Xây dựng công thức bào chế viên nén nổi acyclovir 100 mg

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Tác giả: Minh Ngọc Nguyễn, Thị Hoài Thương Nguyễn, Thế Anh Tài Võ

Ngôn ngữ: vie

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Thông tin xuất bản: Tạp chí Khoa học và Công nghệ - Đại học Nguyễn Tất Thành, 2023

Mô tả vật lý: tr.47

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Acyclovir is an antiviral drug used in the treatment of infections mainly caused by Herpes simplex and Varicella Zoster viruses. However, when taken orally, the drug has low bioavailability (10 - 20)%. The reason acyclovir has low bioavailability is because the drug is mainly absorbed at the end of the stomach and the beginning of the small intestine, so for optimal absorption, the drug must be kept in the stomach. In order to improve treatment effectiveness and increase bioavailability of the drug, the research team has developed a formula for preparing acyclovir 100 mg floating tablets. The study investigated the influence of extended-release excipients (sodium croscarmelose (NaCMC), carbopol, sodium alginate, xanthan gum) and filler excipients on the quality parameters of semi-finished granules and tablets. compressed. The results were tablets prepared according to formula CT12 with ingredients: acyclovir 100 mg and excipients NaCMC (50 mg), carbopol (50 mg), lactose (40 mg), Avicel PH 101 (40 mg), polyvinyl pirrolidone K30 (PVP K30) (20 mg), sodium bicarbonate (100 mg) and magnesium stearate: talc 2% (ratio 1:1) have met the criteria of mass uniformity, hardness, abrasion, and durability. Drug content according to DĐVN V standards, ability to float for over 8 hours and sustained release up to 8 hours (94.90 %).Acyclovir là thuốc kháng virus sử dụng trong điều trị các bệnh nhiễm trùng chủ yếu do virus Herpes simplex và Varicella Zoster gây ra. Tuy nhiên khi dùng theo đường uống thuốc có sinh khả dụng thấp (10 – 20) %, là do acyclovir có sinh khả dụng thấp. Do vậy, để hấp thu được tối ưu thì thuốc phải được giữ ở dạ dày. Nhằm cải thiện hiệu quả điều trị, tăng sinh khả dụng của thuốc, nghiên cứu này xây dựng công thức bào chế viên nén nổi acyclovir 100 mg. Nghiên cứu đã khảo sát sự ảnh hưởng của các tá dược kéo dài giải phóng (natri croscarmelose (NaCMC), carbopol, natri alginat, gôm xanthan) và các loại tá dược độn đến các chỉ tiêu chất lượng của cốm bán thành phẩm và viên nén. Kết quả thu được viên bào chế theo công thức CT12 với thành phần: acyclovir 100 mg và các tá dược NaCMC (50 mg), carbopol (50 mg), lactose (40 mg), Avicel PH 101 (40 mg), polyvinyl pirrolidon K30 (PVP K30) (20 mg), natri bicarbonat (100 mg) và magnesi stearat : talc 2 % (tỉ lệ 1:1) đã đạt các chỉ tiêu về độ đồng đều khối lượng, độ cứng, độ mài mòn, hàm lượng dược chất theo tiêu chuẩn DĐVN V, khả năng nổi trên 8 giờ và giải phóng kéo dài lên đến 8 giờ (94,90 %).

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