Evaluation of Meclizine Orodispersible Tablet Pharmacokinetic in Human Volunteers

NCT04564144 | Unknown Phase 1

• 1 other identifier: meclizine pharmacokinetic
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The main goal of this study is to develop a new oro-dissolvable/dispersible tablet that will augment the dual rapid absorption of MCZ from the buccal cavity as well as prolonging that from the GIT. A dual function tablet is expected to encompass an outer coat of the drug with special excipients that will rapidly disperse and the drug get dissolve and absorb in the buccal cavity and an inner core that will similarly, disperse to release MCZ coated nanoparticles in the saliva. The latter will be subsequently swallowed without water to be absorbed in a prolonged manner from the GIT. This will be advantageous for geriatric as well as pediatric patients, besides, those suffering from dysphagia. The pharmacokinetics profile of the prepared dual function tablet will be assessed in human volunteers through noncompartmental analysis.

Conditions

Emesis

Outcome Measures

Primary Outcomes (5)

• measuring the Meclizine HCl plasma concentration

  Using high performance liquid chromatography to measure the change in plasma drug concentrationز

  over 24 hours after dosing

• measuring the Meclizine HCl Area under the curve

  measuring the Meclizine HCl Area under the curve using high performance liquid chromatography

  over 24 hours after dosing

• measuring the Meclizine HCl apparent clearance (CL/F)

  measuring the Meclizine HCl apparent clearance (CL/F) using high performance liquid chromatography

  over 24 hours after dosing

• measuring the maximum blood concentration of Meclizine HCl

  measuring the maximum blood concentration of Meclizine HCl using high performance liquid chromatography

  over 24 hours after dosing

• measuring the maximum blood concentration time of Meclizine HCl

  measuring the maximum blood concentration time of Meclizine HCl using high performance liquid chromatography

  over 24 hours after dosing

Study Arms (1)

Volunteers receiving the prepared orodispersible tablets

EXPERIMENTAL

6 human volunteers will receive the prepared orodispersible tablets plus a commercial one all containing Meclizine HCl in a parallel manner.

Drug: Meclizine Hydrochloride

Interventions

Meclizine Hydrochloride DRUG

A study will be conducted on the three tested orodispersible tablets and the commercial one (control). 6 volunteers are asked to cease any medication 7 days prior to blood sampling at least. Each volunteer will undergo 4 study sessions with one week of washout period in between (cross-overed to receive the other formulation). All volunteers are asked to fast overnight before taking the tablet. The tablet should be kept for 10 min in the mouth before swallowing without water. Just before taking the tablet, three milliliters of venous blood samples will be drown (predose, 0 h) and at 30, 60, 90, 120, 240, 360, 480, 720 min and 24 h postdose and stored in tubes coated with sodium heparin. Separation of plasma from Blood samples will be carried out by centrifuging at 5000 rpm for 10 min, then, it will be frozen at -20°C until analysis. By employing high-performance liquid chromatography (HPLC), the plasma concentration of MCZ will be assayed

Volunteers receiving the prepared orodispersible tablets

Eligibility Criteria

• Age: 30 Years - 40 Years
• Gender Eligibility Details: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male aged between 30 and 40 years.
• Body weight range of 75kg-95kg.
• Healthy (defined as individuals who are free from significant nasal, cardiac, pulmonary, gastrointestinal, hepatic, renal, haematological, malignancy, endocrine, neurological and psychiatric disease as determined by history, physical examination and screening investigations).
• Non-smoking status. This can include ex-smokers who have given up smoking for \>1 year.
• The subject is able and willing to give written informed consent to take part in the study and is available to complete all study measurements.

You may not qualify if:

• As a result of the medical interview, physical examination or screening investigations, the Investigator or appropriately qualified designee considers the subject unfit for the study.
• The subject has a history of drug or any other allergy, which, in the opinion of the Investigator or appropriately qualified designee, contraindicates their participation, including known or suspected personal history or family history of adverse reactions or hypersensitivity to anti histamines.
• The subject has participated in a study with a new molecular entity during the previous 3 months or any other study during the previous 2 months.
• The subject drinks alcohol.
• The subject is currently taking regular (or a course of) medication, prescribed (including all anti-allergy medication) or not (including over the counter medication or herbal remedies such as St Johns Wort). Paracetamol is an exception and will be permitted at daily doses of up to 4g following all doses of investigational product.
• The subject has tested positive for hepatitis C antibody or hepatitis B surface antigen.
• The subject has tested positive for HIV.
• The subject has a positive drugs of abuse and alcohol test.
• Donation of blood (450 mL or more) within 2 months of screening.
• Donation during the study would result in \>500mL of blood being donated over a 56 day period
• Significant cardiac conduction abnormalities.
• Subjects with Perennial Allergic Rhinitis (PAR) and Seasonal Allergic Rhinitis (SAR), unless subjects with SAR are asymptomatic and it is outside of the pollen season
• Subjects who are unable to comply with study procedures.

Sponsors & Collaborators

• Mansoura University: lead

Study Sites (1)

Mansoura University

Al Mansurah, Dakhalia, 35688, Egypt

RECRUITING

Related Publications (3)

• Wang K, Li L, Song Y, Ye X, Fu S, Jiang J, Li S. Improvement of pharmacokinetics behavior of apocynin by nitrone derivatization: comparative pharmacokinetics of nitrone-apocynin and its parent apocynin in rats. PLoS One. 2013 Jul 30;8(7):e70189. doi: 10.1371/journal.pone.0070189. Print 2013.

  PMID: 23936162 RESULT

• Leach WT, Simpson DT, Val TN, Yu Z, Lim KT, Park EJ, Williams RO 3rd, Johnston KP. Encapsulation of protein nanoparticles into uniform-sized microspheres formed in a spinning oil film. AAPS PharmSciTech. 2005 Dec 6;6(4):E605-17. doi: 10.1208/pt060475.

  PMID: 16408862 RESULT

• Aljimaee YH, El-Helw AR, Ahmed OA, El-Say KM. Development and optimization of carvedilol orodispersible tablets: enhancement of pharmacokinetic parameters in rabbits. Drug Des Devel Ther. 2015 Mar 5;9:1379-92. doi: 10.2147/DDDT.S80294. eCollection 2015.

  PMID: 25834396 RESULT

MeSH Terms

Conditions

Vomiting

Interventions

Meclizine

Condition Hierarchy (Ancestors)

Signs and Symptoms, Digestive; Signs and Symptoms; Pathological Conditions, Signs and Symptoms

Intervention Hierarchy (Ancestors)

Benzhydryl Compounds; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; Hydrocarbons; Organic Chemicals; Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Alaa Y. Darwesh, Dr

  Mansoura University

  PRINCIPAL INVESTIGATOR

Central Study Contacts

Alaa Y. Darwesh, Dr

CONTACT

+201063450461; alyaser_2011@mans.edu.eg

Marwa S. El-Dahhan, Drs

CONTACT

+201001969482; marwaeldahan_1975@yahoo.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: PREVENTION
• Intervention Model: SEQUENTIAL
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 17, 2020
• First Posted: September 25, 2020
• Study Start: June 1, 2020
• Primary Completion: November 1, 2020
• Study Completion: December 1, 2020
• Last Updated: September 25, 2020

Record last verified: 2020-09

Data Sharing

• IPD Sharing: Will not share

Locations

EG (1)