Evaluation and Comparison of Wound Healing Properties of an Ointment (AlpaWash) Containing Brazilian Micronized Propolis and Peucedanum ostruthium Leaf Extract in Skin Ulcer in Rats.

Several previous studies have demonstrated improved wound healing associated with natural-based formulations. Therefore, the purpose of this study was to assess the efficacy of a topical formulation containing both a Brazilian micronized propolis extract and a Peucedanum ostruthium leaf extract for the treatment of wounds created by surgical punch in rats. The study was conducted for 14 days and animals were treated as follows: gauze group (G), polyethylene glycol base ointment (Control), AlpaWash (an ointment containing a Brazilian micronized propolis extract and Peucedanum ostruthium leaf extract [Treatment]), and polysporin (one of the most commonly used topical antibiotic ointments, based on bacitracin zinc and polymyxin B sulfate [Reference Standard]). In general, the results demonstrated that ointments, due to occlusiveness and the ability to maintain moisture under the damaged area, offered improvements when compared to lesions without any treatment. Additionally, the presence of phenolic and flavonoid compounds, as well as antioxidants and antimicrobials, offered improved stimulation and could accelerate wound healing. The Control, Treatment, and Reference Standard groups were able to close the lesion, as measured by the wound healing rate determination and follow-up photographs. However, AlpaWash and Polysporin presented some additional benefits- anti-inflammatory activity, measured using myeloperoxidase and histological count, as well as fibroplasia and hydroxyproline production, suggesting that skin with a better quality could be formed following these two treatments. Therefore, based on the current concern of antibiotic overuse in wound healing, the emergence of multi-resistant organisms and the decrease in newer antibiotics, AlpaWash is considered a prominent formulation to be employed in wound-healing applications.

Antimicrobial Activity of Copaiba (Copaifera officinalis) and Pracaxi (Pentaclethra macroloba) Oils against Staphylococcus Aureus: Importance in Compounding for Wound Care.

The Amazon rainforest is the largest reserve of natural products in the world. Its rich biodiversity of medicinal plants has been utilized by local populations for hundreds of years for the prevention and treatment of various diseases and ailments. Oil extracts from plant species such as Copaifera officinalis and Pentaclethra macroloba are used in compounded formulations for their antiinflammatory, antimicrobial, emollient, moisturizing, and wound-healing activities. The objective of this study was to investigate the in vitro bacteriostatic effect of two Amazonian oils, Copaiba and Pracaxi, against Staphylococcus aureus, a clinically important microorganism responsible for wound infection, to support the use of these oils as novel natural products for compounded wound-treatment modalities. The antibacterial activity of Copaiba and Pracaxi oils against a standard strain of Staphylococcus aureus was assessed using broth microdilution to determine the Minimum Inhibitory Concentration and Minimum Bactericidal Concentration of the oil extracts. Copaiba oil demonstrated antibacterial activity against Staphylococcus aureus, with a Minimum Inhibitory Concentration of 0.3125 mg/mL and a Minimum Bactericidal Concentration of 0.3125 mg/mL. Conversely, Pracaxi oil failed to inhibit Staphylococcus aureus growth. While additional studies are required to further evaluate the antimicrobial activity of Pracaxi oil, even low concentrations of Copaiba oil effectively inhibited Staphylococcus aureus growth, supporting its potential use as a promising adjuvant in compounded topical formulations for wound and scar healing.

Development of ciclopirox olamine topical formulations: evaluation of drug release, penetration and cutaneous retention.

With the aim of reducing system absorption and consequently, the side effects, and simultaneously select a penetration enhancing, three topical formulations with 0.5% ciclopirox olamine (CO) and 15% of propylene glycol (PG), ethoxydiglycol or oleic acid were developed and evaluated regarding the skin penetration and cutaneous retention of the drug using Franz diffusion cells. Release experiments were performed through synthetic membrane while dermatomed pig ear skin was used to evaluate CO skin penetration and skin retention. Retention studies were carried out applying tape stripping method and dosing CO in stratum corneum and in epidermis and dermis. A HPLC method was validated for quantifying CO. All formulations tested with synthetic membrane presented no retention of the drug. Permeation data suggested that there was no systemic absorption of ciclopirox olamine from the studied formulations, even when the skin penetration enhancers were applied. Higher concentrations of the drug were found in the stratum corneum (SC) and also in epidermis and dermis, for all of the developed formulations. The addition of enhancers improved the penetration and cutaneous retention of CO, and propylene glycol promoted higher concentrations in epidermis and dermis, probably because its cumulative effect on the skin and by an efficient solvent power.

Development and in vitro evaluation of extended-release theophylline matrix capsules

Polymers like cellulose (MethocelTM K100MPRCR, K15MPRCR and E4MCR) at different proportions (15-35 percent) were used to slow the release of theophylline (100 mg) from capsules. Volumetric method for powder filling capsules was used to prepare the capsules. Drug release from capsules was performed using apparatus 1, at 100 rpm and 900 mL of intestinal medium without enzymes (pH 7.5), at 37 ºC, following the USP 28th ed. (Test 8). Dissolution profiles were compared to two batches of commercial extended-release capsules. Capsules compounded with 35 percent (wt/wt) of MethocelTM E4MCR showed dissolution profile according to the official especifications. Similar results were reproduced with other ten compounded batches. Commercial extended-release capsules containing theophylline pellets (100 mg) showed quick drug release when submitted to the same test, indicating that, in these conditions, the capsules did not show prolonged release. Mathematical models like zero-order, first-order and Higuchi were applied in kinetic studies of theophylline release from the compounded capsules. Polymers were efficient to control the release of theophylline in capsules involving diffusion and erosion as mechanisms, and that first-order model was the best fitted one for theophylline matrix capsules. These results support that compounded extended-release capsules can be prepared, since the drug release tests can be done.

Cápsulas de liberação modificada contendo 100 mg de teofilina foram preparadas com polímeros derivados da celulose (Methocel® K100MPRCR, K15MPRCR e E4MCR) em diferentes concentrações, 15-35 por cento, empregando-se o método volumétrico. Estudos de liberação do fármaco foram realizados de acordo com a Farmacopéia Americana 28 ed., (Teste 8), empregando aparato 1, rotação de 100 rpm e temperatura de 37 ºC em 900 mL de meio fluido intestinal sem enzimas (pH 7,5). Os perfis de dissolução foram comparados ao de duas especialidades farmacêuticas comerciais. A formulação, com 35 por cento de Methocel® E4MCR, evidenciou perfis de liberação de acordo com as especificações e os resultados foram reprodutíveis para 10 lotes manipulados com a mesma formulação. As cápsulas comerciais de liberação prolongada contendo 100 mg de teofilina (microgrânulos), submetidas ao mesmo ensaio, apresentaram rápida liberação do fármaco, indicando que a liberação não é fator limitante para a absorção. Avaliou-se a cinética de liberação do fármaco empregando os modelos matemáticos de ordem zero, primeira ordem e Higuchi. Conclui-se que as matrizes obtidas foram capazes de modular a liberação, envolvendo os mecanismos de difusão e erosão, prevalecendo o modelo de primeira ordem e que as cápsulas de liberação modificada podem ser manipuladas, desde que testes de liberação sejam realizados.

Estudo biofarmacotécnico de cápsulas de amoxicilina. Análises comparativa de produtos industrializados e magistrais. Cinética de dissolução / Biopharmaceutical study of amoxicilin capsules. Comparative analysis of products from pharmaceutical industries and masterly drugstore. Dissolution kinetic

Cápsulas contendo 500 mg de amoxicilina, provenientes de 3 laboratórios farmacêuticos nacionais A, B e C (3lotes de cada) foram avaliadas quanto à qualidade biofarmacotécnica. Foram realizados teste e perfil de dissolução de acordo com os procedimentos descritos na USP 23. A quantificação do fármaco foi realizada por espectrofotometria no ultravioleta em 274 nm. No processo cinético de dissolução foram considerados os parâmetros: constante de velocidade de dissolução (Kd.), meia-vida de dissolução (td50º°) e eficiência de dissolução (ED). Os produtos A e D mostraram perfis de dissolução diferenciados, sugerindo que são inequivalentes.

Estudo biofarmacotécnico de cápsulas de Amoxicilina. Análise comparativa de produtos industrializados e magistrais. Cinética de dissolução / Biopharmaceutical study of Amoxicilin capsules. Comparative analysis of products from pharmaceutical industries and masterly drugstore. Dissolution kinetic

Cápsulas contendo 500 mg de amoxicilina, provenientes de 3 laboratórios farmacêuticos nacionais A, B e C (3 lotes de cada) e de 2 farmácias magistrais D e E de Juiz de Fora (2 lotes de cada) foram avaliadas quanto à qualidade biofarmacotécnica. Foram realizados teste e perfil de dissolução de acordo com os procedimentos descritos na USP 23. A quantificação do fármaco foi realizada por espectrofotometria no ultravioleta em 274 nm. No processo cinético de dissolução foram considerados os parâmetros: constante da velocidade de dissolução (Kd), meia-vida de dissolução (td 50 por cento) e eficiência de dissolução (ED). Os produtos A e D mostraram perfis de dissolução diferenciados, sugerindo que são inequivalentes.