scholarly journals Evaluation of Grewia ferruginea Hochst ex A. Rich Mucilage as Suspending Agent in Metronidazole Benzoate Suspension

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Tsadkan Gebremeskel Haile ◽  
Gereziher Gebremedhin Sibhat ◽  
Ebisa Tadese ◽  
Desta Tesfay ◽  
Fantahun Molla

Various species of the genus Grewia have been investigated for different pharmaceutical applications as excipients, yet a study on the potential use of Grewia ferruginea mucilage (GFM) as a suspending agent is lacking. Thus, this study is aimed at evaluating the efficacy of Grewia ferruginea mucilage (GFM) as a suspending agent in metronidazole benzoate suspension. The suspensions were prepared using 0.5%, 1%, 1.5%, and 2% w / v of GFM and compared with suspensions prepared from xanthan gum (XGM) and sodium carboxyl methyl cellulose (SCMC) in similar concentrations. The prepared suspensions were evaluated for visual appearance, pH, rheology, sedimentation volume, redispersibility, degree of flocculation, and in vitro drug release profile. Stability study was done at different storage conditions for three months. The results indicated that all the prepared suspension formulations exhibited pseudoplastic flow characteristics with viscosity imparting ability of the suspending agents in the order of XGM > GFM > SCMC ( p < 0.05 ). The flow rate and redispersibility of the formulations prepared with GFM were significantly lower than those with SCMC and higher than those prepared with XGM. At 0.5% w / v suspending agent concentrations, the sedimentation volume of the formulations was in the order of XGM > GFM > SCMC ( p < 0.05 ). However, at all other concentrations, the sedimentation volume of the formulations prepared with GFM had similar results with XGM but exhibited significantly higher sedimentation volume than SCMC. The formulations with GFM showed a higher degree of flocculation at 0.5% w / v concentration but were comparable at 1.5% w / v with XGM containing formulations. The pH, assay, and in vitro release profile of all assessed formulations were within the pharmacopial limit. Thus, based on the finding of this study, it can be concluded that Grewia ferruginea bark mucilage has the potential to be utilized as a suspending agent in suspension formulations.

2019 ◽  
Vol 11 (1) ◽  
pp. 106
Author(s):  
Gina S. El-feky ◽  
Gamal M. Zayed

Objective: The objective of this study was to design an effective topical treatment for oral mucositis.Methods: Poly-(DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) and Poloxamer407 (PLX)/Hydroxy propyl methyl cellulose (HPMC) hydrogel matrix (HG) were used as combined carriers for benzydamine HCL (BNZ). BNZ loaded PLGA nanoparticles were assessed for their particle size, PDI, zeta potential and entrapment efficiency. Scanning electron microscopy, thermosensitivity study, mucoadhesion study, in vitro release and in vivo investigation were used to characterize the combined BZN loaded PLGA NPs HG.Results: Negatively charged NPs with an average diameter of 139±4.92 nm were incorporated into PLX/HPMC HG bases. The gelation temperature of BZN-PLGA-NPs-HGs ranged between 31°C and 36.5°C. When diluted with saliva simulated fluid, BZN-PLGA-NPs-HGs preserved their gelation properties. Mucoadhesion was found lower for formulations prepared with PLX without HPMC. An increase in the concentrations of PLX from 10 to 30% resulted in an increase in adhesion. Both PLGA-NPs and PLGA-NPs-HG provided a biphasic drug release profile while BZN-HG provided monophasic zero order release pattern. The in vivo study showed that animal groups treated with BZN-HG and BZN-PLGA-NPs-HG showed a significantly higher reduction percentage in ulcer surface area compared to those treated with BZN-PLGA-NPs. BZN-PLGA-NPs-HG group needed 10 d of treatment to complete healing versus 16 d, 14 d and 12 d for the complete healing of groups with no treatment, treated with BZN-PLGA-NPs and treated with BZN-HG, respectively.Conclusion: BZN-PLGA-NPs-HG could represent a promising mean for the effective treatment of oral mucositis induced by cancer therapy.


2018 ◽  
Vol 10 (2) ◽  
pp. 52 ◽  
Author(s):  
Akshay Singha Roy ◽  
Sudipta Das ◽  
Arnab Samanta

Objective: The objective of the present study was to formulate and evaluate liposomes loaded with isoniazid.Methods: Liposome of isoniazid was made by thin layer film hydration method. L-α-phosphatidylcholine and cholesterol were used to make multiamellar vesicles. Six batches of liposomes were prepared based on the different weight ratio of L-α-phosphatidylcholine and cholesterol. Differential scanning calorimetry (DSC) study conducted to study in any incompatibility.Results: The prepared liposomes were evaluated by particle size analysis, entrapment efficiency, release study and stability study. Particle sizes were determined from the scanning electron microscopy (SEM) photographs. When particle frequencies were plotted against particle diameter in the histogram, it showed that F1 batch had a skewed distribution towards smaller liposomes while F6 shows a proper bell-shaped curve with a mean at 225 mm. The percentage entrapment efficiency was found to be 8.99 ± 0.15 to 4.19 ± 0.12 % respectively. From the release profile, it was seen that F1 batch was fastest and F6 was slowest to release the drug. The satisfactory batch F1 was packed in Eppendorf tube and stored at 4 °C temperature for one month. At the end of one month, the samples were analyzed for their physical properties, drug entrapment and in vitro release profile. The percentage release was found to be 96.5 ± 3.2 after 4 h.Conclusion: The F1 batch showed most promising results compared to other. No significant change was found during one month’s stability study of final batch (F1).


Author(s):  
SADIA ANWAR ◽  
SYED UMER JAN ◽  
RAHMAN GUL

Objective: The purpose of this study was to formulate and evaluate of Celecoxib cream and it’s in vitro release study. Methods: The release study was conducted, using dialysis cellulose membrane, in Franz cells. The donor chamber was filled with phosphate buffer pH 7.4, released medium were analyzed by UV-Vis spectrophotometer at 250 nm. Kinetics model was used for calculations. The cream was followed by different evaluations like pH measurement, homogeneity, spreadability, stability study, drug content, SEM, XRD studies and skin irritation test was used for the reliability of physical conditions and chemical relation. DD solver and SPSS were used for statistical analyzation of the data. Results: The best in vitro drug release profile achieved with thyme oil in Celecoxib cream. Formulation F2 showed the highest (83%) released. The results of the Celecoxib (1%) were suitable in all constraints. The prepared Celecoxib cream was encouraging for the formulation of transdermal drug delivery. Conclusion: The Celecoxib cream was successfully prepared and could be beneficial for transdermal drug delivery.


2017 ◽  
Vol 1 (1) ◽  
pp. 01-02
Author(s):  
Swathi Goli

The aim of the present study was to develop colon targeted matrix tablets of Metformin HCl using various conc. of selected polymers such as HPMC, Ethyl Cellulose Guar gum and combination of the same. Tablets were prepared by direct compression method and both pre-compression and post- compression parameters for all batches shows in the acceptable ranges. Short term accelerated stability studies was performed according to ICH guidelines temperature of 400±20 and relative humidity of 75%±5% RH to study any physical changes and chemical decomposition of drug, no formulation shown any physical or chemical changes. The compatibility of drugs, polymers and excipients were determined by FT-IR Spectroscopy results showed that the drug was compatible with polymers and all excipients. Dissolution studies were performed for 12 hours study in 1.2 pH for first 2 hrs then in 7.4 pH for next 3hrs followed by 6.8pH phosphate buffer at the temperature of 37±0.50C at 100rpm. The dissolution data so obtained was fitted to various mathematical kinetic models and the drug release followed mixed order and Higuchi’s model. To study release mechanism of drug from matrices the data were fitted to Koresmeyer-Peppas model and the release. In –vitro release profile of Metformin HCl from various polymers showed that drug increasing the conc. of polymers resulted in reduction in the release rate of drug (MTF1 to MTF12). Formulation containing combination of E.C-G.G, HPMC-G.G and E.C-HPMC showed drug release profile for MTF-12 about 38.72% after 12 hrs, MTF-11 about 40.66% after 12 hrs, for MTF-10 about 45.45% after 12 hrs. This is an indicative of retardation of drug release when polymer combination was changed. Results showed that the tablets with higher binding concentration showed minimum drug release. Combination of polymers shows greater retarding of drug release.


2020 ◽  
Vol 14 ◽  
Author(s):  
Sangam Shrestha ◽  
Preethi Sudheer ◽  
Kavitha A.N

Background: Ezetimibe is a cholesterol lowering agent with an oral bioavailability of 50 % by the virtue of its poor solubility, extensive hepatic and intestinal metabolism. Objective: The study is aimed to overcome low bioavailability issues of ezetimibe by formulating an oral disintegrating film. Method: The low solubility of ezetimibe was tackled preparing solid dispersions using mannitol, β-cyclodextrin and urea. The mannitol solid dispersion assimilated oral disintegrating film was prepared and optimized using 2 3 factorial design, where concentration of film formers hydroxypropyl methyl cellulose (K5 & K15) (X1and X2) and super disintegrant, sodium starch glycolate (X3) was used as factors on the response disintegration time (Y). The films were evaluated for physical properties, time of disintegration and drug release profiles. Results and Discussions: Mannitol solid dispersion (1:2 ratio) on the basis of the superior drug content, solubility and in vitro release profile was preferred in film formation. The low crystalline nature of the solid dispersion was very evident by the absence of prominent peaks in the X Ray diffraction pattern and the reduced peak intensity of melting endotherms. The correlation coefficient (R2 ) and statistical parameter analysis of variance specifies implication of linear factors on responses, which is apparent from confidence intervals (Pvalues) less than 0.05. The in vitro release profile of all the eight formulations (F1-F8) in phosphate buffer solution pH 6.8 revealed a significant increment in comparison to ezetimibe. Conclusion: The study revealed that the formulation approach could overcome the biopharmaceutical challenge of solubility as well as low bioavailability issues of ezetimibe.


2017 ◽  
Vol 9 (5) ◽  
pp. 109
Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Randika Dwiputra ◽  
Tryas Yanuari ◽  
Santi Purna Sari ◽  
...  

Objective: Drug delivery to the colon via oral route can be directly treated a variety of diseases in the colon, such as fibrosis. Tetrandrine is a drug that has anti-fibrosis effects. In this study, chitosan-tripolyphosphate (TPP) beads containing tetrandrine was made and evaluated for in vitro release profile and in vivo targeted test.Methods: Chitosan-TPP tetrandrine beads were prepared by ionic gelation method with variation in sodium tripolyphosphate concentration: 3% (Formula 1), 4% (Formula 2), and 5% (Formula 3). All formulae were characterized for its morphology, particle size, moisture content, process efficiency, entrapment efficiency, thermal character, crystallinity, and swelling. Then, the best formula was coated with HPMCP HP-55, CAP, Eudragit L100-55, or Eudragit L100 prior to drug release profile in vitro and in vivo test.Results: Beads from all formulae had an average size: 920.50±0.04 µm, 942.21±0.08 µm, and 1085.95±0.03 µm; Water content: 7.28±0.003%, 5.64±0.005%, and 6.84±0.004%; Process efficiency: 29.70%, 28.96%, and 29.70%; Entrapment efficiency: 16.20±0.63%, 17.02±0.37%, and 20.42±0.70% for Formula 1, 2, and 3, respectively. In addition, the results of in vitro cumulative drug release were 67.36%, 76.04%, 83.12%, 83.21%, 40.16%, 37.98%, 45.86%, 41.71% for Formula 3A-3H, respectively.Conclusion: It can be concluded that Formula 3D (CAP 15%) was chosen as a formulation with the best in vitro profile. Moreover, the in vivo targeted test showed that Formula 3D was able to deliver the beads to the intestine compared to the control beads.


Author(s):  
SUDIPTA DAS ◽  
RIMI DEY

Objectives: A novel formulation was developed with glimepiride loaded trivalent ion Al+3 cross-linked and acetalated gellan gum microspheres. Methods: The glimepiride loaded microspheres were formulated using sodium alginate and gellan gum. Cross-linking agents used for the microspheres were aluminum chloride (AlCl3) and glutaraldehyde (GA). The evaluation processes of prepared microspheres were carried out by in-vitro release study, swelling index, microscopic analysis, and entrapment efficiency. Results: All the formulations show good entrapment efficiency and the maximum entrapment 84.6% was governed by the formulation (F3) cross-linked by AlCl3 and GA and their obtained mean particle size were 12.46±3.21 μm. Release profile of the formulations revealed the sustained design of the drug, particularly this formulation (F3), releasing approximately 40% over 4 h. Conclusions: From this experiment, it can be accustomed that F3 possesses higher standard formulation than the rest due to good release profile and entrapment efficiency. Therefore, the long term stability study is required for future development of this formulation.


Author(s):  
Binil Starly ◽  
Shih-Feng Lan ◽  
David Schmidtke

Dental implants provide support for dental crowns and bridges by serving as abutments for the replacement of missing teeth. The objective of this study was to demonstrate a novel method of controlled localized delivery of antibacterial agents to an implant site using a custom fabricated ring. The study involved incorporating a model antibacterial agent (metronidazole) into custom designed Poly-ε-Caprolactone/Alginate (PCL/Alginate) composite rings to produce the intended controlled release profile. In vitro release studies indicate that pure (100%) alginate rings exhibited an expected burst release of metronidazole in the first few hours, whereas Alginate/PCL composite rings produced a medium burst release followed by a sustained release for a period greater than 4 weeks. By varying the PCL/Alginate weight ratios, we have shown that we can control the amount of antibacterial agents released to provide the minimal inhibitory concentration needed for adequate protection. The developed system demonstrates a controllable drug release profile and the potential for the ring to inhibit bacterial biofilm growth for the prevention of diseases such as peri-implantitis resulting from bacterial infection at the implant site.


2017 ◽  
Vol 4 (2) ◽  
pp. 118
Author(s):  
Vasudha Bakshi ◽  
Swapna S. ◽  
Deepa Kumari Choudhary ◽  
Ch. Revanth ◽  
B. Sai KumarCh. Praveen ◽  
...  

Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract.Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction.Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro. The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR).Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.


Author(s):  
SANJEEVANI DESAI ◽  
DURGACHARAN BHAGWAT ◽  
SUNITA SHINDE ◽  
JOHN DISOUZA

Objective: The present study was aimed to develop of the Guanfacine Hydrochloride Extended-release tablets for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). The dosage regimen of Guanfacine Hydrochloride is 4 mg at every 6 h. The concentration of Guanfacine in plasma is fluctuating. Hence, to control the plasma fluctuation and to avoid toxicity problem, Guanfacine Hydrochloride was chosen as a drug with an aim to develop an extended release system for 20 to 24 h. Methods: The design of the system was based on the use of pH-dependent polymer (Hydroxypropyl Methyl Cellulose), pH-independent polymer (Eudragit L 100-55), along with microenvironment modifiers such as organic acid (Fumaric acid) were used in the formulation. Drug-excipient compatibility was studied by FTIR. Before compression, the granules were evaluated for precompression parameters such as bulk density, tapped density, an angle of repose, compressibility index and Hausner’s ratio. After compression, evaluation tests of tablets such as general appearance, hardness, thickness, weight variation, friability, content uniformity, in vitro release studies and stability studies were performed. Results: Out of 9 formulations, the drug release was found to be within the innovator formulation F9. The stability study of formulation F9 revealed there was no significant change in physical and chemical properties of drug stored at 40 °C/75 % RH, 30 °C/65 % RH, 25 °C/60 % RH for 2 mo. Conclusion: Optimized formulation batch F9 showed highest F2 value which indicates similarity with innovator product. The study indicates that Guanfacine Hydrochloride Extended-release tablet was successfully developed.


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