Anti-Emetic Effectiveness of Cyclizine Films

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Questions and Answers

What is the primary function of the action that lowers vestibular stimulation?

Suppresses nausea and vomiting caused by motion sickness and vestibular disorders.

What is the chemical formula of HPMC?

C56H108O30

What is the primary characteristic of a hydrophilic polymer used in drug delivery films?

It dissolves quickly in the mouth.

Name three medications that have been developed using thin film drug delivery technology.

<p>Rizatriptan, Monosol Rx (testosterone), and Montelukast.</p> Signup and view all the answers

What advantage do Oral Dispersible Films (ODFs) offer compared to traditional dosage forms like tablets and capsules?

<p>They simplify medication administration, especially for individuals with swallowing difficulties.</p> Signup and view all the answers

Explain how intra-oral absorption of medications through ODFs contributes to their effectiveness.

<p>It allows for rapid action and prevents the first-pass effect in the liver, often requiring a lower dosage for therapeutic effect.</p> Signup and view all the answers

What is the key difference between dispersible films and ODTs in terms of disintegration?

<p>Dispersible films disintegrate with very little saliva moisture in less than a minute, while ODTs require more moisture.</p> Signup and view all the answers

What are the primary causes of nausea and vomiting mentioned in the text?

<p>The text highlights chemotherapy, surgery, and medical disorders as primary causes of nausea and vomiting.</p> Signup and view all the answers

Why can dispersible films be used safely in the absence of water?

<p>They dissolve and disintegrate with minimal moisture, making them suitable for consumption even when water is unavailable.</p> Signup and view all the answers

Describe the prevalence of Chemotherapy-Induced Nausea and Vomiting (CINV) according to the text.

<p>CINV affects a significant portion of individuals undergoing chemotherapy, ranging from 70-80% generally, with higher rates reaching 90% for highly emetogenic chemotherapy.</p> Signup and view all the answers

What are the distinct advantages of oral drug administration mentioned in the excerpt?

<p>The text highlights the convenience and ease of oral administration compared to other routes, making it the most commonly used method.</p> Signup and view all the answers

What are the key challenges associated with liquid oral dosage forms as described in the passage?

<p>The excerpt mentions lower bioavailability, slower action time, and difficulties in precise dosing as challenges with liquid oral dosage forms.</p> Signup and view all the answers

List the specific patient groups for whom liquid oral dosages offer a more effective approach compared to traditional oral forms.

<p>The passage highlights newborns, children, elderly patients, bedridden patients, and cancer patients as groups that benefit from liquid oral dosage forms due to difficulties with conventional tablets or capsules.</p> Signup and view all the answers

Explain the difficulties individuals with dysphagia face when taking traditional oral medications.

<p>Patients with dysphagia struggle with swallowing due to conditions like Parkinson's disease or mucositis, which can make traditional pills or capsules challenging to ingest.</p> Signup and view all the answers

What are the key drawbacks associated with traditional oral dosage forms, particularly in scenarios with water scarcity?

<p>The text mentions challenges like difficulties swallowing, water requirements for ingestion, and self-administration complexity in specific patient groups as drawbacks of traditional oral dosage forms.</p> Signup and view all the answers

What is the primary reason for developing cyclizine-loaded polymer films?

<p>The primary reason is to address the issue of nausea and vomiting, offering a potentially more effective and patient-friendly treatment option.</p> Signup and view all the answers

What are the specific patient groups for whom self-administration of traditional oral forms poses difficulties, as mentioned in the excerpt?

<p>The passage mentions children, the elderly, and individuals with water scarcity as groups facing challenges with self-administration of traditional oral medications.</p> Signup and view all the answers

What specific medical condition is mentioned as being particularly susceptible to motion sickness?

<p>Northeast and Northwest Indians are particularly susceptible to motion sickness.</p> Signup and view all the answers

What is one of the key mechanisms by which cyclizine Hcl exerts its anti-emetic effect?

<p>Cyclizine Hcl demonstrates anticholinergic effects by inhibiting acetylcholine receptors.</p> Signup and view all the answers

List two common prescription medications used to treat nausea and vomiting.

<p>Ondansetron and promethazine are two common prescription medications for nausea and vomiting.</p> Signup and view all the answers

What is the primary reason behind making a film formulation for cyclizine Hcl?

<p>The film formulation aims to address the unavailability of the drug's film format, which will likely improve patient compliance and efficacy.</p> Signup and view all the answers

What is the research objective related to evaluating the physical and chemical characteristics of the developed cyclizine-loaded films?

<p>The objective is to evaluate the physical and chemical properties of the developed films, which are crucial for understanding their stability and potential efficacy.</p> Signup and view all the answers

Describe one of the techniques mentioned for characterizing the cyclizine-loaded films.

<p>Scanning Electron Microscopy (SEM) is one of the techniques mentioned for characterizing the films.</p> Signup and view all the answers

What specific aspect of the cyclizine-loaded films is assessed to determine their overall effectiveness in managing nausea and vomiting?

<p>The research assesses the anti-emetic efficacy of the cyclizine-loaded films to determine their overall effectiveness in managing nausea and vomiting.</p> Signup and view all the answers

What is the main benefit of using Orodiapersible Thin Film (OTF) in drug delivery?

<p>OTF avoids the fast pass effect and enhances drug bioavailability.</p> Signup and view all the answers

What are the typical dimensions of Orodiapersible Thin Films?

<p>They are typically 50-150 μm in size.</p> Signup and view all the answers

List two ideal features of an oral thin film.

<p>The film should taste good and be moisture resistant.</p> Signup and view all the answers

Why is Cyclizine HCL described as a histamine H1 receptor antagonist?

<p>It blocks H1 receptors in the vomiting center and vestibular nuclei in the brain.</p> Signup and view all the answers

How does the Orodiapersible Thin Film improve drug absorption rates?

<p>It provides a large surface area for rapid dissolution.</p> Signup and view all the answers

What makes Orodiapersible Thin Films convenient for users?

<p>They can be used without water and are portable.</p> Signup and view all the answers

What is the half-life of Cyclizine, and why is it significant?

<p>The half-life of Cyclizine is 20 hours.</p> Signup and view all the answers

Explain the role of pH in the effectiveness of oral thin films.

<p>The films should be ionized in the oral cavity pH to enhance drug penetration.</p> Signup and view all the answers

What is the significance of conducting compatibility studies in the formulation of oral films?

<p>Compatibility studies ensure that all components of the oral film formulation can coexist without adverse interactions that may affect drug stability or efficacy.</p> Signup and view all the answers

Explain the role of U.V spectroscopy in evaluating oral films.

<p>U.V spectroscopy is used to assess the drug content and purity in oral films by measuring absorbance at specific wavelengths, which indicates the concentration of the drug.</p> Signup and view all the answers

Why is it important to determine the pH of the solution in drug formulation processes?

<p>Determining the pH is crucial as it can influence the solubility, stability, and absorption of the drug, thereby affecting its bioavailability.</p> Signup and view all the answers

What is the function of a calibration curve in the context of drug content analysis?

<p>A calibration curve enables the quantification of the drug concentration in a sample by comparing its absorbance to a standard curve created from known concentrations.</p> Signup and view all the answers

Describe how the partition coefficient can impact the formulation of oral films.

<p>The partition coefficient indicates the distribution of the drug between two phases, which affects its permeability and absorption after administration.</p> Signup and view all the answers

What does the term 'swelling behavior studies' refer to in the context of oral film formulations?

<p>Swelling behavior studies assess how the film interacts with solvents, indicating how much it will expand or dissolve, which influences drug release rates.</p> Signup and view all the answers

What role does differential scanning calorimetry (DSC) play in the evaluation of oral films?

<p>DSC is used to analyze thermal properties of the materials involved, which can indicate physical and chemical stability of the film formulation.</p> Signup and view all the answers

Why are bioequivalence studies important for marketed oral film products?

<p>Bioequivalence studies are crucial to ensure that the marketed product delivers the same therapeutic effect as the reference product, establishing its efficacy and safety.</p> Signup and view all the answers

Flashcards

Nausea and Vomiting

Nausea and vomiting, particularly during chemotherapy, surgery, and other medical disorders.

CINV

Chemotherapy-Induced Nausea and Vomiting.

Postoperative Nausea and Vomiting

High-risk individuals experience 80% of this.

Oral Route

Most common drug administration route, easy and requires less assistance.

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Oral Dosage Forms

Lower bioavailability presents a challenge for this dosage form.

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Challenges of Traditional Oral Dose Forms

Oral route is challenging for children, elderly, and people with dysphagia.

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Dysphagia

A condition where people have difficulty swallowing.

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Mucositis

Inflammation and sores in the mouth, common in cancer patients, making traditional oral dose forms a challenge.

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What is NVP?

Nausea and vomiting in pregnancy (NVP), affecting 70-80% of expectant mothers.

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What is motion sickness?

A condition that affects 30-70% of the population, causing discomfort and nausea due to motion.

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How does cancer treatment affect nausea?

Chemotherapy and radiation therapy often lead to nausea and vomiting in patients.

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What is cyclizine HCL?

A drug with sedative properties that blocks H1 receptors in the brain, suppressing nausea and vomiting.

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What is a cyclizine HCL film?

Film formulation of cyclizine HCL is a promising alternative for treating nausea and vomiting, potentially improving patient compliance.

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What is film formulation?

The process of creating and optimizing cyclizine-loaded polymer films to improve drug delivery and effectiveness.

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What is film characterization?

Analyzing the physical and chemical properties of cyclizine-loaded films to ensure quality and performance.

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What is drug release kinetics and anti-emetic efficacy?

Evaluating the rate at which the drug is released from the film and its effectiveness in reducing nausea and vomiting.

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Orodiapersible Thin Film (OTF)

A revolutionary drug delivery system that dissolves quickly in the mouth, bypassing the first-pass metabolism in the stomach and liver, allowing for faster and more efficient drug absorption.

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Drug content uniformity test

A test to determine if different batches of the same drug have the same chemical composition and dosage.

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First-pass metabolism

The process where drugs pass through the liver before entering the bloodstream. This can significantly reduce the drug's effectiveness.

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FTIR Spectral analysis

A technique used to analyze the structure and composition of molecules by measuring their absorption of infrared light.

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In-vitro drug release study

A test to evaluate the rate and extent of drug release from a dosage form under simulated conditions.

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Fast-dissolving film

A thin, postage stamp-sized film containing medications that dissolves quickly in the mouth. It offers convenience, portability, and is suitable for various age groups.

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Bioequivalence study

A study to assess the safety and effectiveness of a drug formulation by comparing it to a reference product.

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Bypasses the gastrointestinal tract

A key advantage of OTF, enabling drug absorption directly into the bloodstream, avoiding first-pass metabolism.

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Weight Uniformity

Determines if different batches of a drug have consistent weight.

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Bioavailability

The ability of a drug to reach its target site and exert its therapeutic effect.

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Histamine H1 receptor antagonist

A drug that blocks the action of histamine, specifically, the H1 receptor, which is responsible for allergic reactions and motion sickness.

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pH determination

A test to determine the pH of a substance, which indicates its acidity or alkalinity.

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Compatibility studies

Evaluates how well different components of a drug formulation interact.

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Metabolism

The process of breaking down drugs in the body, usually by enzymes, into smaller molecules.

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Solubility

Determines the extent to which a drug dissolves in a solvent, such as water.

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Half-life

The time it takes for the concentration of a drug in the body to reduce by half.

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Hydroxypropyl methylcellulose (HPMC)

A type of polymer used to create thin films for drug delivery, which dissolves quickly in the mouth.

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Oral Dispersible Films (ODFs)

A drug delivery method using thin films that dissolve quickly in the mouth. Useful for patients who have difficulty swallowing.

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Intra-oral Absorption

Drugs absorbed in the mouth bypass the digestive system, leading to faster action and reduced side effects.

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First-Pass Effect

The process where some drugs are destroyed by the liver before reaching the bloodstream.

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Drug Absorption

The process where drugs are absorbed into the bloodstream.

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Buccal/Sublingual Drug Delivery

A method of drug delivery where thin films are placed on the tongue or inside the cheeks, allowing for faster absorption.

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Study Notes

Cyclizine-Loaded Polymer Films

  • Project Title: Cyclizine-Loaded Polymer Films: Evaluation, Characterization, and Anti-Emetic Effectiveness
  • Submitted to: Institute of Pharmacy, Bundelkhand University, Jhansi
  • For: Master of Pharmacy in Pharmaceutics
  • Supervisor: Dr. Sunil Kumar Prajapati, Professor & Head
  • Presented by: Sandeep Kumar, M. Pharm. (2nd Year/3rd Semester), Roll No: 231255155011
  • University: Bundelkhand University, Jhansi, U.P-2024

Introduction

  • Nausea and vomiting (CINV) is a common problem, particularly during chemotherapy and surgery, affecting 70-80% of individuals.
  • Chemotherapy-induced nausea and vomiting (CINV) affects 90% in highly emetogenic cases.
  • Postoperative nausea and vomiting occurs in 20-30% of patients, with high-risk individuals experiencing 80%.
  • Oral routes are the most common drug administration route due to ease of use and less assistance required.
  • Parenteral and liquid oral dosage forms are considered for improved bioavailability and faster action time, but challenges exist in precise dosing, particularly in children and elderly patients.
  • Traditional oral dose forms are often challenging for patient self-administration due to problems like swallowing difficulties, water scarcity, and certain medical conditions.

Delivery System

  • Orodispersible Thin Film (OTF): A novel drug delivery system that dissolves in the oral cavity, avoiding the "fast pass effect" and dissolving within seconds.
  • Ultra-thin films (typically 50-150µm) are gaining popularity.
  • Fast-dissolving films offer enhanced safety, efficacy, and patient adherence, converting drug molecules into oral dosages.
  • Characteristics: Ultra-thin, postage stamp-sized, containing active agents and excipients, offering convenience, portability, and wider acceptability for pediatric and geriatric populations.

Ideal Features of Oral Thin Films

  • Pleasant taste.
  • Moisture resistance.
  • Solubility in saliva.
  • Appropriate tension resistance.
  • Ionization in the oral cavity pH.
  • Ability to penetrate the oral mucosa.
  • Rapid effect.

Advantages of Oral Thin Films

  • No need for water.
  • Safe for use without a water source.
  • Improved stability (no suffocation risk).
  • Ease of application.
  • Bypasses the gastrointestinal tract, increasing bioavailability
  • Lower dosage and side effects.
  • Rapid onset of effects in urgent conditions.
  • Improved drug absorption and bioavailability.
  • Enhanced bioavailability for poorly water-soluble drugs.

Drug Profile: Cyclizine HCL

  • Chemical name: Cyclizine Hydrochloride
  • Formula: C18H22CIN2
  • Molecular weight: 302.8 g/mol
  • Color form: Crystals from petroleum ether, odorless or nearly odorless
  • Melting point: 291-293°C
  • Half-life: ~20 hours
  • Absorption: Within 30 minutes
  • Metabolism: Metabolized to N-demethylated derivative (norcyclizine) with reduced antihistaminic activity.
  • Mechanism of Action: Histamine H1 receptor antagonist, blocks H1 receptors in the vomiting center and vestibular nuclei, suppressing nausea and vomiting caused by motion sickness and other vestibular disorders.

Polymer Profile: HPMC

  • Chemical formula: C56H108O30
  • Molecular weight: 1261.4 g/mol
  • Synonyms: Hydroxypropyl methylcellulose
  • Physical Description: White to off-white powder
  • Melting point: 225-230 °C
  • Boiling point: 1101.5°C
  • Storage temperature: Room temperature (typically 20-25°C)
  • Solubility: Soluble in water
  • Refractive index: 1.52

Literature Review

  • Iqbal et al. (2023) reviewed oral drug strips or dissolving films.
  • Sharma et al. (2022) reviewed delivery technologies that dissolve in the stomach, such as oral dispersible films (ODFs).
  • ODFs simplify drug administration for specific groups like children and elderly.

Research Envisaged

  • Global incidence of nausea and vomiting, prevalence in oncological patients undergoing chemotherapy, and susceptibility to motion sickness.
  • Cyclizine HCL's sedative properties, anticholinergic effects (inhibiting acetylcholine receptors).
  • The development of an oral thin film for treatment of nausea and vomiting.
  • Importance of providing an alternative treatment that enhances patient quality of life.

Objectives

  • Formulate and optimize cyclizine-loaded polymer films using suitable film-forming polymers.
  • Evaluate physical and chemical properties of the developed films.
  • Characterize films in terms of drug release kinetics and anti-emetic efficacy.
  • Assess the overall effectiveness in managing nausea and vomiting.

Plan of Work

  • Literature survey (selection of drug and polymers)
  • Procurement of drug, polymer, and excipients
  • Pre-formulation studies (solubility, pH, compatibility, UV spectroscopy, calibration curve, partition coefficient, FTIR spectral analysis)
  • Differential Scanning Calorimetry (DSC)
  • Scanning Electron Microscopy (SEM)
  • Preparation of oral films using solvent casting technique
  • Evaluation of oral films (weight uniformity, thickness, folding endurance, drug content uniformity, swelling behavior)
  • In-vitro drug release study
  • Bioequivalence of marketed product

Experimental Work

  • Shows placebo oral films in distilled water and ethanol.

References

  • Includes numerous cited research papers (authors and publication years).

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