Paliperidone Ascending Release Tablets Quiz

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Questions and Answers

What was the main aim of the work described in the text?

To investigate the release behavior of paliperidone (PAL) in different tablet formulations (correct)

To compare the release behavior of different psychiatric medications

To analyze the influence of environmental factors on tablet coatings

To study the impact of temperature on drug release from tablets

What were the core and coating layers of the PAL CC tablets comprised of?

Low viscosity hydroxypropyl cellulose (HPC-L) and high density hydroxypropyl methylcellulose (HPMC-D2000)

Microcrystalline cellulose and polyvinyl alcohol

Sodium carboxymethyl cellulose and magnesium stearate

High viscosity hydroxypropyl cellulose (HPC-H) and high viscosity hydroxypropyl methylcellulose (HPMC-K100M) (correct)

What was the fraction of HPC and HPMC used in the formulation of PAL CC tablets that achieved good ascending drug release?

20%

10%

50%

33% (correct)

What was the influence of Eudragit RL-PO on the formulation of PAL CC tablets?

It was part of the combination that contributed to achieving good ascending drug release Signup and view all the answers

What was the drug release mechanism for the PAL CC tablets as per the text?

Combination of diffusion and erosion Signup and view all the answers

What was investigated using gravi- metric analysis in relation to the PAL CC tablets?

Drug release mechanism Signup and view all the answers

What is the main manifestation of schizophrenia, as described in the text?

Decreased interpersonal ability Signup and view all the answers

What are the characteristics of paliperidone extended-release (ER) according to the text?

Smaller fluctuations in blood concentration and less adverse reactions Signup and view all the answers

What technology is utilized in the production of paliperidone extended-release (ER) tablets?

Push-pull osmotic pump (PPOP) technology Signup and view all the answers

What is the FDA approval status for paliperidone in the treatment of schizophrenia?

Approved for the treatment of central nervous system disease schizophrenia Signup and view all the answers

What do traditional antipsychotic drugs mainly suffer from, as per the text?

Frequent dosing requirement and high adverse reaction incidence Signup and view all the answers

What is the overall trend in the incidence and suicide rate related to schizophrenia?

Increasing incidence and increasing suicide rate Signup and view all the answers

What is the driving force to control drug release in the osmotic pump process?

Osmotic pressure Signup and view all the answers

What determines the rate of water absorbed in the gastrointestinal tract?

Thickness and composition of the membrane Signup and view all the answers

What causes ascending release in the osmotic pump process?

Higher drug concentration in the second layer Signup and view all the answers

What is NOT influenced by the pH according to the text?

Drug release rate of the osmotic pump Signup and view all the answers

Which factor leads to controlled and prolonged treatment window according to the text?

Ascending release Signup and view all the answers

What determines the thickness and composition of the membrane in the gastrointestinal tract?

Drug release rate Signup and view all the answers

What is discharged through the pores by the expanded bottom layer in the osmotic pump process?

Drug Signup and view all the answers

What is one of the drawbacks of the osmotic pump process mentioned in the text?

Conspicuous burst release Signup and view all the answers

What results in a complex, high cost, time-consuming process according to the text?

Dangerous conspicuous burst release Signup and view all the answers

Study Notes

Objective of the Study

The main aim was to develop controlled-release tablets of paliperidone (PAL CC) using an osmotic pump-based system.

Composition of PAL CC Tablets

Core layer comprised of paliperidone and lactose
Coating layer comprised of HPC and HPMC

Formulation of PAL CC Tablets

A fraction of 70:30 (HPC:HPMC) achieved good ascending drug release

Influence of Eudragit RL-PO

It helped to control the release of paliperidone from the PAL CC tablets

Drug Release Mechanism

Osmotic pump process, where water is absorbed into the tablet, causing the drug to be released through the pores

Gravimetric Analysis

Used to investigate the water uptake and swelling behavior of the PAL CC tablets

Schizophrenia

Main manifestation: a complex, debilitating mental disorder characterized by hallucinations, delusions, and disorganized thinking

Paliperidone Extended-Release (ER)

Characteristics: an atypical antipsychotic drug, effective in treating schizophrenia, with a prolonged treatment window
Technology utilized: osmotic pump-based system

FDA Approval

Paliperidone is approved for the treatment of schizophrenia

Limitations of Traditional Antipsychotic Drugs

Mainly suffer from limited efficacy, poor tolerability, and a high risk of side effects

Incidence and Suicide Rate of Schizophrenia

The incidence and suicide rate are increasing, making it a significant public health concern

Osmotic Pump Process

Driving force: osmotic pressure
Rate of water absorption: determined by the gastrointestinal tract
Ascending release: caused by the increasing pressure in the tablet
pH-independent: the drug release is not influenced by the pH

Controlled and Prolonged Treatment Window

Determined by the thickness and composition of the membrane, which is influenced by the HPC and HPMC fractions

Osmotic Pump Process Mechanism

The expanded bottom layer discharges the drug through the pores
One drawback: the process can result in a complex, high-cost, time-consuming process

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Description

Test your knowledge on the preparation, release behavior, and mechanisms of ascending release compression-coated (CC) tablets with paliperidone (PAL) and the materials involved in the manufacturing process.