ABSTRACT
Os sistemas multiparticulados contêm o fármaco subdividido em unidades funcionais, que podem ser pellets, grânulos ou minicomprimidos. Oferecem vantagens tecnológicas e biofarmacotécnicas quando comparados aos sistemas monolíticos, apresentando ainda benefícios terapêuticos para os pacientes. Por isso, têm se destacado cada vez mais dentre as novas formas farmacêuticas e sistemas de liberação de fármacos. Os minicomprimidos possuem diâmetro igual ou inferior a 2 - 3 mm e são obtidos através do processo de compressão, utilizando máquinas de comprimir convencionais adaptadas com punções múltiplos. Quanto ao aspecto tecnológico, oferecem vantagens em relação aos pellets e grânulos. O objetivo desta revisão é, portanto, abordar os principais aspectos tecnológicos envolvidos na sua obtenção, destacando suas vantagens e aplicações.
In multiparticulate systems, the drug is subdivided into functional units, which may be in the form of pellets, granules or minitablets. They have technological and biopharmacotechnical advantages over monolithic systems and also offer therapeutic benefits to patients. For these reasons, they have gained prominence among new pharmaceutical dosage forms and drug delivery systems. Minitablets are between 2 and 3 mm in diameter or smaller and are manufactured by means of the direct compression process, with a conventional tablet press adapted with multi-tip punches. In technological terms, they have advantages over both pellets and granules. The objective of this review is, therefore, to discuss the main technological features of minitablet production, highlighting their advantages and applications.
Subject(s)
Biopharmaceutics/trends , Tablets , Technology, Pharmaceutical , Drug Delivery SystemsABSTRACT
Neste estudo buscou-se desenvolver formulações de comprimidos tamponados mastigáveis (CTM) de didanosina com eficiência de dissolução (ED%) e capacidade neutralizante ácida (CNA) otimizados, tendo como base o medicamento referência e especialidades farmacêuticas disponíveis no mercado nacional. Cinco formulações de CTM foram produzidas e avaliadas quanto a ED% e CNA, por meio de ensaio de dissolução e titulação ácido-base, respectivamente. Os resultados iniciais de CNA foram próximos aos encontrados para as especialidades farmacêuticas, aproximadamente 12 mEq HCl, porém distantes do medicamento referência (especialidade A, CNA = 17,93 mEq HCl). Já as formulações derivadas de CTM-4 conduziram à obtenção de comprimidos tamponados com CNA otimizada de aproximadamente 17,5 mEq HCl, o mesmo ocorrendo para ED%, (61,33% e 62,00%, CTM-4-2-1 e3, respectivamente). Esse resultado mostra-se próximo ao valor de 59,33% da especialidade A, quando utilizado o mesmo método de dissolução, indicando haver equivalência entre estas formulações e o medicamento referência para estes parâmetros.
The aim in this study was to develop chewable buffered tablets (CBT) of didanosine with optimized dissolution efficiency (DE) and acid-neutralizing capacity (ANC), using the reference medicine and other pharmaceutical didanosine products available in Brazil as models. Five CBT formulations were prepared and assessed for DE and ANC, through the dissolution test and acid-base titration, respectively. The initial ANC results fell short of those for the reference medicine (product A, ANC= 17.93 mEq HCl), but were close to those obtained for other pharmaceutical products (approximately 12 mEq HCl). The formulations derived from CBT-4 resulted in buffered tablets with an optimized ANC of 17.5 mEq HCl, approximately. The same was found for DE (61.33% and 62.00%, CBT-4-2-1 and CBT 3, respectively). This result proved to be close to that of product A (59.33%), when the same method was used for the dissolution test, indicating that both formulations and the reference medicine were equivalent with respect to these properties.
Subject(s)
Chemistry, Pharmaceutical , Dissolution , Didanosine/pharmacokinetics , Pharmaceutical Preparations , Tablets, Enteric-CoatedABSTRACT
Local anesthetics (LA) belong to a class of pharmacological compounds that attenuate or eliminate pain by binding to the sodium channel of excitable membranes, blocking the influx of sodium ions and the propagation of the nerve impulse. S (-) bupivacaine (S(-)bvc) is a local anesthetic of amino-amide type, widely used in surgery and obstetrics for sustained peripheraland central nerve blockade. This article focuses on the characterization of an inclusion complex of S(-) bvc in2-hydroxypropyl- beta-cyclodextrin (HP-beta -CD). Differential scanning calorimetry, scanning electron microscopy andX-Ray diffraction analysis showed structural changes inthe complex. In preliminary toxicity studies, the cellviability tests revealed that the inclusion complex decreased the toxic effect (p smaller that 0.001) produced by S(-) bvc.These results suggest that the S(-) bvc:HP- beta-CD inclusion complex represents a promising agent for the treatment of regional pain.