Preparation and Quality Evaluation of Carbinoxamine Maleate Sustained-release Suspension / 中国药房

OBJECTIVE:To prepare Carbinoxamine maleate sustained-release suspension,and evaluate its quality. METH-ODS:Using carbinoxamine maleate as raw material,drug-loaded resin was prepared by cation exchange resin;surface coating method was used to finally prepare sustained-release suspension,using Eudragit RS100 as sustained-release coating material to pre-pare sustained-release microparticles. HPLC was conducted to determine the content of carbinoxamine maleate,release degree of original preparations and self-made suspensions was compared,drug-loading capacity was calculated. RESULTS:The drug amount in preparing drug-loaded resin was 2%,reaction temperature was 25 ℃,and reaction time was 4 h;the drug-loading capacity in surface coating was 35%,amount of coating material was 10%,and reaction temperature was 40 ℃. The drug-loading capacities of sustained particles before and after coating were 35.23%,32.72%,respectively;the yield was 96.82%. The carbinoxamine ma-leate in prepared sustained-release suspension accounted for 98.76% of the labeled amount;release degree in 10 h reached about 80%,f2 was 65.73. CONCLUSIONS:Carbinoxamine maleate sustained-release suspension is prepared successfully,and its release is similar to the original preparation.

Avaliação clínica da eficácia e segurança do uso da associação de dipirona sódica, cafeína e maleato de clorfeniramina comparados à associação de paracetamol, cloridrato de fenilefrina e maleato de carbinoxamina no tratamento sintomático de gripe / Evaluation of the clinical efficacy and safety of the use of the association between dipiron, caffeine and clorfeniramine maleate compared to the association of paracetamol, chloridrate of fenilefrine and carbinoxamine maleate on the symptomatic

Duas formas da associação: dipirona sódica, cafeína e maleato de clorfeniramina, ora denominados medicamento A (Apracur®), medicamento B (Benegrip®) foram avaliados comparativamente à associação de paracetamol, cloridrato de fenilefrina e maleato de carbinoxamine (Naldecon®) ora demominada medicamento C, através de estudo clínico mascarado randomizado de caráter prospectivo, com um total de 178 pacientes subdivididos em três grupos, para avaliar a eficácia no tratamento dos sintomas de gripe e resfriados. Como objetivo secundário, visou-se avaliar a tolerabilidade da utilização do medicamento A comparado ao medicamento C e a tolerabilidade da utilização do medicamento B comparado ao medicamento C, devido a uma hipótese estatística de equivalência entre os medicamentos testes e o medicamento controle.Os resultados obtidos relacionados à segurança do uso da medicação demonstraram excelente tolerabilidade dos produtos. Com relação à eficácia, a maioria dos pacientes tratados com o medicamento A ou medicamento B apresentaram eficácia muito boa ou excelente. Os dados obtidos nesse estudo clínico demonstraram a excelente tolerabilidade do medicamento A e medicamento B.