No abstract

Background: In many countries, the hypertension in the pediatric population is considered an important risk of mortality and morbidity. In this sense, it is important to design and develop new pharmaceutical forms for pediatric patients with hypertension. The development of orodispersible mini-tablets (ODMTs) for paediatric use has gained importance within recent years the WHO authorities set up regulations for developing suitable and palatable dosage forms for paediatric patients. Objective: The aim of this study was to design and develop orodispersible mini tablets of enalapril maleate for pediatric use. Methods: Five pharmaceutical formulations were designed. The effects of different co-processed excipients and active pharmaceuthical ingredient at different doses were study. Lactose co-processed excipients selected were Tablettose® 80, MicroceLac® 100 and StarLac®. The micromeritic properties were evaluated for all the physical mixtures. The mini tablets were obtained by direct compression and quality control parameters were determined in accordance with United States Pharmacopeia. Results: Three OMDTs with StarLac® provide good results of hardness, flowability and fast disintegration. One of them, with 0.1 mg of enalapril maleate, showed the best results for the official parameters of hardness (4.0 kp), friability (< 1%), disintegration time (28 s), drug content uniformity (103.6 %) and the best wetting time (23 s). Conclusion: The orodispersible mini tablets with StarLac® showed good officially quality parameters. One of them showed the best wetting time and doses for pediatric patients. This formulation could be considered eligible to be elaborated on an industrial scale.

A phytochemical study was performed on three native plant species from the central-western zone of Argentina: Buddleja cordobensis Grisebach, Baccharis salicina Torr. & A. Gray and Nepeta cataria L. We could obtain verbascoside (1) from B. cordobensis. From N. cataria we could obtain 1, 5, 9-epi-deoxyloganic acid (2) L. Finally, we could isolate 2--(L-rhamnopyranosyl)-3-angeloyloxy-15-acetyloxy-7,13( 14)-E-dienent-labdane (3) and 2--(L-rhamnopyranosyl)-3--angeloyloxy-15-hydroxy-7,13( 14)-E-dien-ent-labdane (4) from B. salicina. Moreover, three derivatives from 1, and one semi-synthetic derivative from 2, were prepared. PCR reaction was used to analyse the activity against DNA polymerase, and cell culture to determine cytotoxicity and antitumoral activity. Verbascoside (1) was strongly active in the nanomolar scale (IC 50 = 356 nM) against DNA polymerization. Moreover, verbascoside was also strongly active in the nanomolar scale against human melanoma cell line (IC 50 = 256 nM) and human colorectal cell line (IC 50 = 320 nM). Furthermore, derivatives 6 and 7 were cytotoxic against both cancer cell lines.

In popular medicine Silybum marianum is used as a hepatoprotective agent. Silymarin is the major constituent. The present work deals with the formulation and evaluation of S. marianum tablets from ethanolic extract by direct compression. The ethanolic extract was obtained from seeds by soxhlet extraction. Two pharmaceutical formulations were prepared using fluid extract as an active principle, and Aeroperl® 300 Pharma as a carrier. In order to improve flow ability and compressibility, co-processed excipients MicroceLac® 100 and FlowLac® 90 were employed. Pre-compression and post-compression parameters were evaluated according to USP 34-NF 29. Besides, silymarin was determined by NMR spectral data. Both formulations showed excellent rheological properties and the best biopharmaceutical parameters were observed in F2 (S. marianum ethanolic extract, aeroperl® 300 Pharma, flowLac® 90, glycolate starch and magnesium stearate) in terms of the friability (0.82 %) and the disintegration time (8.05 min).