Development of a Floating Dosage Form of Ranitidine Hydrochloride by Statistical Optimization Technique

Jain, Sanmati K.; Ms, Srinath; Narendra, C; Sn, Reddy; Sindhu, Anil

doi:10.4103/0975-1483.71619

Cited by 12 publications

(10 citation statements)

References 10 publications

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“…These data suggest that the models used are useful and successfully applied to the development and manufacture of RIF microspheres. The more rapid entry of dissolution medium into the microspheres resulted in a more rapid dissolution of d-glucose, further increasing the channels for diffusion of RIF, as well as increased erosion of the matrix, and these results are similar to those reported elsewhere [54].…”

Section: Responsesupporting

confidence: 88%

“…These results were in contrast to those reported elsewhere [39] in which yield was unchanged despite changes in the API-polymer ratio. It was observed that an increase in pore-forming agent d-glucose, whilst keeping Eudragit ® RLPO at the lowest content, resulted in the formation of microspheres that may break, and the reduction in yield could be as a result of damage of microspheres during filtration, drying and sieving and has been reported [54]. An increase in the Eudragit ® RLPO content whilst keeping d-glucose content low resulted in an increase in % yield and was attributed to the formation of microspheres with a resilient microsphere wall.…”

Section: Responsementioning

confidence: 94%

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Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Mwila

Walker

2020

Pharmaceutics

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The degradation of rifampicin (RIF) in an acidic medium to form 3-formyl rifamycin SV, a poorly absorbed compound, is accelerated in the presence of isoniazid, contributing to the poor bioavailability of rifampicin. This manuscript presents a novel approach in which isoniazid is formulated into gastric-resistant sustained-release microspheres and RIF into microporous floating sustained-release microspheres to reduce the potential for interaction between RIF and isoniazid (INH) in an acidic environment. Hydroxypropyl methylcellulose acetate succinate and Eudragit® L100 polymers were used for the manufacture of isoniazid-loaded gastric-resistant sustained-release microspheres using an o/o solvent emulsification evaporation approach. Microporous floating sustained-release microspheres for the delivery of rifampicin in the stomach were manufactured using emulsification and a diffusion/evaporation process. The design of experiments was used to evaluate the impact of input variables on predefined responses or quality attributes of the microspheres. The percent degradation of rifampicin following 12 h dissolution testing in 0.1 M HCl pH 1.2 in the presence of isoniazid gastric-resistant sustained-release microspheres was only 4.44%. These results indicate that the degradation of rifampicin in the presence of isoniazid in acidic media can be reduced by encapsulation of both active pharmaceutical ingredients to ensure release in different segments of the gastrointestinal tract, potentially improving the bioavailability of rifampicin.

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Section: Responsesupporting

confidence: 88%

Section: Responsementioning

confidence: 94%

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Mwila

Walker

2020

Pharmaceutics

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“…Larger particles tend to aggregate to a greater extent compared with smaller particles, thereby resulting in sedimentation. 29 The mean size of the prepared mucoadhesive NPs was found as 217.1±4.2 nm. Previously, Mazzarino et al 30 produced CSH-coated NPs for buccal drug delivery and the PS was found around 200 nm.…”

Section: Discussionmentioning

confidence: 98%

Development and in vitro Evaluation of Voriconazole Nanoparticle Formulation for Mucosal Application

Rençber

Karavana

2018

tjps

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ÖZAmaç: Bu çalışma, mukozal uygulama için antifungal bir ilaç olan vorikonazolün mukoadezif nanopartikül formülasyonunu hazırlamayı ve değerlendirmeyi amaçlamıştır. Ayrıca vorikonazolün HPLC yöntemi geliştirilmiş ve valide edilmiştir. Gereç ve Yöntemler: Bu çalışmada, kitozan kaplama polimeri kullanılarak vorikonazol içeren mukoadezif nanopartikül hazırlandı. Elde edilen nanopartikül formülasyonu, partikül boyutu, polidispersite indeksi, zeta potansiyeli ölçümü ve mukoadezyon çalışmaları ile karakterize edildi. İlaç yükleme kapasitesi nanopartikülde vorikonazol miktarının belirlenmesi için gerçekleştirildi. İn vitro ilaç salınımı da incelendi. HPLC yöntemi doğrusallık, doğruluk, kesinlik (tekrar edilebilirlik ve tekrar elde edilebilirlik), özgünlük, stabilite, LOD ve LOQ ile valide edildi. Bulgular: Vorikonazol içeren mukoadezif nanopartikül formülasyonu, 217.1±4.2 nm küçük partikül boyutu, 0.335±0.042 dar polidispersite indeksi, %99.052±0.424 ilaç yükleme kapasitesi, +26.82±0.4 mV pozitif zeta potansiyel değeri ile uygun bulunmuştur. Mukoadezyon çalışmasına göre, nanopartikülün, iyonik etkileşim nedeniyle müsinle etkileşime girdiği sonucuna varılabilir. Ayrıca nanopartikül/müsin dispersiyonunun bulanıklığı, müsin dispersiyonunun bulanıklığından daha fazla bulunmuştur. İn vitro ilaç salım çalışmasına göre, vorikonazolün nanopartikül dispersiyonunda homojen olarak dağılmış olduğu ve nanopartikül yüzeyi üzerinde önemli miktarda ilacın adsorbe edildiğini gösteren ani salım etkisi gözlemlenmemiştir. İlaç salımı, birinci dereceden ilaç salımı ile Fick Kanunu'na uymadığını göstermiştir. Önerilen HPLC yöntemi, rutin kalite kontrolü için basit, çok hassas, doğrusal, kesin, hassas, özgün ve stabildir. Sonuç: Bu çalışma, vorikonazol içeren mukoadezif nanopartikül formülasyonunun, mukozal hastalıkların lokal tedavisinde umut verici bir aday olduğunu göstermiştir. Geliştirilen HPLC yöntemi, vorikonazol içeren farmasötik preparatlar için başarılı bir şekilde uygulanabilir. Anahtar kelimeler: Vorikonazol, mukoadezif nanopartikül, kitosan, lokal uygulama, HPLC Objectives: This study aimed to prepare and evaluate mucoadhesive nanoparticle formulations of voriconazole, an antifungal drug, for mucosal application. It was also aimed to develop and validate a HPLC method of voriconazole. Materials and Methods: In this study, mucoadhesive nanoparticles containing voriconazole were prepared using a coating polymer of chitosan. The obtained nanoparticles were characterized via particle size, polydispersity index, zeta potential measurement, and mucoadhesion studies. Drug loading capacity was tested for determination of the voriconazole amount in the nanoparticles. In vitro drug release was also examined. The HPLC method was validated for linearity, accuracy, precision (repeatability and reproducibility), specificity, stability, limits of detection (LOD), and limit of quantification (LOQ). Results:In vitro characterization results of the mucoadhesive nanoparticle formulation containing voriconazole was found to be appropriate ...

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“…Drug release at the end of 3 hours increased from 20.52 % to 32.66 % and from 37.52 % to 44.90 % at high and low levels of polymer ratio (Ethocel standard 45 premium: Eudragit RL 100) respectively as the drug loading increased. That indicates when the amount of Ethocel standard 45 premium was comparatively high it showed greater release retarding property due to its hydrophobic nature (Jain et al, 2010;Shivakumar et al, 2008).…”

Section: Effect Of Formulation Variables On Percent Release At the Enmentioning

confidence: 94%

Formulation and Optimization of Carbamazepine Microspheres by 2 Factor 2 Level Central Composite Design

et al. 2016

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The present investigation was designed to prepare controlled release microspheres of carbamazepine using two polymers of different solubility and permeability characteristics, Ethocel standard 45 premium and Eudragit RL 100. The drug release profile was optimized with the aid of design of experiments (DoE). Microspheres of combined polymers were designed according to 2 2 factorial central composite design (CCD), taking drug loading and polymeric ratio as the independent variables. Total thirteen batches were prepared. The dependent variables were percentage of drug released in 3 hours and 6 hours and mean dissolution time (MDT). The regression parameters of the developed model and graphical interpretation for each response with statistical significance were calculated by using Minitab 17. The relationship between the experimental variables and responses were evaluated by generating response surface plots. Increased amount of Eudragit RL 100 had impact on surface morphology of prepared microspheres. It produced larger holes on the surface due to its higher permeability characteristics. Polynomial mathematical models generated for various response variables using multiple linear regression analysis, were found to be statistically significant (p < 0.05). One optimum formulation (O1) was selected based on USP specification and the second optimum formulation (O2) was selected for the maximization of MDT (hours). Batch O1 showed 22.85 % and 48.78 % drug release after 3 and 6 hours, respectively which were found to be in close agreement with those predicted by the mathematical model. Another optimum formulation, batch O2 showed MDT as 160.61 hours.

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Development of a Floating Dosage Form of Ranitidine Hydrochloride by Statistical Optimization Technique

Cited by 12 publications

References 10 publications

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Development and in vitro Evaluation of Voriconazole Nanoparticle Formulation for Mucosal Application

Formulation and Optimization of Carbamazepine Microspheres by 2 Factor 2 Level Central Composite Design

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