Effect of cellulose acetate phthalate and polyethylene glycol on physical properties and release of theophylline from microcapsules

ABSTRACT The present study describes the development of theophylline microcapsules by a non-solvent addition method and the effect of plasticizer addition on microencapsulation. The release was studied in distilled water and the data were analysed by various mathematical models for determining the mechanism of release. Prepared microcapsules were found to be spherical, free flowing and having more than 80% entrapped drug. The polymer - cellulose acetate phthalate and plasticizer - polyethylene glycol was considered to be affecting the properties of microcapsules including drug release (time for 50% drug release, T50). The formulation with the highest proportion of polymer and without plasticizer (F3) showed the slowest release with T50 = 4.3 h, while the formulation with lower proportion of polymer and 20% (w/w) plasticizer (F13 &14) showed the fastest release of drug with T50 values of 1.2 h and 1.3 h, respectively. The drug release from most of the formulations was found to be following Higuchi model. It is concluded from the results of the present study that cellulose acetate phthalate significantly affects the sustained release of the drug in water, whereas the addition of polyethylene glycol slightly enhances the drug release.

RESUMO O presente estudo descreve o desenvolvimento de microcápsulas de teofilina pelo método sem adição de solvente e o efeito da adição de plastificante na microencapsulação. A liberação foi estudada em água destilada e os dados foram analisados por vários modelos matemáticos para determinação do mecanismo de liberação. As microcápsulas preparadas mostraram-se esféricas, livres de corrente e com mais de 80% de fármaco encapsulado. O polímero - ftalato de acetato de celulose e o plastificante - polietileno glicol - afetaram as propriedades das microcápsulas, incluindo a liberação do fármaco (tempo para liberação de 50% do fármaco, T50). A formulação com a maior proporção de polímero e sem plastificante (F3) se mostrou como a de liberação mais lenta, com T50 = 4,3 h, enquanto as formulações com menor proporção de polímero e 20% de plastificante (m/m) (F13 &14) apresentaram a liberação mais rápida do fármaco, com T50 de 1,2 h e 1,3 h, respectivamente. A liberação do fármaco para a maioria das formulações seguiu o modelo de Higuchi. Concluiu-se, dos resultados do presente estudo, que o ftalato do acetato de celulose afeta significativamente a liberação controlada do fármaco em água, enquanto que a adição de polietileno glicol aumenta ligeiramente a liberação do fármaco.

Organizadores e cortadores de comprimidos: riscos e restrições ao uso / Pill organizers and pill cutters: risks and limitations / Organizadores y cortadores de comprimidos: riesgos y restricciones del uso

Com base em análise documental, foram discutidas e problematizadas as limitações associadas à utilização de organizadores e cortadores de comprimidos, como questão de saúde pública. Os organizadores destinados ao armazenamento e transporte de comprimidos e cápsulas expõem essas formas farmacêuticas a fatores ambientais dos quais estariam protegidos em suas embalagens originais, comprometendo sua estabilidade, eficácia e segurança. Os cortadores oferecem risco adicional quanto a perda da eficácia, reações adversas e intoxicação. Por outro lado, o transporte de medicamentos pelo usuário é reflexo da conciliação entre autonomia e autocuidado e a partição de comprimidos é necessária para cumprir certos regimes posológicos. Conclui-se que cabe aos profissionais observar e orientar pacientes e cuidadores, visando à adequação dessas condutas e à prevenção dos riscos envolvidos.

In this essay, based on documental analysis, the limitations associated with the use of pill organizers and cutters are discussed and analyzed as a matter of public health. The use of the organizers for storing and carrying tablets and capsules exposes these medications to environmental factors from which their original packaging protected them, compromising their stability and safeness. Cutters also pose the additional risk of causing loss of efficacy, adverse reactions and overdose. On the other hand, the user carrying their own medication reflects the balance between autonomy and self-care, and splitting is sometimes required to comply with certain regimens. It can be concluded that healthcare professionals should observe and guide patients and caregivers in order to avoid risks.

Objetivo Con base en análisis documental, se discutieron y señalaron los problemas de las limitaciones asociadas a la utilización de organizadores y cortadores de comprimidos, con respecto a la salud pública. Los organizadores destinados al almacenamiento y transporte de comprimidos y cápsulas exponen las formas farmacéuticas a factores ambientales de los cuales estarían protegidos en sus embalajes originales, comprometiendo su estabilidad, eficacia y seguridad. Los cortadores ofrecen riesgo adicional con relación a la pérdida de la eficacia, reacciones adversas e intoxicación. Por otro lado, el transporte de medicamentos por el usuario es reflejo de la conciliación entre autonomía y autocuidado, y la partición de comprimidos es necesaria para cumplir ciertos regímenes posológicos. Se concluye que resta a los profesionales observar y orientar pacientes y cuidadores, buscando la adecuación de esas conductas y la prevención de los riesgos involucrados.

Modificación de formas farmacéuticas sólidas: relevamiento en un hospital de la Provincia de Córdoba / [Modification of solid dosage forms: survey in a hospital of the Province of Cordoba].

BACKGROUND: In the hospital setting is frequent to manipulate solid dosage forms (SDF, tablets 16 and capsules), which can affect their physicochemical and biopharmaceutical properties, the pharmacoloeffect and sometimes to cause the appearance of undesirable side effects. OBJECTIVES: To identify the medicines whose SDF is altered in a Hospital of Cordoba (Argentina), to determine how these modifications are made and to establish whether they were properly performed or not. METHODS: We retrospectively analyzed the prescriptions made between the 5th and the 11th of March of 2012 and identified impaired requesting SDF modifications. Open interviews were held with nurses and service visits to each hospital to determine how they manipulated the SDF. RESULTS: We analyzed 700 prescriptions for 113 patients, of which 61 (54

) had manipulations of the received SDF (49 for medical prescription, 7 because they had nasogastric tubes, 3 due to patient choice and 2 by nursing decision). Twenty three medicines were manipulated, but only 12 were correctly manipulated. The major changes were partition of tablets and grinding of tablets or microgranules and dispersible in water. CONCLUSION: The SDF of several medicines is altered in the analyzed hospital, many times without medical indication and scientific justification. It would be appropriate to conduct training courses and establish closer collaborations between pharmacy and nursing units in the investigated hospital.