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Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 184
Michael Schütt ◽  
Connor O’Farrell ◽  
Konstantinos Stamatopoulos ◽  
Caroline L. Hoad ◽  
Luca Marciani ◽  

The performance of solid oral dosage forms targeting the colon is typically evaluated using standardised pharmacopeial dissolution apparatuses. However, these fail to replicate colonic hydrodynamics. This study develops a digital twin of the Dynamic Colon Model; a physiologically representative in vitro model of the human proximal colon. Magnetic resonance imaging of the Dynamic Colon Model verified that the digital twin robustly replicated flow patterns under different physiological conditions (media viscosity, volume, and peristaltic wave speed). During local contractile activity, antegrade flows of 0.06–0.78 cm s−1 and backflows of −2.16–−0.21 cm s−1 were measured. Mean wall shear rates were strongly time and viscosity dependent although peaks were measured between 3.05–10.12 s−1 and 5.11–20.34 s−1 in the Dynamic Colon Model and its digital twin respectively, comparable to previous estimates of the USPII with paddle speeds of 25 and 50 rpm. It is recommended that viscosity and shear rates are considered when designing future dissolution test methodologies for colon-targeted formulations. In the USPII, paddle speeds >50 rpm may not recreate physiologically relevant shear rates. These findings demonstrate how the combination of biorelevant in vitro and in silico models can provide new insights for dissolution testing beyond established pharmacopeial methods.

2022 ◽  
Marilyn N. Martinez ◽  
Mark G. Papich ◽  
Raafat Fahmy

Many gaps exist in our understanding of species differences in gastrointestinal (GI) fluid composition and the associated impact of food intake and dietary composition on in vivo drug solubilization. This information gap can lead to uncertainties with regard to how best to formulate pharmaceuticals for veterinary use or the in vitro test conditions that will be most predictive of species-specific in vivo oral product performance. To address these challenges, this overview explores species-specific factors that can influence oral drug solubility and the formulation approaches that can be employed to overcome solubility-associated bioavailability difficulties. These discussions are framed around some of the basic principles associated with drug solubilization, reported species differences in GI fluid composition, types of oral dosage forms typically given for the various animal species, and the effect of prandial state in dogs and cats. This basic information is integrated into a question-and-answer section that addresses some of the formulation issues that can arise in the development of veterinary medicinals.

2022 ◽  
Vol 34 (2) ◽  
pp. 383-388
Gayatri Joshi ◽  
Abhishek Tiwari ◽  
Prashant Upadhyay

Piperine is classified as a class II drug in the biopharmaceutical classification system due to its low aqueous solubility. As a result, piperine herbosomes were created to improve the dissolution rate and in vivo liver protecting activity of piperine and physico-chemical characteristics were used to confirm herbosome formation. The piperine-herbosome formulation revealed spherical particle size of all formulations from P1-P10 and found142.4 ± 0.98 nm for best piperine-herbosome formulation (P2) and a PDI value of 0.237, indicating a homogeneous population of piperine loaded vesicles. In vitro drug release rate and percent entrapment efficiency were determined for all formulations P1-P25 and found to be 95.306 ± 0.21 and 97.306 ± 0.65 in 12 h, respectively for best piperine-herbosome formulation (P2). It exemplifies the complex’s long-term releasing capability. This information suggests that it may have a longer retention time inside the body, extending the duration of effect. The antioxidant potential of pure piperine was determined using the DPPH scavenging method, with an IC50 value of 107.59 ± 0.11 g/mL compared to a formulation with an IC50 value of 93.926 ± 0.03 g/mL. Swiss albino mice of either sex were utilized for the evaluation of hepatoprotective activity. On the 8th day, the hepatotoxicity was caused by giving a single oral dosage of CCl4 (0.5 mL) and the parameters were evaluated on the 9th day. This formulation has the best optimized based on drug content and drug entrapment. Serum glutamic oxaloacetic transaminase (SGOT), serum glutamic-pyruvic transaminase (SGPT), alkaline phosphatase (ALP) and total bilirubin were among the biochemical markers measured. In comparison to normal control (161 ± 0.31 IU/L, 52.78 ± 0.28 IU/L, 121.12 ± 0.14 IU/L and 0.633 ± 1.44 IU/L) and P2 formulation (163.23 ± 0.49 IU/L, 66.9 ± 0.05 IU/L, 128.3 ± 1.15 IU/L and 0.645 ± 0.67 IU/L respectively).

Mangesh Pradeep Kulkarni ◽  
Arun Sharma ◽  
Sagar Tanwar ◽  
Parashara Bhattar Vandana ◽  
Sheetu Wadhwa ◽  

Abstract: Pharmaceutical oral dosage forms are tremendously preferred by both consumers as well as pharmaceutical manufacturers owing to the plethora of benefits they offer. Lozenges (LZs) are one of the dosage forms that provide a palatable means of drug administration and have great importance with respect to their pharmaceutical applications. LZs offer additional benefits to pediatric and geriatric patients, along with people having associated problems with the gastro-intestinal tract. Dysphagia is a common problem faced by all age groups, which gives rise to the need for LZs. Moreover, the foremost merit presented by the medicated LZs includes its augmented retention time in the oral cavity that results in an enhanced bioavailability for buccal or upper gastro-intestinal disorders. Further, LZs can also be used to bypass the first-pass effect. The present review covers various aspects of LZs such as formulation, manufacturing techniques, evaluation parameters, marketed products, patents, and a compilation of research work that has been done on lozenges as a delivery system.

2021 ◽  
Vol 9 (12) ◽  
pp. 136-146
P. Santosh Kumar ◽  
Wuchen a ◽  
Wang Lei ◽  
Zaheer Abbas ◽  

A simple, accurate, precise and rapid stability indicating reverse phase High performance chromatography method was used for estimation of Telmisartan and Hydrochlorothiazide in bulk and fixed-dose combination solid oral dosage form. The proposed analytical method has been validated for specificity, Linearity, Accuracy, Precision and Robustness. The chromatography was achieved in a GL science, Inertsil C8 (Length 125x Diameter 4.0mm Particle size 5µm) column with gradient flow. The optimal chromatographic condition consisted of mobile phase pH 3.0 at a flow rate of 1.2mL/min, with a column temperature of 40°C, run time 14 minutes and detector wavelength of 270nm.

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Mohammadali Poursharifi Ghourichay ◽  
Seyed Hossein Kiaie ◽  
Ali Nokhodchi ◽  
Yousef Javadzadeh

Orally disintegrating tablets (ODTs) rapidly disintegrate or dissolve in the oral cavity without using water. Demand for ODTs has increased, and the field has overgrown in the pharmaceutical industry and academia. It is reported that ODTs have several advantages over other conventional tablets. Since some of them are absorbed from the mouth, pharynx, and esophagus as the saliva passes down into the stomach, in such cases, the bioavailability of the drug improves meaningfully. Furthermore, the immediate release property of ODTs makes them a popular oral dosage form in patients with swallowing challenges, children, and for cases with a need for rapid onset of action. The current review article explains the features of active ingredients and excipients used in the formulation of ODTs, discusses multiple ODT formulation and preparation techniques with their merits and demerits, and also, offers remedies for problems associated with ODTs. Moreover, quality control steps and required considerations are presented.

P.B. Savant ◽  
M.A. Qureshi ◽  
Kshirsagar N. ◽  
Manjusha Kareppa ◽  
Avinash B Thalkari ◽  

The oral dosage forms are the most popular way of taking medicine although having some disadvantages like deliberate absorption and thus onset of action is extend. This can be overcome by administrating the drug in a liquid form i.e. effervescent tablet. The research is a formulation of diclofenac sodium as a effervescent tablet by wet granulation method. The bitter taste of the drug are masked by added sweetening agent (lactose, glucose etc.) In the present work we are prepared effervescent tablet in that we are used active drug diclofenac sodium and other active ingredient acid like tartaric acid and base sodium bicarbonate in different concentrations. The formulation of tablet was done by using wet granulation, wet granulation is found to be acceptable method of effervescent tablet formulation. The various pre-formulation studies was performed hardness, weight variation, disintegration, dissolution etc.

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 2
Abdulrahman Alshadidi ◽  
Ahmad Abdul-Wahhab Shahba ◽  
Ibrahim Sales ◽  
Md Abdur Rashid ◽  
Mohsin Kazi

Background: The current study aimed to design a novel combination of lansoprazole (LNS) and curcumin (CUR) solid oral dosage form using bioactive self-nanoemulsifying drug delivery systems (Bio-SSNEDDS). Methods: Liquid SNEDDS were prepared using the lipid-excipients: Imwitor988 (cosurfactant), Kolliphor El (surfactant), the bioactive black seed (BSO) and/or zanthoxylum rhetsa seed oils (ZRO). Liquid SNEDDS were loaded with CUR and LNS, then solidified using commercially available (uncured) and processed (cured) Neusilin® US2 (NUS2) adsorbent. A novel UHPLC method was validated to simultaneously quantify CUR and LNS in lipid-based formulations. The liquid SNEDDS were characterized in terms of self-emulsification, droplet size and zeta-potential measurements. The solidified SNEDDS were characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), scanning electron microscopy (SEM), in vitro dissolution and stability in accelerated storage conditions. Results: Liquid SNEDDS containing BSO produced a transparent appearance and ultra-fine droplet size (14 nm) upon aqueous dilution. The solidified SNEDDS using cured and uncured NUS2 showed complete solidification with no particle agglomeration. DSC and XRD confirmed the conversion of crystalline CUR and LNS to the amorphous form in all solid SNEDDS samples. SEM images showed that CUR/LNS-SNEDDS were relatively spherical and regular in shape. The optimized solid SNEDDS showed higher percent of cumulative release as compared to the pure drugs. Curing NUS2 with 10% PVP led to significant enhancement of CUR and LNS dissolution efficiencies (up to 1.82- and 2.75-fold, respectively) compared to uncured NUS2-based solid SNEDDS. These findings could be attributed to the significant (50%) reduction in the micropore area% in cured NUS2 which reflects blocking very small pores allowing more space for the self-emulsification process to take place in the larger-size pores. Solid SNEDDS showed significant enhancement of liquid SNEDDS stability after 6 months storage in accelerated conditions. Conclusions: The developed Bio-SSNEDDS of CUR and LNS using processed NUS2 could be used as a potential combination therapy to improve the treatment of peptic ulcers.

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