Thiết kế phân tán rắn của mirtazapine với các hệ thống tá carrier khác nhau: tối ưu hóa, đánh giá in vitro và đánh giá sinh khả dụng

Drug Delivery and Translational Research - 2023
Reem A. Aldeeb1, Mahmoud A. Mahdy2, Hanan M. El-Nahas2, Abeer A. Musallam1
1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, 6th of October City, Giza, 12582, Egypt
2Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt

Tóm tắt

Tóm tắtKỹ thuật phân tán rắn là phương pháp hiệu quả và được sử dụng rộng rãi nhất để tăng cường độ tan và tốc độ giải phóng của các loại thuốc có độ tan trong nước thấp. Mirtazapine (MRT) là một thuốc chống trầm cảm không điển hình được dùng để điều trị trầm cảm nặng. MRT có sinh khả dụng qua đường uống thấp (khoảng 50%) do độ tan trong nước thấp (phân loại BCS II). Mục tiêu của nghiên cứu là xác định điều kiện tối ưu để kết hợp MRT vào các loại polyme khác nhau bằng cách sử dụng kỹ thuật phân tán rắn (SD), với mục đích chọn công thức phù hợp nhất có độ tan trong nước tối ưu, hiệu suất tải và tốc độ hòa tan tối ưu. Thiết kế D-tối ưu đã được sử dụng để chọn phản ứng tối ưu. Công thức tối ưu đã được đánh giá tính chất lý hóa bằng phương pháp quang phổ hồng ngoại Fourier (FT-IR), nhiệt lượng kế quét vi sai (DSC), nhiễu xạ tia X bột (XRPD), và kính hiển vi điện tử quét (SEM). Nghiên cứu sinh khả dụng in vivo đã được tiến hành trên mẫu huyết tương của thỏ trắng. MRT-SDs được chuẩn bị bằng phương pháp bay hơi dung môi sử dụng Eudragit (RL-100, RS-100, E-100, L-100–55), PVP K-30, và PEG 4000 với các tỷ lệ phần trăm thuốc/polyme khác nhau (33.33%, 49.99%, và 66.66%). Kết quả cho thấy công thức tối ưu đạt được bằng PVP K-30 với tỷ lệ phần trăm thuốc là 33.33% mang lại hiệu suất tải là 100.93%, độ tan trong nước là 0.145 mg/ml, và tốc độ hòa tan là 98.12% sau 30 phút. Những phát hiện này đã chứng minh việc cải thiện đầy hứa hẹn các đặc tính của MRT và tăng sinh khả dụng qua đường uống của nó lên 1.34 lần so với thuốc đơn thuần.

Từ khóa


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