scholarly journals Data-Enriched Edible Pharmaceuticals (DEEP) with Bespoke Design, Dose and Drug Release

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1866
Author(s):  
Meie Chao ◽  
Heidi Öblom ◽  
Claus Cornett ◽  
Johan Bøtker ◽  
Jukka Rantanen ◽  
...  
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Storage Condition ◽  
Digital Design ◽  
Qr Code ◽  
Physical Size ◽  
Pharmaceutical Ingredients ◽  
Dry Conditions ◽  
Drug Doses ◽  
Single Dosage

Data-enriched edible pharmaceuticals (DEEP) is an approach to obtain personalized medicine, in terms of flexible and precise drug doses, while at the same time containing data, embedded in quick response (QR) codes at a single dosage unit level. The aim of this study was to fabricate DEEP with a patient-tailored dose, modify drug release and design to meet patients’ preferences. It also aimed to investigate physical stability in terms of the readability of QR code patterns of DEEP during storage. Cannabinoids, namely, cannabidiol (CBD) and delta-9-tetrahydrocannabinol (THC), were used as the model active pharmaceutical ingredients (APIs). Three different substrates and two colorants for the ink were tested for their suitability to fabricate DEEP by desktop inkjet printing. Flexible doses and customizable designs of DEEP were obtained by manipulating the digital design of the QR code, particularly, by exploring different pattern types, embedded images and the physical size of the QR code pattern. Modification of the release of both APIs from DEEP was achieved by applying a hydroxypropyl cellulose (HPC) polymer coating. The appearance and readability of uncoated and polymer-coated DEEP did not change on storage in cold and dry conditions; however, the HPC polymer layer was insufficient in preserving the readability of the QR code pattern in the extreme storage condition (40 °C and 75% relative humidity). To sum up, the DEEP concept provides opportunities for the personalization of medicines, considering also patients’ preferences.

Cholesterol succinyl chitosan anchored liposomes: preparation, characterization, physical stability, and drug release behavior

2010 ◽  
Vol 6 (3) ◽  
pp. 471-477 ◽  
Author(s):  
Yinsong Wang ◽  
Shaoli Tu ◽  
Rongshan Li ◽  
XiaoYing Yang ◽  
Lingrong Liu ◽  
...  
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Release Behavior ◽  
Drug Release Behavior

FIXED-DOSE COMBINATION DRUGS AS TABLET IN TABLET: A REVIEW

2021 ◽  
Vol 1 (9) ◽  
pp. 169-177
Author(s):  
Pavazhaviji P ◽  
Rajalakshmi A. N
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Product Life Cycle ◽  
Pharmacokinetic Profile ◽  
Oral Dosage ◽  
Fixed Dose ◽  
Pharmaceutical Ingredients ◽  
Delayed Release ◽  
Dose Combination ◽  
Compression Coating

The Pharmaceutical industry has become more interested in developing fixed-dose combinations (FDCs) in recent years. FDCs have been used successfully in a variety of clinical areas, including diabetes, HIV/AIDS,and cardiovascular diseases etc. FDCs are intended to extend the product life cycle and enhance patient compliance by decreasing cost. Active Pharmaceutical ingredients are chosen for FDC development based on variety of purposes such as Pharmacokinetic profile, drug-drug interactions, mechanism of action, and manufacturability for successful development. Tablet in tablet technology has gained popularity in recent years for creating modified release products. The compression coating or solvent-free-coating technology is also known as Tablet in Tablet technology. Tablet in Tablet technology is presently the finest alternative technology for the formulation of bilayer tablets for physical separation of active medicines and used to avoid chemical incompatibilities and to produce different drug release patterns such as rapid release, sustained release, controlled release, delayed release, and pulsatile release. This review mainly focuses on combining the techniques of both FDC and Tablet in Tablet formulations which offer a wide variety of benefits such as increased patient compliance, convenience, separation of incompatible ingredients, avoiding close interaction of two drugs, achieving various drug release patterns and maximizing the potency of both drugs over conventional oral dosage forms Keywords: Fixed dose combinations, Tablet in tablet technology, Compression coated tablet, Bilayer tablet, delayed release

A COMPARATIVE ASSESSMENT OF VESICULAR FORMULATIONS: TRANSFERSOMES AND CONVENTIONAL LIPOSOMES LOADED IVABRADINE HYDROCHLORIDE

2020 ◽  
pp. 51-55
Author(s):  
GITA CHAURASIA ◽  
NARENDRA LARIYA
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Physical Appearance ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Molar Ratio ◽  
Drug Release Study ◽  
Release Study

Objective: Ivabradine hydrochloride (IH), a benzazepine derivative used to treat cardiovascular disease angina pectoris. In this study IH-loaded novel carrier systems transfersomes (TFs) and conventional liposomes (CLs) were developed and compared for their efficacy to enhance the stability of drugs from degradation. Methods: TFs formulations (TF-1, TF-2 and TF-3) were prepared by using different biocompatible surfactants; tween-80 (TW), span-80(S) and sodium deoxycholate (SC) in the concentration ratio of 15 parts with 85 parts of soy phosphatidylcholine as phospholipid by thin-film hydration method. These vesicles were compared with CLs formulation (L-1) prepared in 7:3 molar ratio of soy phosphatidylcholine: cholesterol by following the same method. These vesicles were compared for physical appearance, vesicle shape, and size, percentage drug entrapment efficiency (%DEE), deformability index (DI), in vitro percentage cumulative drug release study, and physical stability studies. The chosen optimized novel carriers were observed under scanning electron microscopy. Results: The compared data demonstrated that the physical appearance for all vesicles was turbid and had a spherical shape. The size distribution was in the range of 129.0 nm to 273.5 nm in vesicles. The %DEE (79.0±0.94) and DI (35.0±1.9) was found maximum in TF-1 formulation that was 2.3 times higher than L-1 formulation. The in vitro percentage cumulative drug release study followed second-order polynomial kinetics that was 2.0 times higher than L-1and 2.9 times higher than the plain drug in 30 min (90.4±0.06%) from TF-1. The vesicles were found to be stable at refrigeration conditions. Conclusion: Thus, amongst of all vesicles TW loaded TFs (TF-1) was chosen as an excellent novel vesicular carrier for hydrophilic drugs due to its higher deformability behavior than CLs that protects the certain drugs from biodegradation and provides stability.

scholarly journals Self-assembled sorbitol-derived supramolecular hydrogels for the controlled encapsulation and release of active pharmaceutical ingredients

2015 ◽  
Vol 51 (35) ◽  
pp. 7451-7454 ◽  
Author(s):  
Edward J. Howe ◽  
Babatunde O. Okesola ◽  
David K. Smith
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
The Self ◽  
Active Pharmaceutical Ingredients ◽  
Supramolecular Hydrogel ◽  
Pharmaceutical Ingredients ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Self Assembled ◽  
Ph Controlled

A simple supramolecular hydrogel is able to extract acid-functionalised anti-inflammatory drugs via directed interactions with the self-assembled gel nanofibres and exhibits pH-controlled drug release.

Stability of Imipenem-Cilastatin Sodium in AutoDose Infusion System Bags

2003 ◽  
Vol 38 (2) ◽  
pp. 130-134
Author(s):  
Lawrence A. Trissel ◽  
Quanyun A. Xu
Keyword(s):  
Sodium Chloride ◽  
Chemical Stability ◽  
High Performance ◽  
Physical Stability ◽  
Analytical Techniques ◽  
Storage Condition ◽  
Evaluation Procedure ◽  
Drug Concentrations ◽  
Physical And Chemical ◽  
Infusion System

The objective of this study was to evaluate the physical and chemical stability of imipenem-cilastatin sodium 250 mg/100 mL and 500 mg/100 mL (of each drug component) admixed in 0.9% sodium chloride injection packaged in AutoDose Infusion System bags. Triplicate test samples were prepared by bringing the required amount of imipenem-cilastatin sodium injection to volume with 0.9% sodium chloride injection. A total of 100 mL of each of the test solutions was packaged in each of three ethylene vinyl acetate (EVA) AutoDose bags designed for use in the AutoDose Infusion System for each storage condition. Samples were protected from light and evaluated at appropriate intervals for up to three days at 23°C and 14 days at 4°C. Physical stability was assessed using a multistep evaluation procedure that included turbidimetric and particulate measurement in addition to visual inspection. Chemical stability was assessed with stability-indicating high performance liquid chromatography (HPLC) analytical techniques, based on initial drug concentrations and concentrations at appropriate intervals over the study periods. The admixtures were clear throughout the study when viewed in normal fluorescent room light and with a Tyndall beam. Measured turbidity and particulate content were low initially and exhibited little change throughout the study. HPLC analysis revealed extensive decomposition in the samples, with imipenem being the less stable component. The instability of the imipenem-cilastatin sodium admixtures is consistent with previous studies. Admixtures stored under refrigeration should be used immediately upon warming to room temperature due to the rapid rate of imipenem decomposition. The AutoDose Infusion System bags were not found to affect adversely or improve the physical and chemical stability of this drug.

scholarly journals Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review

2020 ◽  
Vol 2 (2) ◽  
pp. 77
Author(s):  
Dwi Retno Sari ◽  
Yoga Windhu Wardhana ◽  
Taofik Rusdiana
Keyword(s):  
Contact Angle ◽  
Drug Release ◽  
Manufacturing Industry ◽  
Fourier Transforms ◽  
Class Ii ◽  
Production Costs ◽  
Active Pharmaceutical Ingredients ◽  
Scanning Calorimetry ◽  
Pharmaceutical Ingredients ◽  
Volatile Solvents

Many techniques can be used to improve drug solubility, which is the development of the liquisolid technique. This technique has a mechanism for increasing the surface area of the drug as well as wetting from the addition of non-volatile solvents resulting in a lower surface tension and contact angle, so the solubility and drug release very increases. Liquisolid tablets show a lower contact angle compared to the conventional tablets. The liquisolid technique approach is also promising because the process is simple in making low production costs and allows the manufacturing industry, including non-volatile solvents, fillers, dryers, and disintegrants. Liquisolid characterized by specific instruments such as powder x-ray diffraction (PXRD), Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscope (SEM). Several liquisolid techniques are described in this review. The liquisolid technique is proven and able to change the physicochemical properties of active pharmaceutical ingredients, especially the solubility, drug release, and stability of the formula so that this technique can be a solution for class II and IV BCS pharmaceutical active drug classes.Keywords: Active Pharmaceutical Ingredients, Contact Angle, Solubility, Drug Release, Stability, Liquisolid Technique

scholarly journals Formulation and Evaluation of Fast Dissolving Film of Losartan Potassium

2021 ◽  
Vol 68 (1) ◽  
Author(s):  
Bhageerathy A ◽  
Sandhya Murali ◽  
eny Sara Thomas ◽  
Sigi Vasanthkumar ◽  
Prasanth V V
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Losartan Potassium ◽  
In Vivo Studies ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation ◽  
Significant Difference

A total of nine formulations of fast dissolving films of Losartan Potassium were developed by solvent casting method using film forming polymers such as HPMC E5, E15 and E50 and other film modifiers. The appearances of films were transparent, thin, flexible, elastic, smooth and transparent. The weight variation ranged between 16.14 ± 0.192 and 17.31 ± 0.313 and showed that there was no significant difference in the weight of individual formulations. All the formulations showed more than 150 of folding endurance. The drug content was found to be in an acceptable range for all the formulations which indicated uniform distribution of drug. A rapid dissolution of all the film was observed by the dissolution test, in which above 90% of Losartan Potassium was released within 5 min. The formulation F1 showed maximum drug release (98.73) within 5 minutes. Based on the in vitro drug release, drug content and in vitro disintegration time it is found that F1 was selected as the best formulation. The formulations showed satisfactory physical stability at 40°C at 75 % RH. Losartan Potassium (LOSAR-25) is shown in Figure 4. From the results of comparative studies of marketed product and it found that F1 showed 98.73% release within 5 min and LOSAR 25 showed 90.76% release in 30 min. In vitro studies indicate that this potential drug delivery system has considerably good stability and release profile. Nevertheless, further in vivo studies are warranted to confirm these results.

Effect of Tablet Surface Area and Surface Area/Volume on Drug Release from Lamivudine Extended Release Matrix Tablets

2010 ◽  
Vol 3 (1) ◽  
pp. 872-876 ◽  
Author(s):  
Narayana Raju P ◽  
Prakash K ◽  
Rama Rao T ◽  
B.C.S. Reddy ◽  
Sreenivasulu V ◽  
...  
Keyword(s):  
Drug Release ◽  
Surface Area ◽  
Extended Release ◽  
Matrix Tablets ◽  
Diffusion Controlled ◽  
Similar Drug ◽  
Drug Doses ◽  
Key Variables ◽  
Different Shapes ◽  
Release Profiles

The purpose of this study was to investigate the influence of tablet surface area/ volume (SA/Vol) on drug release from extended-release matrix tablets of lamivudine prepared with hydroxy propyl methylcellulose (HPMC). Highly soluble drug such as lamivudine was utilized in this study to give predominantly diffusion-controlled release. Drug release from HPMC matrix tablets with similar values of SA/Vol was comparable within the same tablet shaped tablet. Tablets having the same surface area but different SA/Vol values did not result in similar drug release, tablets with larger SA/Vol values had faster release profiles. Utility of SA/Vol to affect drug release was demonstrated by changing drug doses, and altering tablet shape to adjust SA/Vol. When SA/Vol was held constant, similar release profiles were obtained. Thus, surface area/volume is one of the key variables in controlling drug release from HPMC matrix tablets. Proper use of this variable has practical application by formulators who may need to duplicate drug release profiles from tablets of different sizes and different shapes.

Polymeric Precipitation Inhibitor Based Supersaturable Self-microemulsifying Drug Delivery System of Canagliflozin: Optimization and Evaluation

2021 ◽  
Vol 18 ◽  
Author(s):  
Dilpreet Singh ◽  
Ashok K. Tiwary ◽  
Tejwant Singh Kang ◽  
Neena Bedi
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Physical Stability ◽  
In Vitro Dissolution ◽  
Titration Calorimetry ◽  
Substrate Affinity ◽  
Pharmacokinetic Studies ◽  
Poloxamer 188 ◽  
P Glycoprotein

Background: The present investigation attempts to optimize Supersaturable lipid based formulation (SS SMEDDS) of Biopharmaceutical Classification System (BCS) class IV drug canagliflozin (CFZ) and evaluating the oral bioavailability of the formulation. Methods: Preliminary screening revealed Poloxamer 188 to most effectively inhibit precipitation of CFZ after dispersion during in vitro supersaturation studies. Box Behnken Design was employed for designing different formulations and various statistical analysis were done out to select an appropriate mathematical model. The optimized formulation (OSS 1) was evaluated for in vitro drug release and ex vivo permeation studies to evaluate drug release and permeation rate. Pharmacokinetic studies have been done according to standard methodologies. Results: The optimized formulation (OSS 1) containing 781.1 mg SS SMEDDS and 2.24 % w/w Poloxamer 188 was developed at a temperature of 60°C which revealed nano-globule size with negligible aggregation. Isothermal titration calorimetry revealed the thermodynamic state of formed microemulsion with negative ∆G. The optimized formulation was observed to possess physical stability under different stress conditions and acceptable drug content.. In vitro dissolution of optimized SS SMEDDS revealed higher dissolution rate of CFZ as compared with native forms of CFZ. The permeability of CFZ from optimized SS SMEDDS across various excised segments of rat intestine was observed to be multifold higher that manifested in 2.05-fold higher Cmax and 5.64-fold higher AUC0-36h following oral administration to Wistar rats. Conclusion: The results could be attributed to substantial lymphatic uptake and P-glycoprotein substrate affinity of CFZ in SS SMEDDS investigated through chylomicron and P-glycoprotein inhibition approach, respectively.

scholarly journals Hot Melt Coating of Amorphous Carvedilol

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 519 ◽  
Author(s):  
Jacob Bannow ◽  
Lina Koren ◽  
Sharareh Salar-Behzadi ◽  
Korbinian Löbmann ◽  
Andreas Zimmer ◽  
...  
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Spray Coating ◽  
Aqueous Solubility ◽  
Immediate Release ◽  
In Vitro Lipolysis ◽  
Drug Candidates ◽  
Amorphous Drug ◽  
Hot Melt

The use of amorphous drug delivery systems is an attractive approach to improve the bioavailability of low molecular weight drug candidates that suffer from poor aqueous solubility. However, the pharmaceutical performance of many neat amorphous drugs is compromised by their tendency for recrystallization during storage and lumping upon dissolution, which may be improved by the application of coatings on amorphous surfaces. In this study, hot melt coating (HMC) as a solvent-free coating method was utilized to coat amorphous carvedilol (CRV) particles with tripalmitin containing 10% (w/w) and 20% (w/w) of polysorbate 65 (PS65) in a fluid bed coater. Lipid coated amorphous particles were assessed in terms of their physical stability during storage and their drug release during dynamic in vitro lipolysis. The release of CRV during in vitro lipolysis was shown to be mainly dependent on the PS65 concentration in the coating layer, with a PS65 concentration of 20% (w/w) resulting in an immediate release profile. The physical stability of the amorphous CRV core, however, was negatively affected by the lipid coating, resulting in the recrystallization of CRV at the interface between the crystalline lipid layer and the amorphous drug core. Our study demonstrated the feasibility of lipid spray coating of amorphous CRV as a strategy to modify the drug release from amorphous systems but at the same time highlights the importance of surface-mediated processes for the physical stability of the amorphous form.

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