Preparation andIn Vitro/In VivoEvaluation of Vinpocetine Elementary Osmotic Pump System

Preparation andin vitroandin vivoevaluation of vinpocetine (VIN) elementary osmotic pump (EOP) formulations were investigated. A method for the preparation of VIN elementary osmotic pump tablet was obtained by adding organic acid additives to increase VIN solubility. VIN was used as the active pharmaceutical ingredient, lactose and mannitol as osmotic agent. Citric acid was used as increasing API solubility and without resulting in the API degradation. It is found that the VIN release rate was increasing with the citric acid amount at a constant range. Cellulose acetate 398-3 was employed as semipermeable membrane containing polyethylene glycol 6000 and diethyl-o-phthalate as pore-forming agent and plasticizer for controlling membrane permeability. In addition, a clear difference between the pharmacokinetic patterns of VIN immediate release and VIN elementary osmotic pump formulations was revealed. The area under the plasma concentration-time curve after oral administration of elementary osmotic pump formulations was equivalent to VIN immediate release formulation. Furthermore, significant differences found for mean residence time, elimination half-life, and elimination rate constant values corroborated prolonged release of VIN from elementary osmotic pump formulations. These results suggest that the VIN osmotic pump controlled release tablets have marked controlled release characters and the VIN osmotic pump controlled release tablets and the normal tablets were bioequivalent.

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Concentration-effect relationship of levodopa in patients with Parkinson's disease after oral administration of an immediate release and a controlled release formulation.

British Journal of Clinical Pharmacology ◽

10.1111/j.1365-2125.1995.tb04407.x ◽

1995 ◽

Vol 39 (1) ◽

pp. 39-44 ◽

Cited By ~ 10

Author(s):

S Harder ◽

H Baas ◽

N Bergemann ◽

L Demisch ◽

S Rietbrock

Keyword(s):

Parkinson’S Disease ◽

Parkinson's Disease ◽

Controlled Release ◽

Oral Administration ◽

Immediate Release ◽

Concentration Effect ◽

Release Formulation ◽

Effect Relationship ◽

Controlled Release Formulation ◽

Relationship Of

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Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 32 Factorial Design

Pharmaceutics ◽

10.3390/pharmaceutics10040243 ◽

2018 ◽

Vol 10 (4) ◽

pp. 243 ◽

Cited By ~ 1

Author(s):

Yao Yang ◽

Zhengwei Huang ◽

Xuan Zhang ◽

Jinyuan Li ◽

Ying Huang ◽

...

Keyword(s):

Controlled Release ◽

Single Layer ◽

Suicide Mortality ◽

Pharmacokinetic Parameters ◽

Release Mechanism ◽

Time Curve ◽

Layer Separation ◽

Significant Difference ◽

Paroxetine Hydrochloride ◽

Controlled Release Tablets

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.

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Double-layered osmotic pump controlled release tablets of actarit: In vitro and in vivo evaluation

Asian Journal of Pharmaceutical Sciences ◽

10.1016/j.ajps.2018.05.009 ◽

2019 ◽

Vol 14 (3) ◽

pp. 340-348 ◽

Cited By ~ 6

Author(s):

Yuenan Li ◽

Hao Pan ◽

Hongliang Duan ◽

Jianting Chen ◽

Zhihong Zhu ◽

...

Keyword(s):

Controlled Release ◽

Osmotic Pump ◽

In Vivo Evaluation ◽

Controlled Release Tablets

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Tacrolimus Intrapatient Variability After Switching From Immediate or Prolonged-Release to Extended-Release Formulation, After an Organ Transplantation

Frontiers in Pharmacology ◽

10.3389/fphar.2021.602764 ◽

2021 ◽

Vol 12 ◽

Author(s):

Arnaud Del Bello ◽

Clotilde Gaible ◽

Nathalie Longlune ◽

Anne-Laure Hebral ◽

Laure Esposito ◽

...

Keyword(s):

Extended Release ◽

Organ Transplant ◽

Immediate Release ◽

Prolonged Release ◽

Solid Organ ◽

Safe Procedure ◽

Release Formulation ◽

Blood Concentrations ◽

Extended Release Formulation ◽

Before And After

Background and Purpose: Several formulations of tacrolimus are available, but evidence of the benefit of changing to the most recent formulations is lacking. Tacrolimus intra-patient variability (tacrolimus IPV) is an emerging risk factor associated with poor graft outcomes after solid organ transplantations. Here, we examined the modifications of tacrolimus IPV after switching to a different formulation of tacrolimus.Experimental Approach: We identified 353 solid organ transplant recipients that were switched in our center from immediate-release (IR-tacrolimus) or prolonged-release tacrolimus (PR-tacrolimus) to extended-release, LCP-tacrolimus (LCP-tacrolimus). Among them, 54 patients underwent at least 3 available tacrolimus blood concentrations before and after the switch, allowing us to investigate tacrolimus IPV.Key Results: The switch was considered as a safe procedure since only four of the 353 patients presented a graft rejection after the switch, and no patient was hospitalized for tacrolimus overdose. The tacrolimus IPV estimated by the coefficient of variation (CV-IPV) was stable before and after the switch to LCP-tacrolimus (CV-IPV: 29.0% (IQR 25–75 (15.5; 38.5) before and 24.0% (15.8; 36.5) after the switch, p = 0.65).Conclusion and Implications: Switching from IR- or PR-tacrolimus to LCP-tacrolimus is a safe procedure. However, the CV-tacrolimus IPV was not impacted by the change of formulation.

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Efficacy and Safety of Ivabradine Once-Daily Prolonged-Release versus Twice-Daily Immediate-Release Formulation in Patients with Stable Chronic Heart Failure with Systolic Dysfunction: A Randomized, Double-Blind, Phase 3 Non-Inferiority (PROFICIENT) Study

Cardiology and Therapy ◽

10.1007/s40119-020-00200-8 ◽

2020 ◽

Vol 9 (2) ◽

pp. 505-521

Author(s):

Ajit Mullasari ◽

Keyword(s):

Heart Failure ◽

Chronic Heart Failure ◽

Systolic Dysfunction ◽

Immediate Release ◽

Prolonged Release ◽

Efficacy And Safety ◽

Phase 3 ◽

Double Blind ◽

Release Formulation ◽

Once Daily

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Comparative Efficacy of a Once-Daily Controlled-Release Formulation of Glipizide and Immediate-Release Glipizide in Patients With NIDDM

Diabetes Care ◽

10.2337/diacare.17.12.1460 ◽

1994 ◽

Vol 17 (12) ◽

pp. 1460-1464 ◽

Cited By ~ 36

Author(s):

M. Berelowitz ◽

C. Fischette ◽

W. Cefalu ◽

D. S. Schade ◽

T. Sutfin ◽

...

Keyword(s):

Controlled Release ◽

Immediate Release ◽

Comparative Efficacy ◽

Release Formulation ◽

Once Daily ◽

Controlled Release Formulation

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Design of a controlled release osmotic pump system of ibuprofen

International Journal of Pharmaceutics ◽

10.1016/s0378-5173(97)00250-0 ◽

1997 ◽

Vol 158 (1) ◽

pp. 91-97 ◽

Cited By ~ 20

Author(s):

Nurten Özdemir ◽

Jülide Sahin

Keyword(s):

Controlled Release ◽

Osmotic Pump ◽

Pump System

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Oral Administration of Zolpidem Tartrate in an Abuse-deterrent Formulation Versus an Immediate Release Formulation in Beagle Dogs

Scandinavian Journal of Materials Science ◽

10.2340/scandjms.v1.41 ◽

2021 ◽

pp. 1-6

Author(s):

Amina Vazda ◽

Wei Xia ◽

Håkan Engqvist

Keyword(s):

Controlled Release ◽

Oral Administration ◽

Chemical Properties ◽

Immediate Release ◽

Prescription Drug Abuse ◽

Pharmacokinetic Analysis ◽

Beagle Dogs ◽

Release Formulation ◽

Physical And Chemical ◽

Plasma Profile

Objective: The continuing rise of prescription drug abuse has greatly necessitated the development of an abuse-deterrent formulation. Geopolymers are a promising base for drug design as they allow for tuneable drug release and possess superior physical and chemical properties compared with conventional pharmaceutical excipients.Methods: Geopolymer pellets containing zolpidem tartrate were administrated orally to beagle dogs as a controlled-release formulation with the commercial immediate-release product, Stilnoct® tablets, as the control.Results: The administration of zolpidem tartrate as immediate-release tablets demonstrated an elevated immediate release plasma profile and the zolpidem tartrate in the geopolymers demonstrated a controlled-release plasma profile. The pharmacokinetic analysis demonstrated that immediate-release tablet administration generated much higher plasma concentration when compared with geopolymer pellets administration for zolpidem tartrate. On the other hand, the geopolymer formulation prolonged the time of drug release.Conclusion: Oral administration of zolpidem tartrate in geopolymer pellets demonstrated a controlled-release plasma profile.

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