Disintegration and Dissolution Studies of Plain and Soluble Brands of Aspirin Tablets Embedded in Food Bolus

Background: The practice of embedding solid drugs such as tablets and capsules in food bolus is very common in some parts of Africa especially Nigeria. The reasons for this practice range from an attempt to alleviate the side effect of gastric irritation to masking the unpleasant taste and odour of the drugs.The effects of concomitant administration of food on the disintegration, dissolution and bioavailability of orally administered drugs are well documented. However, information on orally administered solid drugs embedded in food bolus is very scarce.Objective: This study investigated disintegration and dissolution profiles of plain and soluble brands of aspirin tablets embedded in food bolus.Methodology: Disintegration and dissolution tests were carried out on two different brands of commercial, uncoated, immediate release (IR) aspirin tablets (300 mg) using Erweka disintegration test apparatus (GMB, Germany) and USP dissolution apparatus 2 respectively. The two different brands were coded as P (plain aspirin tablet) and S (soluble aspirin tablet). Twenty tablets from P and S brands were randomly selected and embedded in 3 g of freshly prepared food bolus made from gelatinized cassava flour (commonly called “eba”) and labelled PB (plain aspirin tablet embedded in food bolus) and SB (soluble aspirin tablet embedded in food bolus). Disintegration test and dissolution test were equally conducted on PB and SB and compared with P and S.Results: The results indicated that both P and S passed the disintegration test for uncoated tablets, while PB and SB failed the test. Moreover, P, S and SB passed the in vitro dissolution test by releasing more than 80 % of the drug in 30 minutes, while PB failed the test. Embedding the tablets in food bolus significantly prolonged the disintegration time of SB and PB and also significantly affected the dissolution profile and kinetic of drug release from PB but had insignificant effect on SB. ANOVA for the dissolution parameters generated for all the samples showed that the dissolution profile of S was significantly higher (P < 0.05) than the rest. There was no significant difference (P > 0.05) between the dissolution data of SB and P while the dissolution profile of PB was significantly lower (P < 0.05) than that of SB and P.Conclusion: Disintegration and dissolution of plain brand of aspirin may be significantly affected if embedded in food bolus. This may not be so for soluble brand of aspirin.Keywords: Disintegration, Dissolution, Plain and Soluble, Aspirin tablets, Food Bolu

Gene-related prevalence of metabolically healthy obesity in different racio-ethnic groups

The metabolically healthy obesity (MHO) phenotype is partly influenced by race/ethnicity and genetic factors being relatively more prevalent in some groups compared to others. This review examines current evidence on the prevalence of MHO amongst children, adolescents and adults of different racio-ethnic groups; and explores gene variants and single nucleotide polymorphisms (SNPs) that may confer cardioprotection in some racio-ethnic groups compared to others. Literature search of articles published in English was conducted using PubMed, Medline and Google scholar databases, with search terms related to the prevalence of metabolically healthy obesity as well as genetic variants that decrease or increase the risk of metabolic syndrome (MetS). MHO prevalence differed across racio-ethnic groups and gene variants that confer cardioprotection were higher in some racio-ethnic groups compared to others. Lower prevalence of MHO across all ages was particularly reported in the Middle East, while high prevalence was reported in Africans, Americans and some Asian adult population. Excluding environmental and other risk factors, we observed that Caucasians were carriers of gene variants that confer protection against cardiometabolic diseases, whilst Asians showed high frequency of gene variants that increase susceptibility to MetS. A robust understanding of the role of these gene variants, their frequency distribution and racio-ethnic variations may facilitate conceptualisation of appropriate genome wide association studies (GWAS) to determine significant associations between various genetic factors and observed phenotype or disease. This will guide policy formulation and serve as a useful tool in pharmacogenomics and precision medicine. Keywords: Obesity, metabolically healthy obesity, single nucleotide polymorphism, ethnicity, race, metabolic syndrome, gene variant

Microbial dysbiosis-induced obesity: role of gut microbiota in homoeostasis of energy metabolism

The global obesity epidemic has necessitated the search for better intervention strategies including the exploitation of the health benefits of some gut microbiota and their metabolic products. Therefore, we examined the gut microbial composition and mechanisms of interaction with the host in relation to homoeostatic energy metabolism and pathophysiology of dysbiosis-induced metabolic inflammation and obesity. We also discussed the eubiotic, health-promoting effects of probiotics and prebiotics as well as epigenetic modifications associated with gut microbial dysbiosis and risk of obesity. High-fat/carbohydrate diet programmes the gut microbiota to one predominated by Firmicutes (Clostridium), Prevotella and Methanobrevibacter but deficient in beneficial genera/species such as Bacteroides, Bifidobacterium, Lactobacillus and Akkermansia. Altered gut microbiota is associated with decreased expression of SCFA that maintain intestinal epithelial barrier integrity, reduce bacterial translocation and inflammation and increase expression of hunger-suppressing hormones. Reduced amounts of beneficial micro-organisms also inhibit fasting-induced adipocyte factor expression leading to dyslipidaemia. A low-grade chronic inflammation (metabolic endotoxaemia) ensues which culminates in obesity and its co-morbidities. The synergy of high-fat diet and dysbiotic gut microbiota initiates a recipe that epigenetically programmes the host for increased adiposity and poor glycaemic control. Interestingly, these obesogenic mechanistic pathways that are transmittable from one generation to another can be modulated through the administration of probiotics, prebiotics and synbiotics. Though the influence of gut microbiota on the risk of obesity and several intervention strategies have been extensively demonstrated in animal models, application in humans still requires further robust investigation