Applications of Carbohydrates in Pharmacy

1. Associate Professor of Pharmacognosy , Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
•Associate Professor, City of Scientific Research and Technological Applications (SRTA-City), Alexandria,
Egypt
•Senior research fellow, Liaoning University of Traditional Chinese Medicine, China (20118-2019)
•Visiting scholar, School of Pharmacy, University of Mississippi, USA (2012-2014)
Ahmed Metwaly

2. ▪
▪is used (by i.v. or orally) for treatment calcium deficiency.
▪These salts are characterized by being more easily absorbed than other Ca
salts.

3. ▪ Hypocalcaemia
▪ Hyperkalaemia
▪ Magnesium sulphate overdose
▪ Hydrofluoric acid burns
The calcium gluconate reacts with hydrofluoric acid to form insoluble, non-toxic
calcium fluoride. In addition to a 2.5% calcium gluconate gel being applied directly to
the chemical burn
▪ nausea, constipation, and upset stomach.
▪ Rapid intravenous injections of calcium gluconate may cause hypercalcaemia, which can result in
vasodilation, cardiac arrhythmias, decreased blood pressure, and bradycardia.

4. FERROUS GLUCONATE
▪
▪ (orally or by i.v.) is used in iron deficiency.
▪ These salts are characterized by being more easily absorbed than other iron salts.

5. ▪An Sugar alcohol
▪Preparation:
▪Sorbitol is prepared by reduction of glucose

6. Mechanism of action
Sorbitol exerts its laxative effect by drawing water into the large intestine, thereby stimulating bowel movements.
Uses:
• mild laxative
• sweetening agent in dietetic food (not absorbed), chewing gum &
tooth pastes.
• Test of kidney function (iv), not metabolized.

7. ▪Preparation
by reduction of mannose.

8. ▪ Osmotic diuretic
osmotic diuretic that is metabolically inert in humans and occurs naturally in fruits and vegetables
▪ cerebral edema, elevated intracranial pressure, and cerebrospinal fluid
Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid,
into interstitial fluid and plasma. As a result, cerebral edema, elevated intracranial pressure, and cerebrospinal fluid volume and
pressure may be reduced.
▪ laxative, and in
▪ tests of kidney function (not metabolized if i.v.)
Toxicity
Mannitol overdose may result in bronchoconstriction and should be counteracted using a short-acting
bronchodilator and other symptomatic and supportive care,

9. GLUCOSAMINE
Source: strong acid hydrolysis of chitin (shells of crustaceae)
Uses : Glucosamine is generally used over the counter in the symptomatic treatment of
osteoarthritis and joint pain, frequently combined with chondroitin sulfate
It is currently not approved as a prescription product by the FDA, but is widely
available over the counter
O
CH2OH
H
H
OH
OH
H
H
NH2
OH
H

10. ▪ Osteoarthritis (OA) is a progressive and degenerative joint disease marked by loss of cartilage, bone
changes, and synovial membrane inflammation.
▪ provides a building block towards the synthesis of glycosaminoglycans (mucopolysaccharides),
slowing the progression of osteoarthritis and relieving symptoms of joint pain.
▪ Glycosaminoglycans or mucopolysaccharides are long, linear polysaccharides consisting of
repeating disaccharide units (uronic sugar and an amino sugar).
hyaluronic acid
(one of the Glycosaminoglycans )

11. ▪Some in vitro studies show evidence that glucosamine
reduces inflammation via inhibition of interferon gamma
and Nuclear factor kappa B.
Toxicity and side effects
The oral LD50 of glucosamine in rats is >5000 mg/kg.Symptoms of an overdose with
glucosamine may include nausea, vomiting, abdominal pain, and diarrhea

12. ASCORBIC ACID
Preparation:
-extraction from citrus fruits
- synthesis from glucose
Uses:
-Cure its deficiency (scurvy), cold, capillary fragility
-Antioxidant in some pharmaceutical preparations
O
HO
OH
HOHC
CH2OH
O

13. 1. In humans, an exogenous source of ascorbic acid is required for collagen formation and tissue repair by acting as
a cofactor in the synthesis of collagens and other proteins.
2. Ascorbic acid is reversibly oxidized to dehydroascorbic acid in the body.These two forms of the vitamin are
believed to be important in oxidation-reduction reactions.
3. The vitamin is involved in
▪ tyrosine metabolism,
▪ conversion of folic acid to folinic acid,
▪ carbohydrate metabolism,
▪ synthesis of lipids and proteins,
▪ iron metabolism,
▪ resistance to infections,
▪ and cellular respiration.

14. LACTULOSE
▪ Galactose-b-(1,4)-fructose
▪ A semi-synthetic disaccharide (not naturally occurring)
▪ Not absorbed in the GI tract
▪ Used either as a laxative in constipation and for hepatic encephalopathy
Mechanism
• Lactulose is not absorbed in the small intestine nor broken down by human enzymes, thus
stays in the digestive bolus through most of its course, causing retention of water through
osmosis leading to softer, easier-to-pass stool.
• Fermented by the gut flora, producing metabolites which have osmotic powers and
peristalsis-stimulating effects (such as acetate), but also methane associated with flatulence.
• Lactulose is metabolized in the colon by bacterial flora into lactic acid and acetic acid.
These partially dissociate, acidifying the colonic contents the formation of the nonabsorbable
NH4 from NH3, trapping NH3 in the colon and effectively reducing plasma NH3 concentrations.
(hepatic encephalopathy)
• There have also been studies demonstrating the capacity for lactulose to minimize the
formation of gallstones.
• Anticancer potentiality owing to its ability to bind galactin carbohydrates involved in
various tumor progressions

15. SUCRALFATE (Aluminum salt of sucrose orasulfate)

16. ▪ Gastro-duodenal protective agent used in the treatment of gastric and duodenal ulcers and to prevent duodenal ulcer
recurrence
• The mechanism of action of this drug in the healing duodenal ulcers is not yet completely defined
• However,This drug aids in the healing of duodenal ulcers, relieving painful inflammation by creating a protective
mechanical barrier between the lining or skin of the gastrointestinal tract and damaging substances.
• Sucralfate forms a complex that binds to protein-rich exudate found on the surface of ulcers. It binds to albumin
and fibrinogen preventing blood clot lysis by stomach hydrochloric acid.
• In addition, sucralfate acts to increase levels of growth factors locally, and
• Also causes an increase in prostaglandins which are important in the healing of the mucosa (lining) of the
gastrointestinal tract
absorbed from the gastrointestinal tract in very minimal quantities

17. ▪ Overdosage has never been observed with sucralfate. It is unlikely, as administering a maximum dose of up to 12
g/kg/body weight in several animal species did not result in death
▪ This drug is considered a pregnancy Category B drug
▪ Whether this drug is excreted in human milk is currently unknown.
•Constipation
•Dry mouth
•Nausea or gastrointestinal discomfort
•Gas/indigestion

18. Hetastarch
■ It is hydroxyethyl starch (semisynthetic material)
■ Used as plasma expander in case of shock
but it increases bleeding time and cause
allergy.
Introduction
Homopolysaccharides
Heteropolysacchrides
Polysaccharides in pharmacy Honey
Drugs derived from starch
(Starch) OH +
O OH
alkali
Starch O CH2 CH2OH
Etylene oxide Hetastarch

19. PAGE
19
Mechanism of Action
Ethoxylated amylopectins; colloidally expands plasma volume
Pharmacokinetics
Onset: 30 min
Duration: 6-36 hr
Half-life, Elimination: 17 days
Metabolism: Enzymatically degraded by reticuloendothelial system or amylases in blood
Excretion: Urine, feces (by biliary excretion)
Administration: IV
Introduction
Homopolysaccharides
Heteropolysacchrides
Polysaccharides in pharmacy Honey

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20
Adverse Effects
Anaphylaxis (periorbital edema,
urticaria, wheezing, mild temperature
elevation)
Chills
Flu-like symptoms
Myalgia
Peripheral edema
Headache
Pruritus
Vomiting
Salivary gland enlargement
Warnings
Do not use in critically ill adult patients including
those with sepsis, and those admitted to the ICU
Avoid use in patients with pre-existing renal dysfunction
Discontinue use at the first sign of renal injury
Need for renal replacement therapy has been reported
up to 90 days after administration; continue to monitor
renal function for at least 90 days in all patients
Avoid use in patients undergoing open heart surgery
in association with cardiopulmonary bypass due to
excess bleeding
Discontinue at the first sign of coagulopathy
Introduction
Homopolysaccharides
Heteropolysacchrides
Polysaccharides in pharmacy Honey

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21
Cyclodextrins
• are a family of cyclic oligosaccharides, consisting of a macrocyclic ring of glucose subunits
joined by α-1,4 glycosidic bonds.
• Cyclodextrins are produced from starch by enzymatic conversion, Commonly
cyclodextrin glycosyltransferase (CGTase) is employed along with amylas.
• They are used in food, pharmaceutical, drug delivery, and chemical industries, as well as
agriculture and environmental engineering.
• Cyclodextrins are composed of 5 or more α-D-glucopyranoside units linked 1-4, as in
amylose (a fragment of starch).
• Typical cyclodextrins contain a number of glucose monomers ranging from six to eight units
in a ring, creating a cone shape:
α (alpha)-cyclodextrin: 6 glucose subunits.
β (beta)-cyclodextrin: 7 glucose subunits
γ (gamma)-cyclodextrin: 8 glucose subunits
• β-cyclodextrin is ideal for complexation due to perfect cavity size, efficient drug
complexation and loading, availability, and relatively low cost
• Some containing 9, 10, 11, 12 and 13 glucopyranose units have also been reported.
• Some derivatives containing the hydroxypropyl (HP), methyl (M) and sulfobutylether (SBE)
substituents have been commercially used as new pharmaceutical excipients.

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22
Introduction
Homopolysaccharides
Heteropolysacchrides
Polysaccharides in pharmacy Honey

23. PAGE
23
Cyclodextrins are cyclic oligosaccharides of a
glucopyranose, containing a relatively hydrophobic
central cavity and hydrophilic outer surface.
Owing to the lack of free rotation around the bonds
connecting the glucopyranose units, the CDs are not
perfectly cylindrical molecules but are toroidal or
cone shaped.
• As a result it act as molecular containers by
entrapping guest molecules in their internal cavity.
No covalent bonds are formed or broken during drug
CD complex formation.
• Once included in the cyclodextrin cavity, the drug
molecules may be dissociated from the
cyclodextrin molecules through complex dilution in
the aqueous tear fluid. Since no covalent bonds
are formed or broken during the guest–host
complex formation, the complexes are in dynamic
equilibrium with free drug and cyclodextrin
molecules.
Polysaccharides in pharmacy Honey

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24
Introduction
Homopolysaccharides
Heteropolysacchrides
Polysaccharides in pharmacy Honey

25. PAGE
25
Introduction
Homopolysaccharides
Heteropolysacchrides
Polysaccharides in pharmacy Honey

26. PAGE
26
They have been applied for delivery of a variety of drugs, including hydrocortisone,
prostaglandin, nitroglycerin, itraconazol, chloramphenicol. The cyclodextrin confers
solubility and stability to these drugs

27. PAGE
27
Introduction
Polysaccharides in pharmacy Honey

29. Chitin and chitosan

35. Applications of CHO
as delivery system in cancer

36. Heparin
Naturally occurring anionic, sulphated glycosaminoglycan

37. Uses
Heparin is an anticoagulant indicated for thromboprophylaxis and to treat thrombosis associated with a variety of conditions
such as pulmonary embolism and atrial fibrillation
It binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes
thrombin (factor IIa) and factor Xa.
Unfractionated heparin is indicated for prophylaxis and treatment of
• venous thrombosis and its extension,
• prevention of post-operative deep venous thrombosis and pulmonary embolism and
• prevention of clotting in arterial and cardiac surgery.
• In cardiology, it is used to prevent embolisms in patients with atrial fibrillation and
• prevent clotting during dialysis and surgical procedures,
• maintain the patency of intravenous injection devices and prevent in vitro coagulation of blood transfusions and in blood
samples drawn for laboratory values.

38. A serious side-effect of heparin is heparin-induced thrombocytopenia (HIT), caused by an immunological
reaction that makes platelets a target of immunological response, resulting in the degradation of platelets, which
causes thrombocytopenia.This condition is usually reversed on discontinuation, and in general can be avoided
with the use of synthetic heparins.
Heparin is contraindicated in those with risk of bleeding (especially in people with uncontrolled blood
pressure, liver disease, and stroke), severe liver disease, or severe hypertension

39. Acarbose

40. Acarbose is an alpha-glucosidase inhibitor used in adjunctly with diet and
exercise for the management of glycemic control in patients with type 2
diabetes mellitus
Acarbose is a complex oligosaccharide that competitively inhibits the alpha-
glucosidase enzymes to break down ingested carbohydrates into absorbable
monosaccharides, reducing carbohydrate absorption and subsequent
postprandial insulin levels
Acarbose requires the co-administration of carbohydrates in order to exert its therapeutic effect, and as such
should be taken with the first bite of a meal three times daily
Side effects
The symptoms of acarbose overdose are likely to be consistent with its adverse effect profile and
may therefore include significant gastrointestinal (GI) symptoms (flatulence, distension, etc)

41. Hydroxypropyl methylcellulose (Hypromellose)
• is a semisynthetic, inert, and viscoelastic polymer that forms a colloid solution when dissolved in water.
• Used as an ophthalmic protectant and lubricant, in artificial tears,
• Promotes corneal wetting by the stabilization and thickening the precorneal tear film and prolonging
the tear film breakdown time, which is usually shortened in dry eye conditions. Hypromellose also acts to
lubricate and protect the eye

42. Hyaluronic acid is a non sulphated glycosaminoglycan
Hyaluronic acid (HA) is an anionic, nonsulfated glycosaminoglycan
found in connective, epithelial, and neural tissues
The average 70 kg (150 lb) person has roughly 15 grams of hyaluronan
in the body, one-third of which is turned over (i.e., degraded and
synthesized) per day.
• The intra-articular preparations of hyaluronic acid are indicated for knee pain associated with osteoarthritis.
• Hyaluronic acid is used in cosmetic applications to prevent and reduce the appearance of wrinkles on the
face, and as a dermal filler to correct facial imperfections or other imperfections on other parts of the body.
• It is frequently an ingredient in topical applications for wound healing and symptomatic treatment of skin
irritation from various causes.
• Hyaluronic acid may also be indicated in ophthalmological preparations or oral capsules to treat discomfort
caused by dry eyes or conjunctivitis and for its protective qualities during and before eye surgery.
• Finally, hyaluronic acid can be used off-label to coat the bladder for relief of interstitial cystitis symptoms.