scholarly journals Formulation of enteric coated microspheres containing pantoprazole

2021 ◽  
Vol 63 (3) ◽  
pp. 56-62
Author(s):  
Xuan Truong Le ◽  
◽  
Hue Minh Nguyen ◽  
Ngoc Quynh Le ◽  
Thi Thu Loan Trinh ◽  
...  
Keyword(s):  
Gastric Acid ◽  
Morphological Characteristics ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Enteric Coated ◽  
Inhibitor Drug ◽  
Emulsification Solvent Evaporation ◽  
Average Size

Pantoprazole is a first-line proton pump inhibitor drug for the treatment of gastric acid secretion disorders that is known to have minimal side effects and drug interactions. To improve its stability in gastric acid, delayed-release microspheres containing pantoprazole was prepared by emulsification-solvent evaporation using a polymer-containing mixture of hydroxypropyl cellulose (HPC) and ethyl cellulose (EC), which was then coated by alginate and EudragitL100. The morphological characteristics of the microspheres were examined by SEM, the particle size distribution inferred by laser diffraction, and the physical state of drug substance was measured by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and in vitro drug release. The three formulations of microspheres chosen for this study had an average size of 100 μm. The dissolution profile showed less than 10% of the drug was released after 120 min in 0.1-M HCl and more than 75% of drug was released after 45 min in a phosphate buffer with a pH of 6.8.

scholarly journals Encapsulation of Naproxen in Eudragit RSPO Microsphere system: In vitro Characterization and Compatibility Studies

2013 ◽  
Vol 11 (2) ◽  
pp. 147-155 ◽  
Author(s):  
Shovan Paul ◽  
Sharmin Akhter ◽  
Ikramul Hasan ◽  
Syed Shabbir Haider ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Molecular Dispersion ◽  
In Vitro Characterization ◽  
Sustained Action ◽  
Evaporation Technique ◽  
Emulsification Solvent Evaporation

The present study has been performed to encapsulate naproxen to provide sustained action and to minimize local side effects by avoiding the drug release in the upper gastrointestinal tract. Naproxen was microencapsulated by oil-in-oil emulsification-solvent evaporation technique using Eudragit RSPO. The formulations were prepared by sequential increase in drug loading ranging from 10% to 70%. In-vitro drug release was studied in a paddle type dissolution apparatus (USP type II) for six hours in phosphate buffer having pH 7.4. At 10% and 70% loading the release were 42.89% and 86.33%, respectively. The release mechanisms were explored and explained with zero order, first order, Higuchi and Korsmeyer-Peppas models. The correlation-coefficient values of the trend lines of the graphs showed that the formulations were best fitted with Korsmeyer-Peppas release pattern. Microspheres` surface morphologic study was done by scanning electron microscopy. Drug polymer incompatibility studies were performed by Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectroscopy (FTIR). The absence of endothermic melting peak of naproxen in DSC thermogram revealed that the drug might be dispersed in the polymer as solid solution or in a metastable molecular dispersion. But the chemical integrity of Naproxen was not changed or destroyed within the microsphere which was confirmed by FTIR spectral data. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14573 Dhaka Univ. J. Pharm. Sci. 11(2): 147-155, 2012 (December)

scholarly journals Enhancement of Aqueous Solubility, Dissolution Profile, and Oral Bioavailability of Pentoxifylline by Microsponges

2021 ◽  
Author(s):  
Anil Raosaheb Pawar ◽  
Nikhil Arun Shete ◽  
Priyanka Vitthal Jadhav ◽  
Vinayak Kashinath Deshmukh ◽  
Jaswandi Sameer Mehetre
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Aqueous Solubility ◽  
Diffusion Method ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Pure Drug

Microsponge, a novel drug delivery system, is designed to deliver a pharmaceutically active ingredient efficiently at the minimum dose. Microsponge plays an important role in enhancing drug stability, reducing side effects, and modifying drug release profiles. It is mostly used for transdermal delivery. Recent studies also explored their use for oral administration. This study aimed to explore the potential use of the microsponge technique in improving the aqueous solubility and dissolution profile of pentoxifylline (PTX). In this study, microsponges were prepared by a quasi-emulsion solvent diffusion method by varying concentrations of carriers. Nine different ratios of the PTX:Eudragit E-100 with varying amounts of dichloromethane were used. All formulated microsponges were evaluated for %production yield, compatibility of drug excipient, encapsulation efficiency, in vitro drug release, and in vivo bioavailability, as well as recorded by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). Our data suggested that the aqueous solubility of PTX microsponges was four times greater than that of pure drug. The in vitro drug release of selected microsponges (M8) was found to be 70%; furthermore, the in vivo study suggested that the selected formulation significantly enhanced drug concentration in the plasma (9,219 ng/mL in 12 hours) in comparison to pure drug PTX (2,476 ng/mL in 12 hours). SEM showed that the prepared microsponges were spherical with porous nature. Fourier-transform infrared spectroscopy and DSC studies confirmed an absence of incompatibility among drugs and selected excipients. The pH of the selected gel was found to be 6.8, which was compatible with those of skin and oral formulations also. All above data suggested a highly successful and beneficial use of the microsponge technique in enhancing aqueous solubility, dissolution profile, and oral bioavailability of PTX. Microsponge-based delivery of PTX may represent an alternative strategy to improve the bioavailability of the drug.

scholarly journals Preparation, Characterization and Compatibility Studies of Naproxen Loaded Microspheres of Cellulosic and Polymethacrylic Polymeric Blend

2013 ◽  
Vol 12 (1) ◽  
pp. 11-21 ◽  
Author(s):  
Sharmin Akhter ◽  
Shova Paul ◽  
Ikramul Hasan ◽  
Navid Jubaer Ayon ◽  
Syed Shabbir Haider ◽  
...  
Keyword(s):  
Ethyl Cellulose ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Molecular Dispersion ◽  
Sustained Action ◽  
Evaporation Technique ◽  
Dissolution Apparatus ◽  
Emulsification Solvent Evaporation ◽  
Upper Gastrointestinal

Naproxen, a well-known non-steroidal anti-inflammatory drug was encapsulated with cellulosic and polymethacrylic polymers to provide sustained action and to minimize gastro esophageal side effects by avoiding the release of drug in the upper gastrointestinal tract. Emulsification-solvent evaporation technique using Ethyl Cellulose, Eudragit RSPO and their combination as release retardant was the method of choice. The formulations were prepared by keeping the amount of drug fixed to 1g and the total amount of polymer fixed to 1g in which Ethyl Cellulose and Eudragit RSPO were used in varying combination. In-vitro drug release was studied in a paddle type dissolution apparatus (USP type II) for eight hours in phosphate buffer having pH 7.4. After 8 hours, the release of drug was 86.20% for F6 which contains equal amount of Ethyl Cellulose and Eudragit RS PO and 71.57% for F7 which contains only Eudragit RSPO. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer-Peppas and Hixson Crowell models. The correlation-coefficient values of the trend lines of the graphs showed that the formulations were best fitted with Korsmeyer-Peppas release pattern. Microspheres surface morphological study was done by Scanning Electron Microscopy (SEM). Drug polymer incompatibility studies were performed by Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectroscopy (FTIR). The absence of endothermic melting peak of Naproxen in DSC thermogram revealed that the drug might be dispersed in the polymer as solid solution or in a metastable molecular dispersion. But the chemical integrity of Naproxen was not changed or destroyed within the microsphere which was confirmed by FTIR report. Dhaka Univ. J. Pharm. Sci. 12(1): 11-21, 2013 (June) DOI: http://dx.doi.org/10.3329/dujps.v12i1.16295

scholarly journals Cefotaxime Loaded Polycaprolactone Based Polymeric Nanoparticles with Antifouling Properties for In-Vitro Drug Release Applications

Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2180
Author(s):  
Sana Javaid ◽  
Nasir M. Ahmad ◽  
Azhar Mahmood ◽  
Habib Nasir ◽  
Mudassir Iqbal ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
In Vitro Release ◽  
Bacterial Strains ◽  
In Vitro Drug Release ◽  
Antifouling Activity ◽  
Polymeric Drug ◽  
Pure Drug ◽  
Average Size

The objective of the present study was to achieve the successful encapsulation of a therapeutic agent to achieve antifouling functionality regarding biomedical applications. Considering nanotechnology, drug-loaded polycaprolactone (PCL)-based nanoparticles were prepared using a nano-precipitation technique by optimizing various process parameters. The resultant nano-formulations were investigated for in vitro drug release and antifouling applications. The prepared particles were characterized in terms of surface morphology and surface properties. Optimized blank and drug-loaded nanoparticles had an average size of 200 nm and 216 nm, respectively, with associated charges of −16.8 mV and −11.2 mV. Studies of the in vitro release of drug were carried out, which showed sustained release at two different pH, 5.5 and 7.4 Antifouling activity was observed against two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. The zone of inhibition of the optimized polymeric drug-loaded nanoparticle F-25 against both strains were compared with the pure drug. The gradual pH-responsive release of antibiotics from the biodegradable polymeric nanoparticles could significantly increase the efficiency and pharmacokinetics of the drug as compared to the pure drug. The acquired data significantly noted that the resultant nano-encapsulation of antifouling functionality could be a promising candidate for topical drug delivery systems and skin applications.

EFFECT OF DRUG TO B-CYCLODEXTRIN RATIO AND METHOD OF COMPLEXATION IN THE DEVELOPMENT OF B-CYCLODEXTRIN INCLUSION COMPLEX OF OFLOXACIN

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 34-40
Author(s):  
M Panchpuri ◽  
◽  
D Singh ◽  
A Semalty ◽  
M. Semalty
Keyword(s):  
Inclusion Complex ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Dissolution Study ◽  
Drug Content ◽  
Kneading Method ◽  
Made In

Ofloxacin, a second generation fluoroquinolone, shows poor aqueous solubility and dissolution profile. Thus, ofloxacin–β-cyclodextrin complexes were prepared to improve its dissolution by imparting an environment of improved hydrophilicity. Ofloxacin was complexed with β-cyclodextrin (in 1:1 and 1:2 molar ratio) by two different methods namely, solvent evaporation and kneading method. These inclusion complexes were evaluated for solubility, drug content, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. The highest drug content (35.45%) was found in complex made by kneading method (OK1:1) in 1:1 molar ratio. All the complexes OSE1:1, OSE1:2, OK1:1, OK1:2 were found to be showing rough and porous surface morphology in SEM. Solubility as well as the dissolution of the complexes was found to be improved. Complex prepared by kneading method in 1:1 molar ratio (OK1:1) showed a marked improvement in percent drug release (88.94%) than that of pure drug (54.22%) at the end of 1 hour in dissolution study. FTIR, DSC and XRPD data confirmed the formation of inclusion complex. It was concluded that the complex made in 1:1 molar ratio (irrespective of the method) showed better solubility and dissolution profile as compared to complex made in 1:2 molar ratio.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Eight enteric-coated 50 mg diclofenac sodium tablet formulations marketed in Saudi Arabia: in vitro quality evaluation

2020 ◽  
Vol 13 (1) ◽  
Author(s):  
Muhammad M. Hammami ◽  
Rajaa F. Hussein ◽  
Reem AlSwayeh ◽  
Syed N. Alvi
Keyword(s):  
Quality Evaluation ◽  
Diclofenac Sodium ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
United States Pharmacopoeia ◽  
Weight Variation ◽  
Tablet Formulations ◽  
Enteric Coated

Abstract Objective To evaluate in vitro quality of enteric-coated 50 mg diclofenac sodium tablet formulations on Saudi market. Results A reference and seven generic (G1-7) formulations were commercially available in December 2019/January 2020 and were assessed within 25–75% of manufacture-expiration period. Weight variation (range as% difference from mean, n = 20), active substance content (ASC, mean (SD) as% difference from label, n = 20), hardness (mean (SD), n = 10), and friability (% weight loss, n = 20) were 97–103%, 102.0% (3.4%), 15.4 (1.1) kg, and 0.24%, respectively, for the reference. For G2-7, they were ≤ ±5%, 98.6% (4.0%) to 109.9% (1.8%), 11.9 (0.9) to 18.3 (0.8) kg, and ≤ 0.00 to 0.75%, respectively. G1 ASC, hardness, and friability were 111.3% (1.7%), 20.1 (1.7) kg, and 1.10%, respectively. Disintegration time (n = 6) and dissolution profile (n = 8) were also determined. No formulation disintegrated or released ˃ 0.1% of label ASC in 0.1 N HCl for 2 h. The reference disintegrated in 15:00 min:seconds and released a mean (range) of 100% (99–103%) of label ASC by 45 min in phosphate buffer (pH = 6.8). G1-7 disintegrated in 8:53 to 20:37 min:seconds and released 81% (69–90%) (G1) to 109%. Except for borderline performance of G1, all formulations passed in vitro quality tests according to United States Pharmacopoeia.

scholarly journals A Cyclodextrin-Based Controlled Release System in the Simulation of In Vitro Small Intestine

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1212
Author(s):  
Danni Zheng ◽  
Liuxi Xia ◽  
Hangyan Ji ◽  
Zhengyu Jin ◽  
Yuxiang Bai
Keyword(s):  
Complex System ◽  
Small Intestine ◽  
Controlled Release ◽  
Glucose Production ◽  
Scanning Calorimetry ◽  
Release System ◽  
In Vitro Simulation ◽  
Controlled Release System ◽  
Enteric Coated

A novel cyclodextrin (CD)-based controlled release system was developed in the small intestine to control the rate of drug release, on the premise of enteric-coated tablets. The system was designed based on the enzymes exogenous β-cyclodextrin glycosyltransferase (β-CGTase) and endogenous maltase-glucoamylase (MG), wherein MG is secreted in the small intestine and substituted by a congenerous amyloglucosidase (AG). The vanillin-/curcumin-β-CD complexes were prepared and detected by Fourier transform infrared (FT-IR), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC), and host CD degradation was measured based on the glucose yield. The combination of β-CGTase and AG was also functional in the CD complex system. The variations in the concentrations of added β-CGTase, with AG constantly in excess, could effectively alter the rate of host CD degradation and guest release by monitoring glucose production and color disappearance, thus, demonstrating that guest release in the CD complex system could be precisely controlled by changing the amount of β-CGTase used. Thus, the in vitro simulation of the system indicated that a novel controlled release system, based on endogenous MG, could be established in the small intestine. The CD-based controlled release system can be potentially applied in drug delivery and absorption in the small intestine.

Statistical assessment of in vitro drug release kinetics and quality evaluation of desloratadine orally disintegrating generic tablets available in Bangladesh

2020 ◽  
pp. 174113432094775
Author(s):  
Madhabi Lata Shuma ◽  
Shimul Halder
Keyword(s):  
Release Kinetics ◽  
The United States ◽  
Quality Parameters ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Orally Disintegrating Tablets

The objective of the present study was to compare the in vitro equivalence of different orally disintegrating tablets (ODT) of Desloratadine (DES) available in Bangladesh pharmaceutical market with the reference brand. The in vitro dissolution study was carried out using the United States Pharmacopoeia (USP) paddle method and a comparative study were also carried out with the reference brand. Other pharmacopoeial and non-pharmacopoeial quality assessment parameters including hardness, friability, water absorption ratio, and disintegration time etc. were also evaluated. From the results of the dissolution profile of the commercially available products, it found majority of the products didn’t exhibited compendial requirements in dissolution behavior to the reference brand with model-independent approach ( f2 > 50, f1 < 15) and showed statistically significant differences. Additionally, the data of different physical quality parameters revealed that all commercial products complied with the official specifications. From these findings, it could be suggested that the DES-ODT formulations’ available in the Bangladesh market could be prescribed; however additional experiments might require to clarify the interchangeability among the products.

scholarly journals Development and Characterization of Ofloxacin & Prednisolone Loaded Nanostructured Lipid Carriers (Nlc) for Topical Route

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Morphological Characteristics ◽  
Nanostructured Lipid Carriers ◽  
Diffusion Method ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Drug Content

Aim: The present study was designed to develop and characterize nanostructured lipid carriers (NLC) of Ofloxacin and Prednisolone for topical use in case of infections associated with inflammation. Materials and Methods: Ofloxacin was obtained as gift sample from Mankind Pharma Ltd, VillKyarta, P.O. Misserwal, Poonta Sahib, Sir Mour. H.P. Whereas Prednisolone was purchased from Yarrow chem., Mumbai. It was evaluated for its pre-formulation studies (organoleptic properties, melting point, solubility, compatibility, max. wavelength of absorption). NLCs were prepared through melt-emulsification followed by ultra-sonication technique. Further optimized batch of NLCs was incorporated into Gel. Formulated NLCs were evaluated in terms of morphological characteristics, particle size (Polydispersity Index), drug content, In-vitro drug release (using egg membrane), drug release kinetics (Ritger-Peppas diffusion method). Finally, gel containing NLCs was studied by physical characteristics, pH, viscosity, spreadability, drug content, In-vitro drug release and its kinetics. Results and Discussion: In pre-formulation study, drugs were found having the similar properties as described in Indian Pharmacopoeia (IP) and United States Pharmacopoeia (USP). SEM photomicrograph revealed that NLCs were spherical with more or less smooth surface; particle size 512.3-1703 nm and PDI- 0.399-0.742 (ofloxacin) and particle size 539.3-1736.7 nm and PDI- 0.335 - 0.711 (prednisolone);drug content was found in range of 56.7 - 75.6% for ofloxacin and 65.9 – 81.8% for prednisolone. NLC1 demonstrated maximum release rate with 83.37±1.70% and NLC8 73.96±0.53%.NLC6 was best fitted in Korsmeyer - peppas model as the regression coefficients were 0.960, 0.964, 0.977, 0.950, 0.980 & 0.987 respectively and prednisolone NLC 9 (0.953) and they were close to 1. Conclusion: In conclusion, the prepared NLCs had prolonged release effects with good potential for topical delivery of NLC based gel formulation of ofloxacin& prednisolone.

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