scholarly journals Investigation of biopharmaceutical drug properties suitable for orally disintegrating tablets

ADMET & DMPK ◽  
2016 ◽  
Vol 4 (4) ◽  
pp. 335 ◽  
Author(s):  
Asami Ono ◽  
Takumi Tomono ◽  
Takuo Ogihara ◽  
Katsuhide Terada ◽  
Kiyohiko Sugano

<span style="color: black; font-family: 'Calibri','sans-serif'; font-size: 10pt; mso-fareast-font-family: 'Times New Roman'; mso-bidi-font-family: 'Times New Roman'; mso-ansi-language: EN-GB; mso-fareast-language: DE; mso-bidi-language: AR-SA;" lang="EN-GB">The purpose of this study was to evaluate the biopharmaceutical drug properties suitable for orally disintegrating tablets (ODTs). The net charge at pH 7.4, log D<sub>6.5</sub>, the highest dose strength, solubility in water, dose number, and elimination t<sub>1/2</sub> of 57 ODT drugs and 113 drugs of immediate-release (IR) formulations were compared. These drugs were classified according to the Biopharmaceutical Classification System (BCS). A lower dose strength and a longer elimination t<sub>1/2</sub> have been observed as characteristic properties of ODTs. The proportion of basic drugs was higher in the ODTs than in the IR. A significant difference was not observed between the ODT and the IR formulation for log D<sub>6.5</sub>, solubility in water, and dose number. The distributions of the ODT and IR formulations among each BCS class were similar, suggesting that an ODT can be developed regardless of the BCS class of a drug</span>.

2020 ◽  
Vol 11 (7) ◽  
pp. 447-464
Author(s):  
Sally A Helmy ◽  
Heba M El-Bedaiwy ◽  
Soha M El-Masry

Aim: To study the impact of various permeability enhancers on fexofenadine bioavailability. Furthermore, to predict the potential effect of Cremophor® RH 40 on fexofenadine pharmacokinetics at higher doses using Biopharmaceutical Classification System criteria. Experimental methods: The effect of the dose increase (60–360 mg) on the dissolution and permeability behavior of fexofenadine-Cremophor RH 40 formulations was studied in humans. The Biopharmaceutical Classification System criteria of the drug was determined. Results & conclusion: Cremophor RH 40 improved the dissolution and bioavailability of fexofenadine. The pharmacokinetics increased linearly with the dose increase. Absorption number (An) was significantly increased after addition of Cremophor RH 40 in comparison to an unprocessed drug. Similar An values were observed throughout the same dose range. The dose number (D0) values were <1 whereas, all the dissolution number (Dn) values were >1 at the same dose level.


2021 ◽  
Vol 22 (11) ◽  
pp. 5514
Author(s):  
Francesca Truzzi ◽  
Camilla Tibaldi ◽  
Yanxin Zhang ◽  
Giovanni Dinelli ◽  
Eros D′Amen

Polyphenols are natural organic compounds produced by plants, acting as antioxidants by reacting with ROS. These compounds are widely consumed in daily diet and many studies report several benefits to human health thanks to their bioavailability in humans. However, the digestion process of phenolic compounds is still not completely clear. Moreover, bioavailability is dependent on the metabolic phase of these compounds. The LogP value can be managed as a simplified measure of the lipophilicity of a substance ingested within the human body, which affects resultant absorption. The biopharmaceutical classification system (BCS), a method used to classify drugs intended for gastrointestinal absorption, correlates the solubility and permeability of the drug with both the rate and extent of oral absorption. BCS may be helpful to measure the bioactive constituents of foods, such as polyphenols, in order to understand their nutraceutical potential. There are many literature studies that focus on permeability, absorption, and bioavailability of polyphenols and their resultant metabolic byproducts, but there is still confusion about their respective LogP values and BCS classification. This review will provide an overview of the information regarding 10 dietarypolyphenols (ferulic acid, chlorogenic acid, rutin, quercetin, apigenin, cirsimaritin, daidzein, resveratrol, ellagic acid, and curcumin) and their association with the BCS classification.


2016 ◽  
Vol 33 (S1) ◽  
pp. S158-S158
Author(s):  
M. Polikowska ◽  
B. Łoza

IntroductionThe growing rate of depressive disorders causes needs for more effective and more innovative solutions. The modern patients’ challenges make them fail mostly in the treatment compliance. Some reports have described that escitalopram orally disintegrating tablets (ODT) induce faster response and lower dropout rate than oral standard tablets (OST), although both forms have equal bioavailability.AimWe tried to clarify effectiveness rates between escitalopram ODT and OST treatments in depressive patients.MethodAn open-label, 6-month, randomized, flexible-dose study was conducted for direct comparison of the effects of escitalopram ODT (N16) and OST (N15) on dropout rate and clinical outcomes in patients with major depression.ResultsOutcome measures included Hamilton Depression Rating Scale (HDRS), Drug Attitude Inventory-10 (DAI), Clinical Global Improvement Scale (CGI), and Psychological General Well-Being Scale (PGWB). The tolerability was assessed by the UKU scale. No significant difference was found in HDRS, CGI, PGWB and GAF between the two forms of tablets. No significant difference was found in any tolerability rates. However, dropout rate favored escitalopram ODT group (N5, 31.3%) vs escitalopram OST (N7, 47.0%). DAI-10 outcomes, both in patients’ general attitude and subjective feelings, were significantly improved in ODT group (P = 0.000), comparing with OST.DiscussionEscitalopram in its classical form (OST) has become a leader in a group of antidepressants, thanks to safety of use, efficacy and tolerability. In the ODT form, escitalopram can meet additional needs, both clinical and lifestyle. ODT may reduce dropout rate and costs of long-term treatment improving the patients’ compliance.Disclosure of interestThe authors have not supplied their declaration of competing interest.


2011 ◽  
Vol 17 (1) ◽  
Author(s):  
Tyler T. Yu ◽  
Miranda M. Zhang

<p class="MsoNormal" style="text-align: justify; margin: 0in 37.8pt 0pt 0.5in; mso-pagination: none;"><span style="font-family: &quot;CG Times&quot;,&quot;serif&quot;; mso-bidi-font-style: italic;"><span style="font-size: x-small;">This paper discusses the per-capita consumption of imports aspect of international trade.<span style="mso-spacerun: yes;">&nbsp; </span>A research hypothesis is tested to investigate if there is a significant difference among G-7 countries in per-capita consumption of imports and the implication of the testing results for the U.S. - Japan bilateral trade deficit.<span style="mso-spacerun: yes;">&nbsp; </span>The results of the ANOVA and the Kruskal-Wallis test yield insignificant variation in per-capita consumption of imported goods/services among the G-7 countries.<span style="mso-spacerun: yes;">&nbsp; </span>The study recapitulates the reason(s) for the U.S. trade deficit with Japan and essentially states that factors other than trade barriers and restrictions cause the U.S. trade deficit with Japan.<span style="mso-spacerun: yes;">&nbsp; </span>While this result may initially seem counterintuitive and inconsistent with popular wisdom, it may actually help uncover the true causes for the sustained trade deficit with Japan.</span></span></p>


2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Annika Lundkvist Josenby ◽  
Tomasz Czuba ◽  
Ann I. Alriksson-Schmidt

Abstract Background In the Swedish population-based follow-up program and national quality registry for individuals with cerebral palsy (CPUP), physiotherapy (PT) and occupational therapy (OT) treatments are regularly recorded along with functional status. By Swedish law, all citizens irrespective of personal characteristics or socioeconomic status, have the right to receive healthcare and medical treatments as applicable. Previous research has shown gender differences in treatments and interventions received by children with cerebral palsy (CP). The purpose of this study was to examine differences in treatments and interventions by gender and place of birth in children and adolescents participating in CPUP. Methods This was a cross-sectional registry study. Data from the latest PT (n = 2635) and OT assessment forms (n = 3480) in CPUP were extracted for individuals aged 0–17 years. Logistic regressions were used to assess the relationships between the outcome variables and gender and place of birth (including an interaction term gender X place of birth), adjusted for age, Gross Motor Function Classification System (GMFCS) levels and spasticity scores for PT interventions and Manual Ability Classification System (MACS) for OT interventions. Results Results are presented as odds ratios [95% confidence intervals] and p-values. Girls were significantly more likely to have spinal braces than boys; 1.54 [1.07, 2.22] p < 0.05, a significant interaction with place of birth indicated fewer spinal braces prescribed to children born outside of the Nordic countries; 0.20 [0.079, 0.53] p < 0.001. Girls were less likely to have undergone selective dorsal rhizotomy (SDR); 0.49 [0.25, 0.94] p < 0.05. Individuals born outside of the Nordic countries, were significantly less likely to have received intrathecal baclofen (ITB) 0.27 [0.074, 0.98] p < 0.05. Conclusions Of the treatments prescribed, gender differences were observed for spinal braces and having undergone SDR. A statistically significant difference based on place of birth was noted for spinal bracing and having received ITB treatment. Other PT and OT treatments were associated with age, level of spasticity, and functional severity as classified using the GMFCS and the MACS. Increased awareness of differences based on gender, and where a child is born, could be obtained by inter- and intraprofessional discussions.


2020 ◽  
Vol 28 (2) ◽  
pp. 230949902092416
Author(s):  
İsmail Demirkale ◽  
Yüksel Uğur Yaradılmış ◽  
Ahmet Ateş ◽  
Murat Altay

Purpose: Total hip arthroplasty (THA) for high-riding hips is a complex procedure and the requirement for subtrochanteric osteotomy (STO) is an important decision that needs to be taken preoperatively. STO renders this complex surgery even more complicated and there are no guidelines to determine the STO requirement. In this study, the outcomes of THA for patients with high-riding hips were evaluated and a practical classification system is proposed to predict any osteotomy requirement. Methods: A retrospective evaluation was made of 79 hips of 76 patients who underwent THA for high-riding hip dysplasia. The amount of shortening in patients with STO and in patients without STO was compared. All patients were evaluated in respect of Harris hip score, operating time, erythrocyte suspension need, and actual limb length discrepancy. Preoperative radiographs were classified into four types according to the ratio of the distance between the lesser trochanter and the ischial tuberosity with pelvic height (LT-IT/P) to grade the degree of dislocation. Results: The mean follow-up was 30 ± 6.54 months. STO was applied to 47 (60%) hips and not to 32 (40%). There was no statistically significant difference between the groups in respect of the functional scores. STO prolonged the operating time and increased the need for blood transfusion ( p = 0.026, p < 0.001, respectively). When the LT-IT/P index was <0.19 (type 1), no additional surgical approach was required for reduction, at 0.19–0.29 (type 2), the head can be safely reduced with additional reduction methods, and when >0.3 (type 3), a shortening osteotomy will most likely be required. The rate of complications is increased if LT-IT/P is >0.4 (type 4). Conclusion: STO adjunct to THA increases the rate of complications. This practical classification system may guide the surgeon in the decision of whether an STO should be added to the procedure or not. Level of evidence: Level III, clinical trial


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