scholarly journals Influence of Different Dosage Forms on Pharmacokinetics of 6 Alkaloids in Raw Aconiti Kusnezoffii Radix (Caowu) and Chebulae Fructus- (Hezi-) Processed Caowu by UPLC-MS/MS

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Meiru Zhi ◽  
Kaiyang Liu ◽  
Shu Han ◽  
Jinkai Xu ◽  
Weifei Li ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Dosage Form ◽  
Dosage Forms ◽  
Pharmacokinetic Parameters ◽  
Intragastric Administration ◽  
Diterpenoid Alkaloids ◽  
Time Points ◽  
Traditional Mongolian Medicine

Purpose. To study the pharmacokinetics of the 6 alkaloids (aconitine, mesaconitine, hypaconitine, benzoylaconine, benzoylmesaconine, and benzoylhypaconine) in raw Aconiti Kusnezoffii Radix (Caowu) (RC) and Chebulae Fructus- (Hezi-) processed Caowu (HC) in the rats being, respectively, administrated with RC and HC in the dosage forms of powder and decoction and to demonstrate the mechanism of detoxification of HC. Methods. The rats were randomly divided into 4 groups and, respectively, given RC powder, HC powder, RC decoction, and HC decoction by intragastric administration. The contents of the 6 alkaloids in the plasma of the rats were detected at different time points by the UPLC-MS/MS method, and DAS 3.2.7 software was used to calculate, compare, and analyze the detected pharmacokinetic parameters. Results. Compared with those of the RC powder, the values of AUC0‐t and Cmax of the HC powder were all reduced, whereas the values of t1/2z and Tmax were mostly increased. Compared with those of the RC powder, the values of AUC0‐t, Cmax, and t1/2z of the RC decoction were decreased and the value of Tmax of the RC decoction was increased. Compared with those of the RC decoction, the values of AUC0‐t, t1/2z, and Cmax of the diester diterpenoid alkaloids of the HC decoction were all increased. However, there was no marked difference between the pharmacokinetic parameters of the HC powder and the HC decoction. Conclusions. A decrease in the level of absorption and in the rate of elimination of the alkaloids can be detected when HC is administrated in the dosage form of the powder, explaining that in traditional Mongolian medicine (TMM), the purpose of using HC in the dosage forms of pills and powder is for decreasing the toxicity and prolonging the efficacy duration of HC. Decocting can greatly decrease the plasma concentration of the diester diterpenoid alkaloids in RC and increase their rate of elimination. The influence of decocting on RC is greater than that on HC, explaining the rationality of the steaming and boiling methods for processing Caowu and the rationality of boiling Caowu for a longer time beforehand in preparing an herb decoction containing Caowu in TCM.

Effects of Acupuncture at St36 on Pharmacokinetics of Schisandra lignans in rats

2015 ◽  
Vol 33 (3) ◽  
pp. 223-229 ◽  
Author(s):  
De Ji ◽  
Ziwan Ning ◽  
Chunqin Mao ◽  
Yong Sun ◽  
Jing Liu ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Study Groups ◽  
Acupuncture Group ◽  
Pharmacokinetic Parameters ◽  
Intragastric Administration ◽  
Schisandrin B ◽  
Time Curve ◽  
Acupuncture Stimulation ◽  
Concentration Time ◽  
Plasma Concentration Time Curve

Objective To investigate the influence of acupuncture at ST36 on the pharmacokinetics of Schisandra lignans including schisandrin, deoxyschisandrin and schisandrin B after intragastric administration of Schisandra chinensis (SC) in rats. Methods Twelve male Sprague-Dawley rats were randomly divided into two study groups: SC and SC+acupuncture. Rats in both groups received intragastric SC extract at 5.0 g/kg. Rats in the SC+acupuncture group additionally received acupuncture stimulation at ST36 for 30 min after SC administration. Acupuncture needles were rotated bilaterally for 1 min, left in situ for 20 min, then electrically stimulated for 10 min at 50 Hz frequency and 1–3 mA intensity. A sensitive and specific high performance liquid chromatography electrospray tandem mass spectrometry procedure was developed and validated for simultaneous analysis of three bioactive lignans (schisandrin, deoxyschisandrin and schisandrin B) in rat plasma. Results There were significant differences (p<0.05) between the two study groups in various pharmacokinetic parameters. Area under the plasma concentration–time curve (AUC0–t), area under the plasma concentration–time curve to time infinity (AUC0–∞) and peak plasma concentration (Cmax) for schisandrin, absorption half-life (T1/2α) and AUC0–t for deoxyschisandrin, and Cmax for schisandrin B were increased in the SC+acupuncture group compared with the SC group. T1/2α for schisandrin B only and time to peak concentration (Tmax) for all three lignans were reduced following acupuncture. Conclusions Acupuncture stimulation at ST36 affects the pharmacokinetics of SC in rats. Acupuncture may have a beneficial role in promoting the absorption of lignans from extracts of SC.

Spectrophotometric Determination of Alendronate Sodium by using Sodium-1,2-Naphthoquinone-4-Sulphonate

2012 ◽  
Vol 4 (4) ◽  
pp. 1563-1568
Author(s):  
Sagar Suman Panda ◽  
Ravi Kumar B V V ◽  
D Patanaik
Keyword(s):  
Spectrophotometric Method ◽  
Absorption Maximum ◽  
Dosage Form ◽  
Dosage Forms ◽  
Alendronate Sodium ◽  
Colored Complex ◽  
Pharmaceutical Dosage Forms ◽  
Recovery Study ◽  
Assay Conditions

A simple, precise and accurate spectrophotometric method was developed for analysis of the osteoporesis drug alendronate sodium (ALS). The method is based on reaction of the drug with sodium-1,2-naphthoquinone-4-sulphonate (NQS) in presence of alkali to form a brown colored complex giving absorption maximum at 525 nm. The drug obeyed Beer’s law in the range of 5-70 µg/ml with a correlation coefficient of 0.999. The LOD and LOQ values are 1.7 µg/ml and 5.0 µg/ml, respectively. The average recoveries for recovery study were found to be in the range of 99.37%-100.46%. The R.S.D. values for intraday and inter-day precision were found to be 0.48 and 0.62, respectively. The optimized assay conditions were applied successfully for determination of ALS in pharmaceutical dosage forms. No interference was observed from the excipients present in the dosage form. The method is statistically validated as per the ICH requirements.  

Development of Innovative Orally Fast Disintegrating Film Dosage Forms: A Review

2012 ◽  
Vol 5 (2) ◽  
pp. 1666-1674 ◽  
Author(s):  
Bibhu Prasad Panda ◽  
N.S Dey ◽  
M.E.B. Rao
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Dosage Form ◽  
Geriatric Patients ◽  
Dosage Forms ◽  
Delivery Systems ◽  
Design And Development ◽  
Innovative Drug ◽  
Potential Benefits ◽  
Pharmaceutical Industries

Over the past few decades, there has been an increased interest for innovative drug delivery systems to improve safety, efficacy and patient compliance, thereby increasing the product patent life cycle. The discovery and development of new chemical entities is not only an expensive but also time consuming affair. Hence the pharmaceutical industries are focusing on the design and development of innovative drug delivery systems for existing drugs. One such delivery system is the fast disintegrating oral film, which has gained popularity among pediatric and geriatric patients. This fast disintegrating film with many potential benefits of a fast disintegrating tablet but devoid of friability and risk of choking is more acceptable to pediatric and geriatric patients. Formulation of fast disintegrating film can be achieved by various techniques, but common methods of preparation include spraying and casting. These film forming techniques use hydrophilic film former in combination with suitable excipients, which allow the film to disintegrate or dissolve quickly in the mouth within a few seconds without the administration of water. In view of the advantages of the fast disintegrating films over the fast disintegrating tablets and other dosage forms, it has the potential for commercial exploitation. The oral film dosage form not only has certain advantages of other fast disintegrating systems but also satisfies the unmet needs of the market. The present review emphasizes on the potential benefits, design and development of robust, stable, and innovative orally fast- disintegrating films and their future scenarios on a global market as a pharmaceutical dosage form.  

An Overview of Excipients Classification and Their Use in Pharmaceuticals

2020 ◽  
Vol 16 ◽  
Author(s):  
Cansel Kose Ozkan ◽  
Ozgur Esim ◽  
Ayhan Savaser ◽  
Yalcin Ozkan
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Dosage Form ◽  
Dosage Forms ◽  
Design Development ◽  
Pharmaceutical Dosage Form ◽  
Pharmaceutical Dosage Forms ◽  
Product Identification ◽  
Direct Administration ◽  
Active Substances

: The content and the application of pharmaceutical dosage forms must meet several basic requirements to ensure and maintain efficiency, safety and quality. A large number of active substances have limited ability to direct administration. Excipients are generally used to overcome the limitation of direct administration of these active substances. However, the function, behavior and composition of the excipients need to be well known in the design, development and production of pharmaceutical dosage forms. In this review, excipients used to assist in any pharmaceutical dosage form production processes of drugs, to preserve, promote or increase stability, bioavailability and patient compliance, to assist in product identification / separation, or to enhance overall safety and effectiveness of the drug delivery system during storage or use are explained. Moreover, the use of these excipients in drug delivery systems are identified. Excipient toxicity, which is an issue discussed in the light of current studies, also discussed in this review.

scholarly journals Updated List of Light-Sensitive Oral Medications

2019 ◽  
Vol 55 (6) ◽  
pp. 349-365
Author(s):  
Scott Perkins ◽  
Adam Evans ◽  
Allison King
Keyword(s):  
Dosage Form ◽  
Drug Information ◽  
Dosage Forms ◽  
Drug Products ◽  
Solid Dosage ◽  
Oral Medications ◽  
Information Center ◽  
Oral Liquid ◽  
Liquid Products ◽  
Professional Resources

The Campbell University Drug Information Center supports health professionals by providing responses to drug-related inquiries. An inquiry was received by the Drug Information Center for a comprehensive list of oral solutions which should be protected from light. In investigating this request for information, a list of light-sensitive oral prescription drug products published in Hospital Pharmacy in 2009 was identified. This discovery highlighted the need for both an updated list and one which distinguished oral solid products and oral liquid products. The purpose of this project was to update the previously published list and to distinguish between oral solid and liquid dosage forms. The process of updating this list entailed several professional resources. A list of all oral products was obtained and then sorted to clearly identify which products were available in oral solid dosage form only, oral liquid dosage form only, and both dosage forms. Once delineated, the product labels for each medication were scoured for language indicating the product is light sensitive.

scholarly journals Variable Absorption of Clavulanic Acid After an Oral Dose of 25 mg/kg of Clavubactin® and Synulox® in Healthy Cats

2002 ◽  
Vol 2 ◽  
pp. 1369-1378 ◽  
Author(s):  
Tom B. Vree ◽  
Eric Dammers ◽  
Eri van Duuren
Keyword(s):  
Single Dose ◽  
Plasma Concentration ◽  
Oral Dose ◽  
Clavulanic Acid ◽  
Phase I Study ◽  
Pharmacokinetic Parameters ◽  
High Efficacy ◽  
Dose Ratio ◽  
Concentration Time ◽  
Crossover Phase

The aims of this investigation were to calculate the pharmacokinetic parameters and to identify parameters, based on individual plasma concentration-time curves of amoxicillin and clavulanic acid in cats, that may govern the observed differences in absorption of both drugs. The evaluation was based on the data from plasma concentration-time curves obtained following a single-dose, open, randomised, two-way crossover phase-I study, each involving 24 female cats treated with two Amoxi-Clav formulations (formulation A was Clavubactin® and formulation was B Synulox® ; 80/20 mg, 24 animals, 48 drug administrations). Plasma amoxicillin and clavulanic acid concentrations were determined using validated bioassay methods. The half-life of elimination of amoxicillin is 1.2 h (t1/2= 1.24 ± 0.28 h, Cmax= 12.8 ± 2.12 μg/ml), and that of clavulanic acid 0.6 h (t1/2= 0.63 ± 0.16 h, Cmax= 4.60 ± 1.68 μg/ml). There is a ninefold variation in the AUCtof clavulanic acid for both formulations, while the AUCtof amoxicillin varies by a factor of two. The highest clavulanic acid AUCtvalues indicate the best absorption; all other data indicate less absorption. Taking into account that the amoxicillin–to–clavulanic acid dose ratio in the two products tested was 4:1, the blood concentration ratios may actually vary much more, apparently without compromising the products’ high efficacy against susceptible microorganisms.

scholarly journals A REVIEW: ANTI-CANCER NATURAL PRODUCT DRUG DELIVERY SYSTEM DOSAGE FORM AND EVALUATION

2021 ◽  
pp. 41-51
Author(s):  
RIZKA KHOIRUNNISA GUNTINA ◽  
IYAN SOPYAN ◽  
ADE ZUHROTUN
Keyword(s):  
Drug Delivery ◽  
Natural Product ◽  
Drug Delivery System ◽  
Delivery System ◽  
Dosage Form ◽  
Dosage Forms ◽  
Primary Data ◽  
Pharmaceutical Dosage Form ◽  
New Drug

A drug delivery system is a system in which a drug is released from a pharmaceutical dosage form to achieve the desired pharmacological effect. The system consists of conventional and new drug delivery systems. In the new drug delivery system, polymers are used as a matrix. The aim of this article is to find out and understand the formulation and evaluation of natural ingredients that have anticancer activity with different dosage forms and the basis for developing these dosages. Journal searches in this review came from primary data sources on the internet. Journal searches were carried out using a search engine such as Google Scholar, PubMed, and ScienceDirect. In recent years, natural products, such as extract, fraction, and isolate, are getting attention to help treat cancer. Because of their low solubility and bioavailability, the effectiveness tends to be lower than synthetic drugs. Therefore, a dosage form with a new drug delivery system was made to overcome the problem. The dosage forms commonly made are patch, suspension, powder, and emulsion with a new drug delivery system. To ensure the product that has been made met the requirements, they need to be evaluated with various methods like In vitro Study, morphology study, particle size study, and others. Cancer treatment using the natural product can be delivered through several dosage forms like patch, suspension, powder, and emulsion, with specific formulation and manufacturing methods based on several considerations such as natural ingredients properties, dosage form selection, excipient properties, and the purpose of the formulation. Dosage forms that has been made are then evaluated using several evaluation methods.

Effects of oral administration of ticagrelor on the plasma level of adrenaline, histamine, serotonin, and acetylcholine in rat

2020 ◽  
Author(s):  
Xiuling Yang ◽  
Xue Guo ◽  
Li Yanan ◽  
Li Jiaxi ◽  
Liu Yue
Keyword(s):  
Acute Coronary Syndrome ◽  
Plasma Concentration ◽  
Plasma Level ◽  
Adverse Reactions ◽  
Statistical Significance ◽  
Loading Dose ◽  
Time Points ◽  
Coronary Syndrome ◽  
P2y12 Receptor Antagonist ◽  
First Time

Abstract Background: Ticagrelor as a reversible P2Y12 receptor antagonist which plays an important role in the treatment of acute coronary syndrome (ACS). Dyspnea is one of the main adverse reactions of ticagrelor, however the mechanism is not clearly now. The aim of this study was to assess the possible relationship between ticagrelor-related dyspnea and some neurotransmitter in plasma which can contract the bronchial smooth muscle.Methods: The effects of ticagrelor on the plasma level of adrenaline, histamine, serotonin, and acetylcholine was studied in rats. Ticagrelor was administered at a loading dose of 24 mg/kg for the first time, and then maintenance dose 12 mg/kg, twice a day for 6 days. The plasma level of adrenaline, histamine, serotonin, and acetylcholine was determined by LC-MS/MS.Results: The plasma level of serotonin increased after ticagrelor administrating, especially at 1.5h ( p <0.05) reach the level of statistical significance. The level of serotonin in plasma was consistent with ticagrelor blood concentration. Meanwhile, ticagrelor can cause a decrease in the plasma concentration of histamine, and the change was statistically significant at time points of 1.5h, 3.5h and 10.5h respectively. The concentration of the adrenaline and acetylcholine had no change.Conclusions: The results of this study reveal that ticagrelor can increases blood serotonin levels and this may be a cause of dyspnea ticagrelor-related.

scholarly journals Embedded 3D Printing of Novel Bespoke Soft Dosage Form Concept for Pediatrics

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 630 ◽  
Author(s):  
Katarzyna Rycerz ◽  
Krzysztof Adam Stepien ◽  
Marta Czapiewska ◽  
Basel T. Arafat ◽  
Rober Habashy ◽  
...  
Keyword(s):  
Dosage Form ◽  
Drug Loading ◽  
Three Dimensional ◽  
Dosage Forms ◽  
Dose Titration ◽  
Step Method ◽  
Needle Size ◽  
Model Drug ◽  
Semi Solid ◽  
The Impact

Embedded three-dimensional printing (e-3DP) is an emerging method for additive manufacturing where semi-solid materials are extruded within a solidifying liquid matrix. Here, we present the first example of employing e-3DP in the pharmaceutical field and demonstrate the fabrication of bespoke chewable dosage forms with dual drug loading for potential use in pediatrics. LegoTM-like chewable bricks made of edible soft material (gelatin-based matrix) were produced by directly extruding novel printing patterns of model drug ink (embedded phase) into a liquid gelatin-based matrix (embedding phase) at an elevated temperature (70 °C) to then solidify at room temperature. Dose titration of the two model drugs (paracetamol and ibuprofen) was possible by using specially designed printing patterns of the embedded phase to produce varying doses. A linearity [R2 = 0.9804 (paracetamol) and 0.9976 (ibuprofen)] was achieved between percentage of completion of printing patterns and achieved doses using a multi-step method. The impact of embedded phase rheological behavior, the printing speed and the needle size of the embedded phase were examined. Owning to their appearance, modular nature, ease of personalizing dose and geometry, and tailoring and potential inclusion of various materials, this new dosage form concept holds a substantial promise for novel dosage forms in pediatrics.

scholarly journals Hot-Melt 3D Extrusion for the Fabrication of Customizable Modified-Release Solid Dosage Forms

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 738 ◽  
Author(s):  
Jaemin Lee ◽  
Chanwoo Song ◽  
Inhwan Noh ◽  
Sangbyeong Song ◽  
Yun-Seok Rhee
Keyword(s):  
Dissolution Rate ◽  
Dosage Form ◽  
Amorphous State ◽  
Dosage Forms ◽  
Modified Release ◽  
Solid Dosage Forms ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Enhanced Solubility ◽  
Hot Melt

In this work, modified-release solid dosage forms were fabricated by adjusting geometrical properties of solid dosage forms through hot-melt 3D extrusion (3D HME). Using a 3D printer with air pressure driving HME system, solid dosage forms containing ibuprofen (IBF), polyvinyl pyrrolidone (PVP), and polyethylene glycol (PEG) were printed by simultaneous HME and 3D deposition. Printed solid dosage forms were evaluated for their physicochemical properties, dissolution rates, and floatable behavior. Results revealed that IBF content in the solid dosage form could be individualized by adjusting the volume of solid dosage form. IBF was dispersed as amorphous state with enhanced solubility and dissolution rate in a polymer solid dosage form matrix. Due to absence of a disintegrant, sustained release of IBF from printed solid dosage forms was observed in phosphate buffer at pH 6.8. The dissolution rate of IBF was dependent on geometric properties of the solid dosage form. The dissolution rate of IBF could be modified by merging two different geometries into one solid dosage form. In this study, the 3D HME process showed high reproducibility and accuracy for preparing dosage forms. API dosage and release profile were found to be customizable by modifying or combining 3D modeling.

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