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Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.


Author(s):  
MAZIN THAMIR ABDUL-HASAN ◽  
ABULFADHEL JABER NEAMAH Al-SHAIBANI ◽  
ALI N. WANNAS ◽  
KARRAR MOHAMMED HASAN AL-GBURI

Objective: This study was employed to evaluate the quality of marketed oral tablets containing clopidogrel bisulfate. Tablets produced by various companies and commercialized in the Iraq market were used in the study. Methods: Batches of clopidogrel bisulfate conventional tablets (containing 75 mg of drug) were exposed to the quality control tests. These tests involved friability, weight variation, hardness, drug content, disintegration time, and in vitro release study; these tests were conducted depending on USP pharmacopeia. Results: The data indicate that all batches of clopidogrel bisulfate complied with the limitations of USP pharmacopeia for variation of weight, results of the hardness of tablets were 7.2-9.6 Kg/cm2. Friability value (% loss) was less than one, which was within the required limits. The time of disintegration was less than 25 min in both artificial gastric fluid (AGF) and artificial intestinal fluid (AIF). Drug content was observed between 97.1 % and 99.8 %, indicating compliance with the limits of pharmacopeia (85-115 %). An in vitro release study of batches was greater than 80 % within 25 min. Conclusion: All batches of clopidogrel bisulfate were manufactured within the criteria of tablet manufacturing. The quality control tests of tablets showed acceptable pharmaceutical properties (effectiveness and safety) that lie within the limits of USP pharmacopeia.


Author(s):  
LANKALAPALLI SRINIVAS ◽  
SHANTI SAGAR

Objective: The current research was aimed to formulate and evaluate raft forming gastro retentive floating drug delivery systems of Lafutidine for improving gastric residence time and sustained drug release for an extended time. Methods: Using Box–Behnken experimental design 17 formulations of lafutidine GRDDS were designed and evaluated for various parameters like physical appearance, pH, In vitro gelling study, in vitro buoyancy study, measurement of viscosity, density measurement, gel strength, drug content, acid neutralization capacity, the profile of neutralization, in vitro dissolution, release kinetic and stability studies. Results: All the evaluations were performed and observed that the values were within range, and the buoyancy lag time ranged within 14.76 to 25.84 sec and the formulations remained buoyant for more than 8h with the gelling time of 12h, the drug content was ranging from 98.96 to 99.55 %, and in vitro release was 86.86 to 99.34% by the end of 12h. The release kinetics followed zero-order with Higuchi’s model that indicating that drug release was found to be followed by the matrix diffusion process. Conclusion: Out of all formulations F3 was the optimized formulation and it was further characterized for FTIR, DSC, and stability studies, which exposed that there were no interactions amongst drug and excipients and no major change in the formulation and found to be stable.


2022 ◽  
Author(s):  
Qing Yu ◽  
Richard M. England ◽  
Anders Gunnarsson ◽  
Robert Luxenhofer ◽  
Kevin Treacher ◽  
...  
Keyword(s):  

Author(s):  
REESHA PARVEZ BAIG ◽  
MOHAMMAD WAIS

Objective: The present research work of Amphotericin B Proniosomal gel focuses on improving patient compliance by reducing the side effects of conventional intravenous injections and minimizing the problem of physical stability and to localize drug at site of action. Methods: Proniosomal gels are prepared by coacervation phase separation technique using different concentration of non-ionic surfactants (Span and Tween) for uniform vesicle formation, lecithin as permeation enhancer/membrane stabilizer and cholesterol as a vesicle cement providing prolonged release. Prepared gels were evaluated for their viscosity, pH, spreadability, entrapment efficiency, drug content uniformity, extrudability, in vitro drug release, permeability and stability studies. Results: Among the nine formulations, F2 (containing 10 mg drug, 250 mg Span 60, 50 mg Soya lecithin) was found to be promising. Fourier Transform infra-red (FT-IR) spectra studies represented no interaction and physicochemical characteristics were found within the limits. The percentages of drug content and entrapment efficiency were determined to be 95.16%±0.40 and 94.20%±0.20, respectively. In vitro drug release was about 95.72%±0.30. Conclusion: Proniosomal gel could constitute a promising approach for topical delivery of Amphotericin B by encapsulating it in non-ionic surfactant to provide patient compliance with cutaneous fungal infection, which was found to be safe, tolerable and efficacious.


Polymers ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 135
Author(s):  
Muhammad Khurshid Alam Shah ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Shafi Ullah ◽  
Muhammad Shahid Latif ◽  
...  

This study aims to develop chitosan-based voriconazole nanoparticles (NPs) using spray-drying technique. The effect of surfactants and polymers on the physicochemical properties, in vitro release, and permeation of NPs was investigated. The prepared NPs containing various surfactants and polymers (e.g., Tween 20 (T20), Tween 80 (T80), sodium lauryl sulfate (SLS), propylene glycol (PG), and Polyethylene glycol-4000 (PEG-4000)) were physiochemically evaluated for size, zeta potential, drug content, percent entrapment efficiency, in vitro release, and permeation across rats’ skin. A Franz diffusion cell was used for evaluating the in vitro release and permeation profile. The voriconazole-loaded NPs were investigated for antifungal activity against Candida albicans (C. albicans). The prepared NPs were in the nano range (i.e., 160–500 nm) and positively charged. Images taken by a scanning electron microscope showed that all prepared NPs were spherical and smooth. The drug content of NPs ranged from 75% to 90%. Nanoparticle formulations exhibited a good in vitro release profile and transport voriconazole across the rat’s skin in a slow control release manner. The NPs containing SLS, T80, and PG exhibited the best penetration and skin retention profile. In addition, the formulation exhibited a potential antifungal effect against C. albicans. It was concluded that the development of chitosan NPs has a great potential for the topical delivery of voriconazole against fungal infection.


2021 ◽  
pp. 1-12
Author(s):  
Kamran Khan ◽  
Shefaat Ullah Shah ◽  
Yusuf S. Althobaithi ◽  
Kifayat Ullah Shah ◽  
Aman Ullah ◽  
...  

Tremendous increase of fungal infections in hospitalized or immune compromised patients has been reported from the last two decades. These infections are commonly treated using econazole and miconazole that have shorter half-life and produce severe side effects. All such issues can be addressed using targeted drug delivery. We developed SNLs based formulation for the treatment of mycosis. The high pressure homogenization method was employed for formulation followed by characterization, assay for antifungal activity, in vitro drug release and ex vivo permeation. The particle size of Econazole-Betamethasone-loaded SLNs, Econazole-loaded SLNs, Betamethasone-loaded SLNs and Blank SLNs were 377.4±23 nm, 298.7±9 nm, 177.7±15 nm and 113.4±6 nm respectively. The SEM images displayed that droplets are uniform and spherical in shape which ranged from 113.4±6 to 377.4±23 nm. In DSC, the SLNs formulation showed endothermic peak at 185.2 °C±0.9. Drug content of Econazole loaded SLNs was 82±0.1 and its entrapment efficiency was approximately 90.4±0.2. Betamethasone SLNs displayed highest drug content which was 83.5±0.4 while encapsulation efficiency of same formulation was 94.2±0.4. The Econazole and Betamethasone combined SLNs exhibited drug content of 80±0.3 while its encapsulation efficiency was 93.1±0.5. E-SLNs have significantly high drug release (p <  0.05) as compared to other formulation B-SLNs and EB-SLNs.The Econazole loaded formulations displayed antifungal activity with no synergistic or antagonistic effect with each other. Drug permeation from Econazole SLNs, Betamethasone SLNs and combined Econazole and Betamethasone SLNs was 45%, 40% and 38% respectively. Overall, SLN’s are an effective carrier for topical delivery of antifungals agents and that may be helpful in bypassing the serious side effects associated with oral delivery.


Author(s):  
Shital V. Sonawane ◽  
Avish D. Maru ◽  
Mitesh P. Sonawane

Oral nanosuspension of ritonavir was prepared by antisolvent precipitation method using various polymers such as Eudragit RS100, Poloxamer 407, SLS and Methanol.The effect of eudragit RS100 and poloxamer 407 used stabilizer and SLS is surfactant was investigated on particle size and distribution, drug content, entrapment efficiency was observed. Ritonavir is having low solubility and low permeability drug belonging to class-IV according to BCS. Drug-excipient compatibility and amorphous nature of ritonavir drug is prepared nanosuspension was confirmed by FTIR, DSC and Motic microscope studies, respectively. The nanosuspension was further evaluated for drug content, saturation solubility study and entrapment efficiency. The average particle size of ritonavir nanaosuspensions formulas was observed from 0.006 µm to 0.017 µm. The studied in the solubility and dissolution rate there are the increase solubility and dissolution rate of ritonavir nanosuspension.


Author(s):  
Misbah Khanum ◽  

The objective of this work was to prepare Fluconazole nanoparticles, and then incorporated into the freshly prepared gel for transdermal delivery, reducing the oral side effects of the drug and forenhancing stability. Fluconazole is commonly used antifungal agents for the treatment of local and systemic fungal infections. In this study Fluconazole nanoparticles was prepared by using Eudragit RL 100 by nanoprecipitation method with different drugs to polymer (1:1, 1:2 and 1:3) and stabilizer (Poloxamer 188) ratios (0.5%, 0.75% and 1%) and evaluated for various parameters. Drug-excipients compatibility was performed by FTIR study. The particle size, polydispersity index, Zeta potential, % Entrapment efficiency and % drug content of all the formulations were found in the range of 16.8 to 48.9nm, 0.229 to 0.558, -11.6 to -26.6 mv, 28.41% to 95.78% and 59% to 97.38%. From SEM studies it was revealed that Fluconazole nanoparticles particles are spherical in shape and without any agglomeration. From the in-vitro drug release study, it was revealed that sustained release of same formulation last up to 12 hours. From the stability study, it was revealed that the F5 formulation was stable at 40°C ± 2°C /75% ± 5%RH and 4°C. The optimised formulation F5 was selected to prepare Fluconazole loaded nanoparticles based topical gels using different concentration of Carbopol 934 and 940 and characterized for pH, spreadability, drug content, viscosity and in-vitro drug diffusion. Among the five formulations, G5 was selected as the best formulation. The pH of all formulations was found near to the skin pH value. The in-vitrodiffusion study of Fluconazole gel (G5) showed 94.75%. The optimized formulation G5 was checked for mechanism and kinetics of drug release. It is found it following Zero order release and non-Fickian mechanism. The selected Gel formulation G5 was found to be stable at 40°C ± 2°C /75% ± 5%RH and 4°C, it is clear that the formulation did not undergo any chemical changes found more stable at room temperature


Author(s):  
Yogesh Singh ◽  
Anjana Bhardwaj

Topical drug administration is a localized drug delivery system anywhere in the body through ophthalmic, rectal, vaginal and skin as topical routes. Skin is one of the most readily accessible organs on human body for topical administration and is main route of topical drug delivery system. There are various skin infections caused by fungus. An antifungal medication is a pharmaceutical fungicide used to treat mycoses such as athlete’s foot ringworm, candidiasis. Antifungal works by exploiting differences between mammalian and fungal cells to kill the fungal organism without dangerous effect on host. Itraconazole (ITZ) is commonly used in the treatment of fungal infections. It has low bioavailability (55%) because of low aqueous solubility and first pass effect. Hence we attempted to develop Itraconazole-loaded invasomes hydrogel. ITZ-loaded invasomes were prepared by conventional thin layer evaporation technique using Phospholipon 90H, terpene (Limonene) and ethanol. The optimized ITZ-loaded invasomes was incorporated into carbopol 934p (0.5 to 2%) solution to get a hydrogel for improving convenience in superficial application. FT-IR studies revealed no interaction between the drug and excipients. The formulated hydrogel formulation was evaluated with parameter pH, viscosity, gel strength, drug content, spread ability, in-vitro release test, wash ability, extrudability study and stability studies. The formulation OIGF4 showed a drug content of 99.12% and drug release of 99.78% in 72 hrs, which contains carbopol 934p concentration 2%w/w. The present work also focuses on making the formulation more pharmaceutically acceptable.


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