Physical and Chemical Compatibility of Etomidate and Propofol Injectable Emulsions

Pharmacology ◽  
2021 ◽  
pp. 1-14
Author(s):  
Chunling Wang ◽  
Shengnan Wang ◽  
Cuishuan Wu ◽  
Li Lei ◽  
Dong-Xin Wang ◽  
...  
Keyword(s):  
Particle Size ◽  
Dosage Form ◽  
Room Temperature ◽  
Fat Embolism ◽  
Compatibility Study ◽  
Chemical Compatibility ◽  
Unstable System ◽  
Critical Quality Attributes ◽  
Physical And Chemical

<b><i>Introduction:</i></b> The mixture of etomidate and propofol is widely used in clinical practice to improve efficacy of general anesthesia and to minimize side effects. As a thermodynamically unstable system, emulsion is prone to destabilization through mechanisms including coalescence, flocculation, and creaming. Such unwanted phenomenon can induce fat embolism after intravenous administration. This study was aimed to investigate the physical and chemical stability of the mixture of etomidate and propofol in the dosage form of emulsion. <b><i>Methods:</i></b> This compatibility study focused on the critical quality attributes (CQAs) of drug-containing emulsions, such as appearance, pH, particle size and distribution, <i>zeta</i> potential, the observation under centrifugation, and drug content and impurity. <b><i>Results:</i></b> As the results, there were no significant changes in the CQAs of the mixed emulsions up to 24 h after mixing at refrigeration temperature (4°C), room temperature (25°C), and body temperature (37°C). <b><i>Conclusions:</i></b> These results demonstrate that etomidate emulsion is physically and chemically compatible with propofol emulsions up to 24 h at 4°C, 25°C, and 37°C, suggesting that etomidate and propofol can be administrated in mixture without adversely affecting product characteristics, at least in vitro.

Preparation, Characterization, and In Vitro Evaluation of EGCG-Loaded Chitosan Nanoparticles

2011 ◽  
Vol 282-283 ◽  
pp. 539-544 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Zhi Gang An ◽  
Xiao Yu Sui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery Systems ◽  
Room Temperature ◽  
Active Component ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Release Drug

Epigallocatechin-3-gallate (EGCG), a principal polyphenolic, which is most abundant and active component in tea. It is considered key to these healthful qualities. However, EGCG used in clinical application which is still shortcomings of short half-life and low bioavailability. Chitosan (CS) has been widely used in pharmaceutical and medical areas, particularly for its potential in the development of controlled release drug delivery systems due to its well properties. In this study, we prepared EGCG-loaded chitosan nanoparticles by ionic polymeric method using sodium tripolyphosphate(TPP) as ionic polymeric agent successfully. Results controlled conditions (concentration of CS, 2 mg/mL; pH = 5.4; volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min))volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min)) for entrapment efficiency, loading efficiency, mean particle size and Zeta potential, were found to be 62.3 %, 33.8 %, 141.5 ± 0.4 nm and -31.21 ± 0.54 mV, respectively, and CS-EGCG-NPS have well property of sustained release.

scholarly journals Formulation and Characterization of Felodipine as an Oral Nanoemulsions

2021 ◽  
Vol 30 (1) ◽  
pp. 209-217
Author(s):  
Sumaya B. Hamed ◽  
Shaimaa N. Abd Alhammid
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Water Solubility ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Compatibility Study ◽  
Drug Content ◽  
Drug Molecules

            Felodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Results of characterization showed that felodipine nanoemulsion (F3) with (oleic acid 10%) ,(Smix 60% of tween80 :ethanol in a ratio of 3:1), (DDW 30%) was selected as the best formula, since it has a particle size of (17.01)nm, low PDI (0.392), zeta potential (-22.34mV), good dilution without drug precipitation , higher percent of drug content (99.098%) with  acceptable viscosity , and complete release of the drug after (45 min.) with significantly higher (P<0.05)   dissolution  rate in comparison with the pure drug powder. The selected formula (F3) subjected to further investigations as drug and excipient compatibility study by Fourier transform infrared spectroscopy (FTIR) The outcomes of the (FTIR) explain that the distinctive peaks for felodipine were not affected by other components and displayed the same functional group's band with very slight shifting. This indicates that there was no interaction between felodipine and other NE components. Therefore, these excipients were found to be compatible with felodipine. In conclusion, the NE was found to be an efficient method to enhance the dispersibility and permeatioins of drugs that have poor water solubility (lipophilic drugs).

scholarly journals Encapsulation of metronidazole in polycaprolactone microspheres

2019 ◽  
Vol 9 (1) ◽  
pp. 190-194
Author(s):  
Rima Kassab ◽  
Dima Moussa ◽  
Cherine Saliba ◽  
Paolo Yammine
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Compatibility Study ◽  
Drug Encapsulation ◽  
Evaporation Technique ◽  
Ft Ir ◽  
Ir Study

Non-aqueous oil-in-oil solvent evaporation technique is used for the preparation of polycaprolactone microspheres loaded with the antibiotic metronidazole by introducing different masses for the drug. The prepared microspheres are characterized by calculating drug encapsulation and drug loading percentages, measuring the corresponding particle size, performing FT-IR polymer-drug compatibility study and in vitro drug release. Moderate drug encapsulation values with a maximum of 34% are observed due to the low molecular weight of the drug. Microspheres had a particle size ranging between 130 and 280 µm with a spherical profile and porous structure. FT-IR study showed no interactions between the drug and the polymer. Drug release studies showed fast release rates for all the formulations with the slowest release for the highest drug loading. Keywords: polycaprolactone, metronidazole, targeted drug delivery, solvent evaporation.

scholarly journals Antifibrotic Activity and In Ovo Toxicity Study of Liver-Targeted Curcumin-Gold Nanoparticle

2018 ◽  
Vol 86 (4) ◽  
pp. 41 ◽  
Author(s):  
Amirah Adlia ◽  
Ilham Tomagola ◽  
Sophi Damayanti ◽  
Ardyanto Mulya ◽  
Heni Rachmawati
Keyword(s):  
Antioxidant Activity ◽  
Particle Size ◽  
3T3 Cells ◽  
In Ovo ◽  
Particle Size Analyzer ◽  
Size And Morphology ◽  
Nih 3T3 ◽  
Physical And Chemical ◽  
Nih 3T3 Cells

Conjugation of curcumin and gold with green chemistry is an approach to improve the effectiveness of curcumin as anti-fibrosis. In this work, curcumin and gold were conjugated to deliver curcumin to the liver. Curcumin-gold nanoparticles (cAuNPs) were prepared by varying curcumin pH and concentration. The successful of cAuNPs formation were identified by using UV-visible and FTIR spectrophotometers. The particle size and morphology were analyzed using particle size analyzer and cryo-TEM respectively. In vitro antioxidant assay was performed to determine the curcumin activity after conjugation. Physical and chemical stabilities of cAuNPs were studied for one month at 5 °C, 25 °C, and 40 °C. Furthermore, the cAuNPs activity to modulate early marker of fibrosis was tested on NIH/3T3 cells. The optimum condition for cAuNPs synthesis was by using 1.5 mM curcumin at pH 9.3. As compared to free curcumin, cAuNPs showed higher antioxidant activity and maintained the nanosize after stored for one month. In line with the antioxidant activity, cAuNPs 0.25–1 μg/mL reduced the collagen production by NIH/3T3 cells. More importantly, cAuNPs did not demonstrate any effect on the development of chicken embryo. Taken together, the attachment of gold to curcumin in the form of cAuNPs is promising for curcumin targeting to treat hepatic fibrosis.

Stability of Mycophenolate Mofetil as an Extemporaneous Suspension

1998 ◽  
Vol 32 (7-8) ◽  
pp. 755-757 ◽  
Author(s):  
Raman Venkataramanan ◽  
Jacqueline R McCombs ◽  
Sheila Zuckerman ◽  
Bill McGhee ◽  
Jaya Pisupati ◽  
...  
Keyword(s):  
Mycophenolate Mofetil ◽  
Chemical Stability ◽  
Mycophenolic Acid ◽  
Postoperative Period ◽  
Dosage Form ◽  
Room Temperature ◽  
Pediatric Patients ◽  
Early Postoperative Period ◽  
Time Points ◽  
Physical And Chemical

OBJECTIVE: To evaluate the physical and chemical stability of a suspension of mycophenolate mofetil (MMF) prepared in the hospital from commercially available MMF capsules. METHODS: Suspensions of MMF were prepared at room temperature and stored at 5, 25, 37, and 45 °C over a period of 50 to 210 days. The contents of MMF and its degradation product, mycophenolic acid, in the suspension were measured at various time points by HPLC. RESULTS: MMF suspensions were stable (as determined by the presence of ≥90% of the labeled amount) at 45 °C for at least 11 days, at 37 °C for at least 28 days, at 25 °C for at least 28 days, and at 5 °C for at least 210 days. The suspension was also physically stable at 5 °C during the entire test period. CONCLUSIONS: The compounded MMF suspension was stable for at least 11 days at all the temperatures studied and for as long as 210 days at 5 °C. This formulation appears to be clinically acceptable and provides a convenient dosage form for pediatric patients and for adults during the early postoperative period.

Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies

2020 ◽  
Vol 8 (6) ◽  
pp. 452-470
Author(s):  
Brito R. Selvaraj ◽  
Seshaiah K. Sridhar ◽  
Bhaskar R. Kesavan ◽  
Sucharitha Palagati
Keyword(s):  
Particle Size ◽  
Plasma Concentration ◽  
Dosage Form ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Entrapment Efficiency ◽  
Transdermal Patch ◽  
In Vitro Drug Release

Background: The hypothesis is to augment the bioavailability and therapeutic potential of low bioavailable Carvedilol (25-35%) through Nanostructured Lipid Carrier (NLC) loaded Transdermal patch (Nanolipid Transferosomes). Methods: Box-Behnken design was designed to formulate NLC through a hot homogenization technique. About 17 formulations (C1-C17) were formulated by varying the critical material attribute and critical process parameter. Optimization was done based on its critical quality attributes like particle size, zeta potential and entrapment efficiency. Selected NLC (C16) has been fabricated into a transdermal patch through solvent evaporation technique and estimated for thickness, weight variation, moisture content, folding endurance, drug content, in vitro drug release, ex vivo skin permeation studies 48 hrs, in vitro drug release kinetic studies and skin irritation studies. In vivo pharmacokinetics and pharmacodynamic study parameters were compared between carvedilol loaded NLC transdermal patch and a conventional formulation (Coreg CR). Results: NLC (C16) was selected as the best formulation based on desirable, less particle size (201.1 ± 2.02 nm), more zeta potential (-37.2 ± 1.84mV) and maximum entrapment efficiency (87.54 ± 1.84%). Experimental investigations of in vivo dermatopharmacokinetic data shown statistically significant changes (p<0.05) in the parameter (increased AUC0-α, MRT with decreased Cmax, Tmax) when administered through the transdermal patch and on compared to the conventional dosage form. It was observed that there was a significant change with p<0.05 among the pharmacokinetic factors of conventional Carvedilol formulation, Carvedilol NLC and Carvedilol NLC loaded Transdermal patch with a maximum time of peak plasma concentration (Tmax) of 4 hrs, 8 hrs and 8 hrs; maximum peak plasma concentration (Cmax) of 0.258 μg/ml, 0.208 μg/ml and 0.108 μg/ml. Area Under Curve (AUC0-α) was established to be 125.127 μg/ml/h, 132.576 μg/ml.h and 841.032 μg/ml.h. Mean Residence Time (MRT0- α) of the drug was established to be 17 hrs, 19 hrs and 82 hrs, respectively. This data reveals the impact of NLC on the enhancement of bioavailability through a transdermal patch. In vivo pharmacodynamic studies confirm that NLC loaded transdermal patch (Nanolipid Transferosomes) shows a significant control in blood pressure for 48 hrs when compared to the conventional dosage form. Conclusion: This research data concludes that NLC loaded transdermal patch (Nanolipid Transferosomes) was a suitable candidate to enhance the bioavailability of low bioavailable drug-like Carvedilol. Lay Summary: It was inferred from the literature that NLC filled transdermal patches were a novel strategy to increase the solubility and permeability of Carvedilol, which has less bioavailability. It reveals that there was no reproducible preparation for the NLC. It also reveals that the option of formulation and process parameters for the formation of NLC is not clearly justified. On account of this, an uniquely validated and optimized formulation technique was developed for NLC with low soluble and poorly bioavailable carvedilol, tested in Albino wistar rats for enhancement of bioavailability, the same study has been performed and proved.

scholarly journals FORMULATION OF ANDROGRAPHOLIDE TRANSFERSOMES GEL FOR TRANSDERMAL DELIVERY: A PRELIMINARY STUDY

2020 ◽  
pp. 187-191
Author(s):  
SILVIA SURINI ◽  
PUTERI D NASTITI ◽  
ADELIA R PUTRI ◽  
KURNIA SS PUTRI
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery System ◽  
Transdermal Delivery ◽  
Dosage Form ◽  
Entrapment Efficiency ◽  
Preliminary Study ◽  
Span 80 ◽  
Two Phases

Objective: A transfersome is a drug delivery system that offers increased penetration for the transdermal delivery of drugs. The aim of this study wasto assess the application of transfersomes for transdermal delivery of andrographolide.Methods: The development of andrographolide transfersomes for transdermal delivery was conducted in two steps. The first step involved varyingratios of Span 80 and phospholipids to investigate the effect on transfersome deformability using four formulations (P1–P4). Afterward, a second stepinvolved varying ratios of andrographolide in transfersomes to investigate the influence on entrapment efficiency using four formulations (F1–F4).The selected transfersomes were then formulated into a gel dosage form. An in vitro penetration study was conducted by comparing the penetrationfluxes of the transfersome and non-transfersome andrographolide gels using Franz diffusion cells.Results: The results showed that formulation F4 had an entrapment efficiency of 97.02±0.01% and particle size (DV-average) of 524.02 nm. An in vitropenetration study of the andrographolide transfersome gels showed two phases of penetration, with a marked increase in both fluxes. In the firstphase, penetration flux was 23.26±2.34 and 1.28±0.82 μg/cm2·h for the transfersome and non-transfersome andrographolide gels, respectively.Conclusion: The results showed that the transfersome gel is a promising dosage system for transdermal delivery of andrographolide.

scholarly journals PREPARATION, EVALUATION AND STABILITY OF LAMIVUDINE LOADED ALGINATE-TAMARIND MUCILAGE MICROSPHERES

2019 ◽  
pp. 365-370
Author(s):  
Santosh Gada ◽  
ANANDKUMAR Y. ◽  
C. MALLIKARJUNA SETTY
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Room Temperature ◽  
Drug Loading ◽  
In Vitro Release ◽  
Stability Studies ◽  
Effective Level ◽  
Vitro Release ◽  
Drug Encapsulation Efficiency

Objective: The objective of the present study was to investigate the possibility of obtaining a controlled, relatively constant effective level of lamivudine microspheres. Methods: Lamivudine loaded sodium alginate (SA) and tamarind mucilage(TM) mucoadhesive microspheres were prepared by ionic gelation technique with three different proportions of SA and TM with different concentrations of CaCl2. The prepared microspheres were evaluated for drug loading, particle size distribution, surface morphology, FTIR, in vitro wash off, in vitro release and stability studies. Results: The microspheres were found to be free flowing having diameter ranging from 769.22 to 978.56 µm, drug encapsulation efficiency (DEE) was found to be 65.28 to 92.33%. Percent drug release after 12 h were ranging from 85±1.51 to 97±1.44. In vitro release profile of all formulations shows slow controlled release up to 12 h. In vitro wash off studies shown fairly good mucoadhesivity with 20% microspheres adhered after 6h. Stability studies showed that no significant change in particle size and maximum DEE in comparison to the formulation stored at room temperature. Results: The lamivudine loaded SA-TM mucoadhesive microspheres can be conveniently prepared which showed better result and it may be used full for controlling the drug release and improve the bioavailability.

scholarly journals A Biopredictive In Vitro Approach for Assessing Compatibility of a Novel Pediatric Hydrocortisone Drug Product within Common Pediatric Dosing Vehicles

2020 ◽  
Vol 37 (10) ◽  
Author(s):  
Erik Wollmer ◽  
Frank Karkossa ◽  
Lisa Freerks ◽  
Anna-Elena Hetberg ◽  
Greg Neal ◽  
...  
Keyword(s):  
Degradation Products ◽  
Drug Product ◽  
Compatibility Study ◽  
Drug Solubility ◽  
Chemical Compatibility ◽  
Drug Degradation ◽  
Age Related ◽  
Granule Formulation

Abstract Purpose The objective of the present work was to screen whether a novel pediatric hydrocortisone granule formulation can be co-administered with common food matrices and liquids. Methods Pediatric hydrocortisone granules were studied using a biopredictive in vitro approach. Experiments included an in situ chemical compatibility study of active ingredient and drug product with liquid dosing vehicles and soft foods commonly ingested by infants, pre-school- and school children. Drug solubility and stability experiments in the different vehicle types and, drug release/dissolution experiments mimicking age-related pediatric gastric conditions after administering the hydrocortisone granules together with the dosing vehicles and after different exposure/mixing times were performed. Results In the simulated dosing scenarios applied in dissolution experiments, in vitro dissolution in gastric conditions was rapid and complete. Results of the chemical compatibility/stability studies indicated that mixing with the different dosing vehicles studied should not be an issue regarding drug degradation products. Conclusions A novel in vitro approach ensuring a proper risk assessment of the use of dosing vehicles in the administration of pediatric dosage forms was established and applied to a novel pediatric hydrocortisone drug product. The studied dosing vehicles were shown to not alter performance of the drug product and are thus considered suitable for administration with hydrocortisone granules.

scholarly journals Aerosol Characteristics and Physico-Chemical Compatibility of Combivent® (Containing Salbutamol and Ipratropium Bromide) Mixed with Three Other Inhalants: Budesonide, Beclomethasone or N-Acetylcysteine

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 78 ◽  
Author(s):  
Rui Zhang ◽  
Junhua Hu ◽  
Liangjun Deng ◽  
Sha Li ◽  
Xi Chen ◽  
...  
Keyword(s):  
Particle Size ◽  
Ipratropium Bromide ◽  
Fine Particles ◽  
Chronic Respiratory Disease ◽  
Delivery Rate ◽  
Inhalation Therapy ◽  
Chemical Compatibility ◽  
Physico Chemical ◽  
Pressure Chemical

Inhalation therapy with a nebulizer is widely used in chronic respiratory disease. Mixing inhalation solutions/suspensions for simultaneous inhalation is more convenient and might simplify the administration procedure. However, there are no data available to address the in vitro aerosol characteristics and physico-chemical compatibility of Combivent® (containing Salbutamol and Ipratropium bromide) with other inhalation solutions/suspensions. In order to investigate the in vitro aerosol characteristics and physico-chemical compatibility of Combivent® with Budesonide, Beclomethasone, and N-acetylcysteine, the appearance, pH, osmotic pressure, chemical stability, mass median aerodynamic diameter (MMAD), fine particles fraction (FPF), particle size corresponding to X50 (particle size, which accounts for 50% of the total cumulative percentage of volume of all particles), delivery rate, and total delivery of the mixed inhalation solution/suspension were tested. There was no change in the appearance such as a change in color or precipitation formation at room temperature. The pH, osmolality, and chemicals of the mixtures were stable for 24 h after mixing. There were no significant differences between Combivent®, Budesonide, Beclomethasone, N-acetylcysteine, and the mixtures in MMAD, FPF, X50, the delivery rate, and the total delivery. This indicates that the mixtures were physically and chemically compatible. The mixing did not influence the particle size, distribution, or delivery compatibility of the mixtures.

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