scholarly journals PENGARUH MATRIKS PEKTIN DAN HPMC K15M TERHADAP DAYA MENGAPUNG DAN MENGEMBANG SERTA DISOLUSI PADA TABLET FLOATING VERAPAMIL HCl DENGAN METODE FACTORIAL DESIGN

2020 ◽  
Vol 9 (1) ◽  
pp. 27-35
Author(s):  
Valentina Ayuk Armadani ◽  
Siti Aisiyah ◽  
Ilham Kuncahyo

Verapamil HCl merupakan penghambat kanal Ca2+ untuk terapi hipertensi dan angina pectoris. Verapamil HCl memiliki bioavabilitas 10-20% dan waktu paruh 4 jam sehingga dapat dibuat sediaan gastroretentive untuk mempertahankan kadar terapi obat. Penelitian ini bertujuan mengetahui pengaruh matriks pektin dan HPMC K15M terhadap kemampuan mengapung, mengembang dan pelepasan obat pada tablet floating verapamil HCl.Penelitian ini menggunakan empat formula variasi konsentrasi matriks pektin dan HPMC K15M dengan metode kempa langsung kemudian dilakukan pengujian terhadap sifat fisik serbuk dan tablet. Pengaruh dan interaksi antara pektin dan HPMC K15M ditentukan dengan metode factorial design menggunakan software Design Expert.Matriks pektin dan HPMC K15M memberikan pengaruh terhadap kemampuan mengapung, mengembang dan pelepasan obat dari tablet floating verapamil HCl. HPMC K15M berpengaruh dominan terhadap floating lag time yang lebih cepat dan floating time yang lebih lama. Peningkatan HPMC K15M dan pektin menurunkan jumlah pelepasan di awal   dan   kecepatan   pelepasan   obat,   serta   meningkatkan   kemampuan   mengembang. Kombinasi pektin dan HPMC K15 M (1,5:1) mempunyai floating lag time cepat, floating time lama, dan kemampuan mengembang paling besar serta mengikuti orde nol.

2018 ◽  
Vol 6 (2) ◽  
pp. 225
Author(s):  
Lusia Oktora Ruma Kumala Sari ◽  
Tiara Berlianti ◽  
Eka Deddy Irawan

  An effervescent tablet of meloxicam solid dispersion has been developed for geriatric patients who have difficulty swallowing. The objective of this research was to know the optimum concentration of citric acid and sodium bicarbonate which produce the best effervescent tablet. A 2² factorial design was applied to investigate the effect of two factors: concentration of citric acid and sodium bicarbonate (effervescent materials) on hardness, dissolve time, and %drug released t30. Citric acid (6-18 mg) was used as acid source and sodium bicarbonate (18-105 mg) was used as base source. Software Design Expert trial version 10.0.5. was used to determine the optimum formula. The result showed that all formula satisfied the limit of hardness 2-4 kg/cm2 and friability <1%, but only formula (1), b, and ab that satisfied the limit of dissolve time <300 sec and %drug release t30 >70%. Formula A showed dissolve time 436 sec and %drug release t30 less than 70%. Desirability value of 0.917, which indicated the optimum formula, was obtained from the use of citric acid 6 mg and sodium bicarbonate 105 mg.   Keywords: meloxicam, effervescent tablet, solid dispersion, factorial design  


2019 ◽  
Vol 9 (3) ◽  
pp. 234-239
Author(s):  
Vidya Sabale ◽  
Hardikkumar Chaudhari ◽  
Prafulla Sabale

Background: The aim of the present study was to formulate and evaluate floating bioadhesive tablets of Nizatidine which is a competitive, reversible H2-receptor antagonist. Floatingbioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong gastric residence time was prepared. Methods: Polymers used were Hydroxy Propyl Methyl Cellulose (HPMC) K15M as matrix forming water swellable release retarding polymer and carbopol 934P as bioadhesive polymer. The gas generating agents used were sodium bicarbonate and citric acid. The prepared floating bioadhesive tablets of Nizatidine were optimized by 32 factorial design to study independent variable X1 (concentration of CP 934P) and X2 (concentration of HPMC K15M) and dependent variables as floating lag time, cumulative percentage drug release at 12h and swelling index. Tablets were evaluated for various parameters such as hardness, friability, drug content, swelling behavior, floating lag time, bioadhesive strength, drug release profile and stability. Results: All the formulations passed the test for weight variation, hardness, content uniformity and showed acceptable results with respect to drug content (97.93 ± 0.57) and % friability. The tablet containing 25% HPMC K15M and 13.75 % Carbopol 934P was selected as optimized formulation which showed the floating lag time of 74.34±2.08 seconds, drug release of 97.03±0.55% at 12 h (R12h,%), S.I as 79.24±0.87 at 9 h and bioadhesive strength as 10.0023±21.47 g. Stability of the formulation was proved using stability study. Conclusion: The formulated tablets have a potential for controlled release of the drug through floatation and bioadhesion.


Author(s):  
Umesh D Shivhare ◽  
V N Kakade

The present study was aimed to prepare a time-dependent pulsed release system for the programmed release of losartan potassium for the treatment of hypertension. The core tablets of losartan potassium were prepared using wet granulation containing a superdisintegrant. The design was based on 32 full factorial design containing 2 factors evaluated at 3 levels and the experimental trials were performed on coating of the core tablets. Eudragit S100 and Eudragit L100 were used as pH dependent polymers for coating of the tablets. Factors influenced the lag time and In-vitro drug release of formulations, called as dependent factors. Dissolution studies of coated tablets in media with pH (1.2 and 6.8) showed that drug release could be modulated by optimizing the concentration of Eudragit L100: Eudragit S100. Polynomial mathematical model generated for various response variable using multiple linear regression analysis, were found to be statistically significant. Contour plots and response surface plots were drawn and optimum formulation were selected by feasibility and desirability function. The experimental values obtained from the optimized formulation highly agreed with the predicted values. The results of in vitro dissolution studies indicated that formulation P5 is the most successful formulation of the study and exhibited lag time 5.5 h and drug release 95.23 % in 12 h. The total release pattern was very close to the theoretical release profile of pulsed release system. The study showed that lag time prior to drug release was highly affected by the coating level. The dissolution data revealed that the level of coating and the ratio of polymers are very important to achieve an optimum formulation. Stability study of the optimized formulation indicates no significant difference in release profile after a period of one month.


2021 ◽  
Vol 11 (3-S) ◽  
pp. 65-73
Author(s):  
Keyur S. Patel ◽  
Akshar N. Rao ◽  
Deepa R. Patel ◽  
Dhaval M. Patel ◽  
Advaita B. Patel

The objective of the present study was to develop gastroretentive floating tablets of quetiapine fumarate. The gastroretentive floating tablets of quetiapine fumarate were formulated using natrosol 250 HHX as a sustained release polymer and sodium bicarbonate as a gas forming agents.  A 32 factorial design was employed to study the influence of concentration of natrosol HHX 250 (X1) and concentration of sodium bicarbonate (X2) on the dependent variables % drug release at 1h (Y1), % drug release at 8 h (Y2) and floating lag time (Y3). The optimized formulation (O1) showed floating lag time 49 ± 3 sec and % drug release 99.54± 0.81 at 12 h. The in vitro release of F1-F9 batches were found in between 99.95 ± 1.18 %  to  86.32 ±1.71 % at 12 h. Floating lag time of F1-F9 batches were found to be 25± 2 sec to 178 ± 3 sec. FTIR studies shown that there was no  interaction between quetiapine fumarate and excipients. From the factorial design batches it was found that floating lag time was decreased with increasing the amount of sodium bicarbonate and decreasing the amount of natrosol 250 HHX. Here % release of drug was decreased with increase the extent of natrosol 250 HHX. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion. Keywords: Quetiapine fumarate, Natrosol 250 HHX, Sodium bicarbonate, Gastroretentive floating tablets


2018 ◽  
Vol 10 (6) ◽  
pp. 126
Author(s):  
Sanjeevani S. Deshkar ◽  
Arvind S. Pawara ◽  
Satish V. Shirolkar

Objective: The present study aimed at designing of floating matrix tablet of clopidogrel bisulphate by design of experiments.Methods: The tablets were prepared by direct compression technique using hydroxypropyl methylcellulose K15 (HPMC) as a matrix polymer and sodium bicarbonate as a gas generating agent. In order to optimize the concentration of HPMC (X1) and sodium bicarbonate (X2), a 32 full factorial design was employed. The tablet formulations were evaluated for floating lag time (Y1), floating or buoyancy time (Y2), percent water uptake, and differential scanning calorimetry (DSC) and in vitro drug release (Y3).Results: The formulation variables, HPMC concentration, and sodium bicarbonate concentration exerted a significant effect on floating behavior and drug release characteristics of the tablet. The optimized formulation, with 15% sodium bicarbonate concentration and 30 % HPMC concentration resulted in 5±2.6 sec of floating lag time, 22.0±0.6 h of floating time and 42.0±0.99% of clopidogrel bisulphate release in 8 h of dissolution study. The drug release mechanism was identified as nonfickian. The water uptake studies revealed that with an increase in HPMC concentration, there was an increase in swelling index of tablet whereas higher sodium bicarbonate concentration supported the faster erosion of matrix tablets. DSC study revealed no interaction of drug and polymers. The lower percentage error between predicted and observed responses of the optimized formulation validated the design.Conclusion: The study demonstrated successful designing of floating clopidogrel bisulphate tablet with factorial design.


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