RESUMO
Oral suspension is the most preferred dosage form for the paediatric population because of the difficulties related to solid medications, such as the swallowing limitations, bitter taste, and poor oral bioavailability, which can cause serious impairment to attain a successful treatment. Given the importance of successful therapies, there is a need for safe and effective commercially-available paediatric oral suspension and their characterization. For the latter, it is important to identify safe excipients and preservatives. The paediatric group is a diverse category which includes infants and teenagers, with major pharmacokinetics and pharmacodynamics differences, mainly because of physiological and behavioral variations. Therefore, finding a single formulation for paediatric population remains a challenge, as well asthe formulation of stable-in-time suspension. In addition, drug's dissolving characteristic and permeation, are the main determinants for oral absorption, which are closely related to drug release kinetics from the pharmaceutical form. In this context, drug release profile is an important and limiting step in oral bioavailability, particularly for BCS class II drugs; thus, it is possible to increase bioavailability and minimize adverse effects by changing the release rate of such drugs. This review covers all the aspects for paediatric oral suspension development, and analyses the considerations for excipients selection as a crucial task for effectively choosing a safe and effective pharmaceutical form and correctly dosing paediatric patients.
Assuntos
Disponibilidade Biológica , Excipientes , Suspensões , Humanos , Administração Oral , Criança , Excipientes/química , Composição de Medicamentos/métodos , Adolescente , Liberação Controlada de Fármacos , Química Farmacêutica/métodos , Lactente , Preparações Farmacêuticas/administração & dosagem , Preparações Farmacêuticas/químicaRESUMO
Hypertension is one of the major causes of mortality in the world. The non-selective -ß-blocker which includes Timolol maleate (TM) is usually used in hypertension, at a given dose of 10-40 mg. The present research aims to design a tablet-in-tablet (TIT) formulation as a single-unit dosage form to achieve modified and rapid drug release. Wet granulation was used to create the inner core modified release tablet utilising the release modifying agent's Sodium alginate (SA) and Hydroxypropyl methylcellulose (HPMC K4M). The impact of independent factors, SA and HPMC K4M, in different percentages of w/w, which affect the in vitro drug release and swelling index, was investigated using a 32 complete factorial design. The TM outer instant-release shell, which was made using croscarmellose sodium and Microcrystalline cellulose (MCC) in three distinct sizes, was press-coated onto the optimised inner core tablet. The core and outer shell tablets are within acceptable ranges for several physicochemical properties. No indication of interactions between drugs, polymers, and excipients was found in the Fourier transform infrared (FTIR) and Differential scanning calorimetry (DSC) investigations. The inner core tablet's formulation F6 achieves a 96.38% in vitro drug release at 24 h and a swelling index of 52.7%. The TIT-2 was, however, considered as the final tablet-in-tablet formulation because contains fewer excipients and shorter disintegration time than TIT-3.
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Transdermal drug administration has grown in popularity in the pharmaceutical research community due to its potential to improve drug bioavailability, compliance among patients, and therapeutic effectiveness. To overcome the substantial barrier posed by the stratum corneum (SC) and promote drug absorption within the skin, various physical penetration augmentation approaches have been devised. This review article delves into popular physical penetration augmentation techniques, which include sonophoresis, iontophoresis, magnetophoresis, thermophoresis, needle-free injection, and microneedles (MNs) Sonophoresis is a technique that uses low-frequency ultrasonic waves to break the skin's barrier characteristics, therefore improving drug transport and distribution. In contrast, iontophoresis uses an applied electric current to push charged molecules of drugs inside the skin, effectively enhancing medication absorption. Magnetophoresis uses magnetic fields to drive drug carriers into the dermis, a technology that has shown promise in aiding targeted medication delivery. Thermophoresis is the regulated heating of the skin in order to improve drug absorption, particularly with thermally sensitive drug carriers. Needle-free injection technologies, such as jet injectors (JIs) and microprojection arrays, offer another option by producing temporary small pore sizes in the skin, facilitating painless and effective drug delivery. MNs are a painless, minimally invasive method, easy to self-administration, as well as high drug bioavailability. This study focuses on the underlying processes, current breakthroughs, and limitations connected with all of these approaches, with an emphasis on their applicability in diverse therapeutic areas. Finally, a thorough knowledge of these physical enhancement approaches and their incorporation into pharmaceutical research has the potential to revolutionize drug delivery, providing more efficient and secure treatment choices for a wide range of health-related diseases.
Assuntos
Epiderme , Pele , Humanos , Administração Cutânea , Pele/metabolismo , Preparações Farmacêuticas , Sistemas de Liberação de Medicamentos/métodos , Portadores de Fármacos/farmacologiaRESUMO
One of the major causes of death on the globe is cancer. It has remained a significant obstacle for current therapies and has not yet been effectively treated. Conventional treatment strategies available for cancer such as surgery, chemotherapy, radiation therapy etc. have severe adverse effects. The use of herbal active constituents in cancer treatment has tremendous potential to increase the effectiveness of conventional cancer therapy. Natural plant active components have been reported to have strong in vitro pharmacological activity but narrow in vivo absorption. In order to increase their bioavailability and absorption and get around the drawbacks and negative effects of traditional herbal extracts, Phytosomes are one of the growing nanotechnologies that can be used to improve the miscibility of bioactive phytoconstituents in lipid-rich barriers and overcome their poor bioavailability. Many novel drug delivery carriers are employed for targeted delivery of phytoconstituent at the site of action. Phytosomes are well-known biocompatible nanocarriers that can be employed to increase the solubility and permeability of phytopharmaceuticals among various novel drug delivery systems (NDDS). This review mainly focused on various conventional as well as novel approaches and various Nano carrier used in cancer therapies. Also comprising summary of the most recent research on the development and use of phytosomes as a better carrier for herbal constituents in the treatment of cancer. Additionally provides information about the formulation, characterization technique and mechanism of drug release from phytosome. Some of the major herbal active constituents made of phytosome which have shown proven anticancer activity are also studied. Finally, challenges and future perspective related to phytosome in cancer treatment are also discussed.
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The Sediment Delivery Model explains experimental analysis and quantitative assessment of the powdered substance characterizing parameters, which offer pertinent data about the material's appropriateness for direct compression (DC) of tablet, which involves mathematical modeling and Semisolid Control Diagram using software like iTCM. The SeDeM diagram expert system (DES) determines the suitability of excipients and active ingredients for DC and the ratio of API to excipient is calculated. The DC is most suitable as it saves time and makes process easy, but these technique excipients compensate for their poor flow. Thus, a new system was required to help reduce number of experiments and time for making an optimized direct compression tablet. The SeDeM DES is based on quality by design (QbD) (ICH Q8) as it evaluates critical quality attributes that affect finished product's quality. This review mainly focuses on various dosage forms like Solid, Semisolid, Liquisolid, and Solidified liquid dosage forms. These techniques mainly characterize all substances using 12 parameters, resulting 12-sided regular polygon. However, parameters may increase or decrease according to the requirement of a particular dosage form like an Orodispersible tablet 15 and a Semisolid dosage form applying 5 parameters. The rationales behind limits for indexes are justified accordingly.
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Excipientes , Sistemas Inteligentes , Comprimidos , Pós , Pressão , Composição de Medicamentos/métodosRESUMO
A Dry Powder Inhaler (DPI) is a technique as well as a device used to inhale formulation which is in the form of dry powder, and is inhaled through the nose or mouth. It was developed for the purpose of treating conditions like chronic obstructive pulmonary disease (COPD), Asthma, and even cystic fibrosis etc. The aim of the review is to discuss the different methods of preparation of dry powders along with the characterization of DPI. Here we present the outline of different methods like supercritical fluid extraction (SCF), spray drying, and milling. The review focussed on various devices including single and multi-dose devices used in the DPI. It also highlights on recent advances in the DPI including nano particulate system, siRNA-based medication, liposomes, and pro-liposomes based delivery. In COVID-19 silver nanoparticles-based DPIs provide very prominent results in the infected lungs. Moreover, this review states that the AI-based DPI development provides and improvement in the bioavailability and effectiveness of the drug along with the role of artificial neural networks (ANN). The study also showed that nasally administered drugs (nose to brain) can easily cross the blood-brain barrier (BBB) and enter the central nervous system (CNS) through the olfactory and trigeminal pathway which provides effective CNS concentrations at lower dosage. It is suggested that DPIs not only target respiratory complications but also treat CNS complications too. This review provides support and guides the researcher in the recent development and evaluation of DPI.
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COVID-19 , Nanopartículas Metálicas , Humanos , Inaladores de Pó Seco , Lipossomos , Prata , Administração por Inalação , PósRESUMO
Objective: The main aim of this research work was to develop and evaluate cost effective modified release tablets of Capecitabine (CAP) without utilizing coating techniques.Methods: The tablets were prepared by non-aqueous wet granulation method. Hydroxypropyl cellulose (HPC) was used as an extended release matrix former and sodium alginate (SA) was used as sustained release agent due to its gel forming ability. 32 full factorial design was used to study the effect of the independent variables i.e. HPC and SA on dependent variables, in vitro drug release and swelling index. The physiochemical properties of the drug were analyzed by ultraviolet (UV), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (P-XRD). The formulated tablets were evaluated for hardness, thickness, weight variation, content uniformity, swelling index, and in vitro drug release study.Results: The FTIR and DSC studies confirmed that there was no any interaction between drug, polymers and excipients. Also from DSC and P-XRD studies it was clear that the crystalline nature of CAP was remain unchanged in the optimized formulation tablet. Formulation F8 retarded the drug release up to 24 h with the optimum concentration of the both the polymers.Conclusion: We have successfully developed the modified release tablets of CAP with the combination of diffusion and erosion controlled type of drug release mechanism.
Assuntos
Antimetabólitos Antineoplásicos/administração & dosagem , Capecitabina/administração & dosagem , Excipientes/química , Polímeros/química , Alginatos/química , Antimetabólitos Antineoplásicos/química , Capecitabina/química , Celulose/análogos & derivados , Celulose/química , Química Farmacêutica , Cristalização , Preparações de Ação Retardada , Liberação Controlada de Fármacos , ComprimidosRESUMO
Correction for 'Nanocrystalline Fe-Fe2O3 particle-deposited N-doped graphene as an activity-modulated Pt-free electrocatalyst for oxygen reduction reaction' by Vishal M. Dhavale et al., Nanoscale, 2015, 7, 20117-20125.
RESUMO
The size-controlled growth of nanocrystalline Fe-Fe2O3 particles (2-3 nm) and their concomitant dispersion on N-doped graphene (Fe-Fe2O3/NGr) could be attained when the mutually assisted redox reaction between NGr and Fe(3+) ions could be controlled within the aqueous droplets of a water-in-oil emulsion. The synergistic interaction existing between Fe-Fe2O3 and NGr helped the system to narrow down the overpotential for the oxygen reduction reaction (ORR) by bringing a significant positive shift to the reduction onset potential, which is just 15 mV higher than its Pt-counterpart. In addition, the half-wave potential (E1/2) of Fe-Fe2O3/NGr is found to be improved by a considerable amount of 135 mV in comparison to the system formed by dispersing Fe-Fe2O3 nanoparticles on reduced graphene oxide (Fe-Fe2O3/RGO), which indicates the presence of a higher number of active sites in Fe-Fe2O3/NGr. Despite this, the ORR kinetics of Fe-Fe2O3/NGr are found to be shifted significantly to the preferred 4-electron-transfer pathway compared to NGr and Fe-Fe2O3/RGO. Consequently, the H2O2% was found to be reduced by 78.3% for Fe-Fe2O3/NGr (13.0%) in comparison to Fe-Fe2O3/RGO (51.2%) and NGr (41.0%) at -0.30 V (vs. Hg/HgO). This difference in the yield of H2O2 formed between the systems along with the improvements observed in terms of the oxygen reduction onset and E1/2 in the case of Fe-Fe2O3/NGr reveals the activity modulation achieved for the latter is due to the coexistence of factors such as the presence of the mixed valancies of iron nanoparticles, small size and homogeneous distribution of Fe-Fe2O3 nanoparticles and the electronic modifications induced by the doped nitrogen in NGr. A controlled interplay of these factors looks like worked favorably in the case of Fe-Fe2O3/NGr. As a realistic system level validation, Fe-Fe2O3/NGr was employed as the cathode electrode of a single cell in a solid alkaline electrolyte membrane fuel cell (AEMFC). The system could display an open circuit voltage (OCV) of 0.73 V and maximum power and current densities of 54.40 mW cm(-2) and 200 mA cm(-2), respectively, which are comparable to the performance characteristics of a similar system derived by using 40 wt% Pt/C as the cathode electrode.
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Herein, we report the synthesis of a nitrogen-doped graphene (NGr) interpenetrated 3D Ni-nanocage (Ni-NGr) electrocatalyst by a simple water-in-oil (w/o) emulsion technique for oxidation of water to dioxygen. Correlation of adsorption of NGr and subsequent interpenetration through the specific surface plane of nickel particles as well as the concomitant interaction of N and C with Ni in the nano-regime has been investigated. Apart from the benefits of the synergistic interactions between Ni, N, and C, the overall integrity of the structure and its intra-molecular connectivity within the framework help in achieving better oxygen evolution characteristics at a significantly reduced overpotential. The engineered Ni-NGr nanocage displays a substantially low overpotential of â¼290 mV at a practical current density of 20 mA cm(-2) in 0.1 M KOH. In comparison, NGr and Ni-particles as separate entities give overpotentials of â¼570 and â¼370 mV under similar conditions. Moreover, the long term stability of Ni-NGr was investigated by anodic potential cycling for 500 cycles and an 8.5% increment in the overpotential at 20 mA cm(-2) was observed. Additionally, a chronoamperometric test was performed for 15 h at 20 mA cm(-2), which highlights the better sustainability of Ni-NGr under the actual operating conditions. Finally, the quantitative estimation of evolved oxygen was monitored by gas chromatography and was found to be 70 mmol h(-1) g(-1) of oxygen, which is constant in the second cycle as well.
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OBJECTIVE: The purpose of this work was to develop and evaluate buccoadhesive tablets of timolol maleate (TM) due to its potential to circumvent the first-pass metabolism and to improve its bioavailability. METHODS: The tablets were prepared by direct compression using two release modifying polymers, Carbopol 974P (Cp-974p) and sodium alginate (SA). A 3(2) full factorial design was employed to study the effect of independent variables, Cp-974p and SA, in various proportions in percent w/w, which influences the in vitro drug release and bioadhesive strengths. Physicochemical properties of the drug were evaluated by ultraviolet, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (P-XRD). Tablets were evaluated for hardness, thickness, weight variation, drug content, surface pH, swelling index, bioadhesive force and in vitro drug release. RESULTS: The FTIR and DSC studies showed no evidence of interactions between drug, polymers and excipients. The P-XRD study revealed that crystallinity of TM remain unchanged in optimized formulation tablet. Formulation F9 achieves an in vitro drug release of 98.967% ± 0.28 at 8 h and a bioadhesive force of 0.088 N ± 0.01211. CONCLUSION: We successfully developed buccal tablet formulations of TM and describe a non-Fickian-type anomalous transport as the release mechanism.