A seminar on HPMC and its role in pharmaceutical formulations

A seminar on HPMC AND ITS ROLE IN PHARMACEUTICAL FORMULATIONS.: 

A seminar on HPMC AND ITS ROLE IN PHARMACEUTICAL FORMULATIONS . Prepared by MANSI S. ADESHARA ROLL NO : 3 2 ST SEMESTER, M.PHARM, BHAGWAN MAHAVIR COLLEGE OF PHARMACY SURAT . Guided by: MR.NISHANT UPADHYAY MR.SANKET GANDHI ASST. PROFFESOR BMCP, SURAT

Introduction: 

Introduction 28-Aug-12 BMCP(215), VESU 2 It is a cellulose having some parts of hydroxyl groups in form of methyl ether and some in the form of 2- hydroxy propyl ether. The Following Table Shows The Different Grades Of HPMC Based On The Substitution Of Methoxy And Hydroxy Propyl groups. Sr no. Substitution type Methoxy % Hydroxy propyl % Viscosity grades Min Max Min Max 1. 1828 16.5 20.0 23.0 32.0 2. 2208 19.0 24.0 4.0 12.0 3,100,4000,15000,100000 3. 2906 27.0 30.0 4.0 7.5 4. 2910 28.0 30.0 7.0 12.0 3,5 6 15 ,4000,10000 2910- Best Solubility In Organic Solvents

NonproprietaryNames : 

NonproprietaryNames BP: Hypromellose JP: Hydroxypropylmethylcellulose PhEur : Hypromellosum USP: Hypromellose Synonyms Benecel MHPC; E464; hydroxypropyl methylcellulose; HPMC; Methocel ; methylcellulose propylene glycol ether; methyl hydroxypropylcellulose ; Metolose ; Tylopur ; 2-hydroxypropylmethyl ether Functional Category Coating agent; film-former; rate-controlling polymer for sustained release; stabilizing agent; suspending agent; tablet binder; viscosity-increasing agent. 28-Aug-12 3 BMCP(215), VESU

Uses: 

Uses . Formulation Use Concentration oral product tablet binder 2% and 5% w/w extended-release tablet formulations to retard the release of drugs from a matrix 10–80% w/w film-coated tablets film-forming 2–20% w/w eye drops and artificial tear solutions. thickening agent 0.45–1.0% w/w 28-Aug-12 4 BMCP(215), VESU

Uses : 

Uses Oral, ophthalmic and topical pharmaceutical formulations. Emulsifier, Suspending Agent, And Stabilizing Agent In Topical Gels And Ointments. As a protective colloid, it can prevent droplets and particles from coalescing or agglomerating, thus inhibiting the formation of sediments. Used in the manufacture of capsules, as an adhesive in plastic bandages, and as a wetting agent for hard contact lenses. It is also widely used in cosmetics and food products. Description Hypromellose is an odorless and tasteless, white or creamy white fibrous or granular powder. 28-Aug-12 5 BMCP(215), VESU

Understanding product nomenclature: 

Understanding product nomenclature Family of METHOCEL products is very extensive. The initial letter in the product name identifies the type of cellulose ether, as follows: A-type are methylcellulose products E, F, J, and K-type are hydroxypropyl methylcellulose products. The number that follows the initial letter identifies the viscosity grade in millipascal seconds (mPa·s) for the product measured at 2% in water at 20°C. A "C" or an "M" following this number indicates that it is multiplied by the following factors: C: 100 times M: 1,000 times 28-Aug-12 6 BMCP(215), VESU

Understanding product nomenclature: 

Understanding product nomenclature Some commonly used suffixes that identify special products: LV, low viscosity S, surface-treated (cold water dispersible) products P, Premium grade Here are several examples: METHOCEL A4CP, methylcellulose product with viscosity of 400 mPa·s, Premium Grade. METHOCEL E15LVP, hydroxypropyl methylcellulose product with viscosity of 15 mPa·s, Premium Grade. METHOCEL E4MP, hydroxypropyl methylcellulose product with viscosity of 4,000 mPa·s, Premium Grade . 28-Aug-12 7 BMCP(215), VESU

Examples of Viscosity grades of HPMC : 

Examples of Viscosity grades of HPMC 28-Aug-12 8 BMCP(215), VESU

Effect of HPMC on release profile and bioavailability of Nifedipine tablets.: 

Effect of HPMC on release profile and bioavailability of Nifedipine tablets. 28-Aug-12 9 BMCP(215), VESU 1. By altering the concentration of HPMC.

Effect of HPMC on release profile and bioavailability of Nifedipine tablets.: 

Effect of HPMC on release profile and bioavailability of Nifedipine tablets . 28-Aug-12 10 BMCP(215), VESU 2. By altering the degree of polymerization of HPMC(50%) Results of the alterations in concentrations of HPMC state that the concentration of 50%HPMC shows optimum results. Results of alterations in polymerization degree state that the dissolution of NP from the NP-PEG-HPMC tablet prepared using 50% HPMC (2208) was markedly delayed with increasing viscosity of HPMC

Effect of HPMC on release profile and bioavailability of Nifedipine tablets .: 

Effect of HPMC on release profile and bioavailability of Nifedipine tablets . 28-Aug-12 11 BMCP(215), VESU In conclusion, we have demonstrated a preparation method for a new sustained release NP tablet (NP-PEG-HPMC tablet), using a mixture of NP-PEG granules and HPMC. This method increased the NP bioavailability and conferred a characteristic of sustained release, as compared with the powdered form of the drug. These NP-PEG-HPMC tablets prevent abrupt increase in plasma NP concentrations without decrease of NP bioavailability as compared with the NP-PEG tablets.

Effect of HPMC and NA2CO3 ratios in release of Acetaminophen in salting-out taste-masking system: 

Effect of HPMC and NA 2 CO 3 ratios in release of Acetaminophen in salting-out taste-masking system 28-Aug-12 12 BMCP(215), VESU The order of lag time length was DS (100/0) W (C) (less than 0.1 min) < DS (0/100) W (C) (0.1 min) < DS (40/60) W (C) (0.2 min) < DS (60/40) W (C) (1.6 min) < DS (83/17) W (C) , (5.3 min). In salting-out taste-masking system, changes in the water soluble polymer in the salting-out layer induces changes in the drug release rate. Insolubilization of the water-soluble polymer in high salt conc. generates drug release lag times. Subsequent dissolution of the water-soluble polymer in low salt concentrations causes immediate drug release.

Different HPMC viscosity grades as coating agents for an oral time and/or site-controlled delivery system: 

Different HPMC viscosity grades as coating agents for an oral time and/or site-controlled delivery system 28-Aug-12 13 BMCP(215), VESU Release profiles obtained from uncoated cores and systems coated with Methocel ® E5, E50 and K4M aqueous solutions at 16, 8 and 2% (w/v), respectively. Methocel® E50 takes the smallest time for coating. Methocel® E50 affords the best balance among process time necessary for spray-coating, and delaying the drug release profile to suit the chronotropic systems .

Comparative study on Xanthan Gum and HPMC as matrices for controlled-release drug delivery of Caffeine: 

Comparative study on Xanthan Gum and HPMC as matrices for controlled-release drug delivery of Caffeine 28-Aug-12 14 BMCP(215), VESU Typical plots of diffuse out of caffeine from 4% XG and HPMC gels into water . Under similar experimental conditions the diffusion rate of caffeine in HPMC gel is significantly (p < 0.0001) higher than in XG gel. The calculated diffusion coefficient of caffeine in HPMC and XG gels were found to be 5.49 x10 -6 cm 2 /s and 2.48 x 10 6 cm 2 /s, respectively. The release of a drug from XG matrices followed almost time-independent kinetics while the release from HPMC matrices followed time-dependent kinetics.

References : 

References Tatsuya Ishikawa, Yoshiteru Watanabe et al, Effect of hydroxypropylmethylcellulose (HPMC) on the release profiles and bioavailability of a poorly water-soluble drug from tablets prepared using macrogol and HPMC, International Journal of Pharmaceutics 202 (2000) 173–178. Takayuki Yoshida , Hiroaki Tasaki et al.; Mechanism of controlled drug release from a salting-out taste-masking system ;Journal of Controlled Release 131 (2008) 47–53. M.E. Sangalli a, A. Maroni et al; Different HPMC viscosity grades as coating agents for an oral time and/or site-controlled delivery system: a study on process parameters and in vitro performances, European Journal of Pharmaceutical Sciences 22 (2004) 469–476. Mohammad Mahiuddin Talukdar , Renaat Kinget; Comparative study on xanthan gum and hydroxypropylmethyl cellulose as matrices for controlled-release drug delivery. II. Drug diffusion in hydrated matrices; International Journal of Pharmaceutics 151 (1997) 99 107. Handbook of Pharmaceutical Excipients, Edited by Raymond C Rowe, Paul J Sheskey and Siân C Owen , Fifth edition published 2006,pg 346-47. 28-Aug-12 BMCP(215), VESU 15

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28-Aug-12 16 BMCP(215), VESU Thank you Drugs are not always necessary. Belief in recovery always is. ~Norman Cousins