Capsules (2)-SGC PDF Lecture 8 PDF

11/22/2024 Types of Capsules 1  11/22/2024 Types of Capsules A- Hard gelatin B- Soft gelatin Capsules Capsules B- Soft gelatin Capsules (Softgels) 2...

11/22/2024 Types of Capsules 1  11/22/2024 Types of Capsules A- Hard gelatin B- Soft gelatin Capsules Capsules B- Soft gelatin Capsules (Softgels) 2  11/22/2024 Soft gelatin capsule: (a) (one piece)  Composed of one Continuous gelatin shell surrounding the core (drug with or without excipients) (b) Capsule shell Usually contain higher amount of the plasticizer (glycerol, sorbitol , PG)  change the mechanical properties of gelatin  more flexible capsule (c) Medications (usually liquid or semisolid) : the active ingredient can be incorporated into the outer shell, the inner core, or both. A wide range of shapes of soft gelatin capsule is available, including round, oval, oblong, tubular, and pear shaped The common between two types is the shell (gelatin capsule) Composition of Capsule shells 1- Shell material (mainly gelatin) + water 2- colorants 3- plasticizers in soft capsules. 4- Optional excipients (processing aids). 3  11/22/2024 The softgel usually composed of two main components: (b) The filling material (medication (a) The outer gel mass with or without excipients).  That forms the softgel shell Usually Liquid (but not water) 1- Gelatin a- Lipophilic liquids: vegetable oils (e.g. 2- water soyabean oil) for oil- soluble vitamins and 3- plasticizers drugs. 4- other excipients (colorant, b- Hydrophilic liquids: PEG400. preservative…etc) C- Emulsion, Microemulsion and nanoemulsion systems. d – Suspensions (can take up to 30% solid). Advantages of soft gelatin capsules (softgels): 1. The ability to use liquid drug formulations  Better drug absorption  (rapid onset of action). 2. Mask the bitter and unpleasant taste of some liquid medications (cod-liver oil) 3. Ease of use -easy to swallow 4. Elegant appearance. 5. Accurate dose (compared to liquid dosage forms) 6. Overcome problems with manufacturing of oils and liquid drugs (compared to tablets) 7. Formed, filled, and sealed in one operation. 4  11/22/2024 Disadvantages of soft gelatin capsules: 1. Small scale production is not possible not easily prepared except on a large scale and with specialized equipment. 2. Expensive, when compared with direct compression tablets or HGC. 3. There is a more intimate contact between the shell and its liquid contents than exists with dry-filled hard gelatin capsules increased possibility of interactions. 4. Not adaptable to incorporate more than one kind of fill into the same capsule (compare with hard shell capsules). Different forms of softgels a. Regular conventional softgels: Easy to swallow containing oils, solutions or suspensions rapidly release their contents in the stomach  rapid onset of action. 5  11/22/2024 Different forms of softgels b. Chewable softgels:  A highly flavored shell is chewed to release the liquid drug fill to the mouth cavity. Flavored with different flavors such as orange and strawberry for kids.  favorable for children and elderly. c. Suckable softgels:  consist of a gelatin shell containing: Flavored medication to be sucked  Usually for oral dosing of a pediatric product. d. Twist-off :  Softgel has a tag to be twisted or snipped off  allowing access to the fill material.  very useful for unit dosing of topical medication (e.g. skin and hair products) , or inhalations 6  11/22/2024 e. Meltable softgels: designed for use as suppositories or pessaries Different forms of softgels a. Regular conventional softgels b. Chewable softgels c. Suckable softgels d. Twist-off e. Meltable softgels 7  11/22/2024 Advanced forms of softgels: b. Enteric coated capsules: The capsules are coated with gastric-resistant polymer (such as shellac and cellulose acetate phathalate), so they resist dissolution in the low pH of stomach but dissolve in the higher pH of intestine. It is usually used if: A- The drug is destroyed in the gastric fluids. B- The drug is irritating to the gastric mucosa. C- A high local concentration of the drug is desirable in the intestine not stomach , as in the case of anthelmintic. Preparation of soft gelatin capsules: (ROTARY soft capsule machine) Before the encapsulation process takes place, there are two sub- processes that are often carried out simultaneously, yielding the two components of a softgel. These are: (a) the fill matrix for the contents. (b) the gel mass which will provide the softgel shell, This is followed by c) encapsulation into the soft-gel shell (Rotary die encapsulation) All performed in one machine in a continuous process 8  11/22/2024 Preparation of soft gelatin capsules: a) the liquid fill matrix formation The liquid fill matrix containing the active drug substance manufactured separately from preparation of the molten gel. Manufacture of the active fill matrix involves dispersing or dissolving the drug substance in the non- aqueous liquid vehicle using conventional mixer homogenizers. b) formulation of the outer gel mass that forms the soft-gel shell (1) Gelatin + water  gel mass (2) Once the gelatin is fully dissolved  other  plasticizer is added (as glycerol). components of the capsule shell are added (colors, opacifier, flavors and preservatives) (3) Air removed by vacuum  to avoid airbubbles (4) The hot gel mass is then supplied through heated transfer pipes to a cooling drum in the encapsulation machine by casting method  forms two separate gelatin ribbons (5) During this casting process  the gelatin passes through sol-gel transition  Forms gel ribbons the thickness of each is controlled to ± 0.1 mm.  The two gel ribbons are then carried through rollers to the rotary die encapsulation tool 9  11/22/2024 b) formulation of the outer gel mass that c) Drug encapsulation into the forms the soft-gel shell soft-gel shell: (1-3) (4) (5) (5) During this casting process  the gelatin passes through sol-gel transition  Forms gel ribbons the thickness of each is controlled to ± 0.1 mm.  The two gel ribbons are then carried through rollers to the rotary die encapsulation tool. c) Drug encapsulation into the soft-gel shell (Rotary die encapsulation): (6) Accurately metered volumes of the liquid fill matrix are injected from the device into the space between the gelatin ribbons as they pass between the die rolls  Drug is enclosed inside the fusing ribbons to form the body of the capsule around the core drug material. (7) The two softgel capsule halves are sealed together by the application of heat pressure. (8) The formed softgels are released into a cooling collection belt, while the excess gelatin sheets are recycled for re-use 10  11/22/2024 b) formulation of the outer gel mass that c) Drug encapsulation into the forms the soft-gel shell soft-gel shell: (1-3) (4) (6) (7) (8) (5) c) Drug encapsulation into the soft-gel shell: It is possible to make bicoloured softgels using gel ribbons of two different colours. 11  11/22/2024 Limitations for materials for capsules filling: Some materials cannot be used for capsules filling such as 1- Must not dissolve gelatin (aqueous or hydro-alcoholic solutions). 2-Must not contain a high level of free moisture  can be absorbed by gelatin causing it to soften. 3-Deliquescent or Hygroscopic drugs absorb water from the capsule shell  brittle capsule  cracking of the capsule.  The addition of an adsorbent like magnesium carbonate, magnesium oxide overcomes this difficulty. 4- Must not react with gelatin e.g. formaldehyde. 12