scholarly journals PHARMACOLOGY OF NOVAL CANNABINOIDS

2019 ◽  
pp. 1-5
Author(s):  
SUMITHA S. K. ◽  
VEENA S. PATTAMMADY ◽  
R. SAMBATHKUMAR
Keyword(s):  
Cannabis Sativa ◽  
Synthetic Cannabinoids ◽  
Systemic Circulation ◽  
Scientific Investigation ◽  
Direct Relation ◽  
Preclinical Research ◽  
First Pass Metabolism ◽  
First Pass ◽  
Psychoactive Effects ◽  
Pass Metabolism

Cannabis is a plant rich in various compounds that have a variety of impacts on the physiology of humans and the effects of these metabolites have a significant role in managing a variety of clinical diseases. A substantial increase in the use of SC (synthetic cannabinoids) had seen in the last few years especially infrequent cannabis users. The SCs will generate psychoactive effects that were similar to cannabis. However, the composition and pharmacological characteristics of these drugs make them possibly hazardous. Like all drugs, cannabis’ pharmacokinetics depends on the route of administration. Several studies showed that the bioavailability is less in oral administration when compared to inhalation. The main reason for this decrease in oral bioavailability is that cannabinoids undergo the first-pass metabolism before entering into the systemic circulation whereas in inhalation, it enters the circulation directly through the lungs. Cannabis sativa is a psychoactive plant that contains more than 500 components of which 104 cannabinoids had been identified. Of these, 2 components such as Δ9-THC (Δ9-tetrahydrocannabinol) and CBD (cannabidol) were under the scientific investigation. Δ9-THC is the primary cannabinoid which was responsible for the consequences of psychotrophy. The potency of cannabis is assessed based on the THC concentration of a sample that is the main psychoactive cannabinoid in cannabis. The adverse effects are in direct relation to the concentration of THC in the product after regular cannabis use. It can be assumed that several cannabinoids will find their way into the pharmacies from preclinical research within a century.

scholarly journals A comprehensive review on buccal patches

2020 ◽  
Vol 13 (1) ◽  
pp. 130-135
Author(s):  
Seema ◽  
Kapil kumar ◽  
Deepak Teotia
Keyword(s):  
Drug Delivery ◽  
Oral Cavity ◽  
Systemic Circulation ◽  
Drug Formulation ◽  
Delivery Method ◽  
Modern Approach ◽  
Comprehensive Review ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal Patches are the type of drug formulation that has normally a different course of administration through the buccal mucosa for drug delivery. The product is placed between upper gingiva (gums) and cheek to treat local and systemic conditions. Buccal patch have good accessibility to the membranes that line the oral cavity. These patches tend to help drug enter directly into the systemic circulation escaping hepatic first pass metabolism. This type of drug delivery method is considered useful for elevating the bioavailability of drugs. This review is a thorough study to apprehend the procedures involved in assessment of buccal patches and the modern approach towards this type of drug delivery. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

scholarly journals Development and evaluation of buccal patches of theophylline

2021 ◽  
Vol 16 (3) ◽  
pp. 235-240
Author(s):  
Kapil Kumar ◽  
Gurleen Kaur ◽  
Seema ◽  
Deepak Teotia ◽  
Ikram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Buccal Mucosa ◽  
Systemic Circulation ◽  
Pharmacological Response ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Buccal patches are the types of formulations in which the drug is administered through buccal mucosa. these patches are or placed in between the gums and the for the pharmacological response. The main advantage of these patches is there is no first pass metabolism takes place and easily absorb in systemic circulation through themucosa .the main objective of this drug delivery system is to elevate or increase the bioavailability of the drug. the review informs about the steps involve in the preparation of buccal patch and to promote the awareness towards this type of drug delivery system. This article intends to analyze the overall profile of Buccal Patches and scope of future advances.

scholarly journals Right and Left-sided Valve Disease: A Case of Subclinical Intrapulmonary Shunt in an Adult with Malignant Carcinoid

2021 ◽  
Vol 1 (1) ◽  
Author(s):  
Ross M Hansen ◽  
Gregory D Chapman
Keyword(s):  
Systemic Circulation ◽  
Valve Disease ◽  
Intrapulmonary Shunt ◽  
Transesophageal Echocardiogram ◽  
Malignant Carcinoid ◽  
Vasoactive Hormones ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Right ◽  
Pass Metabolism

Carcinoid tumors are highly differentiated neuroendocrine tumors (NET) that most commonly originate from the gastrointestinal tract. Liver metastases bypass first-pass metabolism and liberate vasoactive hormones into systemic circulation, causing flushing and diarrhea. Prolonged levels of circulating serotonin may adversely affect the heart by creating fibrotic endocardial deposits on native valves. The remaining serotonin is metabolized in the pulmonary circuit that leads to pathognomonic valvular disease isolated to the right side of the heart. We present a case of an adult male with known carcinoid syndrome who presented with involvement of right, as well as left-sided valves. He was found to have an intrapulmonary shunt on transesophageal echocardiogram (TEE) with bubble study. Intrapulmonary shunt should be considered, in conjunction with right-to-left shunt, lung involvement, and high levels of serotonin, for carcinoid patients with right and left-sided valve disease.

scholarly journals Formulation and evalution of Transdermal patches of torasemide

2015 ◽  
Vol 1 (1) ◽  
pp. 38 ◽  
Author(s):  
Rajesh Asija ◽  
Avinash Gupta ◽  
Bhagwan Swaroop Maheshwari
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Systemic Circulation ◽  
Topical Drug Delivery ◽  
Intravenous Therapy ◽  
Transdermal Drug Delivery System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Gastric Emptying Time ◽  
Pass Metabolism

The main advantage of Transdermal drug delivery system is to bypass the first pass metabolism, avertance of the risk and annoyance of intravenous therapy and of the varied conditions of absorption, like pH changes, gastric emptying time and presence of enzyme. The Transdermal drug delivery scheme is generally used where the others system of drug administration fails or it is mainly used in edema associates congestive heart failure. The transdermal drug delivery has advantage to deliver medicines via skin to systemic circulation at a predetermined rate and maintain therapeutic concentration for prolong period of time. This review describes the assorted formulation aspects, a variety of excipients, evaluation tests, challenges and drugs explored in the pasture of topical drug delivery.

scholarly journals Overview of Newer Glucocorticosteroid Preparations for Inflammatory Bowel Disease

1990 ◽  
Vol 4 (7) ◽  
pp. 407-414 ◽  
Author(s):  
R Brattsand
Keyword(s):  
Inflammatory Bowel Disease ◽  
Bowel Disease ◽  
Topical Therapy ◽  
Hepatic Metabolism ◽  
Systemic Circulation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Inflammatory Bowel ◽  
Bowel Mucosa ◽  
Pass Metabolism

Because the glucocorticosteroid receptor seems to be uniform in the human body, there is currently no support for a possibility of separating the therapeutic and adverse glucocorticosteroid actions at the receptor level. However, based on a new generation of glucocorticosteroids characterized by a high first pass metabolism in the liver, it seems possible today co reach a more selective topical therapy of inflammatory bowel disease. The properties of three new glucocorticosteroids are presented: the highly potent budesonide, fluticasone propionate and tixocortol pivalate - the latter with only low topical potency. Their properties can be exemplified by budesonide, which is currently the best documented compound. The topical potency of budesonide is 200 and 15 times higher than chose of hydrocortisone and prednisolone, respectively. This means that there is a high potential for anti-inflammatory and immunosuppressive actions on rectal and bowel mucosa. The compound is metabolically stable in the bowel compartment, which allows full retention of glucocorticosteroid activity in the target organ. However, when absorbed and distributed to the liver, there is a 90% first pass hepatic metabolism co metabolites of very low potency. This suggests that after topical application to rectal or bowel mucosa, glucocorticosteroid activity in the systemic circulation is low. This is in contrast to prednisolone, which has a hepatic first pass metabolism of just 20%.

scholarly journals DESIGN AND IN VITRO CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCHES OF DULOXETINE HYDROCHLORIDE

2017 ◽  
Vol 9 (2) ◽  
pp. 52 ◽  
Author(s):  
Himabindu Peddapalli ◽  
Krishna Mohan Chinnala ◽  
Nagaraj Banala
Keyword(s):  
Buccal Mucosa ◽  
Moisture Absorption ◽  
Systemic Circulation ◽  
Content Uniformity ◽  
Duloxetine Hydrochloride ◽  
Weight Variation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

<p><strong>Objective: </strong>Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation, a drug administered through the buccal mucosa enters directly to the systemic circulation, thereby which bypass the drug from the first-pass hepatic metabolism and adverse gastrointestinal effect. Duloxetine hydrochloride (DLX HCL) is a selective serotonin and noradrenaline reuptake inhibitor (SSNRI). It is used in the treatment of depression, diabetic peripheral neuropathic pain and in moderate to severe stress urinary incontinence in women.</p><p>However, it undergoes extensive first-pass metabolism, and it is susceptible to undergo degradation in the acidic environment of the stomach, which results in the poor bioavailability. The objective of the present investigation is to design and evaluate the mucoadhesive buccal patches of DLX HCL with a goal of to increase the bioavailability and improve the patient compliance.</p><p><strong>Methods: </strong>Mucoadhesive buccal patches were prepared by solvent casting technique using mucoadhesive polymers. The patches were evaluated for weight variation, thickness, surface pH, folding endurance, moisture absorption, drug content uniformity, <em>in vitro</em> drug release, mechanical properties and <em>ex vivo</em> permeation studies.</p><p><strong>Results: </strong>The results of the optimised buccal patch F4 indicate that the mucoadhesive buccal patches of duloxetine hydrochloride may be a good choice for improving the bioavailability by bypassing the extensive first pass metabolism and acid degradation in the stomach.</p><p><strong>Conclusion: </strong>Duloxetine hydrochloride can be delivered through the buccal route of drug administration through the buccal patches.<strong></strong></p>

Formulation Development and In Vitro Evaluation of Buccal Tablets of Ramipril

2020 ◽  
Vol 987 ◽  
pp. 83-87
Author(s):  
D.Nagasamy Venkatesh ◽  
Raman Rajeshkumar ◽  
Roan Ngoc Anh Huy
Keyword(s):  
Systemic Circulation ◽  
Formulation Development ◽  
Compression Technique ◽  
Zero Order Kinetics ◽  
Weight Variation ◽  
First Pass Metabolism ◽  
First Pass ◽  
Buccal Tablets ◽  
Pass Metabolism

The main objective of the present investigation was to develop buccal tablets of ramipril, to bypass the first pass metabolism and to improve its oral bioavailability. Ramipril, an ACE inhibitor used in the treatment of hypertension undergoes extensive first pass metabolism and about 25% of the drug reaches the systemic circulation. A unidirectional, bilayered mucoadhesive tablet of ramipril was prepared using HPMC as polymer by direct compression technique. Initially, a backing layer was made by using ethyl cellulose, onto which the drug containing layer as placed and recompressed to get a bilayered tablet. The buccal tablets were evaluated for various parameters such as weight variation test, thickness, hardness, friability, in vitro swelling studies, in vitro mucoadhesion study and in vitro dissolution study. Among the different formulation, the formulation (F1) prepared using 5% HPMC as polymer exhibited satisfactory performance over the other batches and considered as an ideal batch. The release of the drug from the tablets exhibited zero order kinetics and the mechanism of release was governed by diffusion process.

Identification of a Cranberry Juice Product Capable of Inhibiting Enteric CYP3A-Mediated First-Pass Metabolism in Humans

Planta Medica ◽  
2008 ◽  
Vol 74 (03) ◽  
Author(s):  
N Ngo ◽  
Z Yan ◽  
TN Graf ◽  
DR Carrizosa ◽  
EC Dees ◽  
...  
Keyword(s):  
Cranberry Juice ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Development, Characterization and Optimization of Mucoadhesive Tablet for Buccal Delivery of Domperidone

2019 ◽  
Vol 9 (1) ◽  
pp. 37-49
Author(s):  
Jagdale Sachin ◽  
Panbude Aishwarya ◽  
Navasare Priya
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Research Work ◽  
Wet Granulation ◽  
Buccal Delivery ◽  
Scanning Calorimetry ◽  
Mucoadhesive Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism to improve absorption directly into systemic circulation. The present research work was carried with an aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal delivery using different bio-adhesive polymeric combinations. </P><P> Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100, HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100) over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive properties. The interactions between drug and polymers were studied by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). </P><P> Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive strength and swelling index. Conclusion: The developed buccal tablet of domperidone might prove alternative to bypass the hepatic first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.

scholarly journals Effect of oral pretreatment with indomethacin on the intestinal first-pass metabolism of salicylamide in rabbits.

1988 ◽  
Vol 11 (9) ◽  
pp. 620-624 ◽  
Author(s):  
Junzo NAKAMURA ◽  
Nobuaki SEKI ◽  
Hitoshi SASAKI ◽  
Juichiro SHIBASAKI
Keyword(s):  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism
Sign in / Sign up

Export Citation Format

Share Document