MAPLE Data Evaluation Applied the Lag-time

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

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Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v8i2.13868 ◽

2018 ◽

Vol 8 (2) ◽

Author(s):

Poreddy Srikanth Reddy ◽

Penjuri Subhash Chandra Bose ◽

Vuppula Sruthi ◽

Damineni Saritha

Keyword(s):

Sodium Alginate ◽

Xanthan Gum ◽

Lag Time ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Matrix Tablet ◽

Compression Technique ◽

Weight Variation ◽

The Matrix

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.

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Gel-based Microemulsion Design and Evaluation for Topical Application of Rivastigmine

Current Pharmaceutical Biotechnology ◽

10.2174/1389201020666191113144636 ◽

2020 ◽

Vol 21 (4) ◽

pp. 298-304

Author(s):

Chih-Wen Fang ◽

Ling-Chun Tsai ◽

Yaw-Syan Fu ◽

Ting-Yu Cheng ◽

Pao-Chu Wu

Keyword(s):

Topical Application ◽

Skin Irritation ◽

Topical Administration ◽

Lag Time ◽

Enhancement Effect ◽

Microemulsion Formulation ◽

Rat Skin ◽

Glycol Monobutyl Ether ◽

Loading Amount ◽

Hydrophilic Gel

Objective: The aim of the present study was to design nanocarriers for the topical application of rivastigmine. Methods: The effect of cosurfactants, hydrophilic gel and loading amount on the permeability of rivastigmine through rat skin was evaluated. Skin irritation tests and stability tests were performed to evaluate the utility of tested formulations. Results: The results showed that the microemulsion formation and characteristics of drug-loaded formulations were related to many parameters of the components. When using microemulsion systems as a vehicle, the permeation rate remarkably increased about 13.2~24.3-fold and the lag time was significantly shortened from 24 h to 4.7 h. Formulations containing a cosurfactant of Diethylene Glycol Monobutyl Ether (DEGBE) showed higher enhancement effect, while increasing the loading dose from 0.5% to 5% further increased the flux about 2.1-fold and shortened the lag time. Conclusion: The drug-loaded experimental formulation did not cause skin irritation and had good stability at 20ºC and 40ºC storage for at least 3 months. The result showed that gel-based microemulsion formulation could be a promising approach for topical administration.

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