects have been reported, especially in the infants of mothers who took paroxetine during the third trimester of pregnancy, but the contribution of the drug in breastmilk is not clear. Most authoritative reviewers consider paroxetine one of the preferred antidepressants during breastfeeding. Occasional mild side effects such as insomnia, restlessness and increased crying have ben reported in breastfed infants. Mothers taking an SSRI during pregnancy and postpartum may have more difficulty breastfeeding, although this might be a reflection of their disease state. These mothers may need additional breastfeeding support. Breastfed infants exposed to an SSRI during the third trimester of pregnancy have a lower risk of poor neonatal adaptation than formula-fed infants.
- The comparative evidence basis for the efficacy of second-generation antidepressants in the treatment of depression in the US: A Bayesian meta-analysis of Food and Drug Administration reviews. [Meta-Analysis]
- JAJ Affect Disord 2018 08 01; 235:393-398
- CONCLUSIONS: The results illustrate the importance of considering both the effect size and the evidence-load when judging the efficacy of a treatment. In doing so, the currently employed Bayesian approach provided clear insights on top of those gained with traditional approaches.
- Comparative effectiveness of switching paroxetine formulation for treatment of major depressive disorder: an open-label multicenter study. [Journal Article]
- NDNeuropsychiatr Dis Treat 2018; 14:955-966
- CONCLUSIONS: These results suggest that switching the treatment from IR to CR paroxetine could improve depressive symptoms and decrease ADRs. However, these results may have been caused by the psychological effect of drug switching. Hence, future studies with blinded evaluation methods are required to confirm and expand our findings.
- Cross-sectional networks of depressive symptoms before and after antidepressant medication treatment. [Randomized Controlled Trial]
- SPSoc Psychiatry Psychiatr Epidemiol 2018; 53(6):617-627
- CONCLUSIONS: Findings suggest the effects of SSRIs can be studied using the network approach. The increased connectivity, predictability, and communities at week 8 may be explained by the decrease in depressive symptoms rather than specific effects of SSRIs. Future studies with larger samples and placebo controls are needed to offer insight into the effects of SSRIs.
- Parquetina nigrescens leaves: chemical profile and influence on the physical and biochemical indices of sexual activity of male Wistar rats. [Journal Article]
- JIJ Integr Med 2017; 15(1):64-76
- CONCLUSIONS: The AEPN restored both the physical and biochemical indices of male sexual activity/competence via changes in reproductive hormones, NO and PDE5 activity. The pro-sexual activity, attributed to a myriad of mineral, amino acid and secondary metabolite constituents, was best at 80 mg/kg BW of AEPN.
- Single- and multiple-dose pharmacokinetics and tolerability of a paroxetine controlled-release tablet in healthy Chinese subjects . [Clinical Trial, Phase I]
- IJInt J Clin Pharmacol Ther 2017; 55(3):231-236
- CONCLUSIONS: Paroxetine CR tablet is absorbed with a delay of ~ 4 hours after oral administration, and the accumulation factor is ~ 9 at steady state. Paroxetine CR tablet is well tolerated by healthy Chinese subjects. .
- Safety and effectiveness of controlled-release paroxetine in routine clinical practice: results of a postmarketing surveillance study of patients with depression. [Journal Article]
- NDNeuropsychiatr Dis Treat 2015; 11:435-52
- CONCLUSIONS: The results of this study suggest that paroxetine CR is a well-tolerated and efficacious treatment for depression in routine clinical practice.
- Luteal phase and symptom-onset dosing of SSRIs/SNRIs in the treatment of premenstrual dysphoria: clinical evidence and rationale. [Journal Article]
- CDCNS Drugs 2013; 27(8):583-9
- Premenstrual dysphoria (PMD) affects 3-8 % of women in their reproductive years worldwide. This paper summarizes the studies establishing the efficacy of continuous, luteal phase, and symptom-onset d…
Premenstrual dysphoria (PMD) affects 3-8 % of women in their reproductive years worldwide. This paper summarizes the studies establishing the efficacy of continuous, luteal phase, and symptom-onset dosing of selective serotonin reuptake inhibitors (SSRIs) and dual serotonin and norepinephrine reuptake inhibitors (SNRIs) in treating women with PMD. The evidence indicates that for some women, symptom-onset dosing with escitalopram, fluoxetine, and paroxetine controlled release (CR) is as effective as continuous or luteal phase dosing. The wide range of clinical efficacy of SSRIs/SNRIs suggests that they exert their therapeutic effect through multiple pathways. This paper offers a few alternative mechanisms of action to explain the rapid response to SSRIs/SNRIs in women with PMD.
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- Development and comparative evaluation of in vitro, in vivo properties of novel controlled release compositions of paroxetine hydrochloride hemihydrate as against Geomatrix™ platform technology. [Journal Article]
- DDDrug Dev Ind Pharm 2013; 39(8):1175-86
- The objective of this study is to develop, in vitro and in vivo evaluation of novel approaches for controlled release of paroxetine hydrochloride hemihydrate (PHH) in comparison to patented formulati…
The objective of this study is to develop, in vitro and in vivo evaluation of novel approaches for controlled release of paroxetine hydrochloride hemihydrate (PHH) in comparison to patented formulation PAXIL CR(®) tablets of GlaxoSmithKline (Geomatrix™ technology). In one of the approaches, hydrophilic core matrix tablets containing 85% of the dose were prepared and further coated with methacrylic acid copolymer to delay the release. An immediate release coating of 15% was given as top coat. The tablets were further optionally coated using ethyl cellulose. In the second approach, hydrophobic matrix core tablets containing metharylic acid copolymer were prepared. In the third approach, PHH was granulated with enteric polymer and further hydrophobic matrix core tablets were prepared. The effect of polymer concentration, level of enteric coating on drug release was evaluated by in vitro dissolution study by varying dissolution apparatus and the rotation speeds. It was found that increase in concentration of high viscosity hydroxypropylmethylcellulose (HPMC) resulted in reduction of the release rate. The drug release was observed to be dependent on the level of enteric coating and ethyl cellulose coating, being slower at increased coating. The release mechanism of PHH followed zero-order shifting to dissolution dependent by the increase of HPMC content. The formulation was stable without change in drug release rate. In vivo study in human volunteers confirmed the similarity between test and innovator formulations. In conclusion, HPMC-based matrix tablets, which were further coated using methacrylic acid copolymer, were found to be suitable for the formulation of single layer-controlled release PHH.