Comparison of Pharmacokinetic Characteristics of Bilosomal Dispersion Versus Pure Solution of Oral Ropinirole Hydrochloride in Rats

المؤلفون

DOI:

https://doi.org/10.32007/jfacmedbagdad.6622210

الكلمات المفتاحية:

روبينيرول هيدروكلوريد، الناقلات الحويصلية النانوية، البيلوسومات، التوافر الحيوي

الملخص

Background: Ropinirole hydrochloride is a non-ergoline antiparkinson drug. It is a highly hydrophilic drug and classified as class III according to Biopharmaceutical Classification System with low absolute oral bioavailability of approximately 50% upon oral administration due to significant hepatic first-pass metabolism.

Objective: to compare the pharmacokinetic parameters of Ropinirole,  when administered orally in the form of a Ropinirole bilosomal dispersion in contrast to an oral Ropinirole solution.

Methods: This study involved the use of twelve male Wistar rats, with an average weight of 220±11 g, and these rats were divided into two groups, comprising six rats each. A 1.1mg/kg doses of pure Ropinirole and Ropinirole bilosomes were administered orally through gavage after reconstituting in distilled water. Ropinirole was quantified in the rat's plasma using HPLC, subsequently establishing a spiked calibration curve with plasma samples and utilizing paracetamol as an internal standard. The statistics included mean values (± SD; n = 6) for pharmacokinetic parameters, with statistical significance assessed using a Student's t-test.

Results: For the oral bilosomes, the values were 9.4±0.11 μg /ml for Cmax, 3±0.00 h for Tmax, and 55.56±2.12 μg h/ml for AUC0-24. In contrast, for the oral solution, the corresponding values were 7.2±0.14 μg/ml for Cmax, 1.5±0.00 h for Tmax, and  23.70±2.23 μg h/ml for AUC0-24. These parameters were significantly higher (P<0.05) as compared with a pure drug solution. The comparative bioavailability of Ropinirole (AUC0-24 oral solution / AUC0-24 oral bilosomes ) is equal to 42.66%, which indicates the bioavailability of the oral RH solution was less than that of RH bilosomal dispersion.

Conclusions: The use of nano vesicular carriers (bilosomes) shows significant potential as an effective delivery system for improving the oral bioavailability of ropinirole hydrochloride

التنزيلات

تنزيل البيانات ليس متاحًا بعد.

السير الشخصية للمؤلفين

  • Samer K. Ali، Department of Pharmaceutics College of Pharmacy, University of Baghdad, Baghdad, Iraq.

    MSc Student 

  • Entidhar J. Al-Akkam، Department of Pharmaceutics College of Pharmacy, University of Baghdad, Baghdad, Iraq.

    Pharmacist 

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Bilosomes, Bioavailability, nanovesicular carriers, Pharmacokinetics,  Ropinirole hydrochloride.

التنزيلات

منشور

2024-07-01

كيفية الاقتباس

1.
Ali SK, J. Al-Akkam E. Comparison of Pharmacokinetic Characteristics of Bilosomal Dispersion Versus Pure Solution of Oral Ropinirole Hydrochloride in Rats. J Fac Med Baghdad [انترنت]. 1 يوليو، 2024 [وثق 24 نوفمبر، 2024];66(2):201-8. موجود في: https://iqjmc.uobaghdad.edu.iq/index.php/19JFacMedBaghdad36/article/view/2210

تواريخ المنشور

الإستلام

2023-12-08

النسخة النهائية

2023-12-11

الموافقة

2024-08-05

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