Formulasi Dan Evaluasi Transdermal Patch Kalium Diklofenak

<p align="center"><strong>Abstrak</strong></p><p><em> </em></p><p>Kalium diklofenak adalah salah satu obat golongan anti-inflamasi non steroid (AINS) yang memberikan efek samping iritasi pada saluran pencernaan. Tujuan penelitian ini adalah melakukan formulasi dan evaluasi sediaan dengan rute alternatif lain penggunaan kalium diklofenak melalui transdermal <em>patch. Patch </em>dibuat dengan metode penguapan pelarut. Polivinil pirolidon (PVP) digunakan sebagai polimer untuk pembentukan <em>patch </em>transdermal kalium diklofenak dengan dibutil ftalat (DBP) sebagai <em>plasticizer </em>dan mentol sebagai peningkat penetrasi. Uji <em>in vitro</em> dilakukan dengan alat difusi modifikasi <em>Franz </em>dan ditentukan dengan spektroskopi UV-sinar tampak. Kadar zat aktif, berat, ketebalan dan organoleptis dari <em>patch </em>juga ditentukan. Hasil penelitian menunjukan bahwa rata-rata uji laju difusi sediaan <em>patch </em>1,3884 mg/cm² dengan persen permeasi sebesar 8,9 % selama 180 menit.</p><p> </p><p><strong>Kata Kunci :</strong><strong> </strong>Transdermal; <em>Patch</em>; kalium diklofenak; mentol.<strong></strong></p><p><em> </em></p><p align="center"><strong><em>Formulation and Evaluation Patch Transdermal Diclofenac Potassium</em></strong></p><p align="center"><em> </em></p><p align="center"><strong><em>Abstract</em></strong></p><p><em> </em></p><p><em>Diclofenac potassium is one of the non-steroidal anti-inflammatory drugs (NSAIDs) that provides irritating side effects to the digestive tract. The purpose of this study is to formulate and evaluate preparations with alternative routes of using potassium diclofenac through the transdermal patch. </em><em>Preparation of </em><em>the matrix patches used the solvent casting method. Polyvinyl pyrrolidone (PVP) was used as a matrix for the formation of transdermal diclofenac potassium patches, dibutyl phthalate (DBP) as the plasticizer and menthol as the permeation enhancer. The in vitro assay was carried out in a modified Franz diffusion cell and the rates of diffusion were determined by UV spectroscopy. The average drug content, thickness, organoleptic, weight uniformity of the matrix patches was also determined. The results showed that the average dosage rate of diffusion test Patch </em><em>is </em><em>1,3884 mg/cm² with permeation percentage 8,9 % for 180 minutes. </em></p><p><em> </em></p><p><strong><em>Keywords</em></strong><em>: </em><em>Transdermal; Patch; diclofenac potassium; menthol</em></p>

Histological analysis of failed submucosa patches in congenital cardiac surgery

Objective Porcine small intestinal submucosa extracellular matrix is a biological substitute used in cardiovascular surgery to correct congenital heart defects. Previous studies with this material have shown satisfactory results. In contrast, there are singular reports of patch-associated complications with CorMatrix small intestinal submucosa extracellular matrix. We report the histopathological findings of explanted extracellular matrix patches that were removed because of early failure in patients with congenital heart defects. Methods Explanted patch materials from 4 patients (aged 9 months to 41 years), who underwent reoperation due to early patch failure, were analyzed. Initial surgery comprised one aortic valve reconstruction, one pulmonary valve reconstruction, one atrioventricular septal defect repair, and one aortic arch enlargement. The interval between operations ranged from 69 to 553 days. Results Residual extracellular matrix patch material was evident at explantation in all cases and presented as a structured eosinophilic and anucleate specimen. In two cases, a local focus of scarring and pseudocartilaginous transformation with evidence of calcification was found. There was no evidence of absorption of patch material in any case, nor repopulation by organized tissue formation. Conclusions Histologic examination of explanted extracellular matrix patches showed no evidence of resorption or relevant repopulation with resident cells nor formation of functional tissue structures. In contrast, a mixed chronic inflammatory infiltration, early signs of calcification, and scarring as well as focal pseudocartilaginous transformation were found. Considering recent reports, close follow-up of patients with extracellular matrix patches is recommended to evaluate the performance of this novel material and detect potential problems.

Estradiol matrix patches for pubertal induction: stability of cut pieces at different temperatures

Objective Transdermal estradiol patches are primarily designed for adult women. No low-dose patches are licensed for pubertal induction in hypogonadal girls. Low doses can be achieved by cutting a matrix patch into smaller pieces. However, the manufacturers do not guarantee stability or utility of cut estradiol patches. The aim of the study was to assess 1-month stability of cut estradiol patches from four different manufacturers in the laboratory at room temperature (+21°C) and at an elevated temperature (+35°C). Design and methods Estraderm MX 50 µg, Systen 50 µg and Oesclim 25 µg matrix patches were cut into eight pieces while Estradot 50 µg small patches were cut in half. The cut patches were stored in their respective pouches at +21°C or at +35°C for up to 1 month. The estradiol drug was extracted from the patch by ethyl acetate n-hexane and determined by radioimmunoassay. Results Storage at +21°C or +35°C up to 1 month did not reduce the estradiol concentration in Estraderm MX, Systen and Oesclim patches. However, although the estradiol in Estradot patches was not affected by storage at +21°C, at +35°C, estradiol decreased by 57% (±1%) in cut pieces. Conclusions Unused Estraderm MX, Systen and Oesclim patch pieces may be stored for at least 1 month at ≤+35°C. Where estradiol patches for children are not available, cut pieces of these or similar patches can be used for pubertal induction. The Estradot patch was too small to properly cut into low doses and not stable in elevated temperatures.

Formulation, Characterization, and In Vitro Evaluation of Transdermal Patches for Inhibiting Crystallization of Mefenamic Acid

The crystallization of mefenamic acid in transdermal patch is a major problem that makes the patch unstable and decreases the drug release. The additive was used to inhibit crystallization of a mefenamic acid. Among the different types of additives, polyvinylpyrrolidone (PVP) K30 and PVP K90 were studied and found to be highly effective in inhibiting the crystallization of the drug. The PVP presented as a solubilizer agent for mefenamic acid in matrix patches at the different ratio between drug : PVP, 1 : 2 and 1 : 2.5 for using PVP K30 and 1 : 1.5 and 1 : 2 for using PVP K90. The characterizations showed the homogeneous patches without the crystal form of the mefenamic acid in matrix patches. The release profiles of the mefenamic acid from the patches were investigated by Franz diffusion cells. Over the first 1 h, the release behavior of mefenamic acid from the patches obviously increased when PVP was used as a crystallization inhibitor. However, the ratio between drug : PVP K90 at 1 : 2 was found to be the most effective in increasing the drug release from patch. Thus, the PVP could be used as a crystallization inhibitor for mefenamic acid in matrix patches which will increase the drug release.

FORMULATION AND IN-VITRO EVALUATION OF TRANSDERMAL MATRIX PATCHES OF DOXOPHYLLINE.

ABSTRACT Objective: The objective of the present study was to fabricate matrix type transdermal patch with varied proportion of hydrophilic (HPMC E-50) and (PVP) combination incorporating the drug Doxophylline and to execute the physicochemical and in vitro assessment. The motive was to provide the delivery of Doxophylline at a controlled rate across the intact skin to attain a therapeutically effective drug level for a longer time span from transdermal matrix patch.Method: Prefomulation studies and evaluation was done by using different parameter such as Partition coefficient, Physicochemical Compatibility of Drug and Polymer, Physical appearance, Thickness Measurement, Folding Endurance, Weight variation, Percentage moisture lost, Percentage moisture uptake, Drug content Determination.Result: The results shows that patches of Doxophylline obtained by the solvent evaporation method had acceptable physicochemical characteristics and satisfactory percentage drug release. Conclusion: The main conclusion of my work was formulating the Doxophylline transdermal system was to prolong the drug release time, reduce the frequency of administration and to improve patient compliance. Six formulations were prepared using two polymers in different ratios along with plasticizers and penetration enhancer.