scholarly journals Comparison of Modern In Vitro Permeability Methods with the Aim of Investigation Nasal Dosage Forms

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 846
Author(s):  
Csilla Bartos ◽  
Piroska Szabó-Révész ◽  
Tamás Horváth ◽  
Patrícia Varga ◽  
Rita Ambrus
Keyword(s):  
Horizontal Cell ◽  
Systemic Circulation ◽  
High Viscosity ◽  
Dosage Forms ◽  
Vertical Diffusion ◽  
Franz Cell ◽  
Drug Permeability ◽  
Dissolution Tests ◽  
Semi Solid

Nowadays, the intranasal route has become a reliable alternative route for drug administration to the systemic circulation or central nervous system. However, there are no official in vitro diffusion and dissolution tests especially for the investigation of nasal formulations. Our main goal was to study and compare a well-known and a lesser-known in vitro permeability investigation method, in order to ascertain which was suitable for the determination of drug permeability through the nasal mucosa from different formulations. The vertical diffusion cell (Franz cell) was compared with the horizontal diffusion model (Side-Bi-Side). Raw and nanonized meloxicam containing nasal dosage forms (spray, gel and powder) were tested and compared. It was found that the Side-Bi-Side cell was suitable for the investigation of spray and powder forms. In contrast, the gel was not measurable on the Side-Bi-Side cell; due to its high viscosity, a uniform distribution of the active substance could not be ensured in the donor phase. The Franz cell, designed for the analysis of semi-solid formulations, was desirable for the investigation of nasal gels. It can be concluded that the application of a horizontal cell is recommended for liquid and solid nasal preparations, while the vertical one should be used for semi-solid formulations.

scholarly journals FORMULATION OF RIZATRIPTAN BENZOATE SUBLINGUAL TABLETS PREPARED BY DIRECT COMPRESSION WITH DIFFERENT BIOADHESIVE POLYMER: IN VITRO AND EX VIVO EVALUATION

2017 ◽  
Vol 10 (16) ◽  
pp. 36
Author(s):  
Harmanpreet Singh ◽  
Pooja Jaiswal ◽  
Suksham Gupta ◽  
Simerjit Singh
Keyword(s):  
Ex Vivo ◽  
Methyl Cellulose ◽  
Systemic Circulation ◽  
Direct Compression ◽  
Compression Process ◽  
Rizatriptan Benzoate ◽  
Dissolution Tests ◽  
Ex Vivo Permeation ◽  
Bioadhesive Polymers

  Objective: The current investigation deals with formulation and evaluation of fast disintegrating sublingual tablets of rizatriptan benzoate (RTB) to produce its intended therapeutic effect for acute treatment of migraine. When the drug is given by sublingual route, it overcomes the first pass metabolism and quick entry of drug in systemic circulation is obtained. It would result in fast pharmacological response hence faster relief from migraine which is an important criterion in migraine therapy.Methods: In this study, RTB sublingual tablets were prepared using direct compression process using various bioadhesive polymers such as sodium carboxymethyl cellulose, hydroxyl propyl methyl cellulose-K4M, and chitosan at various concentration ranging 0.5-5% w/w along with sodium starch glycolate (SSG) or cross carmellose sodium (CCS) as super disintegrants at different concentration ranging 2-8% w/w.Results: The tablets disintegrated quickly and dissolution tests conclude that RTB was released from the formulation within the compendial limits. The formulations batches (A8 and B8) containing 2% w/w chitosan along with 2% w/w SSG or CCS which disintegrate rapidly and show high dissolution and ex vivo permeation were selected as optimized formulations.Conclusion: The results obtained from the study showed that the bioavailability problem of the drug has been solved as the drug is given by sublingual route and it directly enters into systemic circulation. Furthermore, the formulation overcomes the problems associated with migraine attack as fast disintegrating technology is used.

scholarly journals Formulation Development and Evaluation of Fast Dissolving Oral Film of Midodrine Hydrochloride

2020 ◽  
Vol 10 (3-s) ◽  
pp. 107-110
Author(s):  
Aashish Marskole ◽  
Sailesh Kumar Ghatuary ◽  
Abhishek Parwari ◽  
Geeta Parkhe
Keyword(s):  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
Systemic Availability ◽  
Solvent Casting ◽  
Formulation Development ◽  
Casting Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Dissolution Tests

Oral fast dissolving midodrine hydrochloride films prepared by solvent casting method, PEG 400 was the selected plasticizers, incorporating superdisintegrants such as croscarmellose sodium (CCS) and sodium starch glycolate (SSG) to achieve the goal. Drug content, weight variability, film thickness, disintegration time, endurance, percentage of moisture content, and in vitro dissolution tests were analyzed for the prepared films. In all formulations, the tensile strength value was found from 0.965±0.045 and 1.256±0.032 and the folding capacity was over 100. The assay values ranged from 97.98±0.25 to 99.89±0.36 percent for all formulations. The disintegration time was ranging between 55±9 to 120±6 sec, the minimum time for disintegration was found in formulation F5 (55±9). The prepared F5 formulation shows greater release of the drug (99.25±0.41 percent) within 15 min relative to other formulations. As the drug having low solubility, fast disintegration may leads to more drug availability for dissolution, resulting in faster absorption in systemic circulation increased systemic availability of drug leads to quick onset of action which is prerequisite for hypertension. Keywords: Midodrine hydrochloride, Fast dissolving films, Solvent casting method, Superdisintegrants.

scholarly journals Assessment of “Sameness” and/or Differences between Marketed Creams Containing Miconazole Nitrate Using a Discriminatory in vitro Release Testing (IVRT) Method

2020 ◽  
Vol 88 (1) ◽  
pp. 6
Author(s):  
Potiwa Purazi ◽  
Seeprarani Rath ◽  
Ashmita Ramanah ◽  
Isadore Kanfer
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Vertical Diffusion ◽  
Discriminatory Ability ◽  
Miconazole Nitrate ◽  
Performance Verification Test ◽  
Semi Solid ◽  
Vitro Release ◽  
Release Testing

In vitro release testing (IVRT) provides an efficient method for the evaluation of drug release from semi-solid formulations. The aim of this research was to develop and validate a discriminatory IVRT system using vertical diffusion cells (VDCs) to assess generic topical products containing miconazole nitrate (MCZ). A comprehensive approach addressing all essential suitability criteria supporting the reliability of IVRT results was applied. These include mechanical validation of the VDCs, a performance verification test (PVT), validation of the analytical method (HPLC) used to quantify the drug release and validation of the IVRT method to confirm its precision, reproducibility, discriminatory ability, and robustness. Two marketed generic products were tested and assessed in accordance with the acceptance criteria for “sameness” in the FDA’s SUPAC-SS guidance which requires that the 90% confidence interval (CI) should fall within the limits of 75%–133.33%. One product was found to be in vitro equivalent to the reference product whereas the other was not. The results confirmed the suitability of the IVRT method to accurately measure the release of MCZ from topical cream products and, importantly, demonstrated the necessary discriminatory ability to assess “sameness”/differences of dermatological creams containing MCZ. Furthermore, the developed IVRT method was able to detect differences between formulations, which may be attributed to qualitative (Q1) and quantitative (Q2) properties and the microstructure and arrangement of matter (Q3).

scholarly journals The In-vitro studies and evaluation of telmisartan marketed tablets

2019 ◽  
Vol 9 (1) ◽  
pp. 74-78
Author(s):  
Jayendra Singh Bayas ◽  
Rameshwar Sanjabrao Cheke ◽  
Prachi Lokhande ◽  
Santosh Waghmare ◽  
Shivshankar Gunjegaonkar ◽  
...  
Keyword(s):  
Effective Means ◽  
Systemic Circulation ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Local Market ◽  
Dissolution Test ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Properties

Tablets or capsules taken orally remain one of the most effective means of treatment available. The effectiveness of such dosage forms relies on the drug dissolving in the fluids of the gastrointestinal tract prior to absorption into the systemic circulation. The present study reveals the evaluation of four marketed sample of Telmisartan tablets. The main aim of the study is to conduct dissolution test on the tablets to determine the compliance with a given official monograph. Four different marketed samples of Telmisartan were purchased from local market. The Telmisartan tablets were evaluated for the various in-vitro tablet properties such as thickness, hardness, friability, weight variation, drug content, disintegration time and dissolution rate. In-vitro dissolution test is conducted on four different brands of telmisartan tablets to assess their equivalency. All the four marketed samples of Telmisartan have shown good tablet properties and comply with the pharmacopoeial specification. The in- vitro dissolution showed the 80% drug release within one hour from all the four brands which complies with the specification of pharmacopoeia.

scholarly journals In Vitro Release Testing of Semi-Solid Dosage Forms

2017 ◽  
Vol 24 (3) ◽  
pp. 52-60 ◽  
Author(s):  
Isadore Kanfer ◽  
Seeprarani Rath ◽  
Potiwa Purazi ◽  
Nyengeterai Amanda Mudyahoto
Keyword(s):  
In Vitro Release ◽  
Dosage Forms ◽  
Solid Dosage Forms ◽  
Solid Dosage ◽  
Semi Solid ◽  
Vitro Release ◽  
Release Testing

Formulation and Evaluation of Bilayer Sustained Release Tablets of Salbutamol and Theophylline

2009 ◽  
Vol 2 (3) ◽  
pp. 638-646
Author(s):  
R. Nagaraju ◽  
Rajesh Kaza
Keyword(s):  
Ethyl Cellulose ◽  
Xanthan Gum ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Dissolution Studies ◽  
Sustained Release Tablets ◽  
Dissolution Apparatus ◽  
Single Dosage

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.

Nanocurcumin: A Double-Edged Sword for Microcancers

2020 ◽  
Vol 26 (45) ◽  
pp. 5783-5792
Author(s):  
Kholood Abid Janjua ◽  
Adeeb Shehzad ◽  
Raheem Shahzad ◽  
Salman Ul Islam ◽  
Mazhar Ul Islam
Keyword(s):  
Intracellular Signaling ◽  
Dosage Forms ◽  
The Body ◽  
In Vivo Studies ◽  
Mrna Levels ◽  
Anticancer Activities ◽  
Road Map ◽  
Anticancer Effects

There is compelling evidence that drug molecules isolated from natural sources are hindered by low systemic bioavailability, poor absorption, and rapid elimination from the human body. Novel approaches are urgently needed that could enhance the retention time as well as the efficacy of natural products in the body. Among the various adopted approaches to meet this ever-increasing demand, nanoformulations show the most fascinating way of improving the bioavailability of dietary phytochemicals through modifying their pharmacokinetics and pharmacodynamics. Curcumin, a yellowish pigment isolated from dried ground rhizomes of turmeric, exhibits tremendous pharmacological effects, including anticancer activities. Several in vitro and in vivo studies have shown that curcumin mediates anticancer effects through the modulation (upregulation and/or downregulations) of several intracellular signaling pathways both at protein and mRNA levels. Scientists have introduced multiple modern techniques and novel dosage forms for enhancing the delivery, bioavailability, and efficacy of curcumin in the treatment of various malignancies. These novel dosage forms include nanoparticles, liposomes, micelles, phospholipids, and curcumin-encapsulated polymer nanoparticles. Nanocurcumin has shown improved anticancer effects compared to conventional curcumin formulations. This review discusses the underlying molecular mechanism of various nanoformulations of curcumin for the treatment of different cancers. We hope that this study will make a road map for preclinical and clinical investigations of cancer and recommend nano curcumin as a drug of choice for cancer therapy.

scholarly journals Effect of temperature, CO2 and O2 on motility and mobility of Anisakidae larvae

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Aiyan Guan ◽  
Inge Van Damme ◽  
Frank Devlieghere ◽  
Sarah Gabriël
Keyword(s):  
Enzymatic Digestion ◽  
Infected Fish ◽  
Effect Of Temperature ◽  
Video Recordings ◽  
Different Temperatures ◽  
Semi Solid ◽  
Zoonotic Parasites ◽  
The Impact ◽  
Phosphate Buffered Saline

AbstractAnisakidae, marine nematodes, are underrecognized fish-borne zoonotic parasites. Studies on factors that could trigger parasites to actively migrate out of the fish are very limited. The objective of this study was to assess the impact of different environmental conditions (temperature, CO2 and O2) on larval motility (in situ movement) and mobility (migration) in vitro. Larvae were collected by candling or enzymatic digestion from infected fish, identified morphologically and confirmed molecularly. Individual larvae were transferred to a semi-solid Phosphate Buffered Saline agar, and subjected to different temperatures (6 ℃, 12 ℃, 22 ℃, 37 ℃) at air conditions. Moreover, different combinations of CO2 and O2 with N2 as filler were tested, at both 6 °C and 12 °C. Video recordings of larvae were translated into scores for larval motility and mobility. Results showed that temperature had significant influence on larval movements, with the highest motility and mobility observed at 22 ℃ for Anisakis spp. larvae and 37 ℃ for Pseudoterranova spp. larvae. During the first 10 min, the median migration of Anisakis spp. larvae was 10 cm at 22 ℃, and the median migration of Pseudoterranova spp. larvae was 3 cm at 37 ℃. Larval mobility was not significantly different under the different CO2 or O2 conditions at 6 °C and 12 ℃. It was concluded that temperature significantly facilitated larval movement with the optimum temperature being different for Anisakis spp. and Pseudoterranova spp., while CO2 and O2 did not on the short term. This should be further validated in parasite-infected/spiked fish fillets.

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