Quantification of in situ granulation-induced changes in pre-compression, solubility, dose distribution and intrinsic in vitro release characteristics of ibuprofen–cationic dextran conjugate crystanules

2014 ◽  
Vol 471 (1-2) ◽  
pp. 453-477 ◽  
Author(s):  
Amos Olusegun Abioye ◽  
Adeola Kola-Mustapha ◽  
George Tangyie Chi ◽  
Sunday Ilya
INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (07) ◽  
pp. 33-35
Author(s):  
A Dubey ◽  
◽  
P Prabhu ◽  
N Nair ◽  
K Beladiya ◽  
...  

The aim of the present investigation was to develop a combination of timolol maleate and travoprost niosomal in situ gelling system for the treatment of glaucoma. Niosomes were prepared by thin film hydration technique using rotary flash evaporator. A 32 factorial design was utilized to study the effect of the molar ratio of Span 60 (X1) and cholesterol (X2) on vesicle size, drug entrapment efficiency and in vitro release study. On the basis of vesicle size, maximum entrapment efficiency and in vitro release of drug, best formulations were selected for the preparation of niosomal in situ gel (Drop). On the basis of gelling time and viscosity, optimized ratio of the polymers was selected for the desired preparation. Selected niosomal batches were dispersed in carbopol 940 and HPMC K4M polymer solution (combination IF6) to form in situ gel niosomal formulations (Drop). The gelling time of the niosomal in situ gel (NIF1) was found to be the best (+++) and the viscosity was found to be 1190 cP. Zeta potential, average size analysis, polydispersibility index value was found to be -45.1 mV, 256.5 nm, 0.228 respectively. In vitro drug release was found to be within the range of 50.23 ± 0.54 to 60.23 ± 0.33% over the period of 6 h. IOP lowering activity of best formulation (NIF1) showed more significant and sustained effect than the marketed eye drops. Best formulation (NIF1) was found to be stable, sterile, non irritant and isotonic. Hence niosomal in situ gelling combination system may have the potential of bringing better application than the conventional ocular therapy with improved ocular bioavailability and increased patient compliance.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Elham Khodaverdi ◽  
Fatemeh Kheirandish ◽  
Farnaz Sadat Mirzazadeh Tekie ◽  
Bibi Zahra Khashyarmanesh ◽  
Farzin Hadizadeh ◽  
...  

In situ forming delivery systems composed of block copolymers are attracting substantial attention due to their ease of use, biocompatibility, and biodegradability. In this study, the thermoresponsive triblock copolymer PLGA-PEG-PLGA was studied as a dexamethasone delivery system. Dexamethasone, a synthetic glucocorticoid, is used clinically to improve inflammation, pain, and the hyperemesis of chemotherapy, and it is applied experimentally as a differentiation factor in tissue engineering. PLGA-PEG-PLGA was synthesised under microwave irradiation for 5 min. The obtained copolymer was characterised to determine its structure and phase transition temperature. An in vitro release study was conducted for various copolymer structures and drug concentrations. The yield of the reaction and HNMR analysis confirmed the appropriateness of the microwave-assisted method for PLGA-PEG-PLGA synthesis. Phase transition temperature was affected by the drug molecule as well as by the copolymer concentration and structure. An in vitro release study demonstrated that release occurs mainly by diffusion and does not depend on the copolymer structure or dexamethasone concentration.


2014 ◽  
Vol 15 (3) ◽  
pp. 772-780 ◽  
Author(s):  
Tarek A. Ahmed ◽  
Hany M. Ibrahim ◽  
Ahmed M. Samy ◽  
Alaa Kaseem ◽  
Mohammad T. H. Nutan ◽  
...  

2009 ◽  
Vol 10 (1) ◽  
pp. 104-112 ◽  
Author(s):  
Ferhan Sevgi ◽  
Aysu Yurdasiper ◽  
Buket Kaynarsoy ◽  
Ezgi Turunç ◽  
Tamer Güneri ◽  
...  

Author(s):  
ANKITA KAPOOR ◽  
G. D. GUPTA

Objective: The present research work aims at describing the formulation, optimization and evaluation of ion activated ocular in-situ gel of gatifloxacin for treatment of bacterial conjunctivitis so as to overcome patient inconvenience, precorneal drug elimination, variation in efficacy, vision blurring and frequent instillation associated with conventional eye drops and ointments. Methods: In-situ gel was prepared using gellan gum as an ion activated phase transition polymer and HPMC K100M as release retardant. Gatifloxacin was characterized by spectrophotometry. Crystalline state of the drug was determined using X Ray Diffraction study. The developed formulation exhibited instantaneous gel formation in simulated lacrimal fluid (pH 7.4), which was further evaluated for its rheology, irritancy parameters, in vitro release, trans-corneal permeation and antimicrobial activity. Results: Gatifloxacin exhibited λmax 286 nm obeying Beer Lambert’s law and pH-dependent solubility at a pH range of 2 to 4. 0.6% gellan gum and 0.4% HPMC K100M were optimized in the formulation which exhibited a viscosity of 55 cps in sol form and 325 cps in gel form with pseudoplastic behavior and prolonged in vitro release. Permeation of formulation was 75.8% in 7 h with log P of drug 0.59. Developed isotonic and non-irritant formulation had a lower apparent permeability coefficient of 8.15 x 10-5 cm/sec as compared to marketed formulation. Conclusion: A Formulation can be viewed as an efficacious medicine by virtue of its higher zone of inhibition, ability to enhance precorneal residence time and consequently ocular bioavailability with lesser frequency of administration attributed to slow and prolonged diffusion of the drug from the polymeric solutions.


2011 ◽  
Vol 236-238 ◽  
pp. 2491-2494
Author(s):  
Rui Sun ◽  
Si Hao Chen ◽  
Chen Chen Xing

Huperzine A loaded microspheres are prepared using a W/O solvent evaporation method. The fixed speed release system is that microspheres composed with thermosensitive methylcellulose based hydrogel. SEM is used to analysis the surface morphology of Huperzine A loaded microspheres, which is shown that the difference of the size of microspheres. The size less than 200µm can be used as injection. Gelation experiment shows that the methylcellulose based solution can be transformed into in-situ hydrogel in 15 minutes at body temperature. The result of in vitro release shows that Huperzine A released in a nearly fixed speed. All the meterials of experiment can be biodegrated completely without operating to remove the gel. This is a promising long-term injection system, which is security and controlable for clinic.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 216 ◽  
Author(s):  
Jie Yan ◽  
Zhi-Yu Guan ◽  
Wei-Feng Zhu ◽  
Ling-Yun Zhong ◽  
Zhuo-Qi Qiu ◽  
...  

In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.


2019 ◽  
Vol Volume 14 ◽  
pp. 7447-7460 ◽  
Author(s):  
Cui Meng ◽  
Weipeng Wei ◽  
Yuhe Wang ◽  
Kunqin Zhang ◽  
Ting Zhang ◽  
...  

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