Optimization of Pothomorphe umbellata (L.) Miquel topical formulations using experimental design.

Pothomorphe umbellata is a native plant widely employed in the Brazilian popular medicine. This plant has been shown to exert a potent antioxidant activity on the skin and to delay the onset and reduce the incidence of UVB-induced skin damage and photoaging. The aim of this work was to optimize the appearance, the centrifuge stability and the permeation of emulsions containing P. umbellata (0.1% 4-nerolidylchatecol). Experimental design was used to study ternary mixtures models with constraints and graphical representation by phase diagrams. The constraints reduce the possible experimental domain, and for this reason, this methodology offers the maximum information while requiring the minimum investment. The results showed that the appearance follows a linear model, and that the aqueous phase was the principal factor affecting the appearance; the centrifuge stability parameter followed a mathematic quadratic model and the interactions between factors produced the most stable emulsions; skin permeation was improved by the oil phase, following a linear model generated by data analysis. We propose as optimized P. umbellata formulation: 68.4% aqueous phase, 26.6% oil phase and 5.0% of self-emulsifying phase. This formulation displayed an acceptable compromise between factors and responses investigated.

Optimization of poorly compactable drug tablets manufactured by direct compression using the mixture experimental design.

The poor flowability and bad compressibility characteristics of paracetamol are well known. As a result, the production of paracetamol tablets is almost exclusively by wet granulation, a disadvantageous method when compared to direct compression. The development of a new tablet formulation is still based on a large number of experiments and often relies merely on the experience of the analyst. The purpose of this study was to apply experimental design methodology (DOE) to the development and optimization of tablet formulations containing high amounts of paracetamol (more than 70%) and manufactured by direct compression. Nineteen formulations, screened by DOE methodology, were produced with different proportions of Microcel 102, Kollydon VA 64, Flowlac, Kollydon CL 30, PEG 4000, Aerosil, and magnesium stearate. Tablet properties, except friability, were in accordance with the USP 28th ed. requirements. These results were used to generate plots for optimization, mainly for friability. The physical-chemical data found from the optimized formulation were very close to those from the regression analysis, demonstrating that the mixture project is a great tool for the research and development of new formulations.

Total flavonoids quantification from O/W emulsion with extract of Brazilian plants.

A new derivative spectrophotometric (DS) method was proposed and validated for quantification of total flavonoids from in O/W emulsion with polyacrylamide (and) C13-14 isoparaffin (and) laureth-7 containing Catuaba (Trichilia catigua Adr. Juss) (and) Marapuama (Ptychopetalum olacoides Bentham) extract. DS method was optimized to perform the assay in most favorable conditions. Linearity, specificity and selectivity, recovery (Rc, %), precision (R.S.D., %), accuracy (E, %), detection (LOD, microg ml(-1)) and quantification limits (LOQ, microg ml(-1)) were established for method validation. First-derivative at 388.0 nm (zero-to-peak; amplitude= +/- 0.12; wavelength range= 300.0-450.0 nm and Deltalambda = 4 nm) offered linearity for rutin concentrations ranging from 10.0 to 60.0 microg ml(-1) in ethanol 99.5%. Second-derivative provided to be unsuitable for interval evaluation obtaining unacceptable accuracy. Analytical method was validated for first-derivative, according to the experimental results: correlation coefficient (r = 0.9999); specificity to total flavonoids quantification, expressed in rutin, at wavelength 388.0 nm and selectivity with elimination of interference from matrix; Rc = 108.78%; intra- and inter-run precision (1.30-3.65% and 3.48-4.68%), and intra- and inter-run accuracy (100.00-112.19% and 101.25-118.44%); LOD = 0.62 microg ml(-1) and LOQ = 1.86 microg ml(-1).

Validation assay for total flavonoids, as rutin equivalents, from Trichilia catigua Adr. Juss (Meliaceae) and Ptychopetalum olacoides Bentham (Olacaceae) commercial extract.

An ultraviolet spectrophotometric method was validated for total flavonoid quantitation, as rutin equivalents, present in the Trichilia catigua Adr. Juss (Meliaceae) and Ptychopetalum olacoides Bentham (Olacaceae) commercial extract. Parameters as linearity, interval (range), specificity, estimated limit of detection (LOD, microg/mL), estimated limit of quantitation (LOQ, microg/mL), recovery (R, %), precision or relative standard deviation (RSD, %), and accuracy (E, %) were established. The analytical method was validated according to the experimental results: correlation coefficient (r = 0.9997); interval (RSD = 0.15-0.47%; E = 98.98-101.24%); specificity to total flavonoids quantitation, as rutin equivalents, at wavelength 361.0 nm; LOD = 0.09 microg/mL and LOQ = 0.27 microg/mL; R = 99.36-102.14%; adequate intra- and interrun precision (0.30-0.49% and 0.31-0.81%), and intra- and interrun accuracy (100.60-102.38% and 98.58-100.38%).

Avaliação da cinética de dissolução de ampicilina em comprimidos comercializados no Brasil / Dissolution kinetics of ampicillin from tablets available in Brazilian market

No presente estudo, foram avaliadas quatro especialidades farmacêuticas (A, B, C e D) contendo ampicilina, na forma de comprimidos, sendo que, do fabricante A, foram tomados dois lotes (A1 e A2). O perfil de dissolução dos produtos foi traçado utilizando-se as condições descritas na Farmacopéia Americana (USP 23, 1995), retirando-se alíquotas nos intervalos de: 1, 5, 10, 20, 30 e 45 minutos. Após a determinação da ordem do processo de dissolução, foram calculados os parâmetros cinéticos: eficiência de dissolução (ED), constante de velocidade de dissolução (k) e meia-vida de dissolução (t ANTPOT. 50 por cento). Os resultados indicaram que os produtos apresentam acentuada discrepância, porém, A2 e B mostraram-se semelhantes quanto ao processo de dissolução, não sendo evidenciadas diferenças significativas quanto ao valor de ED