TYLOPUR® – Water soluble cellulose ethers by Shin-Etsu

Introduction

TYLOPUR® is Hypromellose (HPMC) and a versatile pharmaceutical excipient. TYLOPUR® is manufactured at Tyloshin 2 plant at SE Tylose GmbH & Co. KG in Wiesbaden, Germany. This plant operates under GMP conditions and fulfills the requirements of the pharmaceutical industry. SE Tylose is a materials producer with an emphasis on a stable supply of high-quality products.

One of TYLOPUR® applications is film coating and it is easy to use as a coating material to provide an excellent finish. In addition, TYLOPUR® is effective as a granulation binder since it does not interact with drugs, has superior stability and has a nonionic character. It is available in various viscosity grades for the granulation process.

TYLOPUR® can also be used as a hydrophilic matrix agent for sustained release tablets. The hydrophilic matrix system is the simplest sustained release technology for oral dosage forms, consisting essentially of a drug and a water soluble highly viscous polymer, such as hypromellose. Shin-Etsu has focused on controlled release technology and found that by controlling the chemical and physical properties of the HPMC, a more reproducible drug release  an be achieved.

Another application of TYLOPUR® is to enhance the solubility of drugs, for example using solid dispersion technologies. TYLOPUR® can also replace gelatine for hard shell capsule manufacturing because of its greater stability.

Shin-Etsu has application laboratories located worldwide and is able to offer you technical services. These
laboratories are continuously making valuable contributions to pharmaceutical technology; detailed technical data
is available and formulation advices can be offered. We can also provide you with Quality by Design (QbD) samples
for your development projects. Please contact your technical sales manager for further information.

Description

Substitution Types and Major Applications

The substitution type describes the amount of methoxy and hydroxypropoxy substituents on the cellulose backbone
of TYLOPUR® and is mentioned in the pharmacopeia monographs. TYLOPUR® includes several grades with different
kind of substitution, low viscosity and high viscosity grades.

Physicochemical Properties

True Density
1.26 – 1.31 g/cm3 (measured with helium pycnometer)

Tapped Density
0.50 – 0.70 g/cm3

Equilibrium Moisture Content
The relationship between relative humidity and equilibrium moisture content of TYLOPUR® is shown in Figure 1 and
2. In Figure 1, Tylopur 606 (low viscosity) was compared with povidone (PVP) and hydroxypropyl cellulose (HPC),
and there is no difference between TYLOPUR® and HPC. In Figure 2, high viscosity TYLOPUR® with different
substitution were compared and no difference was found.

Applications

TYLOPUR® is soluble in water and mixed solvents. It may form lumps, which require a long time to dissolve, if it is added to such solvents all at once. Therefore, TYLOPUR® should be dissolved according to the following procedures.

Dissolving in Water

Add all of the TYLOPUR® in about 1/3 of the water, previously heated to above 80 °C, while stirring well. Because
hot water is a poor solvent for TYLOPUR® a uniformly wet dispersion is obtained. Then, add cold water to make the
prescribed volume while stirring well. When the temperature of the water falls to below 30 °C, TYLOPUR® can
dissolves completely and the solution can be used as a coating fluid. If a high-power stirrer is used, TYLOPUR® can
be readily dissolved by adding it gradually to the water at below 30 °C with stirring. Care must be taken to avoid
bubble or foam formation.

At 6 – 10 % polymer concentration (viscosity less than 100 mPas) any formed bubbles disappear when the solution
is left to stand for several hours. Shin-Etsu Silicone KM-72 (Polydimethylsiloxane) from Shin-Etsu Chemical can be
employed as antifoaming agents.

Dissolving in Organic Solvents

Pour a prescribed volume of ethanol into a container and add all of the TYLOPUR® in it while stirring. When a uniform dispersion is obtained, add methylene chloride gradually and stir gently to form a well-wetted dispersion as the coating solution.

Although great care is taken to avoid any foreign material contamination, it is recommended to sieve the product and/or filter the product solution before usage.

If difficulties arise concerning the dissolution apparatus, removal of bubbles from the coating solution or during the filtration of solutions, Shin-Etsu can offer technical advice based on extensive experience and know-how.

See the full brochure on “TYLOPUR®” here

(click the picture to download the brochure)

Source: Shin-Etsu, brochure “TYLOPUR®”

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