کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2504601 1557466 2009 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
پیش نمایش صفحه اول مقاله
Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying
چکیده انگلیسی

A mucoadhesive combination of a maize starch (Amioca®, mainly consisting of amylopectine) and a cross-linked acrylic acid-based polymer (Carbopol® 974P) was spray-dried with metoprolol tartrate (used as model molecule) in order to develop a powder suitable for nasal drug delivery via a one-step manufacturing process. The bioavailability of metoprolol tartrate after nasal administration of this powder to rabbits was compared with powders manufactured via other procedures: (a) freeze-drying of a dispersion prepared using the co-spray-dried powder, (b) freeze-drying of a dispersion prepared using a physical mixture of drug and mucoadhesive polymers. After co-processing via spray-drying a low bioavailability (BA 10.8 ± 2.3%) was obtained, whereas manufacturing procedures based on freeze-drying yielded a higher BA: 37.9 ± 12.8% using the co-processed powder and 73.6 ± 24.9% using the physical mixture. The higher bioavailability was due to the deprotonation of poly(acrylic acid) during neutralisation of the dispersion prior to freeze-drying. This induced repulsion of the ionised carboxyl groups and a lower interaction between poly(acrylic acid) and starch, creating a less compact matrix upon hydration of the polymer and allowing an easier escape of metoprolol tartrate from the matrix. This study showed that co-processing of a mucoadhesive Amioca®/Carbopol® 974P formulation with metoprolol tartrate via co-spray-drying did not provide any added value towards the bioavailability of the drug after nasal administration of the mucoadhesive powder.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 379, Issue 1, 8 September 2009, Pages 67–71
نویسندگان
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