The objective of the work is to enhance the solubility, dissolution, and pharmacokinetic properties of glibenclamide (GLB) via cocrystallization technique.
Glibenclamide is an oral hypoglycemic agent ...used for treating non-insulin-dependent (type II) diabetes mellitus. It exhibits poor aqueous solubility and oral bioavailability, thereby compromising its therapeutic effect. Therefore, utilizing cocrystal approach for enhancing the solubility will modulate the physicochemical properties of GLB without altering its molecular structure.
Cocrystal was prepared by solution crystallization method using coformer malonic acid. The cocrystal was characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared (FT-IR) studies. The prepared cocrystal was subjected to solubility, in vitro dissolution, and pharmacokinetic studies.
The DSC endotherms, PXRD patterns, and the FT-IR spectra of the cocrystal established the formation of a cocrystal. The formation of eutectic mixture was refuted upon comparing the DSC endotherm and PXRD pattern of the cocrystal with that of the physical mixture. GLB showed a twofold enhancement in solubility and a significant improvement in the rate of dissolution (p < 0.05, independent t-test) after cocrystallization. The pharmacokinetic parameters on male Sprague Drawly rats showed 1.45 enhancement in AUC
0-24
and 1.36-fold enhancement in the C
max
of GLB as compared to the pure drug.
These findings demonstrate that cocrystallization technique was able to tailor the solubility and dissolution profile of GLB leading to an enhanced pharmacokinetic property.
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IJS, IZUM, KILJ, NUK, PILJ, SAZU, UL, UM, UPUK
OBJECTIVES: Psoriasis is a chronic inflammatory disease showing co-existence with metabolic syndrome (MS), as has been confirmed by numerous epidemiologic studies in recent times. In this study, the ...aim was to ascertain the beneficial effects of pioglitazone in psoriasis, simultaneously targeting the improvement of MS parameters.
MATERIALS
AND METHODS: We conducted a prospective randomized open-labeled parallel-group interventional study in patients of moderate-to-severe chronic plaque psoriasis. A total of 90 patients were inducted in study and divided into three groups of standard treatment (methotrexate 7.5 mg/week for 12 weeks), active treatment (pioglitazone 15 mg tablets once daily for 12 weeks), and their combination. Primary outcome was taken as percentage Psoriasis Area and Severity Index (PASI) improvement from baseline; secondary outcomes were PASI-75, safety profile, and MS parameters.
RESULTS: Intergroup evaluation of PASI score showed that standard treatment methotrexate and active treatment pioglitazone were comparable. Combination of methotrexate and pioglitazone proved superior in efficacy from both standard and active treatment in 8 and 12 weeks. Adverse drug reactions were mild and treated symptomatically. Pioglitazone and combination group also demonstrated beneficial efficacy in parameter of MS hence establishing it as a potential therapy in psoriasis with MS.
CONCLUSIONS: Pioglitazone alone or in combination with standard treatment may be a safe alternative drug for psoriasis coexisting with MS proving beneficial for both.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
Novel nanovesicular gel of
extract was developed and evaluated for its anti-inflammatory and antipsoriatic activity.
Transferosomes were prepared using soya phosphatidylcholine and edge activators ...(Tween 80, Span 80, and sodium deoxycholate) by a modified lipid film hydration technique using rotary evaporator and evaluated for various parameters. The quantification and standardization of extract have been carried out using its alkaloid content as berberine as biomarker. Topical application of imiquimod (IMQ) (immune modifier) on the shaved back of mice developed psoriasis-like inflammation followed by histopathological study of inflamed skin.
The size of transferosomes was in the range of 265-345 nm whereas polydispersity index ranges from 0.10 to 0.63, and for zeta potential, it was from -19.3 to -43.3 mV. Transferosomes were further added to Carbopol 934P for gel formation and subsequently evaluated for their physicochemical properties. Their efficacy against inflammation, IMQ-induced psoriasis, and skin sensitivity was compared with conventional formulation (commercial formulation-Angle Gloss, Phytolab Pvt. Ltd.). Percent inhibition of edema by transferosomal gel (55.76%) was more as compared to conventional gel of extract (33.5%) found out by Carrageenan-induced paw edema method. Primary irritation index was found to be <0.4 inferring its safe use for topical formulation.
Histopathological report showed that, in psoriasis-induced animal treated with topical application of extract loaded transferosomal gel showed a marked reduction in thickness of epidermis, length of rete ridges as compared to conventional gel formulation. It can be inferred that
extract loaded transferosomal gel can function as potential anti-inflammatory and antipsoriatic formulation.
The objective of the present research work was to prepare
extracts (roots, ethanolic 70%v/v) loaded transferosomal gel, to perform
characterization and
evaluation of their efficacy against inflammation as well as imiquimod (IMQ)-induced psoriasis in animalsThe remarkable enhancement in the
release efficiency of
extract loaded transferosomal gel resulted in improved anti-inflammatory activity. The prepared novel formulation of
has also shown its efficacy against IMQ-induced psoriasis.
SPC: Soyaphosphatidylcholine, PDI: Polydispersity index, IMQ: Imiquimod, EA: Edge activator, BE: Berberine, TEM: Transmission electron microscopy, PBS: Phosphate buffered saline, H and E: Hematoxylin and eosin, ZP: Zeta potential, EE: Entrapment efficiency.
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...there is a need to search for therapeutic options for the treatment of MS. Aims and Objective: The present study was conducted to evaluate the protective effect of Pterocarpus marsupium (Bijasar) ...in animal model of high carbohydrate diet-induced MS. Materials and Methods: Adult male Wistar rats were divided into three groups. 6 The patient compliance is also poor as there is frequent and multiple dosing schedule. ...there is a need to explore newer molecular entities for the treatment of this syndrome. 9 Thus, the present study was conducted to evaluate the protective effect of P marsupium on the body weight, abdominal circumference (AC), blood sugar, and serum triglycerides in animal model of high carbohydrate dietinduced MS. MATERIALS AND METHODS Animals Wistar rats (Rattus norvegicus) of either sex weighing 150250 g and aged about 6-8 weeks were used in the study. 18 The study demonstrated the potential therapeutic benefits of P. marsupium in the treatment of various components of MS. The limitations of the study were that, due to the time constraint, we could not discuss the potential therapeutic benefits of P marsupium on the chronic complications of MS. CONCLUSION The study concluded that high sucrose diet may lead to the development of various changes associated with MS. There was a reduction in body weight, AC, blood sugar, and serum triglycerides in animals treated with P marsupium.
Background: The present work has been planned to find out the effect of Punica granatum and Rosuvastatin on learning and memory in Scopolamine induced cognitive deficits in rats. Scopolamine being an ...anticholinergic agent is used fervently in experimental models for memory deficits and has been widely implicated for the screening of cognitive dysfunction. Punica granatum (Pomegranate) has shown to suppress tumor neuronal cells, hence it can be a potential agent in providing neuroprotection for preventing the development and progression of AD. There are conflicting reports indicating the role of statins as a neuroprotective agent. This contradiction led us to investigate the effect of the role of Rosuvastatin on memory. The test agents were further compared to the standard treatment group acetylcholinesterase inhibitor i.e. Donepezil.Methods: Male wistar rats 150-200gms were divided into 4 groups of 6 rats each. Amnesia was induced by scopolamine 3mg/kg ip at day 5 in all the groups. Group1 (amnesic control) given distilled water; group 2(standard treatment i.e. Donepezil 0.5mg/kg orally); group 3(Rosuvastatin group10mg/kg orally); group 4 (Punica granatum juice 500mg/kg orally) The methods for validating cognition deficits were behavioural tests like Cook’s pole response and Passive Avoidance response.Results: It was evident from our research that the Punica granatum juice and Rosuvastatin effectively antagonized the scopolamine induced cognitive impairment in the paradigms studied. The neuroprotective effect of Punica granatum juice was better as compared to the Rosuvastatin group and the effects of the former were comparable with the standard treatment i.e. Donepezil group.Conclusions: Punica granatum has a remarkable protective role in memory function, learning, cognition and behavior in Scopolamine induced amnesia model of Alzheimer’s disease which was better than Rosuvastatin treatment.
Background: The study has been performed to evaluate the efficacy of budesonide delivery by different form of devices like nebulizer, metered dose inhaler and dry powder inhaler to adult patients of ...chronic stable bronchial asthma. The changes in pulmonary function test parameters have been consider for evaluation.Methods: This prospective study was undertaken to assess the relative efficiency of budesonide administered from devices like nebulizer, metered dose inhaler and dry powder inhaler in adult patients of chronic stable bronchial asthma. Fifty subjects where administered budesonide (1mg) via nebulizer, budesonide (400 microgram) by metered dose inhaler and dry powder inhaler consecutively each week for four weeks under direct supervision. To analyze the effect of budesonide delivered through different devices pulmonary function test was carried out on the subject before and one hour after administration of the drug on each visit.Results: No significant difference in Peak expiratory flow rate (P=0.77), forced expiratory volume in one second (P=0.851), forced vital capacity (P=0.178) and forced expiratory volume in one second and forced vital capacity ratio (P=0.298) was seen after giving budesonide by different devices.Conclusions: Budesonide delivered by different devices (nebulizer, metered dose inhaler, and dry powder inhaler) have similar effect on lung function in patients of chronic stable bronchial asthma. In the daily clinical practice, the correct choice of an inhaler device should be related with the patient's characteristics. They may be used interchangeably depending on availability, cost and compliance of the patients.
Objective: The objective of our study is to assess the prescription and drug utilization pattern in a tertiary care teaching and referral hospital in Uttar Pradesh, to investigate the rational use of ...drugs.
Methods: The study was carried out in the general medicine outpatient department (OPD) setting for a period of 3 months in our tertiary care teaching and referral hospital. The prescriptions were randomly sampled and the photocopies of all the prescriptions were obtained from the OPD during the period of the study and were processed and analyzed for the demographic profile, drug profile, fixed-dose combinations, therapeutic classes of antibiotic prescribed, morbidity profile according to the disease pattern, and prescription pattern including the errors in prescription and the assessment of polypharmacy.
Results: A total of 350 prescriptions were randomly sampled, out of which 312 prescriptions were fit to be analyzed. The total number of drugs in 312 prescriptions was 1022. Basic information of patient was written in 79.25% prescriptions, 84.25% prescriptions were legible, and only 71.21% prescriptions were complete. The majority of prescriptions had at least five drugs ordered which constituted around 43.14% of total number of prescriptions leading to polypharmacy.
Conclusions: Our study highlights that there is a scope for improvement in prescribing patterns in areas of writing legible and complete prescriptions. To lay down the principles of rational pharmacotherapeutics, proper training of the prescribers on rational prescription writing is the need of an hour for improving the quality of prescriptions.
Introduction: COVID 19 disease has wrecked a havoc as pandemic in the entire world. It causes cardiac manifestations, digestive system disturbances, and adversely affecting other organs. As a result, ...ardent efforts are underway to find effective antiviral treatments targeting possible mechanisms to identify a specific medication for the disease to curb its progression and to prevent patients sufferings, one such therapy being injectable antiviral treatment namely, Remdesivir. Objectives: To evaluate the clinical outcomes and safety profile of Remdesivir in COVID-19 patients in a tertiary care center. Methods: An observational retrospective cohort study was planned with sample size of 210 patients suffering from active moderate to severe COVID 19 disease admitted in a single center tertiary care hospital requiring injectable anti-viral therapy that is Remdesivir. Patient data was collected from the case record forms. Primary outcomes in terms of length of hospital stay, duration of treatment with Remdesivir, survival rate in patients on Remdesivir and assessment of the days for the COVID 19 positive test to eventually become negative in patients and secondary outcome in terms of safety were evaluated. Results: There was a clinically significant improvement in the SPO2 levels from the time of admission till discharge. The appearance of adverse effects was taken as the secondary outcome. Hepatic and renal toxicity was observed after completion of treatment whereas no immunological abnormalities were observed. Conclusion: Until stronger evidences come to the fore, we cannot derive substantial inference that our injectable antiviral therapy drug namely, Remdesivir is efficacious for treating COVID-19.
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