Preparation and Evaluation of Olanzapine Tablets

 

C. Kumaresan

M. Pharm, Ph. D, Formulator, Chennai, India.

 

ABSTRACT:

In pharmaceutics developing, improving and producing tablet is worldwide interests. The production cycle helps to remove the potential problems and advantageous to patient compatibility. The patient requirement is widely known by the pharmaceutical production cycle. The stable dry product with approved shelf life period, easy performance characteristics, accurate dosage, acceptable embossment on tablets, the preparation of unique shape such as round, oval etc. Tablet advantages are portable, easy to administer, are a small bulk, and mask of any unpleasant tastes or appearances. A number of excipients are used for tablet manufacturing. A number of excipients and punches types can seriously reduce the life of tablet press components. Mixing, blending and granulation procedures are importance in the characteristics of tablets. The Tablet is a solid dosage form. Immediate release tablets with olanzapine prepared. The prepared olanzapine tablets were evaluated for physical, chemical characteristics were studied.

 

 

 

INTRODUCTION:

Patents are good to pharmaceutical innovation. The pharmaceutical products such as new chemical entities, new products formulation method, and devices used to intake formulations are patented. The olanzapine chemical formula is 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b] [1,5] benzodiazepine. The molecular formula is C₁₇H₂₀N₄S, and molecular weight of 312.44. olanzapine is yellow crystalline solid and practically insoluble in water. The olanzapine in class II drug according to biopharmaceutical classification (1-2). The drug olanzapine is an antipsychotic drug that affects brain chemicals. It used to treat the condition such as schizophrenia and bipolar disorder (manic depression) above the age 12 years. The bioavailability and half-life of olanzapine is 60-65% and elimination half life 33hours, 51.8 hours respectively (3).

 

 

The immediate release tablet desintegrate rapidly and get dissolved to release medicaments. The immediate release olanzapine pressed in hand compression machine as oval shape, the dose is 5/10mg and then film coated in perforated pan coater (4-6).

 

MATERIALS AND METHODS:

The olanzapine, starch, hydroxy propyl methyl cellulose film coating grade, microcrystalline cellulose, talc, magnesium sterate, obtained from orchid pharmaceuticals, Chennai. The dimethyl sulphoxide, pH phosphate buffer, purified water obtained from Mohamed sathak trust, Chennai.

 

Preparation of Olanzapine tablets:

Preparation of granules:

The wet granulation method was used to prepare the olanzapine granules. The olanzapine is mixed with starch and starch paste is added into it. The wet mass were kept on the tray and dried in hot air oven at 60ºC for 3 hours, The dried granules were passed into 40 mesh sieve.

 

Preparation of blend:

The microcrystalline cellulose, talc and magnesium sterate were passed into 60 mesh sieve. The olanzapine granules were mixed with the sieved microcrystalline cellulose and blended for 10 minutes. Then added sieved talc and magnesium sterate to the above mixture and blended for 5 minutes. The olanzapine blend is stored in polythene bag and tied well. The physicochemical properties of blend such as flowability, moisture content, assay and blend drug uniformity were evaluated.

 

Compression of tablet:

The oval shape punch and die were used to compress the olanzapine blend. The single station rotary compression machine used. The blend is used to compress 5mg and 10mg tablet. The tablet weight checked during compression. Once tablet ejected collected in polythene bag. The tablet thickness, hardness, friability, disintegration and dissolution were studied.

 

Film coating of tablet:

The hydroxy propyl methyl cellulose is passed in 60 mesh sieve. Filmcoating solution were prepared with hydroxy propyl methyl cellulose solution dispersed in purified water and stirred with stirrer for 45 minutes for complete hydroxylation. The compressed tablets were coated upto 8% weight buildup of the tablet. The film coated tablets were collected in polythene bags.

 

Evaluation of the blend and tablets:

Flow property of blend:

The Tapdensity/bulk density:

The 5gm powder kept in 100ml measuring cylinder and find the volume, The tapped for 250 times and found the volume. The bulk density (ρ_B) and tapped density (ρ_T) were found by the formula mass/volume.

 

Carr’s index or compressibility index expressed as C= 100(1-ρ_B/ρ_T); compressibility index found good, between 15-16.

 

The hausner ratio expressed as H= ρ_T/ ρ_B, Hausner ratio is number correlated to flowability of a powder. Flowability found good, between 1.14 to 1.16.

 

Content uniformity of the blend:

The blend taken from 12 different places and this powder dissolved in 100ml buffer pH7.4. This solution diluted with buffer solution to find out the absorbance in ultra violet spectroscopy at λmax 227nm. The uniformity of drug content evaluated.

 

Weight/height/thickeness of the tablet:

Weight of the tablet checked in digital weighing balance, height and thickness of the tablet were checked in Vernier caliper.

 

Table 1. Content Uniformity of the blend

S. No	Sampling point	Content uniformity (%)
1	Top 1	98.7
2	Top 2	98.5
3	Top 3	99.1
4	Middle 7	98.7
5	Middle 8	99.2
6	Middle 9	98.7
7	Bottom 10	99.1
8	Bottom 11	98.6
9	Bottom 12	99.3

 

Hardness:

The hardness checked in hardness tester and hardness complies as per requirement of the tablet.

 

Friability:

The 2.5g of the tablet were taken into the friabilator. The friabilator rotated for 25 rotation per minute for 4 minutes and checked the weight. The 2.3g weight, 92%w/w found after friability testing.

 

Disintegration test:

Six tablets were kept in disintegrator at 37ºC and operated the disintegration apparatus, all tablets were disintegrated within1 minutes.

 

Dissolution test:

Six tablets were set aside in dissolution paddle apparatus 2 at 37ºC and ran the dissolution apparatus, all tablets were dissoluted within 3 minutes.

 

Drug content of the tablet:

The 10 tablets were crushed in motor pestle and powder. This powder dissolved in 2.5 ml of dimethyl sulphoxide and volume made upto 100ml with pH7.4. This solution diluted with buffer solution to find out the absorbance in ultra violet spectroscopy at ¥max λmax 227 nm. The drug content evaluated.

 

Table 2. Drug content

S. No	Drug Content (%)
1	98.8
2	98.6
3	98.9
4	98.5
5	99.1
6	98.8
7	98.7
8	99.2
9	99.1
10	99.4

 

CONCLUSIONS:

The prepared tablets are stable, the tablets characters such as thickness, weight, hardness, friability, disintegration, dissolution were evaluated. The drug content complies as per evaluation. Further clinical studies of the prepared tablets will be tested in future. This immediate release film coated tablets were successfully prepared and evaluated.

 

ACKNOWLEDGMENTS:

The author would like to acknowledge the work of, Professor Dr. PK Manna, Department of Pharmacy, Annamalai University, Chidambaram and, Dr. MS Mohan, Orbicular Pharmaceuticals, Hyderabad on the subject of tableting, I express my sincere thanks to Dr. Kamalakar Reddy, Heterodrugs, Hyderabad, Dr. Sanjay Jain, SCOPE, Indore on the subject of tablet coating.

 

REFERENCES:

1.     https://www.drugbank.ca/drugs/DB00334 downloaded on 15/03/20, 8.56 AM

2.     https://pubchem.ncbi.nlm.nih.gov/compound/Olanzapine, downloaded on 15/03/20, 9.30 AM

3.     https://psychopharmacologyinstitute.com/publication/olanzapine-pharmacokinetics-2159, downloaded on 15/03/20, 9.50 AM

4.     https://www.webmd.com/drugs/2/drug-1644-9274/olanzapine-oral/olanzapine-oral/details, downloaded on 15/03/20, 10.00 AM

5.     http://jpet.aspetjournals.org/content/262/2/545, downloaded on 15/03/20, 10.00 AM

6.     Olanzapine Orally Disintegrating Tablet: A Review of Efficacy and Compliance, Luis San, Marta Casillas, Antonio Ciudad, and Inmaculada Gilaberte, CNS Neurosci Ther. 2008 Fall; 14(3): 203–214.

7.     Designing of olanzapine sustained release matrix tablets for the treatment of schizophrenia, Chinmaya Keshari Sahoo, Gude Bhargavi, Kokkula Satyanarayana, Nalini Kanta Sahoo, Alok kumar Moharana, International Journal of Biopharmaceutics. 2015; 6(1): 37-42.

 

 

Accepted on 11.06.2020      ©Asian Pharma Press All Right Reserved