Once daily controlled release matrix tablet of Prochlorperazine maleate: Influence of Ethocel(?) and/or Methocel(?) on in vitro drug release and bioavailability.
Summary of "Once daily controlled release matrix tablet of Prochlorperazine maleate: Influence of Ethocel(?) and/or Methocel(?) on in vitro drug release and bioavailability."
Context: Controlled release (CR) matrix tablet of Prochlorperazine maleate was developed to improve its patient compliance. Methods: Tablet formulations F1, F2 and F3 based on different concentrations of Methocel(?) K100 LV-CR Premium, were compacted by direct compression method while tablet formulations F4, F5 and F6, based on distinct blends of Methocel(?) K100 LV-CR Premium and Ethocel(?) Standard 7FP Premium, were compressed by flow-bound dry granulation-slugging method. The prepared powder mixtures, granules and tablets were evaluated for their physicochemical performance. Bioequivalence study of the optimized test tablet versus reference-conventional Stemitil(?) tablet was conducted on rabbits, using HPLC-UV system at ?(max) 254?nm. Results: The test tablet, containing 28% Methocel(?) and 58% Ethocel(?) (F6) exhibited desired zero order kinetics for 24?h and was found stable at accelerated storage conditions for 6 months. In vitro drug release rate decreased as the Ethocel(?) content in the blend was increased, perhaps due to slower penetrability of water. Hydrodynamic conditions and hardness of tablets could not affect drug release kinetics. The tablet displayed significantly (p?0.05) optimized peak drug concentration-C(max) (45???3.42 vs. 64.5???4.03), extended half life-t(1/2) (16.071???3.97 vs. 5.257???1.314?h) and bioequivalence to the reference tablet taken three times a day (1409???15 ng?h/mL vs. 1346???23?ng h/mL). The tablet showed strong Level A correlation (R(2)?=?0.8458) between drug absorbed in vivo and drug released in vitro. Conclusion: The developed tablet may be adopted by pharmaceutical industry to improve patient compliance of the Prochlorperazine maleate.
Pharmacy, Univeristy of Peshawar , Peshawar 25120 Pakistan.
This article was published in the following journal.
Name: Drug development and industrial pharmacy
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/21749268
- DOI: http://dx.doi.org/10.3109/03639045.2011.595416
Medical and Biotech [MESH] Definitions
Dosage forms of a drug that act over a period of time by controlled-release processes or technology.
Matrix Metalloproteinase 20
A secreted matrix metalloproteinase that is the predominant proteolytic activity in the enamel matrix. The enzyme has a high specificity for dental enamel matrix protein AMELOGENIN.
Matrix Metalloproteinase 16
A transmembrane domain-containing matrix metalloproteinase. It is synthesized as an inactive zymogen that is activated by the proteolytic action of PROPROTEIN CONVERTASES. Matrix metalloproteinase 16 plays a direct role in the cleavage of proteins in the pericellular environment. In addition it can function indirectly by enzymatically activating the proprotein form of other MATRIX METALLOPROTEINASES such as the zymogen of MATRIX METALLOPROTEINASE 2.
Matrix Metalloproteinase 11
A secreted matrix metalloproteinase that is believed to play a role in EXTRACELLULAR MATRIX remodeling and cell fate determination during normal and pathological processes. Matrix metalloproteinase 11 was originally isolated in primary BREAST NEOPLASMS and may be involved in the process of tumorigenesis.
Containers, packaging, and packaging materials for drugs and biological products. These include those in ampule, capsule, tablet, solution or other forms. Packaging includes immediate-containers, secondary-containers, and cartons. In the United States, such packaging is controlled under the Federal Food, Drug, and Cosmetic Act which also stipulates requirements for tamper-resistance and child-resistance. Similar laws govern use elsewhere. (From Code of Federal Regulations, 21 CFR 1 Section 210, 1993) DRUG LABELING is also available.
Enalapril maleate, one of the Angiotensin converting enzyme (ACE) inhibitor is effective in the treatment of hypertension. Enalapril maleate is selected for the present study. The aim of this study wa...
Controlled-release (CR) matrix tablet of 4 mg risperidone was developed using flow bound dry granulation-slugging method to improve its safety profile and compliance. Model formulations F1, F2, and F...
To study the release profiles of Ambroxol hydrochloride in matrix tablets with different fillers and controlled release materials, and investigate the potential impact on different fillers on the matr...
A tablet formulation based on hydrophilic matrix with a controlled drug release was developed, and the effect of polymer concentrations on the release of primaquine diphosphate was evaluated. To achie...
Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel(R) K100 LV-CR and Ethocel(R) standard 7FP premium by the dry granulation slugging method. Drug...
To evaluate the tolerability and safety of inhaled prochlorperazine To evaluate the pharmacokinetics of inhaled prochlorperazine
The study was designed to assess the steady-state pharmacokinetic profile of paroxetine after 14 day repeated daily dosing of the controlled release tablet formulation (25 mg) in healthy C...
The objective of this open-label, randomized, two-period, crossover study was to evaluate the oral bioavailability of the Mallinckrodt controlled-release test tablet formulation of oxycodo...
To assess the safety of Staccato Prochlorperazine on cardiac repolarization (QTc interval duration) at 2 dose levels compared to placebo in healthy volunteers.
This is a randomised, controlled, open, two-armed, two-period cross-over, multi-centre phase II/III study to assess the safety, tolerability and pharmacokinetics of once-daily oral modifie...