scholarly journals Stability Study of Isoniazid and Rifampicin Oral Solutions Using Hydroxypropyl-Β-Cyclodextrin to Treat Tuberculosis in Paediatrics

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 195
Author(s):  
Ana Santoveña-Estévez ◽  
Javier Suárez-González ◽  
Amor R. Cáceres-Pérez ◽  
Zuleima Ruiz-Noda ◽  
Sara Machado-Rodríguez ◽  
...  

(1) Background: First-line antituberculosis treatment in paediatrics entails the administration of Isoniazid, Pyrazinamide, and Rifampicin. This study examines the possibility of developing a combined dose liquid formulation for oral use that would facilitate dose adjustment and adherence to treatment for younger children. (2) Methods: The active pharmaceutical ingredients stability under in vitro paediatric digestive pH conditions have been checked. The samples were studied as individual or fixed combined paediatric dosages to determine the pH of maximum stability. The use of hydroxypropyl-β-cyclodextrin to improve Rifampicin solubility and the use of ascorbic acid to increase the stability of the formulation have been studied. (3) Results: Maximum stability of combined doses was determined at pH 7.4, and maximum complexation at pH 8.0. Taking this into account, formulations presented the minimum dose of two active pharmaceutical ingredients dissolved. The addition of ascorbic acid at 0.1% w/v enables the detection of a higher remaining quantity of both drugs after three days of storage at 5 °C. (4) Conclusions: a formulation which combines the minimum paediatric dosages dissolved recommended by WHO for Isoniazid and Rifampicin has been developed. Future assays are needed to prolong the stability of the formulation with the aim of incorporating Pyrazinamide to the solution.

2021 ◽  
Vol 9 (9) ◽  
pp. 1869
Author(s):  
Joanna Kaczorowska ◽  
Eoghan Casey ◽  
Gabriele A. Lugli ◽  
Marco Ventura ◽  
David J. Clarke ◽  
...  

Enterotoxigenic Escherichia coli (ETEC) and Shigella ssp. infections are associated with high rates of mortality, especially in infants in developing countries. Due to increasing levels of global antibiotic resistance exhibited by many pathogenic organisms, alternative strategies to combat such infections are urgently required. In this study, we evaluated the stability of five coliphages (four Myoviridae and one Siphoviridae phage) over a range of pH conditions and in simulated gastric conditions. The Myoviridae phages were stable across the range of pH 2 to 7, while the Siphoviridae phage, JK16, exhibited higher sensitivity to low pH. A composite mixture of these five phages was tested in vivo in a Galleria mellonella model. The obtained data clearly shows potential in treating E. coli infections prophylactically.


2020 ◽  
Vol 10 (7) ◽  
pp. 2265
Author(s):  
Maria Râpă ◽  
Laura Mihaela Stefan ◽  
Traian Zaharescu ◽  
Ana-Maria Seciu ◽  
Anca Andreea Țurcanu ◽  
...  

Bionanocomposites including poly(lactic acid) (PLA), collagen, and silver nanoparticles (AgNPs) were prepared as biocompatible and stable films. Thermal properties of the PLA-based bionanocomposites indicated an increase in the crystallinity of PLA plasticized due to a small quantity of AgNPs. The results on the stability study indicate the promising contribution of the AgNPs on the durability of PLA-based bionanocomposites. In vitro biocompatibility conducted on the mouse fibroblast cell line NCTC, clone 929, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay showed high values of cell viability (>80%) after cell cultivation in the presence of bionanocomposite formulations for 48 h, while the percentages of lactate dehydrogenase (LDH) released in the culture medium were reduced (<15%), indicating no damages of the cell membranes. In addition, cell cycle analysis assessed by flow cytometry indicated that all tested bionanocomposites did not affect cell proliferation and maintained the normal growth rate of cells. The obtained results recommend the potential use of PLA-based bionanocomposites for biomedical coatings.


Drug Research ◽  
2020 ◽  
Vol 70 (08) ◽  
pp. 367
Author(s):  
Jaideo Pandey ◽  
Ravi Shankar ◽  
Manish Kumar ◽  
Kuldeep Shukla ◽  
Beena Kumari

Abstract Background Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. Objectives In this research mucoadhesive microspheres were developed in order to carry out the absorption of drug through nasal mucosa with the aim to improve therapeutic efficacy, avoid hepatic first pass metabolism and increase residence time. Material and Methods Mucoadhesive microspheres of Granisetron using chitosan as polymer were prepared by emulsification cross-linking method to increase the residence time on the mucosa. The surface of prepared microspheres was characterized by SEM (Scanning electron microscopy) and evaluated for particle size, encapsulation efficiency, production yield, swelling ability, in-vitro mucoadhesion, in-vitro drug release and stability study. Result Among all the formulations F6 with drug/polymer ratio of 1:3 displayed the best result. On drug release kinetic model study, all the formulations follow Zero order. Stability studies revealed that the microspheres kept at 25±2°C and 60±5% RH showed the maximum stability. Conclusion After all the evaluation parameters and result obtained it can be said that these results confirmed the suitability of Granisetron mucoadhesive chitosan microspheres for nasal delivery system.


1950 ◽  
Vol 28e (1) ◽  
pp. 19-32 ◽  
Author(s):  
James Campbell ◽  
W. G. Tubb

The stability of ascorbic acid in aqueous solution was increased under certain conditions by oxalic acid, metaphosphoric acid, glutathione, thiourea, and sodium diethyldithiocarbamate. A slight protective effect was exerted by creatinine; but formic, phthalic, and orthophosphoric acids, creatine, and caffeine had no demonstrable effect. In all these instances the pH, concentrations of reagents, etc., must be considered. In oxalate and thiourea maximum stability occurred at pH 2.5 to 3.0 and in glutathione at pH 3.6 to 4.2. The latter substance itself was also most stable at pH 3 to 4. At the optimum pH a concentration of 40 mM of oxalate gave maximal protection, this being independent of the initial concentration of ascorbic acid over the range 2 to 20 mM. Thus a stoichiometric relationship between the concentrations of the ascorbic acid and the oxalate required for protection was not found. A region of minimum solubility of oxalate in water occurred at pH 2.4 to 3.0, which coincides with the pH at which the maximum protective effect occurs and with the highest relative concentration of sodium hydrogen oxalate (or sodium hydrogen oxalate monohydrate). The absorption of ultraviolet light by ascorbic acid was altered by pH, the maximum shifting from 244 to 268 mμ from pH 2.8 to 4.5. The molecular extinction coefficient of ascorbic acid also changed with pH and was minimal at pH 4.0. This effect occurred in oxalate, which has a specific protective effect, and also in formate and orthophosphate, which have no specific protective effect. The possible mechanisms for the protection of ascorbic acid by oxalate are discussed.


2018 ◽  
pp. 13-18
Author(s):  
M.M. Kuzhko ◽  
T.M. Tlustova ◽  
O.S. Denysov ◽  
T.A. Sprynsian ◽  
Yu.V. Shukha

PURPOSE. To evaluate the stability of mixtures of anti-tuberculosis drugs for intravenous administration used for treatment of sensitive and resistant tuberculosis in time and in conditions close to the conditions of the use. MATERIALS AND METHODS. Studied combinations: ethambutol + isoniazid in various concentrations, ethambutol + levofloxacin, ethambutol + moxifloxacin. In the stability study, samples were taken for analysis of the appearance, pH and concentration of drugs at specified times (immediately after mixing, after 16, and 24 hours). RESULTS. The results of the chromatographic study indicate the absence of chemical interaction between the active pharmaceutical ingredients, high physical and chemical stability of the mixtures for up to 24 hours of storage under conditions close to the conditions of use, except the mixture of isoniazid with ethambutol, in which it is recommended to reduce the storage term to 16 hours due to the complexity of interpretation and the nature of potential impurities. CONCLUSIONS. Study results indicate the possibility of simultaneous administration of a mixture of isoniazid and ethambutol when the preparation of the mixture was not more than 16 hours prior to administration and mixtures of ethambutol + levofloxacin and ethambutol + moxifloxacin with the preparation of the mixture no more than 24 hours before administration.


Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.


Author(s):  
Cloé L. Esposito ◽  
Plamen Kirilov

With the increase in occupation-specific risks of lip cancer associated with solar radiation, there is a need for developing photoprotective lipsticks to protect skin against harmful effects of UV radiation. Considering the unique chemical and physical properties of low-molecular-weight organogelators (LMOGs), the present study intended to assess the UV protective properties of LMOGs-based lipstick formulations. In this study, dibenzylidene-D-sorbitol (DBS) and 12-hydroxystearic acid (12-HSA) were used to formulate lipsticks : L1 (1% DBS), L2 (10% 12-HSA), L3 (1.5% DBS) and L4 (control, no LMOGs). The lipstick formulations were tested for in vitro sun protection factors (SPF), UVA protection factor (UVA-PF), thermal, mechanical and texture analyses. Lipsticks with LMOGs exhibited higher UVA-PF and SPF, and more particularly 12-HSA-based lipstick. Results showed also the viscoelastic and heat-resistant properties of LMOGs and their effect of increasing pay-off values. In general, texture analysis indicating that 12-HSA-based lipstick was significantly harder to bend compared to control, while other formulations became softer and easier to bend throughout the stability study. Finally, sensorial and instrumental analyses permitted to classify lipsticks into two groups. This work suggests the potential use of LMOGs as a structuring agent for lipsticks paving the way towards more photoprotective and sustainable-derived alternatives.


CrystEngComm ◽  
2022 ◽  
Author(s):  
Liyu Liu ◽  
Jian-Rong Wang ◽  
Xuefeng Mei

Cocrystallization has been recognized as one of the most successful approaches to address stability problems of active pharmaceutical ingredients (APIs) in the past few decades. However, scant attention has been...


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