Design and study of lamivudine oral controlled release tablets

Ravi, Punna Rao; Ganga, S.; Saha, Ranendra Narayan

doi:10.1208/pt0804101

Cited by 28 publications

(15 citation statements)

References 28 publications

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“…To gain an idea of the release properties of the generated materials, the drug release profiles were plotted against zero-order, first-order, Higuchi, Hixson-Crowell and Ritger-Peppas models and their R 2 values were compared as is a common practice in the literature [62][63][64][65][66][67][68].…”

Section: Cpt Release Assay By Fluorimetrymentioning

confidence: 99%

Controlled Drug Delivery From Composites of Nanostructured Porous Silicon and Poly( L -Lactide)

et al. 2012

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Aims: Porous silicon (pSi) and poly(L-lactide) (PLLA) both display good biocompatibility and tunable degradation behavior, suggesting that composites of both materials are suitable candidates as biomaterials for localized drug delivery into the human body. The combination of a pliable and soft polymeric material with a hard inorganic porous material of high drug loading capacity may engender improved control over degradation and drug release profiles and be beneficial for the preparation of advanced drug delivery devices and biodegradable implants or scaffolds. Materials & methods: In this work, three different pSi and PLLA composite formats were prepared. The first format involved grafting PLLA from pSi films via surface-initiated ring-opening polymerization (pSi–PLLA [grafted]). The second format involved spin coating a PLLA solution onto oxidized pSi films (pSi–PLLA [spin-coated]) and the third format consisted of a melt-cast PLLA monolith containing dispersed pSi microparticles (pSi–PLLA [monoliths]). The surface characterization of these composites was performed via infrared spectroscopy, scanning electron microscopy, atomic force microscopy and water contact angle measurements. The composite materials were loaded with a model cytotoxic drug, camptothecin (CPT). Drug release from the composites was monitored via fluorimetry and the release profiles of CPT showed distinct characteristics for each of the composites studied. Results: In some cases, controlled CPT release was observed for more than 5 days. The PLLA spin coat on pSi and the PLLA monolith containing pSi microparticles both released a CPT payload in accordance with the Higuchi and Ritger–Peppas release models. Composite materials were also brought into contact with human lens epithelial cells to determine the extent of cytotoxicity. Conclusion: We observed that all the CPT containing materials were highly efficient at releasing bioactive CPT, based on the cytotoxicity data. Original submitted 16 December 2010; Revised submitted 29 September 2011; Published online 6 March 2012

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Section: Cpt Release Assay By Fluorimetrymentioning

confidence: 99%

Controlled Drug Delivery From Composites of Nanostructured Porous Silicon and Poly( L -Lactide)

et al. 2012

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“…The influence of HPMC K100 LV CR in regulating the drug release was found to be more pronounced vis-à-vis PEO 303. This can be attributed to the swellable nature of HPMC K100 LV CR, which forms a glassy barrier on the dosage form plausibly owing to the water sorption mechanism and tend to regulate the drug release by Fickian diffusion mechanism (34). The evaluation of 2D-contour plots also revealed analogous observation among the studied polymers with moderate interactions prevailing between them, as is evident from the curved contour lines.…”

Section: Characterization Of the Floating-bioadhesive Tabletsmentioning

confidence: 54%

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

et al. 2015

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ABSTRACT. The objective of the present studies was systematic development of floating-bioadhesive gastroretentive tablets of cefuroxime axetil employing rational blend of hydrophilic polymers for attaining controlled release drug delivery. As per the QbD-based approach, the patient-centric target product profile and quality attributes of tablet were earmarked, and preliminary studies were conducted for screening the suitability of type of polymers, polymer ratio, granulation technique, and granulation time for formulation of tablets. A face-centered cubic design (FCCD) was employed for optimization of the critical material attributes, i.e., concentration of release controlling polymers, PEO 303 and HPMC K100 LV CR, and evaluating in vitro buoyancy, drug release, and ex vivo mucoadhesion strength. The optimized formulation was embarked upon through numerical optimization, which yield excellent floatation characteristic with drug release control (i.e., T 60% >6 h) and bioadhesion strength. Drug-excipient compatibility studies through FTIR and P-XRD revealed the absence of any interaction between the drug and polymers. In vivo evaluation of the gastroretentive characteristics through X-ray imaging and in vivo pharmacokinetic studies in rabbits revealed significant extension in the rate of drug absorption (i.e., T max , K a , and MRT) from the optimized tablet formulation as compared to the marketed formulation. Successful establishment of various levels of in vitro/in vivo correlations (IVIVC) substantiated high degree of prognostic ability of in vitro dissolution conditions in predicting the in vivo performance. In a nutshell, the studies demonstrate successful development of the once-a-day gastroretentive formulations of cefuroxime axetil with controlled drug release profile and improved compliance.

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“…Hydroxypropyl methylcellulose (HPMC, hydrophilic) has been a popular release-retarding polymer in simple matrix tablets (19,20) and floating gastro-retentive tablets (21,22). Fine particle ethyl cellulose (FPEC) was successfully used in the formulation of extended-release tablets of some non-ionizable drugs (23).…”

Section: Introductionmentioning

confidence: 99%

Development of Controlled-Release Matrix Tablet of Risperidone: Influence of Methocel®- and Ethocel®-Based Novel Polymeric Blend on In Vitro Drug Release and Bioavailability

et al. 2011

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Abstract. Controlled-release (CR) matrix tablet of 4 mg risperidone was developed using flow bound dry granulation-slugging method to improve its safety profile and compliance. Model formulations F1, F2, and F3, consisting of distinct blends of Methocel® K100 LV-CR and Ethocel® standard 7FP premium, were slugged. Each batch of granules (250-1,000 μm), obtained by crushing the slugs, was divided into three portions after lubrication and then compressed to 9-, 12-, and 15-kg hard tablets. In vitro drug release studies were carried out in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8) using a paddle dissolution apparatus run at 50 rpm. The CR test tablet, containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness, exhibited pH-independent zero-order release kinetics for 24 h. The drug release rate was inversely proportional to the content of Ethocel®, while the gel layer formed of Methocel® helped in maintaining the integrity of the matrix. Changes in the hardness of tablet did not affect the release kinetics. The tablets were reproducible and stable for 6 months at 40±2°C/75±5% relative humidity. Risperidone and its active metabolite, 9-hydroxyrisperidone, present in the pooled rabbit's serum, were analyzed with HPLC-UV at λ max 280 nm. The CR test tablet exhibited bioequivalence to reference conventional tablet in addition to the significantly (p<0.05) optimized peak concentration, C max , and extended peak time, T max , of the active moiety. There was a good association between drug absorption in vivo and drug release in vitro (R 2 =0.7293). The successfully developed CR test tablet may be used for better therapeutic outcomes of risperidone.

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Design and study of lamivudine oral controlled release tablets

Cited by 28 publications

References 28 publications

Controlled Drug Delivery From Composites of Nanostructured Porous Silicon and Poly( L -Lactide)

Controlled Drug Delivery From Composites of Nanostructured Porous Silicon and Poly( L -Lactide)

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

Development of Controlled-Release Matrix Tablet of Risperidone: Influence of Methocel®- and Ethocel®-Based Novel Polymeric Blend on In Vitro Drug Release and Bioavailability

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