Presenting the Definition, Classification, and Composition of Drug Suspensions.

6. Some examples of emulsions

6.1. Natural emulsion

Prepared from oil seeds and has no pharmacological effect. Convention: one part seed is prepared into 10 parts emulsion.

For example: Peanuts 10g Distilled water 100ml

The emulsion oil phase is the oil in the seeds, the emulsion water phase is distilled water and water in the seeds, the emulsifier is the albumin in the seeds.

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Procedure: Soak peanuts in hot water, remove the silk shell, put the white peanuts in a mortar, add an equal amount of distilled water and grind thoroughly into a smooth paste, add the remaining water and grind well, rub through gauze to collect the emulsion.

6.2. Potio emulsion

Presenting the Definition, Classification, and Composition of Drug Suspensions.

Potio has 3 types: main potio, emulsion potio and suspension potio.

Potio emulsion combines water-soluble and oil-soluble pharmaceutical ingredients and additives into a homogeneous liquid form.

Example: Rp Bromoform 2g

Sodium benzoate 4g

Codeine phosphate 0.2g

Single syrup 20g

Oil emulsion v.s. 100ml

Mf potio

Oil phase: includes oil of oil emulsion and Bromoform

Water phase: distilled water of emulsion, simple syrup, codeine phosphates and sodium benzoate. Emulsifier gum arabic 9g.

Procedure: weigh and grind 9g of gum arabic/clean, dry mortar. Dissolve 2g of bromoform in 10g of vegetable oil, add the oil phase to the gum, stir gently to absorb the gum evenly, add 18ml of water, use a pestle to beat quickly and continuously to get a thick emulsion.

Dissolve sodium benzoate in 20ml hot water then dissolve codeinphosphas.

Use the remaining water to dilute the thick emulsion, then mix the sodium benzoate solution, codeine phosphates and simple syrup into the diluted emulsion, adding enough water to make 100ml.

Bottled and labeled properly, with the words “shake before use” added to the label.

6.3. Medicinal oil emulsion

Oil emulsions are prepared from pharmacologically active oils. They may or may not dissolve additional synergistic active ingredients and additives. The oil ratio is very high, so a mixture of emulsifiers must be used: gum arabic – agar – jelly or tween – span.

Example Rp Paraffin Oil 35g

Tween 80 and span 80 6g Distilled water q.s. 100ml

Procedure: weigh paraffin oil into a glass cup, heat water at 60 o C and dissolve span into hot oil.

Heat water to about 65 o C, dissolve tween 80 into hot water.

Combine two phases using dispersing force to create an emulsion and pass the emulsion through a homogenizer.

Bottled and labeled properly, with the words “shake before use” added to the label.

6.4. Injectable emulsions

Prepared from fats such as vegetable oils: soybean oil, sesame oil, olive oil for infusion to provide fatty acids and energy for the body.

The size of the oil phase should be approximately 0.5µm in diameter (< 1µm and no particles > 1µm).

Strong, non-toxic, easily metabolized emulsifiers such as de-cephalinized lecithin and hydrogenated to saturate fatty acids or polysorbate (Tween) or polyglyceryl monooleate (Demol), polypropylene derivatives with PEG (Pluronic).

Increase viscosity with glucose, sorbitol, glycerol. Antioxidant tocopherol 0.1%.

Prepare under sterile conditions, store in silicon-lined vials and in an inert atmosphere (nitrogen).

Substances that do not change the composition of blood and cause red blood cells to clump. For example: Cotton seed oil 15ml

Dextrose 4 g

Lecithin 1.2 g

Pluronic F.68 0.3 g

Distilled water to 100ml

Combine oil and lecithin. Heat to 70 o C.

Add Dextrose and Pluronic F.68 to water, heat to 90 o C.

Mix the two phases together and then disperse them in a homogenizer. Bottle. Steam for 20 minutes at 15 PSI (1kgf).

Currently, sterile emulsions for injection are usually prepared by homogenization at high temperature and pressure, by which emulsions with a size smaller than 1 µm can be prepared. For sterilization, heat or filtration can be used.


VALUATION

I. Choose true or false:

1. Sterile emulsions for injection are usually prepared by homogenization at moderate temperature and pressure.

2. Medicinal oil emulsions are prepared from oils that have no pharmacological effects.

3. Natural emulsions are prepared from oil seeds and have no pharmacological effects.

4. When preparing medicated oil emulsions, it is conventional to use one part of the granules to make 10 parts of emulsion. Answer:

5. When preparing an emulsion, the longer the stirring time and the greater the dispersion force, the easier it is for the emulsion to form.

6. D/N emulsions are more easily formed when oil is added to water. Answer:

7. Changing pH will change the emulsification mechanism of Gelatin. Answer:

8. PEG is an emulsion stabilizer due to increasing the viscosity of the medium. Answer 9. Oral emulsions are N/D type emulsions. Answer

10. A concentrated emulsion is one where the concentration of the dispersed phase is less than 10% of the total system. Answer:

II. Fill in the blanks:

1. Injectable emulsions are prepared from fats such as vegetable oils to provide

.....(A)..... and ...(B)..... for the body.

2. In the oil-medicinal emulsion, the oil phase ratio is ...(A).... so a mixture of .....(B).... must be used such as: Gum ....(C).... or tween-span

3. In natural emulsions, the oil phase is ....(A)...., the water phase in the emulsion is....(B)....... and the emulsifier ..(C).... is present in the seeds.

4. The main disadvantage of emulsions is.......

5. In an emulsion, the oil phase includes all the active ingredients and the carrier or excipients.

.....(A).... The aqueous phase consists of liquids or is dissolved in liquids....(B)....

6. To evaluate the quality of emulsion, people rely on the following parameters:

A. Shape and size of dispersed phase particles B. .........................................

C. ...... of the dispersion medium and the dispersed phase.

D. Decomposition time and ..........

7. The stable emulsifiers commonly used in preparing emulsions are: .....(A)......., Polyvinylic alcohol and .....(B).........

8. Normally, depending on the nature of the emulsifier, two types of emulsions will form:

....(A)... and .....(B).....

9. Emulsions are microheterogeneous mechanical dispersions formed by two liquids ....(A)..... In which one liquid is .....(B).... into the second liquid.

10. Drug emulsion consists of three main parts: .....(A)......., Emulsifier and .....(B)....

III. Choose the best answer:

1. Tweens belong to the group of surfactants:

A. Ionization, cation

B. Non-ionizing, for D/N emulsions

C. Non-ionizing, for N/D emulsions

D. Bisexual

2. Gum arabic belongs to the group of emulsifiers:

A. Active surface

B. Synthetic water-based adhesive.

C. Natural water-based glue, used for D/N emulsions

D. Natural water-based glue, used for N/D emulsions

3. Cholestrol is an emulsifier and wetting agent used to prepare:

A. Cream D/N B. Lotio

C. Potio emulsion D. Ointment emulsion N/D

4. The ratio of gum arabic used to emulsify the oil base is mainly based on:

A. Gum quality

B. Density of dispersant

C. Viscosity of the dispersion medium

D. pH of the dispersion medium

5. To determine the parameters of the emulsion, we rely on the following factors:

A. Dispersion phase ratio.

B. Viscosity of the dispersed phase

C. Shape and size of particles of the dispersion medium

D. Decomposition time of emulsifier

6. The emulsion is more stable when:

A. The greater the concentration of the dispersed phase

B. The smaller the concentration of the dispersed phase

C. The larger the size of the dispersed phase particles

D. Low viscosity of dispersion medium.

7. Emulsifiers in the form of small particles are:

A. Solids that dissolve in water and do not dissolve in oil

B. Solids that are soluble in oil and insoluble in water

C. Solid insoluble in water and oil in the form of very fine powder

D. Solid insoluble in water and oil in the form of semi-fine powder

8. Saponins:

A. Easily soluble in water, is an emulsifier that creates N/D emulsions

A. Easily soluble in water and oil, is an emulsifier that creates D/N emulsions

C. Easily soluble in water and alcohol, is an emulsifier that creates D/N emulsions

D. Easily soluble in water and alcohol, is an emulsifier that creates N/D emulsions

9. Carbohydrates are substances that:

A. Has large molecules and is easily soluble or swells in oil

B. Has large molecules and is easily soluble or swells in water

C. Has small molecules and is easily soluble or swells in water

D. Has large molecules and is easily soluble in water.

10. The type of emulsion depends on:

A. Solubility, permeability and emulsifier ratio

B. Solubility, permeability and dispersion ratio

C. Solubility, permeability and substance ratio of the dispersion medium

D. Solubility and permeability of emulsifiers.

IV. Answer the following questions:

1. Describe the concept and advantages and disadvantages of emulsion?

2. Given the formula:

Castor oil 30g

Gum Arabic 10g

Peppermint essential oil 3 drops

Gum syrup 20g

Distilled water to 100ml

Find the method of emulsion preparation and type of emulsion?

3. Given the formula:

Paraffin oil 500ml

Adragant Gum 2.5g

Gum Arabic 50g

Jelly 5g

Lemon essential oil 1ml Vanillin 0.2g

Sodium benzoate 1.5g

Glycerin 50ml

Distilled water 1000ml

Find the right combination of emulsifiers?

4. Given the formula:

Paraffin oil 50g

Polyethyleneglycol 400 7g

Sodium bezoate 0.2g

Single syrup 20g

Distilled water to 100ml

Look for emulsifier in the formula, type of emulsifier and method of preparation?

5. Describe the types of emulsions and how to identify the type of emulsion?

6. Describe the technique of preparing emulsions by separating each co-miscible solvent phase with two phases?

7. Describe the technique of preparing emulsion using wet and dry glue methods?

8. List the factors that affect the formation and stability of emulsions?

CHAPTER 7

MEDICINAL SUNSCREEN


TARGET

1. Describe the definition, classification, and composition of drug suspensions.

2. Analyze the advantages and disadvantages of drug mixtures

3. Describe common methods of preparing drug mixtures.

4. Analyze the composition, methods and preparation sequence of some drug suspensions on the market.


CONTENT:

1. General

1.1. Definition

Drug suspensions are liquid medicines for oral, injection, or topical use containing insoluble solid pharmaceutical ingredients dispersed uniformly in the form of very small particles (diameter greater than 0.1 micrometers) in a carrier such as water or oil.

The term “Milk” is sometimes used to refer to suspensions with an aqueous carrier intended for drinking (e.g. Milk of Magnesia). The term “Magma” is often used to describe suspensions of inorganic solids such as bentonite dispersed in water, which have a strong tendency to hydrate and to aggregate the solid particles to produce a viscous texture and thixotropic rheology.

The term “Topical” is used to classify suspensions and emulsions applied to the skin for topical action.

Complete suspension for immediate use: Is a cloudy liquid or liquid with a layer of sediment at the bottom of the bottle, when shaken gently this sediment must be evenly dispersed back into the carrier.

Powder or granule form: Before use, convert into a complete suspension by shaking with an appropriate amount of carrier.

The suspension is not for intravenous or intra-arterial use.

1.2. Classification of suspensions

1.2.1. According to the origin of the conductor

- Water suspension - Oil suspension - Glycerin suspension

1.2.2. By route of administration

- Oral suspension

- Suspension for subcutaneous and intramuscular injection (not for intravenous or spinal injection)

- External suspension

1.2.3. According to particle size

Coarse suspension is a heterogeneous dispersion of solid particles larger than 1 m, with the maximum limit of solid particles in the range of 50 - 75 m.

Colloidal suspension (collodial suspension) also known as turbid suspension is a micro-heterogeneous dispersion system of solid particles with size smaller than 1 m, for example aluminum hydroxide and magnesium hydroxide suspension. In colloidal suspension, the size of solid particles is almost as small as colloidal particles, so they follow Brownian motion and other thermodynamic phenomena, so they are quite stable and often in a turbid liquid state.

1.3. Ingredients

Pharmaceutical substances

The main active ingredients are solids that are insoluble or very slightly soluble in the carrier. There are two types:

type:


- Insoluble type but has a surface of particles that are easily permeable in the dispersion medium

- Type of conductor that is difficult to penetrate

Distributed environment

- Dispersion medium includes water and polar liquids, or oil and other substances.

nonpolar liquid

- There are also pharmaceutical preservatives, flavoring agents, and anti-mold preservatives.

1.4. Characteristics of drug suspension

- The outstanding feature is that the drug has a mechanical dispersion structure, so it is not thermodynamically stable, the dispersed phase will gradually separate from the dispersion medium.

- Suspension is a cloudy liquid or liquid with a layer of sediment at the bottom of the bottle. When shaken, the sediment will disperse back into the cloudy liquid.

- Regarding naming the mixtures, they are named according to their usage.

- In terms of physics and chemistry, suspensions are heterogeneous dispersions, composed of a solid dispersed phase and a liquid dispersion medium.

1.5. Advantages and disadvantages of drug mixtures

1.5.1. Advantages

- Solid drugs that are insoluble or slightly soluble in carriers can be prepared in liquid form, and drugs can be introduced into the body through more routes than when prepared in solid form; oral medications are easier for children.

- Limits the disadvantages of some drugs when dissolved, they will not be stable, have an unpleasant taste, and irritate the digestive mucosa (antibiotics).

- Make the drug work slower but last longer or limit the effect of the drug locally.

- Limit the toxic effects of some drugs.

1.5.2. Disadvantages

- It is a heterogeneous dispersion system, thermodynamically unstable, difficult to prepare and unstable.

- If not prepared and used carefully, the dosage will not be accurate and may be harmful to the patient.

1.6. Quality requirements for suspension drugs General requirements :

When left undisturbed, the solid drug can be separated but must return to a state of homogeneous dispersion in the carrier when gently shaken for 1 - 2 minutes and maintained in that state for several minutes.

Requirements for pH, qualitative, quantitative, volume error and other technical requirements : Meet the regulations in the separate monograph.

Suspension for injection or eye drops :

Must meet the requirements for Sterility Testing and particle size requirements specified in the specific monograph.

Powder or granules for mixing suspension :

Must meet the general requirements of Powder or Granule form.

When left alone, the dispersed solid may separate into separate layers but must return to a state of uniform dispersion in the carrier. Gently shake the bottle for 1-2 minutes and maintain that state of dispersion for several minutes.

2. Factors affecting the formation, stability and bioavailability of drug suspensions

2.1. Effect of permeability of dispersion medium of insoluble solids .

For the suspension to form and stabilize, the solid particles must be permeable to the dispersion medium.

- Solid hydrophilic drugs are easy to prepare to meet the requirements of liquid drug suspensions.

- Solid, water-soluble pharmaceuticals are easy to prepare to meet the requirements of oil suspensions.

To make the solid drugs hydrophilic into hydrophilic, people use molecular surfactants with two parts: hydrophilic and hydrophilic. When added to the two solid-liquid phases of the molecular suspension, the surfactant will orient the contact surface of the two phases to create a molecular membrane, ions are created around the solid particles, reducing the surface tension between the two phases, so the solid particles are more permeable to the carrier.

In addition, hydrophilic colloids or some very small particle hydrophilic inorganic solids are also used to convert hydrophilic solids into hydrophilic ones.

When preparing injectable and topical drug suspensions, surfactants are used as permeating agents.

To prepare oral suspensions, people use hydrocolloids or hydrophilic solids in the form of small particles as permeating agents.

2.2. Effect of two-phase density

The smaller the difference in density between the dispersed solid drug and the dispersion medium liquid, the more stable and sustainable the suspension will be.

2.3. Effect of dispersed particle size

The smaller the size of the dispersed particles (due to the strong dispersing force and the ability of the wetting agent to disperse like a surfactant), the easier it is to form and stabilize the suspension.

2.4. Effect of viscosity of the carrier

The greater the viscosity of the carrier, the easier and more stable the suspension will be.

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