Anti-inflammatory and wound healing effects of an essential oils-based bioadhesive gel after oral mucosa biopsies: preliminary results.

Post-operative management of patients receiving oral biopsy includes the control of edema, pain, infection, and re-epithelization at the surgical site. This clinical study investigates the topical use of a bioadhesive gel, containing essential oils, to promote wound healing and prevent post-operative pain and infection, avoiding the need for surgical suture and chlorhexidine applications. Ten patients, who needed to receive oral biopsies (≤6 mm in diameter) for the diagnosis of mucosal oral lesions, were enrolled. The bioadhesive gel successfully controlled the post-surgical pain; at 1-week follow-up visit, no signs of infection nor side effects were reported and the surgical sites were completely healed. The bioadhesive gel resulted in a very promising agent for the post-operative management of oral biopsy site, without the need for surgical suture and chlorhexidine applications.

Structure and properties of domperidone and its succinate salt.

This paper describes the structure and properties of the drug domperidone and a novel 1:1 domperidone succinate salt. The new salt is characterized by means of thermal, spectroscopic, microscopic and powder diffraction measurements. The crystal structures of the salt and, for the first time, of pure domperidone have been determined by means of single-crystal X-ray diffraction. In both structures, the piperidine ring of domperidone adopts the expected chair conformation, and supramolecular centrosymmetric R2(2)(8) motifs are formed by N-H...O hydrogen bonds between chlorine-substituted oxobenzimidazolyl groups. Further N-H...O hydrogen bonds occur between non-substituted oxobenzimidazolyl groups and the resulting C(4) motifs originates hydrogen-bonded chains, extending along the crystallographic b axis. In the salt, a single N-H...O hydrogen bond forms between the protonated nitrogen of the piperidine ring and the carboxylic O atom of the succinate ion. Two alternative and mutually exclusive positions for the nonsubstituted oxobenzimidazolyl group have also been observed; this disorder makes the hydrogen-bonded chains originating from the bicyclic group polar. The dissolution behaviour of the salt in dosage form is compared with two reference commercial products. The salt shows an increased solubility, a characteristic that could be of great advantage from a pharmaceutical view point.

An experimental and theoretical investigation of loperamide hydrochloride-glutaric acid cocrystals.

Cocrystallization is a powerful method to improve the physicochemical properties of drugs. Loperamide hydrochloride is a topical analgesic for the gastrointestinal tract showing low and pH-dependent solubility; for this reason, an enhancement of its solubility or dissolution rate, particularly at the pH of the intestinal tract, could improve its local efficacy. Here we prepared cocrystals of this active principle with glutaric acid and so obtained a new crystalline solid representing a viable alternative to improve the physicochemical properties and thus the pharmaceutical behavior of the drug. Differential scanning calorimetry, X-ray powder diffraction, Fourier infrared spectroscopy, solid-state NMR, and scanning electron microscopy coupled to the energy-dispersive X-ray spectrometry were used to investigate the new solid-phase formation. DFT calculations at B3LYP/6-31G(d) level of theory, in the gas phase, including frequencies computation, provided a rationale for the interaction between loperamide hydrochloride and glutaric acid. The cocrystals showed improved water solubility in comparison with loperamide HCl, and the pharmaceutical formulation proposed was able to release the drug more rapidly in comparison with three reference commercial products when tested at neutral pH values.