Step 3: Add Solution A to Solution B under ultra-shear homogenization and continue ultra-shear homogenization at speed 6000 rpm for 30 min.Step 4: Add purified water under ultra-shear homogenization drop wise in the centre of the container. The dispersion is further homogenized for 15 min at room temperature with homogenization speed 6000 rpm.Step 5: Formulated Ethosomes forms the cloudy homogenous liquid. The Ethosomes were stored at temperature 4°C ± 0.5°C for further evaluation (Table 1) [3,7-9]. Preparation of gel:Step 1: Ethosomes equivalent to 1% of Tramadol HCl is calculated. AbstractTopical administration of drugrs is better for local action and the efficiency of the topically administered drug is increased with Liposome, proliposomes and ethosomes. Tramadol HCl has used the local anaesthetic. Ethosomes were formulated using soya lecithin, cholesterol, ethanol and purified water using ultra shear homogenizer. Ethosomes were evaluated for vesicle size, shape, optical microscopy and in-vitro release study. FS05 and FC05 have better drug release profile than the other formulation. The ethosomes were entrapped in gel matrix of carbopol 980 in different concentration 0.75%, 1.00%, 1.25% and 1.50% w/w. The formulated gel formulation were evaluated with parameter drug content, pH, viscosity, spreadability, in-vitro release test, and ex-vivo study. The formulation FS05 C03 and FC05 C03 have better in-vitro and ex-vivo drug release profile which contains Carbopol 980 concentration 1.25%w/w. Both the formulation FS05 C03 and FC05 C03 were stable for 3 Months at room temperature and accelerated storage condition. The 3 M stability sample of FS05 C03 has maintained the drug release profile but the drug release profile of formulation FC05 C03 has dropped significantly.
Aim/Background: Nifedipine (NIF) is act as Calcium channel blocker which belongs to chemical class dihydropyridine and used in the treatment of hypertension. An anal fissure (AF) is the most common anorectal conditions encountered in clinical practice. Patient anal fissures experience anal pain with defecation and minor bleeding. Emulgel formulations are considered a combination of emulsion and gels and emulgel has advantages of both. Emulgels have better penetration of actives than conventional topical formulations. Materials and Methods: Emulgel formulations are prepared with the lowest concentration of emulsifiers 1.5-4.0%. Carbomer homopolymer type C used as a polymeric emulsifier while formulating the formulation. The concentrations of Polymeric emulsifiers, high HLB surfactant and low HLB surfactants are varied to two level concentrations two optimize the formulations. Sorbitan monooleate and Polysorbate 20 used as surfactants. Results: Emulgel formulations are evaluated for homogeneity, consistency, grittiness, compatibility, pH, Viscosity, drug content, spreadability, extrudability and in-vitro drug release from the formulations. The optimized formulation has been charged for stability study at room temperature and accelerated storage condition. Stability results are similar to the initial results. In-vitro drug release profile of the initial time point versus 3M stability time point at accelerated and room temperature storage condition is similar. Conclusion: Carbomer homopolymer type C can be employeed as polymeric emulsifiers to stabilize unstable to stable emulsion.
Levonadifloxacin is a novel benzoquinolizine subclass of fluoroquinolone, active against quinolone-resistant Staphylococcus aureus. A phase 3 trial for levonadifloxacin and its oral prodrug was recently completed. The present study identified area under the concentration-time curve for the free, unbound fraction of a drug divided by the MIC (fAUC/MIC) as an efficacy determinant for levonadifloxacin in a neutropenic murine lung infection model. Mean plasma fAUC/MIC requirement for static and 1 log10 kill effects against 9 S. aureus were 8.1 ± 6.0 and 25.8 ± 12.3, respectively. These targets were employed in the selection of phase 3 doses.
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