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Omar Y Mady,1 Adam A Al-Shoubki,2 Ahmed A Donia3 1Pharmaceutical Technology Department, Faculty of Pharmacy, Tanta University, Tanta, Egypt; 2Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Omar Al-Mukhtar University, Al-Bayda, Libya; 3Department of Pharmaceutical Technology, Menoufia University, Shebeen El-Kom, EgyptCorrespondence: Omar Y Mady Tel +201141819661Email omer.mady@gmx.atAdam A Al-ShoubkiPharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Omar Al-Mukhtar University, Al-Bayda, LibyaTel +218922826802Email adim.alsanousi@omu.edu.lyBackground: Sorbitan monostearate is a surfactant used in the food industry. It was proved as a penetration enhancer to metformin HCl via a paracellular pathway. It is solid at room temperature and has a low melting point. Therefore, it was selected, as a granulating agent for metformin HCl.Methods: Multi-level factorial design was applied to determine the optimized formula for industrial processing. The selected formulations were scanned using an electron microscope. Differential scanning calorimetry was used to ascertain the crystalline state of a drug. A modified non-everted sac technique, suggested by the authors, was used to evaluate the in vitro permeation enhancement of the drug. To simulate the emulsification effect of the bile salt, a tween 80 was added to the perfusion solution. As a pharmacodynamic marker, blood glucose levels were measured in diabetic rats.Results: The results showed that drug permeability increases in the presence of tween 80. Drug permeability from granules increased than that of the pure drug or pure drug with tween 80. The prepared granules decreased blood glucose levels of diabetic rats than the pure drug and drug plus tween 80. There was an excellent correlation between the results of the drug permeation percent in vitro and the dropping of blood glucose level percent in vivo.Conclusion: Improving the drug permeation and consequently, the drug pharmacodynamic effect in addition to an excellent micromeritics property of the prepared drug granules showed the dual enhancement effect of the suggested industrial procedure. Therefore, we suggest the same industrial procedure for other class III drugs.Keywords: sorbitan monostearate, class III drugs, factorial design, modified non-everted sac

This study aims to improve the RXB bioavailability using hybrid nanoparticles. A modified melt dispersion technique created different formulas with varying GMO-SAIB: RXB and GMO: SAIB ratios, with fixed GMO-SAIB: poloxamer 407 ratios. The PS, PDI, ZP, and EE were measured to determine the optimal formula, which was selected using Design-Expert™ software. The optimized formula was lyophilized and tested for PS, PDI, ZP, and EE. The chosen lyophilized formula (L4) was characterized using FTIR, DSC, PXRD, dissolution studies, and pharmacokinetics studies. The study found correlations between variables and identified how GMO-SAIB concentration affects drug encapsulation. The dissolution parameters were calculated, including % Q5 and % DE). The % Q5 values were 68.4 ± 1.7% and 89.7 ± 3.6% for Xarelto and L4 tablets, respectively. The % DE values were 89.7 ± 0.4% and 97.5 ± 2.1% for Xarelto and L4 tablets, respectively. The AUC values were 2117.0 ng.h/mL (±77.3) and 3919.4 ng.h/mL (±134.8) for Xarelto and L4 tablets, respectively. The Cmax values were 241.3 ng/mL (±21.0) and 521.5 ng/mL (±91.5) for Xarelto and L4 tablets, respectively. In conclusion, the study found that using GMO-SAIB as co-formers effectively enhanced the bioavailability of RXB. The authors recommend using the hybrid nanoparticles technique and suggest further research to enhance its effectiveness for drug delivery.

The future of dosage form design is expected to move towards the production of personalized dosage forms tailored to each patient. The 3D printer was introduced to solve that problem but is not easy to use in a pharmacy. Herein, a new 3D mold technology is adopted for tablet manufacturing. Preparation of amlodipine tablets was used as a Biopharmaceutics Classification System Class 1 drug model to study this technology. Different concentrations of either starch or Avicel-based formulations and different concentrations of hydroxypropyl methylcellulose as a binder for mass formation were used. The mass formed for each formula was cast into the mold for tablet preparation. Different non-pharmacopeial and pharmacopeial quality-control tests of the prepared tablets by using the 3D mold were compared to a marketed tablet product of amlodipine. 3D-molded tablets showed compliance properties with the tablet pharmacopeial quality standard. Studying the equivalence of the 3D mold tablets to the brand marketed product under biowaiver conditions was carried out. The difference and similarity factors studies of molded tablets prepared using starch or Avicel as a filler and 2.5% of hydroxypropyl methylcellulose showed acceptable characters to the drug brand name. It is predicted that by using this simple technique, it would be possible to produce tablets with designed disintegration and release profiles, which could potentially allow the tailoring of the drug release and hence personalize the medicine for each patient., (Copyright© by International Journal of Pharmaceutical Compounding, Inc.)

Penetration enhancement of metformin hydrochloride via its molecular dispersion in sorbitan monostearate microparticles is reported. This represents basic philosophy to maximize its entrapment for maximum penetration effect. Drug dispersion in sorbitan monostearate with different theoretical drug contents (TDC) were prepared. Products showed excellent micromeritics and actual drug content (ADC) increased by increasing TDC. The partition coefficient of the drug products showed huge improvement. This indicates the drug entrapped in the polar part of sorbitan monostearate as a special image which effects on the drug release. The drug permeation profiles from the different products are overlapped with nearly equal permeation parameters. The permeation results suggested the main driving force for improving the drug paracellular pathway is its dispersion in sorbitan monostearate and is independent of ADC. Pharmacodynamic of the products showed a significant improvement than the drug alone at p ˂ 0.05. ANOVA test indicated the insignificant pharmacodynamic difference between the low, middle, and high ADC of the products. An excellent correlation founded between the drug permeation and pharmacodynamic precents. Drug permeation driving force via the paracellular pathway is its entrapment in sorbitan monostearate and independent on ADC. The technique is simple and the products had excellent micromeritics., (© 2021. The Author(s).)

Candesartan cilexetil (CC) is an antihypertensive drug. It has low solubility and faces hepatic first-pass metabolism after oral ingestion. We formulated bioadhesive buccal films and studied the respective drug pharmacokinetics. Different bioadhesive films were prepared (40, 80, 120, 160, 200, and 240 mg CC per film) by using the solvent casting method. The drug concentrations used affect the drug entrapment mechanism, which was reflected in the film physicochemical properties like thickness, weight, drug content, bioadhesion, and drug release. Low drug concentration (F2, 40 mg per film) led to minute drug crystal dispersion while increasing the drug concentration (F7, 240 mg per film) showed drug crystal encapsulation, which affects the drug release. The drug pharmacokinetic from the prepared films was studied compared to the oral form by serial blood sampling via an inserted catheter in the carotid of rats. High-Performance Liquid Chromatography assay was used to measure the plasma concentration of CC in different forms. Compared to other films, the F2 showed the highest maximal concentration (Cmax) and the lowest elimination half-life (t 1/2 ). Bioadhesion buccal film of CC has better bioavailability, especially at low concentrations. The ease, robustness, and ruggedness of the preparation suggests the same procedure for drugs like CC.

Surfactants are well known as permeation enhancers. Span 60 microparticles encapsulating different concentrations of metformin HCl were prepared by using rapid congeal melting technique. Electro-scanning microscope showed smooth surface but less round microparticles. The actual drug content was nearly equal in the different particle sizes of the microparticles. Differential scanning calorimetry results indicated the molecular distribution of the drug molecules with no evidence of drug thermal degradation. The drug release profile from the microparticles has, in each case, burst and there was incomplete drug release. The drug partition coefficient is markedly enhanced as a result of its molecular dispersion in Span 60, indicating the increasing of the drug lipophilicity as a result of its encapsulation in the polar part of the surfactant. Non-everted sac was used to study the drug permeability after solving its critical points. Compared to pure drug, the permeability profile of the drug increased from the Span 60-encapsulated drug, with a total permeation of 68% and drug absorption enhancement of 253%. The drug permeation enhancement mechanism was suggested to be molecular dispersion in the matrix, which is emulsified by Tween 80, and this leads to increasing the hydrophilic paracellular pathway of the drug. Considering the emulsification system of the GIT, which emulsifies the Span 60 instead of Tween 80, a huge improvement of the biopharmaceutics classification system class III permeability and consequently bioavailability could be expected. In addition, this study will open the door to the use of the same technique for enhancing the drug absorption mechanisms by the paracellular pathway for rapid and complete pharmacological effect.