EmesisPhase 1/2NCT04564144
Evaluation of Meclizine Orodispersible Tablet Pharmacokinetic in Human Volunteers
A Phase 1/2 study testing Meclizine Hydrochloride in people with Emesis, run by Mansoura University at 1 site in Egypt.
Trial 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. Read more about this study
- Who is it for?
- Ages 30 to 40 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Emesis
- What is being tested?
- Meclizine Hydrochloride
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 6 participants
- Where
- 1 siteEgypt
- Study dates
- 1 Jun 2020to 1 Dec 2020
- Phase
- Phase 1/2
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 30 to 40 years
- Men only
- Healthy volunteers accepted
- Adult
Who may be able to join
- 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.
Who cannot join
- 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.
Show all 13Show fewer
- 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.
Trial locations and contacts
1 site in 1 country.
Egypt1 site, 1 recruiting
- Recruiting
Mansoura University
Al Mansurah, Dakhalia, 35688
Alaa Y. Darwesh, Dr, +201063450461, alyaser_2011@mans.edu.eg
Marwa S. El-Dahhan, Drs, +201001969482, marwaeldahan_1975@yahoo.com
About this study
Official title: A New Dual Function Oro-Dissolvable/Dispersible Meclizine HCL Tablet to Challenge Patient Inconvenience: In-Vitro Evaluation and In-Vivo Assessment in Human Volunteers
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.
Read the detailed 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
- Conditions
- Emesis
- Being tested
- Meclizine Hydrochloride
- Medical subject headings
- Vomiting
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Meclizine HydrochlorideDrug
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
| Study group | Role | What they receive |
|---|---|---|
| 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. Receives: Drug: Meclizine Hydrochloride |
What is being measured
The primary outcome is the main question the study is designed to answer.
measuring the Meclizine HCl plasma concentration
Using high performance liquid chromatography to measure the change in plasma drug concentrationز
Measured: 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
Measured: 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
Measured: 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
Measured: 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
Measured: over 24 hours after dosing
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted25 Sep 2020
- Study start1 Jun 2020
- Primary completion1 Nov 2020 (estimated)
- Study completion1 Dec 2020 (estimated)
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (3)Papers the sponsor has linked to this study.
- Other trials for EmesisStudies of the same condition, open and under way.
- More trials run by Mansoura UniversityThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1/2
- Primary purpose
- Prevention
- Allocation
- Not applicable
- Intervention model
- Sequential
- Masking
- None (open label)
- Enrolment
- 6 participants (estimated)
Sponsor and investigators
- Lead sponsor
- Mansoura University
- Sponsor type
- University, hospital or other
- Responsible party
- Sponsor
- Investigators
- Alaa Y. Darwesh, Dr, Principal investigator, Mansoura University
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT04564144
- Sponsor's protocol ID
- meclizine pharmacokinetic
- Status last verified
- Sep 2020
- First submitted
- 17 Sep 2020
- Last updated
- 25 Sep 2020
- Results posted
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- No
Publications
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.
PubMed 23936162Leach 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.
PubMed 16408862Aljimaee 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.
PubMed 25834396
Study at a glance
From the registry record, last updated by the sponsor on 25 Sep 2020. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A New Dual Function Oro-Dissolvable/Dispersible Meclizine HCL Tablet to Challenge Patient Inconvenience: In-Vitro Evaluation and In-Vivo Assessment in Human Volunteers
- ClinicalTrials.gov ID
- NCT04564144
- Acronym / sponsor ID
- meclizine pharmacokinetic
- Conditions
- Emesis
- Phase
- Phase 1/2
- Study type
- Interventional
- Recruitment status
- Unknown status
- Enrolment
- 6 participants (estimated)
- Lead sponsor
- Mansoura UniversityUniversity, hospital or other
- Study start
- 1 Jun 2020 (actual)
- Primary completion
- 1 Nov 2020 (estimated)
- Study completion
- 1 Dec 2020 (estimated)
- First posted
- 25 Sep 2020 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
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.
Detailed 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
Study design
- Primary purpose
- Prevention
- Allocation
- Not applicable
- Intervention model
- Sequential
- Masking
- None (open label)
- Number of arms
- 1
| Arm | Type | Receives |
|---|---|---|
| Volunteers receiving the prepared orodispersible tablets | Experimental | Drug: Meclizine Hydrochloride6 human volunteers will receive the prepared orodispersible tablets plus a commercial one all containing Meclizine HCl in a parallel manner. |
Who may qualify
- Ages
- 30 to 40 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (5 listed)
- 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.
Key exclusion criteria (13 listed)
- 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.
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| Meclizine HydrochlorideA 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 | Drug | Volunteers receiving the prepared orodispersible tablets |
Primary outcome
measuring the Meclizine HCl plasma concentration
Time frame: over 24 hours after dosing
Using high performance liquid chromatography to measure the change in plasma drug concentrationز
measuring the Meclizine HCl Area under the curve
Time frame: over 24 hours after dosing
measuring the Meclizine HCl Area under the curve using high performance liquid chromatography
measuring the Meclizine HCl apparent clearance (CL/F)
Time frame: over 24 hours after dosing
measuring the Meclizine HCl apparent clearance (CL/F) using high performance liquid chromatography
measuring the maximum blood concentration of Meclizine HCl
Time frame: over 24 hours after dosing
measuring the maximum blood concentration of Meclizine HCl using high performance liquid chromatography
measuring the maximum blood concentration time of Meclizine HCl
Time frame: over 24 hours after dosing
measuring the maximum blood concentration time of Meclizine HCl using high performance liquid chromatography
Results and safety
Results are not available in the source record.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 25 Sep 2020.
- Results publication: PubMed 23936162Wang 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.
- Results publication: PubMed 16408862Leach 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.
- Results publication: PubMed 25834396Aljimaee 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.
- Individual participant dataSharing planned: No
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Alternate Nostril Breathing (ANB) for 1st Trimester Nausea and Vomiting
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Emesis Pregnancy
Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Alaa Y. Darwesh, Dr principal investigator
Mansoura University
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1/2 study testing Meclizine Hydrochloride in people with Emesis, run by Mansoura University at 1 site in Egypt.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 5 inclusion and 13 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: status not confirmed, as of the sponsor's last update on 25 Sep 2020. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in Egypt. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this combined phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Phase 2 studies give the treatment to a larger group to see whether it has the intended effect and to keep checking safety.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
Results are not available in the source record.
How can a doctor refer a patient or contact the research team?
Contact Alaa Y. Darwesh, Dr (+201063450461, alyaser_2011@mans.edu.eg), or a site near the patient. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
measuring the Meclizine HCl plasma concentration (time frame: over 24 hours after dosing). The study lists 5 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT04564144, which also lists 3 linked publications.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 25 Sep 2020; AzTrials last refreshed its copy on 8 Nov 2026.