Extended release promethazine HCl using acrylic polymers by freeze-drying and spray-drying techniques: formulation considerations

Abstract

The present study investigated a novel extended release system of promethazine hydrochloride (PHC) with acrylic polymers Eudragit RL100 and Eudragit S100 in different weight ratios (1:1 and 1: 5), and in combination (0.5+1.5), using freeze-drying and spray-drying techniques. Solid dispersions were characterized by Fourier-transformed infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), Nuclear magnetic resonance (NMR), Scanning electron microscopy (SEM), as well as solubility and in vitro dissolution studies in 0.1 N HCl (pH 1.2), doubledistilled water and phosphate buffer (pH 7.4). Adsorption tests from drug solution to solid polymers were also performed. A selected solid dispersion system was developed into capsule dosage form and evaluated for in vitro dissolution studies. The progressive disappearance of drug peaks in thermotropic profiles of spray-dried dispersions were related to increasing amount of polymers, while SEM studies suggested homogenous dispersion of drug in polymer. Eudragit RL100 had a greater adsorptive capacity than Eudragit S100, and thus its combination in (0.5+1.5) for S100 and RL 100 exhibited a higher dissolution rate with 97.14% drug release for twelve hours. Among different formulations, capsules prepared by combination of acrylic polymers using spray-drying (1:0.5 + 1.5) displayed extended release of drug for twelve hours with 96.87% release followed by zero order kinetics (r 2 = 0.9986).Uniterms: Promethazine hydrochloride/extended release. Drugs/extended release. Eudragit RL100. Eudragit S100. Acrylic polymers. Spray drying/pharmacotechnics. Freeze drying/pharmacotechnics. Extended realease/pharmacotechnics. Pharmaceutical formulations/evaluation. O presente trabalho compreendeu estudo de um novo sistema de liberação prolongada de cloridrato de prometazina (PHC) com polímeros acrílicos Eudragit RL100 e Eudragit S100 em diferentes proporções em massa (1:1 e 1:5) e em combinação (0,5+1,5), utilizando técnicas de liofilização e de secagem por aspersão As dispersões sólidas foram caracterizadas por espectrofotometria no infravermelho por transformada de Fourier (FT-IR), calorimetria diferencial de varredura (DSC), difratometria de raios X (PXRD), Ressonância Magnética Nuclear (RMN), microscopia eletrônica de varredura (SEM) e, também, por estudos de solubilidade e de dissolução in vitro em HCl 0,1 N (pH 1,2), água bidestilada e tampão fosfato (pH 7,4). Realizaram-se, também, testes de adsorção da solução do fármaco nos polímeros sólidos. Desenvolveu-se sistema de dispersão sólida exclusiva dentro das cápsulas, que foi avaliado por meio de estudos de dissolução in vitro. Relacionou-se o desaparecimento progressivo de picos do fármaco em perfis termotrópicos de dispersões secas por spray à quantidade aumentada de polímero, enquanto os estudos de SEM sugeriram dispersão homogênea do fármaco no polímero. O Eudragit RL100 apresentou maior capacidade de adsorção do que o Eudragit S100 e, dessa forma, a combinação de (0,5+1,5) para S100 ...

S(-) and R(+) species derived from antihistaminic promethazine agent: structural and vibrational studies

“…Consequently, the biological activities and effects of these types of species on human health are obviously resulted of their nature and structural, electronic and topological properties. Hence, the interest to study another antihistaminic agent, in this case promethazine (PTZ) [10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33], which has two N–CH 3 groups (as diphenhydramine) linked to a chiral carbon and, as a consequence two enantiomeric S and R structures are expected for their three free base, cationic and hydrochloride species. PTZ hydrochloride is a drug used to treatment of nausea, vomiting, and dizziness associated with motion sickness and, besides possesses anti-pruritic, anti-allergic, anticholinergic, antihistaminic, central nervous system depressant, and with general anaesthetics effects.…”

Graphene Reinforced Polymer Matrix Nanocomposites: Fabrication Method, Properties and Applications

“…The polymerization of one polymer is conducted in the presence of another polymer resulting in interpenetrating polymer networks. Polymer electrolytes are prepared using this technique [59]. The preparation method of the blend polymer can impact the miscibility between two or more polymers than their properties.…”

IMPROVEMENT AND ESTIMATION OF ORALLY DISINTEGRATING TABLETS CONTAINING PILOCARPINE 2-Hydroxy PROPYL Β-Cyclodextrin INCLUSION COMPLEX BY RESPONSE SURFACE METHODOLOGY

“…There were critical contrasts in dissolution profiles for unadulterated medication, corporal blend, and lyophilized blend. Accounting DE10 min esteems, dissolution pace for Pilocarpine was expanded in the request: unadulterated medication less than 1:1 corporal blend less than 1:1 lyophilized blend proposing that dissolution flow is affected by lyophilization technique used to set up incorporation complex [24]. Following 4 min, the level of unadulterated medication broken down was 41.23% in any case, the rate medicates dissolution from the physical blend, lyophilized complex was 69.03%, and 89.23% individually.…”