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1.
Yakugaku Zasshi ; 140(8): 1013-1024, 2020.
Artigo em Japonês | MEDLINE | ID: mdl-32741859

RESUMO

Novel dosage form designs aiming at patient centric drug therapy are summarized here based on my carrier research in this field. The common key word for this research is particle design. The topics will be divided into two parts, based on the type of particle: coarse particles (powder) and colloidal particles. The former includes the preparation and characterization of functional particles prepared using a spray dryer. Solid dispersions, solvent deposition particles and dry emulsion systems are described. Polymer coated liposomes are described as a useful drug delivery carrier in several administration routes. As chitosan, a mucoadhesive polymer, was used as a coating polymer, the resultant chitosan-coated liposome was found to work as a good carrier for peptide drugs such as insulin and calcitonin in the gastrointestinal tract after oral administration. In another administration route (inhalation), polymer-coated liposomes enhanced the absorption of the drugs. Liposomal carriers applied to the surface of the eye as eye drops are able to deliver drugs to the posterior part of the eye, such as the retina. As a typical example of patient centric dosage form design, particle designs for the preparation of orally disintegrating tablets and films were introduced in one of our recent studies on oral dosage form design.


Assuntos
Formas de Dosagem , Sistemas de Liberação de Medicamentos , Desenho de Fármacos , Lipossomos , Tamanho da Partícula , Administração por Inalação , Administração Oral , Calcitonina/administração & dosagem , Quitosana , Coloides , Humanos , Insulina/administração & dosagem , Polímeros
2.
Medicine (Baltimore) ; 99(24): e20666, 2020 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-32541510

RESUMO

BACKGROUND: Knee osteoarthritis (KOA) is a common chronic disorder of knee and the leading cause of pain in the elderly with an overall prevalence of 50% in people over 60 years of age. This disease is an important factor affecting the quality of life of middle-aged and elderly people, and its main symptom is knee joint pain. Due to the pain, the knee joint activity function is limited, bringing great pain to patients, affecting their quality of life, effective prevention, and treatment of KOA is a modern medical problem. METHODS: The 60 patients who met the inclusion criteria were randomly divided into the treatment group and the control group. In this study, single center, randomized control and equivalent clinical trial were used for treatment. The treatment group received Yuanhu Zhitong dropping pills within 4 weeks, and the control group received diclofenac sodium sustained-release capsule treatment within 4 weeks. The main measures were visual analogue scale (VAS), WOMAC osteoarthritis index score and gastrointestinal symptoms rating scale (GSRS).Secondary measures included biochemical markers and adverse reactions during treatment. RESULT: The results of this trial will be published on the website of China Clinical Trial Registration Center (http://www.chictr.org.cn/searchprojen.aspx) and in peer-reviewed journals or academic conferences. CONCLUSIONS: This study is to assess the efficacy and safety of Yuanhu Zhitong dropping pills for knee osteoarthritis (KOA). REGISTRATION: PROSPERO (registration number ChiCTR1900024712).


Assuntos
Artralgia/tratamento farmacológico , Artralgia/etiologia , Medicamentos de Ervas Chinesas/uso terapêutico , Osteoartrite do Joelho/complicações , Manejo da Dor/métodos , Fitoterapia , Ensaios Clínicos Controlados Aleatórios como Assunto/métodos , Projetos de Pesquisa , Formas de Dosagem , Humanos , Método Simples-Cego
3.
AAPS PharmSciTech ; 21(5): 139, 2020 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-32419049

RESUMO

A recently published FDA guidance on chewable tablets has addressed the quality attributes of this class of dosage forms. This study evaluated disintegration as a quality attribute for a number of commercially available chewable antacid tablets. Additionally, acid-neutralizing-capacity values were evaluated. A number of the products exhibited prolonged disintegration times-which were far longer than those of conventional immediate-release tablets. The mean disintegration times ranged from 6 to more than 60 min in distilled water and from 9 to over 60 min in 0.1 N HCl. The products with longer disintegration times had higher breaking force and tensile strength values. Despite the range in disintegration times, all products met the criteria for acid-neutralizing capacity. These results indicate a need for patients to be aware of the need to thoroughly chew antacid tablets upon administration. Given these considerations, disintegration testing would be a useful quality control test in evaluating these dosage forms as the implicit assumption by the manufacturer that patients will chew the product sufficiently may not be met in every case.


Assuntos
Antiácidos/administração & dosagem , Antiácidos/química , Química Farmacêutica , Formas de Dosagem , Cinética , Solubilidade , Comprimidos , Resistência à Tração , Estados Unidos , United States Food and Drug Administration , Água
4.
N Z Med J ; 133(1512): 22-30, 2020 04 03.
Artigo em Inglês | MEDLINE | ID: mdl-32242175

RESUMO

AIMS: To assess a persuasive multimodel approach to decreasing unnecessary intravenous (IV) clarithromycin use for community-acquired pneumonia (CAP) in Canterbury District Health Board (CDHB) hospitals. METHODS: In December 2013, CDHB guidelines for empiric treatment of CAP changed to prioritise oral azithromycin over IV clarithromycin. The multimodel approach we used to implement this change included obtaining stakeholder agreement, improved guidelines access, education and pharmacist support. The impact of the intervention was evaluated by comparing macrolide usage and expenditure for the four years pre- and post-intervention. RESULTS: Mean annual clarithromycin IV use decreased by 72% from 6.4 to 1.8 defined daily doses (DDDs) per 1,000 occupied bed days (OBDs) post-intervention, while oral azithromycin increased by 833% (4.2 to 39.2 DDDs per 1,000 OBDs). Concurrently, oral clarithromycin use decreased by 91% (32.9 to 2.9 DDDs per 1,000 OBDs), and roxithromycin by 71% (17.0 to 5.0 DDDs per 1,000 OBDs). Mean annual total macrolide use decreased by 21% (68.2 to 53.9 DDDs per 1,000 OBDs), while expenditure decreased by 69% mainly through avoided IV administration. CONCLUSIONS: A persuasive multimodel approach to support adoption of CAP guidelines produced a sustained decrease in IV clarithromycin use, which may have clinical benefits such as reduced occurrence of catheter-related complications.


Assuntos
Antibacterianos/administração & dosagem , Gestão de Antimicrobianos/normas , Azitromicina/administração & dosagem , Claritromicina/administração & dosagem , Infecções Comunitárias Adquiridas/tratamento farmacológico , Pneumonia/tratamento farmacológico , Administração Intravenosa , Administração Oral , Antibacterianos/economia , Gestão de Antimicrobianos/economia , Azitromicina/economia , Claritromicina/economia , Formas de Dosagem , Fidelidade a Diretrizes , Hospitais , Humanos , Nova Zelândia
5.
Allergol. immunopatol ; 48(2): 124-129, mar.-abr. 2020. tab
Artigo em Inglês | IBECS | ID: ibc-191814

RESUMO

OBJECTIVE: This study aimed to assess the regular use of long-term asthma-control medication and to determine inhaler techniques in asthmatic children. METHODS: The study was conducted on asthmatic children aged 6-18 years. Information on rescue and controller medications was given and the proper inhalation technique was demonstrated. One month later, patients and parents were asked to answer a questionnaire on drug use and to demonstrate their inhaler techniques. RESULTS: One hundred children and/or their parents were interviewed for the study. All of the patients identified long-term asthma-control medications while quick-relief asthma medications were identified by 93% of the patients. Of the patients, 34% described the dose of their quick-relief medication correctly. All steps in the inhalation technique were correctly carried out by 60.6% of patients using a metered-dose inhaler (MDI), 80% of patients using a Turbuhaler, and 58% of patients using a capsule-based dry-powder inhaler (DPI). Of the participants, 73% reported regular use of long-term asthma-control medications. While the mean age of the patients regularly using long-term asthma medications was 9.05 ± 2.5 years, that of patients not compliant with the regular treatment was 10.29 ± 3.26 years (p = 0.04). The most common reason for irregular drug use was forgetting to take the drug. CONCLUSION: Adherence to long-term asthma-control medications tends to be better in younger patients. Since the most common cause of irregular drug use is forgetting to take the drug, repeated training is necessary to ensure asthma control and the successful treatment of asthmatic children


No disponible


Assuntos
Humanos , Masculino , Feminino , Criança , Adolescente , Asma/tratamento farmacológico , Administração por Inalação , Antiasmáticos/administração & dosagem , Assistência de Longa Duração , Inquéritos e Questionários , Cooperação e Adesão ao Tratamento , Asma/diagnóstico , Estudos Prospectivos , Formas de Dosagem , Inaladores Dosimetrados
7.
AAPS PharmSciTech ; 21(2): 72, 2020 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-31953566

RESUMO

Our research group has pioneered the development of liquisolid pellets as a new drug delivery system targeting at the improvement of the dissolution rates of poorly water-soluble drugs, combining the technological and biopharmaceutical advantages of both multiparticulate and liquisolid systems. Recently, Lam and collaborators claimed the invention of "liqui-pellets" as "the emerging next-generation oral dosage form which stems from liquisolid concept in combination with pelletization technology". However, the concept of liqui-pellet is not novel. As we demonstrate in this commentary, liqui-pellets are the same type of preparation as our previously and extensively reported liquisolid pellets. Liquisolid pellets have been disclosed in a patent application and public peer-reviewed articles covering the concept, preparation and challenges associated with these systems. There are no technical differences that justify excluding our previous reports as the first reports on liquisolid pellets or liqui-pellets. This commentary highlights the similarities between liquisolid pellets and liqui-pellets, focusing on the anteriority of liquisolid pellets as disclosed by our group.


Assuntos
Formas de Dosagem , Biofarmácia , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Implantes de Medicamento
8.
J Chromatogr A ; 1616: 460795, 2020 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-31918849

RESUMO

Based on our previous work with "pseudostationary-ion exchanger sweeping", we use this strategy to develop a sensitive, reliable and robust method for the analysis of the newly-FDA approved hepatitis C antiviral drugs namely; sofosbuvir (SOV), daclatasvir (DAC), ledipasvir (LED) and velpatasvir (VEP) in their pure forms and co-formulated pharmaceutical dosage forms using micellar electrokinetic chromatography (MEKC) as a separation method. For the first time, a successful separation of all the investigated compounds was achieved in less than 8 min using a basic background electrolyte (BGE) composed of 25 mmol L-1 SDS + 20% (v/v) ACN (acetonitrile) in 10 mmol L-1 disodium tetraborate buffer (final apparent pH is 9.90). A special focus was given to optimize the composition of the sample matrix to maintain the solubility of the analytes within the sample zone while gaining additional benefits regarding analyte zone focusing. It was found that replacing phosphoric acid (as a sample matrix) with a zwitterionic/isoelectric buffering compound (L-glutamic acid) has a substantial positive impact on the obtained enrichment efficiency. The interplay of other enrichment principles such as the retention factor gradient effect (RFGE) is also discussed. A full validation study is performed based on the pharmacopeial and ICH guidelines. The obtained limits of detection and quantitation are as low as 0.63 and 1.3 µg mL-1; respectively for SOV and DAC and 1.3 and 2.5 µg mL-1; respectively for LED and VEP using UV-DAD as a detection method. The selectivity of the developed method for determination of the studied compounds in their pharmaceutical dosage forms or in the presence of ribavirin (RIB) or elbasvir (ELB), which are other prescribed medications in the treatment regimen of patients with hepatitis C virus infection, is demonstrated. It is shown that with acidic sample matrix and basic BGE, an efficient and precise approach was designed in which analyte adsorption on the capillary wall was minimized while keeping repeatable peak height, peak area and migration time together with the highest possible enrichment efficiency.


Assuntos
Antivirais/análise , Cromatografia Capilar Eletrocinética Micelar/métodos , Hepacivirus/efeitos dos fármacos , Sofosbuvir/análise , Adsorção , Antivirais/química , Benzimidazóis , Benzofuranos , Carbamatos/análise , Carbamatos/química , Ciclodextrinas/química , Formas de Dosagem , Eletrólitos/química , Fluorenos , Compostos Heterocíclicos de 4 ou mais Anéis/análise , Compostos Heterocíclicos de 4 ou mais Anéis/química , Humanos , Imidazóis/análise , Imidazóis/química , Limite de Detecção , Modelos Lineares , Metanol/química , Reprodutibilidade dos Testes , Sofosbuvir/química , Solubilidade , Temperatura , Ureia/química
9.
AAPS PharmSciTech ; 21(2): 38, 2020 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-31897797

RESUMO

In the study, we developed a novel oral dosage form of Compound Danshen to resolve the problems of low bioavailability, disequilibrium in drug release, and stomach degradation of active components of Compound Danshen in conventional formulas. A colon-specific osmotic pump capsule (COPC) of Compound Danshen was prepared using a semipermeable shell with the core components. Using a single-factor method, we obtained the optimal formulation that consisted of Salvia miltiorrhiza extract, Panax notoginseng extract, Borneol, sodium chloride, polyethylene oxide wsr-N10, hydroxypropyl-ß-cyclodextrin, and ludipress. Moreover, in vitro dissolution test showed simultaneous releases of active ingredients from Compound Danshen COPC over 12 h at pH 7.8, displaying zero-order release characteristics. The impetus of drug release mainly depended on the difference in osmotic pressure across the capsule shell. Next, scanning electron microscopy showed morphological changes in the capsule shell during the dissolution test. More importantly, pharmacokinetic study in beagle dogs indicated that relative bioavailability was 330.58% and retention time was greatly prolonged in Compound Danshen COPC, compared with those in marketed Compound Danshen tablet products. Finally, in vivo imaging studies in beagle dogs showed that COPC was stable in gastrointestinal tract and the drug was specifically released in the colon region. A colon-specific osmotic pump capsule (COPC) of Compound Danshen was developed and optimized to achieve simultaneous zero-order release of multiple active components of Compound Danshen in the colon. More importantly, the COPC have proved to improve the bioavailability and prolong the retention time of Compound Danshen, compared with those in a marketed product.


Assuntos
Formas de Dosagem , Medicamentos de Ervas Chinesas/administração & dosagem , Administração Oral , Animais , Disponibilidade Biológica , Canfanos/química , Colo/metabolismo , Preparações de Ação Retardada , Cães , Composição de Medicamentos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacocinética , Excipientes , Pressão Osmótica , Panax notoginseng/química , Salvia miltiorrhiza/química , Solubilidade
10.
Ultrason Sonochem ; 62: 104861, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31796325

RESUMO

Emodin is a bioactive compound with strong anti-inflammatory and antioxidant properties. Micellar casein is casein concentrates close to the native state of casein micelles. The interaction of emodin and micellar casein under heat treatment in the absence and presence of ultrasound was investigated, and the properties of microencapsulated emodin in micellar casein were compared. Fluorescence experiments proved that the major interaction between emodin and micellar casein was through hydrophobic forces under heat treatment in the absence and presence of ultrasound. However, ΔH, ΔS and ΔG of emodin-casein complexation without sonication were higher than those with sonication, in contradiction to binding constants. The particle sizes of emodin-casein complexes in the presence of ultrasound were smaller than those without sonication, while the specific surface area showed an opposite trend. As to encapsulation, emodin-casein capsules under heat-sonication treatment showed higher antioxidant properties than those of heat treatment alone under similar experimental conditions. Interestingly, micellar casein-emodin encapsulation in the presence of ultrasound showed a lower release rate of emodin in gastrointestinal conditions than that without ultrasound at the emdoin concentration of 10 µmol per gram casein. Ultrasound has been shown to be a potential processing technology for customizing the release kinetics of bioactive compounds.


Assuntos
Caseínas/química , Emodina/química , Temperatura Alta , Micelas , Ondas Ultrassônicas , Antioxidantes/farmacologia , Caseínas/farmacologia , Formas de Dosagem , Emodina/farmacologia , Interações Hidrofóbicas e Hidrofílicas , Tamanho da Partícula , Difração de Pó , Ligação Proteica , Análise Espectral/métodos , Termodinâmica
11.
Talanta ; 208: 120362, 2020 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-31816808

RESUMO

Dobutamine (DBT) is a sympathomimetic amine drug that was designed as an inotropic agent for use in congestive heart failure. Hence, there was an impetus to develop a rapid and accurate method for monitoring the concentration of DBT within clinical samples. To address this critical need, a novel In2O3 and functionalized multi-walled carbon nanotubes nanocomposite (In2O3@FMWCNTs) was successfully prepared and applied in an electrochemical sensor to detect DBT. The resulting sensor displayed electrocatalytic toward the oxidation of DBT, which attributed to the synergistic effect of In2O3 and FMWCNTs. Electrochemical impedance spectroscopy (EIS) studies revealed that the smaller charge transfer resistance value (Rct) was observed at In2O3@FMWCNTs modified glassy carbon spherical (GCS) paste electrode (PE) as compared to that of In2O3NPs/GCSPE, FMWCNTs/GCSPE and GCSPE, which authenticates its good conductivity. Furthermore, the calculated value of standard rate constant (ks) for the modified electrode demonstrates the fast electron transfer between DBT and the electrode surface. The fabricated electrochemical sensor indicated high selectivity and sensitivity for DBT determination over the oxidation of uric acid and ascorbic acid. The limit of detection of DBT at In2O3@FMWCNTs/GCSPE was found to be 1.42 × 10-10 M. The proposed sensor is effectively used for the detection of DBT in biological fluids, clinical patient blood and in injection dosage form.


Assuntos
Técnicas Biossensoriais/métodos , Dobutamina/sangue , Técnicas Eletroquímicas/métodos , Eletrodos , Índio/química , Nanocompostos/química , Nanotubos de Carbono/química , Ácido Ascórbico/química , Catálise , Dobutamina/metabolismo , Dobutamina/urina , Formas de Dosagem , Composição de Medicamentos , Humanos , Concentração de Íons de Hidrogênio , Limite de Detecção , Oxirredução , Ácido Úrico/química
12.
AAPS PharmSciTech ; 21(1): 28, 2019 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-31858320

RESUMO

While polyethylene oxide (PEO)-based matrix tablets are frequently used as abuse-deterrent dosage forms, there is limited information available regarding how the selection of formulation components and manufacturing processes affect the resulting abuse-deterrent properties. The objective of the current study was to evaluate the effects of formulation and process variables on the abuse-deterrent features of PEO-containing tablets. Directly compressed tablets were prepared using three different PEO molecular weights (100,000; 900,000; and 5,000,000). As anticipated, sintering/thermal treatment above the melting point of PEO was crucial to impart crush-resistant features (tablet hardness > 500 N). In addition to the sintering temperature, the weight fraction of PEO in the tablets affected their mechanical strength, and at least 50% w/w PEO was required to impart the desired crush-resistant features. In addition, the formulation and process variables also impacted syringeability and injectability of the PEO gels formed when the tablets were hydrated to simulate attempted drug extraction. High molecular weight PEO (900,000 and 5,000,000) produced gels more resistant to syringeability and injectability compared to low molecular weight PEO (100,000). Sintering above the polymer melting point decreased PEO crystallinity after cooling, and longer sintering times resulted in PEO degradation producing lower viscosity gels with reduced resistance to syringeability and injectability. Although sintering above the melting point of PEO imparts optimal mechanical strength to the tablets, prolonged sintering durations negatively impact polymer stability and alter the resulting abuse-deterrent features of the PEO-based tablet formulations.


Assuntos
Preparações de Ação Retardada , Polietilenoglicóis/química , Polietilenoglicóis/farmacologia , Comprimidos/química , Química Farmacêutica , Formas de Dosagem , Dureza , Peso Molecular
13.
Presse Med ; 48(12): 1520-1526, 2019 Dec.
Artigo em Francês | MEDLINE | ID: mdl-31761608

RESUMO

Non-adherence to antihypertensive treatment is one of the critical contributors to sub-optimal blood pressure control. The French Society of Hypertension remembered that urine and serum biochemical detection of antihypertensive drugs could be useful in a patient with resistant hypertension. Talking to a patient with biochemically confirmed non-adherence to blood pressure-lowering therapy and repeating them improved adherence to drugs. Despite its usefulness, biochemical detection of antihypertensive drugs is not routinely effective in France as they are not reimbursed by French Medical Care, except in patients attending hospitals. The list of blood pressure-lowering drugs able to be biochemically detected in France and their modalities are recorded here.


Assuntos
Anti-Hipertensivos/uso terapêutico , Hipertensão/tratamento farmacológico , Hipertensão/epidemiologia , Adesão à Medicação/estatística & dados numéricos , Anti-Hipertensivos/economia , Pressão Sanguínea/efeitos dos fármacos , Formas de Dosagem , Custos de Medicamentos , França/epidemiologia , Humanos , Hipertensão/economia
14.
United European Gastroenterol J ; 7(9): 1164-1170, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31700629

RESUMO

Background: Budesonide-MMX has an established role in the management of relapsing mild-to-moderate ulcerative colitis. Data regarding effectiveness and tolerability in real-life clinical practice are limited. Aim: The aim of this study was to assess the use of budesonide-MMX in ulcerative colitis, as well as short-term effectiveness and tolerability in real-life practice. Methods: We conducted a retrospective study of adult patients with mild-to-moderate ulcerative colitis treated with budesonide-MMX at four tertiary inflammatory bowel disease centres in Italy from June 2016 to February 2018. Demographic and clinical features of patients, the use of budesonide-MMX, disease course and concomitant therapy were recorded. The primary outcome assessed was clinical remission at 2 months. Results: A total of 82 patients with active mild-to-moderate ulcerative colitis were included in the study with a mean age of 45.9 years and a median partial Mayo Score of 4 (interquartile range 3-5). A total of 41 patients were male. Overall, 36 had extensive colitis, 38 left-sided colitis and eight proctitis. Treatments at the time of inclusion included 10 patients receiving biologic therapy, seven azathioprine and 54 mesalazine or salazopyrin. The main reasons for the addition of budesonide-MMX were clinical relapse (47.5%) or inadequate response to current therapy (39.0%). In total, 50% of patients achieved clinical remission, whereas 9.8% had clinical improvement. No response was noted in 40.2% of subjects. Using multivariate binary logistic regression, a moderate degree of activity was the main independent predictor of non-response. Eight significant adverse effects were reported in six patients with three discontinuing treatment. Conclusion: In real-life clinical practice, budesonide-MMX is commonly used in combination with other therapies, both for acute disease flares and for partial response to therapy.


Assuntos
Budesonida/administração & dosagem , Colite Ulcerativa/tratamento farmacológico , Glucocorticoides/administração & dosagem , Adulto , Idoso , Anti-Inflamatórios não Esteroides/uso terapêutico , Azatioprina/uso terapêutico , Budesonida/uso terapêutico , Colite Ulcerativa/patologia , Formas de Dosagem , Quimioterapia Combinada , Feminino , Glucocorticoides/uso terapêutico , Humanos , Imunossupressores/uso terapêutico , Itália , Modelos Logísticos , Masculino , Mesalamina/uso terapêutico , Pessoa de Meia-Idade , Análise Multivariada , Estudos Retrospectivos , Índice de Gravidade de Doença , Sulfassalazina/uso terapêutico , Resultado do Tratamento
15.
United European Gastroenterol J ; 7(9): 1171-1182, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31700630

RESUMO

Background: Cortiment®MMX® (budesonide MMX®) is currently approved for the induction of remission in mild-to-moderate ulcerative colitis (UC) patients when 5-ASA treatment is not sufficient. Data in real-life settings are lacking. Methods: This was a multicentre observational prospective cohort study conducted in Europe and Canada. Effectiveness, safety, and tolerability of Cortiment®MMX® in a real-life setting of patients treated for mild-to-moderate UC was investigated. Patients were prescribed Cortiment®MMX® in accordance with the Summary of the Product Characteristics (SmPC).The primary endpoint was the clinical benefit of Cortiment® MMX® in routine practice (improvement ≥ 3 points in the clinical sub-scores of the Ulcerative Colitis Disease Activity Index, UCDAI). Results: Data from 326 patients with mild-to-moderate UC were analysed for the primary endpoint. Clinical benefit was achieved in 60.1% (196/326) of patients at the end of Cortiment®MMX® treatment. Clinical remission (UCDAI clinical sub-score ≤ 1), full symptoms resolution (rectal bleeding (RB) = 0 and stool frequency (SF) = 0) and symptoms resolution (RB = 0 + SF ≤ 1) at the end of the Cortiment®MMX® treatment were achieved in 51.8%, 45.1% and 63.2% of patients, respectively. The median time to symptoms resolution was 30 days (range 29.0-36.0 days). Fifty patients (14.3%) had to discontinue Cortiment®MMX® due to adverse events; 17.5% of patients (n = 61) reported at least one adverse event related to the study drug. Conclusions: This was the first time that a large cohort study was conducted with Cortiment®MMX® in a real-life setting. It demonstrated that Cortiment®MMX® is effective, safe and well tolerated in about 60% of UC patients.


Assuntos
Budesonida/administração & dosagem , Colite Ulcerativa/tratamento farmacológico , Glucocorticoides/administração & dosagem , Adulto , Anti-Inflamatórios não Esteroides/uso terapêutico , Budesonida/uso terapêutico , Estudos de Coortes , Formas de Dosagem , Quimioterapia Combinada , Feminino , Glucocorticoides/uso terapêutico , Humanos , Masculino , Mesalamina/uso terapêutico , Pessoa de Meia-Idade , Estudos Prospectivos , Índice de Gravidade de Doença , Resultado do Tratamento
16.
AAPS PharmSciTech ; 20(8): 332, 2019 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-31705211

RESUMO

Individualized dosing is often required in pharmacotherapy, particularly for pediatric and geriatric patients and adjustment of drugs that demand dose adaptation. This study aimed to evaluate critical quality attributes (CQAs) of doses obtained by distinct approaches for achieving individual dosing. Approaches were evaluated as follows: subdivision of tablets by splitter and hand (haloperidol) and delivery by plastic dropper bottle (haloperidol), glass dropper bottle (clonazepam), dosing cup (sodium valproate), and dosing syringe (carbamazepine), including brand name, generic, and similar marketed products. Measuring devices were packaged with their respective product. Drug content uniformity was assessed to each substance according to pharmacopeial methods. Tablets subdivided by splitter had the poorest performance among all approaches, in which doses ranged around 60% of the labeled amount (Acceptance Value = 58.1 and RSD = 23.2%). The greatest performances were observed for the dosing syringe which fulfilled all the requirements for dose precision and for the glass dropper bottle. There were significant differences in dose delivery between manufacturers of the same medicine when measuring the same volume or number of drops. High drug content variability is extremely harmful to pharmacotherapy and may result in therapeutic failure or toxicity. It is crucial that measuring devices and scoring of tablets be checked for functionality and standardized for different manufacturers of the same medicine. Part of the approaches for achieving individual dosing did not meet the quality needs for drug content and uniformity. Yet, our findings show that more accurate and precise dosing can be accessed when using the dosing syringe and glass dropper bottle.


Assuntos
Anticonvulsivantes/administração & dosagem , Anticonvulsivantes/normas , Formas de Dosagem/normas , Sistemas de Liberação de Medicamentos/métodos , Controle de Qualidade , Seringas/normas , Administração Oral , Idoso , Criança , Relação Dose-Resposta a Droga , Humanos , Comprimidos
17.
Int J Pharm ; 572: 118808, 2019 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-31678387

RESUMO

Topical application of poorly water-soluble antibiotics cannot achieve the desired therapeutic concentration within cornea. The purpose of this study was to fabricate, characterize and evaluate in-vivo effectiveness of amphotericin B (AmB) containing microneedle ocular patch (MOP) against fungal keratitis. MOP containing free or liposomal AmB was fabricated using micromolding technique to mimic contact lens. MOPs were prepared using dissolvable polymeric matrix including polyvinyl alcohol and polyvinyl pyrrolidone. AmB loaded MOP were studied for their physical and mechanical properties, drug loading and dissolution rate, corneal insertion and drug permeability. MOP loaded with 100 µg AmB had a compression strength of 35.1 ±â€¯6.7 N and required an insertional force of 1.07 ±â€¯0.17 N in excised human cornea. Ex-vivo corneal permeation studies revealed significant enhancement in AmB corneal retention with the application of MOP compared with free AmB or liposomal AmB application. Furthermore, AmB loaded MOP application significantly (P < 0.05) reduced the Candida albicans load within cornea as evaluated in both ex-vivo model and in-vivo rabbit infection model. Histological examination showed that AmB MOP treatment improved the epithelial and stromal differentiation of corneal membrane. AmB containing MOPs can be developed as minimally invasive corneal delivery device for effective treatment of fungal keratitis.


Assuntos
Anfotericina B/administração & dosagem , Antifúngicos/administração & dosagem , Candida albicans/efeitos dos fármacos , Candidíase/tratamento farmacológico , Sistemas de Liberação de Medicamentos/instrumentação , Infecções Oculares Fúngicas/tratamento farmacológico , Ceratite/tratamento farmacológico , Agulhas , Administração Oftálmica , Anfotericina B/química , Animais , Antifúngicos/química , Candidíase/microbiologia , Força Compressiva , Modelos Animais de Doenças , Formas de Dosagem , Composição de Medicamentos , Infecções Oculares Fúngicas/microbiologia , Humanos , Ceratite/microbiologia , Masculino , Miniaturização , Permeabilidade , Fosfatidilcolinas/química , Álcool de Polivinil/química , Povidona/química , Coelhos
18.
Endocrine ; 66(1): 87-94, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31617168

RESUMO

Levothyroxine (T4) is a critical-dose drug, because little variations in the blood concentration may cause treatment failure as well as iatrogenic thyrotoxicosis. Despite the dose response of this drug being more carefully titrated nowadays, several papers still report that a significant fraction of patients treated with levothyroxine demonstrate a TSH which is not on target. Moreover, some widespread gastrointestinal disorders as well as interfering drugs and foods may cause the "refractoriness" of a significant number of patients to an expected dose of thyroxine. The increasing awareness of the mechanisms interfering with the oral thyroid hormone bioavailability and the body of evidence regarding the complexity of treatment in certain classes of patients prompted pharmaceutical research to identify new hormonal formulations to optimize the performance of this drug. In this brief review, the progression of the scientific knowledge of novel T4 formulations use has been analyzed.


Assuntos
Tiroxina/administração & dosagem , Formas de Dosagem , Humanos , Medicina de Precisão
19.
Ann Pharm Fr ; 77(6): 460-467, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31564418

RESUMO

OBJECTIVE: Bupropion is a noradrenaline and dopamine reuptake inhibitor which is used as an antidepressant drug. Few HPLC and spectrophotometric methods have been reported before for the determination of bupropion. Most of the previous methods reported for determination of bupropion in pharmaceutical dosage forms are somehow dangerous to health and environment because of using organic solvents. METHOD: In the present method bupropion was determined in pharmaceutical dosage forms by spectrofluorimetry after ion-pair complex formation with eosin Y. The ion-pair complex formation was optimized for reagent amount, buffer pH and time. RESULT: The developed method was linear over the range of 3-120µgmL-1 with an acceptable precision (CV<1.5%) and accuracy (Error<1%). CONCLUSION: The present method is applicable for determination of bupropion in pharmaceutical dosage forms for routine quality control analysis.


Assuntos
Bupropiona/análise , Espectrometria de Fluorescência/métodos , Bupropiona/administração & dosagem , Formas de Dosagem , Amarelo de Eosina-(YS) , Concentração de Íons de Hidrogênio , Íons/química , Estrutura Molecular , Espectrofotometria , Comprimidos
20.
Rev Esp Quimioter ; 32 Suppl 2: 35-37, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31475808

RESUMO

In the past, the dose of an antibiotic was chosen, always from among those that were well tolerated, by considering those with the ability to exceed the MIC of bacteria in plasma. This approach, which has still not widely changed, is contrast-ed with the pharmacokinetic and pharmacodynamic (PK/PD) relationships, which indicate that the efficacy of antibiotics is directly related to parameters that relate the sequence of con-centrations over time with a parameter of the MIC effect in vitro. Until now, three types of PK/PD relationships have been established for antibiotics: the inhibitory coefficient (Cmax/MIC), the efficacy time (T>CMI) and the relationship between the exposure of the drug and the MIC (AUC/MIC).


Assuntos
Antibacterianos/farmacologia , Antibacterianos/farmacocinética , Prescrições de Medicamentos , Antibacterianos/administração & dosagem , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Infecções Bacterianas/microbiologia , Formas de Dosagem , Humanos , Testes de Sensibilidade Microbiana
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