Formulation, Development and Scale-Up of Fixed-Dose Combination Tablets Containing Zidovudine, Lamivudine and Nevirapine.
BACKGROUND
The development of antiretroviral associations in a single dosage form aims to ensure improved efficacy, low costs and better adherence to treatment.


OBJECTIVE
This work performed the pharmacotechnical development, coating, and stability studies of fixed-dose combination tablets of zidovudine, lamivudine and nevirapine (300 + 200 + 150 mg, respectively).


METHODS
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, and direct compression (DC) and wet granulation (WG) methods were tested aiming the development of the pharmaceutical form. 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.


RESULTS
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 ratio of excipients to improve formulation properties.


CONCLUSION
Thus, this study brings a new therapeutic alternative for HIV treatment, contributing to the development of another possibility to simplify drug administration.
['Lavra|Zênia Maria Maciel|ZMM|', 'de Medeiros|Flávia Patrícia Morais|FPM|', 'da Silva|Rosali Maria Ferreira|RMF|', 'Rosa|Talita Atanazio|TA|', 'Wanderley Sales|Victor de Albuquerque|VA|', 'Barros Silva|Laysa Creusa Paes Barreto|LCPB|', 'de Sousa|André Luiz Moreira Domingues|ALMD|', 'de Lima|Leduar Guedes|LG|', 'Rolim|Larissa Araújo|LA|', 'Neto|Pedro José Rolim|PJR|']
D019380:Anti-HIV Agents D004338:Drug Combinations D004339:Drug Compounding D000076722:Drug Development D004355:Drug Stability D019259:Lamivudine D019829:Nevirapine D013607:Tablets D013678:Technology, Pharmaceutical D015215:Zidovudine
coating polymers HIV AIDS Drug stability highly active antiretroviral therapy tablet.