Formation mechanism of wet-compressed rapidly disintegrating tablets containing a poorly water-soluble model drug

In this project we have prepared the tablets with a coating of pH-sensitive polymer Kollicoat MAE 30DP. For this purpose the core tablets prepared from poorly water soluble model drug and other excipients were coated by a fluidized bed apparatus at the exhaust air temperature of 30°C and spraying rate of 0.55 g/min. The highest coating time was 384 min which leads to the film thickness of 648 µm. The coated tablets were gastric resistant for one hour and resistant against intestinal fluid pH 6.8 up to 70 min. The coating film has a good quality with smoothness and dense packing. However, if the thickness was high e.g. 600 µm the film surface had more wavy structure. The results served to formulate the colon delivery system.

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EFFECT OF CROSSLINKER AMOUNT ON HYBRID HYDROGELS SWELLING AND DRUG RELEASE

10.46793/iccbi21.125m ◽

2021 ◽

Author(s):

Maja Markovic ◽

◽

Vesna Panic ◽

Julijana Tadic ◽

Rada Pjanovic

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Targeted Drug Delivery ◽

Targeted Delivery ◽

Water Soluble ◽

Soluble Model ◽

Hybrid Hydrogels ◽

Poorly Water Soluble ◽

Targeted Drug ◽

Model Drug

Targeted drug delivery is powerful tool which researchers use to achieve safer and more efficient therapy of many diseases, including various types of cancer. Many chemotherapeutics are poorly water- soluble, so their encapsulation and targeted delivery remain quite challenge. Hydrogels based on poly(methacrylic acid) (PMAA) are widely investigated for targeted drug delivery due to their pH sensitivity, non-toxicity and biocompatibility. Still, due to the PMAA highly hydrophilic nature, PMAA can only be used for encapsulation and targeted delivery of water-soluble drugs. Our previous research was directed towards overcoming this limitation: PMAA was modified with amphiphilic protein – casein and poorly-water soluble model drug – caffeine – was encapsulated (PMAC). Present study is focused on investigation how variation of amount of one of the most important hydrogels network parameter such as crosslinker affect PMAC swelling properties and caffeine release. The group of hybrid hydrogels – PMAC – was synthesized with various amount of crosslinker: 0.4mol%, 0.8mol%, 1.6mol% and 3.2mol% with respect to methacrylic acid. Swelling behavior of hybrid hydrogels and caffeine release was investigated in two environments which simulated human stomach and intestines. Obtained results showed that targeted delivery of poorly water-soluble model drug was achieved and that its release can be prolonged up to 24h. Also, kinetic of poorly water-soluble drug release can be easily modified only by changing crosslinker amount. PMAC hybrid hydrogels have huge potential for targeted delivery of poorly water-soluble active substances.

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Formation and controlled release of the inclusion complex of water soluble model drug neutral red with β -cyclodextrin grafted sodium alginate

Journal of Controlled Release ◽

10.1016/j.jconrel.2011.08.161 ◽

2011 ◽

Vol 152 ◽

pp. e116-e118 ◽

Cited By ~ 2

Author(s):

Shiping Zhang ◽

Xuemei Qiao ◽

Bihuang Hu ◽

Yongkuan Gong

Keyword(s):

Controlled Release ◽

Inclusion Complex ◽

Sodium Alginate ◽

Neutral Red ◽

Water Soluble ◽

Soluble Model ◽

Model Drug

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Investigation of Nanoscale Structure of Self-Emulsifying Drug Delivery System Containing Poorly Water-Soluble Model Drug

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.970.272 ◽

2014 ◽

Vol 970 ◽

pp. 272-278 ◽

Cited By ~ 3

Author(s):

Mont Kumpugdee-Vollrath ◽

Yotsanan Weerapol ◽

Karin Schrader ◽

Pornsak Sriamornsak

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Correlation Spectroscopy ◽

Water Soluble ◽

Wide Range ◽

Poorly Water Soluble ◽

Nanoscale Structure ◽

Model Drug ◽

20 Nm

This work has a focus on the self-emulsifying drug delivery system (SEDDS), which can be used in pharmaceutical field for increasing bioavailability of poorly water-soluble drugs. The model drug resveratrol was used because of its poor water-solubility and is of interest because of its wide range of pharmacological effects. It is beneficial to understand the mechanism of SEDDS formation in the human body, therefore, the determination of nanoscale structure was carried out. For this purpose, small angle X-ray scattering (SAXS), photon correlation spectroscopy (PCS), and transmission electron microscopy (TEM) techniques were applied. We have found that the size and size distribution of particles were in nanometers. The inner structure of SEDDS was ordered with the lamellar distances (d-spacing) of < 20 nm. It seems that the prepared SEDDS in water form large oil drops (200-400 nm) in water as well as small micelles with the droplet size of 10-20 nm.

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Novel application of mixed solvency concept in the development of oral liquisolid system of a poorly soluble drug, cefixime and its evaluation

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i6-s.2167 ◽

2018 ◽

Vol 8 (6-s) ◽

pp. 5-8 ◽

Cited By ~ 1

Author(s):

Rinshi Agrawal ◽

RK Maheshwari

Keyword(s):

Drug Loading ◽

Research Work ◽

Water Soluble ◽

Dsc Studies ◽

Water Soluble Drug ◽

Poorly Soluble ◽

Poorly Water Soluble ◽

Poorly Soluble Drug ◽

Model Drug ◽

Poorly Water Soluble Drug

Application of mixed solvency has been employed in the present research work to develop a liquisolid system (Powder formulation) of poorly water soluble drug, cefixime (as model drug). Material and Methods: For poorly water soluble drug cefixime, combination of solubilizers such as sodium acetate, sodium caprylate and propylene glycol as mixed solvent systems were used to decrease the overall concentration of solubilizers required to produce substantial increase in solubility and thereby resulting in enhanced drug loading capacity of cefixime. The procured sample of cefixime was characterized by melting point, IR, UV and DSC studies. Stability studies of liquisolid system of cefixime were performed for two months at room temperature, 30˚C and 40˚C. All the formulations were physically, chemically, and microbiologically stable. Conclusion: Mixed solvency concept has been successfully employed for enhancing the drug loading of poorly water soluble drug, cefixime. Keywords: Solubility, cefixime, liquisolid system, mixed solvency concept.

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