Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment
Oral administration of dipyridamole (DIP) with acetylsalicylic acid (ACA) is recommended in thromboembolic conditions or for the treatment of myocardial infarction and stroke. The present study presents an alternative dosage form of these two active ingredients, consisting of a honey core and a dark...
Saved in:
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-05-01
|
| Series: | Applied Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2076-3417/15/11/6048 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1850129349970231296 |
|---|---|
| author | Georgios Kamaris Nikoletta Pantoudi Konstantina Chachlioutaki Catherine K. Markopoulou |
| author_facet | Georgios Kamaris Nikoletta Pantoudi Konstantina Chachlioutaki Catherine K. Markopoulou |
| author_sort | Georgios Kamaris |
| collection | DOAJ |
| description | Oral administration of dipyridamole (DIP) with acetylsalicylic acid (ACA) is recommended in thromboembolic conditions or for the treatment of myocardial infarction and stroke. The present study presents an alternative dosage form of these two active ingredients, consisting of a honey core and a dark chocolate coating. The composition masks the bitter taste, is palatable and ensures compliance of a wide range of patients, mainly pediatric. For the simultaneous quantitative determination of the analytes, a Diode Array Detector/Fluorescence Detector (HPLC-DAD/FLD) method was used with a C18 column (250 mm × 4.6 mm, 5 μm) and an isocratic two-phase system (A: H<sub>2</sub>O 0.2% formic acid—B: Acetonitrile-H<sub>2</sub>O 90:10 <i>v</i>/<i>v</i>) 65:35 <i>v</i>/<i>v</i>. The method was validated according to ICH guidelines (r<sup>2</sup> > 0.999, RSD < 2.3%, % Recovery > 95.4%), and a stability study of the two active ingredients as well as salicylic acid (SAL), which is a hydrolysis product of ACA, was followed. Finally, a digestion protocol (oral cavity–stomach–intestine) for edible materials was applied to determine the release rate of ACA, DIP and SAL in the gastrointestinal tract, while an in vitro permeability study (P<sub>app</sub>) was subsequently performed in Franz cells. The results show satisfactory behavior of ACA and DIP and provide a trigger for further studies of the formulation. |
| format | Article |
| id | doaj-art-befeb649db074e13b60df189fca92294 |
| institution | OA Journals |
| issn | 2076-3417 |
| language | English |
| publishDate | 2025-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Applied Sciences |
| spelling | doaj-art-befeb649db074e13b60df189fca922942025-08-20T02:33:01ZengMDPI AGApplied Sciences2076-34172025-05-011511604810.3390/app15116048Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability AssessmentGeorgios Kamaris0Nikoletta Pantoudi1Konstantina Chachlioutaki2Catherine K. Markopoulou3Laboratory of Pharmaceutical Analysis, Department of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of Pharmaceutical Analysis, Department of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of Pharmaceutical Technology, Department of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceLaboratory of Pharmaceutical Analysis, Department of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, GreeceOral administration of dipyridamole (DIP) with acetylsalicylic acid (ACA) is recommended in thromboembolic conditions or for the treatment of myocardial infarction and stroke. The present study presents an alternative dosage form of these two active ingredients, consisting of a honey core and a dark chocolate coating. The composition masks the bitter taste, is palatable and ensures compliance of a wide range of patients, mainly pediatric. For the simultaneous quantitative determination of the analytes, a Diode Array Detector/Fluorescence Detector (HPLC-DAD/FLD) method was used with a C18 column (250 mm × 4.6 mm, 5 μm) and an isocratic two-phase system (A: H<sub>2</sub>O 0.2% formic acid—B: Acetonitrile-H<sub>2</sub>O 90:10 <i>v</i>/<i>v</i>) 65:35 <i>v</i>/<i>v</i>. The method was validated according to ICH guidelines (r<sup>2</sup> > 0.999, RSD < 2.3%, % Recovery > 95.4%), and a stability study of the two active ingredients as well as salicylic acid (SAL), which is a hydrolysis product of ACA, was followed. Finally, a digestion protocol (oral cavity–stomach–intestine) for edible materials was applied to determine the release rate of ACA, DIP and SAL in the gastrointestinal tract, while an in vitro permeability study (P<sub>app</sub>) was subsequently performed in Franz cells. The results show satisfactory behavior of ACA and DIP and provide a trigger for further studies of the formulation.https://www.mdpi.com/2076-3417/15/11/6048acetylsalicylic acid and dipyridamoleHPLC-DAD/FLD detectorchocolate–honey formulationdigestion protocolpermeability assessment |
| spellingShingle | Georgios Kamaris Nikoletta Pantoudi Konstantina Chachlioutaki Catherine K. Markopoulou Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment Applied Sciences acetylsalicylic acid and dipyridamole HPLC-DAD/FLD detector chocolate–honey formulation digestion protocol permeability assessment |
| title | Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment |
| title_full | Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment |
| title_fullStr | Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment |
| title_full_unstemmed | Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment |
| title_short | Analysis of Aspirin and Dipyridamole in a Modern Pharmaceutical Formulation-Drug Release Study and Permeability Assessment |
| title_sort | analysis of aspirin and dipyridamole in a modern pharmaceutical formulation drug release study and permeability assessment |
| topic | acetylsalicylic acid and dipyridamole HPLC-DAD/FLD detector chocolate–honey formulation digestion protocol permeability assessment |
| url | https://www.mdpi.com/2076-3417/15/11/6048 |
| work_keys_str_mv | AT georgioskamaris analysisofaspirinanddipyridamoleinamodernpharmaceuticalformulationdrugreleasestudyandpermeabilityassessment AT nikolettapantoudi analysisofaspirinanddipyridamoleinamodernpharmaceuticalformulationdrugreleasestudyandpermeabilityassessment AT konstantinachachlioutaki analysisofaspirinanddipyridamoleinamodernpharmaceuticalformulationdrugreleasestudyandpermeabilityassessment AT catherinekmarkopoulou analysisofaspirinanddipyridamoleinamodernpharmaceuticalformulationdrugreleasestudyandpermeabilityassessment |