PHARMACEUTICAL CAPSULE
Capsule
Capsule is solid
dosage forms in which one or more medicinal and or inert substances are
enclosed within a small shell or container generally prepared from
a suitable form of gelatin. Depending
upon their formulation, the gelatin capsule shells may be hard or soft.
Characteristics:
1. May be swallowed whole by the
patient.
2. May be inserted into the rectum
for drug release and absorption from the site.
3. The contents may be removed from the gelatin shell and employed as a pre measured medicinal powder, the
capsule shell being use to contain a dose of the medicinal substance.
4. Elegance.
5. Ease of use.
6. Portability.
7. Tasteless shell to mask the unpleasant taste/odor of the drug.
8. Permits physician to prescribe the exact medication needed by the
patient.
9. Conveniently carried.
10. Readily identified.
11. Easily taken.
12. tasteless when swallowed.
13. Commonly embossed or imprinted on their surface the manufacturer’s name and product code readily
identified.
Components of
Capsules
1. Gelatin.
2. FD & C and D & C
colorant.
3. Sugar.
4. Water – 12 to 16 % but may vary
depending on the storage condition.
5. Sulfur dioxide (.15%) – prevent
decomposition during manufacture.
6. Opaquants/Opacifying agent –
titanium dioxide.
Type
of capsule
The two main
types of capsules are-
1-Soft gel
encapsulation
In 1834, Mothes
and Dublanc were granted a patent for a method to produce a single-piece
gelatin capsule that was sealed with a drop of gelatin solution.
They used
individual iron moulds for their process, filling the capsules individually
with a medicine dropper.
Modern
soft-gel encapsulation uses variations of a process developed by R.P. Scherer
in 1933.
His innovation was to use a rotary die to produce the capsules, with
the filling taking place by blow molding.
This method reduced wastage, and was
the first process to yield capsules with highly repeatable dosage.
2. HARD
GELATIN CAPSULES
Two-part hard
gelatin capsule
Also referred to as “DFC” Dry Filled Capsule.
Manufactured into two
sections, the capsule body and a shorter cap.
A recent innovation in capsule shell design is the Snap-Fit, Coni-Snap,
and Coni Snap Supro hard gelatin capsules.
Capsule
size
|
Empty Hard |
||||
|
Size |
Outer Diameter (mm) |
Height or Locked Length (mm) |
Actual Vol. (mL) |
Typical Fill Weights (mg) 0.70 Powder Density |
|
000 |
9.91 |
26.14 |
1.37 |
960 |
|
00 |
8.53 |
23.30 |
0.95 |
665 |
|
0 |
7.65 |
21.70 |
0.68 |
475 |
|
1 |
6.91 |
19.40 |
0.50 |
350 |
|
2 |
6.35 |
18.00 |
0.37 |
260 |
|
3 |
5.82 |
15.90 |
0.30 |
210 |
|
4 |
5.31 |
14.30 |
0.21 |
145 |
|
5 |
4.91 |
11.10 |
0.13 |
90 |
For human use,
empty capsules ranging in size from 000 the largest to 5 the smallest. Generally, hard gelatin capsule are used to
encapsulate between 65 mg to 1 gram.
Characteristic
§ Usually
use in the extemporaneous compounding of Rx.
§ Made of gelatin, sugar, and water.
§ Clear, colorless and essentially tasteless.
§ Colored with various FD & C and D & C
dyes and made opaque by adding agents such as titanium dioxide.
Combination of colorants and Opaquants to make
them distinctive, many with caps and bodies of different colors.
Plasticizers:-
§
The amount of
plasticizers used to make the capsule to hard or soft.
§
The plasticizers are
used – Glycerin, Sorbitol.
Preservatives:-
§
If included, is
generally a mixture of Methylparaben (4part) and Propylparaben
(1part) to the extent of 0.2%.
Flavors:-
§
If added, should not
exceed 2%.
§
Generally the flavors
are used- Ethyl vanillin or essential oils.
Sugar:-
§
If included, may be up
to 5% to give the gelatin shell desirable chewable characteristics.
Additives:-
a) Diluents:-
§
The diluents have to be
added to bring the medicament up to a desired bulk.
§
The quantities of
diluents are related to the dose of the medicament and the capsule size.
b) Protective
sorbents:-
§
Sometimes some inert
materials are included to prevent the absorption of moisture by hygroscopic
substances.
§
Materials like –
oxides and carbonates of Mg or Ca.
c) Glidants:-
§ Glidants
become essential when the powders are filled by automated machinery requiring
their regular flow in the capsule bodies.
§
Glidants like– Talc,
Stearates.
d) Anti-dusting
compounds:-
§ These
are the compounds which prevent the flow of dust particle of the drug in the
air to causes health hazards.
§ Anti-dusting
compounds like- inert edible oils.
Gelatin
§ It is obtained by the partial hydrolysis of collagen
obtained from skin, white connective tissue and bones of animals.
§ Available in
the form of a fine powder, a coarse powder, shreds, flakes, or sheets.
§ Stable in air
when dry but when become moist – subject to microbial decomposition.
§ HGC contain
13 to 16 % of moisture.
§ Extreme
dryness- capsules may become brittle and crumble.
Manufacture of
Hard Gelatin Capsule
§ Manufactured
into 2 sections, the capsule body and the shorter cap.
§ The 2
parts overlap when joined, with the cap fitting snugly over the open end of the
capsule body.
§ Shells are produced by chemical dipping of pins or pegs of the desired shape and diameter into a
temperature-controlled reservoir of melted gelatin mixture.
§ The
pegs made of manganese bronze, are affixed to plates, each capable of holding
up to about 500 pegs.
§ Each plate is mechanically lowered to the
gelatin bath, the peg submerge to the desired depth and maintained for the desired period to achieve the proper
length and thickness of coating.
§ The plate and the pegs are slowly lifted from
the bath and the gelatin dried by a gentle flow
of temperature-and humidity-controlled air.
§ When dried, each capsule part is trimmed
mechanically to the proper length and removed
from the pegs, the capsule bodies and caps are joined.
Capsules
parameter as per I.P.
|
Product |
Dose (m.g.) |
Conversion (m.g.) |
Drug content (%) |
Dissolution (%) |
|
amoxicillin |
250 |
285 |
90-110 |
80 |
|
Ampicilline Trihydrate |
250 |
287 |
92.5-104.5 |
75 |
|
Cephalexin Monohydrate |
250 |
270 |
90-110 |
75 |
|
Doxycycline |
100 |
116 |
90-120 |
65 |
|
Rifampicine |
150 |
165 |
92.5-107.5 |
70 |
Filling Hard
Capsules Shells
1. Use Punch Method
§ powder
is placed on a sheet of a clean paper or porcelain plate,
§ using
spatula – formed into a cake having a depth of approximately one-fourth to
one-third the length of the capsule body,
§ then
empty capsule body is held between the thumb and forefinger and punched
vertically into the powder cake repeatedly until filled,
2.
Feton capsule filling
- with empty capsule in the loader
tray, the tray placed on top of the filler unit, - the loader inserts the capsules into the
filling unit and is removed, and
the top plate is lifted to separate the caps from the bodies, - the powder is placed on the unit and the
capsule bodies filled, - the top plate is returned to the
unit and the caps placed on filled capsule bodies,
Process Capsule
Filling
1. Milling /Sieving of all Ingredients.
2. Blending Powder Blender / Empty Capsules.
3. Capsule Filler.
4. Capsule
cleaner.
5. Capsule injection screen.
6. Capsule check-weighing system/reject.
7. Finished capsules.
ProFill 100
– The ProFill 100 Capsule Filling Machine utilizes an advanced design for
fool-proof manual filling of two-piece capsules.
With the ProFill 100 machine,
there is no need for expensive capsule filling equipment and electrical/vacuum
connection.
Capsule Filling Machine:-
Manual and Semi-Automatic Capsule
Filling Machine
Finishing:-
The filled the
sealed capsules necessitate finishing operation before inspection, bowling or
packing in strips and labeling. The following steps are involve in the
finishing process-
§ Pan
polishing.
§ Cloth
dusting.
§ Brushing.
§ Sealing.
§ Inspection
(ROTOSORT).
Evaluation
of capsules:-
1.
Uniformity of weight.
2.
Content of active
ingredients in capsules.
3.
Disintegration.
4.
Dissolution.