Evaluation of Meclizine Orodispersible Tablet Pharmacokinetic in Human Volunteers

Phase

1/2

Condition

Vomiting

Treatment

N/A

Clinical Study ID

NCT04564144

meclizine pharmacokinetic

Ages 30-40
Male
Accepts Healthy Volunteers

Study 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.

Eligibility Criteria

Inclusion

Inclusion Criteria:

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 examinationand 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 thestudy and is available to complete all study measurements.

Exclusion

Exclusion Criteria:

As a result of the medical interview, physical examination or screeninginvestigations, the Investigator or appropriately qualified designee considers thesubject unfit for the study.
The subject has a history of drug or any other allergy, which, in the opinion of theInvestigator or appropriately qualified designee, contraindicates their participation,including known or suspected personal history or family history of adverse reactionsor hypersensitivity to anti histamines.
The subject has participated in a study with a new molecular entity during theprevious 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 medicationor herbal remedies such as St Johns Wort). Paracetamol is an exception and will bepermitted 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 surfaceantigen.
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 dayperiod
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.

Study Design

June 01, 2020

December 01, 2020

Study Description

The oral route is the most advantageous one for delivering drugs due to patient compliance and its convenient administration. Fast disintegrating drug delivery systems are those that disintegrate immediately in the buccal cavity liberating the drug which dissolves or disperses in the saliva without need of water. The European Pharmacopeia adopted oro-dispersible tablets (ODT) for a tablet that disintegrate or disperse in less than 60 sec in the buccal cavity before swallowing. So, the drug dissolution and absorption in addition to onset of clinical influence and drug bioavailability may be considerably better than those detected from conventional tablets and capsules. ODTs were initially industrialized to increase the patient compliance (children, geriatric and bedridden patients).

Nanoparticulate delivery systems have been investigated widely in the pharmaceutical industry owing to protection from degradation in GIT, the ability to control release of drugs and improvement of bioavailability.

Meclizine HCL, an antihistamine, has been widely used for prophylactic treatment of nausea, vomiting and management of dizziness accompanying motion sickness. MCZ is commonly used due to fewer adverse effects than other antihistaminic drugs but its onset of action is about 1 h and possesses short half-life. MCZ is a poor water soluble drug and associated with slow rate of absorption from oral route, therefore, there is a need to improve its dissolution and so ensure the maximum therapeutic utility. However, many different formulations of MCZ have been investigated to improve its overall solubility in order to enhance its bioavailability, such as; complexation with cyclodextrin, preparation of solid dispersions as oro- dispersible tablets and fast dissolving tablet by sublimation method. Moreover, authors will investigate the ability of floating microspheres to increase the half-life of MCZ

Connect with a study center

Mansoura University
Mansoura, Dakhalia 35688
Egypt
Active - Recruiting

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