Shaik zia .. b-cyclodextrin

A Seminar on cyclodextrins:

A Seminar on cyclodextrins

Slide 2:

Presented to, Dr.Sunil Raj Raga M.Pharm (PhD) Dept of Industrial Pharmacy Karnataka college of Pharmacy,Bidar Seminar Presented By: Shaik Zia-Ur-Rahman M.Pharm, Ist yr Industrial Pharmacy

DISCOVERY::

DISCOVERY: Cyclodextrins have been discovered 100 years ago & called as ” CELLULOSINE ” Firstly by the Scientist A.Villers in the Year 1891. Secondly by F.Schardinger Identified 3 different Also reffered as “ Schardinger sugars ”

INTRODUCTION::

INTRODUCTION: Cyclodextrin are a group of cyclo-oligosaccharides which forms inclusive complexes (with poorly water soluble compound) in drug development, cyclodextrin technology can be used. The poorly dissolution of the relatively insoluble drugs has for long been problem in a formulation of oral dosage forms. This limits the aspects such as ABSORPTION and BIOAVAILABILITY. There fore several approaches have been followed in improving solubility of drugs one being complexation using cyclodextrin

TYPES OF CYCLODEXTRINS:

TYPES OF CYCLODEXTRINS Alpha cyclodextrin – contains 6 glucosepyranose units. Beta cyclodextrin – contains 7 glucosepyranose units. Gama cyclodextrin – contains 8 glucosepyranose units.

TYPES OF CYCLODEXTRINS:

TYPES OF CYCLODEXTRINS

STRUCTURE OF B-CYCLODEXTRIN:

STRUCTURE OF B-CYCLODEXTRIN

REASON……?:

REASON……?

Production of Cyclodextrins::

Production of Cyclodextrins: The production of CYCLODEXTRINS is relatively simple & involves treatment of ordinary starch with a set of easily available Enzymes commonly “ cyclodextrin Glycosyl transferase” is employed along with alpha-Amylase.

CHARACTERISTICS OF BETA-CYCLODEXTRIN:

CHARACTERISTICS OF BETA-CYCLODEXTRIN No. of glucose units = 7 Molecular weight =1135 Solubility in water at R.T=1.85g/100ml Optical rotation=162 + 0.5 Cavity diameter=6.0-6.5 Ǻ Height of torus=7.9 + 0.1 Ǻ Diameter of outer peripheral=15.4 + 0.4 Approx. vol. of cavity=262 Ǻ

CHEMISTRY OF CYCLODEXTRIN:

CHEMISTRY OF CYCLODEXTRIN These are enzymatic conversion products of starch, partially pre hydrolised starch & mixture of acyclic dextrin's. Cyclodextrin molecule have cylindrical shape with a central axial cavity as a consequences of formation of glucose pyranose units.

Slide 15:

Cyclodextrins are not perfectly clylindrical molecules but are toroidal or coned shaped. All hydroxyl groups are located on one side of molecule All primary hydroxy groups are located on another side. The lining of internal cavity is formed by oxygen bridge atoms which makes the cavity slightly apolar

PHARMACEUTICAL USEFUL DERIVATIVES OF BETA-CYCLODEXTRIN: HYDROPHILIC DERIVATIVES:

PHARMACEUTICAL USEFUL DERIVATIVES OF BETA-CYCLODEXTRIN: HYDROPHILIC DERIVATIVES Methylated b-cyclodextrin- Dimethyl & trimethyl b-cyclodextrin Hydroxylated b-cyclodextrin- Hydroxyethyl, 2-hydroxypropyl, 3-hydroxypropyl, 2,3,dihydroxypropyl b-cyclodextrin

HYDROPHIBIC DERIVATIVES:

HYDROPHIBIC DERIVATIVES Ethylated beta-cyclodextrin Diethyl beta-cyclodextrin Tri ethyl beta-cyclodextrin IONISABLE DERIVATIVES carboxymethyl b-cyclodextrin

ADVANTAGES OF B-CYCLODEXTRIN:

ADVANTAGES OF B-CYCLODEXTRIN HYDROPHILIC B-CYCLODEXTRIN- Markedly improved solubility, rate of dissolution of poorly soluble drugs including fat-soluble vitamin, steroid hormones & cardiac glucosides HYDROXILATED B-CYCLODEXTRIN- They show higher aqueous solubility, faster dissolution rate, bioadaptability.

Slide 20:

HYDROPHOBIC CYCLODEXTRIN- Control the rate of release of water soluble drug IONISABLE CYCLODEXTRIN DERIVATIVES- Have unique biological activities such as antibacterial & heparin mimic activity.

METHODS OF PREPARATION OF B-CYCLODEXTRIN:

METHODS OF PREPARATION OF B-CYCLODEXTRIN PHYSICAL MIXTURE METHOD Here the physical mixture of the drug & cyclodextrin in equivalent ratio (1:2) was obtained by making pulverized powder with mesh no. 100 together spatula.

Slide 22:

KNEADING METHOD : Here the cyclodextrin was dissolved in a small volume of water-methanol solution with ratio 6:4,solution to this accurately weighed qty. of drug is added in small amount, the thick slurry was kneaded for 45min & then dried at 45 degree celcius temp. the dried mass was pulverised and sieved through mesh no. 100

Slide 23:

CO-EVAPORATION METHOD : The aqueous solution of cyclodextrin was added to an alcoholic solution of drug, the resulting mixture was stirred for 1 hour and evaporated at temp. 45degree until dried. It was then pulvarised & sieved by mesh no. 100.

Slide 24:

SOLID DISPERTION METHOD : The drug and molar quantity of cyclodextrin was dissolved in methanol then the solution was evaporated in vacuum at 40 degree Celsius with a rotary evaporator the collected powder was stored under vacuum in desiccator for three days and analyzed .

Slide 25:

SPRAY DRYING METHOD : The drug & molar Quantity of cyclodextrin was dissolved in methanol then the solution was evaporated in vacuum at 40 o C with a rotary evaporator. The collected powder was stored under vacuum in desiccators for 3 days & analyzed.

Slide 26:

NEUTRALIZATION METHOD : The drug & cyclodextrin in different molar ratio were separately dissolved in 0.1N HCL & 0.1N NAOH was added to precipitate the complex at PH 7.5 the ppt. was washed with distilled water, pulverized and passed through sieve no. 80 & stored in desiccator over fused calcium carbonate.

CD effect on important drug properties in Formulation::

CD effect on important drug properties in Formulation: Effect on Drug solubility & Dissolution. Effect on drug Bioavailability. Effect on Drug safety. Effect on Drug Stability.

CD Application in Drug Delivery:

CD Application in Drug Delivery Oral drug delivery Parentral Drug Delivery Ocular Delivery Nasal Drug Delivery Rectal Drug Delivery Controlled Drug Delivery Colon-Specific Drug Delivery

Slide 30:

To increase dissolution rate of drug To improve bioavailability of the drug To increase chemical & physical stability. To decrease irritation To increase the solubility To improve organoleptic properties of a drug.

REFERENCES:

REFERENCES INTERNET SEARCH GOOGLE SEARCH KEY WORDS USED : CYCLODEXTRIN, BETA-CYCLODEXTRIN, ROLE OF B-CYCLODEXTRIN IN DRUG SOLUBILITY. SCIENTICA PHARMACEUTICA. NOVEL DRUG DELIVERY SYSTEM BY N.K JAIN.

THANK YOU:

THANK YOU The Hunk Icon…