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1.
Braz. J. Pharm. Sci. (Online) ; 58: e191123, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394050

ABSTRACT

Chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) is a problem, often occurs in patient. Inspite of high bioavailability, the demerits such as: hepatic first pass metabolism and invasive nature of oral and parenteral dosage forms can be avoided with anti-emetic therapy of transdermal device. The major objective of the present study is to modify the hydrochloride (HCl) form of Ondansetron (OND) to the base form followed by improvement of solubility and permeability of OND by employing solid dispersion (SD) loaded patches. Preformulation study, as observed, begins with an approach to enthuse solubility of OND by SD technique choosing different carriers. The choice of carriers was rationalized by phase solubility study. Several combinations of transdermal films were prepared with pure drug, carriers and SDs with plasticizer Ka values of OND-HPßCD binary system were found lower (54.43 to 187.57 M-1) than that of OND-PVP K-30 binary system (1156.77 to 12203.6 M-1). The drug content of SDs and patches were found satisfactory. Better permeation rate (236.48±3.66 µg/3.935 cm2) with promising flux enhancement (8.30 fold) was found with DBP loaded SD patch (P6*). Hence, enhancement of solubility and permeability of P6* ensures that it can successfully enhance the bioavailability


Subject(s)
Plasticizers/adverse effects , Solubility , Ondansetron/antagonists & inhibitors , Patients/classification , Vomiting , Pharmaceutical Preparations/analysis , Postoperative Nausea and Vomiting , Dosage Forms , Drug Therapy/instrumentation , Methods , Motion Pictures/classification
2.
Braz. J. Pharm. Sci. (Online) ; 58: e19487, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394028

ABSTRACT

Abstract Simple, precise, accurate and specific spectrophotometric methods are progressed and validated for concurrent analysis of Furosemide (FUR) and Spironolactone (SPR) in their combined dosage form depend on spectral analysis procedures. Furosemide (FUR) in the binary mixture could be analyzed at its λmax 274 nm using its recovered zero order absorption spectrum using constant multiplication method (CM). Spironolactone (SPR) in the mixture could be analyzed at its λmax 238 nm by ratio subtraction method (RS). Concurrent determination for FUR and SPR in their mixture could be applied by amplitude modulation method (AM), absorbance subtraction method (AS) and ratio difference (RD). Linearity ranges of FUR and SPR were (2.0µg/mL-22.0 µg/mL) and (3.0µg/mL-30.0 µg/mL), respectively. Specificity of the proposed spectrophotometric methods was examined by analyzing the prepared mixtures in laboratory and was applied successfully for pharmaceutical dosage form analysis which have the cited drugs without additives contribution. The proposed spectrophotometric methods were also validated as per as the guidelines of ICH. Statistical comparison was performed between the obtained results with those from the official methods of the cited drugs, using one-way ANOVA, F-test and student t-test. The results are exhibiting insignificant difference concerning precision and accuracy


Subject(s)
Spectrophotometry/methods , Spironolactone/antagonists & inhibitors , Pharmaceutical Preparations/administration & dosage , Furosemide/antagonists & inhibitors , Analysis of Variance , Dosage Forms , Methods
3.
Braz. J. Pharm. Sci. (Online) ; 57: e18896, 2021. tab, graf
Article in English | LILACS | ID: biblio-1339309

ABSTRACT

Tizanidine hydrochloride is a centrally acting skeletal muscle relaxant, used in the management of spasticity. This drug is commercially available only as tablets, which highlights the need to develop oral liquid formulations. In the hospital environment, this aspect is circumvented by the preparation of suspensions, to allow administration to children and adults with impaired swallowing, but there are no data regarding their stability. The purpose of this study was to evaluate the physicochemical andmicrobiological stability of liquid dosage forms prepared in the hospital environment from tizanidine hydrochloride tablets, applying high performance liquid chromatography (HPLC) and microbiological analysis. A simple and stability-indicating HPLC method was developed and validated for specificity, linearity, limits of detection and quantification, precision, accuracy and robustness. The liquid formulations were placed in amber PET and glass bottles, which were stored under three different conditions: at room temperature, under refrigeration and at 40 ºC. The liquid formulations were analyzed and demonstrated chemical stability for 56 days, allowing their use for long periods. However, the determination of microbiological stability showed that these formulations are prone to microbial contamination, which has dramatically reduced its stability to 7 days, in both bottles and at all evaluated temperatures


Subject(s)
Tablets/pharmacology , Pharmaceutical Preparations/analysis , Microbiological Techniques/instrumentation , Chromatography, High Pressure Liquid/methods , Sensitivity and Specificity , Amber , Dosage Forms , Drug Stability , Methods
4.
Braz. J. Pharm. Sci. (Online) ; 56: e17737, 2020. tab, graf
Article in English | LILACS | ID: biblio-1132050

ABSTRACT

The aim of this work was to perform solubility studies for fexofenadine hydrochloride and establish dissolution conditions for this drug in oral suspension dosage form. The solubility study was executed through the shake-flask method, below 37 ºC±1 ºC, at 100 rpm stirring for 12 h in three buffer solutions: hydrochloric acid pH 2.0, acetate pH 4.5 and phosphate pH 6.8. The dissolution test was developed in vessels containing 900 mL of the same buffer, employing the paddle apparatus in speed of 25 and 50 rpm, below 37 ºC±0.5 ºC. The drug was classified as low solubility according to the Biopharmaceutics Classification System, since the dose/solubility ratio was higher than 250 mL in all media tested (326.55 mL in buffer pH 2.0; 2,456.33 mL in buffer pH 4.5 and 1,021.16 mL in buffer pH 6.8). The dissolution test showed that a release of 85% in 30 min could be established. The rotation speed of 25 rpm, media volume of 900 mL and insertion of the samples through weighted syringes are adequate. The buffered media pH 2.0 could be chosen as dissolution media.


Subject(s)
Solubility , Suspensions/pharmacology , Dissolution/methods , Biopharmaceutics , Pharmaceutical Preparations/analysis , Chromatography, High Pressure Liquid/methods , Dosage Forms
5.
Geriatr., Gerontol. Aging (Impr.) ; 13(3): 126-132, jul-set.2019. tab
Article in English | LILACS | ID: biblio-1097037

ABSTRACT

BACKGROUND: Tablet splitting appears common in older adults, but its safety, and the factors associated with this practice, remain unclear. OBJECTIVE: To identify which psychotropic drugs are most often split, which doses are intended with this practice, and whether these doses are provided by the Brazilian Unified Health System (SUS) or commercially available. METHODS: Cross-sectional descriptive study of 632 geriatric outpatients. The number of individuals who split tablets was identified, as well as the psychotropic drugs they used and split. The availability of these drugs on the SUS network and on the market was assessed by checking the 2017 National Formulary of Essential Medicines (RENAME 2017) and the Dictionary of Proprietary Medicinal Products (Dicionário de Especialidades Farmacêuticas) respectively. RESULTS: Tablet splitting was reported by 178 patients (28.2%). This practice was significantly more common among those aged 80 years or older. Tablet splitting was significantly associated with a greater number of medical visits and a higher pill burden. The most commonly affected therapeutic classes were antipsychotics (23.9%), other psychotropic drugs (18.7%) and antidepressants (12.3%). Of the 20 psychotropic drugs split, 45% were available on the SUS. CONCLUSIONS: Tablet splitting poses a challenge, as there is no guarantee of uniformity of concentration of the active ingredient in the split halves. Although the psychotropic drugs that were split in this sample are commercially available, most were not available from SUS in the desired dose forms for older adults.


INTRODUÇÃO: O fracionamento de comprimidos é comum em pacientes geriátricos, mas a segurança e os fatores associados a essa prática permanecem incertos. OBJETIVO: Identificar quais medicamentos psicotrópicos são mais frequentemente fracionados, quais doses se destinam a essa prática e se essas dosagens são fornecidas pelo Sistema Único de Saúde (SUS) ou comercialmente disponíveis. MÉTODOS: Estudo descritivo transversal de 632 pacientes ambulatoriais geriátricos. O número de indivíduos que fracionou os comprimidos foi identificado, bem como os medicamentos psicotrópicos que foram usados e fracionados. A disponibilidade desses medicamentos na rede SUS e no mercado foi avaliada através da verificação do Formulário Nacional de Medicamentos Essenciais (RENAME) de 2017 e do Dicionário de Especialidades Farmacêuticas, respectivamente. RESULTADOS: A partição de comprimidos foi relatada por 178 pacientes (28,2%). Essa prática foi significativamente mais comum entre aqueles com 80 anos ou mais. O fracionamento dos comprimidos foi significativamente associado a um maior número de consultas médicas e a uma maior carga de comprimidos. As classes terapêuticas mais comumente afetadas foram antipsicóticos (23,9%), outros medicamentos psicotrópicos (18,7%) e antidepressivos (12,3%). Dos 20 medicamentos psicotrópicos fracionados, 45% estavam disponíveis no SUS. CONCLUSÕES: O fracionamento de comprimidos representa um desafio, pois não há garantia de uniformidade de concentração do ingrediente ativo nas metades fracionadas. Embora os medicamentos psicotrópicos fracionados nesta amostra estejam disponíveis comercialmente, a maioria não estava disponível no SUS nas formas de dosagem desejadas para a população geriátrica.


Subject(s)
Humans , Male , Female , Middle Aged , Aged , Aged, 80 and over , Psychotropic Drugs/administration & dosage , Antipsychotic Agents/administration & dosage , Drugs, Essential/administration & dosage , Fractionated Drugs , Antidepressive Agents/administration & dosage , Outpatients , Health of the Elderly , Cross-Sectional Studies , Dosage Forms
6.
Braz. J. Pharm. Sci. (Online) ; 55: e17520, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039059

ABSTRACT

We propose to evaluate the dissolution properties of rosuvastatin calcium (ROSC) capsules in different media to characterize the discriminatory power of the assay method. Dissolution assays were performed in media with different pH, and including the surfactant sodium dodecyl sulfate (SDS). Several immediate-release formulations were manufactured using the commercial raw material characterized as amorphous solid. The hydrophobic adjutant magnesium stearate was employed in some formulations due to its negative effect in the wettability and dissolution efficacy of solid dosages. These formulations showed the lower dissolution efficacy values in media without surfactant; however, when SDS was added to the medium, the dissolution efficacy increased, and the discriminatory power was lost. In spite of micellar solubilization does not increase the ROSC solubility, it modifies the discriminatory power of the assay method, increasing the wettability of the powder mixtures. The crystalline form M of ROSC was recrystallized in our laboratory, and it showed lower solubility in water than amorphous solid. However, its dissolution properties were not influenced by SDS. These results are important to develop dissolution assays for other hydrophilic drugs with increased water solubility, once that dissolution media with surfactants increase the wettability of the formulations, leading to an overrated dissolution rate.


Subject(s)
Capsules/analysis , Dissolution/analysis , Rosuvastatin Calcium/analysis , Solubility , Chromatography, High Pressure Liquid/instrumentation , Dosage Forms
7.
Braz. J. Pharm. Sci. (Online) ; 55: e18129, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039036

ABSTRACT

A simple, sensitive, precise, accurate and robust high performance liquid chromatographic method has been developed for simultaneous estimation of saxagliptin (SAXA) and dapagliflozin (DAPA) in pharmaceutical formulation. Design of experiments (DoE) was applied for multivariate optimization of the experimental conditions of RP-HPLC method. Risk assessment was performed to identify the critical method parameters. Three independent factors; mobile phase composition, flow rate and column temperature were used to design mathematical models. Central composite design (CCD) was used to study the response surface methodology and to study in depth the effects of these independent factors. Desirability function was used to simultaneously optimize the retention time and resolution of SAXA and DAPA. The optimized and predicted data from contour diagram consisted of acetonitrile and ortho phosphoric acid (0.1%) in the ratio of 50:50 respectively, at a flow rate of 0.98 ml/min and column temperature 31.4 °C. Using these optimum conditions baseline separation of both drugs with good resolution and run time of less than 6 min were achieved. The optimized assay conditions were validated according to ICH guidelines. Hence, the results clearly showed that Quality by design approach could be successfully applied to optimize RP-HPLC method for simultaneous estimation of SAXA and DAPA.


Subject(s)
Pharmaceutical Preparations/classification , Chromatography, High Pressure Liquid/methods , Diabetes Mellitus, Type 2/classification , Tablets/administration & dosage , Dosage Forms , Process Optimization/methods
8.
Article in Korean | WPRIM | ID: wpr-786522

ABSTRACT

PURPOSE: This study aimed to investigate the characteristics of poisoning drug ingested by younger children, and to compare the clinical outcome by drug forms.METHODS: This was a retrospective analysis based on medical records from the Emergency Department based Injury In-depth Surveillance (EDIIS) registry in Korea from January to December 2015. Patients aged 7 years or younger visiting the emergency department (ED) with drug poisoning were included. We classified the forms of drugs as tablets or syrup, and analyzed the characteristics by size, color, and shape. In addition, clinical outcomes and ED length of stay were compared according to the drug forms.RESULTS: A total of 308 cases were collected, and 202 patients finally were analyzed. Tablets and capsules (TACs) were more common than syrup (67.3% vs. 32.7%). Regarding clinical outcomes, patients who took TACs had higher admission rate (17.6% vs. 7.6%, P = 0.040) without a significant difference in ED length of stay compared to those who took syrups. While commonly ingested drugs in TACs were hormones, sedative and analgesics, frequent drugs in syrup were antihistamines and cold drugs. In 136 case of TACs, median long and short axes were 0.85 cm (interquartile range [IQR], 0.7–1.1 cm) and 0.72 cm (IQR, 0.59–0.82 cm), respectively. Chromatic TACs were 80 cases (58.8%) and more common than achromatic TACs. Round shapes were preferred than angular ones (96.3% vs. 3.7%).CONCLUSION: In younger children poisonings, the TACs showed higher incidence and admission rate compared to syrups. Especially, chromatic TACs and round shapes were preferred. Therefore, drugs with these characteristics need to be stored more carefully.


Subject(s)
Analgesics , Capsules , Child , Dosage Forms , Drug Compounding , Emergency Service, Hospital , Histamine Antagonists , Humans , Incidence , Korea , Length of Stay , Medical Records , Poisoning , Retrospective Studies , Tablets
9.
Clin. biomed. res ; 38(1): 1-7, 2018.
Article in English | LILACS | ID: biblio-988442

ABSTRACT

Introduction: Pharmacotherapy is the main therapeutic resource for the management of diseases. However, the number of drugs prescribed, dose frequency, and mode of administration can make the treatment more complex and influence treatment outcomes. The aim of this study was to measure the complexity of prescribed medication regimens in primary health care (PHC) services in Ribeirão Preto, Brazil. Methods: This cross-sectional study included 1,009 participants: 889 from primary health units and 120 from family health units in Ribeirão Preto, Brazil. Treatment complexity was assessed using the Medication Regimen Complexity Index (MRCI). Results: MRCI mean scores were 12.5 points (SD = 9.3) and dose frequency was the major contributor to increase the score. The complexity of pharmacotherapy showed a significant correlation with the number of prescribed medications (r = 0.93, p < 0.01), but not with patients' age (r = 0.28, p < 0.01). There is also no difference in complexity between the sexes (p = 0.83) and the types of primary health care service (p = 0.31). An analysis of variance revealed that patients with lower levels of education receive more complex prescriptions (p < 0.01). Conclusions: The pharmacotherapy prescribed in PHC services from Ribeirão Preto, Brazil is complex, and there is a need to concentrate efforts and adopt strategies to simplify drug prescription without compromising patient's clinical status.


Subject(s)
Humans , Male , Female , Adolescent , Adult , Middle Aged , Young Adult , Drug Prescriptions , Primary Health Care , Dosage Forms , Drug Therapy, Combination , Medication Adherence , Socioeconomic Factors , Cross-Sectional Studies , Treatment Outcome
10.
Braz. J. Pharm. Sci. (Online) ; 54(4): e00228, 2018. tab, graf
Article in English | LILACS | ID: biblio-1001573

ABSTRACT

Dextromethorphan hydrobromide (DM) sustained release matrix pellets containing 10% w/w drug were prepared by an extrusion/spheronization technique. The effect of mixing different concentrations of ethyl cellulose (EC), hydroxypropyl methylcellulpse (HPMC K10), and Carbopol 934 with Avicel PH101 on the rheological properties of pellet wet mass was evaluated using mixer torque rheometry (MTR). The prepared pellets were characterized for size, drug content, and in-vitro DM release rate. The results showed that increasing the concentration of the hydrophobic polymer (EC) with Avicel PH101 decreased wet mass consistency, represented by mass mean line torque. Lower binder ratio was required for optimum wet massing, while mixing with swellable polymers (HPMC and Carbopol) caused a noticeable increase in both mean line torque and binder ratio. Combinations of HPMC and Carbopol at higher concentrations resulted in controlled in vitro release of DM from the prepared pellets. Furthermore, mathematical treatment of the in vitro release data of DM from the prepared pellets showed that all formulations except those containing 5% Carbopol plus 5% HPMC (F10) follow first order release. n values of these formulation were in the range of 0.09-0.40, which support an anomalous non-Fickian release.


Subject(s)
Dextromethorphan/analysis , Drug Implants/pharmacology , In Vitro Techniques , Dosage Forms
11.
Article in English | WPRIM | ID: wpr-716735

ABSTRACT

Nowadays antibiotic resistance is a worldwide serious problem that mainly affects public health. Omadacycline is a unique antibiotic which has two available dosage forms such as intravenous (IV) and oral that development for community-acquired bacterial infectious disease treatment. It is a modified form of older tetracycline at C-9 aminomethyl substituent of 6-member core ring of tetracycline. Modification form shows its activity against efflux pump and ribosomal protein protection mechanism of tetracycline resistance. Generally, omadacycline is effective against methicillin-resistant S. aureus (MRSA), Streptococcus pneumoniae, vancomycin-resistant Enterococcus (VRE), Legionella and Chlamydia spp. Efficacy, safety and tolerability profile of omadacycline those compares with recent antibiotics shows that omadacycline is less resistant than others. One derivative from tetracycline derivatives is 9-neopentylaminomethylminocycline called omadacycline was discovered and ongoing phase III clinical experiments as a therapy for acute bacterial skin and skin structure infections (ABSSSI) as well as community-acquired bacterial pneumonia (CABP). Omadacycline seems to be a strong drug candidate for future promising new antibacterial agent that is effective against ABSSSI and CABP.


Subject(s)
Anti-Bacterial Agents , Bacterial Infections , Chlamydia , Communicable Diseases , Dosage Forms , Drug Resistance, Microbial , Enterococcus , Legionella , Magic , Methicillin Resistance , Pneumonia, Bacterial , Public Health , Ribosomal Proteins , Skin , Streptococcus pneumoniae , Tetracycline , Tetracycline Resistance
12.
Rev. Asoc. Odontol. Argent ; 105(3): 116-122, sept. 2017. tab, graf
Article in Spanish | LILACS | ID: biblio-973106

ABSTRACT

Una de las principales preocupaciones de los pacientes que van a ser sometidos a un procedimiento odontológico es el dolor que dicho procedimiento pueda ocasionar. Por lotanto, lograr un control eficaz y seguro de ese dolor es una parte esencial de la práctica odontológica diaria. Los fármacos de primera elección para el tratamiento del dolor y el edemason, sin lugar a dudas, los antiinflamatorios no esteroideos(AINEs). Principios activos como el ibuprofeno (y sus congéneres) o sus derivados permiten controlar simultáneamente el dolor y el edema posquirúrgicos de una forma eficaz y segura. En muchas ocasiones, el AINE prescrito para mantener al paciente asintomático o con síntomas tolerables es suficiente. Sin embargo, cuando esto no ocurre, debemos recurrir a otrosfármacos, o realizar asociaciones con fármacos que complementen el efecto analgésico y trabajen logrando un sinergismo de potenciación que incremente el efecto buscado y disminuya los efectos adversos de cada una de las sustancias por separado, utilizando menores dosis. Un ejemplo comprobado de esas asociaciones es la de ibuprofeno con paracetamol. En el presente artículo se sugieren diversas estrategias pre- y posoperatorias para el manejo del dolor de origen inflamatorio, y un protocolo para su tratamiento.


Subject(s)
Humans , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Pain, Postoperative/drug therapy , Ibuprofen/pharmacology , Acetaminophen/pharmacology , Drug Combinations , Drug Synergism , Dosage Forms , Analgesics/pharmacology , Analgesics/pharmacokinetics , Analgesics/therapeutic use
13.
Braz. dent. j ; 28(4): 482-488, July-Aug. 2017. tab, graf
Article in English | LILACS | ID: biblio-888662

ABSTRACT

Abstract The present study evaluated the effect of NaF and CPP-ACP/NaF varnishes to reduce erosion produced by soft drink (SD) combined or not with pediatric liquid medicine. Enamel specimens were pre-treated with fluoride varnish, according to the following groups: NaF varnish (Duraphat®) or CPP-ACP/NaF varnish (MI varnishTM). Two types of erosive cycles were made: by soft drink erosion (SDE) or by pediatric liquid medicine plus soft drink erosion (PLM/SDE). Bovine enamel specimens were randomly assigned in six groups (n=10): G1=NaF + SDE; G2=CPP-ACP/NaF + SDE; G3=Distilled and deionized (DD) water + SDE; G4=NaF + PLM/SDE; G5=CPP-ACP/NaF + PLM/SDE and G6=DD water + PLM/SDE. Before treatments, the sample surface was divided in two areas (unexposed area-UA and exposed area-EA). The specimens were evaluated by 3D non-contact profilometry technique to determinate tooth structure loss (TSL) and surface roughness (Sa). Scanning electron microscopy (SEM) analysis was also performed. After SDE, G2 presented the lowest TSL values compared to G3 (p=0.008). G1 and G2 did not differ between them (p=0.203) and no groups differed among them despite Sa. Regarding TSL and Sa, G4 and G5 differed from G6 (p=0.0001), but not between them (p=1.00). Examining 3D and SEM images, the greatest differences between UA and EA were observed for G3 and G6. CPP-ACP/NaF varnish seems to be a promising treatment to reduce enamel loss from the erosion produced by a soft drink. Both varnishes also showed capacity to reduce TSL and Sa after erosion by soft drink combined to pediatric liquid medicine.


Resumo O presente estudo avaliou o efeito dos vernizes de NaF e CPP-ACP/NaF na redução da erosão promovida por refrigerante e associada a um medicamento líquido pediátrico. Os espécimes de esmalte foram pré-tratados com verniz fluoretado, de acordo com o grupo de alocação: verniz NaF (Duraphat®) ou verniz CPP-ACP NaF (verniz MITM). Dois tipos distintos de desafio erosivo foram realizados: erosão com refrigerante (ER) ou erosão com medicamento líquido pediátrico e refrigerante (MLP/ER). Espécies de esmalte bovino foram aleatorizados em seis grupos (n=10): G1 = NaF + ER; G2 = CPP-ACP/NaF + ER; G3 = Água destilada e deionizada (DD) + ER; G4 = NaF + MLP/ER; G5 = CPP-ACP/NaF + MLP/ER e G6 = DD água + MLP/ER. Antes dos tratamentos, a superfície das amostras foi dividida em duas áreas (não exposta-NE e área exposta-AE). Os espécimes foram avaliados pela técnica de perfilometria 3D de não-contato para determinar a perda de estrutura dentária (PED) e a rugosidade superficial (RS). A microscopia eletrônica de varredura (MEV) também foi utilizada. Após ER, G2 apresentou os menores valores de PED comparado ao G3 (p=0,008). G1 e G2 não diferiram entre si (p=0,203) e não houve diferença entre os grupos no que diz respeito a RS. Os resultados de PED e RS para a MLP/ER mostraram que G4 e G5 diferiram de G6 (p=0,0001), mas não diferiram entre si (p=1,00). Examinando as imagens 3D da perfilometria e de MEV, as maiores diferenças entre UA e EA foram observadas para G3 e G6. O verniz CPP-ACP/NaF parece ser um tratamento promissor para reduzir a perda de esmalte por erosão produzida por refrigerante e ambos os vernizes mostraram capacidade em reduzir a PED e RS após erosão com medicamento líquido pediátrico associado a refrigerante.


Subject(s)
Humans , Animals , Child , Cattle , Tooth Erosion/etiology , Carbonated Beverages/adverse effects , Fluorides, Topical/pharmacology , Drug Therapy , Tooth Erosion/prevention & control , Microscopy, Electron, Scanning , Dosage Forms
14.
Rev. bras. anestesiol ; 67(3): 231-237, Mar.-June 2017. tab, graf
Article in English | LILACS | ID: biblio-843392

ABSTRACT

Abstract Background and objectives: Tramadol hydrochloride is a centrally-acting synthetic opioid analgesic binding to specific opioid receptors. It is used in the management of chronic pain and is recommended as first line drug in the treatment of postoperative or orthopedic injury induced acute pain. The present work is designed to prepare and evaluate mucoadhesive buccal film of tramadol hydrochloride as a novel form of prolonged analgesia for patients with orthopedic injuries. Methods: Buccal films of tramadol hydrochloride were prepared by solvent casting method. The prepared films were evaluated for the various evaluation parameters like thickness, surface pH, weight uniformity, content uniformity, folding endurance, swelling index, in vitro drug release study, in vitro test for mucoadhesion and in vivo studies (primary mucosal irritancy test and analgesic activity). Results: All the formulations exhibited good results for physicochemical characterizations. In in vitro drug release study the films exhibited controlled release more than 12 hours. The formulation BFT2 (containing chitosan and PVP K-90) showed no irritant effect on buccal mucosa and elicit the significant in vivo analgesic activity with 57.14% analgesia against that of standard (61.04%). It was concluded that the mucoadhesive films of tramadol hydrochloride can be effectively used to alleviate the severe pain of orthopedic injuries with prompt onset and prolonged action.


Resumo Justificativa e objetivos: O cloridrato de tramadol é um analgésico opioide de ação central que se liga a receptores opioides específicos. É usado no tratamento de dor crônica e recomendado como fármaco de primeira linha para o tratamento no pós-operatório ou em dor aguda induzida por lesão ortopédica. O presente estudo visa a preparar e avaliar o filme bucal mucoadesivo de cloridrato de tramadol como uma nova forma de analgesia prolongada para pacientes com lesões ortopédicas. Método: Filmes bucais de cloridrato de tramadol foram preparados pelo método de evaporação de solvente. Os filmes preparados foram avaliados para os vários parâmetros de avaliação, como espessura, pH da superfície, uniformidade do peso, uniformidade do conteúdo, resistência a dobras, índice de intumescimento, estudo de liberação da droga in vitro, teste in vitro para mucoadesão e estudos in vivo (teste de irritação da mucosa primária e atividade analgésica). Resultados: Todas as formulações apresentaram bons resultados para caracterizações físico-químicas. Em estudo de libertação de droga in vitro, os filmes exibiram liberação controlada por mais de 12 horas. A formulação de BFT2 (com quitosana e PVP K-90) não mostrou efeito irritante sobre a mucosa bucal e provocou uma atividade analgésica significativa in vivo com 57,14% de analgesia versus a do padrão (61,04%). Concluiu-se que os filmes mucoadesivos de cloridrato de tramadol podem ser usados eficazmente para aliviar a dor intensa de lesões ortopédicas com início rápido e ação prolongada.


Subject(s)
Animals , Male , Rats , Tramadol/administration & dosage , Adhesives , Drug Delivery Systems , Pain Management/methods , Analgesics, Opioid/administration & dosage , Treatment Outcome , Rats, Wistar , Dosage Forms , Mouth Mucosa
15.
Rev. Col. Bras. Cir ; 44(2): 116-124, Mar.-Apr. 2017. tab
Article in English | LILACS | ID: biblio-842660

ABSTRACT

ABSTRACT Objective : to evaluate pain in patients with lower limb venous ulcer who used non-adherent Ibuprofen foam dressing (IFD). Methods : we conducted a prospective study of patients with lower limb venous ulcers treated from April 2013 to August 2014. We used the Numerical Scale and McGill Pain Questionnaire, performing the assessments at the moment of inclusion of the patient in the study and every eight days thereafter, totaling five consultations. We divided the patients into two groups: 40 in the Study Group (SG), who were treated with IFD, and 40 in the Control Group (CG), treated with primary dressing, according to tissue type and exudate. Results : at the first consultation, patients from both groups reported intense pain. On the fifth day, SG patients reported no pain and the majority of CG reported moderate pain. Regarding the McGill Pain Questionnaire, most patients of both groups reported sensations related to sensory, affective, evaluative and miscellaneous descriptors at the beginning of data collection; after the second assessment, there was slight improvement among the patients in the SG. After the third consultation, they no longer reported the mentioned descriptors. CG patients displayed all the sensations of these descriptors until the fifth visit. Conclusion : non-adherent Ibuprofen foam dressing is effective in reducing the pain of patients with venous ulcers.


RESUMO Objetivo: avaliar a dor em pacientes portadores de úlcera venosa de membros inferiores que utilizaram curativo de espuma não aderente com Ibuprofeno (CEI). Métodos: estudo prospectivo de pacientes portadores de úlceras venosas de membros inferiores tratados no período de abril de 2013 a agosto de 2014. Foram utilizados os questionários Escala Numérica e Questionário de Dor de McGille, as avaliações eram feitas no momento da inclusão do paciente no estudo e a cada oito dias, totalizando cinco consultas. Os pacientes foram divididos em dois grupos: 40 no Grupo Estudo (GE), que foram tratados com CEI, e 40 no Grupo Controle (GC), tratados com curativo primário, conforme o tipo de tecido e exsudato. Resultados: na primeira consulta os pacientes de ambos os grupos relataram dor intensa. No quinto dia os pacientes do GE relataram ausência de dor e a maioria do GC relatou dor moderada. Com relação ao Questionário de Dor de McGill, a maioria dos pacientes de ambos os grupos, no início da coleta de dados, relataram sensações relacionadas aos descritores sensorial, afetivo, avaliativo e miscelânea, sendo que entre os pacientes do GE houve discreta melhora após a segunda consulta. Após a terceira consulta já não referiram os descritores citados. Os pacientes do GC manifestaram todas as sensações desses descritores até quinta a consulta. Conclusão: o curativo de espuma não aderente com Ibuprofeno é eficaz na redução da dor de pacientes portadores de úlceras venosas.


Subject(s)
Humans , Male , Female , Aged , Aged, 80 and over , Bandages , Varicose Ulcer/therapy , Ibuprofen/administration & dosage , Analgesics, Non-Narcotic/administration & dosage , Pain Management , Pain/etiology , Varicose Ulcer/complications , Pain Measurement , Prospective Studies , Dosage Forms , Middle Aged
16.
Infection and Chemotherapy ; : 135-139, 2017.
Article in English | WPRIM | ID: wpr-105544

ABSTRACT

The posaconazole tablet formulation was developed to have improved bioavailability compared to the oral suspension. Here, we compared posaconazole plasma concentration (PPC) with the posaconazole oral suspension versus the tablet in Korean patients undergoing remission induction chemotherapy for hematologic malignancies. PPC was measured at 3, 8, and 15 days of treatment with the oral suspension (174 patients) or the tablet (40 patients). At all time-points, mean PPC was significantly higher with the tablet compared to the oral suspension. Our findings suggest that posaconazole tablets generate an optimal PPC earlier and in more patients than the oral suspension among Korean patients.


Subject(s)
Antifungal Agents , Biological Availability , Dosage Forms , Drug Therapy , Hematologic Neoplasms , Humans , Plasma , Remission Induction , Tablets
17.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (1): 149-154
in English | IMEMR | ID: emr-185752

ABSTRACT

The indole alkaloid Yohimbine has been used for over two centuries in the treatment of erectly dysfunction. Several formulations containing yohimbine salts, yohimbe bark power or extract are marketed worldwide. Determination of the amount of yohimbine in such formulation is a challenging task due to their complex nature. Extraction followed by acid-base purification resulted in a relatively pure alkaloids containing fractions. The exact amounts of yohimbine free base in different formulations were determined by densitometric HPTLC validated methods using silica gel TLC plates. Standard curve for yohimbine was generated using yohimbine hydrochloride subjected to the same acid-base treatment as the used samples. All formulations found to contain yohimbine though some with less concentration than the labeled amount


Subject(s)
Chromatography, Thin Layer , Adrenergic alpha-2 Receptor Antagonists/analysis , Calibration , Reproducibility of Results , Densitometry , Dosage Forms
18.
Braz. J. Pharm. Sci. (Online) ; 53(2): e15154, 2017. tab, graf
Article in English | LILACS | ID: biblio-839485

ABSTRACT

ABSTRACT Diclofenac sodium (DS) and diacerein (DC) have emerged as a potential combination therapy for the treatment of knee osteoarthritis. Therefore a validated analytical method is essential for the simultaneous estimation of both from combined dosage form. A ratio derivative spectrophotometric and a chromatographic technique have been developed for the simultaneous determination of DS and DC. The quantification was done at 263.00 nm for DC and 304.50 nm for DS in the first method, whereas 257 nm for DC and at 274 nm for DS for LC-DAD analysis in chromatographic method using acetate buffer and methanol as the mobile phase at a flow-rate 0.50 mL/min. Both of these methods are found to be linear in the concentration range under study with r2 value 0.999 and 0.996 for DS and DC respectively in ratio derivative spectroscopy and 0.998 and 0.999 for DS and DC respectively in LC-DAD study. Both of these methods are found to be accurate and precise, though greater robustness and precision is observed with chromatographic analysis over the ratio derivative spectroscopy. Statistically there was no significant difference between proposed ratio derivative spectrophotometric and LC-DAD methods.


Subject(s)
Comparative Study , Laboratory and Fieldwork Analytical Methods , Diclofenac/analysis , Spectrum Analysis/methods , Chromatography, High Pressure Liquid/instrumentation , Validation Study , Dosage Forms/standards
19.
Braz. J. Pharm. Sci. (Online) ; 53(4): e00176, 2017. tab, graf
Article in English | LILACS | ID: biblio-889425

ABSTRACT

ABSTRACT Meloxicam (MLX) is a non-steroidal, anti-inflammatory drug that is prescribed in the treatment of rheumatoid arthritis and osteoarthritis. MLX is practically insoluble in water and exhibits a slow onset of action. In this study, MLX solid dispersions (MLX SDs) were prepared to improve the water solubility of this poorly water-soluble drug. Then orally disintegrating tablets (ODT) of MLX were developed using MLX SD to decrease the onset of action of this drug. MLX, poloxamer 188, and crospovidone of different ratios were melted in molten poloxamer 188 as a hydrophilic carrier. The optimum SD with the highest saturation solubility in water (13.09±0.34 microgram/mL) consisting of MLX: poloxamer 188: crospovidone in the ratio of 1:2:0 was used for the preparation of MLX ODTs. MLX ODTs were prepared by the direct compression method and optimized by the 23 factorial design. The effect of the superdisintegrant concentration, the mannitol-avicel ratio, and the level of compression force on the disintegration time, hardness, and percent of dissolved MLX from MLX ODTs after 30 min was evaluated. DSC and XRD analysis approved an amorphous form of MLX in SDs. The optimized ODT formulation containing 10% of superdisintegrant, and mannitol and avicel in the ratio of 4:1 respectively was compressed using a high level of compression force. The optimized ODT showed hardness (34.37±2.1 N) and friability (1.26±0.04%). This formulation showed a rapid disintegration in 12.66±2.5 seconds, which 82.66±5.1% of the MLX released within 30 min. MLX ODTs, prepared from MLX SD, could be introduced as a suitable dosage form of MLX with improved solubility and the onset of action.


Subject(s)
Solubility , Tablets/analysis , Pharmaceutical Preparations/chemical synthesis , Osteoarthritis/prevention & control , Arthritis, Rheumatoid/prevention & control , Dosage Forms
20.
Braz. J. Pharm. Sci. (Online) ; 53(4): e00216, 2017. tab, graf
Article in English | LILACS | ID: biblio-889428

ABSTRACT

ABSTRACT The search for new pharmaceutical dosage forms and different drug delivery systems already used in therapeutics is a global trend, serving as an opportunity to expand the portfolio for the pharmaceutical industry. In this context, multiparticulate systems, such as pellets, granules, and minitablets, represent an attractive alternative, given the range of possibilities they provide. Among the methods used in the production of these systems, we highlight the process of extrusion-spheronization for pellet manufacture, wet granulation and hot-melt extrusion for the obtention of granules, and direct compression for minitablets. Although highly versatile, depending on the technology chosen, many processes and formulation variables can influence the ensuing stages of manufacture, as well as the final product. Therefore, the characterization of these small units is of fundamental importance for achieving batch homogeneity and optimal product performance. Analyses, including particle size distribution, morphology, density, porosity, mechanical strength and disintegration, are example tests used in this characterization. The objective of this review was to address the most widely used tests for the physical evaluation of multiparticulate systems.


Subject(s)
Pharmaceutical Preparations , Physical Phenomena/classification , Drug Compounding/statistics & numerical data , Straining of Liquids , Drug Delivery Systems , Dosage Forms , Test Taking Skills/methods
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