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Formulation and evaluation of sustained releasedomperidone hydrochloride transdermal patches to treat motion sickness
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Objective: Transdermal route of drug delivery is superior than oral route because it avoids first pass effect, ensures better patient compliance, reduce dosing frequency especially in extended-release formulation and is easy to use. Domperidone HCl is DA2 receptor antagonistic and is used to prevent nausea and vomiting. The objective was to formulate a domperidone HCl extended-release transdermal drug delivery system to treat motion sickness. Methods: Five different formulations were formed using different solvents (methanol and dichloromethane) and polymers (HPMC and Eudragitl-100) by solvent evaporation method. 500mg of domperidone HCl was added in each patch and dibutyl phthalate was added as plasticizer. A 3% w/v PVA layer was used as backing. All these formulations were evaluated for their physicochemical properties (weight variation, thickness, folding endurance and tensile strength), in-vitro drug release, drug contents determination, any incompatibility between drug and excipients by FTIR and DSC and skin irritation. Results: All formulations exhibited good physicochemical properties and percentage drug release during 24 hours was 79.3%, 97.1%, 96.8%, 74.7% and 59.7% respectively. F-YM showed maximum in-vitro drug release. The optimized formulation (F-YM) followed Korsmeyer Peppas release model with n=0.383 showing that the system was following dissolution dependent drug release. No interaction between drug and excipients was detected by DSC and FTIR. No skin irritation was detected. Conclusion: The extended release transdermal patches of domperidone HCl to treat motion sickness were prepared and formulation F-YM showed optimized behavior with maximum in vitro drug release.
AMMANIF Academic Publisher
Title: Formulation and evaluation of sustained releasedomperidone hydrochloride transdermal patches to treat motion sickness
Description:
Objective: Transdermal route of drug delivery is superior than oral route because it avoids first pass effect, ensures better patient compliance, reduce dosing frequency especially in extended-release formulation and is easy to use.
Domperidone HCl is DA2 receptor antagonistic and is used to prevent nausea and vomiting.
The objective was to formulate a domperidone HCl extended-release transdermal drug delivery system to treat motion sickness.
Methods: Five different formulations were formed using different solvents (methanol and dichloromethane) and polymers (HPMC and Eudragitl-100) by solvent evaporation method.
500mg of domperidone HCl was added in each patch and dibutyl phthalate was added as plasticizer.
A 3% w/v PVA layer was used as backing.
All these formulations were evaluated for their physicochemical properties (weight variation, thickness, folding endurance and tensile strength), in-vitro drug release, drug contents determination, any incompatibility between drug and excipients by FTIR and DSC and skin irritation.
Results: All formulations exhibited good physicochemical properties and percentage drug release during 24 hours was 79.
3%, 97.
1%, 96.
8%, 74.
7% and 59.
7% respectively.
F-YM showed maximum in-vitro drug release.
The optimized formulation (F-YM) followed Korsmeyer Peppas release model with n=0.
383 showing that the system was following dissolution dependent drug release.
No interaction between drug and excipients was detected by DSC and FTIR.
No skin irritation was detected.
Conclusion: The extended release transdermal patches of domperidone HCl to treat motion sickness were prepared and formulation F-YM showed optimized behavior with maximum in vitro drug release.
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