Formulation and evaluation of sustained release microspheres of rosin containing aceclofenac

Aceclofenac was microencapsulated using rosin by o/w emulsion solvent evaporation technique. The effect of three formulation variables including the drug:polymer ratio, emulsifier (polyvinyl alcohol) concentration and organic solvent (dichloromethane) volume were examined. The prepared batches were characterized for microspheres particle size distribution, encapsulation efficiency and in vitro release behavior. The study reveals that drug:polymer ratio had a considerable effect on the entrapment efficiency, however particle size distribution of microspheres was more dependent on the volume of dichloromethane and polyvinyl alcohol concentration rather than on the drug: polymer ratio. Drug, polymer concentrations were varied to obtain optimum release profile for sustaining the action of the drug

Design and Evaluation of Matrix Diffusion Controlled Transdermal Patches of Diltiazem Hydrochloride

Se desarrolló un sistema matricial de tipo dispersivo para la administración transdérmica de clorhidrato de Diltiazem usando diferentes proporciones de colofonia con Eudragit RL PM y polivinil pirrolidona. El parche preparado con colofonia y polivinil pirrolidona no era transparente y muestra una distribución irregular de polivinil pirrolidona, lo que puede ser debido al carácter hidrófi lo de ésta. Se investigó el efecto de los polímeros sobre las propiedades tecnológicas; es decir, la liberación del fármaco, la velocidad de transmisión del vapor de agua, la pérdida porcentual de humedad y el grosor. El parche con colofonia: Eudragit RL PM (6:4) dio como resultado una liberación de 2651 mcg en 24 horas. Con el objeto de mejorar la liberación, se incluyeron distintas proporciones de alcanfor en la formulación. El parche con colofonia: Eudragit RL PM (6:4) y un 5% p/v de alcanfor dio como resultado una liberación constante del fármaco a lo largo de un período de 24 horas. La formulación F8 resultó ser la más satisfactoria en lo que a las propiedades tecnológicas se refi ere. Se llevaron a cabo estudios posteriores de permeación e irritación de la piel en ratas y conejos respectivamente. Por lo tanto, se puede concluir que con el parche de colofonia: Eudragit RL PM en proporción 6:4 con un 5% p/v de alcanfor, se alcanzan los objetivos deseables en sistemas de administración transdérmica de fármacos tales como anular el efecto de primer paso, una amplia liberación y una frecuencia de administración reducida.A matrix dispersion type transdermal drug delivery system of Diltiazem Hydrochloride was developed using different ratios of rosin with Eudragit RL PM and polyvinyl pyrrolidone. The patch prepared by the combination of rosin and polyvinyl pyrrolidone was not transparent one, and shows an uneven distribution of polyvinyl pyrrolidone, which may be due to the hydrophilic nature of polyvinyl pyrrolidone. The effect of the polymers on the technological properties, i.e., drug release, water vapor transmission rate, percentage moisture loss and thickness were investigated. The patch containing rosin: Eudragit RL PM (6:4) showed a release of 2651 mcg in 24 h. In order to improve the release various proportions of camphor was included in the formulation. The patch containing rosin: Eudragit RL PM (6:4) with 5% w/v of camphor showed a sustained release of the drug extending over a period of 24 h. Formulation F8 emerged as the most satisfactory formulation as far as the technological properties were concerned. Further skin permeation and skin irritation studies were carried out on rat skin and rabbit respectively. Therefore it can be concluded that the patch containing rosin: Eudragit RL PM in the ratio 6:4 with 5%w/v of camphor achieved the desired objectives of transdermal drug delivery systems, such as overcoming of fi rst pass effect, extended release and reduced frequency of administration

Formulation and evaluation of oral sustained release of Diltiazem Hydrochloride using rosin as matrix forming material

Rosin, a natural resin, was used as a hydrophobic matrix material for the controlled release, using diltiazem HCl as model drug. Matrix tablets were prepared by direct compression method using rosin as matrix forming material in different proportions and with different diluent combinations. The tablets prepared were flat faced, retained their shape throughout. The method of preparation of matrix system and its concentration were found to have pronounced effect on the release of diltiazem HCl. The release was found to follow both the first order kinetics and fickian diffusion. The drug delivery was analyzed using the paddle method according to USP XXIII. All the studies were done in phosphate buffer pH 7.4. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and invitro release studies. The results suggest that the rosin is useful in developing sustained release matrix tablets, prolong release of water soluble drug for up to 24h. Rosin thus promises considerable utility in the development of oral sustained release drug delivery systems

Formulación y evaluación de liberación sostenida oral de Diltiazem clorhidrato usando resina como material formador de matriz

Rosin, a natural resin, was used as a hydrophobic matrix material for the controlled release, using diltiazem HCl as model drug. Matrix tablets were prepared by direct compression method using rosin as matrix forming material in different proportions and with different diluent combinations. The tablets prepared were flat faced, retained their shape throughout. The method of preparation of matrix system and its concentration were found to have pronounced effect on the release of diltiazem HCl. The release was found to follow both the first order kinetics and fickian diffusion. The drug delivery was analyzed using the paddle method according to USP XXIII. All the studies were done in phosphate buffer pH 7.4. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and invitro release studies. The results suggest that the rosin is useful in developing sustained release matrix tablets, prolong release of water soluble drug for up to 24h. Rosin thus promises considerable utility in the development of oral sustained release drug delivery systems.Colofonia, una resina natural, se utilizó como un material de matriz hidrofóbica para la liberación controlada, utilizando HCl diltiazem como fármaco modelo. Los comprimidos de matriz se prepararon por el método de compresión directa usando resina como material formador de matriz en diferentes proporciones y con diferentes combinaciones de diluyente. Las tabletas preparadas eran de cara plana, conservan su forma en todas partes. El método de preparación del sistema de matriz y su concentración se encontró que tenían efecto pronunciado sobre la liberación de diltiazem HCl. La liberación se encontró que sólo deben observarse las cinética de primer orden y de difusión de Fick. La administración de fármacos se analizó mediante el método de paletas de acuerdo con la USP XXIII. Todos los estudios se realizaron en tampón de fosfato de pH 7,4. Se evaluaron los comprimidos de matriz de su espesor, dureza, friabilidad, variación de peso, contenido de drogas y de liberación in vitro estudios. Los resultados sugieren que la colofonia es útil en el desarrollo de tabletas de matriz de liberación sostenida, prolongar la liberación del fármaco soluble en agua durante un máximo de 24 horas. así colofonia promete considerable utilidad en el desarrollo de sistemas de administración de fármacos de liberación sostenida oral

Antioksidativno djelovanje biljke Desmodium gangeticum i njezinih fenola u artritičnih štakora

Total alcoholic extract of Desmodium gangeticum, which exhibited significant anti-inflammatory activity, was evaluated for the possible mode of action by studying its antioxidant potential in adjuvant-induced arthritic rats. Activity guided fractionation and isolation were carried out. The phenolics fraction showed maximum potency. Solid phase extraction followed by preparative HPLC of the active phenolic fraction yielded for the first time two potent antioxidant compounds, caffeic acid and chlorogenic acid, from this plant. The biological antioxidant defense system involving the superoxide dismutase, glutathione and catalase, showed a significant increase with their levels close to the normal control with a decrease in the lipid peroxide content upon administration of D. gangeticum extract (100 mg kg-1) and its phenolics (50 mg kg-1) in arthritic rats, thereby indicating the extracts antioxidant property under arthritic conditions.Ispitivan je mogući mehanizam protuupalnog djelovanja alkoholnog ekstrakta biljke Desmodium gangeticum na artritičnim štakorima. Nakon frakcioniranja, najjače djelovanje pokazale su fenolne frakcije. Ekstrakcijom i preparativnom HPLC kromatografijom iz fenolne frakcije izolirana su, prvi put iz te biljke, dva spoja sa snažnim antioksidativnim djelovanjem, kavena i klorogena kiselina. Biološki antioksidativni obrambeni sustav koji se sastoji od superoksidismutaze, glutationa i katalaze značajno je porastao u odnosu na kontrolnu skupinu, nakon davanja ekstrakta D. gangeticum (100 mg kg-1) i njegovih fenola (50 mg kg-1) artritičnim štakorima. Istovremeno se smanjio sadržaj peroksida u lipidima. To ukazuje da ekstrakt djeluje antioksidativno u stanju upale

In vivo Antidiabetic and Antioxidant Potential of Stephania hernandifolia in Streptozotocin-Induced-Diabetic Rats

Stephania hernandifolia (Menispermaceae) is a medicinal plant, used by herbalists for treating various diseases, one of which is diabetes mellitus, in Darjeeling. However, its antidiabetic activity has not been scientifically investigated so far. The aim of this study, therefore, is to investigate the antidiabetic and antioxidant potential of the powdered corm of Stephania hernandifolia. This was tested in normal and Streptozotocin (STZ)-induced diabetic rats, using oral administration of ethanol and an aqueous extract (400 mg/kg body weight) of Stephania hernandifolia corm. After the oral administration of water and ethanol extracts at doses of 400 mg/kg body weight, blood glucose levels were monitored at specific intervals and it was found that they were significant lowered. Glibenclamide was used as a standard drug at a dose of 0.25 mg/kg. The experimental data revealed that both extracts has significant antihyperglycemic and antioxidant activity in Streptozotocin-induced rats compared to the standard drug. The antioxidant activity in vitro was measured by means of the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and Superoxide-free radical scavenging assay. Ascorbic acid, a natural antioxidant, was used as a control. The extracts of ethanol and aqueous were strongly scavenged DPPH radicals, with IC50 being 265.33 and 217.90 µg/ml, respectively. Although the extracts of ethanol and aqueous were moderately scavenged, the superoxide radical were with IC50 values of 526.87 and 440.89 µg/ml. The study revealed that the ethanolic extract exhibited more significant antidiabetic and antioxidant activity then the aqueous extract