scholarly journals Pharmacokinetic Evaluation of Twice-Daily Extended-Release Carbamazepine (CBZ) and Four-Times-Daily Immediate-Release CBZ in Patients with Epilepsy

Epilepsia ◽  
1998 ◽  
Vol 39 (3) ◽  
pp. 274-279 ◽  
Author(s):  
William R. Garnett ◽  
Benjamin Levy ◽  
Angus M. McLean ◽  
Yuxin Zhang ◽  
Richard A. Couch ◽  
...  
Keyword(s):  
Extended Release ◽  
Immediate Release ◽  
Patients With Epilepsy ◽  
Pharmacokinetic Evaluation

scholarly journals QbD based Eudragit coated Meclizine HCl immediate and extended release multiparticulates: formulation, characterization and pharmacokinetic evaluation using HPLC-Fluorescence detection method

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Faaiza Qazi ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Fahad Siddiqui ◽  
Muhammad Iqbal Nasiri ◽  
...  
Keyword(s):  
Extended Release ◽  
Geometric Mean ◽  
Compartmental Analysis ◽  
Immediate Release ◽  
Drug Analysis ◽  
Fluorescence Method ◽  
Pharmacokinetic Parameters ◽  
Comparative Pharmacokinetic ◽  
Time Period ◽  
Pharmacokinetic Evaluation

Abstract This study is based on the QbD development of extended-release (ER) extruded-spheronized pellets of Meclizine HCl and its comparative pharmacokinetic evaluation with immediate-release (IR) pellets. HPLC-fluorescence method was developed and validated for plasma drug analysis. IR drug cores were prepared from lactose, MCC, and PVP using water as granulating fluid. Three-level, three-factor CCRD was applied for modeling and optimization to study the influence of Eudragit (RL100-RS100), TEC, and talc on drug release and sphericity of coated pellets. HPLC-fluorescence method was sensitive with LLOQ 1 ng/ml and linearity between 10 and 200 ng/ml with R2 > 0.999. Pharmacokinetic parameters were obtained by non-compartmental analysis and results were statistically compared using logarithmically transformed data, where p > 0.05 was considered as non-significant with a 90% CI limit of 0.8–1.25. The AUC0–t and AUC0–∞ of ER pellets were not significantly different with geometric mean ratio 1.0096 and 1.0093, respectively. The Cmax of IR pellets (98.051 ng/ml) was higher than the ER pellets (84.052 ng/ml) and the Tmax of ER pellets (5.116 h) was higher than the IR pellets (3.029 h). No significant food effect was observed on key pharmacokinetic parameters of ER pellets. Eudragit RL100 (6%) coated Meclizine HCl pellets have a potential therapeutic effect for an extended time period.

scholarly journals Successful bilateral electroconvulsive therapy in a patient with a seizure disorder taking levetiracetam, lorazepam, and zonisamide: A case report

2021 ◽  
Vol 11 (1) ◽  
pp. 23-26
Author(s):  
Ian R. McGrane ◽  
Rachel E. Tenison ◽  
Dana M. Bimler ◽  
Robert C. Munjal ◽  
Jason R. Molinaro
Keyword(s):  
Bipolar Disorder ◽  
Electroconvulsive Therapy ◽  
Extended Release ◽  
Medication Management ◽  
Immediate Release ◽  
Seizure Threshold ◽  
Treatment Resistant ◽  
Evening Dose ◽  
Patients With Epilepsy ◽  
Higher Doses

Abstract Electroconvulsive therapy (ECT) may be considered for treatment of severe, treatment-resistant, and emergent depression associated with MDD or bipolar disorder. Patients with epilepsy usually take medications that raise the seizure threshold, which poses challenges during ECT. We report a 66-year-old male with epilepsy taking levetiracetam extended-release (XR), lorazepam, and zonisamide requiring ECT for severe MDD. After literature review, the XR form of levetiracetam was changed to higher doses of the immediate-release (IR) formulation, and zonisamide was discontinued 2 days prior to ECT in the hospital and was resumed when the patient underwent outpatient continuation ECT. The patient was treated to remission after receiving 8 acute bilateral ECT treatments before being transitioned to continuation ECT. We provide a brief review of medication management of antiepileptic drugs and other medications that increase the seizure threshold during ECT. To our knowledge, this is the first reported case describing the management of levetiracetam, lorazepam, and zonisamide concomitantly during ECT. Our case suggests that utilizing the IR formulation of levetiracetam, administering the evening dose early the day prior to the procedure, and temporarily discontinuing zonisamide prior to bilateral ECT is effective for the treatment of severe MDD while maintaining seizure prophylaxis.

Comparative steady-state pharmacokinetic evaluation of immediate-release topiramate and USL255, a once-daily extended-release topiramate formulation

Epilepsia ◽  
2013 ◽  
Vol 54 (8) ◽  
pp. 1444-1452 ◽  
Author(s):  
Meir Bialer ◽  
Tawfeeq Shekh-Ahmad ◽  
Tricia L. Braun ◽  
Mark B. Halvorsen
Keyword(s):  
Steady State ◽  
Extended Release ◽  
Immediate Release ◽  
Once Daily ◽  
Pharmacokinetic Evaluation

scholarly journals Benznidazole Extended-Release Tablets for Improved Treatment of Chagas Disease: Preclinical Pharmacokinetic Study

2016 ◽  
Vol 60 (4) ◽  
pp. 2492-2498 ◽  
Author(s):  
Marcelo Gomes Davanço ◽  
Michel Leandro Campos ◽  
Talita Atanazio Rosa ◽  
Elias Carvalho Padilha ◽  
Alejandro Henao Alzate ◽  
...  
Keyword(s):  
Chagas Disease ◽  
Extended Release ◽  
Hydroxypropyl Methylcellulose ◽  
Immediate Release ◽  
Relative Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Therapeutic Success ◽  
Preclinical Pharmacokinetics ◽  
Bioavailability Study

ABSTRACTBenznidazole (BNZ) is the first-line drug for the treatment of Chagas disease. The drug is available in the form of immediate-release tablets for 100-mg (adult) and 12.5-mg (pediatric) doses. The drug is administered two or three times daily for 60 days. The high frequency of daily administrations and the long period of treatment are factors that significantly contribute to the abandonment of therapy, affecting therapeutic success. Accordingly, this study aimed to evaluate the preclinical pharmacokinetics of BNZ administered as extended-release tablets (200-mg dose) formulated with different types of polymers (hydroxypropyl methylcellulose K4M and K100M), compared to the tablets currently available. The studies were conducted with rabbits, and BNZ quantification was performed in plasma and urine by ultraperformance liquid chromatography methods previously validated. The bioavailability of BNZ was adequate in the administration of extended-release tablets; however, with the administration of the pediatric tablet, the bioavailability was lower than with other tablets, which showed that the clinical use of this formulation should be monitored. The pharmacokinetic parameters demonstrated that the extended-release tablets prolonged drug release from the pharmaceutical matrix and provided an increase in the maintenance of the drug concentrationin vivo, which would allow the frequency of administration to be reduced. Thus, a relative bioavailability study in humans will be planned for implementation of a new product for the treatment of Chagas disease.

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