Nghiên cứu điều chế Microemulgel chứa Diosmin và Quercetin

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Tác giả: Đức Hạnh Nguyễn, Lê Hà Vũ

Ngôn ngữ: Vie

Ký hiệu phân loại: 615.19 Pharmaceutical chemistry

Thông tin xuất bản: Tạp chí Y học Việt Nam (Tổng hội Y học Việt Nam) 2023

Mô tả vật lý: 288-294

Bộ sưu tập: Metadata

ID: 409235

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Chủ đề

Diosmin và quercetin là hai hoạt chất có tác dụng kháng viêm, làm bền thành mạch, có tiềm năng ứng dụng bào chế dạng thuốc dùng qua da hỗ trợ điều trị suy giãn tĩnh mạch. Cả hai hoạt chất diosmin và quercetin đều có độ tan trong nước kém. Vì vậy, đề tài nghiên cứu phát triển dạng bào chế microemulgel chứa diosmin và quercetin (DQE). Độ tan của diosmin và quercetin trong các tá dược được xác định bằng phương pháp quá bão hoà để lựa chọn tá dược cho công thức vi nhũ tương (VNT). Giản đồ pha được xây dựng sử dụng phương pháp chuẩn độ nước. Hoạt chất được tải vào công thức VNT được chọn và đánh giá cảm quan, pH, độ nhớt, kích thước tiểu phân. Độ bền vật lý của VNT chứa diosmin và quercetin (DQM) được đánh giá qua 6 chu kỳ nhiệt, mỗi chu kỳ bao gồm 2 giai đoạn: 4 ± 1oC trong 48 giờ và 45 ± 1oC trong 48 giờ và ly tâm tốc độ 10.000 vòng/ phút trong 30 phút. DQE được điều chế từ DQM và khảo sát phối hợp với các tá dược tạo gel khác nhau (HPMC, Sepinov Derm, Sepimax Zen). Tính chất của DQE được đánh giá gồm: cảm quan, pH, độ nhớt, độ dàn mỏng. DQM được chọn có kích thước giọt là 165,6 ± 2,0 nm (PDI=0,267) và bền với thử nghiệm sốc nhiệt và ly tâm. DQE có thành phần công thức gồm Plurol oleique CC479: Cremophor RH 40: Transcutol P: Nước: Sepinov Derm với tỷ lệ lần lượt là 15 %: 16,67 %: 8,33 %: 60 %: 0,1 % (kl/kl). Hàm lượng diosmin và quercetin trong DQE lần lượt là 0,005 % và 0,01 % (kl/kl). DQE có pH là 3,95 và có tính chất lưu biến phi Newton kiểu giả dẻo. Nghiên cứu đã xây dựng thành công công thức DQE chứa 0,005% diosmin và 0,01% quercetin. Kết quả nghiên cứu có thể làm tiền đề cho việc phát triển dạng bào chế dùng ngoài để hỗ trợ điều trị suy giãn tĩnh mạch., Tóm tắt tiếng anh, Diosmin and quercetin are active ingredients, possess anti-inflammatory effects, stabilize blood vessels, and could be the potential API for transdermal formulations for the treatment of varicose veins. Both diosmin and quercetin have poor water solubility. This study aimed at developing a microemulgel dosage form containing diosmin and quercetin (DQE). The solubility of diosmin and quercetin in excipients was investigated by using the saturation method to select excipients of microemulsion. The phase diagram was constructed using the water titration method. Active ingredients were loaded into selected microemulsion formulations and evaluated for organoleptic, pH, viscosity, and particle size. The physical stability of microemulsion containing diosmin and quercetin (DQM) was evaluated through 6 thermal cycles, each cycle consisted of 2 phases: 4 ± 1oC for 48 hours and 45 ± 1oC for 48 hours and high-speed centrifugation at 10000 rpm for 30 minutes. DQE was prepared from DQM and investigated in combination with different gelling excipients (HPMC, Sepinov Derm, Sepimax Zen). The properties of DQE were evaluated including: organoleptic, pH, viscosity, and thinness. The selected DQM had a droplet size of 165.6 ± 2.0 nm (PDI=0.267) and was resistant to thermal and centrifugation tests. The chosen DQE consisted of Plurol oleique CC479: Cremophor RH 40: Transcutol P: Water: Sepinov Derm with the ratios of 15%: 16.67%: 8.33%: 60%: 0.1% (kl/kl), respectively. The contents of diosmin and quercetin in DQE were 0.005% and 0.01% (w/w), respectively. DQE had a pH of 3.95 and possessed the pseudoplastic non-Newtonian rheological properties. The study has successfully developed a DQE formulation containing 0.005% diosmin and 0.01% quercetin. The results could be useful for the development of a transdermal dosage form to support the treatment of varicose veins.

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