Darunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It needs to be combined with ritonavir, which increases the bioavailability to 82%. The aim of this study was to evaluate the in-vivo efficacy of the darunavir-SLN and demonstrate lymphatic transport as a contributing pathway in increasing the drug bioavailability. The SLN was prepared by hot-homogenization technique using GMS as lipid. In-vitro drug release from SLN at the 12th hour was retarded (80.6%) compared to marketed tablet (92.6%). Ex-vivo apparent permeability of the freeze-dried SLN across everted rat intestine was 24 × 10 at 37 °C and 5.6 × 10 at 4 °C. The presence of endocytic process inhibitors like chlorpromazine and nystatin reduced it to 18.8 × 10 and 20.2 × 10, respectively, which established involvement of endocytic mechanism in the uptake of SLN. In-vivo pharmacokinetic studies on rats demonstrated increase in the AUC of SLN (26) as compared to that of marketed tablet (13.22), while the presence of lymphatic uptake inhibitor cycloheximide lowered the AUC of SLN to 17.19 which further led credence to the involvement of lymphatic uptake behind improved bioavailability. The detection of darunavir in the lymphatic fluid of the rats administered with darunavir-SLN further reinforced the conclusion of SLN being taken up by the lymphatic system.
Higher accumulation of liposomal drug in inflammatory area and specific release of liposomes by enteric coated capsules provide better option for the treatment of colonic disease.
Background: Among all available dosage form, tablet is most widely used because of its stability and patient acceptability. The better aesthetic quality like color, texture, mouth feel, and taste masking depended on film and sugar coatings, so the coating is an important part in the formulation of the tablet. The present work aims to comprehensively review the formulation, characterization, and challenges in the development of Tablet in Tablet dosage form. Main text: Film and sugar coatings have the number of disadvantages; most important one is the utilization of aqueous or organic solvent that leads to toxicity. To overcome this problem in the year 1896, Noyes firstly introduced the compression coating or Tablet in Tablet technique. In the development of Tablet in Tablet dosage form, substantial attention among researchers and various research reports and patents inputs can be found in the literature. Also, we focused on the recent advancements in techniques like one-step dry-coating (OSDrC®) for manufacturing Tablet in Tablet dosage form. Conclusion: The current review gathered information on the latest patent, formulation, advantages, and disadvantages of Tablet in Tablet or compression coating. The review also elaborates on the importance of Tablet in Tablet techniques in the development of a modified release system.
Chlorthalidone was subjected to various forced degradation conditions. Substantial degradation of chlorthalidone was obtained in acid, alkali, and oxidative conditions. Further full factorial experimental design was applied for acid and alkali forced degradation conditions, in which strength of acid/alkali, temperature, and time of heating were considered as independent variables (factors) and % degradation was considered as dependent variable (response). Factors responsible for acid and alkali degradation were statistically evaluated using Yates analysis and Pareto chart. Furthermore, using surface response curve, optimized 10% degradation was obtained. All chromatographic separation was carried out on Phenomenex HyperClone C 18 column (250 × 4.6 mm, 5 μ), using mobile phase comprising methanol : acetonitrile : phosphate buffer (20 mM) (pH 3.0 adjusted with o-phosphoric acid): 30 : 10 : 60% v/v. The flow rate was kept constant at 1 mL/min and eluent was detected at 241 nm. In calibration curve experiments, linearity was found to be in the range of 2–12 μg/mL. Validation experiments proved good accuracy and precision of the method. Also there was no interference of excipients and degradation products at the retention time of chlorthalidone, indicating specificity of the method.
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