Development of Prolonged Delivery of Tramadol and Dissolution Translation by Statistical Data Treatment

2011 ◽  
Vol 4 (1) ◽  
pp. 1331-1337
Author(s):  
P B Parejiya ◽  
B S Barot ◽  
P K Shelat
Keyword(s):  
Drug Release ◽  
Study Data ◽  
Stability Study ◽  
Dissolution Time ◽  
Matrix Tablet ◽  
Burst Effect ◽  
The Matrix ◽  
The Mean ◽  
The Difference ◽  
Dissolution Efficiency

The present study was carried out to fabricate a prolonged design for tramadol using Kollidon SR (Polyvinyl acetate and povidone based matrix retarding polymer). Matrix tablet formulations were prepared by direct compression of Kollidon SR of a varying proportion with a fixed percentage of tramadol. Tablets containing a 1:0.5 (Drug: Kollidon SR) ratio exhibited a rapid rate of drug release with an initial burst effect. Incorporation of more Kollidon SR in the matrix tablet extended the release of drug with subsequent minimization of the burst effect as confirmed by the mean dissolution time, dissolution efficiency and f2 value. Among the formulation batches, a direct relationship was obtained between release rate and the percentage of Kollidon SR used. The formulation showed close resemblance to the commercial product Contramal and compliance with USP specification. The results were explored and explained by the difference of micromeritic characteristics of the polymers and blend of drug with excipients. Insignificant effects of various factors, e.g. pH of dissolution media, ionic strength, speed of paddle were found on the drug release from Kollidon-SR matrix. The formulation followed the Higuchi kinetic model of drug release. Stability study data indicated stable character of Batch T6 after short-term stability study.

Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

<p>Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>

Colon targeting oral matrix tablets of mesalamine: Design, development and invitro evaluation

2020 ◽  
Vol 10 (1) ◽  
pp. 18-27
Author(s):  
Audinarayana N ◽  
Anala Srinivasulu ◽  
Vellore Sruthikumari ◽  
Likitha ◽  
Ananda Deepak V
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Stability Study ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Matrix Tablet ◽  
Cellulose Acetate Phthalate ◽  
Design Development ◽  
Release Pattern ◽  
The Matrix

The principle in this present research is to formulate Mesalamine containing colon targeted tablets by using different polymers and evaluate the effect of different polymers in drug release pattern. The matrix tablets of Mesalamine are formulated by polysaccharides based polymers like Cellulose acetate phthalate (CAP), Ethyl cellulose (EC), Guar gum (GG) and Xanthan gum (XG) which protects the drug to release in Stomach and Small Intestine. The invitro drug dissolution investigation of F2 (GG and XG) Matrix tablet was controlled by swelling into a viscous gel in colonic pH, which have been accomplished as the best tablet. The optimized tablet F2 was found to be stable in stability study (short term) with reproducible evaluation data, which also shows the highest swelling index, increased viscosity in colonic pH. The drug release pattern from the F2 formulation follows swelling and erosion behavior. From the data it show that F2 tablets suitable for providing colon targeted drug delivery.

scholarly journals Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186-192 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.DOI: http://dx.doi.org/10.3329/icpj.v1i8.11248 International Current Pharmaceutical Journal 2012, 1(8): 186-192 

scholarly journals Development and evaluation of sustained release losartan potassium matrix tablet using kollidon SR as release retardant

2012 ◽  
Vol 48 (4) ◽  
pp. 621-628 ◽  
Author(s):  
Shahid Sarwar ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.

scholarly journals Formulation, Optimization, and Characterization of Repaglinide Loaded Nanocrystal for Diabetes Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Gajanan Shinde ◽  
Mitesh Patel ◽  
Manan Mehta ◽  
Rajesh Kesarla ◽  
Ganesh Bangale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymer Concentration ◽  
Study Data ◽  
Stability Study ◽  
Diabetes Therapy ◽  
Peg 4000 ◽  
Number Of Cycles

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

Deconvolution Analysis of Renograms Obtained with Simultaneously Administered 99mTc-DTPAand 131l-Hippuran

1988 ◽  
Vol 27 (05) ◽  
pp. 188-194 ◽  
Author(s):  
V. Kempi
Keyword(s):  
Ureteral Obstruction ◽  
Mean Transit Time ◽  
Retention Function ◽  
Renal Handling ◽  
Deconvolution Analysis ◽  
Transit Times ◽  
The Matrix ◽  
Absolute Amplitude ◽  
The Mean ◽  
The Difference

Seventy patients were studied with a dual radionuclide technique. The conventional renograms and the blood curve were subjected to deconvolution analysis using the matrix algorithm method, and the following curve data calculated from the retention functions: absolute and relative amplitudes, minimum time of the retention function, maximum time of the retention function and mean transit time. The findings with the two radiopharmaceuticals 99mTc-DTPA and 131l-Hippuran were compared under normal and pathological conditions. The correlations between the data with 99mTc-DTPA and those with 131l-Hippuran were highly significant (p <0.01). So was the correlation between the absolute amplitude of the retention curve and the rate of uptake based on the corresponding renogram (p <0.01). Due to the difference in the renal handling of the two tracers, longer maximum times were obtained with 99mTc-DTPA. The mean transit times were also longer with 99mTc-DTPA, except in kidneys with parenchymal insufficiency. The highest amplitudes were found in normal kidneys, while the lowest values were observed in parenchymal insufficiency. In the group with acute ureteral obstruction, the mean transit times tended to be increased. The maximum times were even more increased. With both tracers it is possible to distinguish between the three groups of renal conditions studied here: Normal, parenchymal insufficiency, and acute ureteral obstruction.

scholarly journals FORMULATION AND EVALUATION OF SYNTHESIZED QUINAZOLINONE DERIVATIVE FOR COLON SPECIFIC DRUG DELIVERY

2017 ◽  
Vol 10 (3) ◽  
pp. 207
Author(s):  
Vidya Viswanad ◽  
Shammika P ◽  
Aneesh Tp
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Site Specific ◽  
The Matrix

ABSTRACTObjective: The current research deals with the formulation and evaluation of synthesized quinazolinone derivative for colon site specific delivery.Methods: The synthesized quinazolinone derivative was enteric coated 5% Eudragit L-100 with by wet granulation method using guar gum, pectin,and guar gum pectin combination as hydrophilic polymer. The prepared matrix tablet was characterized by differential scanning calorimetry andevaluated for different pre-compression and post-compression studies and drug release profiles.Results: All the matrix tablets were within the range of pharmacopeial limits with better flow properties. All the six formulations of matrix tablets haddisintegrated within 5-6 minutes. The optimized formulation selected was F6 formulation combination of guar gum and pectin with 95.79% of drugrelease than compared to the remaining formulation. The optimized matrix tablets followed zero order kinetics with Fickian diffusion.Conclusion: The results proposed that the combination of guar gum and pectin coated tablet with 5% Eudragit L-100 of synthesized quinazolinonederivative is a promising colon site specific delivery.Keywords: Quinazolinone derivative, In vitro drug release, Disintegration time, Guar gum, Pectin, 5% Eudragit L-100, Colon site-specific delivery, Wetgranulation, Compression.

scholarly journals Chitosan inserts for periodontitis: Influence of drug loading, plasticizer and crosslinking on in vitro metronidazole release

2007 ◽  
Vol 57 (4) ◽  
pp. 469-477 ◽  
Author(s):  
Romi Barat ◽  
Anegundha Srinatha ◽  
Jayanta Pandit ◽  
Shampa Anupurba ◽  
Neelam Mittal
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Dissolution Time ◽  
Cross Linking ◽  
Burst Release ◽  
Casting Method ◽  
The Mean ◽  
Polymer Ratio

Chitosan inserts for periodontitis: Influence of drug loading, plasticizer and crosslinking onin vitrometronidazole releaseChitosan based metronidazole (MZ) inserts were fabricated by the casting method and characterized with respect to mass and thickness uniformity, metronidazole loading andin vitrometronidazole release kinetics. The fabricated inserts exhibited satisfactory physical characteristics. The mass of inserts was in the range of 5.63 ± 0.42 to 6.04 ± 0.89 mg. The thickness ranged from 0.46 ± 0.06 to 0.49 ± 0.08 mm. Metronidazole loading was in the range of 0.98 ± 0.09 to 1.07 ± 0.07 mg except for batch CM3 with MZ loading of 2.01 ± 0.08 mg. The inserts exhibited an initial burst release at the end of 24 h, irrespective of the drug to polymer ratio, plasticizer content or cross-linking. However, further drug release was sustained over the next 6 days. Cross-linking with 10% (m/m) of glutaraldehyde inhibited the burst release by ~30% and increased the mean dissolution time (MDT) from 0.67 to 8.59 days. The decrease in drug release was a result of reduced permeability of chitosan due to cross-linking.

scholarly journals Acute kidney injury following supine mini-PNL versus retrograde intrarenal surgery in patients with renal stones < 3 cm: a prospective comparative study

2020 ◽  
Vol 26 (1) ◽  
Author(s):  
Metin Yığman ◽  
Semih Tangal ◽  
Tuba Candar ◽  
Mehmet İlker Gökçe
Keyword(s):  
Acute Kidney Injury ◽  
Kidney Injury ◽  
Renal Stones ◽  
Primary Treatment ◽  
Study Data ◽  
Complication Rates ◽  
Duration Of Hospitalization ◽  
Prospective Comparative Study ◽  
The Mean ◽  
The Difference

Abstract Background The purpose of the current study was to prospectively compare mini-PNL and RIRS for development of acute kidney injury (AKI), success, and complication rates in a cohort of patients with kidney stones less than 3 cm. Methods In this prospective study, data of 60 consecutive patients underwent mini-PNL (n = 31) or RIRS (n = 29) was investigated. Urinary NGAL levels were measured preoperatively and at postoperative 6th hour to evaluate AKI. Success and complication rates were also compared. Results The mean stone size was significantly higher in the mini-PNL group (24.6 mm vs. 18.2 mm, p = 0.02). The mean postoperative NGAL levels were 45.6 ± 12.4 and 48.1 ± 13.6 for the mini-PNL and RIRS groups, respectively. The increase was statistically significant for both groups (p: 0.01). The difference between the two groups for mean postoperative NGAL measurements was not statistically significant (p = 0.47). The SFR was significantly higher in the mini-PNL group (96.7% vs. 79.3%, p = 0.04). The complication rates were similar for the two groups (p = 0.99). The mean duration of operation was 48.2 ± 22.5 min in the mini-PNL group and 62.6 ± 18.1 min in the RIRS group (p = 0.03). The median duration of hospitalization was 1 day for both groups. Conclusions In patients with renal stones < 3 cm in diameter, mini-PNL in supine position provides higher SFR and shorter operative times with similar rates of complications and AKI when compared with RIRS. Mini-PNL should be considered as the primary treatment option together with RIRS for renal stones and should not be ruled out for being a more invasive option.

scholarly journals Formulation and characterization of choline fenofibrate sustained release capsule

2018 ◽  
Vol 8 (6-s) ◽  
pp. 251-254
Author(s):  
Nidhi Jain ◽  
Rohit Jain ◽  
Surendra Dangi
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Smooth Surface ◽  
Stability Study ◽  
Matrix Tablet ◽  
Fenofibric Acid ◽  
Dry Granulation ◽  
Regular Shape

The drug ABT-335 (Fenofibricacid ) choline fenofibrate found to be useful in the treatment of dyslipidemia as compare with other fibrate. So the present investigation to developed mini-tablets to overcome the dose dumping problem by regular shape, uniformity, smooth surface excellent size and encapsulated in capsule to improve the efficacy and bioavailability of the drug. Different formulations were developed by utilizingcontrolling of the release rate and gel forming polymers like microcrystalline cellulose, hypromellose by dry granulation technique. Among all formulation SRM-3 having the drug release for longer period of time as compare to other formulation. SRM-3 was found to be stable during stability study for one month. Keywords: ABT-335 (Fenofibric acid) choline fenofibrate, like microcrystalline cellulose, hypromellose, sustained release matrix tablet.

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