Suspensão oral de rutina interfere na hiperplasia hepática em ratos / Oral rutin suspension intervene in hepatic hyperplasia in rats

ABSTRACT BACKGROUND: Rutin is a flavonol glycoside that can be found in a wide variety of vegetables and has activity, anti-cancer, anti-inflammatory and anti-diabetic properties. OBJECTIVE: This study investigated the effect of rutin oral administration on Wistar rats submitted to hepatic hyperplasia after partial hepatectomy (PH). METHODS: To achieve this, we considered the analysis of hepatic hyperplastic and plasma biochemical activity of Wistar rats, subjected to treatment with rutin 40 mg/kg/day for 10 days in group 1 (G1) or saline in group 2 (G2), followed by partial hepatectomy. RESULTS: The results indicated an increase in the number of mitoses after 24 hours and 48 hours (P=0.0022 and P=0.0152, respectively) of PH in the group that received rutin, as well as an increase in AST serum levels after 24 hours (P=0.0159) and 48 hours (P=0.0158) and alkaline phosphatase after 24 hours (P=0.015) in the same group, in relation to the respective controls. The group that received rutin showed a more evident variation than the control group when comparing the 24 hour and 48 hour results regarding AST, number of mitoses and number of apoptosis (P<0.005). CONCLUSION: It was concluded that rutin intervened in hepatic hyperplasia after 24 hours and 48 hours of PH, favoring hepatic hyperplasia.

RESUMO CONTEXTO: A rutina é um flavonoide que pode ser encontrado em grande variedade de vegetais e apresenta atividades anticâncer, anti-inflamatória e antidiabética. OBJETIVO: O objetivo deste estudo foi investigar o efeito da administração oral de rutina sobre a hiperplasia hepática em ratos Wistar submetidos à hepatectomia parcial. MÉTODOS: Foi realizada a análise da hiperplasia hepática e da bioquímica plasmática dos ratos Wistar tratados com rutina 40 mg/kg por 10 dias no grupo 1 (G1) ou salina no grupo 2 (G2), seguido da hepatectomia parcial. RESULTADOS: Os resultados indicaram aumento do número de mitoses após 24 e 48 horas (P=0,0022 e P=0,0152, respectivamente) da hepatectomia parcial no grupo que recebeu rutina, além de um aumento nos níveis séricos de AST após 24 horas (P=0,0159) e 48 horas (P=0,0158) e de fosfatase alcalina após 24 horas (P=0,015) no mesmo grupo, em relação aos respectivos controles. O grupo que recebeu rutina mostrou variação mais evidente do que o grupo controle quando se comparou os resultados de 24 horas e 48 horas em relação a AST, número de mitoses e número de apoptoses (P<0,005). CONCLUSÃO: Foi possível concluir que a rutina interferiu na hiperplasia hepática após 24 e 48 horas após a hepatectomia parcial, favorecendo a hiperplasia hepática.

Evidencing the impact of drug store storage conditions on the quality and stability of amoxicillin powders for oral suspension marketed in Peru

One of the most promising strategies against antimicrobial resistance is to strengthen the monitoring of the quality of medicines in middle- and low-income countries. In Peru, several drug alerts related to quality defects of one of the most commonly used antibiotics, amoxicillin powder for oral suspension, have been reported. This study compared the quality and stability of three amoxicillin powders for oral suspension manufactured by national laboratories and stored for 1 and 3 months in drug stores of populated cities located in the coast, jungle, and the Andes. Esthetic appeal evaluation, delivered volume and pH, and drug content determination were conducted with non-reconstituted and reconstituted samples. In-use stability was also tested after 1 week of refrigeration. All the results were within the specifications of the United States Pharmacopeia for the duration of the study but after 3 months of storage in Tarapoto, clusters formation, smell and taste changes, and a statistically significant reduction in pH and drug content were observed. Based on this and taking also into account the factors affecting the stability of this dosage form of amoxicillin, we can assume these variations are associated with high temperatures and relative humidities during longer periods of storage in drug stores.

Development of an oral suspension containing dry extract of Aleurites moluccanus with anti-inflammatory activity

Abstract Aleurites moluccanus L. (Willd.), Euphorbiaceae, is a tree that is native to Indonesia and India. Various parts of this tree are commonly used in traditional medicine to treat pain, fever, inflammation, hepatitis, gastric ulcer and other ailments. An oral suspension containing dried extract of A. moluccanus was developed and in vivo anti-inflammatory activity was evaluated. Extract 100 and 50 mg/ml loaded oral suspensions were prepared using different suspending agents. The formulations were analysed by their appearance, pH, density, redispersion time, rate of settling, rheological behaviour, distribution of particle size and zeta potential. The dose uniformity was determined by measuring the content of total phenolic compounds expressed in swertisin by a validated HPLC method, as well as the dissolution profile. The stability of oral suspensions was analysed in accelerated studies (40 °C for 6 months). The anti-inflammatory activity was analysed using an in vivo paw oedema model. The taste and odour of the suspensions were shown to be characteristic of the extract. Carmellose sodium (CS; 0.5%) and microcrystalline cellulose and carmellose sodium mixture (MCCS; 1%) showed better physical behaviour. The content of total phenolic compounds was 1.6 mg/ml and approximately 100% of the total phenolic compounds dissolved within 10 min. During the stability study, the formulations were approved by their physical–chemical properties and were shown to lose 12–14% of total phenolic compounds at 40 °C after 6 months. Suspensions containing 50 mg/ml of standardised dried extract inhibited around 35 ± 7.6% of paw oedema. Formulations containing CS showed more anti-inflammatory activity. Suspensions containing dry extract of A. moluccanus were successfully obtained and showed physical and physical–chemistry properties that were appropriate and characteristic of this dosage form, suitable for administration in paediatric and elderly populations, making this an alternative to tablets.

Efficacy and safety of oxcarbazepine oral suspension in epileptic children:a clinical study / 西安交通大学学报(医学版)

ABSTRACT:Objective To study the efficacy and safety of oxcarbazepine (OXC)oral suspension on children with different kinds of epilepsy.Methods A total of 83 children with epilepsy were selected from the Pediatric Department of the First Affiliated Hospital of Xi’an Jiaotong University and Xi’an Children’Hospital from June 201 1 to June 2014.They were treated with OXC monotherapy or adjunctive therapy.Use open-label and self-contrast method.The initial dose of OXC was 8 -10 mg/(kg·d),and then was added 10 mg/(kg·d)per 7 days until it reached the minimum effective dose.Generally,the maintenance dose was about 20-40 mg/(kg·d).The follow-up duration was 6 - 12 months.Results 83 cases were eventually included and 5 cases withdrew.We elvaluated the efficacy every 3 months.The results were as follows:the first stage (1,2,3 months)resulted in a 41.0% of full control rate and a 71.8% of total effective rate;the second stage (4,5,6 months)resulted in a 46.2% of full control rate and a 76.9% of total effective rate;the third stage (7,8,9 months)resulted in a 59.0%of full control rate and a 79.5% of total effective rate.There were no significant differences in the efficacy of the three stages.54 cases with partial seizures resulted in a 59.3% of full control rate and a 79.6% of total effective rate;24 cases with generalized seizure resulted in a 45.8% of full control rate and a 62.5% of total effective rate. There was no statistical significant difference in the efficacy of the two seizure types.43 cases with monotherapy resulted in a 58% of full control rate and a 79% of total effective rate,35 cases with add-on therapy resulted in a 40.0% of full control rate and a 57.1% of total effective rate.24 cases with < 2 resulted in a 41.7% of full control rate and a 62.5% of total effective rate,54 cases with 2-6 resulted in a 59.3% of full control rate and a 83.3% of total effective rate.14 cases of children were reported to have at least one adverse drug reactions,the specific symptoms included emotional instability unstable, hypohidrosis, somnolence, dizzness, headache, vomiting, urorrhea,lack of appetite,aggressive behavior and hypomnesia.Adverse reactions were mild and most of them could subside over time.Conclusion OXC oral suspension has a good efficacy and safety when treating children with partial seizures or generalized tonic-clonic seizures of epilepsy.

Compound ocimum oil oral suspension in the treatment of 382 children with acute diarrhea (Piweixure Syndrome) / 中国基层医药

Objective To investigate the efficacy and safety of compound ocimum oil oral suspension in the treatment of children with acute diarrhea(Piweixure Syndrome).Methods 382 children with acute diarrhea(Piweixure Syndrome) were selected for the multi center and open clinical trial.All patients was treated by compound ocimum oil oral suspension based on age and weight,6 months below 3mL thrice a day,6-＜ 12months 5mL thrice a day,12-＜24 months 10mL thrice a day,24 months upper 20-40 mL thrice a day.The course was three days.The efficacy and safety was observed.Results The total efficiency was 93.98％,there were 274 cases with marked effect and 85 case with effective in analysis on clinical efficacy.There were significant differences between before and after therapy on symptoms and signs as defecation frequency,defecation characters and defecation disesthesia (x2 =467.43,524.51,263.03,all P ＜ 0.05).Conclusion Compound ocimum oil oral ouspension in the treatment of children with acute diarrhea(Piweixure Syndrome) has definite effect and safety.It would be applied to clinical wildly with advantages as shorten the course,decreased diarrhea times and improved clinical symptoms.

Development and validation of a dissolution method using HPLC for diclofenac potassium in oral suspension

The present study describes the development and validation of an in vitro dissolution method for evaluation to release diclofenac potassium in oral suspension. The dissolution test was developed and validated according to international guidelines. Parameters like linearity, specificity, precision and accuracy were evaluated, as well as the influence of rotation speed and surfactant concentration on the medium. After selecting the best conditions, the method was validated using apparatus 2 (paddle), 50-rpm rotation speed, 900 mL of water with 0.3% sodium lauryl sulfate (SLS) as dissolution medium at 37.0 ± 0.5°C. Samples were analyzed using the HPLC-UV (PDA) method. The results obtained were satisfactory for the parameters evaluated. The method developed may be useful in routine quality control for pharmaceutical industries that produce oral suspensions containing diclofenac potassium.

O presente estudo descreve o desenvolvimento e validação de um método de dissolução in vitro para avaliação da liberação de diclofenaco potássico suspensão oral. O teste de dissolução foi desenvolvido e validado de acordo com as diretrizes internacionais. Parâmetros como linearidade, especificidade, precisão e exatidão foram avaliados, bem como a influência da velocidade de rotação e a concentração de tensoativono meio. Depois de selecionar as melhores condições, o método foi validado usando o aparato 2 (pás), velocidade de rotação de 50 rpm, 900 mL de água com 0,3% de lauril sulfato de sódio (LSS) como meio de dissolução a 37,0 ± 0,5 ºC. As amostras foram analisadas pelo método de CLAE-UV (PDA). Os resultados obtidos foram satisfatórios para os parâmetros avaliados. O método desenvolvido pode ser útil na rotina de controle de qualidade para as indústrias farmacêuticas que produzem suspensões orais contendo diclofenaco potássico.

A simple method for the quantification of diclofenac potassium in oral suspension by high-performance liquid chromatography with UV-detection

A rapid, simple and low cost method was developed to determine diclofenac potassium (DP) in oral suspension, using a reverse-phase column (C8, 150 mm x 4.6 mm, 5 µm), mobile phase containing methanol/buffer phosphate (70:30 v/v, pH 2.5), at a flow rate of 1.0 mL/min, isocratic method, and ultraviolet detection at 275 nm. A linear response (r = 1.0000) was observed in the range of 10.0-50.0 µg/mL. Validation parameters such as linearity, specificity, precision, accuracy and robustness were evaluated. The method presented precision (repeatability: relative standard deviation = 1.21% and intermediate precision: between-analyst = 0.85%). The specificity of the assay was evaluated by exposure of diclofenac potassium under conditions of stress such as hydrolysis, photolysis, oxidation and high temperature. The method presented accuracy values between 98.28% and 101.95%. The results demonstrate the validity of the proposed method that allows determination of diclofenac potassium in oral suspension and may be used as an alternative method for routine analysis of this product in quality control.

Desenvolveu-se método simples, de baixo custo para determinar o diclofenaco potássico (DP) em suspensão oral, usando coluna de fase reversa (C8, 150 mm x 4,6 mm, 5 µm), fase móvel contendo metanol/tampão fosfato (70:30 v/v, pH 2,5), com fluxo de 1,0 mL/min, método isocrático e detecção no ultravioleta a 275 nm. Observou-se resposta linear (r = 1,0000) na faixa de 10,0-50,0 µg/mL. Avaliaram-se parâmetros de validação, como linearidade, especificidade, precisão, exatidão e robustez. O método apresentou precisão (repetibilidade: desvio padrão relativo = 1,21% e precisão intermediária: entre analista = 0,85%). A especificidade do ensaio foi avaliada pela exposição do diclofenaco potássico a condições de estresse, tais como hidrólise, fotólise, oxidação e alta temperatura. O método apresentou valores de exatidão entre 98,28% e 101,95%. Os resultados mostram a validade do método proposto, que permite a determinação de diclofenaco potássico em suspensão oral e pode ser utilizado como alternativa para análise de rotina desse produto no controle de qualidade.