The purpose of this research was to optimize the formulation factors for maximum in vitro permeation of gatifloxacin from aqueous drops through excised goat cornea and to evaluate the permeation characteristics of drug from selected marketed eyedrop formulations. Permeation studies were conducted by putting 1 mL of formulation on the cornea (0.67 cm 2 ) fixed between the donor and receptor compartments of an all-glass modified Franz diffusion cell and measuring gatifloxacin concentration in the receptor (containing normal saline under stirring) by spectrophotometry at 291.5 nm, after 120 minutes. Raising the drug concentration of the drops increased the drug permeation but decreased the percent permeation and the in vitro ocular availability. Raising the pH of the formulation from pH 5 to 7.2 increased both the drug permeation and the in vitro ocular availability. Eyedrops containing benzalkonium chloride (BAK; 0.01% wt/vol) and disodium edetate (EDTA; 0.01% wt/vol) showed maximum permeation, followed by Zymar, BAK (0.01% wt/vol), Gatilox, Gatiquin, and Gate (statistically significant P G .05 compared with control). In vitro titration of the formulations with 0.1N NaOH indicated the presence of a buffer in Zymar (pH 6) and Gate (pH 5.8), which may cause irritation and induce lacrimation, resulting in reduced ocular availability in vivo. Thus, formulation with BAK and EDTA, which is unbuffered, has a better likelihood of being absorbed in vivo. The BAK-EDTA formulation significantly (P G .05) increased the permeation of gatifloxacin through paired excised corneas of goat, sheep, and buffalo, compared with the control formulation. The goat cornea showed the greatest increase in permeation, followed by the sheep and buffalo corneas.
The aim of this study was to prepare and characterise oral delivery of morin hydrate-loaded micellar nanocarriers using Pluronic P127 and Pluronic F123 for the effective management of Alzheimer's disease. After administration of formulation brain and blood drug concentration were found to be highest for optimised morin hydrate-loaded micellar nanocarriers as compared to plain morin hydrate. Significant (p < 0.05) reduction in assessed pharmacodynamic parameters was observed after administration of morin hydrate-loaded micellar nanocarriers as compared to disease control group. Chronic treatment with morin-loaded micelles significantly increased the memory in AlCl induced Alzheimer's disease in Wistar rats.
The aim of the present study is to develop embelin-loaded guar gum microparticles through emulsification technique. The in vitro release of the optimised formulation was found to be 88.5 ± 3.8% in 24 h, has exhibited remarkably sustain and delayed the release of embelin at a specific site. Embelin-loaded microparticles showed average particle size of 12.9 ± 0.75 µm. The statistical analysis was carried out by one-way ANOVA followed by comparison test of Bonferroni. P values < 0.05 were considered as significant. The in vivo study concluded that pre-treatment of embelin prevents dinitrobenzenesulfonic acid (DNBS)-induced colitis in rats and depicts protective activity against ulcerative colitis due to its antioxidant and anti-inflammatory actions. This approach produces comparatively less side effect to another conventional dosage form.
Objective: The objective of the present study was to prepare the fast disintegrating tablet of Ambroxol Hydrochloride for respiratory disorders such as bronchitis, asthma and cough for pediatrics. Material and Methods: The tablets were prepared by direct compression technique. Superdisintegrants such as Sodium Starch Glycolate was optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time and uniformity of drug content. Optimized formulation was further evaluated by in-vitro dissolution test, drug-excipient compatibility and accelerated stability study. Results: Sodium Starch Glycolate was optimized as 4% for formulation on the basis of least disintegration time. 1% Microcrystalline Cellulose was selected as optimum binder concentration on the basis of least disintegration time. Percent weight variation and content uniformity was well within the acceptable limit. The friability was less than 1%. The wetting time and disintegration time was practically good for all formulations. The results obtained with FTIR studies and accelerated stability study showed that there was no interaction between the drug and excipients used in the formulation. Conclusion: It was concluded that by employing commonly available pharmaceutical excipients such as superdisintegrants, hydrophilic and swellable excipients and proper filler a fast disintegrating tablet of Ambroxol Hydrochloride for pediatrics used in respiratory disorders were formulated successfully with desired characteristics which disintegrated rapidly; provide rapid onset of action and enhance the patient convenience and compliance.
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