Glimepiride is often combined with metformin HCl as an oral antidiabetic in type II diabetes mellitus, which provides a complementary and synergistic effect with multiple targets for insulin secretion. Glimepiride includes class II of BCS, which solubility practically insoluble in water but high permeability, which will impact the drug's small bioavailability. In contrast, metformin HCl includes class III of BCS, which has a high solubility in water, but low permeability is absorbed approximately 50-60% in the digestive tract given orally. The co-crystallization method can be used to improve the glimepiride solubility properties and the permeability properties of metformin HCl by interrupting glimepiride with metformin HCl physically. This study aims to identify the physical interactions between glimepiride and metformin HCL using a thermal analysis of Differential Scanning Calorimetry (DSC) and then confirmed by a computational approach. Identifying the physical interactions between glimepiride and metformin HCL was carried out by plotting the melting points generated from the endothermic peaks of the DSC thermogram at various compositions versus the mole ratios of the two were further confirmed by the computational approach using PatchDock. The results of the phase diagram analysis of the binary system between glimepiride and metformin HCl show a congruent pattern, which indicates the formation of co-crystal or molecular compounds at a 1 : 1 mole ratio at 228°C. Computational approach results showed that the interaction between glimepiride and metformin HCl did not form new compounds but heterosinton formation that was stable in molecular dynamics simulations.

Glimepiride (GMP) is an oral antidiabetic drug classified as BCS class II, demonstrating extremely limited solubility, with a solubility level below 0.00384 mg/mL. Some generic drug manufacturers producing GMP (copy product) tablets encountered bioavailability issues due to poor dissolution, which did not meet the requirements. Therefore, measures were taken to enhance solubility through the modification of polymorphs. It is known that GMP exists in two polymorphic forms, namely Form I and an alternative Form II, which exhibits higher solubility in water. This study aims to produce and characterize the polymorph-modified GMP compared to non-modified GMP, develop an optimal formulation for polymorph-modified GMP tablets that adhere to pharmaceutical requirements as a representative copy drug model, and determine its similarity factor to Amaryl® as the innovator. The research methodology involved initiating the study by examining the polymorph transformation of GMP through the utilization of techniques such as neat grinding, solvent drop grinding, and solvent evaporation. The resulting samples were characterized using DSC, PXRD, and SEM analysis. The performance assessment encompassed the evaluation of flow properties, compressibility index, solubility, and dissolution rate compared to the non-modified GMP. Based on the characterization results, the best polymorph-modified GMP sample was used to produce a tablet formulation containing 4 mg of GMP using the direct compression method as a copy tablet model. In vitro equivalence testing was performed using a comparative dissolution test on the polymorph-modified GMP tablet compared to its innovator, Amaryl® 4 mg, in three different dissolution media, followed by determining the equivalence status using the similarity factor (f2) calculation. Based on the screening results of polymorph transformation, it was determined that the polymorph-modified GMP, using all three techniques, did not undergo a transition from Form I to Form II. Instead, it underwent amorphization, primarily observed in the solvent evaporation technique. Tablets containing polymorph-modified GMP using the solvent evaporation technique were able to enhance the in vitro dissolution rate profile compared to non-modified GMP tablets. The f2 values for the comparative in vitro dissolution test in acetate buffer pH 4.5 and phosphate buffer pH 6.8 were 60.15 ± 0.27 and 88 ± 0.35, respectively within acceptance criteria of 50–100. However, in KCl/HCl buffer pH 1.2, the f2 value was 45.15 ± 0.23. It was concluded that the polymorph-modified GMP tablet was not similar to its innovator, Amaryl®.

Pharmaceutical excipients such as P-glycoprotein inhibitors can also increase the solubility and affinity of drugs to the intestinal membrane, enhance paracellular pathways and endocyte uptake, and activate lymph transport pathways, thereby increasing the bioavailability of oral drugs. This review aims to review and assess the performance of pharmaceutical excipients as P-glycoprotein permeability inhibitors in improving oral drug bioavailability in drug formulations by evaluating meta data from P-glycoprotein efflux in permeability and pharmacokinetics studies. The review results are pharmaceutical excipients that have proven effective as P-glycoprotein inhibitors from the surfactant and polymer groups, namely TPGS and Poloxamer 188, respectively. All nanosystems incorporating pharmaceutical excipients as P-gp inhibitors show potential in enhancing the permeability and bioavailability of oral drugs when compared to conventional formulations. The effectiveness of these systems has been evaluated through in vitro (Caco-2 cells), ex vivo (everted gut sac), in situ (SPIP), and in vivo (AUC) methods.

Metformin is the first line in type 2 Diabetes Mellitus (DM). Metformin is available as an innovator drug and copy drug. The high price of innovator drugs makes it difficult for patients to obtain the required drugs. Therefore, many pharmaceutical industries have developed a copy of the innovator drug. To obtain .a distribution license, the pharmaceutical industry must conduct a bioequivalence test on metformin copy tablets to ensure that the copy drug has the same efficacy, safety, and quality as the innovator drug. However, several surveys show that most patients believe that the effectiveness of copy drugs is not equivalent to the innovator drug. This study aims to determine the bioavailability profile and bioequivalence profile of Metformin copy tablets to Glucophage^® (Merck) innovator tablets so that it can provide an overview of the effectiveness of copy drugs with innovator drugs and the public no longer hesitate to use copy drugs. Metformin copy tablets are declared bioequivalent to the innovator drug if they provide a Confidence Interval (CI) value of 90% in the 80-125% range. All 500 mg, 850 mg, and 1000 mg doses of metformin copy tablets, both fasting and eating conditions, gave bioequivalent results to the innovator Glucophage^® based on 90% CI.

Self emulsifying drug delivery systems (SEDDS) dikembangkan sebagai metode untuk meningkatkan kelarutan obat lipofilik seperti ibuprofen, serta untuk meningkatkan absorpsi dan laju disolusi obat. Oleh karena itu penelitian ini bertujuan untuk mengembangkan formulasi SEDDS ibuprofen yang memenuhi syarat secara farmasetik dan meningkatkan bioavailabilitas ibuprofen. Formula SEDDS diperoleh dari uji kelarutan ibuprofen dan optimasi formula pada berbagai konsentrasi minyak, surfaktan dan kosurfaktan. Asam oleat, cremophor RH 40 dan propilenglikol masing-masing terpilih sebagai minyak, surfaktan dan kosurfaktan dengan perbandingan fase minyak : (surfaktan + kosurfaktan) 1:9 dan pebandingan surfaktan : kosurfaktan (3:2). Formula SEDDS optimum dievaluasi meliputi pengukuran persen transmitan, pengujian dispersibilitas, pengujian robustness, pengujian stabilitas (sentrifugasi, heating cooling cycle, freeze thaw cycle), penentuan ukuran partikel dan uji laju disolusi. Formula SEDDS ibuprofen terbaik memenuhi persyaratan persen transmitan (99,7% ± 0,872), waktu dispersibilitas (41,48 detik ± 1,3), stabil pada pengujian robustness, tidak terjadi pemisahan fasa pada pengujian stabilitas, serta memiliki ukuran globul dalam kisaran mikrometer yaitu 114,7 ± 0,692 nm. Hasil uji laju disolusi in vitro pada menit ke-10 menunjukkan bahwa sediaan SEDDS ibuprofen lebih tinggi dibandingkan dengan serbuk ibuprofen murni, yaitu masing-masing sebesar 90,04 ± 1,764% dan 59,30 ± 1,638%.

Body wash merupakan salah satu sediaan kosmetik pembersih yang umum digunakan untuk membersihkan tubuh yang mengandung surfaktan sebagai salah satu bahan utamanya. Surfaktan sebagai bahan utama yang digunakan dalam sediaan body wash memiliki manfaat sebagai pembasah, pembersih, dan bahan pembusa. Mekanisme surfaktan dalam membersihkan kotoran di kulit yaitu berikatan dengan stratum korneum. Penggunaan surfaktan dalam jangka panjang dapat menyebabkan pembengkakan keratin dalam korneosit, kerusakan struktural pada stratum korneum, meningkatkan Transepidermal Water Loss (TEWL) dan denaturasi protein, sehingga diperlukan sediaan pembersih yang mengandung surfaktan yang aman dan tidak mengiritasi kulit. Penulisan kajian pustaka ini bertujuan untuk mengetahui kemampuan surfaktan dalam mempertahankan stabilitas busa guna membersihkan kotoran di permukaan kulit dan juga mengetahui tingkat iritasi surfaktan berdasarkan nilai zein pada formulasi sediaan body wash. Kajian pustaka ini dilakukan menggunakan metode penelitian secara komparatif dengan mengumpulkan data dari berbagai sumber pustaka yang sesuai dengan kriteria inklusi dan kriteria eksklusi. Hasil dari kajian pustaka menunjukkan bahwa surfaktan mengalami peningkatan stabilitas busa ketika dikombinasikan dengan polimer ataupun saponin dari ekstrak tanaman. Pengujian potensi iritasi surfaktan dengan kombinasi dari berbagai jenis surfaktan anionik, amfoterik, dan non ionik dengan penambahan beberapa zat seperti polimer, ekstrak tanaman, ekstrak dari fermentasi Bacillus, talkum ataupun penambahan alkil poliglukosida menghasilkan potensi iritasi yang lebih rendah jika dibandingkan dengan surfaktan tunggal.