Solid self microemulsification of Atorvastatin using hydrophilic carriers: a design

Kishore, Raj; Yalavarthi, Prasanna Raju; Vadlamudi, Harini Chowdary; Vandana, K.R.; Rasheed, Arun; Sushma, M

doi:10.3109/03639045.2014.938655

Cited by 27 publications

(11 citation statements)

References 20 publications

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“…Before filling into capsules, the powders were subjected to micromeritic properties studies like bulk density, Hausner ratio and angle of repose [23,25] .…”

Section: Melt Granulation Techniquementioning

confidence: 99%

“…Constant stirring at (37 ± 1) C was maintained by keeping the whole set up on a thermostatic magnetic stirrer. The aliquots were collected at periodical intervals of time up to 6 h. The receptor compartment was set for sink condition using phosphate buffer solution pH 7.4 [23] . Ex-vivo studies were carried out by replacing cellophane membrane with goat intestine sac.…”

Section: Diffusion Studiesmentioning

confidence: 99%

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Potential of microemulsified entacapone drug delivery systems in the management of acute Parkinson's disease

Vadlamudi

Yalavarthi

Venkata

et al. 2016

Journal of Acute Disease

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A B S T R A C T Objective:To design solid self-microemulsifying drug delivery system (S-SMEDDS) of entacapone and evaluate for its anti-Parkinson's potentials. Methods: Solubility studies were performed in various vehicles i.e., oils, surfactants and co-surfactants and pseudo-ternary phase diagrams were plotted to understand the microemulsion formation region. Liquid self-microemulsifying drug delivery systems (SMEDDS) were developed using gingelly and rice bran oil as lipid vehicles, Tween 80 and Span 20 as surfactants and glycerin, propylene glycol as co-surfactants. They were characterized by Fourier transform infrared spectroscopy, pH, viscosity, zeta potential, polydispersibility index and droplet size analysis and evaluated for drug content, in-vitro release, in-vitro diffusion and ex-vivo permeation. Optimized liquid SMEDDS were converted into S-SMEDDS by adsorption and melt granulation procedures. Characterization by differential scanning calorimetry, SEM, micrometrics, reconstitution property, moisture content and evaluation by drug content, drug release kinetics and shelf-life were performed for S-SMEDDS. Parkinsonism was induced and pharmacodynamic potentials of S-SMEDDS were evaluated. Results: S-SMEDDS formulation AG8 had shown the highest drug release of 90.92% within 60 min. Pharmacodynamic studies also proved the efficiency of entacapone S-SMEDDS against Parkinsonism. Conclusions: Entacapone S-SMEDDS is an effective drug delivery system that offers more predictable and extensive drug release with enhanced shelf-life in the treatment of acute Parkinsonism.

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“…Before filling into capsules, the powders were subjected to micromeritic properties studies like bulk density, Hausner ratio and angle of repose [23,25] .…”

Section: Melt Granulation Techniquementioning

confidence: 99%

Section: Diffusion Studiesmentioning

confidence: 99%

Potential of microemulsified entacapone drug delivery systems in the management of acute Parkinson's disease

Vadlamudi

Yalavarthi

Venkata

et al. 2016

Journal of Acute Disease

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“…The pellets were then tested for their flow properties, drug content, and in vitro drug release. 21,22…”

Section: Stability Studymentioning

confidence: 99%

Biopharmaceutical Process of Diclofenac Multiparticulate Systems for Chronotherapy of Rheumatoid Arthritis

Battu

Yalavarthi

Subbareddy

et al. 2018

tjps

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Diklofenak sınırlı çözünürlük, düşük biyoabsorpsiyon ve gastrik toksisite gösterir. Çalışmanın amacı, yukarıdaki kısıtlamaları ele almak ve RA'nın kronoterapisi için çok birimli bir formülasyon tasarlamaktır. Gereç ve Yöntemler: DC, SSG ve GG ile katı dispersiyonları hazırlandı. Aynı boyutlu (∼400 µm) nonpareil çekirdekler, hemen salım yapan pelletler (DMP-1 ve DMP-2) ve kontrollü salımlı pelletler (DMP-3 ve DMP-4) üretmek için katı dispersiyonlarla kaplandı. Elde edilen kontrollü salım pelletleri, pulsatil salım pelletleri (DMPP) elde etmek için metakrilat polimerleri ile daha da katmanlı hale getirildi. DMPP için çözünürlük, FTIR, DSC, mikrometrik, SEM, etkin madde içeriği, etkin madde salımı, farmakokinetik ve stabilite çalışmaları yapıldı. Bulgular: DC'nin çözünürlüğü, katı dispersiyonlardaki hidrofilik taşıyıcıların varlığına bağlı olarak 164 kat arttı. FTIR spektrumunda ve termogramlarda kimyasal ve fiziksel etkileşimler gözlemlenmedi. Akışkanlaştıran yataklı işlemci, 19.5 dereceden daha az bir akış açısı ve %95.18 ile %98.87 arasında DC içeriği olan yüksek kaliteli, yuvarlak ve düzenli pelletlerin üretimini kolaylaştırdı. Maksimum etkin madde 12 saat sonunda DMPP'den salındı. Objectives: Diclofenac exhibits limited solubility, low bioabsorption and gastric toxicity. The objective of the study was to address the above limitations and to design a multi-particulate formulation for the chronotherapy of RA. Materials and Methods: Solid dispersions of DC with SSG and GG were prepared. Uniform-sized (∼400 µm) non-pareil seeds were coated with solid dispersions to produce immediate-release pellets (DMP-1 and DMP-2) and controlled-release pellets (DMP-3 and DMP-4). The resultant controlled-release pellets were further layered with methacrylate polymers to obtain pulsatile-release pellets (DMPP). Solubility, FTIR, DSC, micrometrics, SEM, drug content, drug release, pharmacokinetics, and stability studies were performed for DMPP. Results: The solubility of DC was improved by 164-folds due to the presence of hydrophilic carriers in the solid dispersions. No chemical and physical interactions were noticed in FTIR spectra and also in thermograms. A fluidized bed processor facilitated the production of high-quality, circular, and regular pellets with an angle of repose less than 19.5 degrees and DC content between 95.18% and 98.87%. The maximum drug was released from DMPP at the end of 12 hours. DMP-1 and DMP-2 pellets had 2 hr of drug release and pulsatile, controlled-release pellets had a 6 hr lag phase followed by 12 hr controlled release. Both DMP-1 and DMP-2-immediate showed first-order release followed by Hixson-Crowell kinetics, whereas DMPP pellets followed zero-order release with Higuchi's kinetics. The maximum concentration of DC in plasma was 400.8 ng/mL at 5 hr for DMP-2 and 381.1 ng/mL at 14 hr for DMPP-5. The solubility of DC was increased with the application of solid dispersion and in turn increased the pharmacokinetics. The pellets were plausibly stable over a period of 90 days. Conclusion: Thus, multi-p...

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“…The absolute bioavailability of ATC is only 14%, and the inhibition activity of HMG-CoA reductase was only 30% . The main reasons for this phenomenon are poor drug solubility in aqueous solution, easier degradation in acid medium, and fast elimination in vivo. , To improve ATC gastrointestinal absorption, researchers attempted a series of lipid based carrier systems including nanoparticles, self-emulsifying system, and dry emulsion system. − However, although these lipid carrier systems can promote the drug bioavailability to varying degrees, some drawbacks cannot be ignored. The use of large amount of organic solvent and high proportion of coemulsifier can bring potential safety risk, and complicated processes such as dialysis, ultrafiltration, and freeze-drying are not suitable for large-scale production.…”

Section: Introductionmentioning

confidence: 99%

Combination of Phospholipid Complex and Submicron Emulsion Techniques for Improving Oral Bioavailability and Therapeutic Efficacy of Water-Insoluble Drug

et al. 2018

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Water-insoluble drugs cannot be absorbed effectively through the gastrointestinal tract due to insufficient solubility and often face the problems of low bioavailability and poor therapeutic efficacy. To overcome these biopharmaceutical challenges, lipid-based formulations were suggested and have been researched in recent years. In this study, we used atorvastatin as a model drug to prepare a phospholipid complex prodrug system to upgrade its lipophilicity and further developed a drug loaded submicron emulsion to improve its in vivo bioavailability. The mean particle size and zeta potential of submicron emulsion were 122.7 nm and -22.7 mV. Intestinal absorption of atorvastatin from submicron emulsion was significantly improved compared with free drug, and the absorption rate constant ( K) and apparent permeability coefficients ( P) increase 2.88-fold and 2.45-fold, respectively. After oral administration, the atorvastatin plasma concentration of the emulsion group was much higher than that of free drug and the area under the curve (AUC) reached to 4.033 mg/L·h (2.58-fold). In vivo pharmacodynamics results revealed that atorvastatin submicron emulsion showed excellent antihyperlipidemia efficacy by reducing the total cholesterol, triglyceride, and low density lipoprotein cholesterol (LDL-cholesterol) levels and simultaneously increasing the high density lipoprotein cholesterol (HDL-cholesterol) level in comparison with Lipitor. In conclusion, drug-phospholipid complex loaded submicron emulsion was a promising oral delivery system for improving in vivo absorption behavior and therapeutic efficacy for water-insoluble drugs.

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Solid self microemulsification of Atorvastatin using hydrophilic carriers: a design

Abstract: The solid form of atorvastatin liquid SMEDDS had been formulated successfully with enhanced shelf life and solubility.

Cited by 27 publications

References 20 publications

Potential of microemulsified entacapone drug delivery systems in the management of acute Parkinson's disease

Potential of microemulsified entacapone drug delivery systems in the management of acute Parkinson's disease

Biopharmaceutical Process of Diclofenac Multiparticulate Systems for Chronotherapy of Rheumatoid Arthritis

Combination of Phospholipid Complex and Submicron Emulsion Techniques for Improving Oral Bioavailability and Therapeutic Efficacy of Water-Insoluble Drug

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