Deficiency of ubidecarenone (coenzyme Q) has been described based on failure of biosynthesis caused by gene mutation, inhibition of biosynthesis by HMG coA reductase inhibitors or for unknown reasons in ageing and cancer. The amount of coenzyme Q in the diet is not sufficient to increase serum coenzyme Q significantly; thus, a pharmaceutical therapy is needed in these pathologies. Ubidecarenone has a very slightly water solubility so much so that its dissolution rate from oral solid dosage form is very low in the human gastric pH. This behavior causes variable gastrointestinal absorption strictly dependent on the formulation and several months may be necessary before therapeutical effect appears. The present work rises from the need of ASL Napoli 3 South Pharmaceutical Service, to produce a new galenic formulation of ubidecarenone in high oral dose (capsules, 250 mg for unit) for patients affect by amyotrophic lateral sclerosis (ALS). Preformulative studies were carried out to set up the process parameters (excipients, formulation, production technique) useful to improve the drug dissolution rate and bulking properties of the powders.
UNA INNOVATIVA FORMULAZIONE NEO-GALENICA DI UBIDECARENONE AD ALTO DOSAGGIO
LAURO, Maria Rosaria;SANSONE, FRANCESCA;AQUINO, Rita Patrizia
2011-01-01
Abstract
Deficiency of ubidecarenone (coenzyme Q) has been described based on failure of biosynthesis caused by gene mutation, inhibition of biosynthesis by HMG coA reductase inhibitors or for unknown reasons in ageing and cancer. The amount of coenzyme Q in the diet is not sufficient to increase serum coenzyme Q significantly; thus, a pharmaceutical therapy is needed in these pathologies. Ubidecarenone has a very slightly water solubility so much so that its dissolution rate from oral solid dosage form is very low in the human gastric pH. This behavior causes variable gastrointestinal absorption strictly dependent on the formulation and several months may be necessary before therapeutical effect appears. The present work rises from the need of ASL Napoli 3 South Pharmaceutical Service, to produce a new galenic formulation of ubidecarenone in high oral dose (capsules, 250 mg for unit) for patients affect by amyotrophic lateral sclerosis (ALS). Preformulative studies were carried out to set up the process parameters (excipients, formulation, production technique) useful to improve the drug dissolution rate and bulking properties of the powders.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
