Formulation and Evaluation of Vaginal Bioadhesive Drug Delivery System of Acyclovir

Acyclovir is an anti-viral, which has been used in the treatment of vaginal disorder. Acyclovir is almost completely absorbed after oral administration but has low bioavailability of about 10-15% because of first pass metabolism. As first pass metabolism removes approximately 85-90% of the drug, so for clinical efficacy of the drug it should be frequently administered. Hence an attempt has been made to produce sustained release dosage form of the acyclovir which can be specifically employed for the treatment of vaginal disordered by Herpes simplex virus. The Mucoadhesive tablets of acyclovir has been prepared by direct compression methods and evaluated for various parameter such as thickness, friability, hardness, drug content, weight variation, swelling index, surface pH, bioadhesive force, bioadhesive time, drug release etc. The kinetic data was applied to the optimized formulations. So formulation of acyclovir in a vaginal mucoadhesive tablet dosage form will decrease the frequency of administration, which can lead to an improvement in patient adherence and thereby improving its clinical efficacy.

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Gastroretentive drug delivery system of a lipid lowering agent

International Current Pharmaceutical Journal ◽

10.3329/icpj.v2i9.16077 ◽

2013 ◽

Vol 2 (9) ◽

pp. 152-155

Author(s):

D. Krishnarajan ◽

N. Senthil Kumar ◽

Rajesh Yadav

Keyword(s):

Guar Gum ◽

Lipid Lowering ◽

In Vitro Dissolution ◽

Wet Granulation ◽

Natural Polymers ◽

First Pass Metabolism ◽

First Pass ◽

Mucoadhesive Tablets ◽

Pass Metabolism

The objective of this study was to develop mucoadhesive tablets of Simvastatin using natural polymers. Simvastatin has short biological half-life and high first pass metabolism hence which was designed to increase the gastric residence time which prolong the drug release. The tablets were prepared by wet granulation technique using Carbopol-934, guar gum, xanthine gum and chitosin as polymers. Formulations were evaluated for different parameters like hardness, friability, uniformity of weight, swelling characteristics, in vitro dissolution and kinetic studies. The dissolution was carried out for 12 hours in which the formulation with guar gum has shown highest dissolution release profile (F9). Thus the present study concludes that mucoadhesive tablets of simvastatin can be a good way to pass the extensive hepatic first pass metabolism and to improve the bioavailability of simvastatin.DOI: http://dx.doi.org/10.3329/icpj.v2i9.16077 International Current Pharmaceutical Journal, August 2013, 2(9): 152-155

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Effect of various Polymers on Drug Release from Mucoadhesive Tablets of Cefixime Trihydrate

Research Journal of Pharmaceutical Dosage Forms and Technology ◽

10.52711/0975-4377.2021.00030 ◽

2021 ◽

pp. 167-173

Author(s):

Kumara Swamy Samanthula ◽

Agaiah Goud Bairi ◽

Shobha Rani Satla ◽

Mahendra Kumar CB

Keyword(s):

Drug Release ◽

Diffusion Mechanism ◽

In Vitro Release ◽

In Vitro Dissolution ◽

Content Uniformity ◽

First Pass Metabolism ◽

First Pass ◽

Mucoadhesive Tablets ◽

Pass Metabolism

Cefixime trihydrate (CT) is a third-generation cephalosporin antibiotic and is used in the management of various infections caused by Gram +ve as well as Gram – ve bacteria. It has a plasma half-life of 3-4 h. It has poor oral bioavailability due to hepatic first pass metabolism. Hence, an attempt was made to develop CT mucoadhesive tablets for buccal delivery to avoid first-pass metabolism and improved oral delivery. CT mucoadhesive tablets developed using HPMC K4M, Na-CMC, guar gum and chitosan as rate controlling polymers and mucoadhesive agent, respectively and compressed by direct compression method. The prepared CT mucoadhesive tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, assay, mucoadhesive strength and in vitro release. From the results, all the evaluated parameters were within the pharmacopoeial limits. The in-vitro dissolution studies indicated that the CTmucoadhesive tablets formulation (F2) showed 99.7±1.4 % of drug release after 8 h and chose as the optimized formulation. The kinetic models suggest that the drug release follows Higuchi’s kinetics and tablets drug release was controlled by a diffusion mechanism.

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Review on Lozenges

Research Journal of Pharmacology and Pharmacodynamics ◽

10.52711/2321-5836.2021.00016 ◽

2021 ◽

pp. 75-78

Author(s):

Mahesh Babasaheb Kolap ◽

Pratiksha Kisan Omase ◽

Abhijeet Vijay Dashwant ◽

Rutuja Shrikant Namde

Keyword(s):

Oral Cavity ◽

Active Ingredient ◽

Retention Time ◽

Dosage Form ◽

Wide Range ◽

First Pass Metabolism ◽

First Pass ◽

Classification Evaluation ◽

Gastric Irritation ◽

Pass Metabolism

Lozenges are one of the widely used solid, unit dosage form of medicament which are meant to be dissolved in mouth or pharynx. The benefits of the medicated lozenges is they increase the retention time of the dosage form in oral cavity which increases bioavailability, reduces gastric irritation and bypasses first pass metabolism. This dosage form can be adopted for local as well as systemic therapy and a wide range of active ingredient can be incorporated in them. The present review covers more or less all aspects associated with lozenge such as its manufacturing, classification, evaluation and its application Lozenges are one of the widely used solid, unit dosage form of medicament which are meant to be dissolved in mouth or pharynx. The benefits of the medicated lozenges is they increase the retention time of the dosage form in oral cavity which increases bioavailability, reduces gastric irritation and bypasses first pass metabolism. This dosage form can be adopted for local as well as systemic therapy and a wide range of active ingredient can be incorporated in them. The present review covers more or less all aspects associated with lozenge such as its manufacturing, classification, evaluation and its application.

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REVIEW ON HERBAL LOZENGES PREPARED FOR COLD AND FLU.

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v10i3.869 ◽

2021 ◽

Vol 10 (3) ◽

Author(s):

Darwhekar G. N ◽

Mudgal Kajal ◽

Koko Sweta. S

Keyword(s):

Traditional Medicine ◽

Retention Time ◽

Dosage Form ◽

Herbal Formulation ◽

First Pass Metabolism ◽

First Pass ◽

Care And Treatment ◽

Gastric Irritation ◽

Pass Metabolism

Traditional medicine and herbal formulation have been used by mankind for the care and treatment of various diseases and disorder. Throat infections are most common diseases in today’s world. However it is not taken too seriously by people long term throat infection can lead to severe throat problems pharyngitis and also cancer. The polyherbal lozenges are solid preparation that contains one or more medicaments usually during a flavored, sweetened base that are intended to dissolve or disintegrate slowly within the mouth. The benefits of they medicated lozenges is that they increase a retention time of the dosage form in mouth which increases bioavailability, reduces gastric irritation and bypasses first pass metabolism. Keywords: polyherbal lozenges, pharyngitis

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

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.13793 ◽

2017 ◽

Vol 9 (2) ◽

pp. 52 ◽

Cited By ~ 2

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

Objective: 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.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.Methods: 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, in vitro drug release, mechanical properties and ex vivo permeation studies.Results: 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.Conclusion: Duloxetine hydrochloride can be delivered through the buccal route of drug administration through the buccal patches.

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Formulation Development and In Vitro Evaluation of Buccal Tablets of Ramipril

Materials Science Forum ◽

10.4028/www.scientific.net/msf.987.83 ◽

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.

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

Planta Medica ◽

10.1055/s-2008-1075176 ◽

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

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

Drug Delivery Letters ◽

10.2174/2210303108666181108120840 ◽

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. 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). 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.

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