The present study was done to develop and evaluate a matrix transdermal patch for bisoprolol fumarate. Different combinations of Eudragit RS 100 and HPMC E5 were used with polyethylene glycol 400 as a plasticizer on a polyvinyl alcohol backing layer by the solvent evaporation technique. The patches were evaluated for organoleptic characteristics and physicochemical parameters. Initial in vitro dissolution experiments were conducted to optimize formulation parameters prior to ex vivo skin permeation studies. Eudragit RS 100 and HPMC E5 (9:1) combination was studied for skin permeation because of the sustain release effect. The effect of control patch and permeation enhancer including Tween 80, propylene glycol, and DMSO were evaluated at 10%-40% concentration in the Franz diffusion cell using excised abdominal skin of rabbit. Different kinetic models were used to interpret the release kinetics and drug release mechanism. The patch M04-PE containing 40% Tween 80 had better sustained release effect and had closer flux to the desired flux. M04-PE followed the zero-order kinetics with super case II release drug mechanism.

No abstract

Context:Nepeta ruderalis Buch.-Ham. (Lamiaceae), locally known as Badranj Boya, is an aromatic herb used traditionally as an antispasmodic, antidiarrhoeal, and anti-asthamatic remedy.Objective: Aqueous methanolic extract of N. ruderalis was studied to investigate its traditional uses.Materials and methods: Study was conducted from September 2015 to February 2016. In vitro spasmolytic and broncho-relaxant activity of crude extract of N. ruderalis (whole plant) was evaluated at 0.01–10 mg/mL final bath concentration in isolated rabbit jejunum and tracheal tissues, using PowerLab data acquisition system (Transonic Systems Inc., Ithaca, NY). In vivo antidiarrhoeal activity was evaluated in castor oil-induced diarrhoeal mice at the dose of 300 and 500 mg of crude extract orally.Results: Crude extract of N. ruderalis completely relaxed spontaneously contracting, high K+ (80 mM) and carbachol (1 μM) induced contracted jejunum with an EC50 value of 5.85 (5.45–6.27), 4.0 (3.80–4.23) and 2.86 (2.48–3.29), similar to verapamil. Nr.Cr relaxed high K+ and carbachol induced contractions, at 5 and 10 mg/mL with an EC50 value of 2.37 (2.11–2.67) and 3.26 (2.9–3.67), respectively, and also displaced calcium concentration–response curves toward right at 0.1 and 0.3 mg/mL. Nr.Cr exhibited antidiarrhoeal protection at a dose of 300 and 500 mg/kg, similar to verapamil, whereas no acute toxicity signs were seen up to 5 g/kg in healthy mice.Discussion and conclusion: Results suggest the presence of spasmolytic and broncho-relaxant effects in the crude extract of N. ruderalis, possibly mediated through calcium channel-blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal and airway disorders.

ABSTRACT:The basic purpose of the current study was to formulate controlled release matrix tablets loaded with loxoprofen sodium using pectin and hydroxypropylmethyl cellulose (HPMC). The effect of these polymers on the release pattern of drug from the formulated matrix system was evaluated. Different concentrations of these polymers alone as well as polymeric blends were used in tablets formulation using wet granulation technique. The differential scanning calorimetric technique was used to detect the chemical interactions between ingredients. Precompression studies were done to assess fineness and flow properties of the granules. Hardness, friability, weight variations, and percentage drug contents were calculated for the evaluation of compressed tablets. F9 formulated in the combination of HPMC and pectin in the ratio of 30:10 showed better retardation during dissolution studies. Upon application of statistical models, the diffusion process was found to be dominant for drug release following the Higuchi model. HPMC and pectin were found suitable for the formulation of controlled release matrix tablets. C 2014 Wiley Periodicals, Inc. Adv Polym Technol 2015, 34, 21493; View this article online at wileyonlinelibrary.com.