NGHIÊN CỨU BÀO CHẾ VÀ ĐÁNH GIÁ VIÊN NANG ZIDOVUDINE 250MG BẰNG PHƯƠNG PHÁP XÁT HẠT ƯỚT

Abstract

Background: Zidovudine (ZDV), an antiretroviral drug for HIV, exhibits poor flowability and potential polymorphism, hindering the manufacture of granules for encapsulation. Objectives: To develop 250 mg ZDV capsules using wet granulation and to evaluate product quality, stability over 10 weeks under the studied storage condition, and possible solid-state changes of the active ingredient. Materials and methods: Fillers (lactose, corn starch, wheat starch), binder (10% w/v aqueous PVP K30) and the glidant talc were screened. Granules were prepared by wet granulation. Evaluation criteria included flowability, density, volume of encapsulation, mass uniformity, assay and drug release. Stability under the studied condition (10 weeks at 30°C/80% RH) was assessed using dissolution testing and X-ray powder diffraction (XRD). Results: ZDV material exhibited very poor flowability. The formulation capable of encapsulation comprised ZDV 250 mg, lactose monohydrate 100 mg, PVP K30 5,0 mg (10% aqueous solution), and talc 3,5 mg per capsule. Granules exhibited good flowability, capsules met all pharmacopoeial specifications. After 10 weeks of storage, drug release and XRD profiles showed no meaningful change. Conclusions: A wet granulation process and formulation were established for ZDV 250 mg capsules. No meaningful changes in dissolution performance or solid-state characteristics were observed over the study period under the studied storage condition.