Wang, Zheng-Hua; Hong, Mo; Sun, Xiao-Yu; He, Gui-Yuan
Alpinetin, a type of novel plant flavonoid derived from Alpinia katsumadai Hayata, has been demonstrated to exhibit multiple biochemical and pharmacological activities. The phenyl hydroxyl group existed in alpinetin is susceptible to the glucuronidation catalyzed by UDP-glucuronosyltransferase (UGT).
The aim of the present study is to develop a sensitive and specific ultra-fast liquid chromatography (UFLC)-mass spectrum (MS) method to determine the glucuronidation activity of alpinetin in the liver microsomes obtained from different species, including human liver microsomes (HLMs), rat liver microsomes (RLMs), mice liver microsomes (MLMs), and dog liver microsomes (DLMs). The alpinetin’s glucuronide was purified, and the structure was elucidated...
Chelles, Daniel R.; Marins, Eugênio R.; Legey, Ana P.; Mol, Atonio C.A.; Santos-Oliveira, Ralph
Hospitals nuclear pharmacies are sectors related to research, education and assistance of pharmacists and physicians, specially the ones who work with nuclear pharmacy. The education in nuclear pharmacy is one of the most important aspects in this field. Due to the hard conditions in operating nuclear pharmacies (i.e. dose exposition, radiation protection procedures) it is difficult in most of the cases show to the students this environment. An intelligent and innovative form to dribble this obstacle is the association of new technologies, like virtual reality to educate without expose the students to dangerous situation inherent to the radioisotope manipulation. In...
Mezadri, Telmo. J.; Tames, David R.; Reis, Renata K.T.; Ortolan, Xana R.
The objective of this work was to study the effects of green propolis on skin wounds in diabetic rats. We used 10 animals, creating two wounds of 5 mm in diameter on the dorsal region, using a punch.
The left wounds were treated topically with Brazilian green propolis (5 %) while the right wounds received nothing. The tissue repair was evaluated in microscopy after 72 h. The results showed similar numbers of leukocytes and macrophages, however the number of fibroblasts, cell density and fibrillogenesis were increased in the experimental group, indicating the action of propolis on the skin wounds.
Nogueira, Thaísa A.; Barbosa, Leandro A.; Calili-Elias, Sabrina
Informing patients about rational drug use is necessary when therapies involve medications with adverse effects that can compromise treatment adherence. The aim of the present study was to evaluate the importance of the pharmaceutical professional in home visits. The study focused on a Palliative Care Unit Home Care Program, which orients patients and/or caregivers about home drug use. Paid pharmaceutical visits were conducted among 47 patients. During the first visit, incorrect medication prescriptions were observed for 21 patients (61.7 %); after subsequent visits, the average rate of correct prescription was 75 %. The present study observed a need for a...
Andrade, Fernando C.; Mota, Marcelo M.; Barreto, André S.; Sousa, Damião P.; Quintans Júnior, Lucindo José; Santos, Márcio R.V.
Cardiovascular effects induced by citronellal in rats were investigated in this study. In LNAME hypertensive rats, the oral acute administration of citronellal (200 mg/kg) was able to significantly reduce the blood pressure. In normotensive rats, citronellal (5-40 mg/kg, i.v.) induced hypotension, which was not affected by pre-treatment with atropine, hexamethonium, L-NAME or indomethacin, and bradycardia, which was abolished by atropine and hexamethonium, but not by L-NAME or indomethacin. ECG records revealed that citronellal induced sinoatrial block, which was abolished after atropine. In intact rings of rat mesenteric artery pre-contracted with phenylephrine (10 μM), citronellal (10 –6 to 10 –1 M)...
Tariq, Imran; Saeed-El-Hassan, Syed; Mateen, Omer; Karim, Sabiha; Atif Raza, Syed; Farhan Sohail, Muhammad
The present study was designed to evaluate the prescribing trend among the tuberculosis (TB) patients in different hospitals of Pakistan. In this study under directly observed therapy (DOT) programme, 38 patients including adults and children of both sexs who admitted suffering with either pulmonary or extra pulmonary TB, were selected. The majority of the patients were from rural areas (64 %) and the rest of patients from urban cities. The selected patients included both of initial phase (39 %) and continuation phase (61 %) and were receiving once daily dosing of rifampicin, isoniazid, pyrazinamide, and ethambutol combination (RHZE), and ethambutol...
Zhao, Hua-Dong; Bao, Guo-Qiang; He, Xian-Li; Wu, Tao; Wang, Cheng-Guo; Wang, Sheng-Zhi; Zang, Li; Lu, Jian-Guo; Du, Xi-Lin
UDP-glucuronosyltransferase (UGT) 1A1, one of the most important UGT isoforms, can metabolize a variety of endogenous substances and xenobiotics. UGT1A1-catalyzed glucuronidation reaction plays a key role in many clinical events, including Gilbert syndrome and irrinotecan-induced diarrhea toxicity. The present study aims to investigate the inhibition of UGT1A1 by levothyroxine which is clinically used to treat thyroid hormone deficiency, and occasionally to prevent the recurrence of thyroid cancer.
The recombinant UGT1A1was used as enzyme source, and 4-methylumbelliferone (4-MU) was utilized as a non-specific probe substrate. The results showed that levothyroxine inhibited the UGT1A1-catalyzed 4- MU glucuronidation in a dose-dependent manner. Furthermore, Lineweaver-Burk...
Ahmad, Maqsood; Syed, Nawazish-i-Husain; Akhtar, Muhammad; Erum, Alia; Mahmood, Qaisar; Alamgeer, Qaisar
Berberis lycium Royle is used in folk medicines for treating various ailments however it has not been investigated in cardiac problems at pharmacological level. Here, iono- and chronotropic effects of B. lycium root bark’s aqueous extract and berberine were studied on frog-heart. Present data showed that aqueous extracts of B. lycium and berberine exhibited dose-dependent negative chronotropic and ionotropic effects and at higher doses both caused a heart block. Berberine also displayed a positive ionotropic effect but at very low doses. Diltiazem did not antagonize positive ionotropic effect of berberine indicating that this activity is independent of L-type calcium channels,...
Jiang, Xiaofei; Zhan, Peng; Liu, Xinyong; Clercq, Erik de
The development of novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosterism principle, two novel 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives have been designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. The results indicate that these compounds show good activities against HIV-1. Especially, compound 9B (EC50 = 0.019 μM) was more effective than the reference drugs nevirapine and delavirdine.
Vieira, Daniela C.M.; Ricarte, Patrícia C.; Salgado, Hérida R.N.
The validation of a microbiological assay, applying agar diffusion method for determination of the active of cefuroxime in power for injection, is described. Using a strain of Micrococcus luteus ATCC 9341 as the test organism, cefuroxime was measured in concentrations ranging from 30.0 to 120.0 μg/mL.
The method validation showed that it is linear (r = 0.9999), precise (relative standard deviation = 0.37 %) and accurate (it measured the added quantities). Microbiological assay is satisfactory for quantitation of cefuroxime in powder for injection and the validity of the proposed bioassay, which is a simple and a useful alternative methodology for cefuroxime...
Wang, Chuan-Qiang; Song, Ming-Zhu; Zhu, Hou-Wei; Yi, Jia-Jun; Luan, Ming-Chun; Shi, Ai-Yuan; Qu, Yan-Qing
Levothyroxine, a synthetic form of thyroid hormone, has been clinically used to treat thyroid hormone deficiency. UDP-glucuronosyltransferases (UGTs) are important phase II drug-metabolizing enzymes, and UGTs-inhibition based drug-drug interaction has been widely reported. The aim of the present study is to investigate the inhibitory effect of levothyroxine towards UGT1A6-catalyzed 4-methylumbelliferone (4-MU) glucuronidation. The results showed that levothyroxine inhibited UGT1A6-catalyzed 4-MU glucuronidation reaction in a dose-dependent manner. Furthermore, Lineweaver-Burk and Dixon plots showed the inhibition of UGT1A6 by levothyroxine was best fit to competitive inhibition, and the inhibition kinetic parameter (Ki ) was determined to be 15.3 μM. Given that UGT1A6...
Songkro, Sarunyoo; Tanmanee, Niwan; Maneenuan, Duangkhae; Chuchome, Thitima; Lo, Nai-Lun; Boonme, Prapaporn
The aim of this work was to investigate the potential of Glucam® P-20 as a skin penetration enhancer for diclofenac sodium microemulsions across excised newborn pig skin. Glucam® P-20 (GP-20) or PPG-20-methyl glucose ether is generally used as a humectant, emollient and fragrance fixative. The w/o microemulsions composed of Tween 80, Eutanol G and water were formulated. The concentration of diclofenac sodium was 1 % w/w while the amounts of GP-20 were varied from 0-20 % w/w, ME-1 (0 %), ME-2 (5 %), ME-3 (10 %) and ME-4 (20 %). All microemulsions were transparent with Newtonian flow behaviour. The mean...
Zaragoza-Fernández, Pilar; Gastelurrutia, Miguel Á.; Cardero, Manuel; Martínez-Martínez, Fernando
This article assesses the impact of an intensive intervention in community pharmacies (involving diet, salt intake, alcohol and regular physical exercise) on blood pressure in hypertensive, treatment-compliant patients who are not controlled with antihypertensive agents. An 8-week randomised, prospective, experimental study was conducted on an intervention group and control group at community pharmacies in Murcia. The 150 participants had a diagnosis of hypertension not controlled with antihypertensive agents, but with good adherence to treatment. The intervention group’s systolic and diastolic blood pressure (BP) levels fell by 16.08 and 9.95 mm Hg, respectively, and the control group by 1.79 and 0.95...
Holguín, Andrés R.; Delgado, Daniel R.; Martínez, Fleming
In this work the Extended Hildebrand Solubility Approach (EHSA) was applied to evaluate the solubility of the analgesic drug indomethacin in propylene glycol + water mixtures at 298.15 K. An acceptable correlative capacity of EHSA was found using a regular polynomial model in order four (overall deviation lower than 2.2 %), when the W interaction parameter is related to the solubility parameter of the mixtures. Nevertheless, the deviations obtained in the estimated solubility with respect to experimental solubility were similar to those obtained directly by means of an empiric regression of the experimental solubility as a function of the mixtures’...
Romano-Lieber, Nicolina S.; Ribeiro, Eliane
To determine the incidence of adverse drug events (ADE) that resulted in the need for children’s emergency care, a total of 23,286 pediatric emergency case notes were analyzed. They were selected on the basis of the ICD code indicating a possible ADE. ADEs were found in 13 case notes (0.06 %), predominantly among girls and mainly in the 1 to 5 year age group. About half of the observed events occurred as a result of accidental ingestion, 27.3 % were suicide attempts, and 27.3 % arose due to the discontinuation of treatment. Antiepileptic drugs were those most often involved. Three...
Torri, Eliane; Nicoleti, Celso R.; Zimmermann, Lizandra M.; Machado, Vanderlei G.
Di–hydroxymethyl–di–2–(pyrrolyl)methane (DMPM) and 7,7,8,8–tetracyanoquinodimethane (TCNQ) were dissolved in acetonitrile to form a π–π charge–transfer complex, which exhibits a deep blue color. This complex is decomposed with the addition of captopril. It was possible to observe a change from the vivid blue color to pale orange–yellow, which is related to the formation of a new n–π complex between TCNQ and captopril. The formation kinetics of the complex between DMPM and TCNQ in acetonitrile was studied, it being concluded that the interaction between the two compounds is a photochemical process. Spectrophotometric titrations of TCNQ with DMPM were carried out and the results...
Khan, Hafeezullah; Maheen, Safirah; Bashir, Sajid; Abbas, Ghulam; Sher, Muhammad; Ashraf, Zaman; Mahmood, Asif; Sarfraz, Mohammad K.
The objective of study was to take and evaluate opinions of the physicians about various aspects of self-medication. A self-fabricated questionnaire of 38 questions was distributed among 292 physicians. Prominent involvement of females in self-medication was suggested by 176 (60 %) physicians. The self-medication trend is more common in financially lower class as reported by 146 (50 %) physicians and in uneducated community as suggested by 165 (57 %) physicians. Family habits and easy to remember brand names were considered as a major source of drug information reported by 155 (53 %) and 187 (64 %) physicians, respectively. Both over...
Wang, Liqiang; Hou, Yuan-Yuan; Peng, Jiamin; Qi, Xizhen; Zhang, Qi; Bai, Fang; Bai, Gang
This study was performed to screen α-glucosidase inhibitors from the actinomycete metabolites library by high throughput screening. Twelve strains of actinomycete were considered to be α-glucosidase inhibitors producing strains; then effective inhibitory strain PW409 was fermented and separated by bioactivity based HPLC, two fractions showing remarkable inhibitory activities; the two compounds were identified as 1-deoxynojirimycin (DNJ) and miglitol by mass spectrometry, comparing with authentic standards, and relevant literature. The quantification analysis of DNJ and miglitol by HPLC-MS/MS showed that the average concentrations of DNJ and miglitol in broth of strain PW409 were 11.2 and 95.8 mg/L, respectively. This is the...
Santos, Veronica C.J.; Sanches Giraud, Cristina; Lanchote, Vera L.; Santos, Luciana M.; Carmona, María J. C.; Santos, Silvia R. C. J.
The aim of the present study was to evaluate intrathecal morphine outcome on postoperative pain and apply pharmacokinetic/pharmacodynamic model to justify morphine consumption, plasma concentration and pain intensity during coronary artery bypass grafting surgery. Thirty six patients were prospectively randomized for general anesthesia and allocated in the control or morphine (400 μg intrathecal) group. At postoperative period, all patients received a loading dose of morphine (1 mg bolus), and then patient-controlled analgesia device was installed and delivered until 36 h. Blood samples was collected from venous catheter, morphine plasma concentrations were determined by liquid chromatography and pain intensity evaluated by...
Khan, Muhammad N.; Hussain, Khalid; Bukhari, Nadeem I.; Latif, Abida; Hashmi, Furqan K.; Hussain, Amjad; Karim, Sabiha; Islam, Muhammad; Masood, Muhammad
The adsorption of certain metal ions and dyes on powdered seeds (pits) of Phoenix sylvestris (Arecaceae) suggests the investigation of such material for the adsorption of oral poisoning substances from the gastrointestinal tract. Therefore, the present study was undertaken to prepare different types of adsorbents from date pits and explore their adsorption capacity for paracetamol at two physiological conditions, enzyme free simulated gastric and intestinal fluids. The activated charcoal was used as a control.
The equilibrium contact time, determined by combining the three forms of date pits and activated charcoal separately with paracetamol in a ratio of 15:1 w/w in both...