RESUMO
For the simultaneous measurement of Ethinylestradiol (EE) and Drospirenone (DP) in fixed-dose combination hormones tablets, a reverse-phase high-performance liquid chromatographic (RP-HPLC) method was developed. A specific, precise and accurate RP-HPLC method was developed and validated to analyse the drugs in rat plasma. The fluorescence detection for EE was made at λ= 200-310 nm and Ultraviolet-visible (UV/Vis) detection for DP was made at 270 nm. The typical EE and DP retention times were 4.19 and 5.30 minutes, respectively. The limit of detection (LOD) and limit of detection (LOQ) for EE were 0.121 and 0.282µg/mL and LOD and LOQ for DP were 2.23 and 7.697µg/mL respectively. The regression coefficient (r2) of EE and DP were 0.9937 and 0.9913 respectively. Precision's relative standard deviation (RSD) was less than 5%. The analyte recoveries of both drugs stayed within 95% of each other. All other validation parameters adhered to ICH standards. Throughout the analytical process, the analyte was stable. The advantages of the method developed include stability under different conditions and a low limit of quantification that was in micrograms. Its applicability was confirmed by the analysis of EE and DP levels in plasma samples in a designed pharmacokinetic study in rats after oral administration.
Assuntos
Bioensaio , Etinilestradiol , Animais , Ratos , Cromatografia Líquida de Alta Pressão , Administração OralRESUMO
The current paper explains how to make mesoporous silica microparticles (MSM) by mixing water and dichloromethane. Several dichloromethane-water ratios were used to adjust the reaction mixture for the first time to easily synthesize mesoporous silica micro particles with regulated particle size. By carefully modifying the concentrations of water and dichloromethane, a higher level of consistency was achieved in the production of micro particles, i.e. to a 2:1 v/v ratio. It was discovered that variations in the dichloromethane-to-water ratios significantly affect the surface roughness and morphologies of mesoporous silica particles along with size. This is most likely because the solvent affects how quickly tetraethyl orthosilicate (TEOS) and how quickly inorganic species polymerize. In all experiments, conditions were maintained the same at 25oC temperature and 1000 rpm. Scanner electron microscopy (SEM), Fourier transform infrared (FTIR) and X-ray powder diffraction (XRD) methods were used to identify the structure of MSM. The in vitro cytotoxicity assays showed that the produced particles, which had a diameter of 1.0 m, were safe for usage in the cellular system.
Assuntos
Cloreto de Metileno , Projetos de Pesquisa , Tamanho da Partícula , Dióxido de Silício/toxicidade , ÁguaRESUMO
The study aimed to prepare and characterize biodegradable sustained-release beads of letrozole (LTZ) for treating cancerous disease. The ionotropic gelation method was used for the preparation and calcium chloride (CaCl2) was used as a gelating agent, while chitosan (CTS) and sodium alginate (NaAlg) as biodegradable polymeric matrices in the blend hydrogel beads. The beads were characterized for their size, surface morphology, drug entrapment efficiency, drug-polymer interaction and crystallinity using different analytic techniques, including optical microscopy, Scanning Electron Microscopy (SEM), UV-spectroscopy, Fourier-transform Infrared Spectroscopy (FTIR), Thermo gravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC) and X-ray Diffraction Analysis (XRD) respectively. In vitro swelling studies were also applied to observe the response of these polymeric networks against different pH (at 1.2, 6.8 and 7.4 pH). The results from TGA and DSC exhibited that the components in the formulation possess better thermal stability. The XRD of polymeric networks displays a minor crystalline and significant amorphous nature. The SEM micrographs revealed that polymeric networks have uneven surfaces and grooves. Better swelling and in vitro outcomes were achieved at a high pH (6.8,7.4), which endorsed the pH-responsive characteristics of the prepared beads. Hence, beads based on chitosan and sodium alginate were successfully synthesized and can be used for the controlled release of letrozole.
Assuntos
Quitosana , Preparações de Ação Retardada , Letrozol , Quitosana/química , Tamanho da Partícula , Polímeros , Alginatos/química , Espectroscopia de Infravermelho com Transformada de Fourier , Ácidos Hexurônicos/química , Microscopia Eletrônica de Varredura , Ácido Glucurônico/químicaRESUMO
Context: Arthritis is an inflammatory disease of diarthrodial joints and is associated with swollen inflamed joints, disruption of joints, and loss of integrity of articular cartilage and synovial joints. Objective: The current review intended to examine the data on the epidemiology, causes, clinical diagnosis, and prevention and control of different types of arthritis and on the use of medicinal plants in gouty arthritis. Design: The research team performed a literature review, searching relevant literature databases, including bioRxiv, medRxiv, Google Scholar, Embase, PsychINFO, and PubMed. The search terms were arthritis, diarthodial joints, use of medicinal plants in gouty arthritis, and synovial joints. Setting: The study took place in the main library of the University of Sargodha in Sargodha, Pakistan. Results: The research team identified 135 studies, and eventually 92 unique academic publications were included in the analysis. Arthritis can develop and progress in any musculoskeletal joint, and most commonly occurs in knees, hips, shoulders, and hands. Major risk factors for arthritis include age, obesity, trauma, other diseases, and smoking. Arthritis is classified into various types, including rheumatoid arthritis (RA), osteoarthritis (OA), gouty arthritis, septic arthritis, and psoriatic arthritis (PsA). RA and OA are the most common types worldwide. RA is an autoimmune disease in which the body's immune cells attack the joints. OA develops due to damage of cartilage, tissues, and joints due to age, obesity, or stress on joints. Gouty arthritis develops due to hyperuricemia; deposits of monosodium urate crystals can lead to gouty arthritis. Septic arthritis occurs due to a microbial infection in synovial joints because in synovial joints the basement membrane is absent. PsA develops due to the psoriasis-skin disease. Conclusions: The current review showed that different types of arthritis has different causes and pathogeneses. Pain in joints is a major and common symptom in all types of arthritis. Arthritis is managed pharmacologically and nonpharmacologically. Treatment is different for each class of arthritis according to its cause and symptoms.
Assuntos
Artrite Gotosa , Artrite Psoriásica , Artrite Reumatoide , Osteoartrite , Plantas Medicinais , Anti-Inflamatórios não Esteroides/uso terapêutico , Artrite Gotosa/tratamento farmacológico , Artrite Psoriásica/diagnóstico , Artrite Psoriásica/tratamento farmacológico , Artrite Reumatoide/tratamento farmacológico , Humanos , Obesidade , Osteoartrite/tratamento farmacológico , Ácido Úrico/uso terapêuticoRESUMO
CONTEXT: A completely unique coronavirus (2019-nCoV), formally referred to as severe acute respiratory syndrome (SARS-CoV-2), appeared in China. SARS-CoV-2 is an etiological mediator of coronavirus 2 (COVID-19), characterized by pneumonic contagion in human beings. In spite of forceful suppression, this virus has spread worldwide. No specific drugs have been approved by the FDA for treating COVID-19 patients. OBJECTIVE: The study intended to examine the data from studies on clinical management of COVID-19. DESIGN: The research team performed a literature review, searching relevant literature databases. The sources of data included bioRxiv, medRxiv, Google Scholar, Embase, PsychINFO, WanFang Data, and PubMed. The search terms were treatment of the novel coronavirus, management of nCoV-19, chloroquine, and hydroxychloroquine. SETTING: The study took place in the main library of the University of Sargodha in Sargodha, Pakistan. RESULTS: The study identified 42 unique studies that had reported and confirmed over 1500 cases of nCoV-19 by April 21, 2020. The studies found that clinical management, for patients who presented with symptoms, included supportive care and control measures that comprised mechanical ventilator support and supplementary oxygen. CONCLUSIONS: There have been intensive attempts to explore drug therapy for the prophylaxis and treatment of SARS-CoV-2 infection during this COVID-19 pandemic. Several drugs have been identified which including remdesivir, two antimalarials (chloroquine and hydroxychloroquine) and immunosuppressive agents. The effects of most drug interventions are currently highly uncertain and several drugs and vaccines are under trail for the effective treatment of COVID-19 virus, until an effective treatment will discover social distancing and physical hygiene should be practiced strictly.
Assuntos
COVID-19 , Pandemias , Antivirais/uso terapêutico , China , Humanos , Paquistão , SARS-CoV-2RESUMO
Rumex dentatus has been used traditionally for ailment of cardiovascular diseases. The aim of the present study was to assess cardiovascular effects in isolated perfused rabbit heart. Aqueous and n-butanolic fractions were assessed for their effect on perfusion pressure (PP), force of contraction (FC) and heart rate (HR) of rabbit heart using Langendorff's method. The possible mechanisms of action of extracts/fraction were assessed with and without application of different agonist/antagonist. Phytochemical, toxicity and anti-oxidant activities were also determined. Both extracts at 1mg/mL dose produced a highly significant decrease in FC and HR but PP remained unchanged. Moreover, aqueous fraction of Rumex dentatus at 0.001mg/mL dose produced a highly significant decrease in FC and HR but no significant change in PP was observed. Atropine 10-5 M did not inhibit the cardiac depressant response of both fractions. Furthermore, both fractions blocked the positive ionotropic and chronotropic effects of adrenaline and calcium chloride. Phytochemical studies have shown the presence of some phytochemicals. Acute and sub-chronic toxicity studies demonstrated that test extracts are safe and produced no significant changes in haematological and biochemical parameters. Crude extract showed significant antioxidant activity like ascorbic acid. This study revealed that this plant have good cardiac depressant effect.
Assuntos
Antioxidantes/farmacologia , Fármacos Cardiovasculares/farmacologia , Coração/efeitos dos fármacos , Preparação de Coração Isolado , Extratos Vegetais/farmacologia , Rumex/química , Animais , Atropina/farmacologia , Cloreto de Cálcio/farmacologia , Fármacos Cardiovasculares/efeitos adversos , Epinefrina/farmacologia , Feminino , Frequência Cardíaca/efeitos dos fármacos , Preparação de Coração Isolado/métodos , Masculino , Camundongos , Contração Miocárdica/efeitos dos fármacos , Extratos Vegetais/efeitos adversos , Coelhos , Ratos , Ratos Sprague-Dawley , Rumex/efeitos adversosRESUMO
Present study was conducted to validate the folkloric claims of morus nigra l. (moraceae) using invasive blood pressure measuring and ex vivo vasorelaxant experimental techniques. Intravenous administration of mn. Aq in 0.01-30 mg/kg doses caused significant decrease in mean arterial pressure and heart rate in fructose-induced hypertensive rats. It also showed relaxation in high k+ [80 mm] and pe (1µm) mediated aortic contraction with ec50 1.25 and 3.72mg/ml values, respectively. Vaso-relaxant effect of mn.aq was partially blocked in presence of l-name with ec50, 5.32mg/ml value, but showed concentration dependent significant inhibition of ligand gated and voltage gated ca+2 channels and intracellular ca+2 release, similar to verapamil. Findings of current study designate that aqueous fraction of m. Nigra possesses antihypertensive activity with concentration-dependent vaso-relaxant effect predominantly mediated through endothelial-independent calcium channel blocking pathways accompanied by partial involvement of endothelium-dependent nos mediated relaxation.
Assuntos
Anti-Hipertensivos/farmacologia , Canais de Cálcio/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Hipertensão/tratamento farmacológico , Morus/química , Extratos Vegetais/farmacologia , Administração Intravenosa , Animais , Pressão Sanguínea/efeitos dos fármacos , Modelos Animais de Doenças , Frutas/química , Frequência Cardíaca/efeitos dos fármacos , Masculino , RatosRESUMO
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 acdisolâ (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/químicaRESUMO
CONTEXT: The novel Corona Virus (nCoV-19) was initially reported in Wuhan, China during December 2019, and later people with nCoV-19 were identified in different parts of the world. Infected people had shown symptoms resembling pneumonia, but about 50% of patients were asymptomatic. OBJECTIVE: The study intended to examine the data from studies on nCoV-19. DESIGN: The research team performed a literature review, searching relevant literature databases. The sources of data included bioRxiv, medRxiv, Google Scholar, Embase, PsychINFO, WanFang Data and PubMed. The search terms were novel Corona Virus, and nCoV-19 structure. SETTING: The study took place in the main library of the University of Sargodha, Sargodha, Pakistan. RESULTS: The study identified 22 studies that had reported and confirmed over 2000 cases of nCoV-19 by January 26, 2020. The studies found that the virus was transmitted through respiratory droplets. The virus has two serotypes, OC43 and 229E. CONCLUSIONS: No specific curative therapy is available for CoVid-19. However, certain precautionary measures may potentially reduce the transmission, including washing hands, using sanitizers frequently, avoiding public gatherings, and quarantining or isolating patients. This virus has spread globally and immunocompromised individuals, and especially older individuals, are at significant risk. Community and healthcare professionals have a positive role to play in controlling the spread of the disease.
Assuntos
Betacoronavirus/classificação , Infecções por Coronavirus/epidemiologia , Infecções por Coronavirus/prevenção & controle , Pandemias/prevenção & controle , Pneumonia Viral/epidemiologia , Pneumonia Viral/prevenção & controle , COVID-19 , Humanos , SARS-CoV-2 , SorogrupoRESUMO
Topical candidiasis is a known skin fungal infection which is usually treated by conventional dosage forms such as cream, gel, emulgel which are having numerous adverse effects on skin. To overcome such disadvantages, different novel drug delivery systems have been considered. Polymer based nano-particulate systems have shown good skin penetration after topical application. Therefore, in the present study the main focus was on the pathology, pathogenesis, and consequently topical treatment of candidiasis. Nanogel containing miconazole have been prepared from the natural polymers i.e. gelatin and chitosan. The nanogel of miconazole (100 mg) nitrate was formulated by modified emulsification-diffusion technique and characterized for different parameters. From all the seven nanogel formulations named as F1 to F7, F1 (Gelatin and Chitosan in the percentage of 82.85 and 17.15 respectively) have been selected as model formulations. The reason behind that was as per ICH stability guideline, the formulations F1 was found optimum and stable. Miconazole nanogel formulations F1 also showed the maximum release i.e. 78 % approximately. XRD showed the formulated nanogel was in crystalline shape. In summary, the miconazole nanogel drug delivery systems have two main advantages i.e. they are topical preparation as well as nano sized. It can be postulated that nanogel may be a best approach to treat the fungal skin diseases.
Assuntos
Antifúngicos/administração & dosagem , Sistemas de Liberação de Medicamentos , Miconazol/administração & dosagem , Animais , Composição de Medicamentos , Estabilidade de Medicamentos , Feminino , Camundongos , Miconazol/química , Nanogéis , Polímeros/química , Espectroscopia de Infravermelho com Transformada de Fourier , ViscosidadeRESUMO
In the present study, we synthesized silver (Ag) nanoparticles using aqueous extracts of clove (Syzygium aromaticum) (SAE). This synthesis of green silver nanoparticles (AgNP) was a novel and effectual tool against the Newcastle Viral Disease (NDV). Syzygium aromaticum extract was used as reducing and stabilizing agent for synthesis of silver nanoparticles. AgNP were characterized using diversity of biophysical methods inclusive of Fourier transform infrared spectroscopy (FTIR), UV-VIS spectroscopy and Transmission electron microscopy (TEM) for morphology and size. Furthermore, XRD analysis confirmed the crystalline nature of the particles. In current investigations, the antiviral activity of clove buds silver nanoparticles was inspected in-vitro and in-ovo. Embryonated chicken eggs were used to perform the cytotoxicity assay of the clove extract silver nanoparticles (CESN). CESN showed in vitro antiviral activity against NDV in embryonated eggs.
Assuntos
Antivirais/farmacologia , Nanopartículas Metálicas/administração & dosagem , Extratos Vegetais/farmacologia , Prata/farmacologia , Syzygium/química , Animais , Galinhas , Química Verde/métodos , Doença de Newcastle/tratamento farmacológico , Vírus da Doença de Newcastle/efeitos dos fármacos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Água/químicaRESUMO
The present study was aimed to evaluate the effect of educational intervention provided to the patients of hypertension through pharmacist with the goal to improve knowledge about hypertension, adherence to prescribed medicines, blood pressure control and HRQoL(Health Related Quality of Life).A total of 384 patients were assigned randomly into 2 groups including intervention and control groups each having 192 patients. Urdu versions of knowledge questionnaire regarding hypertension, medication adherence scale (MMAS-U) by Morisky and EuroQol scale (EQ-5D) were utilized. Each patient's blood pressure was measured. After educational intervention, an increase was found in mean knowledge score about hypertension (18.18 ± 4.00), adherence score (5.89 ± 1.90), HRQoL score (0.73 ± 0.12) and Visual Analogue Scale (VAS) score (69.39 ± 5.90) among the IG. The blood pressure control also improved and lower systolic (131.81 ± 10.98 mmHg) and diastolic blood pressures (83.75 ± 6.21 mmHg) were observed among the patients of IG. This study showed that educational programs are useful for patients in increasing patient's levels of knowledge about hypertension, improving adherence to prescribed medication and enhancing blood pressure control. This increase is in turn accountable to improve HRQoL.
Assuntos
Conhecimentos, Atitudes e Prática em Saúde , Hipertensão/psicologia , Adesão à Medicação/psicologia , Farmacêuticos/psicologia , Papel Profissional/psicologia , Qualidade de Vida/psicologia , Adulto , Idoso , Anti-Hipertensivos/uso terapêutico , Pressão Sanguínea/efeitos dos fármacos , Pressão Sanguínea/fisiologia , Feminino , Humanos , Hipertensão/tratamento farmacológico , Masculino , Pessoa de Meia-Idade , Educação de Pacientes como Assunto/métodos , Educação de Pacientes como Assunto/tendências , Farmacêuticos/tendênciasRESUMO
The current study was designed to evaluate mucoadhesive buccal tablet containing metronidazole (MTZ) for local action aided by Hydroxypropylmethylcellulose K4M (HPMC) and Carbopol 940® (CP) as mucoadhesive polymers with other ingredients like sodium starch glycolate (SSG), polyvinyl pyrollidone K30 (PVP) as disintegrant and binders respectively. Formulations (F1-F8) were prepared by direct compression method and characterized for different physicochemical parameters. Results showed that the average weight and friability were within USP limits. Maximum mucoadhesive time was observed for F2 (14 hr) containing moderate amount of HPMC and CP used in the study. Up most mucoadhesive strength value was observed with F3 containing highest amount of HPMC used. Results indicated that high amount of HPMC was linked with the moderate to higher mucoadhesive strength and time. Maximum swelling index was observed in F7 (191.3%). Only F1-F3 showed complete in vitro MTZ release within 3 hr. Formulations containing PVP released MTZ incompletely over time while SSG released earlier. Formulation F1 was considered best in terms of MTZ release (100.5%) with diffusion based Korsmeyer-Peppas release kinetics. Therefore, MTZ exhibiting best physicochemical characters in mucoadhesive buccal tablet was found in F1 containing HPMC and CP in amounts of 37.5 mg and 25 mg, respectively, for local action.
Assuntos
Anti-Infecciosos/química , Desenvolvimento de Medicamentos/métodos , Gengivite , Metronidazol/química , Mucosa Bucal , Periodontite , Adesividade , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/análise , Gengivite/tratamento farmacológico , Gengivite/microbiologia , Humanos , Derivados da Hipromelose/administração & dosagem , Derivados da Hipromelose/análise , Derivados da Hipromelose/química , Metronidazol/administração & dosagem , Metronidazol/análise , Mucosa Bucal/efeitos dos fármacos , Mucosa Bucal/microbiologia , Periodontite/tratamento farmacológico , Periodontite/microbiologia , ComprimidosRESUMO
Solubility is concerned with solute and solvent to form a homogenous mixture. If solubility of a drug is low, then usually it is difficult to achieve desired therapeutic level of drug. Most of the newly developed entities have solubility problems and encounter difficulty in dissolution. Basic aim of solubility enhancement is to achieve desired therapeutic'level of drug to produce required pharmacological response. Different techniques are being used to enhance the solubility of water insoluble drugs. These techniques include particle size reduction, spray drying, kneading method, solvent evaporation method, salt formation, microemulsions, co-solven- cy, hydrosols, prodrug approach, supercritical fluid process, hydrogel micro particles etc. Selection of solubility improving method depends on drug properties, site of absorption, and required dosage form characteristics. Variety of polymers are also used to enhance solubility of these drugs like polyethylene glycol 300, polyvinyl pyrrolidone, chitosan, ß-cyclodextrins etc.
Assuntos
Portadores de Fármacos , Excipientes/química , Preparações Farmacêuticas/química , Polímeros/química , Solventes/química , Tecnologia Farmacêutica/métodos , Água/química , Química Farmacêutica , Composição de Medicamentos , Tamanho da Partícula , SolubilidadeRESUMO
Irrational drug use practices are a burden to healthcare facilities. Poor prescribing practices affect the overall management and cost of treatment of non-communicable diseases that are the major cause of mortality and morbidity worldwide. In an effort to improve prescribing practices, this study was designed to assess prescribing, consultation and facility indicators in healthcare facilities of Punjab and Sindh provinces of Pakistan from December 2012 to December 2013. In this cross-sectional study, random and convenient sampling were used to collected data from both private and public healthcare facilities. Quantitative data were collected using structured questionnaire, observations and prescription analysis, whereas qualitative information on factors influencing prescribing practices was obtained by interviewing medical practitioners. A total of 13693 prescriptions were obtained from 500 patient-prescriber encounters. Results show that history taking, physical examination and diagnoses were adequate while generic prescribing was four-fold less than drugs prescribed by brands. Average number of drugs prescribed was 4.63 with more prescribing tendency in private facilities. 45.07% prescription costs were less than Rs. 150. Sulfonylureas, statins and ACE inhibitors were highly prescribed drugs for diabetes, hyperlipidemia and hypertension. Prescribing practices were dominantly influenced by severity of disease (73% Punjab; 81% Sindh), patient age (75% Punjab; 68% Sindh) and availability of drugs (62% Punjab; 56% Sindh) whereby 91% practitioners in Sindh and 52% in Punjab rely on medical representatives as the source of drug information. Moreover, the pharmacy and therapeutic committees in all facilities were non-functional along with non-availability of essential drug list in 87% health facilities. Thus, there are considerable opportunities to improve the rational use of medicines in Pakistan including low prices for generics, physician education, prescribing guidelines and formularies.
Assuntos
Tratamento Farmacológico/estatística & dados numéricos , Prescrição Inadequada/estatística & dados numéricos , Adulto , Idoso , Estudos Transversais , Uso de Medicamentos , Medicamentos Genéricos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Paquistão , Assistência Farmacêutica , Adulto JovemRESUMO
Alendronate sodium, a bisphosphonate drug, it is used to treat osteoporosis and other bone diseases. The present study was designed to conduct comparative bioavailability analysis of oral formulations of aledronate sodium through an open-label, randomized, 2-sequence, 2-period crossover study. Healthy adult male Pakistani volunteers received a single 70 mg dose of the test or reference formulation of alendronate sodium followed by a 7 day washout period. Plasma drug concentrations were determined using a validated HPLC post column fluorescence derivatization method. AUC(01,) AUC(0-8,) C(max). and T(max) were determined by non-compartmental analysis and were found within the permitted range of 80% to 125% set by the US Food and Drug Administration (FDA). Results show that both in vitio and in vivo assays of all test brands were within the spec- ification of the US Pharmacopoeial limits and were statistically bioequivalent. No adverse events were reported in this study.
Assuntos
Alendronato/farmacocinética , Conservadores da Densidade Óssea/farmacocinética , Administração Oral , Adulto , Alendronato/administração & dosagem , Área Sob a Curva , Disponibilidade Biológica , Estudos Cross-Over , Composição de Medicamentos , Humanos , MasculinoRESUMO
The microbial and chemical analysis of illicit drug samples from different areas of Pakistan i.e. Quetta, Karachi, Lahore and Islamabad was conducted in a cross-sectional study at National Institute of Health, Islamabad. The drug samples were confiscated by Anti Narcotics Force (ANF), Pakistan. Microbial analysis was done by estimating bioburden which revealed the presence of gram negative and positive bacteria's, fungus, Streptococcus, Staphylococcus species. Trypton soya agar was used for total aerobic count, MacConkey agar for gram-negative bacteria, Sabouraud dextrose agar for fungus and Vogel-Johnson agar for Streptococcus and Staphylococcus species. Colour tests were applied to identify the drug samples. Qualitative and quantitative analysis of suspected samples of Heroin, morphine, cocaine and acetic anhydride was made by employing different chromatographic techniques i.e. Thin-layer chromatography (TLC) and High-performance liquid chromatography (HPLC). The samples were found to be adulterated with paracetamol, diazepam and Dextromethorphen. Acetic anhydride was adulterated with hydrochloric acid (HCl). There is lack of information providing structured advice on responses to the consequences of illicit drug adulteration. Robust and rehearsed interventions and communication strategies would provide a basis for response for a wide variety of organisations. Research into the usefulness of media warnings about adulteration of illicit drugs is required.
Assuntos
Bactérias/isolamento & purificação , Contaminação de Medicamentos , Tráfico de Drogas , Fungos/isolamento & purificação , Drogas Ilícitas/análise , Técnicas Bacteriológicas , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Estudos Transversais , Humanos , Drogas Ilícitas/efeitos adversos , Paquistão , Medição de RiscoRESUMO
Present investigation concern with combination of two drugs for the treatment of gout. One of these drug (naproxen sodium) is pain killer which is sustain their action within the body for 12 hours and the other drug (colchicine) is anti-gout, which release as conventional dosage. After oral administration naproxen will act as sustain release dosage and increase patient compliance about six batches of tablet were developed and evaluate .For the sustain release action polymers Methocel K4M and HPMCK15were used. These polymers were used in combination used with other inactive ingredients. Two methods were used for proration of final tablets. In 1st method only naproxen sodium granules were prepared which are sustained released. In second method these granules were mixed with colchicines powder and other all inactive ingredients. This method is easy and cost effective characterization of pallets and final tablets were performed. Final tablets were evaluated for all tests like appearance, friability, dissolution, hardness, assay, weight variation and in-vitro release study performed. The results obtained were satisfactory and complies with USP specification. Formulation containing combination of Methocel K4M and HPMC K15 showed good sustain release profile for 12 hours.
Assuntos
Colchicina/química , Supressores da Gota/química , Naproxeno/química , Administração Oral , Colchicina/administração & dosagem , Preparações de Ação Retardada , Combinação de Medicamentos , Composição de Medicamentos , Estabilidade de Medicamentos , Supressores da Gota/administração & dosagem , Derivados da Hipromelose/química , Cinética , Modelos Químicos , Naproxeno/administração & dosagem , Solubilidade , Comprimidos , Água/químicaRESUMO
Medicinal plants are crucial for about 80% of the world population in developing and developed countries for their primary and basic health care needs owing to better tolerability, superior compatibility with human body and having lesser side effects. The present study was conducted on various solvent extracts of three plant samples of Indian and Nepali origin Swertia Chirayita (Roxb.) Buch-ham (Chiratia) collected from various places to establish their comparative phytochemical analysis, chromatographic profile, hepatoprotective and antioxidant activities. Nepali Swertia Chirayita was found to have finest Chromatographic profile (TLC). Phytochemical analysis revealed Alkaloids, flavonoids, saponins, ascorbic acid, glycosides, steroids and triterpenoids in all samples. Different solvent fractions of the methanolic plant extracts of Swertia chirayita were assessed for hepatoprotective activity by carbon tetrachloride-induced liver damage in rats. The grade of protection was measured by using biochemical parameters such as serum glutamate oxalate transaminase (SGOT/AST), alkaline phosphatase (ALP), serum glutamate pyruvate transaminase (SGPT/ALT) and total bilirubin. The in-vitro antioxidant activity of the extracts was also evaluated by the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay. The methanolic and aqueous extracts, at a dose of 200mg/kg and 300mg/kg, produced significant (p<0.05) hepatoprotection by decreasing the activities of the serum enzymes and bilirubin while there were marked scavenging of the DPPH free radicals by the fractions. Decreased observed in the biochemical parameters suggests that the plant extracts possesses hepatoprotective as well as antioxidant activities without any significant variation amongst them. These activities reside mainly in the methanolic extract of whole plant.
Assuntos
Antioxidantes/farmacologia , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Swertia/química , Tetracloreto de Carbono , Cromatografia em Camada Fina , PaquistãoRESUMO
Niosomes has gained tremendous popularity as ultimate drug carrier. Lot of research work is being carried out on preparation of niosomes for ophthalmic use having no significant effect on vision and its sustained release pattern. Chloramphenicol niosomes were prepared using two different ratios of cholesterol, drug and surfactant, termed as EIN-1, EIN-2 by ether injection method and their entrapment efficiency, particle size. The in vitro drug release pattern was observed for ten hours. The EIN-2 showed 90% entrapment and released 81% of entrapped drug after 10 hours. Zeta potential & viscosity were determined and in-vivo comparison was made with Chloramphenicol eye drops where it exhibited Cmax of 15 µ g/ml. Stability studies were done to determine shelf life. MIC of selected strain of S. aureus was also determined. EIN 2 niosomal suspension was compared with Chloramphenicol eye drops in experimental conjunctivitis in albino rabbits. In-vitro studies are encouraging as niosomes released about 75% of total entrapped drug by EIN-1 and 81% of total entrapped drug by EIN 2. In vivo study shows that niosomes released the drug in eye in acceptable range and showed a sustained release pattern without affecting the vision. Niosomes were found ultimate ophthalmic drug carriers capable to release drug in sustained and determined pattern.