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1.
J Pak Med Assoc ; 74(4): 661-665, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38751258

RESUMO

Objectives: To identify various species of non-lactose fermenting gram-negative bacilli involved in urinary tract infections, and to determine their antimicrobial resistance pattern. METHODS: The retrospective, descriptive, cross-sectional study was conducted from January 1 to April 1, 2022, at the Dow University of Health Sciences, Karachi, and comprised data from the institutional diagnostic laboratory that was related to urine samples regardless of age and gender from January 1, 2020, to December 31, 2021. Data was analysed using SPSS version 25. RESULTS: Of the 103,887 urine samples, 41,280(39.7%) were positive, 51,146(49.2%) showed no bacterial growth, 11,000(10.6%) had non-significant bacterial growth and 461(0.4%) had mixed bacterial growth. Of the positive samples, 18359(44.5%) were positive in 2020, and 22,921(55.5%) in 2021. Gram-negative lactose fermenting bacteria included escherichia coli 23,123(22.3%) and klebsiella pneumoniae 2,993(2.9%), gram-negative non-lactose fermenting bacteria included pseudomonas aeruginosa 1,110(1.07%), and gram-positive bacteria included enterococcus 8,008(7.7%). Pseudomonas aeruginosa was most resistant against tobramycin 880(79.3%) and least resistant against piperacillin-tazobactam 146(13%). CONCLUSIONS: Piperacillin-tazobactam was highly sensitive drug against non-lactose fermenting uro-pathogens.


Assuntos
Antibacterianos , Bactérias Gram-Negativas , Infecções Urinárias , Humanos , Bactérias Gram-Negativas/efeitos dos fármacos , Infecções Urinárias/microbiologia , Infecções Urinárias/tratamento farmacológico , Estudos Transversais , Estudos Retrospectivos , Masculino , Feminino , Antibacterianos/farmacologia , Farmacorresistência Bacteriana , Klebsiella pneumoniae/efeitos dos fármacos , Klebsiella pneumoniae/metabolismo , Escherichia coli/efeitos dos fármacos , Escherichia coli/metabolismo , Pseudomonas aeruginosa/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Infecções por Bactérias Gram-Negativas/microbiologia , Infecções por Bactérias Gram-Negativas/tratamento farmacológico , Adulto , Paquistão , Enterococcus/efeitos dos fármacos , Pessoa de Meia-Idade
2.
Pak J Pharm Sci ; 37(1): 115-121, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38741407

RESUMO

Migraine is one of the common neurological disease affecting around 23% of the Pakistani population. Prompt treatment is required to regain the functional ability of patients. The present study was designed to develop sumatriptan succinate orodispersible tablets that would quickly overcome acute migraine episodes using 22 full-factorial design. The chitosan and sodium starch glycolate were taken as independent variables; friability, disintegration, dispersion time and water absorption ratio as response variables. Eight trial formulations were generated by Design Expert® software. The main effect plots were used to check the interaction of formulations with response variables. All trial formulations showed good micromeritic properties in terms of angle of repose (19.59o-24.57°), Carr's index (17.08-24.90%) and Hausner's ratio (1.20-1.33). The tablets wetted quickly (17.1- 39 sec) in dispersion medium, showed higher water absorption ratio (188-341 sec) and disintegrated quickly (13-20 sec) with an excellent dissolution rate (94-99%). The main effect plots show interactions between the independent variables against most of the study responses. A 22 full-factorial model was found to be effective in studying the influence of formulation variables on response parameters. Both chitosan and sodium starch glycolate can be used in combination to fabricate an effective orodispersible formulation of sumatriptan succinate.


Assuntos
Quitosana , Transtornos de Enxaqueca , Amido , Sumatriptana , Comprimidos , Sumatriptana/administração & dosagem , Sumatriptana/química , Transtornos de Enxaqueca/tratamento farmacológico , Amido/química , Amido/análogos & derivados , Amido/administração & dosagem , Quitosana/química , Humanos , Administração Oral , Solubilidade , Composição de Medicamentos , Química Farmacêutica , Excipientes/química
3.
Artigo em Inglês | MEDLINE | ID: mdl-37843797

RESUMO

The mangrove ecosystem is the world's fourth most productive ecosystem in terms of service value and offering rich biological resources. Microorganisms play vital roles in these ecological processes, thus researching the mangroves-microbiota is crucial for a deeper comprehension of mangroves dynamics. Amplicon sequencing that targeted V4 region of 16S rRNA gene was employed to profile the microbial diversities and community compositions of 19 soil samples, which were collected from the rhizosphere of 3 plant species (i.e., Avicennia marina, Ceriops tagal, and Rhizophora mucronata) in the mangrove forests of Lasbela coast, Pakistan. A total of 67 bacterial phyla were observed from three mangroves species, and these taxa were classified into 188 classes, 453 orders, 759 families, and 1327 genera. We found that Proteobacteria (34.9-38.4%) and Desulfobacteria (7.6-10.0%) were the dominant phyla followed by Chloroflexi (6.6-7.3%), Gemmatimonadota (5.4-6.8%), Bacteroidota (4.3-5.5%), Planctomycetota (4.4-4.9%) and Acidobacteriota (2.7-3.4%), Actinobacteriota (2.5-3.3%), and Crenarchaeota (2.5-3.3%). After considering the distribution of taxonomic groups, we prescribe that the distinctions in bacterial community composition and diversity are ascribed to the changes in physicochemical attributes of the soil samples (i.e., electrical conductivity (ECe), pH, total organic matter (OM), total organic carbon (OC), available phosphorus (P), and extractable potassium (CaCO3). The findings of this study indicated a high-level species diversity in Pakistani mangroves. The outcomes may also aid in the development of effective conservation policies for mangrove ecosystems, which have been hotspots for anthropogenic impacts in Pakistan. To our knowledge, this is the first microbial research from a Pakistani mangrove forest.

4.
Clin Med Insights Case Rep ; 15: 11795476221112819, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35898804

RESUMO

Urinary tract infection (UTI) is caused by bacteria growing in urine and affect kidneys, bladder, ureters, and urethra. Women with diabetes are at high risk of developing UTI. This is a case of a 60-year-old postmenopausal woman with uncontrolled type-I diabetes mellitus and hypertension, who presented with an acute onset of dysuria, burning micturition, and increased frequency. This case highlights the shortfall in the preliminary management plan of performing imperative clinical laboratory investigations including urine detailed report (DR), urine culture and sensitivity(C/S), and plasma glucose testing to initiate antimicrobial treatment. UTI requires to be treated precisely in diabetic patients with the help of a comprehensive diagnosis for signs of dysuria, frequent urination, and pelvic pain. The treatment of UTIs should always begin with culture and sensitivity analysis while the patient is symptomatic, to initiate antimicrobial treatment. Comorbidities should be managed appropriately during treatment to achieve desired therapeutic outcomes.

5.
PLoS One ; 17(6): e0270587, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35771842

RESUMO

This study was conducted to determine the various socio-demographic, economic, and clinical variables (SDECVs) which influence the health-related quality of life (HRQoL) of hypertensive patients. Three hundred and fifty hypertensive patients participated in this study through a structured questionnaire and EQ 5D 5L. 211(60.28%) participants had stage 1, and 139 (39.7%) had stage 2 hypertension. No participants reported severe problems in any domain on EQ 5D 5L. Generalize Linear Model (GLM) was used to assess the association between HRQoL and SDECVs. The mean utility and VAS score was 0.64 (±0.15) and 63.17 (±11.01) respectively. The participants of the stage 1 hypertension group had a significantly better score on each domain of EQ 5D 5L as compared to stage 1 (0.027, 0.010, 0.00, 0.00, 0.048). No participant in either group reported extreme problems in any domain. Among socio-demographic factors, the males, non-smokers, income sharing, and healthy normal hypertensive patients had better HRQoL (0.009, 0.016, 0.019, and 0.003). A lower cost of treatment was also associated with better HRQoL (0.017). Among clinical variables, stage 1 hypertension had better HRQoL than stage 2(0.035). The number of prescribed antihypertensive drugs had no effect on the quality of life (0.253), however, the non-pharmacologic interventions such as reduction in salt and oil consumption (0.035), reduction in beverages consumption (0.0014) and increased water intake (0.010) had resulted in better QoL. The patients who reported dizziness had poor HRQoL while patients who had cardiac problems and diabetes reported a significantly lower EQ-VAS score. The effect of gender on the HRQoL of hypertensive patients who had comorbid conditions was significant in the case of renal, respiratory, visual problems, and dizziness where females had a lesser utility score than males. The study reports on significant determinants which should be taken into account in an attempt to improve the health-related quality of life of hypertensive patients.


Assuntos
Hipertensão , Qualidade de Vida , Algoritmos , Estudos Transversais , Tontura , Feminino , Nível de Saúde , Humanos , Hipertensão/epidemiologia , Masculino , Inquéritos e Questionários
6.
Pak J Pharm Sci ; 34(4(Supplementary)): 1519-1525, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34799327

RESUMO

Empagliflozin is a selective inhibitor of sodium glucose co-transporter II, given as mono therapy or an add-on treatment to reduce the glycated hemoglobin levels in type 2 diabetes. This work deals with designing, formulating and optimizing empagliflozin (10mg) immediate release (IR) tablets by direct compression technique using different excipients. Through central composite rotatable design (CCRD), total nine formulations (EF1-EF9) were generated by changing the composition of binder avicel PH 102® (X1) and superdisintegrant acdisol⌖ (X2). Formulation runs with in suitable weight range and powder properties were subjected to compression. The influence of interaction of excipients on friability (Y1), hardness (Y2) and disintegration (Y3) were analyzed by fitting the polynomial quadratic model with response surface methodology (RSM). Trials EF2, EF7, EF8 and EF9 exhibited acceptable tablet attributes upon physico-chemical testing. Different dissolution models were applied to observe the in vitro drug release pattern in phosphate buffer of pH 6.8. The cumulative drug release of IR tablet batches followed the Weibull kinetics with regression coefficient (r2) values of 0.983-0.992. Empagliflozin trials were exposed to accelerated storage conditions (40±2°C/ 75±5% RH) for stability testing. Shelf life period of exposed formulations were computed in range of 22 to 25 months. Keeping in view of the results, it is concluded that the employed technique of preparation and optimization are observed to be excellent for developing immediate release empagliflozin (10mg) tablets.


Assuntos
Compostos Benzidrílicos/química , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Excipientes/química , Glucosídeos/química , Inibidores do Transportador 2 de Sódio-Glicose/química , Dureza , Cinética , Pós , Solubilidade , Comprimidos/química
7.
Pak J Pharm Sci ; 34(3(Supplementary)): 1081-1087, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-34602436

RESUMO

The current investigation is based on efficient method development for the quantification of empagliflozin in raw and pharmaceutical dosage forms, as no pharmacopoeial method for the drug is available so far. The developed analytical method was validated as per ICH guidelines. C18 column with mobile phase (pH 4.8) consisted of 0.1% trifluoroacetic acid solution and acetonitrile (70:30 v/v) was used for drug analysis. The calibration plot showed good linear regression (r2>0.999) over the concentration of 0.025-30 µg mL-1. The LOD and LOQ were found to be 0.020 µg mL-1 and 0.061 µg mL-1, respectively. The percentage recovery was estimated between 98.0 to 100.13%. Accuracy and precision data were found to be less than 2%, indicating the suitability of method for routine analysis in pharmaceutical industries. Moreover, the drug solution was found to be stable in refrigerator and ambient room temperature with mean % accuracy of >98%. Empagliflozin contents were also tested in both the raw API and marketed tablet brands using this newly developed method. The mean assay of raw empagliflozin and tablet brands were ranged from 99.29%±1.12 to 100.95%±1.69 and 97.18%±1.59 to 98.92%±1.00 respectively. Based on these findings, the present investigated approach is suitable for quantification of empagliflozin in raw and pharmaceutical dosage forms.


Assuntos
Compostos Benzidrílicos/análise , Glucosídeos/análise , Inibidores do Transportador 2 de Sódio-Glicose/análise , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Formas de Dosagem , Reprodutibilidade dos Testes
8.
BMC Complement Med Ther ; 21(1): 135, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33933037

RESUMO

BACKGROUND: Nerium oleander (L.) is well known traditionally used medicinal plant with several pharmacological activities. However, the anti-bacterial, anti-inflammatory activity and in vivo toxicity potential of floral parts of this plant are not reported. Therefore the present study was designed to investigate these activities of Nerium oleander ethanolic flower extract (NOEE) in different animal models. METHODS: Antimicrobial activity of plant extract was compared with five different antibiotics using the disk diffusion method. The time-killing kinetic assay and bacterial killing mechanism of NOEE were also performed. Anti-inflammatory activity was assessed using granuloma induced by cotton-pellet, rat paw edema induced by carrageenan and levels of different inflammatory biomarkers on healthy Wistar rats. The protein and mRNA expressions of nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß) were also measured. Acute (14 days) and sub-acute (28 days) oral toxicity studies were also performed on healthy Sprague Dawley rats. RESULTS: NOEE produced highly significant (P < 0.005) and significant (P < 0.05) zones of inhibition at 30 mg/mL and 20 mg/mL respectively against most of the tested bacterial strains. NOEE produced a more drop in viable counts of Gram-negative isolates within 20 min. After 12 h exposure with NOEE, the SEM images of MRSA showed the destruction of cell membrane. NOEE showed highly significant (P < 0.005) anti-inflammatory activity in cotton-pellet and carrageenan inflammatory models. In addition, treatment with NOEE also decreased the production of NO, PGE2, TNF-α and IL-1ß in the rat paw after treated with carrageenan. Similarly, NOEE also suppressed the inducible nitric oxide synthase (iNOS), TNF-α, IL-1ß, and cyclooxygenase-2 (COX-2) mRNA expressions. It is also showed highly significant reduction in total leukocyte count (73.09%) and C-reactive protein levels (54.60%). NOEE also inhibited COX-1, COX-2, 5-LO and 12-LO in a highly significant manner. Moreover, acute and sub-acute toxicity studies of NOEE in rats confirm the toxicity with hepatotoxicity at higher doses (2000 mg/kg) i.e. four times greater than the therapeutic dose. CONCLUSION: It is concluded that crude flower extract of N. oleander is a potent antimicrobial and anti-inflammatory agent with no toxicity potential at therapeutic doses.


Assuntos
Antibacterianos , Anti-Inflamatórios , Nerium , Extratos Vegetais , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/toxicidade , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Feminino , Inflamação/induzido quimicamente , Inflamação/metabolismo , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Ratos , Ratos Sprague-Dawley , Testes de Toxicidade Aguda
9.
PLoS One ; 15(9): e0238951, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32898192

RESUMO

The aim of the study was to determine the various pharmacokinetic parameters of the newly developed cost-effective aceclofenac 100 mg tablet formulation (F-15) and to establish the bioequivalence against the marketed brand (ACEMED). Both products (test and reference) were given to 12 healthy non-smokers male subjects with overnight fasting of >10hr. The study was a randomized, single-dose, open-label, two sequence, and two treatment crossover design, with a washout period of 2 weeks. Blood samples (5 mL) from the human subjects were collected before (0 hr) and after drug administration at 13different time points (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12 and 18 hrs). The drug plasma concentration was analyzed by a validated RP-HPLC method using a solvent system containing acetonitrile and deionized water (60:40% v/v). Linearity was found to be 0.999 over the drug concentration range of 50µg/mL to 0.05µg/mL with LLOQ and LOD of 0.05µg/mL and 0.025µg/mL respectively. Non-compartmental pharmacokinetic analysis was performed using Kinetica® (ver. 5.1) software. Using the log-transformed data Cmax, AUC0-t, AUC0-∞, AUMCtot, and MRT were calculated. The Cmax of the test and brand was found to be 8.629±1.251µg/mL and 8.478±0.913µg/mL. The AUC0-t and AUC0-∞ of the test and the reference were computed to be 20.890 ±2.2021µg/mL.h, 23.272 ±1.914 µg/mL.h and 19.850 ±2.911 µg/mL.h, 22.890 ± 2.110 µg/mL.h correspondingly. Two-way analysis of variance (ANOVA) test and two one-sided t-test (p>0.05; non-significant) were applied to assess the variation in the period, sequence, subjects, and treatment. Geometric mean ratios for above mentioned pharmacokinetic parameters of reference/test were found within the acceptable FDA limits of 80-125% using 90% CI. There was no inter and intrasubject variation (p> 0.05) that was observed. Therefore, the directly compressible aceclofenac (100 mg) test formulation and the commercial reference tablets were declared to be biosimilar.


Assuntos
Diclofenaco/análogos & derivados , Adulto , Análise de Variância , Área Sob a Curva , Química Farmacêutica/métodos , Cromatografia Líquida de Alta Pressão/métodos , Estudos Cross-Over , Diclofenaco/metabolismo , Diclofenaco/farmacocinética , Voluntários Saudáveis , Humanos , Masculino , Comprimidos/farmacocinética , Equivalência Terapêutica
10.
Pak J Pharm Sci ; 33(4(Supplementary)): 1899-1906, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33612475

RESUMO

Aim of this study to evaluate the safety profile, hepatoprotective and in-vivo antioxidant activities of Dicliptera bupleuroides Nees. Toxicity studies were conducted in human RBCs and DNA by using standard procedures. Acute hepatoprotective investigation was carried out in albino rats by treated with all six fractions of D. bupleuroides 350 mg/kg/day. ALT, AST, ALP and total bilirubin (TB) were performed. The n-hexane fraction (200 mg/kg/day) exhibited appropriate hepatoprotective activity hence subjected to chronic study (14 days). Paracetamol induced the hepatotoxicity (350mg/kg) and silymarin (50 mg/kg) was standard drug. Liver function tests, liver peroxidation tests and histopathological examination were performed at the end. Hexane fraction showed significant decrease in the level of ALT (88.1±7.8), AST (93.8±7.6), ALP (136.3±8.4) and TB (0.6±0.03) as compared to the standard drug (p>0.05). Rats treated with ethyl acetate fraction showed decrease in MDA (42.8±0.7) while GSH was found to be increased (107.7±1.8) against the toxic group (51.3±2.9), (73.6±4.0) respectively. All the drug extracts decreased the oxidative stress and protect the DNA from free hydroxyl radicals. DNA damage protection activity of these fractions is due to phytochemicals present in these fractions. These results indicate that the plant fractions possess significant hepatoprotective and antioxidant activities with no toxic effects.


Assuntos
Acanthaceae/química , Acetaminofen/farmacologia , Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Analgésicos não Narcóticos/farmacologia , Animais , Tetracloreto de Carbono/farmacologia , Feminino , Humanos , Testes de Função Hepática/métodos , Masculino , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Wistar , Silimarina/farmacologia
11.
Pak J Pharm Sci ; 32(4(Supplementary)): 1821-1827, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31680078

RESUMO

Lycopene, the active component of Lycopersicon esculentum species, has been reported for the protecting capabilities against ultra-violet induced skin pigmentation, antioxygen and antityrosinase activities. In the present study, extract of tomato fruit was obtained from the Lycopersicon esculentum plant using solvent system comprised of hexaneethanol-acetone. The phyto chemical active constituent lycopene was then identified by spectrophotometric technique at 470nm. Micro emulsions were developed containing different ratio of water, isopropyl myristate (oil), tween 80 and propylene glycol as surfactant and co-surfactant respectively via pseudoternary phase diagram. Various physicochemical tests were performed including globular size, conductivity, viscosity, scanning electron microscopy (SEM), refractive index (RI) and pH measurement for the formulation characterization. Results of physical and chemical stability studies showed that the micro emulsion with proportion of surfactant: co-surfactant of 2:1 (Smix) was found to be optimized formulation and with enhanced stability. Therefore, concluded that the stability of the micro emulsion was dependent on the proportions of surfactant co-surfactant, water and oil in the preparation.


Assuntos
Emulsões/química , Extratos Vegetais/química , Solanum lycopersicum/química , Sistemas de Liberação de Medicamentos/métodos , Miristatos/química , Óleos de Plantas/química , Polissorbatos/química , Solubilidade/efeitos dos fármacos , Tensoativos/química , Viscosidade/efeitos dos fármacos , Água/química
12.
Pak J Pharm Sci ; 32(3 (Supplementary)): 1245-1251, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31303597

RESUMO

The aim of the current study was to formulate sustain release (SR) tablets of ketoprofen. Five batches (batch I -V) of matrix based ketoprofen tablet were prepared by dry granulation method using hydroxyl propyl methyl cellulose (15000cps). Compatibility of formulation excipients with drug was explored through FT-IR technique. Various physical and chemical parameters of all tablet batches were evaluated with multi-point dissolution profile (for 24hrs) for formulation optimization. Release kinetics of trials was estimated by model dependent and independent methods. Formulations having excellent quality attributes were then compared with marketed ketoprofen SR tablets. Accelerated stability study was also conducted to compute the shelf life of the optimized formulation. FT-IR scans illustrated the compatibility of ketoprofen with all tablet excipients. On the basis of testing results and controlled release pattern batch II was set to be an optimized trial having shelf life of 37 months. All trial batches (batch I-V) and the marketed brand exhibited highest linearity towards zero order and Korsmeyer-Peppas model with non-fickian anomalous transport (n=0.541-0.655).


Assuntos
Cetoprofeno/química , Cetoprofeno/farmacocinética , Comprimidos/química , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Excipientes/química , Derivados da Hipromelose/química , Espectroscopia de Infravermelho com Transformada de Fourier , Comprimidos/farmacocinética
13.
Pak J Pharm Sci ; 32(2 (Supplementary)): 793-798, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31103974

RESUMO

Cinitapride has been widely given in gastro-esophageal reflux disease (GERD) and dysphagia due to irregularities of GI motilities. Mouth dissolving tablets were prepared for rapid availability and action of drug. Multi-point dissolution studies were conducted in 0.1 N HCl solution of pH 1.2 and phosphate buffer of pH 4.5 and 6.8. Drug release profile showed higher liberation of cinitapride at lower pH then basic medium (<80%). Formulation containing crospovidone (10%) was found to be optimized trial having excellent quality pharmaceutical attributes. The lowest AIC, highest MSC and regression (> 0.9) values were observed for Weibull kinetics in all dissolution medium reflecting the excellent model fitting for the present study. Accelerated stability testing data showed excellent results of drug assay (>99%) along with physical characteristics indicating the absence of drug degradation as well excipient interaction. The estimated shelf life period of various optimized trial formulations was found in between 33 to 41 months.


Assuntos
Benzamidas/química , Benzamidas/farmacocinética , Comprimidos/química , Comprimidos/farmacocinética , Administração Oral , Benzamidas/administração & dosagem , Soluções Tampão , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Concentração de Íons de Hidrogênio , Cinética , Comprimidos/administração & dosagem
14.
Pak J Pharm Sci ; 31(6 (Supplementary): 2725-2731, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30587486

RESUMO

Cinitapride hydrogen tartarate is relatively a new prokinetic agent that widely prescribed for GERD and epigastric pain. Present study was aimed to develop and optimize cinitapride (1 mg) immediate release (IR) tablet formulation(s) by direct compression using central composite rotatable technique. Overall nine formulations (FC1-FC9) were generated by varying the composition of binder avicel PH 102 (X1) and superdisintegrant crospovidone (X2). The effect of interaction of excipients on hardness (Y1), friability (Y2), disintegration (Y3) and dissolution at 15 min (Y4) were analyzed by RSM plotting. On the basis of physico-chemical evaluation FC3, FC4 and FC6 were found to be the optimized formulations however; FC3 was selected to be the best trial owing to excellent drug release (100.17%) with least friability (0.14%). These IR tablets showed the release pattern similar to the Weibull model with r2 value of 0.978-0.998. The dissimilarity (f1) and similarity indexes (f2) of FC3, FC4, FC6 with the marketed product were estimated to be 2.57 and 76.51, 4.51 and 64.46, 4.32 and 66.78 respectively. Trial optimized formulations were highly stable with the shelf lives of 58-64 months. So, keeping in view the results of present investigation, it is concluded that the technique of manufacturing and optimization is found to be excellent for developing immediate release cinitapride tablets.


Assuntos
Benzamidas/síntese química , Benzamidas/metabolismo , Química Farmacêutica/métodos , Força Compressiva , Desenho de Fármacos , Composição de Medicamentos , Comprimidos
15.
Pak J Pharm Sci ; 31(5(Supplementary)): 2157-2162, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30393227

RESUMO

Healthcare professionals including physicians and pharmacists have been trying since long to come across and work out regarding the issue of generic alternatives, which is highly affected by factors like therapeutic efficacy, cost effectiveness, aesthetic and elegant appearance and implementation of packaging number over the drug product. However, the community pharmacist professionals are also facing difficulty in making decision regarding selection and dispensing the most efficacious brand to the patients. In this regard, the initiation of recent approaches for the development of amenable drug products has led to evolve the concept of generating new avenues for achieving higher patient compliance. Hence, the objective of this study was to evaluate the quality attributes and make comparisons regarding different brands of Dexibuprofen available in market of Karachi, Pakistan. The study is based on evaluation of physical chemical parameters of five different brands. Moreover, a comparative dissolution profile of selected brands of Dexibuprofen was also performed by applying numerous approaches. DEX-1was selected as reference while DEX-2- DEX-5 was selected as test brands. Results of all the selected brands met all the compendial requirements. Interpretation of the entire aforementioned test was evaluated using model independent, model- dependent and one - way ANOVA. The work presented in this study has been designed to provide quality standard products easily accessible in Pakistani market.


Assuntos
Anti-Inflamatórios não Esteroides/farmacocinética , Anti-Inflamatórios não Esteroides/normas , Liberação Controlada de Fármacos , Ibuprofeno/análogos & derivados , Pesquisa Qualitativa , Anti-Inflamatórios não Esteroides/análise , Humanos , Ibuprofeno/análise , Ibuprofeno/farmacocinética , Ibuprofeno/normas , Equivalência Terapêutica
16.
Pak J Pharm Sci ; 31(5(Supplementary)): 2143-2148, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30393225

RESUMO

Casuarina equisetifolia L. is an important medicinal plant widely used to treat various diseases particularly ulcers, diabetes, cough, diarrhea and many infectious and skin diseases. The aim of this research study was to examine the killing mechanism and killing kinetics assay of methanolic bark extract of C. equisetifolia against some highly resistant human pathogens. The comparison on antibacterial activity of extract was firstly done with six different well reputed antibiotics using disk diffusion method. The broth dilution method was used to measure the MIC and MBC values. The mechanism of killing was identified by scanning electron microscopy (SEM) technique. Results showed that higher inhibitory zones were produced by methanolic plant extract than that of some tested antibiotics. The lower MIC and MBC values indicated the antibacterial potency of plant extract. The extract of C. equisetifolia produced a more drop in optical density of S. aureus, MRSA B. subtilis and S. epidermidis up to 12 hrs. The complete destruction of the cell membrane of MRSA was observed after 12 h treatment with plant extract. It is concluded that crude bark extract of C. equisetifolia is potent antimicrobial agent and produced both bacteriostatic and bactericidal effects. Its killing time was extremely faster especially against MRSA. The cell membrane rapturing is a suggested killing mechanism of plant extract.


Assuntos
Antibacterianos/farmacologia , Fagales , Metanol/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Casca de Planta , Extratos Vegetais/farmacologia , Antibacterianos/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/crescimento & desenvolvimento , Humanos , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana/métodos , Extratos Vegetais/isolamento & purificação
17.
Pak J Pharm Sci ; 31(5): 1827-1836, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30150177

RESUMO

In this study cost effective direct compression technique was used for the development and optimization of intermediate release (IntR) ketoprofen tablets using central composite design (CCRD). Fifteen different formulations (F1-F15) were developed using (X1) microcrystalline cellulose (Avicel PH-102) (18-51%), (X2) methocel K4M (0.1-25%) and (X3) starch (1.5-18%) as selected variables while responses were % friability and Carr's Index (compressibility index). Powder blends of all formulations were evaluated using Angle of Repose, Carr's Index and porosity. Results of powder blends comply with USP standards and are classified as Fair Excellent. From F1-F15 only four formulations i.e. F6, F7, F14 and F15 were selected on acceptable weight basis, micromeritic properties and on the concentration of excipients. For the assessment of physico chemical properties of the optimized formulations different tests were performed. All results were found to be adequate range. In vitro assessment of the optimized formulations were also carried out in different dissolution media i.e. pH 1.2, phosphate buffer 4.5, pH 6.8 and pH 7.5. Release behaviour of F6, F7, F14 and F15 were estimated by using one - way ANOVA, model - independent, model dependent methods. Results of f1 and f2 showed that all the test formulations i.e. F6, F7, F14 were found to be similar with the reference formulation i.e. F15 at various dissolution media. Also all the formulations followed Hixson-Crowell kinetic model. The parameter n showed Anomalous transport (non - fickian diffusion). The mean dissolution time (MDT) was found to be in the range of 2.632-2.922. Results of ANOVA indicated no significant difference within and between formulations at different dissolution media as p values were found to be >0.05. Also all the selected formulations were found to be stable at accelerated conditions.


Assuntos
Anti-Inflamatórios não Esteroides/farmacocinética , Desenho de Fármacos , Desenvolvimento de Medicamentos/métodos , Liberação Controlada de Fármacos , Cetoprofeno/farmacocinética , Anti-Inflamatórios não Esteroides/síntese química , Cetoprofeno/síntese química
18.
Pak J Pharm Sci ; 31(4(Supplementary)): 1469-1474, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30058537

RESUMO

In this research work biowaiver studies of newly developed and optimized Meloxicam 7.5mg and 15mg water dispersible formulations were carried out at different dissolution media i.e. 0.1N HCl, phosphate buffer pH 4.5, pH 6.8, and pH 7.5 at 50 rpm. For this purpose reference (MA9 and MB9) and tests (MA2, MA4, MA6, MA7 and MA8 (15 mg) and MB2, MB4, MB6, MB7and MB8 (7.5 mg) formulations were compared. In vitro patterns were analyzed by using model-independent and model-dependent methods. Results indicated that all formulation at pH 0.1N HCl and phosphate buffer pH 4.5 followed Weibull model, while at pH 6.8 and pH 7.5 all formulations followed Hixson-Crowell model. Similarly results of model independent methods demonstrated that all the reference formulations were found to be similar with the tests formulations. Results indicated that Biowaiver could be granted to all the optimized water dispersible meloxicam formulations of both batches, so waiver for bioequivalence study can be allowed.


Assuntos
Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/química , Química Farmacêutica/métodos , Meloxicam/análise , Meloxicam/química , Anti-Inflamatórios não Esteroides/farmacocinética , Composição de Medicamentos , Liberação Controlada de Fármacos , Meloxicam/farmacocinética , Comprimidos
19.
J Coll Physicians Surg Pak ; 28(7): 536-540, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29950259

RESUMO

OBJECTIVE: To assess the risk factors, frequency and transience rate for ventilator-associated pneumonia in geriatric patients. STUDY DESIGN: Cross-sectional, descriptive study. PLACE AND DURATION OF STUDY: Various campuses of Ziauddin University Hospital and Civil Hospital, Karachi, from April 2016 to May 2017. METHODOLOGY: Critically ill geriatric patients (aged 60 years and above) in intensive care units, were selected who had received mechanical ventilation. Various risk factors, microbial fate, and related clinical outcomes were measured in the selected cohort of 350 patients. RESULTS: It was found that 72% (n=252) of study population was elderly who received ventilation for more than 48 hours with a higher mortality rate of 59.5%. Frequency of VAP was found to be 18% (n=63). A high rate of VAP was observed in geriatric cohort, i.e. n=47 association of age in VAP (p=0.611) in non-significant while mortality values and admission status were significantly associated with VAP (p<0.001). CONCLUSION: The factual challenge nowadays is to present the real estimate of the clinical consequences of VAP in geriatric cohort. Such studies will help in formulating an optimal institutional policy and rational approach to decrease rates of mortality.


Assuntos
Unidades de Terapia Intensiva , Pneumonia Associada à Ventilação Mecânica/epidemiologia , Respiração Artificial/efeitos adversos , Centros de Atenção Terciária , Idoso , Estudos Transversais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Paquistão , Fatores de Risco
20.
Protein Pept Lett ; 25(7): 619-625, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29956606

RESUMO

BACKGROUND: For about 30 years Human Immunodeficiency Virus (HIV) has been a significant social and health issue. It has been a perilous opponent in the human contest against HIV. At the end of 2015 there were 26.7 million people worldwide who were affected by the Human Immunodeficiency Virus (HIV) and this number is expected to increase. Unfortunately, currently there are no vaccines available for prevention and control of HIV. The global burden of HIV articulates the need for anti-HIV therapeutic factors. Venom toxins are commonly prescribed for treatment of various medical disorders. Honey Bee venom has recently been proven to be safe and maybe therapeutic in a specified dose. This therapeutic effect is due to the uptake of melittin by HIV infected cells which leads to decreased HIV gene expression and replication. Similarly, Scorpion venom acts as a therapeutic agent against HIV. Snake venoms have antiviral activity against defense mechanisms of viruses. CONCLUSION: Antiretroviral therapy is promising in the fight against HIV because it limits viral replication. It has the potential to reduce the passage of HIV-1 and to limit the viral load in infected people. This review aims to shed light on an infectious potential of active constituents of bee, scorpion and snake venom articulated in many recent studies.


Assuntos
Venenos de Abelha , Infecções por HIV/tratamento farmacológico , Venenos de Serpentes , Animais , Fármacos Anti-HIV/farmacologia , Fármacos Anti-HIV/uso terapêutico , Peptídeos Catiônicos Antimicrobianos/farmacologia , Peptídeos Catiônicos Antimicrobianos/uso terapêutico , Venenos de Abelha/farmacologia , Venenos de Abelha/uso terapêutico , HIV-1/efeitos dos fármacos , Humanos , Venenos de Serpentes/farmacologia , Venenos de Serpentes/uso terapêutico
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