Investigation on Dissolution Pattern and Mathematical Modeling of Drug Release of UDCA by Complextaion with b-Cyclodextrin-Choline Dichloride Coprecipitate

The objective of the present investigation was to study the effect of presence of choline dichloride (CDC) in β-cyclodextrin (β-CD) on in vitro dissolution of Ursodeoxycholic acid (UDCA) from molecular inclusion complexes. The molecular inclusion complexes of UDCA with β-CD coprecipitated with CDC were prepared using kneading method. In vitro dissolution of pure drug, physical mixtures and cyclodextrin inclusion complexes (UDCA-β-CD- CDC) were carried out. Molecular inclusion complexes of Ursodeoxycholic acid with coprecipitated β-CD showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0.1 N HCl, pH1.2 and phosphate buffer, pH 7.4. Inclusion complexes with 1:2M ratio showed maximum dissolution rate in comparison to other ratios. FT-IR spectroscopy and differential scanning calorimetry studies indicated no interaction between UDCA and β-CD-CDC in complexes in solid state. Dissolution enhancement was attributed to the formation of water soluble inclusion complexes with the precipitated form of β-CD. The in vitro release from all the formulations was best described by first order kinetics followed by Higuchi release model. In conclusion, dissolution of Ursodeoxycholic acid can be enhanced by using the β-CD-CDC coprecipitate as a host st molecolec

Dissolution behaviour of aceclofenac-PVP coprecipitates

Aim: The objective of the present investigation was to study the effect of PVP on in vitro dissolution of aceclofenac from coprecipitates. Materials and Methods: Aceclofenac coprecipitates (CP) with different drug loadings were prepared and in vitro dissolution studies of pure drug, physical mixtures and coprecipitates were carried out. Results: Coprecipitates of aceclofenac with PVP showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0.1 N HCl, pH1.2 and phosphate buffer, pH, 7.4. Coprecipitates in 1:2 ratio showed maximum dissolution rate in comparison to other ratios. Amorphous nature of the drug in coprecipitates was confirmed by scanning electron microscopy and a decrease in enthalpy of drug melting in coprecipitates compared to the pure drug. FT- IR spectroscopy and differential scanning calorimetry studies indicated no interaction between aceclofenac and PVP in coprecipitates in solid state. Dissolution enhancement was attributed to decreased crystallinity of the drug and to the wetting, eutectic formation and solubilizing effect of the carrier from the coprecipitates of aceclofenac. Conclusion: dissolution of aceclofenac can be enhanced by the use of hydrophilic carriers like PVP

Comparative Investigation on in vitro release of extemporaneously prepared norfloxacin semisolid formulations with marketed silver sulfadiazine 1% cream, USP using model independent approach

Objective In an attempt for better treatment of bacterial infections, various semisolid formulations containing 5% w/w of norfloxacin were prepared and evaluated for in vitro drug release and in vitro skin permeability using dialysis membrane and rat abdominal skin respectively. The in vitro diffusion and permeation profile of the prepared formulation was compared with marketed silver sulfadiazine cream 1%, USP using model independent approach. Methods Various semisolid formulations were prepared with different dermatological bases using standard procedures. In vitro diffusion and permeation studies were carried out using Keshary-Chein (KC) type diffusion cell using dialysis membrane and rat abdominal skin respectively. Results The f1 lower than 15 and f2 higher than 50 indicated similarities in the in vitro diffusion and permeation profiles of the extemporaneously prepared selected semisolid formulations and marketed silver sulfadiazine 1% cream, USP. Conclusion Amongst all the semisolid formulations prepared, carbopol gel base was found to be most suitable dermatological base for norfloxacin, the results obtained for in vitro diffusion, and in vitro skin permeation studies are comparable with that of marketed silver sulphadiazine 1% cream, USP

Dozirani pripravci aceklofenaka za topičku primjenu: In vitro i in vivo karakterizacija

Aceclofenac is a new generation non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties. It is available in the form of tablets of 100 mg. Importance of aceclofenac as a NSAID has inspired development of topical dosage forms. This mode of administration may help avoid typical side effects associated with oral administration of NSAIDs, which have led to its withdrawal. Furthermore, aceclofenac topical dosage forms can be used as a supplement to oral therapy for better treatment of conditions such as arthritis. Ointments, creams, and gels containing 1 % m/m aceclofenac have been prepared. They were tested for physical appearance, pH, spreadability, extrudability, drug content uniformity, in vitro diffusion and in vitro permeation. Gels prepared using Carbopol 940 (AF2, AF3) and macrogol bases (AF7) were selected after the analysis of the results. They were evaluated for acute skin irritancy, anti-inflammatory and analgesic effects using the carrageenan-induced thermal hyperalgesia and paw edema method. AF2 was shown to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation, compared to AF3 and AF7. Hence, AF2 may be suggested as an alternative to oral preparations.Aceklofenak je lijek nove generacije nesteroidnih protuupalnih lijekova sa izraženim protuupalnim i analgetskim djelovanjem. Dostupan je u obliku tableta od 100 mg. U ovom radu razvijeni su dozirani pripravci za topičku primjenu u svrhu smanjenja ili uklanjanja nuspojava povezanih s oralnom primjenom nesteroidnih protuupalnih lijekova. Ti pripravci mogu se upotrijebiti kao dodatak peroralnoj terapiji artritisa i srodnih bolesti. Opisana je priprava mazila, krema i gela s 1 % m/m aceklofenaka te njihova fizička svojstva, pH, mazivost, istiskivost, jednolikost sadržaja ljekovite tvari, difuzija i permeabilnost in vitro. Nakon analize rezultata za daljnja ispitivanja odabrani su gelovi pripravljeni na bazi Carbopola 940 (AF2, AF3) i makrogola (AF7). Ispitana je akutna iritacija kože, protuupalno i analgetsko djelovanje koristeći karagenom induciranu termičku hiperalgeziju i edem šape. Pripravak AF2 bio je značajno (p < 0,05) učinkovitiji u inhibiciji hiperalgezije s upalom nego pripravci AF3 i AF7. Stoga se AF2 može predložiti kao alternativa peroralnim pripravcima

Preparation, Characterization and In Vitro Evaluation of Aceclofenac Solid Dispersions

The objective of the present investigation was to study the effect of various water soluble carriers like urea, mannitol, PVP and PVP/VA-64 on in vitro dissolution of aceclofenac from solid dispersions. Aceclofenac binary solid dispersions (SD) with different drug loadings were prepared using the melting or fusion method. In vitro dissolution of pure drug, physical mixtures and solid dispersions were carried out. Solid dispersion of aceclofenac with all four carriers (urea, mannitol, PVP and PVP/VA-64) showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0.1 N HCl, pH1.2 and phosphate buffer, pH, 7.4. Solid dispersions containing PVP showed maximum dissolution rate in comparison to formulation containing urea, mannitol and PVP/VA-64. Amorphous nature of the drug in solid dispersion was confirmed by scanning electron microscopy and a decrease in enthalpy of drug melting in solid dispersion compared to the pure drug. FT-IR spectroscopy and differential scanning calorimetry studies indicated no interaction between aceclofenac and carriers in solid dispersions in solid state. Dissolution enhancement was attributed to decreased crystallinity of the drug and to the wetting, eutectic formation and solubilizing effect of the carrier from the solid dispersions of aceclofenac. In conclusion, dissolution of aceclofenac can be enhanced by the use of various hydrophilic carriers like urea, mannitol, PVP and PVP/VA-64

Role of microRNAs (miRNAs) in the pathophysiology of Diabetes mellitus

© 2017 EDIZIONI MINERVA MEDICA. Diabetes mellitus is becoming the critical problem among the entire world and it is difficult to understand the molecular mechanism representing the concept of diabetic pathology. Recently the knowledge of the involvement of genetics in type 2 diabetes mellitus (T2DM) susceptibility has sketched a great concentration towards the transcriptional activity of β cells within the pancreas. This disease becomes the leading cause of death, so it is necessary to study the molecular pathogenesis, phenotypes, and characteristics to design the therapeutic parameters. Here in this review role of miRNA is being illustrated as it plays a crucial role in the pathogenesis, progression, and fate of beta cells of pancreas regulating the insulin secretion. Here in this review, we try to include the effects and pathophysiology of various miRNA in diabetes mellitus and on the various sites of the human body