scholarly journals Effects of coating on the release profile of drug combination from hydrophilic matrix pellets

1970 ◽  
Vol 2 (2) ◽  
pp. 53-58
Author(s):  
Muhammad Shahidul Islam ◽  
Md Moniruzzaman ◽  
Ruknuzzaman Rony ◽  
Tasnuva Haque
Keyword(s):  
Ascorbic Acid ◽  
Ferrous Sulfate ◽  
Ferrous Sulphate ◽  
Film Coating ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Pharmaceutical Sciences ◽  
Coating Composition ◽  
Pan Coater

In this work zinc sulfate, ferrous sulfate and ascorbic acid was formulated on the same pellet by combination pelletization technique and their and in vitro dissolution studies were performed by using United States Pharmacopoeia (USP) apparatus type II. In addition, effect of different types of polymers, formulation variables and variations in coating composition on the release of drug were studied. The desired release profile for ferrous sulfate was 35% for 1st hour, 45-75% for 2nd hour and 60-85% for third hour and not less than 85% for 4th hour. The release rate controlling polymer used was various concentrations of Methoccel K15M CR with different concentrations of Microcrystalline cellulose (Avicel PH 101). The maximum release percentage of Ferrous Sulphate was obtained from 2.5 % of Methocel K15M CR and 30 % Avicel PH 101 containing pellets (F-4) and it was 92.32%. And the minimum release percentage of Ferrous Sulphate was obtained from 10 % of Methocel K15M CR and 35.7% Avicel PH 101 containing pellets (F-1) and it was 86.36%. The release profile from other formulations containing 35.4% Methocel K 15M CR & 7.5% Avicel (F-2) and 32% Methocel K 15M CR & 4% Avicel (F-3) were also within desired range. The effect of Eudragit coating (enteric) and the presence of PEG and HPMC in the film coating composition on the drug release were also investigated. Hydrophobic matrix pellets prepared using lower concentrations of Methocel K15M CR were found to be best suited for modulating the delivery of the ferrous sulphate from the combination.  Key words: Non Pariel Seeds (NPS); Pan Coater; Ascorbic acid; Methocel K15M CR; Pelletization; PEG; Avicel PH 101; Xanthan gum.DOI: 10.3329/sjps.v2i2.5824Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 53-58

scholarly journals In Vitro Dissolution Evidence for Sustained and Prolonged Release of Vitamin C in a Phosphatidyl Choline-Enriched Lipid Encapsulation

2021 ◽  
Vol 5 (Supplement_2) ◽  
pp. 1328-1328
Author(s):  
Mastaneh Sharafi ◽  
Tyler White ◽  
Kelli Fowler ◽  
Kevin Ewell ◽  
Noe Galvan ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Los Angeles ◽  
Vitamin C ◽  
Phosphatidyl Choline ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Prolonged Release ◽  
Lauryl Sulfate

Abstract Objectives In vitro dissolution tests are valuable first-step tools in the development of bioavailable delivery systems, making it possible to assess the performance of novel technologies in releasing active ingredients through the amount dissolved in a dissolution medium. The objective of this study was to evaluate whether phosphatidyl choline-enriched lipid encapsulation releases the majority of vitamin C as ascorbic acid past the stomach in a standard in vitro dissolution procedure and to assess the release profile. Methods A novel phosphatidyl choline-enriched lipid encapsulation that is solid at room temperature was tested for dissolution in a standard dissolution apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. One serving (included 1000 mg ascorbic acid) was placed into vessels containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.8) for an additional 360 minutes. Aliquots were tested for ascorbic acid concentration at 8 time points by titration. The data was compared with 1000 mg of regular ascorbic acid in a capsule format. Results The phosphatidyl choline-enriched lipid encapsulation released 36% of the vitamin C at 2 hours in the acid phase and released 56% at 3 hours, 67% at 4 hours, 85% at 6 hours and 98% at 8 hours in the intestinal phase. Regular vitamin C filled capsules released 100% of the vitamin C at 30 minutes. Conclusions The dissolution results indicated that phosphatidyl choline-enriched lipid encapsulation can pass the stomach and release the majority of vitamin C in the small intestine. The encapsulation demonstrated a sustained and prolonged release of vitamin C over an 8 hour period. The release profile observed in this in vitro study suggests phosphatidyl choline-enriched lipid encapsulation may improve nutrient absorption and bioavailability which requires further testing including human clinical trials. Funding Sources This study was supported by Lonza (Greenwood, SC) and Ritual (Natals Inc, Los Angeles, CA).

Double Coated Tablets of Nimesulide for Colon Targeting

2010 ◽  
Vol 3 (2) ◽  
pp. 1000-1005
Author(s):  
M S Shaikh
Keyword(s):  
Targeted Drug Delivery ◽  
Film Coating ◽  
In Vitro Dissolution ◽  
In Vitro Drug Release ◽  
Novel Approach ◽  
Eudragit E ◽  
Coating Weight ◽  
Targeted Drug Delivery System

The present study was aimed at developing oral colon targeted drug delivery system for Nimesulide utilizing recently designed and patented system called CODESTM, which consisted of a lactulose containing core overcoated with both Eudragit E and Eudragit L designed to rapidly disintegrate in the colon, in order to give a new life for an existing banned drug. CODESTM tablets were prepared by tabletting Nimesulide and lactulose, followed with film coating of Eudragit. The prepared tablets were evaluated on the basis of in vitro dissolution study and in vivo disintegration study was performed by gamma scintigraphic evaluation in rats. The onset of Nimesulide release was found to dependent on the coating level of Eudragit E, and at Eudragit E coating level of 8% (coating weight gain), the onset of in vitro drug release was found to be optimum. When the same was subjected on scintigraphic evaluation for in vivo disintegration study, there was a reasonable agreement between the in vitro/in vivo data. It is concluded that Nimesulide can be targeted to hindgut by a novel approach of CODESTM.

Formulation and Evaluation of Novel Enteric Coated Extended Release Multiparticulates of Model NSAID Ketoprofen

2010 ◽  
Vol 3 (2) ◽  
pp. 994-999
Author(s):  
Lotlikar V ◽  
S Shidhaye ◽  
U Kedar ◽  
V Kadam
Keyword(s):  
Rheumatoid Arthritis ◽  
Dosage Form ◽  
Extended Release ◽  
In Vitro Dissolution ◽  
Ph Responsive ◽  
Model Drug ◽  
Enteric Coated ◽  
Pan Coater ◽  
Barrier Coat

The aim of this study was to develop a pH responsive enteric coated extended release multiparticulate dosage form containing a model drug ketoprofen, a nonsteroidal anti-inflammatory drug used for rheumatoid arthritis. The drug loaded pellets in matrix form were prepared by using extrusion/spheronization method. The optimized pelletization method revealed that extrusion using 1 mm sieve plate and spheronization friction disc of 2mm carried out at 700 rpm for 5-10 minutes resulted in good spherical pellets and uniformity in size. Evaluated core pellets were coated with polymer Eudragit® RS 30D on Fluid bed coater to achieve a sustainable release for 12 hours. Ketoprofen as like other NSAID have been reported for gastric mucosal irritation so a pH responsive barrier coat of Eudragit L®100-55 was employed on a pan coater for abstaining release in acidic media. The formulated pellets were characterized for shape and size uniformity, friability, surface morphology studies. The particle size of core and polymer coated pellets were found to be in the range of 0.95-1.2 mm and 1.32-1.51 mm respectively. The pellets were spherical in shape with smooth texture and uniformity in size. In-vitro dissolution tests were carried out for pellets in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the ketoprofen from formulated pellets was established in pH 1.2 for a period of 2 h, followed by pH 7.5 for rest of the study. The study concluded that the formulated multiparticulate dosage form of ketoprofen was able to relieve symptoms of rheumatoid arthritis.

Formulation Development of Metoprolol Succinate Controlled Release Tablets using Ethyl-cellulose-polyvinyl-pyrrolidone Coating

2015 ◽  
Vol 8 (2) ◽  
pp. 2851-2857
Author(s):  
Kiran Kumar Vangara ◽  
Kishore K. Konda ◽  
Shiva K. Ravula ◽  
Pradeep K Vuppala ◽  
Vijay K. Sripuram ◽  
...  
Keyword(s):  
Weight Gain ◽  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Film Coating ◽  
Release Profile ◽  
Water Soluble ◽  
Metoprolol Succinate ◽  
Water Soluble Drug

It is challenging to develop a controlled release (CR) formulation for a freely water soluble drug molecule without using rate controlling polymers in the core matrix. This study is aimed to develop and evaluate cost-effective ethyl cellulose (EC)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet. Simple core tables of MS were compressed and coated with a solution composed of hydrophobic rate controlling polymer, EC and water soluble pore forming polymer, PVP. The effect of formulation parameters such as the ratio of EC to PVP and tablet coating weight gain on the in-vitro drug release were evaluated. Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed release profile was calculated.It was observed that drug release rate increased with a decrease in the ratio of ethyl cellulose to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with EC and PVP at a ratio of 60:40 %w/w and 9% weight gain showed matching release profile to marketed tablet with f2 value of 72.25. The optimized formulation showed pH independent in-vitro release. This study successfully demonstrated that EC-PVP film coating can effectively control the release rate of freely soluble drugs. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed tablet was developed.  

scholarly journals Nanoparticle-Based Rifampicin Delivery System Development

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 2067
Author(s):  
Marjan Motiei ◽  
Luis Pleno de Gouveia ◽  
Tomáš Šopík ◽  
Robert Vícha ◽  
David Škoda ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Physicochemical Properties ◽  
Protective Effect ◽  
Chronic Wounds ◽  
System Development ◽  
Release Profile ◽  
New Drugs ◽  
Alkaline Ph ◽  
Ft Ir

The alkaline milieu of chronic wounds severely impairs the therapeutic effect of antibiotics, such as rifampicin; as such, the development of new drugs, or the smart delivery of existing drugs, is required. Herein, two innovative polyelectrolyte nanoparticles (PENs), composed of an amphiphilic chitosan core and a polycationic shell, were synthesized at alkaline pH, and in vitro performances were assessed by 1H NMR, elemental analysis, FT-IR, XRD, DSC, DLS, SEM, TEM, UV/Vis spectrophotometry, and HPLC. According to the results, the nanostructures exhibited different morphologies but similar physicochemical properties and release profiles. It was also hypothesized that the simultaneous use of the nanosystem and an antioxidant could be therapeutically beneficial. Therefore, the simultaneous effects of ascorbic acid and PENs were evaluated on the release profile and degradation of rifampicin, in which the results confirmed their synergistic protective effect at pH 8.5, as opposed to pH 7.4. Overall, this study highlighted the benefits of nanoparticulate development in the presence of antioxidants, at alkaline pH, as an efficient approach for decreasing rifampicin degradation.

Optimization and In-vitro Evaluation of Coating Process for Film-Coated Tablets

2017 ◽  
Vol 13 (11) ◽  
Author(s):  
Marwan Abdelmahmoud Abdelkarim Maki ◽  
Palanirajan Vijayaraj kumar ◽  
Yeong Siew Wei
Keyword(s):  
Weight Gain ◽  
Scale Up ◽  
Film Coating ◽  
Inlet Temperature ◽  
Coating Process ◽  
Coating Quality ◽  
Tablet Coating ◽  
Spray Rate ◽  
Pan Coater

AbstractThe proper efficiency of the tablet-coating process often results in a coating within adequate quality, which might avoid the rejection of the film-coated tablets, minimize the operating expenses and production time. In general, the optimum coating system performance and coating conditions are important for achieving the desirable tablet-coating uniformity and manufacturing reproducibility. In this study, HPMC-aqueous-based tablet film coating successfully conducted in a perforated pan coater for process scale-up using the spray-coating technique. Certain process parameters such as spray rate, inlet air temperature, pan temperature, atomizing pressure as well as pan speed were maintained carefully and the optimum coating quality was achieved with acceptable film performance. At lower initial pan speed, the strength of the coated tablets was remarkably improved and the highest weight gain obtained. The smoothest and uniform film obtained at high spray rate, high pan speed, and low atomizing pressure. The results revealed that the optimum film-coating quality and uniformity achieved at a spray rate of 480 ml/min, atomizing pressure at 5 bar, inlet temperature at 85 to 90 °C, pan temperature at 58 °C, initial pan speed at 1.5 rpm and final pan speed at 4.0 rpm using side-vented pan coater. At initial pan speed of 1.5 rpm, the strength of the coated tablets remarkably improved with minimum edges erosion, which increases the weight gain up to 3.3%w/w.

scholarly journals Comparative Dissolution Study of Different Brands of Amoxicillin Trihydrate Capsules Available in Bangladesh

1970 ◽  
Vol 2 (2) ◽  
pp. 72-75 ◽  
Author(s):  
Naz Hasan Huda ◽  
Yeakuty Marzan Jhanker ◽  
AFM Shahid-Ud-Daula ◽  
Most Nazma Parvin ◽  
Shammy Sarwar
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Pharmaceutical Sciences ◽  
National Brand ◽  
National Brands ◽  
Time Period ◽  
Amoxicillin Trihydrate ◽  
Dissolution Apparatus ◽  
Comparative Dissolution

Commercially available twenty national and four multinational brands of Amoxicillin Trihydrate capsules werestudied  in water  for 60 minutes using USP reference dissolution apparatus. All, except  two national brands(Code: NB-8 and NB-15); complied with  the USP  in vitro dissolution specification  for drug release (not  lessthan 80% of the labelled amount of amoxicillin trihydrate should be dissolved in 60 minutes). Drug releasesfrom those two brands were 75% and 67% respectively within the specified time period. Key words: In vitro Dissolution; Market preparations; Amoxicillin Trihydrate; Capsule; National Brand;Multinational Brand.DOI: 10.3329/sjps.v2i2.5827Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 72-75

scholarly journals Developing Clinically Relevant Dissolution Specifications for Oral Drug Products—Industrial and Regulatory Perspectives

Pharmaceutics ◽  
2019 ◽  
Vol 12 (1) ◽  
pp. 19 ◽  
Author(s):  
Mark McAllister ◽  
Talia Flanagan ◽  
Karin Boon ◽  
Xavier Pepin ◽  
Christophe Tistaert ◽  
...  
Keyword(s):  
In Vitro Dissolution ◽  
Oral Drug ◽  
Regulatory Agencies ◽  
Pharmaceutical Sciences ◽  
Drug Products ◽  
Future Developments ◽  
In Silico Modeling ◽  
Regulatory Sciences ◽  
Key Questions

A meeting that was organized by the Academy of Pharmaceutical Sciences Biopharmaceutics and Regulatory Sciences focus groups focused on the challenges of Developing Clinically Relevant Dissolution Specifications (CRDS) for Oral Drug Products. Industrial Scientists that were involved in product development shared their experiences with in vitro dissolution and in silico modeling approaches to establish clinically relevant dissolution specifications. The regulators shared their perspectives on the acceptability of these different strategies for the development of acceptable specifications. The meeting also reviewed several collaborative initiatives that were relevant to regulatory biopharmaceutics. Following the scientific presentations, a roundtable session provided an opportunity for delegates to discuss the information that was shared during the presentations, debate key questions, and propose strategies to make progress in this critical area of regulatory biopharmaceutics. It was evident from the presentations and subsequent discussions that progress continues to be made with approaches to establish robust CRDS. Further dialogue between industry and regulatory agencies greatly assisted future developments and key areas for focused discussions on CRDS were identified.

scholarly journals Improvement of the Bioavailability and Glycaemic Metabolism of Cinnamon Oil in Rats by Liquid Loadable Tablets

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Chunchao Han ◽  
Bo Cui
Keyword(s):  
Insulin Secretion ◽  
Blood Glucose ◽  
Plasma Concentration ◽  
Time Profile ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Parameters ◽  
Cinnamon Oil ◽  
Concentration Time

The purpose of this study is to investigate the bioavailability and glycaemic metabolism of cinnamon oil (CIO) carried by liquid-loadable tablets (CIO-LLTs), the carrier of a CIO self-emulsifying formulation (CIO-LS). The results of tests performed to evaluate the physical properties of the CIO-LLT complied with Chinese Pharmacopeia (2010). The release profile suggested that the CIO-LLT preserved the enhancement of in vitro dissolution of cio. After orally administration, the plasma concentration-time profile and pharmacokinetic parameters suggested that a significant increase (P<0.0001) in theCmax, AUC andFwere observed in the CIO-LLT. The blood glucose and the HbA1c were significantly decreased in alloxan-induced hyperglycemic rats (P<0.05,P<0.01, resp.), while the level of insulin secretion was markedly elevated in alloxan-induced hyperglycemic rats (P<0.05). The alloxan-damaged pancreaticβ-cells of the rats were partly recovered gradually after the rats were administered with CIO-LLT 45 days later. CIO-LLT could improve the bioavailability and glycaemic metabolism of CIO.

Electrosprayed PVP/Shellac Composite Medicated Microparticles for Providing Biphasic Drug Release Profile

2014 ◽  
Vol 633-634 ◽  
pp. 562-566
Author(s):  
Yong Hui Wu ◽  
Deng Guang Yu ◽  
Qian Su ◽  
Cheng Lei Cai ◽  
Ji An Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Average Diameter ◽  
Release Profile ◽  
Vinyl Pyrrolidone ◽  
In Vitro Dissolution ◽  
Hydrophilic Polymer ◽  
Drug Release Profile ◽  
Poly Vinyl Pyrrolidone

The present study reports that a sustained release profile could be transferred into a biphasic drug release profile when a hydrophilic polymer was encapsulated into the medicated microparticles. The multiple component composite microparticles were fabricated using a single fluid electrospraying process to treat a co-dissolving solution consisting of a polymer matrix (shellac), an active ingredient (FA), and an additional hydrophilic polymer (poly vinyl pyrrolidone, PVP). FESEM results showed that the microparticles M1 consisting of shellac and FA had an average diameter of 1.27 ± 0.38 μm, whereas the microparticles M2 consisting of shellac, FA and PVP had an average diameter of 1.51 ± 0.34 μm. Both the two types of microparticles were essentially amorphous composites due to the favourable secondary interactions between the components, as demonstrated by ATR-FTIR tests. In vitro dissolution tests demonstrated that the addition of PVP in the microparticles M2 made them give a typical biphasic drug release profile, whereas the double-component microparticles provided a sustained release profile. This study shows a simple way for developing advanced drug delivery systems through tailoring the components of polymer excipients using electrospraying.

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