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Percutaneous Absorption of Analgesics in the Presence of Permeation Enhancers

Thesis Info

Access Option

External Link

Author

Shah, Syed Nisar Hussain

Program

PhD

Institute

Bahauddin Zakariya University

City

Multan

Province

KPK

Country

Pakistan

Thesis Completing Year

2009

Thesis Completion Status

Completed

Subject

Applied Sciences

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/1408

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676726850203

Similar


The transdermal route has been recognized as a highly potential route of systemic drug delivery and provides the advantage of avoidance of the first-pass effect, ease of use and withdrawal (in case of side-effects), and better patient-compliance. However, the major limitation of this route is the difficulty of permeation of drug through the skin which can be improved by the use of penetration enhancers. Studies have been carried out to find safe and suitable permeation enhancers to promote the percutaneous absorption of drugs. The aim of present study was to evaluate the effect of various enhancers on percutaneous absorption of Diclofenac Diethylamine (DDA) across silicone membrane and full thickness rabbit skin. The enhancers used in this study were propylene glycol (PG), polyethylene glycol (PEG 400), Glycerol (Gly), Oleic acid (OA) and Turpentine oil (TO). DDA was chosen as a lipophilic drug having a molecular weight of 316.7 and partition coefficient (Ko/w) of 4.40. Prior to start the diffusional experiments, the solubility studies were conducted for the saturated solutions and their concentrations at 1, 2, 3 & 4% (v/v) each of these enhancers. The enhancing effect of enhancers was found to be significantly greater than that of standard without enhancer (control). Diffusional experiments were conducted using modified Franz-diffusion cell across silicone membrane and full thickness rabbit skin, with constant stirring of receptor phase containing phosphate buffered saline (PBS) as receptor solution (pH 7.4±0.1) at 37°C±2. 1 ml of sample was applied in the donor compartment for diffusional studies across silicone membrane while 20 ml of sample was applied in the donor compartment in case of rabbit skin experiments. ‘Benchmark’ parameters with which to compare the performance of the other vehicles are the flux values and these values from propylene glycol (PG), polyethylene glycol (PEG) and glycerol (Gly) have statistically insignificant difference (P>0.05) in their saturated solutions across silicone membrane whereas all Flux values for saturated enhancer’s solutions are statistically insignificant except values for Glycerol which are significantly high across rabbit skin only. To explain the difference in values of flux between saturated and control may be the differential uptake of enhancer’s by the SC of the skin, while flux values for all concentrations of enhancer’s across rabbit skin were statistically significant (P<0.05) and on the basis of these values it can be recommended that the 4% concentrations of the enhancers used can be best formulated DDA in a topical product. The input-rate of all the enhancers has shown a trend of increase with the increase in the enhancer’s solution concentrations. The DDA binary formulations showed the significantly high permeation rate and the content of enhancers’ concentration in formulations influenced the skin permeation rate substantially for DDA. As the content of enhancers’ concentration was decreased from 4% to 1% of DDA binary formulations, the skin permeation rate of DDA also decreased which may be due to thermodynamic activity of drug in the formulation as DDA is poorly water soluble (~42.28mg/ml at 37°C±2) and yet solublised in the enhancers’ mixture. Data from permeation experiments revealed that the DDA permeated across membrane/or skin at a faster rate in the presence of PG and PEG than the other vehicles studied. This finding was in line with evidence from Franz-type diffusion experiments in which flux was consistently higher from formulations. On the basis of flux values that solutions made by PG and PEG as enhancers may be recommended to formulate topical preparations. The vehicles used were predominantly influencing the partition of the drug into the rabbit skin rather than the diffusion throughout the study. Consequently, changes in diffusion and/or partition may occur as a result of absorption or depletion of permeation enhancers inside the membrane/or skin over time which validates our results.
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ڈاکٹر سید عبدالحفیظ سلفی

ڈاکٹر سیدعبد الحفیظ سلفی
افسوس ہے کہ ۸؍ جون کی شب میں ڈاکٹر سید عبدالحفیظ سلفی کا انتقال ہوگیا، مجھے ذاتی طور پر اس کا بڑا صدمہ ہے، میں بچپن ہی سے ڈاکٹر صاحب کے نام نامی سے واقف تھا، میرے والد مرحوم اہلِ حدیث کے بعض اکابر کے ساتھ ان کا تذکرہ بھی کرتے تھے اس لیے اسی زمانے سے ان کی عقیدت دل میں جاگزیں ہوگئی تھی۔
زیارت اور ملاقات کا شرف تو دو ہی ایک بار حاصل ہوا تاہم ان کی محبت، شفقت، حسنِ خلق، خلوص، درد مندی، نیکی، شرافت اور دینداری کا اثر ابھی تک قلب پر باقی ہے، ایک بار کسی کانفرنس میں ان کا عالمانہ خطبہ سننے کا اتفاق ہوا جو قرآن و حدیث کے حوالوں سے بھرا ہوا تھا۔ ایک بار ان کے ایک صاحب زادے ڈاکٹر عبدالعزیز سلفی اپنے استاد اور ہمارے سابق رفیق مولانا عبدالرحمان پرواز اصلاحی مرحوم سے ملنے دارلمصنفین تشریف لائے تو مجھ سے بہت گھل مل گئے، ان سے اور مولانا پرواز مرحوم سے جو کچھ عرصہ دارالعلوم احمدیہ سلفیہ لہریا سرائے اور بھنگہ سے بھی وابستہ رہے، ڈاکٹر سید عبدالحفیظ صاحب کے بارے میں جو کچھ سنا اس سے ان کے مرد مومن ہونے کا راز آشکار اور ان کیـ ’’دنوں کی تپش‘‘ اور ’’شبوں کے گداز‘‘ کا اندازہ ہوا، وہ واقعی ایک موحد، عالم باعمل، داعی اور متبع سنت تھے۔ گزشتہ سال اسی زمانے میں ڈاکٹر عبدالعزیز سلفی سے ندوۃ العلما لکھنؤ میں ملاقات ہوئی تو لپٹ گئے، ڈاکٹر صاحب کی خیریت دریافت کرنے پر بتایا کہ بہت کمزور ہوگئے ہیں۔
ڈاکٹر سید عبدالحفیظ مرحوم عامل بالحدیث تھے، ایک زمانے میں آل انڈیا جمعیتہ اہل حدیث کے امیر بھی تھے، عقیدہ و مسلک میں پختگی کے باوجود ان میں عصبیت نہ تھی، وہ مسلمانوں کے اجتماعی مسائل میں دوسرے فرقہ کے لوگوں کے...

زواج المسيار: حقيقته و حكمه

The term “Nikah Misyar” (translated sometimes as “travellers’ marriage” or “marriage of convenience”) is not found in the Qur’an, Sunna or classical works of Islamic jurisprudence. It is a term that has been introduced recently. However, the concept can be found being discussed in the works of classical Muslim jurists (fuqaha). This is a marriage contract between a man and a woman, with the condition that the spouses give up one, two or several of their rights by their own free will. Some people consider that the misyar marriage can meet the needs of young people whose resources are too limited to settle down. However, there have been some (Sunni) scholars and organizations that have opposed the concept of Nikah Misyar altogether. As for the Islamic ruling concerning such marriages, there are two issues to consider: 1) Validity and permissibility; and 2) Appropriateness. Different scholars gave different opnions regarding these two imporatant issues. In this article, Nikah/zawaj Misyar was discussed in detail, describing different point of views and ruling in facvour and against Nikah Misyar.

Amelioration of Iron Deficiency in Groundnut Arachis Hypogaea L.

Groundnut is an important cash crop of Pothwar region (Attock and Chakwal districts) of Pakistan. This crop faces iron deficiency in the region due to calcareousness of soils. Iron is ranked fourth abundant element comprising 5% of the crust of earth. However due to high pH (7.5-8.5) of soils; iron availability to the plants is limited, as a 44result groundnut yield is significantly decreased. Development of tolerant genotypes under iron limitation is the widely acceptable strategy practiced all over the world. This study was planned to identify locally grown groundnut genotypes tolerant to iron deficiency, and to investigate chemical amendments for mitigation of iron deficiency. To achieve the objectives hydroponics and pot experiments were performed in triplicate in Completely Randomized Design (CRD) under iron sufficient and iron deficient conditions at National Agricultural Research Centre (NARC), Islamabad. Seeds were obtained from BARI (Barani Agricultural Research Institute, Chakwal) and NARC, Islamabad. Amongst all tested genotypes, BARI-2000 performed well in soils as well as in hydroponics under iron limited conditions, whereas BARD-699 was found susceptible to iron deficient conditions with iron deficiency tolerance indexes of 56% and 36% respectively. The data were further supported by iron reducing capacity of both genotypes. Iron reducing capacity of BARI-2000 was the highest 4 days after iron deficiency stress (15.3 μmol per g 2 h fresh weight of plants) as compared to other genotypes, while BARD-699 showed significantly low iron reducing capacity (5.8 μmol per g 2 h fresh weight of plants). For amelioration of iron deficiency in BARI-2000 and BARD-699, various chemicals (Fe-EDTA, FeSO4, citric acid, sequestrene, and surfactant) were used. Several morpho-physiological parameters were recorded under various amendments. BARD-699 was more responsive to foliar applications, while BARI-2000 was found more responsive to Fe-EDTA. Foliar applications were found more effective in reducing iron chlorosis as compared to soil applications of chemical amendments. Molecular markers data showed genotypic similarities amongst genotypes. BARI-2000 was related to 96CG005 and both the genotypes were tolerant to iron deficiency. Four varieties viz., Banki, BARI-2000, BARD-699 and Chakori were used to study the expression levels of eight genes (AhIRT1, AhFRO1, AhNRAMP1, AhYSL1, AhYSL3, AhYSL4, AhYSL6 and AhFER3) involved in uptake and translocation of iron under iron limited conditions through real time PCR analysis. BARI-2000 and Chakori were closely related based on gene expression and pot experiment data. Expression level of AhIRT1 was low in BARI-2000 and Chakori in roots under iron deficient conditions, whereas the same was higher in shoots. The tolerant genotypes can be used in hybridization programs for improving yield and iron deficiency tolerance in groundnut.