Čvrste disperzije silimarina: Karakterizacija i utjecaj načina priprave na oslobađanje

The influence of preparation methodology of silymarin solid dispersions using a hydrophilic polymer on the dissolution performance of silymarin was investigated. Silymarin solid dispersions were prepared using HPMC E 15LV by kneading, spray drying and co-precipitation methods and characterized by FTIR, DSC, XRPD and SEM. Dissolution profiles were compared by statistical and model independent methods. The FTIR and DSC studies revealed weak hydrogen bond formation between the drug and polymer, while XRPD and SEM confirmed the amorphous nature of the drug in co-precipitated solid dispersion. Enhanced dissolution compared to pure drug was found in the following order: co-precipitation > spray drying > kneading methodology (p sušenje sprejom > metoda gnječenja (p < 0.05). Iz svih pripravaka oslobađanje je bilo sporije, bez obzira na metodu priprave. Pripravci dobiveni metodom koprecipitacije bili su stabilni, a oslobađanje silimarina iz njih bilo je 2,5 bolje u odnosu na čisti lijek

IJPER Jan-Mar

The purpose of present study was to develop once a day sustained release enteric coated tablet of Fluoxetine HCl by direct compression method. Design was prepared for nine batch using fenugreek mucilage at 40%, 50% and 60% concentration ; HPMC at 10%, 15% and 20%; Compritol ATO 888 at 10%, 15% and 20% and ethyl cellulose at 2%, 3% and 4% concentration. Fenugreek mucilage was extracted from dried ripe seeds of Trigonella foenum-graecum (Fabaceae). Cellulose acetate phthalate was used as enteric coating agent. The tablets were characterized for weight variation, crushing strength, friability, drug content and in vitro drug release study. All the formulations were complied with standard specifications. The Drug excipients compatibility study was performed by DSC and IR Spectroscopy and no incompatibility was found. The results of in vitro dissolution studies indicated that formulations X2, X5 and X8 released 7.03%, 7.03%, 4.75% of Fluoxetine respectively at the end of 2 hour and 98.17%, 78.12%, 65.45% of Fluoxetine respectively at the end of 24 hour. Increased release rate was observed in polymer in the order HPMC K 100M &gt; ethyl cellulose &gt; Compritol ATO 888. Formulation X2 (50% fenugreek mucilage and 15% HPMC K 100M) could extend drug release up to 24 hour and it exhibited satisfactory drug release within first 2 hours and total release pattern was very close to marketed product. The 0 mechanism of drug release was found to be diffusion coupled with erosion. Optimized formulation was found to be stable when exposed to 40 C/ 75 % of relative humidity for 3 month

Formulation and evaluation of clotrimazole transdermal spray

<p><i>Context</i>: Transdermal spray (TS) of clotrimazole (CTZ) was formulated to improve the drug transport through the skin up to 12 h to achieve the antifungal efficacy.</p> <p><i>Objective</i>: The aim of present study was to formulate and evaluate antifungal transdermal spray to improve the permeation of clotrimazole across the skin and to decrease the dosing frequency in fungal infection.</p> <p><i>Materials and methods</i>: Different ratios of ethanol and acetone and various grades of eudragit and ethyl cellulose were evaluated according to six criteria: viscosity, drying time, stickiness, appearance and integrity on skin and water washability. Propylene glycol (PG) and polyethylene glycol 400 (PEG 400) were used in the study as plasticizer and solubilizer. The TS was evaluated for <i>in vitro</i> drug release, spray angle, spray pattern, average weight per dose, pH, drug content, evaporation time, leak test and antifungal efficacy study.</p> <p><i>Results and discussion</i>: Eudragit E100 and blend of ethanol and acetone (80:20) satisfied the desired criteria. The selection of optimized batch was based on the results of <i>in vitro</i> drug release, spray pattern and spray angle. The optimized batch showed the spray angle <85° and uniform spray pattern. The formulation containing PG showed higher drug release than PEG 400. The inclusion of eutectic mixture consisting of camphor and menthol (1:1) showed improved drug transport through the rat skin and larger mean zone of inhibition indicating the improved antifungal efficacy.</p> <p><i>Conclusion</i>: The TS of CTZ can be an innovative and promising approach for the topical administration in the fungal diseases.</p

SIMULTANEOUS DETERMINATION OF MOXIFLOXACIN HYDROCHLORIDE AND DIFLUPREDNATE BY RATIO DERIVATIVE SPECTROPHOTOMETRY

Objective: Ratio derivative spectrophotometric method has been developed for the simultaneous determination of Moxifloxacin HCl (MH) and Difluprednate (DIFLU) in Phosphate Buffer pH 7.4. Methods: In this method, the overlapping spectra of MH and DIFLU were well resolved by making use of the first-derivative of the ratios of their direct absorption spectra. The derivative ratio absorbances of MH and DIFLU were measured at λmax 325.8 and λmax 238.0 nm, respectively for their quantification. MH and DIFLU were determined in the concentration range of 2-10 μg/ml and 4-20 μg/ml respectively. Results: The method was validated as per the ICH guideline and accuracy, precision are found to be within the acceptable limit. The limits of detection and quantitation were found to be 0.1144 and 0.3466 μg/ml, respectively for MH and 0.0311 and 0.094 μg/ml, respectively for DIFLU. Conclusion: The proposed ratio first derivative spectrophotometric method is novel, rapid, simple, sensitive, accurate, precise and does not require separation of MH and DIFLU hence successfully applied for simultaneous estimation of MH and DIFLU in marketed eye drops (liquid dosage form). Â&nbsp

Role of stabilizing agents in the formation of stable silver nanoparticles in aqueous solution: Characterization and stability study

<p>The stability of silver nanoparticles is controlled mainly by two major factors, namely, aggregation and oxidation. In the present study, silver nanoparticles were synthesized by using different series of reducing agents like a strong reducing agent (sodium borohydride), a mild reducing agent (tri-sodium citrate), and a weak reducing agent (glucose) with different capping agents, namely, polyvinyl pyrrolidone (PVP K 30), starch, and sodium carboxyl methyl cellulose (NaCMC). The synthesized silver nanoparticles were characterized by UV-Visible absorption spectroscopy, dynamic light scattering (DLS), atomic force microscopy (AFM), and anti-microbial activity. The particle size of silver nanoparticles varies in the following order: sodium borohydride < tri-sodium citrate < glucose. Combination of sodium borohydride–polyvinyl pyrrolidone and tri-sodium citrate-polyvinyl pyrrolidone yields stable silver nanoparticles compared to other combinations of reducing agents and capping agents. The stability results confirmed that a refrigerated condition (8°C) was more suitable for storage of silver nanoparticles. Anti-microbial activity of silver nanoparticles synthesized in a sodium borohydride–polyvinyl pyrrolidone mixture shows a larger zone of inhibition compared to other silver nanoparticles. Anti-microbial results confirmed that the anti-microbial activity is better with smaller particle size. The size and stability of silver nanoparticles in the presence of different combinations of stabilizing and capping agents are reported.</p