Getting Close to Know The Pharmaceutical Excipient (1)

     According to Indonesian’s health law number 36 in 2009, that included into category of pharmaceutical dosage form are modern drugs, traditional medicines and cosmetics. In the formulation, these pharmaceutical preparations contain of active ingredients and also additional ingredients or known as excipients.

     Excipients are ingredients added into pharmaceutical formulation, with the aim as a support in the preparation formula, so that the intended use of the preparation can be achieved. Excipients will facilitate the conditions of the mass of preparations so that the production process can be carried out easily. In addition, the presence of excipients will help the dissolution of active ingredients in the body. In pharmaceutical formulation, the excipient must have the following requirements:

1.     Safety

The excipients must be safe. As much as possible, excipients should not contain pathogenic microorganisms, a toxicity that can damage the active ingredients and have a negative impact on organs in the body. These requirements are fundamental in the selection of excipients. Apart from that, the dose of use of excipients must be considered.

2.     Inert

Excipients may not have a formulation's side effect or pharmacological impact on the active ingredients. As in formulation, excipients may not influence the active ingredients so that they can change the characteristics of the active ingredients. In addition, pharmacologically, excipients may not have a therapeutic effect in the body or toxicity.

3.     Stability

The excipient must have physical, chemical and microbiological stability during storage, both before use and after the production process until a pharmaceutical dosage form is obtained.

4.     Supports bioavailability

The bioavailability of drugs in the body is a determining factor for the success of drug therapy. Excipients in a preparation formulation must be able to support this. Excipients in the formulation should not inhibit the release of active ingredients which will have an impact on the bioavailability of drugs in the body.

5.     Cheap and easy to obtain

Continuity and the availability of excipients on the market is also a factor that must be considered by a formulator before choosing the excipient. This will have an influence on the sustainability of the industry in producing preparations.

     In pharmaceutical dosage form, excipients can be considered as vehicles for active ingredients to enter the body. Therefore, the excipient will naturally interact with the active ingredient. This interaction must be considered by a formulator so they have not a negative impact on active ingredients and patients. Interactions that can occur are:

1.     Physical interactions.

It is an interaction that does not involve changes in components, structures or chemical reactions. Physical interaction is more directed towards incompatibility that can be happen not only between of each excipients but also excipients with active ingredients. This interaction generally causes physical change of the product and that dissolution rate. Some examples of physical interactions are the processes of complex formation, adsorption and solid dispersion.

2.     Chemical interactions.

This type of interaction involves a chemical reaction between the excipient and the active ingredient. Chemical interactions generally have an adverse effects on the product. This is because of the chemical reaction that produce a new compounds. This product has an influence to the production process, the physical form of the drugs and also the formation of new products that can have a negative effect on health. One example of chemical interactions is the hydrolysis reaction.

3.     Biopharmaceutical interactions

It is an interaction that occurs when the pharmaceutical dosage form has entered into the body and then cause physiological reactions. This interaction is influenced by the composition of fluids in the body, coefficient partition of the active ingredient, dissolution and absorption rate of the drug in the body.

     By understanding the mechanism of interaction, the formulator will be able to choose the right excipient for the formulation. By this, the bioavailability of the active ingredients will be met so that the therapeutic effect will be achieved.

Source :

1.      A. Alfaridz dan I. Musfiroh. “Interaksi Antara Zat Aktif dan Eksipien dalam Sediaan Farmasi”. Majalah Farmasetika, 5 (1) 2020, hal. 23-31.

2.      Departemen Kesehatan RI. “Undang-Undang Republik Indonesia Nomor 36 Tahun 2009 Tentang Kesehatan”. 2009. Jakarta: Kementrian Kesehatan RI.

3.      Effionora Anwar. “Eksipien dalam Sediaan Farmasi: Karakterisasi dan Aplikasi”. 2012. Jakarta : PT. Dian Rakyat