Preformulation studies for the development of a microemulsion formulation from Ambrosia peruviana All, with anti-inflammatory effect

Abstract Natural products are considered an important source of the therapeutic arsenal currently available. Among these alternatives are the seeds of Ambrosia peruviana (altamisa), whose extract has shown an anti-inflammatory effect. The main objective of this work was to perform a preformulation study of Ambrosia peruviana seeds ethanolic extract, where the main factors that affect the physical, chemical, and pharmacological stability of the extract were evaluated, as well as a compatibility study by differential scanning calorimetry (DSC) analysis against different excipients. A dry extract was obtained by rotary evaporation of the seeds macerated with 96% ethanol. The anti-inflammatory activity was determined by measuring its effect on NO production in RAW 264.7 macrophages, stimulated with LPS. The results showed that the dry extract maintained its stability over time when stored at a temperature of 4 and 25ºC, demonstrating its biological activity, the content of phenolic compounds, and its physicochemical parameters remain practically invariable. However, when exposed to high temperatures (60 ºC) it was affected. The thermal analysis revelated that the behavior of most of the selected excipients and the dry extract was maintained, which indicates that it did not present incompatibilities, therefore they can be candidates for formulating a microemulsion.

Development of new ophthalmic suspension prednisolone acetate 1%

Formulation of a new Prednisolone acetate [1%] ophthalmic suspension to obtain a better contactibility of the drug at the site of action. The formulation was evaluated and optimized based on physiological, physicochemical and pharmaceutical parameters and prepared aseptically, keeping particle size between 1-3 micro m, while viscosity enhancer, preservative, chelating agent were used to increase the transient residence time, antimicrobial preservation respectively. Isotonicity of the formulation was maintained. Buffering agents used were having buffering capacity NMT 0.05%. pH adjusted at which Prednisolone acetate was stable. The finished product subjected to stress conditions to check the physical stability of the formulation. The formulation was packed in LDPE plastic vials, and subjected to accelerated stability studies at 40°C and the kinetic and predictive method was employed for the determination of degradation rate constant and shelf life. The results showed that the development of a new ophthalmic formulation having significantly better contact time by the selection and optimization of viscosity [HPMC] that obtained [21 cps] with better stability studies. The results concluded that prednisolone acetate 1.0 per cent ophthalmic suspension is more effective than prednisolone phosphate 1.0 per cent ophthalmic solution in suppressing corneal inflammation

Prophylactic effect of plaster and cataplasm contained ketoprofen in rats with adjuvant arthritis

This study demonstrates that prophylactic effect of plaster and cataplasm contained ketoprofen in adjuvant arthritis therapy by X-ray. Adjuvant arthritis was induced by a single injection of Freund's complete adjuvant. Mature female Sprague-Dawley rats were designated to 3 groups such as nontreated control, plaster-treated (PT) and cataplasm-treated (CT), each of which was composed of ten animals. The PT and the CT groups showed reduced primary paw swelling, but secondary paw swelling was not affected. Bony changes were observed in all regions of the femur and tibia of the nonadjuvant-injected leg and the adjuvant-injected leg. The mean radiographic scores of the PT and the CT groups were significantly lower than those of the control group from day 0 to 7 of the experimental period (p<0.05, p<0.01). The CT rats showed reduced poly-arthritis development than the PT rats. Our results suggest that radiographic assessment of bony changes is more suitable for measuring changes in long bones such as femur or tibia than in vertebrae. The prophylactic effect of CT prominently suppressed edematous swelling and bony changes in arthritic limb compared with PT.

Comparative study of the efficacy and tolerability of Secnidazole suspension (single dose) and Tinidazole suspension (two days dosage) in the treatment of amebiasis in children

Amebiasis caused by Entamoeba histolytica may be considered the most aggressive parasitic disease affecting human intestine, causing acute amoebic colitis and extra-intestinal diseases of high morbidity and mortality. 5-nitroimidazoles are the drugs of choice. In this multicenter, open and randon clinical trial, the efficacy and tolerability of secnidazole suspension in a single oral dose of 1ml/kg was compared with 0.5ml/kg doses of tinidazole suspension given for 2 consecutive days to 303 Entamoeba histolytica-positive children aged 2 to 13. Patients with extra-intestinal complications were excluded from the study. Clinical and parasitological follow-up using the Faus and Kato-Katz method were carried out 7, 14, and 21 days after treatment. Clinical improvement/cure was observed in 93 percent of the patients in the secnidazole group and 91 percent in the tinidaloze group. Parasitological sucess was reported for 77 percent and 63 percent of the secnidazole and tinidazole patients, respectively, showing a significant statistical difference between the two groups (p=0.007). Both drugs were well tolerated, and the adverse effects reported were mild, consisting mainly of digestive disturbances. This comparative study showed that a single oral dose of 1ml/kg of secnidazole produced a significantly higher parasitological cure rate than 2 doses of tinidazole. Secnidazole is a safe and effective drug for the treatment of uncomplicated intestinal amebiasis.