- Developing a Stable Aqueous Enteric Coating Formulation with Hydroxypropyl methylcellulose acetate succinate (HPMCAS-MF) and Colloidal Silicon Dioxide as Anti-tacking Agent. [Journal Article]
- IJInt J Pharm 2018 Feb 16
- The purpose of this study was to use statistical design of experiments to develop a stable aqueous enteric coating formulation containing stabilizing excipients, such as polyethylene glycol that can ...
The purpose of this study was to use statistical design of experiments to develop a stable aqueous enteric coating formulation containing stabilizing excipients, such as polyethylene glycol that can minimize hydroxypropyl methylcellulose acetate succinate aggregation and minimize spray-nozzle clogging at elevated processing temperatures. The mechanisms of stabilization (i.e. charge stabilization and molecular interactions) were studied by performing zeta potential and FTIR studies. Electrostatic stabilization by sodium lauryl sulfate and hydrogen bonding by polyethylene glycol provided dispersion stability and yielded a stable aqueous coating formulation that prevented spray-nozzle clogging. An enteric coated tablet with better gastric resistance was obtained by incorporating fumed silica (Aerosil®R972) as the anti-tacking agent instead of talc. Dissolution testing on the riboflavin enteric coated tablets showed a good enteric release profile without releasing riboflavin in 0.1 N HCl, and completely disintegrating within 10 min in phosphate buffer (pH 6.8).
- Women with hereditary breast cancer predispositions should avoid using their smartphones, tablets, and laptops at night. [Editorial]
- IJIran J Basic Med Sci 2018; 21(2):112-115
- Breast cancer is the most common malignancy among women, both in the developed and developing countries. Women with mutations in the BRCA1 and BRCA2 genes have an increased risk of breast and ovarian...
Breast cancer is the most common malignancy among women, both in the developed and developing countries. Women with mutations in the BRCA1 and BRCA2 genes have an increased risk of breast and ovarian cancers. Recent studies show that short-wavelength visible light disturb the secretion of melatonin and causes circadian rhythm disruption. We have previously studied the health effects of exposure to different levels of radiofrequency electromagnetic fields (RF-EMFs) such as mobile phones, mobile base stations, mobile phone jammers, laptop computers, and radars. Moreover, over the past several years, we investigated the health effects of exposure to the short wavelength visible light in the blue region emitted from digital screens. The reduction of melatonin secretion after exposure to blue light emitted from smartphone's screen has been reported to be associated with the negative impact of smartphone use at night on sleep. We have shown that both the blue light and RF-EMFs generated by mobile phones are linked to the disruption of the circadian rhythm in people who use their phones at night. Therefore, if women with hereditary breast cancer predispositions use their smartphones, tablets and laptops at night, disrupted circadian rhythms (suppression of melatonin caused by exposure to blue light emitted from the digital screens), amplifies the risk of breast cancer. It can be concluded that women who carry mutated BRCA1 or BRCA2, or women with family history of breast cancer should avoid using their smartphones, tablets and laptops at night. Using sunglasses with amber lenses, or smartphone applications which decrease the users' exposure to blue light before sleep, at least to some extent, can decrease the risk of circadian rhythm disruption and breast cancer.
- Impact of a Universal Medication Schedule on rationalising and understanding of medication; a randomised controlled trial. [Journal Article]
- RSRes Social Adm Pharm 2018 Feb 10
- CONCLUSIONS: A UMS approach may improve patients understanding and use of their medicines.
- Internet pseudoscience: Testing opioid containing formulations with tampering potential. [Journal Article]
- JPJ Pharm Biomed Anal 2018 Feb 10; 153:16-21
- Drug tampering practices, with the aim to increase availability of drug delivery and/or enhance drug effects, are accessible on Internet and are practiced by some portion of recreational drug users. ...
Drug tampering practices, with the aim to increase availability of drug delivery and/or enhance drug effects, are accessible on Internet and are practiced by some portion of recreational drug users. Not rarely, recreational misuse may result in toxic and even fatal results. The aim of the present study was to assess the tampering risk of medicaments containing different formulations of an opioid in combination with paracetamol or dexketoprofen, following the procedures reported in dedicated forums on the web. Tablets and suppositories containing codeine, tramadol and oxycodone were extracted following the reported "Cold water extraction"; dextromethorphan was extracted from cough syrup following the procedure reported as "Acid/base extraction" and fentanyl was extracted from transdermal patches according the procedure reported in Internet. The tampered products and opportunely prepared calibrators in water were analysed by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The separation of the analytes was carried on Agilent ZORBAX Eclipse Plus C18 (RRHT 2.1 mm × 50 mm, 1.8 μm) by the gradient elution of 0.01% formic acid in water and 0.01% formic acid in methanol. Acquisition was by MRM mode considering at least two transitions for compound. Declared recoveries for these home-made extractions claimed to exceed 99% for the opioid and to complete remove paracetamol, often associated to liver toxicity and thus to obtain a "safer" preparation. In this study, the authors demonstrated that rarely the recoveries for the opioid reached 90% and that up to 60% of the paracetamol amount remained in solution. Thus, high risks for health remained both for the potential lethality of the opioid content, but also for the sub-lethal chronic use of these mixtures, which contained still uncontrolled, ignored, but often important amounts of paracetamol.
- Fabricating 3D printed orally disintegrating printlets using selective laser sintering. [Journal Article]
- IJInt J Pharm 2018 Feb 14
- Selective laser sintering (SLS) is a three-dimensional printing (3DP) technology employed to manufacture plastic, metallic or ceramic objects. The aim of this study was to demonstrate the feasibility...
Selective laser sintering (SLS) is a three-dimensional printing (3DP) technology employed to manufacture plastic, metallic or ceramic objects. The aim of this study was to demonstrate the feasibility of SLS to fabricating novel solid dosage forms with accelerated drug release properties, and with a view to create orally disintegrating formulations. Two polymers (hydroxypropyl methylcellulose (HPMC E5) and vinylpyrrolidone-vinyl acetate copolymer (Kollidon®VA 64)) were separately mixed with 5% paracetamol (used as a model drug) and 3% Candurin®gold sheen colorant; the powder mixes were subjected to SLS printing resulting in the manufacture of printlets (3DP tablets). Modulating the SLS printing parameters altered the release characteristics of the printlets, with faster laser scanning speeds accelerating drug release from the HPMC formulations. The same trend was observed for the Kollidon®based printlets. At a laser scanning speed of 300 mm/s, the Kollidon®printlets exhibited orally disintegrating characteristics by completely dispersing in less than 4 seconds in a small volume of water. X-ray micro-CT analysis of these printlets indicated a reduction in their density and an increase in open porosity, therefore, confirming the unique disintegration behaviour of these formulations. The work reported here is the first to demonstrate the feasibility of SLS 3DP to fabricate printlets with accelerated drug release and orally disintegrating properties. This investigation has confirmed that SLS is amenable to the pharmaceutical research of modern medicine manufacture.
- Effects of para-methoxyamphetamine (PMA) on agonistic encounters between male mice. [Journal Article]
- PBPharmacol Biochem Behav 2018 Feb 14
- Para-methoxyamphetamine (PMA) is a synthetic drug chemically similar to the recreational drug 3,4-methylenedioxy-methamphetamine (MDMA or "ecstasy") and often replaces MDMA in tablets that show an "e...
Para-methoxyamphetamine (PMA) is a synthetic drug chemically similar to the recreational drug 3,4-methylenedioxy-methamphetamine (MDMA or "ecstasy") and often replaces MDMA in tablets that show an "ecstasy" logo. PMA displays a higher toxic potential than MDMA, but the behavioral profile of PMA has been scarcely studied in animal models. Here we evaluated the effects of PMA (2, 4, 8, and 12 mg/kg, i.p.) on agonist encounters between male mice using an ethopharmacological approach, the isolation-induced aggression model. Likewise, since PMA and MDMA share common mechanisms of action, we compared the behavioral profile of PMA with that induced by MDMA (8 mg/kg, i.p.) which behavioral effects in this model are well characterized. Individually housed mice were exposed to anosmic standard opponents 30 min after drug administration. The encounters were videotaped and evaluated using an ethologically based analysis. PMA (all doses) significantly reduced offensive behaviors (threat and attack), however, a detailed behavioral analysis suggests that the observed antiaggressive effect seems to be unspecific, showing a complex dose-dependent behavioral profile. Thus, antiaggresive actions observed after the administration of the lowest dose were accompanied by increases in social investigation, avoidance/flee behaviors and non-social explorations, together with a reduction of digging behavior. This pattern reflects both approach-contact behaviors and avoidance-flee behaviors. From 4 mg/kg to 12 mg/kg, the increase in social investigation previously observed disappears, and there is a slight increase in immobility, together with a different behavioral pattern that suggests anxiogenic effects of PMA, similar to those reported after the administration of MDMA. The higher doses of PMA exhibit a behavioral profile very similar to that observed in animals treated with MDMA, with the exception of the immobility produced by PMA. These findings show for the first time the non-specific antiaggressive profile of PMA in the model of aggression induced by isolation in male mice.
- Evaluation of the safety, tolerability, and efficacy of pimavanserin versus placebo in patients with Alzheimer's disease psychosis: a phase 2, randomised, placebo-controlled, double-blind study. [Journal Article]
- LNLancet Neurol 2018; 17(3):213-222
- CONCLUSIONS: Pimavanserin showed efficacy in patients with Alzheimer's disease psychosis at the primary endpoint (week 6) with an acceptable tolerability profile and without negative effect on cognition. Further follow-up to week 12 did not show significant advantage for pimavanserin versus placebo.
- Proton Pump Inhibitors and Chronic Kidney Disease: Is It Related to the Accumulation of Toxic Breakdown Products Spontaneously Formed in the Enteric-Protected Tablets? [Letter]
- GGastroenterology 2018 Feb 13
- In Vitro Screening of the Antibacterial and Anti-Candida Properties of Crushed Nonantimicrobial Drugs Frequently Prescribed in Nursing Homes. [Journal Article]
- RGRes Gerontol Nurs 2018 Feb 13; :1-9
- Frail older adults often experience swallowing disorders, prompting nursing staff to crush tablets, open capsules, and mix drugs into their meals or gelled water. However, crushing drugs can lead to ...
Frail older adults often experience swallowing disorders, prompting nursing staff to crush tablets, open capsules, and mix drugs into their meals or gelled water. However, crushing drugs can lead to pharmacological and gustatory problems. As crushed drugs can stay in prolonged contact with oral microbial biofilm, the current study aimed to investigate their antimicrobial properties. Crushed drugs were diluted in 1 mL of isotonic water and assayed in vitro for: (a) growth inhibition of five bacterial strains and Candida albicans by the diffusion method; (b) inhibition of Streptococcus salivarius and C. albicans biofilm formation; and (c) elimination of a preformed biofilm of S. salivarius and C. albicans after 5-minute contact. Eight of 29 crushed drugs inhibited bacterial and/or fungal growth on agar plates. Twenty-eight of 29 crushed drugs reduced the total biomass when incubated with S. salivarius, and 28 of 29 crushed drugs inhibited C. albicans biofilm formation. Preformed biomass was reduced by ≥25% by seven of 29 drugs. Crushed drugs may unbalance oral ecosystems and contribute to oral inflammation. [Res Gerontol Nurs. 20xx; xx(x):xx-xx.].
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- Modified release paracetamol overdose: a prospective observational study (ATOM-3). [Journal Article]
- CTClin Toxicol (Phila) 2018 Feb 16; :1-10
- CONCLUSIONS: Drug regulatory authorities are considering restrictions on MR paracetamol preparations. Following an acute MR paracetamol overdose, this study found that many patients had a persistently elevated paracetamol concentrations, many required prolonged treatment and some developed liver injury despite early acetylcysteine treatment. Furthermore, activated charcoal and increased acetylcysteine did not appear to significantly alter the risk of liver injury. Hence, research into better treatment strategies is required.