Formulation Technology Research

BOC Sciences applies a professional formulation technology research platform to provide comprehensive technical services related to pharmaceutical formulations.

Services Scope

• New technology for preparation

Selecting the appropriate formulation technology is an effective way to solve the problems of poor water solubility, poor stability and low bioavailability of drugs. Commonly used formulation technologies include solid dispersion technology, inclusion technology, microencapsulation, liposome preparation technology, etc. The use of modern preparation technology to disperse drugs in a system with special structure, so that the research and development of innovative drug preparations that are different from traditional routes of administration, can improve the research level of drug preparations.

1. Solid Dispersion Technology

Solid dispersion refers to the dispersion system formed by the drug in molecular, colloidal, microcrystalline or amorphous state, and highly dispersed in suitable carrier material. The formulation technology used to make a drug into a solid dispersion is called solid dispersion technology. As an intermediate of a preparation, solid dispersion can be designed into drop pills, capsules, tablets, ointments, suppositories and injections according to the properties of the drug and the route of administration.

After the drug is made into a solid dispersion, it has the following advantages:

• Increase the solubility and dissolution rate of poorly soluble drugs, improve bioavailability, and reduce the dosage.
• Controlled drug release or controlled drug release in the small intestine.
• Delay the hydrolysis and oxidation of the drug through the encapsulation of the carrier.
• Mask the bad smell and irritation of the drug.
• Solidify the liquid medicine.

The carrier materials used in solid dispersion technology can be divided into three categories: water-soluble, insoluble and enteric. During use, single or several carrier materials can be selected according to the preparation purpose to achieve immediate release or sustained release effect.

Traditional solid dispersion techniques include melting method, solvent method, solvent-melting method, spray (freeze) drying method, grinding method, etc. New solid dispersion technologies include electrostatic deposition technology, hot melt extrusion technology, supercritical fluid technology, microwave quenching technology, etc.

The verification of the solid dispersion can be carried out by means of dissolution rate measurement, thermal analysis, X-ray diffraction, infrared spectroscopy, nuclear magnetic resonance and the like.

The solid dispersion technology used for different drugs mainly depends on the properties of the drug and the structure, properties, melting point and solubility of the carrier material.

2. Inclusion Technology

Inclusion compound refers to a special complex formed by a molecule being fully or partially included in the cavity structure of another molecule.

After the drug is made into an inclusion compound, it has the following advantages:

• Increase the solubility and bioavailability of poorly soluble drugs.
• Prevent the volatilization of the drug and improve the stability of the drug.
• Mask the bad smell of the drug.
• Reduce the toxicity and irritation of the drug.
• Powder the liquid medicine.
• Regulate the release rate of the drug preparation.

Commonly used inclusion materials include cyclodextrin, cholic acid, starch, cellulose, protein, nucleic acid, etc.

Commonly used inclusion techniques mainly include saturated aqueous solution method, grinding method, ultrasonic method, freeze drying method, spray drying method, etc.

The verification methods of inclusion complexes include X-ray diffraction, infrared spectroscopy, nuclear magnetic resonance, thermal analysis, and ultraviolet spectrophotometry.

3. Preparation Technology of Microcapsules and Microspheres

Microencapsulation is to use natural or synthetic polymer materials (called capsule materials) as the membrane wall shell, and wrap solid drugs or liquid drugs (called capsule cores) to form drug storage-type microcapsules, referred to as microcapsules. If the drug is dissolved and/or dispersed in the polymer material matrix, the tiny spherical entities of the matrix type are formed, which are called microspheres.

Fig. 1 Microencapsulation technology

The characteristics of drug microencapsulation are as follows:

• Mask the bad smell and taste of the drug
• Improve the stability of the drug
• Prevent the drug from being in the stomach or reduce the irritation to the stomach
• Solidify the liquid medicine
• Reduce the compatibility changes of compound drugs
• Control the release rate of the drug preparation
• Make the drug focus on the target area, improve the curative effect, and reduce the toxic and side effects of the drug
• Bioactive substances such as live cells and vaccines can be encapsulated without causing loss of activity or denaturation

The preparation methods of microcapsules include three types: physical-chemical method, physical-mechanical method and chemical method. Different preparation methods are selected according to the properties of the drug and the capsule material and the particle size, release requirements and targeting requirements of the microcapsules.

The preparation method of microspheres is similar to the preparation method of microcapsules. Different preparation methods of microspheres can be selected according to the properties of drugs and materials.

4. Liposome Preparation Technology

Liposomes are bilayer spherical vesicles composed of lipids such as phospholipids. Liposomes encapsulate drugs in lipid bilayers to form a micro-drug delivery system, which is a new dosage form similar to microcapsules.

Liposome pharmaceutical preparations have the following characteristics:

• The preparation process is simple. General drugs are easier to encapsulate in liposomes.
• The same liposome can encapsulate both water-soluble and fat-soluble drugs.
• Make the drug have targeting characteristics in vivo.
• Reduce drug toxicity and enhance drug efficacy.
• Reduce the elimination rate of the drug, prolong the action time of the drug, and improve the stability of the drug.

Liposome preparation techniques mainly include thin film dispersion method, reverse phase evaporation method, double emulsion method, melting method, injection method, freeze-drying method, etc.

Fig. 2 Liposome structure

• Technical Support for Preparation
  
  • Hot melt extrusion technology
  • Liquid Capsule Filling Technology
  • Transdermal technology
  • Membrane Controlled Release Technology

• Advantages of services
  
  • Diverse Technology Platforms
  • Research on traditional dosage forms and high-end formulations
  • Experienced technical team

Relying on professional technical level and rich research experience, BOC Sciences can ensure the standard and efficient completion of preparation technology research and quality research, and finally realize the industrial production of products.