Developing a Flexible Pediatric Dosage Form for Antiretroviral Therapy: A Fast-Dissolving Tablet

Abstract

Current presentations of the anti-HIV drugs lopinavir and ritonavir make appropriate dosing for children difficult. We conducted a feasibility study to develop a formulation for these drugs with child-safe excipients in a flexible dosage form for children across the pediatric age spectrum. The freeze-drying in blister approach was used to produce fast-dissolving tablets (FDTs), as these can be dispersed in fluids for easy administration, even to infants, and appropriate portions of the dispersion can be given for different ages/weights. We combined various ratios of polymers, surfactants, and bulking agents to incorporate the 2 highly hydrophobic drugs while maintaining drug stability, rapid disintegration, and good handling properties. The final FDT was robust and disintegrated in 0.5 mL of fluid in 10 s with up to 4 tablets dissolving in 2 mL to achieve varying doses accommodated in a common teaspoon. Drug recovery after dissolution in small volumes of liquid or fluid foods was 90%-105%. The final candidate FDT was stable at 40°C, 75% relative humidity for up to 3 months. FDTs are a promising flexible dosage form for antiretroviral treatment for pediatric patients, especially in low-resource settings.

Trends in the Characterization Methods of Orodispersible Films

“…The dried sample is then subjected to a stepwise increase and decrease in relative humidity from 0 to 95% and 95 to 0%, respectively at 25 ºC. The total weight of water absorbed (sorption phase) and lost (desorption phase) are recorded [32][33][34].…”

“…It is worth noting that, preservatives are sometimes included in ODF formulations to deter the microbial activities [24]. The quantification of residual water is generally obtained using thermogravimetry, infrared light balances, or Karl Fischer titration [32]. In some situations, thermogravimetric analysis (TGA) helps to define the type of water associated to the matrix.…”

Masalah dan Pengembangan Formulasi Obat untuk Bentuk Dosis Anak-Anak

“…Tablet juga tidak mengalami perubahan setelah uji stabilitas dipercepat pada suhu 40°C dan kelembaban 75%. Tablet yang dihasilkan juga dapat dilarutkan dalam susu atau makanan cair lainnya (Lal et. al, 2017).…”

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“…For these reasons tablets which will quickly dissolve or disintegrate within the oral cavity have attracted an excellent deal of attention. [1] A fast dissolving tablet (FDT) system may be outlined as an indefinite quantity type for oral administration that once placed in the mouth, quickly spread, or dissolved and may be enclosed in a type of liquid. [2] Recently, a quick dissolving formulation is popular as novel drug delivery systems as a result of their straightforward to administer and result in higher data patient compliance.…”