(1). Introduction
Hydroxypropyl methylcellulose (HPMC), also known as hydroxypropyl methylcellulose, is a versatile semi-synthetic cellulose ether with a variety of pharmaceutical applications. The application of HPMC in the pharmaceutical field is mainly due to its excellent physical and chemical properties, including film-forming, gelling, thickening, adhesion and stability. As an inert and non-ionic compound, HPMC can effectively provide controlled release, taste masking, film-forming, adhesion and protection functions in pharmaceutical preparations.
(2). Composition and preparation
HPMC is modified by partial methylation and hydroxypropylation of cellulose by etherification of cellulose with methanol and propylene oxide under alkaline conditions. The properties of HPMC, such as viscosity, gelation temperature and solubility, are affected by its substituent content and molecular weight. The production of pharmaceutical grade HPMC must meet strict quality standards to ensure its purity and consistency to meet the requirements of pharmaceutical preparations.
(3). Physical and chemical properties
Film-forming property: HPMC can form a transparent, colorless, flexible film.
Water solubility: It dissolves rapidly in cold water, but forms a gel in hot water.
Viscosity control: The viscosity of the HPMC solution can be controlled by adjusting its concentration and molecular weight.
Chemical inertness: It is chemically stable under most conditions and does not react with drug ingredients.
(4). Pharmaceutical applications
4.1 Controlled release preparations
HPMC plays an important role in sustained-release and controlled-release preparations. It can form a gel barrier, control the dissolution rate of the drug, and achieve the purpose of prolonging the drug’s action time.
Oral controlled-release tablets: By mixing with the drug, it forms a matrix for slow release of the drug. As the main excipient in some sustained-release tablets, HPMC can gradually hydrate and form a gel layer to control the release of the drug.
Microspheres and microcapsules: As a film-forming agent or suspension stabilizer, it is used to encapsulate drug particles and reduce the release rate.
4.2 Coating Materials
As coating materials, HPMC can provide drug protection, control release, improve appearance, and mask unpleasant odors or tastes.
Enteric coating: HPMC is combined with other polymers to make enteric coatings that are resistant to gastric juice, ensuring that the drug is released in the intestine rather than in the stomach.
Film coating: Film coating used for tablets or granules to improve stability and swallowing comfort.
4.3 Binders
The binding properties of HPMC make it an ideal binder for tablet preparation. It can improve the compressibility of powders and the mechanical strength of tablets.
Tablets: Used as a binder in wet granulation to ensure that powders can be compressed into strong and uniform tablets.
Granular preparations: HPMC can improve the uniformity and strength of granules and reduce disintegration time.
4.4 Thickeners and suspending agents
As thickeners and suspending agents, HPMC can improve the stability and uniformity of liquid preparations.
Oral liquids: Improve taste and stability and prevent precipitation of ingredients.
Topical application: Used as a thickener in creams and gels to provide appropriate viscosity and touch.
4.5 Ophthalmic Applications
HPMC is widely used in ophthalmic preparations, especially artificial tears and ophthalmic gels.
Artificial tears: As a lubricant, it provides a comfortable moisturizing effect and relieves dry eye symptoms.
Ophthalmic gel: Prolongs the residence time of the drug on the ocular surface and improves the efficacy.
4.6 Capsules
HPMC can be used to produce vegetarian capsules (HPMC capsules) as a substitute for gelatin capsules, suitable for vegetarians or patients who are allergic to animal-derived ingredients.
Vegetarian capsules: Provide similar dissolution properties to gelatin capsules and are not affected by the ethical issues of animal-derived ingredients.
(5). Advantages
Biocompatibility: HPMC is non-toxic and non-irritating, suitable for a variety of drug preparations.
Chemical stability: Does not react with active pharmaceutical ingredients and maintains drug activity.
Versatility: Can be used in controlled release, coating, bonding, thickening and suspension.
Environmentally friendly: HPMC is made from natural cellulose and is renewable and biodegradable.
6. Challenges and Prospects
Although HPMC has many advantages in drug preparations, there are also challenges in some cases. For example, its physical properties may need to be optimized to ensure uniform drug release at high drug loads. In addition, future research may focus on further improving the application of HPMC in high-performance drug delivery systems by molecular modification or combining with other excipients to enhance its performance.
Pharmaceutical grade hydroxypropyl methylcellulose (HPMC) plays an irreplaceable role in modern pharmaceutical formulations due to its versatility and excellent physicochemical properties. From controlled release, coating to bonding and thickening, the application range of HPMC is wide and expanding. With the advancement of technology and the development of new drugs, HPMC will play a more important role in future drug delivery systems.