New Orodispersible Mini Tablets of Enalapril Maleate by Direct Compression for Pediatric Patients

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.

Mini-Tablets: A Valid Strategy to Combine Efficacy and Safety in Pediatrics

“…Moreover, in contrast to hydrochlorthiazide, the enalapril formulation with Ludiflash ® did not achieve the required content uniformity. Regardless, since enalapril has gained importance in recent years among the scientific community, further efforts have been made to develop enalapril-containing oro-dispersible MTs for pediatric use [54]. In addition to mannitol and isomalt, lactose co-processed excipients were also employed to design MTs by direct compression.…”

Synthesis, Characterization, and Cytotoxicity Assessment of New 4-Benzyl-1,3-Oxazole Derivatives Incorporating 4-[(4-Bromophenyl)sulfonyl]phenyl Fragment

“…UV-Vis spectra were registered for methanolic solutions (≈ 0.025 mM) on an Analytik Jena AG Specord 40 spectrophotometer. FT-IR spectra were recorded in KBr pellets on a Bruker Vertex 70 spectrometer, absorption peaks being described as very strong, vs; strong, s; medium, m; weak, w. NMR spectra were acquired on a Varian Gemini 300 BB instrument at 300 MHz for 1 H and 75 MHz for 13 C. Combined 2D spectra (COSY, HETCOR) were also recorded. DMSO-d 6 or CDCl 3 as deuterated solvents were used.…”

“…5-Hydroxy-1,3-oxazoles exist in their corresponding keto tautomer: 1,3-oxazol-5(4H)-ones which present cytotoxic [9,10], antiviral [11], plant growth regulating properties [12]. Some representants of N-acyl-α-amino acids class show biological activities, such as antihypertensive [13], anticancer [14], mucolytic [15], antianaemic [16], anti-ulcer effect [17], and are specific antidotes in acute intoxications [18,19]. N-Acyl-αamino-ketones display anti-inflammatory [20], antiviral [21,22] and antithrombotic action [23].…”

Electrospun Structural Hybrids of Acyclovir-Polyacrylonitrile at Acyclovir for Modifying Drug Release

“…Different kinds of modified release profiles have special advantages for therapeutic applications. For example, the immediate release of a drug is essential when rapid action is required, and is welcomed by patients with conditions such as pains or fevers and heart attacks [34][35][36][37][38]. Alternatively, sustained drug release for a long time period is popular with patients for cases where the administration frequency can be reduced for a better quality of life [39][40][41][42][43][44].…”