Scribd
Upload
31 views7 pages

5 Drug Profile

Drug profile information about famotidine

Uploaded by

17 Payal chavan
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
31 views7 pages

5 Drug Profile

Drug profile information about famotidine

Uploaded by

17 Payal chavan
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
You are on page 1/ 7

Chapter 5 Drug and Excipient Profile

DRUG PROFILE
CLOPIDOGREL BISULPHATE

Figure 10: clopidogrel structure

IUPAC Name- Methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-


c]pyridine- 5-yl)acetate

Clopidogrel is an antiplatelet medication used to reduce the risk of heart disease and stroke
in those at high risk. It is also used together with aspirin in heart attacks and following the
placement of a coronary artery stent (dual antiplatelet therapy). It is taken by mouth. Onset
of effects is about two hours and lasts for five days. It comes under BCS class 2.

Molecular formula -C16H16ClNO2S


Molecular weight - 321.8 g/mol
Synonyms- 113665-84-2
(S)-Clopidogrel
Plavix
Storage- Store clopidogrel at room temperature near 77°F (25°C).
Drug Class- Antiplatelet
Dose- 75-150 mg
Melting point- 158ºC
Mechanism of action-
Clopidogrel is metabolized to its active form by carboxylesterase-1.3 The active form is a
platelet inhibitor that irreversibly binds to P2Y12 ADP receptors on platelets. This binding
prevents ADP binding to P2Y12 receptors, activation of the glycoprotein GPIIb/IIIa
complex, and platelet aggregation

Solubility-1] water-0.1183g/mol

Formulation and Evaulation of Clopidogrel Bisulphate Nanosponges


26
Chapter 5 Drug and Excipient Profile

2]The solubility of clopidogrel in alcohols is ranked as ethanol > propanol > butanol >
isopropanol

Absorption-

A 75mg oral dose of clopidogrel is 50% absorbed from the intestine.


Clopidogrel can be taken with or without food. A meal decreases the AUC of
the active metabolite by 57%. The active metabolite of clopidogrel reaches a
maximum concentration after 30-60 minutes.

Volume of distribution- The apparent volume of distribution of clopidogrel is


39,240±33,520L.5

Metabolism-

85-90% of an oral dose undergoes first pass metabolism by carboxylesterase 1


in the liver to an inactive carboxylic acid metabolite.about 2% of clopidogrel is
oxidized to 2- oxoclopidogrel. This conversion is 35.8% by CYP1A2, 19.4%
by CYP2B6, and 44.9% by CYP2C194 though other studies suggest
CYP3A4,CYP3A5, and CYP2C9 also contribute. 2-oxoclopidogrel is further
metabolized to the active metabolite.

Route of elimination-

An oral dose of radiolabeled clopidogrel is excreted 50% in the urine and 46%
in the feces over 5 days.9 The remainder of clopidogrel is irreversibly bound to
platelets for their lifetime, or approximately 8-11 days.

Duration of action- 5 days

Adverse effects-
Headache, nausea, easy bruising, itching, and heartburn. More severe side
effects include bleeding and thrombotic thrombocytopenic purpura.

Contraindication-
Hypersensitivity to the drug or components of it.
Active pathologic bleeding such as intracranial bleeding or peptic ulcers.
CYP2C19 poor metabolizers.

Formulation and Evaulation of Clopidogrel Bisulphate Nanosponges


27
Chapter 5 Drug and Excipient Profile

PPIs diminish the antiplatelet effect of clopidogrel's active metabolite.

Formulation and Evaulation of Clopidogrel Bisulphate Nanosponges


28
Chapter 5 Drug and Excipient Profile

EXCIPIENTS PROFILE

ETHYL CELLULOSE-

Figure 11: Ethyl cellulose structure


Synonyms- Aquacoat; E462 Ethocel Surlease.

Molecular formula- C20H38O11

Molecular weight- 454.g/mol.


Melting point- 244-255°C
Solubility- Soluble in esters, aromatic hydrocarbons, alcohols and ketones.
Form- Powder
Appearance-White
Hardness- 52-61 (Sward, 3-mil. film)
Viscosity- 46 cP, 5 % in toluene/ethanol 80:20(lit.)
Transition temp- Tg 120-124 °C
Density- 1.14 g/mL at 25 °C(lit.)

Formulation and Evaulation of Clopidogrel Bisulphate Nanosponges


29
Chapter 5 Drug and Excipient Profile

EUDRAGIT

Figure 12 : Eudragit structure


Synonyms- 2-(methoxycarbonyl)-1-propene 2-methyl-2-propenoic acid
methyl ester
Appearance- Colourless
Odour-Unpleasant, acrid and repulsive.
Solubility- Soluble in warm water Miscible with most organic solvents
Density 1.02g/cm3
Molar mass- 86.06g/mol
Boiling point- 161⁰C
Melting point- 15⁰C

POLY VINYL ALCOHOL-

Figure 13: Poly vinyl alcohol

Synonyms- Airvol, elvanol, gohsenol, PVA, vinyl alcohol polymer

Formulation and Evaulation of Clopidogrel Bisulphate Nanosponges


30
Chapter 5 Drug and Excipient Profile

Name and CAS Registry Number-Ethanol,homopolymer [900-895]

Empirical Formula-(C2H4O)n
Melting point: 228⁰C for fully hydrolysed grades
180⁰C-190⁰C for partially hydrolysed grades
Refractive Index- nD25=1.49-1.53
Solubility-PVA is soluble in water and insoluble in organic.

Formulation and Evaulation of Clopidogrel Bisulphate Nanosponges


31
Chapter 1 Introduction

Formulation and Evaluation of Clopidogrel Bisulphate Nanosponges Tablets


32

You might also like

pFad - Phonifier reborn

Pfad - The Proxy pFad of © 2024 Garber Painting. All rights reserved.

Note: This service is not intended for secure transactions such as banking, social media, email, or purchasing. Use at your own risk. We assume no liability whatsoever for broken pages.


Alternative Proxies:

Alternative Proxy

pFad Proxy

pFad v3 Proxy

pFad v4 Proxy