INDUSTRIAL PRODUCTION,ESTIMATION AND UTILIZATION OF THE�PHYOTCONSTITUENT ATROPINE

INDUSTRIAL PRODUCTION,ESTIMATION AND UTILIZATION OF THE�PHYOTCONSTITUENT ATROPINE

USEFUL FOR B.PHARM 5TH SEM

1. INDUSTRIAL PRODUCTION,ESTIMATION AND UTILIZATION OF THE PHYOTCONSTITUENT ATROPINE

2. SOURCE Atropine is a synthetically-derived form of the endogenous Tropane alkaloid isolated from the plant Atropa belladonna Atropa belladonna, Datura stramonium and Duboisia myoporoides .

3. ATROPINE : Molecular Formula: C 17 H 23 NO 3 Synonyms Of ATROPINE dl-Hyoscyamine Tropine tropate Atropin Atropen Molecular Weight: 289.4 g/mol

4. Introduction MECHANISM OF ACTION Atropine competitively blocks acetylcholine , a neurotransmitter, from acting on the muscarini c receptors in the body. As a result, atropine dilates the pupils , increases heart rate, and reduces salivation and other secretions .

5. INDUSTRIAL PRODUCTION OF ATROPINE New, E fficient and C ommercially feasible process for the preparation of atropine and atropine salts has been developed The process provides a high yield . In addition, the process has the advantage of proceeding efficiently , for many of the steps, at ambient temperature .

6. TWO STEPS INVOLVED The process includes 2 steps (a) Producing acetyltropoyl chloride; and (b) Reacting the acetyltropoyl chloride with tropine other necessary reagent or reagents to form atropine.

7. STEP 1: Production of Acetyltropoyl Chloride Acetyltropoyl chloride Dimethylformamide (DMF)CATALYST Tropic acid (3-hydroxy-2-phenylpropanoic acid) Acetyl chloride C hlorinating agent (oxalyl chloride) + +

8. Step 2: Reacting the acetyltropoyl chloride with tropine to form Atropine It involves 2 steps Step a: The tropine is first reacted with methanesulfonic acid to form tropine methanesulfonate Step B: The acetyltropoyl chloride solution is contacted with the tropine methanesulfonate to form Atropine Tropine Methane sulfonic acid Tropine methanesulfonate + Tropine methanesulfonate Acetyltropoyl chloride Atropine +

9. Estimation of Atropine An isocratic RP-HPLC method was developed Conditions: Column: C18 column Mobile phase : Methanol:5 mmol potassium dihydrogen phosphate buffer (50: 50, v/v) The flow rate :1 mL min-1 Detection:UV detector at 264 nm. The retention time{Rt} for atropine sulphate was found to be 4.797 minutes . The LOD and LOQ for atropine sulphate were found to be 23.07 and 69.91 ng mL-1

10. TLC Atropine was identified by TLC Two different solvent systems were given the best results: a. n-Butanol/acetic acid /distilled water (4:1:5 ) b. water/ acetic acid (8:2 ) The Rf values for standard atropine in solution a and b were found to be ( 0.74 and 0.82 ), respectively while the Rf value for atropine that extracted with both solution a and b were found to be (0.72, 0.81) Detection: UV radiation which gave bright blue color

11. Identification of atropine using TLC with two solvent system Atropine (Standard) Rf Colour in UV Radiation Solvent system (a) 0.74 Bright blue Solvent system (b) 0.82 Bright blue Atropine (Extracted) Rf Colour in UV Radiation Solvent system (a) 0.72 Bright blue Solvent system (b) 0.81 Bright blue

12. UV-Visible measurements Ultra-violet spectrum was measured in ethanol as a solvent. Figure shows the maximum absorption for atropine which is equal to 283.1nm

13. Utilization of ATROPINE Atropine is used for many medicinal purposes. More common uses include administration before anesthesia to decrease mucus secretions , such as saliva. During anesthesia and surgery, atropine is used to maintain a normal heart rate Atropine sulfate, a salt of atropine, is also used to block or reverse the adverse effects caused by some medicines and certain types of pesticides. Atropine is also used in ophthalmology . In this regard, atropine is administered prior to eye examinations to dilate the pupil, and to relieve pain caused by swelling and inflammation of the eye

14. Contraindications It is generally contraindicated in people with Glaucoma, P yloric stenosis, or P rostatic hypertrophy , P reanesthetia

15. MARKETED PREPARATIONS