Diclofenac salts, II. Solid dispersions in PEG6000 and Gelucire 50/13.
A number of systems were prepared at five compositions (5, 10, 20, 30 and 40% w/w) of diclofenac/N-(2-hydroxyethyl) pyrrolidine salt and acidic diclofenac in PEG6000 and Gelucire 50/13, as physical mixtures and as solid dispersions. Powder X-ray diffractograms for the systems examined show shifted and normal peaks, suggesting that the drug is present inside the samples in different physical states. Differential scanning calorimetry does not offer important information, since drug solubility into the carriers increases with temperature and thermograms show only the melting point peak of the carriers. Hot-stage microscopy examination explains that, in high concentration samples, the drug is present either dissolved into the carriers, or precipitated as microcrystals, or undissolved crystals of larger size. Gelucire 50/13 allows the formation of larger crystals than PEG, using both the chemical forms of the drug. The release percentage of the drug from PEG6000/acidic diclofenac reaches 50% after few minutes in the most favourable case and appears to be dependent on the composition of the samples: the more diclofenac is present as dissolved in the pre-treated samples, the higher is the release. The optimum composition was found in the range of 5-10% w/w.
Fini
Adamo
A
Istituto di Scienze Chimiche, Università di Bologna, Bologna, Italy. adamo.fini@unibo.it
Moyano
José R
JR
Ginés
Juan M
JM
Perez-Martinez
José I
JI
Rabasco
Antonio M
AM
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004008:Diclofenac / Q000008:administration & dosage* / Q000737:chemistry*; D004655:Emulsions; D005079:Excipients; D005223:Fats; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009821:Oils; D011092:Polyethylene Glycols; D012995:Solubility; D014961:X-Ray Diffraction
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D005079:Excipients; D005223:Fats; D009821:Oils; C071184:Gelucire 50-13; D004008:Diclofenac; D011092:Polyethylene Glycols