Ameliorating Insulin Signalling Pathway by Phytotherapy
Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa in Ethnopharmacology of Wild Plants, 2021
Subramania et al. (2008) had immense passion to discover alternative medicine for type 2 diabetes. During the experiment, the research team used ethanolic extract for both in vitro and in vivo studies. The extract showed appreciable α-glucosidase inhibitory effect in a concentration-dependent manner (IC50 17.2 ± 0.15 mg/mL) and a weak α-amylase inhibitory activity (IC50 50.9 ± 0.17 mg/mL). The in vivo studies demonstrated that A. paniculata extracts significantly (P < 0.05) reduced peak blood glucose and area under curve in diabetic rats when challenged with oral administration of starch and sucrose. Hence, α-glucosidase inhibition may be one of the mechanisms for the extract to exert anti-diabetic activity and indicates that the extract can be considered as a potential candidate. Erindyah et al. (2013) made an effervescent tablet containing the solution of A. paniculata and E. uniflora and tolbutamide to justify hypoglycemic effect. On the treatment of effervescent solution and tolbutamide (a prescribed medicine) to the glucose loaded rats, the blood glucose level showed significant differences (p ≤ 0.05), while comparing with the negative control or placebo group. The solution of effervescent tablets decreased blood glucose levels by 13.1% than the negative control (solution of sodium CMC 0.5%). Decreasing blood glucose level of the test solution compared to the placebo by 16.57% proved that extracts contain potential anti-diabetic ingredients.
Effervescent Granulation
Dilip M. Parikh in Handbook of Pharmaceutical Granulation Technology, 2021
The dry blending of powders would be the ideal process for effervescent tablet manufacturing, but it is limited to ingredients with proper compressibility that are able to ensure a homogeneous mixture with no risk of segregation. It is recommended when the active ingredient cannot be wet granulated because it is unstable in the presence of water or contains some water of crystallization that could be difficult to manage during granulation. It is a quick and simple way of manufacturing in bin tumblers, ribbon, twin-cone, and V-type blenders and suitable for continuous mixers but requires the right selection of raw materials, possibly already available in granular form.
Oral potassium overdose: a case series
Published in Clinical Toxicology, 2021
Arushi Madan, Christopher Morris, Anna Goggin, Katherine Z. Isoardi
The two formulations of oral potassium available in Australia are an immediate-release effervescent tablet and a sustained-release tablet, both of which are prescription-only Schedule 4 drugs [1]. The effervescent tablet consists of a combination of potassium chloride, potassium bicarbonate and potassium carbonate providing 548 mg potassium and 283 mg of chloride (14 mmol potassium, 8 mmol chloride) [2]. The sustained-release tablet formulation consists of 600 mg potassium chloride crystals (8 mmol potassium, 8 mmol chloride) coated with insoluble wax and pressed into a wax matrix, from which the potassium chloride slowly diffuses [3]. In therapeutic use, peak potassium concentration is reached around two and five hours after ingestion of immediate and sustained-release preparations respectively and both formulations have >90% bioavailability [4]. With larger sustained-release ingestions, the insoluble wax matrix may contribute to forming pharmacobezoars, which can cause delayed or erratic absorption and/or local toxicity with gastrointestinal perforation or obstruction from increased contact of the irritant potassium [5]. While hyperkalaemia increases gastrointestinal motility, potential co-ingestion with agents delaying motility, such as anticholinergic drugs, may further increase risk of local toxicity. Crushing or chewing tablets may increase early systemic absorption by impairing the slow-release mechanism [5]. These factors together can result in significant variability in peak concentration, time-to-peak concentration, potential physiological adaptation, and associated onset and duration of clinical effects.
Development and anti-Candida evaluation of the vaginal delivery system of amphotericin B nanosuspension-loaded thermogel
Published in Journal of Drug Targeting, 2018
Tianyuan Ci, Luo Yuan, Xiaoyan Bao, Yuting Hou, Hao Wu, Haifeng Sun, Dinglingge Cao, Xue Ke
AmB NPs/thermogel solution was administrated into the vagina of mice via a pipette. The dose of AmB was referred to that of the effervescent tablet. In clinic, the suggested AmB dose of effervescent tablet was 10 mg/day (0.2 mg/kg) for human. And the administration dose of mouse was calculated by the equation of Danimal = k × Dhuman, in which Dhuman means the drug dose of human of 0.2 mg/kg, k means the conversion coefficient between human and mouse of 12.3, according to FDA Guidance for Industry-Estimating the Maximum Safe Starting Dose in Initial Clinical Trials for Therapeutics in Adult Healthy Volunteers. Thus, the three dosage of AmB NPs/thermogel in this experiment was set as 5, 2.5 and 1.25 mg/kg. Normal Saline and AmB effervescent tablet (2.5 mg/kg) were administrated as negative and positive control, respectively. And for the commercial tablet group, the tablets (bought in drugstore and used for humans, denoted as containing 5 mg AmB per tablet) was first grinded to powders and then administrated via a very small experimental spoon to the mice vagina according to the drug dose. The drugs of different formulations were administrated for 5 consecutive days, denoted as Day 1 to Day 5.
A randomised trial to compare 200 mg micronised progesterone effervescent vaginal tablet daily with 250 mg intramuscular 17 alpha hydroxy progesterone caproate weekly for prevention of recurrent preterm birth
Published in Journal of Obstetrics and Gynaecology, 2018
Shruti Shambhavi, Rashmi Bagga, Pallavi Bansal, Jasvinder Kalra, Praveen Kumar
The strengths of the study are that it was randomised and all women had ≥ one prior singleton PTB (>16 to <37 weeks), making it a homogenous group. Modifiable risk factors for PTB (infections) were treated so that they did not interfere with the results and compliance to medication was ascertained. The vaginal progesterone effervescent tablet which was used has been reported to have an efficient mechanism for mucosal absorption (Levy et al. 1999; Paulson et al. 2014). The lack of a control group may be considered as a limitation, but it was deemed unethical to withhold a medication which is the standard of care in such women. A small sample size proved to be limiting in drawing meaningful inferences, especially in spontaneous PTB rates at <34 and <28 weeks. The lack of blinding during the treatment was also a limitation.
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