<b>Release of Acetazolamide from Swellable Hydroxypropylmethylcellulose Matrix Tablets</b>

Dortunç, Betül; Gunal, Nesrin

doi:10.3109/03639049709146165

Cited by 15 publications

(11 citation statements)

References 5 publications

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“…However, the percent drug recovery and drug content uniformity results were not reported [8]. Also, quantification of acetazolamide in matrix tablets containing HPMC K4M or K15M was reported, but the quantitative assay method and drug content uniformity results were not reported [9]. A review of the literature indicated that no specific method has been reported for quantification of a lipophilic drug substance contained in HPMC matrix tablets.…”

Section: Introductionmentioning

confidence: 99%

Method to recover a lipophilic drug from hydroxypropyl methylcellulose matrix tablets

2001

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A reverse-phase high-performance liquid chromatographic (HPLC) method for recovery of the lipophilic drug, alprazolam, from matrix tablets containing the hydrophilic polymer hydroxypropyl methylcellulose (HPMC) was developed. Lipophilic drugs, such as alprazolam, are difficult to completely extract and quantitate from tablets containing HPMC polymer. The percentage of recoveries of alprazolam from placebo powder spiked with alprazolam stock solution and from placebo powder mixed with alprazolam powder were about 100% and 85% to 95%, respectively. The validated method using water to completely dissolve HPMC before the addition of a strong solvent to dissolve and extract the drug from the HPMC solution was shown to be the most reproducible method. Different molecular weight distributions of the HPMC polymer, such as HPMC-K4M and HPMC-K100LV, did not influence the dissolution results of alprazolam using this validated method. Similarly, the excipients composing the matrix tablet formulations, such as dicalcium phosphate dihydrate, dicalcium phosphate anhydrous, calcium sulfate dihydrate, sucrose, dextrose, and lactose monohydrate, did not influence the percent recovery of alprazolam. The recovery method reported herein was shown to be the most efficient to achieve complete recovery of alprazolam from powder blends and tablets containing a variety of excipients and different grades of HPMC.

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Section: Introductionmentioning

confidence: 99%

Method to recover a lipophilic drug from hydroxypropyl methylcellulose matrix tablets

2001

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“…An increase in the viscosity of the stagnant layer results in a corresponding decrease in drug release (due to thicker gel layer formation). 24 The dissolution profiles of SR pravastatin tablets were subjected to kinetic modeling. The results are presented in Table 4 and Figures 1-4.…”

Section: Resultsmentioning

confidence: 99%

Statistical Design and Optimization of Sustained Release Formulations of Pravastatin

Gunda¹,

Manchineni²

2020

tjps

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Bu çalışmanın amacı, biyofarmasötik sınıflandırma sistemi III grubunda yer alan lipit düşürücü etkili pravastatinin sürekli salım yapan formülasyonunun geliştirilmesidir. Gereç ve Yöntemler: Pravastatin'in sürekli salım tabletleri, direkt kompresyonla 3 2 faktöryel tasarıma göre çeşitli oranlarda hidroksi metil propil selüloz (HPMC) K4M ve sodyum karboksi metil selüloz kullanılarak hazırlanmıştır. Pravastatin'in uzun süreli salınımını elde etmek için bağımsız değişkenler olarak HPMC K4M (X 1) ve sodyum karboksi metil selüloz (X 2) miktarları; %10, %50, %75 ve %90 ilaç salımı için geçen süreler ise bağımlı değişkenler olarak seçilmiştir. Bulgular: Dokuz formülasyon geliştirilmiş ve bu formülasyonlara farmakopede belirtilen kontrol testleri uygulanmıştır. Sonuçlar geliştirilen tüm formülasyonların standart limit değerler arasında olduğunu göstermiştir. Tüm formülasyonların disolüsyon parametreleri kinetik modellere uygulanarak çeşitli istatistiksel parametreler belirlenmiştir. Polinomiyal denklemler bağımlı değişkenler için geliştirilmiş ve doğrulanmıştır. 25 mg HPMC K4M ve 25 mg sodyum karboksimetil selüloz içeren formülasyondan (F 5) pravastatin salımı, ticari preparatı (Pravachol) ile benzer bulunmuştur (benzerlik faktörü f 2 =89,559; fark faktörü f 1 =1,546). Sonuç: En iyi formülasyonunun (F 5), Higuchi kinetiği, Fick kanununa uymayan difüzyonun sıfırıncı derece kinetiğine (n=0,864) uygun davranış gösterdiği bulunmuştur. Anahtar kelimeler: Pravastatinin, sürekli salım tableti, HPMC K4M, 3 2 faktöriyel tasarım, sıfırıncı derece kinetik, Fick kanununa uymayan difüzyon mekanizması Objectives: The objective of the current study was to formulate a sustained release (SR) formulation for pravastatin. Pravastatin is a lipid lowering, biopharmaceutical classification class-III agent. Materials and Methods: SR tablets of pravastatin were prepared using variable amounts of hydroxy methyl propyl cellulose (HPMC) K4M and sodium carboxy methyl cellulose in various proportions by direct compression in a 3 2 factorial design. The amounts of the polymers HPMC K4M and sodium carboxy methyl cellulose required to obtain prolonged release of drug were chosen as independent variables, X 1 and X 2 , respectively, whereas times taken for 10%, 50%, 75%, and 90% drug release were chosen as dependent variables. Results: Nine formulations were developed and were checked using pharmacopoeial tests. The results showed that all the factorial batches were within the standard limits. The dissolution parameters of all formulations were subjected to kinetic fitting and various statistical parameters were determined. Polynomial equations were developed and verified for dependent variables. Formulation F 5 , containing 25 mg of HPMC K4M and 25 mg of sodium carboxy methyl cellulose, was the formulation most similar (similarity factor f 2 =89.559, difference factor f 1 =1.546) to the marketed product (Pravachol). Conclusion: The best formulation (F 5) follows Higuchi's kinetics and non-Fickian diffusion zero order kinetics (n=1.083).

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“…As we know that viscosity of polymer is inversely proportional to the rate of drug release, variation in the viscosity is due the formation of thicker gel layer in formulation. 18 The In vitro drug release profile of Olmesartan medoxomil SR tablet formulations was subjected to goodness of fit test by linear backward step-wise regression analysis according to kinetic / mathematical models to know the drug release mechanism. Kinetic plots shown in Figure 1-4.…”

Section: Resultsmentioning

confidence: 99%

Design, development, and in vitro evaluation of sustained release tablet formulations of olmesartan medoxomil

Gunda¹

2018

MOJDDT

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Objective: The purpose of present research work is to develop the sustained release formulation for Olmesartan medoxomil using 3 2 factorial design. Olmesartan an Antihypertensive agent, angiotensin-II receptor (type AT1) blocker and BCS class-II agent.Methods: Sustained Release tablets of Olmesartan medoxomil were prepared using different quantities of HPMCK4M and Xanthan Gum in combinations by direct compression technique. The concentration of Polymers, HPMCK4M and Xanthan gum required to achieve the drug release was selected as independent variables, X 1 and X 2 respectively whereas, time required for 10% of drug release (t 10% ), 50% (t 50% ), 75% (t 75% ) and 90% (t 90% ) were selected as dependent variables.Results: Nine formulations were prepared and are evaluated for various pharmacopoeial tests. The results reveals that all formulations were found to be with in the pharmacopoeial limits and In vitro drug release profiles of all formulations were fitted in to various Kinetic models. The statistical parameters like intercept, slope & correlation coefficient were calculated. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations were checked by designing 2 check point formulations (C 1 , C 2 ). Conclusion:According to SUPAC guidelines formulation (F 5 ) containing combination of 15% HPMCK4M and 15% Xanthan gum, is the most identical formulation (similarity factor f 2 = 91.979, dissimilarity factor f 1 = 1.546 & No significant difference, t=0.0338) to marketed product (BENICAR). Best Formulation F 5 follows First order, Higuchi's kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion Anomalous Transport. (n=0.828). Hardness:This was performed by using Monsanto Hardness Tester. The force at which diametric breakage of tablet was occurred noted as hardness. A hardness of about 2-4kg/cm 2 is preferred for mechanical stability. Friability:The test was carried out with the help of Roche friabilator.Design, development, and in vitro evaluation of sustained release tablet formulations of olmesartan medoxomil 166

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Release of Acetazolamide from Swellable Hydroxypropylmethylcellulose Matrix Tablets

Cited by 15 publications

References 5 publications

Method to recover a lipophilic drug from hydroxypropyl methylcellulose matrix tablets

Method to recover a lipophilic drug from hydroxypropyl methylcellulose matrix tablets

Statistical Design and Optimization of Sustained Release Formulations of Pravastatin

Design, development, and in vitro evaluation of sustained release tablet formulations of olmesartan medoxomil

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