scholarly journals Formulation and Evaluation of Release Kinetics of Diltiazem Hydrochloride from Kollicoat SR 30 D Coated Pellets Prepared by Air Suspension Technique

1970 ◽  
Vol 43 (3) ◽  
pp. 321-332
Author(s):  
Afsana Akhter ◽  
Monzurul Amin Roni ◽  
Mohammad Shahriarul Absar ◽  
Golam Kibria ◽  
Reza-ul Jalil

The purpose of the present study is to investigate the effect of polyvinyl acetate on the release kinetics of diltiazem hydrochloride from coated pellets prepared by solution and suspension layering technique. Kollicoat SR 30 D, an aqueous dispersion of polyvinyl acetate with different weight ratios was chosen to sustain the release of the drug. Drug was loaded with hydroxypropyl methyl cellulose on nonpareil seeds then coated with the Kollicoat SR 30 D. In vitro dissolution studies were carried out using USP dissolution apparatus Type-2. No significant difference was found in drug release from uncoated pellets and the pellets coated with 5% polymer load. With 10% polymer load, the initial release was minimized but from 2nd hour the release was quick-tempered. Better sustaining effect was found from 15- 20% polymer loaded pellets. The mean dissolution time was 2.5h and 4h while the polymer load was 15% and 20% respectively. Also these two cases 80% drug was released at 6h and 9h respectively. The physical parameters of the prepared pellets were also compared in this study. The release of drug from the coated pellets appeared to follow Higuchi's release kinetics.Key words: Diltiazem, Pellets, Kollicoat SR 30 D, Aqueous coating, Physical parameters, Release kinetics.DOI = 10.3329/bjsir.v43i3.1147Bangladesh J. Sci. Ind. Res. 43(3), 321-332, 2008

Author(s):  
Dumpeti Janardhan ◽  
Sreekanth Joginapally ◽  
Bharat V. ◽  
Rama Subramaniyan P.

The purpose of this investigation was to prepare a gastroretentive drug delivery system of Ofloxacin. Ofloxacin is a fluoroquinolone antibacterial which acts by inhibiting the topoisomerase enzyme which is essential in the reproduction of the bacterial DNA. It is highly soluble in acidic media and precipitates in alkaline media thereby losing its solubility. Hence, a gastroretentive system was developed to enhance the bioavailability by retaining it in the acidic environment of the stomach. Different formulations were formulated using various concentrations of hydroxy propyl methyl cellulose, sodium carboxy methyl cellulose, sodium bicarbonate and citric acid. The formulations were evaluated for quality control tests and all the physical parameters evaluated are within the acceptable limits of Indian Pharmacopoeia. All the formulations were subjected to in-vitro dissolution studies and compared with the marketed formulation. The floating lag time was below 15 seconds for all the formulations except F1 and F2. The floating duration was found to be more than 24 hours in all except F1, F2 and F10. Formulations F7 and F8 were used to study the effect of sodium bicarbonate and formulations F9 and F10 for the effect of hardness on the drug release. Drug release kinetics was studied for prepared formulations and optimized formulation F5 was found to follow zero order kinetics with r2 =0.993. The statistical analysis of the parameters of dissolution data obtained before and after storage for 3 months at 25°C/ 60%RH and 40°C/75%RH showed no significant change indicating the two dissolution profiles were similar.


2002 ◽  
Vol 70 (2) ◽  
pp. 189-198
Author(s):  
Genç Lütfi ◽  
Hegazy Nahed ◽  
Arica Betül

Matrix tablets of ketorolac trometharnine (KT) were prepared by direct compression technique and Carbopol 934, 940 and 1342 have been used as polymers in different concentrations (5-15 % ). For the quality control of tablets; physical tests as crushing strength, diameter-height ratio and fkiability, KT amount assay and in vitro dissolution techniques were performed and dissolution profiles were plotted and evaluated kinetically. The in vitro release kinetics of ten different formulations of KT matrix tablet were studied at pH 1.2 and pH 7.0 using the USP dissolution technique and apparatus with basket assembly. Dissolution results were evaluated kinetically and statistically. According to our results, different types and concentrations of carbopol to tablet formulations may effect in controlled drug release.


Drug Research ◽  
2017 ◽  
Vol 67 (07) ◽  
pp. 412-418 ◽  
Author(s):  
Arun Reddy ◽  
Narendar Reddy

AbstractClarithromycin (CM), a broad spectrum macrolide antibiotic used to eradicate H. pylori in peptic ulcer. Clarithromycin (CM) is well absorbed from the gastrointestinal tract, but has a bioavailability of 50% due to rapid biodegradation. The aim of this investigation was to increase the gastric residence time, and to control the drug release of clarithromycin by formulating into multiple unit floating mini-tablets. Floating tablets were prepared by using direct compression method with HPMC K4M and Polyox WSR 1105 as release retarded polymers and sodium bicarbonate as gas generating agent. The prepared mini-tablets were evaluated for thickness, weight variation, friability, hardness, drug content, in vitro buoyancy, swelling studies, in vitro dissolution studies by using modified Rossett-Rice test and in vivo radiographic studies in healthy human volunteers in fasting conditions. DSC analysis revealed that no interaction between drug and excipients. All the physical parameters of the tablets were within the acceptable limits. The optimized formulation (F6) had showed controlled drug release of 99.16±3.22% in 12 h, by zero-order release kinetics, along with floating lag time of 9.5±1.28 s and total floating time of 12±0.14 h. X-ray imaging studies revealed that in vivo gastric residence time of clarithromycin floating mini-tablet in the stomach was about 3.5 h. The results demonstrated that the developed floating mini-tablets of clarithromycin caused significant enhancement in gastric retention time along with sustained effect and increased oral bioavailability.


2012 ◽  
Vol 11 (1) ◽  
pp. 37-43 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Madhabi Lata Shuma ◽  
Abu Shara Shamsur Rouf

The objective of the present study was to develop a once-daily sustained release matrix tablet of Aceclofenac using hydroxypropyl methyl cellulose (Methocel K 100M CR) as release controlling factor and to  evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct  compression method. The powder blends were evaluated for angle of repose, loose bulk density, tapped bulk density,  compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 24  hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus in phosphate buffer (pH 7.4). The powder blends showed satisfactory flow properties, compressibility index and drug content etc. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-3 (40% Methocel K100M CR of total weight of tablet) could extend the drug release up to 24 hours and the total release pattern was very close to the theoretical release profile. By comparing the dissolution profiles with the originator brand of Arrestin SR, the formulation F-3 exhibited drug release profile like originator brand. From this study, a decrease in release kinetics of the drug was observed by  increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which  was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion  mechanism in all cases. The drug release from the formulation (F-3) was satisfactory after 3 months storage in 400C  and 75% RH. Besides, this study explored both of the optimum concentration and effect of polymer(s) on  Aceclofenac release pattern from the tablet matrix for 24 hour period. The matrix tablet of Aceclofenac using HPMC  with molecular weight of K100M controlled the drug release effectively for 24 hours; hence the formulation can be  considered as a once daily sustained release tablet of Aceclofenac in order to improve patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12485 Dhaka Univ. J. Pharm. Sci. 11(1): 37-43, 2012 (June)


2009 ◽  
Vol 59 (3) ◽  
pp. 313-323 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Ch. Patra ◽  
V. Patro ◽  
...  

Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.


1970 ◽  
Vol 7 (1) ◽  
pp. 39-45 ◽  
Author(s):  
Bishyajit Kumar Biswas ◽  
Md Safiqul Islam ◽  
Farida Begum ◽  
Abu Shara Shamsur Rouf

In the present study esomeprazole sustained release tablet matrix was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K15M & Methocel K100 LVCR by direct compression method. Different amount of Methocel K15M was used to develop matrix builder in the seven proposed formulations (F1-F7) for the study of release rate retardant effect at 20%, 25%, 30%, 35%, 40%, 45% and 50% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for first two hours and then in the simulated intestinal medium (pH 6.8) for 8 hours using USP dissolution apparatus II. The formulation F-5 (40%) and F-6 (45%) met the optimum release rate of esomeprazole for 10h period of in vitro dissolution study. The release kinetics of formulation F-5 and F-6 very closely followed Higuchi kinetic order than first order and zero order kinetics. Similarly Methocel K100 LVCR was used to develop matrix builder in another seven proposed formulations (F8-F14). It was found that formulations F-11 (35%), F-12 (40%) and F-13 (45%) met the desired release rate of esomeprazole for 10h period. The release kinetics of formulation F-11, F-12 and F-13 followed Higuchi kinetic order. Between these two polymers, Methocel K100 LVCR showed better release retardant effect than Methocel K15M. Key words: Esomeprazole, Direct compression, Controlled release, Methocel K15M and Methocel K100 LVCRDOI = 10.3329/dujps.v7i1.1216 Dhaka Univ. J. Pharm. Sci. 7(1): 39-45, 2008 (June)  


2013 ◽  
Vol 2 (2) ◽  
pp. 70-79
Author(s):  
Umme Rahela ◽  
Md Mizanur Rahman Moghal ◽  
Sayed Masudur Rahman Dewan ◽  
Mohammad Nurul Amin

The present study was designed to evaluate the polymeric effect of METHOCEL K15MCR on the sustained release drug product of Carvedilol. Carvedilol matrix tablets were formulated by direct compression method using METHOCEL K15MCR polymer in various percentages. Physical parameters were tested and the dissolution procedure was performed by using USP (II) paddle method for eight hours to examine the release kinetics. In the study, METHOCEL K15MCR polymer was found to cause the strong retardation of the drug release. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer-Peppas equations. In the context, it can be suggested with a satisfactory result that this sustained release Carvedilol tablets can be marketed to treat patient ensuring proper healthcare. DOI: http://dx.doi.org/10.3329/ijpls.v2i2.15452 International Journal of Pharmaceutical and Life Sciences Vol.2(2) 2013: 70-79


Author(s):  
SALMA AULIA ◽  
LINA WINARTI ◽  
YUDI WICAKSONO

Objective: This study aimed to find the best SNEDDS meloxicam formula and analyze the release kinetics of meloxicam SNEDDS and non-SNEDDS using DDSolver.  Methods: Meloxicam SNEDDS was prepared using sunflower seed oil, Cremophor RH 40 as a surfactant, and polyethylene glycol (PEG) 400 as a co-surfactant.  Results: The best formula obtained subjected to the in vitro dissolution study was analyzed using DDSolver. The study shows one selected formula consists of 10% sunflower seed oil, 70% cremophor RH 40, and 20% PEG 400 with a 20.5 nm±12 nm droplet size. The dissolution study showed that SNEDDS could significantly increase the meloxicam release compared to the non-SNEDDS formulation. The kinetics of meloxicam release from SNEDDS formulations follow the Weibull release model (β = 1.00).  Conclusion: This study concludes that SNEDDS best prepared in sunflower seeds oil: Chremophor RH 40: PEG 400 ratio of 1: 7: 2 and has the potency to increase the solubility and dissolution of meloxicam.


1970 ◽  
Vol 6 (2) ◽  
pp. 87-92
Author(s):  
Golam Kibria ◽  
Reza-ul Jalil

In the present study an attempt has been made to investigate the effect of ethylcellulose as a rate retarding material to sustain the release of diltiazem hydrochloride from pellets prepared by air suspension technique. Aqueous ethylcellulose dispersion (Surelease) with different weight ratios was chosen to sustain the release of the drug. Drug was loaded on dummy seeds by following matrix system as well as barrier coating system. The comparative study of this two manufacturing processes was also the goal of this study. In vitro dissolution studies were carried out using USP dissolution apparatus Type-2. The release of drug was faster from matrix system than that of barrier coating system. About 100% drug was released within 3 hours with 5% polymer load from both systems. While the polymer content was 10%, about 4h & 7h required for 50% & 80% drug release respectively from barrier coating system. The effect of ethylcellulose on the release of diltiazem hydrochloride was found to be predominant in barrier coating system than that of the matrix system. In the matrix system the drug comes to dissolution media easily and water soluble additives form channel very fast. The kinetic study of the drug was performed and it was revealed that the release of drug from pellets appeared to follow zero order kinetics. Key words: Diltiazem; Pellets; Pseudolatex; Aqueous coating; Manufacturing process; Release kinetics. Dhaka Univ. J. Pharm. Sci. 6(2): 87-92, 2007 (December)


Author(s):  
Narayana R. Padala ◽  
Prakash K. ◽  
C. S. Reddy Bonepally ◽  
Krishnaveni B. ◽  
Shantakumari K. ◽  
...  

The objective of the present study was to prepare and characterize the microcapsules for the controlled release of Stavudine using cellulose acetate butyrate (CAB), ethyl cellulose (EC), hydroxy propyl methyl cellulose phthalate (HPMCP). The microcapsules were prepared by solvent evaporation method using acetone and liquid paraffin as a drug dispersion and liquid manufacturing phase, respectively. The prepared microcapsules were characterized for particle size distribution (PSD), percent drug content, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared microcapsules were filled in hard gelatin capsules and kept for accelerated stability study as per ICH guidelines for about 3 months. The prepared microcapsules were spherical and free flowing. The entrapment efficiency was found to be 25-45%. The release of drug from the microcapsules was extended upto 12 hours and more. FTIR and DSC thermo graphs showed stable character of stavudine. Scanning electron microscopic study revealed that then microcapsules were spherical and porous in nature. The release kinetics study revealed that the prepared microcapsules were best fitted to the Higuchi model, first order and followed by Zero order and indicating that the drug release was diffusion controlled. The release was mainly influenced by the type of polymer and its viscosity. The DSC study revealed that there is no drug to polymer interaction and showed the stable character of the drug which was further confirmed by the assay of accelerated stability of microcapsules.


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