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Journal of Dental Anesthesia and Pain... Dec 2016Topical anesthetics act on the peripheral nerves and reduce the sensation of pain at the site of application. In dentistry, they are used to control local pain caused by... (Review)
Review
Topical anesthetics act on the peripheral nerves and reduce the sensation of pain at the site of application. In dentistry, they are used to control local pain caused by needling, placement of orthodontic bands, the vomiting reflex, oral mucositis, and rubber-dam clamp placement. Traditional topical anesthetics contain lidocaine or benzocaine as active ingredients and are used in the form of solutions, creams, gels, and sprays. Eutectic mixtures of local anesthesia cream, a mixture of various topical anesthetics, has been reported to be more potent than other anesthetics. Recently, new products with modified ingredients and application methods have been introduced into the market. These products may be used for mild pain during periodontal treatment, such as scaling. Dentists should be aware that topical anesthetics, although rare, might induce allergic reactions or side effects as a result of an overdose. Topical anesthetics are useful aids during dental treatment, as they reduce dental phobia, especially in children, by mitigating discomfort and pain.
PubMed: 28879311
DOI: 10.17245/jdapm.2016.16.4.237 -
Molecules (Basel, Switzerland) Jan 2017The influence of heating at a temperature of 50 °C and UV-irradiation of propolis drops and spray on their free radical scavenging activity was determined. The kinetics...
The influence of heating at a temperature of 50 °C and UV-irradiation of propolis drops and spray on their free radical scavenging activity was determined. The kinetics of interactions of the propolis samples with DPPH free radicals was analyzed. Interactions of propolis drops and propolis spray with free radicals were examined by electron paramagnetic resonance spectroscopy. A spectrometer generating microwaves of 9.3 GHz frequency was used. The EPR spectra of the model DPPH free radicals were compared with the EPR spectra of DPPH in contact with the tested propolis samples. The antioxidative activity of propolis drops and propolis spray decreased after heating at the temperature of 50 °C. A UV-irradiated sample of propolis drops more weakly scavenged free radicals than an untreated sample. The antioxidative activity of propolis spray increased after UV-irradiation. The sample of propolis drops heated at the temperature of 50 °C quenched free radicals faster than the unheated sample. UV-irradiation weakly changed the kinetics of propolis drops or spray interactions with free radicals. EPR analysis indicated that propolis drops and spray should not be stored at a temperature of 50 °C. Propolis drops should not be exposed to UV-irradiation.
Topics: Biphenyl Compounds; Electron Spin Resonance Spectroscopy; Free Radical Scavengers; Hot Temperature; Ophthalmic Solutions; Oral Sprays; Oxidation-Reduction; Picrates; Propolis; Ultraviolet Rays
PubMed: 28098798
DOI: 10.3390/molecules22010128 -
European Journal of Pharmaceutical... Nov 2023The oral delivery of biologics such as therapeutic proteins, peptides and oligonucleotides for the treatment of colon related diseases has been the focus of increasing... (Review)
Review
The oral delivery of biologics such as therapeutic proteins, peptides and oligonucleotides for the treatment of colon related diseases has been the focus of increasing attention over the last years. However, the major disadvantage of these macromolecules is their degradation propensity in liquid state which can lead to the undesirable and complete loss of function. Therefore, to increase the stability of the biologic and reduce their degradation propensity, formulation techniques such as solidification can be performed to obtain a stable solid dosage form for oral administration. Due to their fragility, stress exerted on the biologic during solidification has to be reduced with the incorporation of stabilizing excipients into the formulation. This review focuses on the state-of-the-art solidification techniques required to obtain a solid dosage form for the oral delivery of biologics to the colon and the use of suitable excipients for adequate stabilization upon solidification. The solidifying processes discussed within this review are spray drying, freeze drying, bead coating and also other techniques such as spray freeze drying, electro spraying, vacuum- and supercritical fluid drying. Further, the colon as site of absorption in both healthy and diseased state is critically reviewed and possible oral delivery systems for biologics are discussed.
Topics: Excipients; Desiccation; Freeze Drying; Biological Products; Colon
PubMed: 37429482
DOI: 10.1016/j.ejps.2023.106523 -
Clinical Oral Investigations Dec 2023The oral cavity constitutes an attractive organ for the local and systemic application of drug substances. Oromucosal tablets, gels, or sprays are examples of the... (Review)
Review
OBJECTIVES
The oral cavity constitutes an attractive organ for the local and systemic application of drug substances. Oromucosal tablets, gels, or sprays are examples of the formulations applied. Due to the elution through the saliva, the residence time of the formulation at the application site is relatively short. Medical devices placed in the oral cavity, with a reservoir for an active substance, play an important role in solving this problem.
MATERIALS AND METHODS
In this review, we discuss the devices described in the literature that are designed to be used in the oral cavity, highlighting the advantages, disadvantages, and clinical applications of each of them.
RESULTS
Among the intraoral medical devices, special types are personalized 3D-printed devices, iontophoretic devices, and microneedle patches.
CONCLUSION
We anticipate that with the development of 3D printing and new polymers, the technology of flexible and comfortable devices for prolonged drug delivery in the oral cavity will develop intensively.
CLINICAL RELEVANCE
The presented review is therefore a useful summary of the current technological state, when in fact none of the existing devices has been widely accepted clinically.
Topics: Drug Delivery Systems; Printing, Three-Dimensional; Tablets
PubMed: 37982874
DOI: 10.1007/s00784-023-05377-5 -
Pharmaceutics May 2022Ursodeoxycholate (UDCA) has low oral bioavailability and pH-dependent solubility and permeability. Thus, we developed a pH-modified extended-release formulation of UDCA...
Ursodeoxycholate (UDCA) has low oral bioavailability and pH-dependent solubility and permeability. Thus, we developed a pH-modified extended-release formulation of UDCA using NaCO as the alkalizing agent and hydroxypropyl methylcellulose (HPMC) as the release-modifying agent. The optimized pH-modified controlled-release UDCA formulation, with the UDCA:HPMC:NaCO ratio of 200:600:150 (//), was prepared using a spray-drying method. Then, the formulation's solubility, dissolution, and pharmacokinetic properties were characterized. In a pH-modified extended-release formulation of UDCA, the solubility of UDCA was increased to 8 mg/mL with a sustained dissolution for 12 h. Additionally, the spray-dried formulation exhibited amorphous states without molecular interaction among UDCA, NaCO, and HPMC. Moreover, the plasma UDCA concentration of the formulation maintained a higher UDCA concentration for up to 48 h than that of UDCA itself or the non-extended-release UDCA formulation. Consequently, the formulation significantly increased the AUC compared to UDCA or the non-extended-release UDCA formulation in rats. In conclusion, we have improved UDCA's solubility and dissolution profile by preparing a pH-modified extended-release formulation with the UDCA:HPMC:NaCO ratio of 200:600:150 (//), which effectively increased the oral bioavailability of UDCA by 251% in rats.
PubMed: 35631622
DOI: 10.3390/pharmaceutics14051037 -
Pharmaceutics Dec 2023Developing drugs that are highly selective to host tissues but are the least toxic remains one of the most difficult challenges in cancer treatment. Recent studies have...
Developing drugs that are highly selective to host tissues but are the least toxic remains one of the most difficult challenges in cancer treatment. Recent studies have shown that tumor cells from a variety of sources can express vitamin D3 receptors and that the response to vitamin D3 and its analogs is prone to growth arrest and cell death. However, conventional vitamin D3 drug formulations lack dose control and cannot target specific cells or tissues. The aim of this study was to prepare vitamin D3 nanospray for inhalation delivery route. This study evaluated the physical properties of the formulation (particle size distribution and biological stability), the total number of sprays per bottle, the spray volume per spray, and the loading variance of the spray. The optimized vitamin D3 spray formula is easy to spray, has fewer drips, and has a fast drying time. It can be stored for 3 months at 37 ± 2 °C temperature, 75 ± 5% relative humidity, and away from light, and can maintain biological stability. This study showed that compared with traditional nasal sprays, the spray has a larger fan angle (82.1 degrees) and beam width (104.88 mm), more symmetrical spray on both sides of the spray column, a faster coverage of the administration site, and a wider range, which is suitable for inhalation delivery routes.
PubMed: 38258036
DOI: 10.3390/pharmaceutics16010025 -
Minerva Anestesiologica Jan 2019Sore throat and hoarseness are common complications after surgery. Flurbiprofen spray has been successfully used for treatment of oral inflammations, but its effects on... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Sore throat and hoarseness are common complications after surgery. Flurbiprofen spray has been successfully used for treatment of oral inflammations, but its effects on postoperative sore throat and hoarseness are unknown. We conducted this study to evaluate the effectiveness of flurbiprofen spray on postoperative sore throat and hoarseness, by comparing it with benzydamine hydrochloride spray and placebo.
METHODS
One hundred fifty patients who were scheduled to undergo elective ear surgery were enrolled. Patients were randomized to three groups of 50 patients each; flurbiprofen oral spray, benzydamine hydrochloride oral spray and placebo spray groups. Patients received sprays just before intubation, and the incidence and severity of postoperative sore throat and hoarseness were evaluated by a blinded investigator at 0, 1, 6 and 24-hour post extubation. Patients were also questioned for possible side effects at all time points.
RESULTS
The sore throat severity scores were significantly lower in treatment groups when compared to placebo group at all time points (P=0.003/108). Similarly, the incidence of sore throat was significantly lower in both of the treatment groups (P=0.007/104). The incidence of hoarseness and hoarseness scores were significantly lower in treatment groups when compared to placebo group (P=0.006/105 and P=0.005/104, respectively). While none of the patients complained of any adverse effects in flurbiprofen group, only two patients in benzydamine hydrochloride group experienced numbness.
CONCLUSIONS
Both oral flurbiprofen and benzydamine hydrochloride sprays were found to be more effective than placebo in decreasing the incidence and severity of postoperative sore throat and hoarseness, with no adverse effects.
Topics: Adolescent; Adult; Aerosols; Anti-Inflammatory Agents, Non-Steroidal; Benzydamine; Double-Blind Method; Ear; Female; Flurbiprofen; Hoarseness; Humans; Incidence; Male; Middle Aged; Pharyngitis; Postoperative Complications; Prospective Studies; Young Adult
PubMed: 29756749
DOI: 10.23736/S0375-9393.18.12703-9 -
Life (Basel, Switzerland) May 2022Multiple sclerosis (MS) is known as an autoimmune disease that damages the neurons in the central nervous system. MS is characterized by its most common symptoms of... (Review)
Review
Multiple sclerosis (MS) is known as an autoimmune disease that damages the neurons in the central nervous system. MS is characterized by its most common symptoms of spasticity, muscle spasms, neuropathic pain, tremors, bladder dysfunction, dysarthria, and some intellectual problems, including memory disturbances. Several clinical studies have been conducted to investigate the effects of cannabis on the relief of these symptoms in MS patients. The efficacy of () in the management of MS outcomes such as spasticity, pain, tremors, ataxia, bladder functions, sleep, quality of life, and adverse effects were assessed in this review. Most clinical studies showed the positive effects of cannabinoids with their different routes of administration, such as oromucosal spray and oral form, in reducing most MS symptoms. The oromucosal spray Nabiximols demonstrated an improvement in reducing MS spasticity, pain, and quality of life with a tolerated adverse effect. Oral cannabinoids are significantly effective for treating MS pain and spasticity, while the other symptoms indicate slight improvement and the evidence is quite inconsistent. Oromucosal spray and oral cannabis are mainly used for treating patients with MS and have positive effects on treating the most common symptoms of MS, such as pain and spasticity, whereas the other MS symptoms indicated slight improvement, for which further studies are needed.
PubMed: 35629350
DOI: 10.3390/life12050682 -
Journal of Family Medicine and Primary... Jun 2020According to the World Health Organization (WHO) Framework Convention for Tobacco Control (FCTC), tobacco cessation is a primary health-care service that should be... (Review)
Review
According to the World Health Organization (WHO) Framework Convention for Tobacco Control (FCTC), tobacco cessation is a primary health-care service that should be provided not only to the people having adverse habits of consuming tobacco but also to the nonconsumer, as they can also be harmed due to its deleterious effects. Tobacco has been regarded as a potential risk factor for oral diseases such as oral potentially malignant disorders and oral cancers. Various aids of achieving cessation have been studied, including education of the ill effects of tobacco to the patient, behavioral counseling, and pharmacotherapy. Various pharmacological interventions are available nowadays but nicotine replacement therapy (NRT) is most widely used. The various types of NRT products results in general and breakthrough craving relief with immediate release of nicotine. All of these products have different levels of efficacy and variable rates of nicotine absorption. Knowledge of these will be beneficial for the patients, the budding dentist and the nation in the upcoming days ahead.
PubMed: 32984096
DOI: 10.4103/jfmpc.jfmpc_313_20 -
Drugs in R&D Sep 2023The benefit of exogenous melatonin is based on its bioavailability, which depends on the galenic form, the route of administration, the dosage, and the individual... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
The benefit of exogenous melatonin is based on its bioavailability, which depends on the galenic form, the route of administration, the dosage, and the individual absorption and rate of hepatic metabolism.
OBJECTIVE
The objective of this study is to investigate the bioavailability of melatonin after administration of an oral prolonged-release tablet (PR form) and an immediate-release sublingual spray (IR form). The main metabolite of melatonin, 6-sulfatoxymelatonin (6-SMT), was also measured, which has not been done in previous studies. Its determination is important as an index of the hepatic transformation of melatonin.
METHODS
In this single-center, open-label, randomized, crossover study, 14 healthy male volunteers received one tablet of the PR form (1.9 mg melatonin) or two sprays of the IR form (1 mg melatonin) during two visits separated by a washout period. Blood samples were collected over 7 and 9 h for the IR and PR form, respectively, to determine the main pharmacokinetic parameters.
RESULTS
The observed kinetics were consistent with those expected for immediate and prolonged-release forms. Pulverization of the spray resulted in an early, high plasma melatonin peak (C: 2332 ± 950 pg/mL; T: 23.3 ± 6.5 min), whereas tablet intake produced a lower peak (C: 1151 ± 565 pg/mL; T: 64.2 ± 44.2 min; p < 0.001 for comparison of C and T) followed by a plasma melatonin plateau and a more prolonged decay over time. Plasma melatonin/6-SMT AUC ratio was 0.09 for the PR form and 0.16 for the IR form. Both galenic forms were well tolerated.
CONCLUSIONS
The results suggest that the galenic forms containing melatonin assessed in this study are suitable for the treatment of certain sleep disorders such as sleep onset delay and transient nocturnal awakenings for the IR form and insomnia for the PR form.
TRIAL REGISTRY
Registration number: NCT04574141.
Topics: Humans; Male; Biological Availability; Cross-Over Studies; Melatonin; Tablets; Volunteers; Administration, Oral; Area Under Curve
PubMed: 37438493
DOI: 10.1007/s40268-023-00431-9