RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, BANGALORE
KARNATAKA
ANNEXURE – II
PROFORMA FOR REGISTERATION OF SUBJECTS FOR M. PHARM
DISSERTATION
1 / Name of the Candidate & Permanent Address(In block letters) / Mr. MD ZUBAIR AHMED
S/O AB WAHEED
H.No: 5-1-138/1, AHMED BAGH GOLE KHANA, BIDAR – 585401
2 / Name of institution / R R K Samithi’s College of Pharmacy,
Naubad, BIDAR- 585402.
3 / Course of Study and Subject / M. Pharmacy (PHARMACEUTICS)
4 / Date of Admission to Course / 29/07/2011
5 / Title of the Topic:
" FORMULATION AND EVALUATION OF TRANSDERMAL DRUG
DELIVERY SYSTEM OF TELMISARTAN "
6 / BRIEF RESUME OF THE INTENDED WORK;
6.1 Need for the Study:
Transdermal drug delivery is a successful controlled technology in terms of number of approved products. The feasibility of transdermal route for systemic drug delivery has lead to successful development and marketing of transdermal delivery systems of several drugs1,2. Presently several classes of drugs are under investigation to determine their potential for TDDS development, such systems helped to overcome the side effects associated with conventional system of medication,which require multi-dose therapy3,4.There are many advantages to administering drugs by routes that bypass the gastrointestinal tract. One such route is the transdermal in which the drug agent is applied to the skin in a patch or device of some type so that sufficient quantity penetrates the skin to exert a systemic effect. There are several theoretical advantages to this approach not the least of which is the drug avoids being metabolized by the liver after absorption and the gastrointestinal irritation is avoided5. Thus the patient compliance long term therapy and bypassing first-pass metabolism can be reduced simultaneously increasing the bioavailability.
To improve the bioavailability and reduce the local and systemic side effects the need to formulate the transdermal delivery arises. The main components of transdermal patches are backing layer, drug reservoir, and pressure sensitive adhesives.
Telmisartan is Angiotensin II antagonist & is formed from angiotensin I in a reaction catalyzed by ACE enzyme (kininase II). The elimination half-life is approximately 24 hours. The bioavailability was 15% after tablet ingestion. Peak serum concentration (Cmax) 0.5 to 1 hour6.
6.2 Review of Literature:
A thorough literature survey on the topic has been done and very prominent are:
Barry BW,7 Recently, the transdermal route has vied with oral treatments as the most successful innovative research area in drug delivery. The worldwide transdermal patch market approaches 2 billion pound, yet is based on only ten drugs---scopolamine, nitroglycerine, colonidine, nicotine with a lidocane soon to be marketed7. Barhate SD, Patel MM, Sharma AS,8 Carvedilol transdermal patches were prepared by using combination of EudragitRS100 and polyvinyl pyrrolidine (PVP K30) along with glycerin, polyethylene glycol as plasticizers. It was observed that the system with PVA:PVP in the ratio 8.6 along with used plasticizers was promising controlled release transdermal drug delivery system for carvedilol. Formulated transdermal patches of carvedilol, exhibits zero-order release kinetics.
Samip SS, Prabhu P,9 Transdermal patches of papaverine hydrochloride were prepared by the solvent casting method using ethyl cellulose: PVP, PVA: PVP and Eudragit RL-100: Eudragit RS-100 using different ratios. The physicochemical parameters such as flexibility, thickness, smoothness, weight variation, moisture content, hardness and tensile strength were evaluated for the prepared patches. The formulation exhibited flexibility, uniform thickness and weight, smoothness, good drug content (92 to 96%), and little moisture content. Thein vitrodiffusion studies were carried out using modified Keshery-Chein cell using cellophane as the diffusion membrane and the formulation followed the Higuchi diffusion mechanism.
Nakohiro Nishida, Kazuhiro Taniyama, Toshihiro Sawabe.10 Valsartan (VAL) is a highly selective angiotensin II type 1 receptor blocker that has been widely used for the treatment of hypertension. When administrated orally in humans, VAL is rapidly absorbed. Its maximum concentration occour at 2-4 hrs VAL is not metabolized by cytochrome P450 and is mostly excreted without metabolic conversion The bioavailability (BA) of VAL is 10–35% This low BA of VAL is mainly due to poor absorption in the gastrointestinal tract, which is mainly attributed to the ionized tetrazole and/or carboxyl group of VAL, in the tract. Additionally, food intake is known to reduce the Cmax and AUC of VAL by 50% and 40%, respectively which may reduce its pharmacological effect. Therefore, if we can improve the BA of VAL and minimize the effect of food intake, we should be able to confer further therapeutic benefits to hypertensive patients. The transdermal administration of VAL is a possible solution to overcome these problems.
6.3 Objectives of the Study:
· To formulate Telmisartan transdermal drug delivery system by solvent casting method using poly vinyl pyrrolidone (PVP K30), EudragitRS100, Eudragit RL100 etc., as polymer. Glycerin, polyethylene glycol 400 and propylene glycol as a plasticizers.
· To perform the characterization studies like weight variation, thickness, drug content uniformity, folding endurance etc., of the prepared formulations.
· To perform compatibility studies using IR spectroscopy.
· To evaluate in vitro drug release and kinetic studies of the prepared
formulations.
· To carryout stability studies as per ICH guidelines.
MATERIALS AND METHODS:
7.1. Source of data:
· The profile of telmisartan is collected from the literatures.
· It is a laboratory-based method so in vitro release data will be collected from the in vitro Franz-diffusion studies.
· The information about formulation and evaluation parameters will be collected by referring to Indian journal of pharmaceutical sciences, Indian drugs, AAPS pharmascitech Journal of research in medical sciences, Scientia Pharmaceutica, The Indian Pharmacist, Iranian journal of pharmaceutical research etc.
· Referring to pharmaceutics journals from the entire national and international journals will do present investigation.
· Resent information in the area will be updated by literature survey through e-publishing, Internet and current periodicals.
· Compatibility studies between drug and polymers will be done by IR spectroscopy available in our college laboratory.
· All the basic facilities like dial calipers, diffusion cell etc. Fabrication of equipment to perform diffusion studies will be done in our college.
7.2 METHOD OF COLLECTION :
Phase I:
· IR spectroscopy is used to perform compatibility studies of drug with polymer and different plasticizers.
Phase II:
Formulations prepared will be subjected to parameters like weight variation by electronic balance, water absorption characteristics, thickness of transdermal patch by dial calipers, assay of formulations will be performed using phosphate buffer pH 7.4 by UV spectrophotometer at 296nm for drug content uniformity11.
Phase III:
The in vitro diffusion studies will be carried out by using Franz-diffusion cell at (32±50C, 80 ml phosphate buffer pH7.4, at 80 rpm). The freshly excised skin was sandwiched between donor and acceptor compartment, with formulated patch on epidermal side. Samples were withdrawn through the sampling port at different time intervals for a period of 24 hours and analyzed spectro- photometrically at 296 nm11.Statistical analysis of data obtained from the results.
Phase IV:
Stability studies are performed for formulation as per ICH guidelines.
7.2 Does the study require any investigation or intervention to be conducted on patient or other human or animals? If so please describe briefly)
------Not under the plan of work------
7.4 Has ethical clearance been obtained from your institution in case of 7.3?
------Not applicable------
8. / LIST OF REFERENCES;
1) Anampally S, Aukunuru J; Development of granisetron transdermal films: IN VITRO AND EX VIVO Characterization. Indian drugs May 2010. Page no. 21-28
2) Chien yie w. Novel drug delivery systems. Marcell dekker. Inc.newyork, 301-380.
3) Babu RJ, Pandit JK. Effect of penetration enhancers on the release and skin permeation of bupranolol from reservoir-type transdermal delivery systems. International Journal of Pharmaceutics. 2005; 288: 325-334.
4) Pandey S, Praveen SH,and Udupa N. Formulation and evaluation of Nimeuslide Transdermal Drug delivery systems Indian J. Pharm.Sci.2000:62(5): 376-379.
5) Wang j, Ruan j, zhang c, ye y, cai y, Wu Y. Development and evaluation of sinomenine transdermal patch. Pakistan Journal of Pharma Science 2008; 21(4): 407- 410.
6) Martindale, The Complete Drug Reference, 34th Edition.2005. Page No. 1010.
7) Barry BW, Novel mechanisms and devices to enable successful transdermal drug delivery. 2001; European journal of pharmaceutical sciences(14):101-114..
8) Barhate SD, Patel MM, Sharma AS. Formulation and Evaluation of transdermal drug delivery system of carvedilol. Journal of Pharmacy Research 2009; 2(4): 663-665.
9) Samip SS, Prabhu P. Formulation and evaluation of transdermal patches of papaverine hydrochloride. international journal of pharmaceutical sciences 2010; 4(1):79-86.
10) Nakohiro Nishida, Kazuhiro Taniyama, Toshihiro Sawabe. Development and evaluation of a monolithic drug-in-adhesive patch for valsartan. international journal of pharmaceutics 2010; (402):103-109.
11) Ilango k, Shiji kumar P.S; Simultaneous estimation of telmisartan and hydrocholorothiazide in pharmaceutical dosage form. Asian journal of pharmaceutical and health sciences. 2011- Feb.
.
9. / Signature of the candidate / MD ZUBAIR AHMED
10. / Remarks of the Guide / This work is help full for studies on anti hypertensive drugs in TDD System.
11. / Name and Designation of
(in block letters)
11.1 Guide
11.1 Signature / Dr. K Sreenivasa Rao
Principal & HOD
R R K’ S College of Pharmacy, Naubad Bidar.
12. / Name and Designation
(In block letters)
12.1 Co – Guide
12.2 Signature / ------
------
13. / 13.1 Remarks of th Principal.
13.2 Signature / Dr. K Sreenivasa Rao