Development of microparticles and microparticulated tablets containing piperine

Abstract Piper nigrum (black pepper) is used in Indian traditional medicine and its main alkaloid, Piperine (PIP), presents antioxidant, antitumor and neuroprotective pharmacological properties. This substance is insoluble in aqueous media and can irritate the gastrointestinal tract. Aiming to avoid these inconvenient characteristics and enable PIP oral administration, this study suggested the PIP microencapsulation through the emulsion-solvent evaporation method and the preparation of microparticulated tablets by direct compression. An UV-spectroscopy method was validated to quantify PIP. Microparticles and microparticulated tablets were successfully obtained and the microparticles exhibited excellent flow. The scanning electron microscopy images showed that PIP microparticles were intact after compression. The in vitro release showed a controlled release of PIP from microparticles and PIP microparticles from tablets in comparison to PIP and PIP tablets. The release profiles of PIP microparticles and the microparticulated tablets were similar. Therefore, tablets containing PIP microparticles are promising multiparticulated dosage forms because a tablet allows microparticles administration and the intact ones promote a controlled release, decreasing its irritating potential on the mucosa.

Intoxicación severa por Nicotiana glauca (Palán Palán) con miocardio atontado / Severe poisoning by Nicotiana glauca (Palán Palán) with stunned myocardium

Resumen Nicotiana glauca también llamada Palán Palán, es un arbusto con hojas verdes azuladas y despulidas y una flor amarilla tubular pendulante que presenta alcaloides piridínicos, como nicotina, nornicotina, anatabina y anabastina (análogo estructural de la Nicotina). Se presenta el caso clínico de una paciente de 50 años con cuadro agudo de debilidad muscular generalizada que evoluciona con paro respiratorio, tras la ingesta accidental de una cantidad desconocida de hojas de Nicotiana glauca, cultivadas en una huerta hogareña mediante técnica de hidroponía y confundidas por su conviviente con espinaca. Presentó aumento de lactato y Troponina Ultra Sensible e Hipoquinesia Global de Ventrículo Izquierdo en el ecocardiograma, compatible con Aton tamiento Miocárdico (AM), que evolucionó favorablemente. Si bien hay pocos reportes, se han informado muertes de animales y humanos, tras la ingesta accidental de Nicotiana glauca. El inicio del cuadro es rápido, con patrón bifásico, con vómitos y estímulo simpático, seguido por bloqueo ganglionar y neuromuscular, pudiendo presentar paro respiratorio, shock, convulsiones y coma. El AM es una disfunción miocárdica prolongada con retorno gradual de la actividad contráctil, posterior a un episodio breve de isquemia grave, puede ser asintomático, pudiendo presentar alteraciones en el electrocardiograma, enzimas cardíacas o ecocardiograma. Generalmente presenta pronóstico favorable, pudiendo presentar insuficiencia cardíaca ante patologías concurrentes o aumento de requerimientos de oxígeno.

Abstract Nicotiana glauca is a shrub with bluish green leaves and a pendulous tubular yellow flower. It has pyridine alkaloids, such as nicotine, nornicotine, anatabine and anabastine (structural analog of Nicotine). We present the case of a 50 years old pa- tient with acute generalized muscle weakness that evolves to respiratory arrest, after accidentally ingesting an unknown quantity of Nicotiana glauca leaves, grown in a home vegetable garden, using a hydroponic technique and confused by her cohabiting with spinach. She presented increased lactate and Ultra Sensitive Troponin and Left Ventricular Global Hypokinesia in the echo- cardiogram, compatible with Myocardial Stunned, that it evolved favorably. There are few reports, animal and human deaths have been reported following accidental ingestion of Nicotiana glauca. The onset of the symptoms is early, with a biphasic pattern, with vomiting and sympathetic stimulation, followed by ganglionic and neuromuscular blockage and may present respiratory arrest, shock, seizures and coma. Myocardial Stunned is a prolonged myocardial dysfunction with gradual return of contractile activity after a brief episode of severe ischemia, it can be asymptomatic, and it can present alterations in the electrocardiogram, cardiac enzymes or echocardiogram. Generally presents a benign prognosis, being able to present heart failure with concurrent patholo- gies or increased requirements.

Comparative assessment of effect of malt with different bud length on prolactin in hyperprolactinemia rat

Malt is the mature fruit of Hordeum vulgare L. after germination and drying and has been applied for treatment female abnormal galactorrhea. Previous studies have showed total alkaloids in malt have anti-HPRL effect. However, total alkaloids of malt change with the growth cycle, and the specified levels of total alkaloids in different bud length of malt have not been decided. To determine the definitive level of total alkaloids in different buds of malt and the most suitable bud length for clinical application by comparing effects on hyperprolactinemia rat. During the budding of malt, the content of total alkaloids first increased and then decreased, and it peaked at a bud length of 0.75 cm. Treated the HPRL model rats with different buds of malt, the PRL level was decreased, the number of PRLpositive cells and the mRNA expression level in the pituitary were significantly declined, and the number of dopamine D1 and D2 receptors in the hypothalamus was increased. The above changes were most significant in 0.75 cm bud. These results suggest that in terms of the content of effective substance and the effects on HPRL model rats, a malt bud length of 0.75 cm is optimal for clinical application.