Formulation, Development and Scale-Up of Fixed-Dose Combination Tablets Containing Zidovudine, Lamivudine and Nevirapine.

The development of antiretroviral associations in a single dosage form aims to ensure good efficacy, low costs and better adherence to treatment.

Thereby, this work aimed to perform the pharmacotechnical development and stability studies of coated tablets of fixed-dose combination of zidovudine, lamivudine and nevirapine (300 + 200 + 150 mg, respectively). To develop the pharmaceutical form, the direct compression (DC) and wet granulation (WG) methods were tested, and the qualitative and quantitative planning of diluents (101 and 250 microcrystalline cellulose, spray dried monohydrate lactose and corn starch) and coating polymers (Opadry white II HP® and Instacoat Aqua Moistshield II®) were analyzed.

Quality control was carried out according to the specifications set by official compendia. The chosen formulation was scaled-up and the industrial batches were submitted to accelerated and long-term stability studies. The batches obtained by WG met the requirements, using 101 microcrystalline cellulose, corn starch and Opadry white II HP® as excipients.

The DC trial was not possible due to the need of a greater proportion of excipients to improve the characteristics of the drugs. Thus, this study brings a new therapeutic alternative for HIV treatment, offering another possibility to simplify drug administration. Continue reading