A Proposed Methodology for In Vitro Evaluation of Bitterness in Drug Solutions and In Vitro Drug Release Samples

Purpose

Ethical and safety concerns, paediatric taste panels and predictivity in early drug development for strategic decisions are some of the reasons for seeking in vitro methods of bitterness evaluation for drugs and drug products. In this study, taste panel studies and in vitro drug release studies have been performed, correlated to each other and proposed as an analytical tool for evaluation of bitterness.

Methods

Bitterness threshold and bitterness scores for different solutions of ondansetron hydrochloride (ONS) were estimated by taste panel studies. In vitro drug release studies on taste-masked drug product in pharmacopoeial apparatus and an in-house-developed apparatus were performed and correlated to drug release studies in oral cavity.

Results

Concentration of 22 μg/ml and below was perceived bitterless by all the volunteers of taste panel. A second-order polynomial equation (y?=?0.6206x ²???0.2011x???0.7796; correlation coefficient R ²?=?0.991) was derived as a relationship between bitterness score and log ONS concentration. Drug release in in-house-assembled apparatus and oral cavity were not statistically different (α?=?0.05) at both 60 and 120 s.

Conclusions

Bitterness threshold and bitterness scores are helpful in evaluation of bitterness in drug solutions and samples obtained from drug release studies.     

Generation of regulatory dendritic cells and CD4+Foxp3+ T cells by probiotics administration suppresses immune disorders

The beneficial effects of probiotics have been described in many diseases, but the mechanism by which they modulate the immune system is poorly understood. In this study, we identified a mixture of probiotics that up-regulates CD4⁺Foxp3⁺ regulatory T cells (Tregs). Administration of the probiotics mixture induced both T-cell and B-cell hyporesponsiveness and down-regulated T helper (Th) 1, Th2, and Th17 cytokines without apoptosis induction. It also induced generation of CD4⁺Foxp3⁺ Tregs from the CD4⁺CD25⁻ population and increased the suppressor activity of naturally occurring CD4⁺CD25⁺ Tregs. Conversion of T cells into Foxp3⁺ Tregs is directly mediated by regulatory dendritic cells (rDCs) that express high levels of IL-10, TGF-β, COX-2, and indoleamine 2,3-dioxygenase. Administration of probiotics had therapeutical effects in experimental inflammatory bowel disease, atopic dermatitis, and rheumatoid arthritis. The therapeutical effect of the probiotics is associated with enrichment of CD4⁺Foxp3⁺ Tregs in the inflamed regions. Collectively, the administration of probiotics that enhance the generation of rDCs and Tregs represents an applicable treatment of inflammatory immune disorders.     

Plantar fasciitis and impaired vision: A case report

We report a case of acute bilateral central serous chorioretinopathy in a patient who received a local injection of triamcinolone for the treatment of plantar fasciitis. Central serous chorioretinopathy is a serious, though rare, ocular complication of steroid treatment and it may occur even when the steroid is administered at a site as remote from the eye as the foot. This case report highlights the need for greater awareness of this complication amongst all medical personnel who prescribe steroids. It is advisable that patients, undergoing steroid treatment for any cause, be alerted to the risk of sudden visual impairment.     

Multilocular peritoneal inclusion cyst--a case report

Multilocular Peritoneal Inclusion Cyst (MPIC) is a rare mesothelial lesion. It is most commonly found in women of reproductive age group involving the abdominal and pelvic peritoneum. Previously, this lesion was often confused with cystic lymphangioma, but now its mesothelial origin has been confirmed. We report a case of a 26-year old female who underwent Caesarean section during which cysts which were multiloculated, thin-walled and filled with serous fluid, were incidentally discovered. Its histopathologic examination established the diagnosis