Ketan Patel

Increase in anal resting pressure (ARP) is considered as the primary cause of chronic anal fissure (CAF). Reduction in ARP is the primary objective in treatment of CAF. Topical diltiazem is considered as first-line treatment option in CAF as surgical treatment may be associated with several post operative complications including permanent incontinence in some cases. Few studies have reported that lidocaine alone is inferior to anal dilators for pain relief in CAF which suggest that relief of internal anal sphincter is required for effective symptomatic management. The aim of this study was to evaluate whether combined treatment with diltiazem and lidocaine has any significant advantage over diltiazem monotherapy in patients with CAF. To evaluate this, 150 patients were enrolled and randomized to either treatment group. ARP, pain intensity and adverse events were recorded at various time points over 20 days study period. Fall in the mean ARP from baseline was comparable in both the study groups. However, significantly greater fall in pain intensity from baseline was observed with combined treatment with diltiazem and lidocaine, which can be attributed to the additional local anesthetic effects of lidocaine with combination treatment. No patient had any systemic or local adverse effects. Global assessment by patients and investigator was also favourable for combination treatment. We conclude that combined treatment with topical diltiazem and lidocaine is safe and effective option for pharmacological treatment of CAF, and addition of lidocaine to diltiazem significantly increases the pain relief achieved with diltiazem alone.

Solid dispersion of Oxcarbazepine (OXC) was prepared by hot melt extrusion of OXC with hydrophilic polymer. The main objective was to explore the potential of Hot Melt Extrusion technique (HME) as an industrial scalable green technique for the preparation of solid dispersion and therefore enhancement of dissolution of poorly soluble drug. Polymer for extrusion was selected on the basis of solubility parameters and glass transition (Tg). OXC solid dispersion was prepared using Kollidon VA 64 and Soluplus as hydrophilic carrier. OXC and polymer was mixed in different ratio and extrudates were evaluated for appearance, DSC, PXRD, flow property and dissolution characteristics. DSC and PXRD studies revealed the significant reduction in crystallinity of OXC. OXC-kollidon VA 64 extrudates have good flow property having angle of repose 29° and carr’s index 11.2 and good compressibility with hardness 5-6 kg/cm2. Particle size of extrudates exhibited significant effect on disintegration time and dissolution. OXC release was found to be complete within 45 min from tablets of OXC hot melt extrudates while plain OXC showed just 39 % release. Solid dispersion of OXC was successfully developed using HME technology followed by formulating it into directly compressible tablets.