Relatively, a large percentage of world population is affected by diabetes mellitus, out of which approximately 5-10% with type 1 diabetes while the remaining 90% with type 2. Insulin administration is essential for type 1 patients while it is required at later stage by the patients of type 2. Current insulin delivery systems are available as transdermal injections which may be considered as invasive. Several non-invasive approaches for insulin delivery are being pursued by pharmaceutical companies to reduce the pain, and hypoglycemic incidences associated with injections in order to improve patient compliance. While any new insulin delivery system requires health authorities' approval, to provide long term safety profile and insuring patients' acceptance. The inhalation delivery system Exubera® has already become clinically available in the United States and Europe for patients with diabetes as non-invasive delivery system.

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Self-emulsifying drug delivery systems (SEDDS) are mixtures of oils and surfactants, ideally isotropic, and sometimes containing cosolvents, which emulsify spontaneously to produce fine oil-in-water emulsions when introduced into aqueous phase under gentle agitation.1) Recently, SEDDS have been formulated using medium chain triglyceride oils and nonionic surfactants, the latter being less toxic. Upon peroral administration, these systems form fine emulsions (or microemulsions) in gastro-intestinal tract (GIT) with mild agitation provided by gastric mobility.2,3) Potential advantages of these systems include enhanced oral bioavailability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the hostile environment in gut. [4][5][6] The process of self-emulsification proceeds through formation of liquid crystals (LC) and gel phases, the properties of which significantly affect the formation of droplets and interface available for partitioning of drug.5-9) Many workers claim various rational applications of SEDDS for delivering and targeting lipophilic drugs (e.g., WIN 54954, 1) N-4472, 10) idebenone, 11) coenzyme Q10, 12) vitamin E, 13) halofantrine, 14) and cyclosporin A. 15) However, very few reports are available of SEDDS of water insoluble or poorly soluble hydrophobic compounds. Therefore the concept of using griseofulvin in SEDDS was considered for the present study, where the drug is present in solution form.Griseofulvin is an antifungal agent first isolated from a Penicillium spp. in 1939. It is effective after oral ingestion and reaches the skin and hair. It is deposited primarily in keratin precursor cells. Ingestion with a heavy meal and reduction in particle size enhances the absorption of griseofulvin.16) Griseofulvin systematic (IUPAC) name is (2S,6ЈR)-7-chloro-2Ј,4,6-trimethoxy-6Ј-methyl-3H,4ЈH-spiro[1-benzofuran-2,1Ј-cyclohex[2]ene]-3,4Ј-dione (Fig. 1), and its formula is C 17 H 17 ClO 6 with molecular weight 352.766 g/mol. The compound is insoluble in water (8.64 mg/l). It has a logP/hydrophobicity 2.15 (partition system octanol/water), and its pK a /isoelectric point is not available.17) Griseofulvin inhibits fungal mitosis by disrupting the mitotic spindle through interaction with polymerized microtubules. 18)Griseofulvin is administered orally. Its microcrystalline and ultramicrocrystalline forms are available as tablets. The microcrystalline form also comes in a pediatric suspension form. The typical dose of microcrystalline form is 500-1000 mg/d. Ultramicrocrystalline form is administered at doses of 330-990 mg/d. 19) Since the bioavailability of poorly water-soluble drugs can be influenced by interactions with food or by the physicochemical conditions in the gastrointestinal (GI) tract, 20) oral preparation of griseofulvin is commonly prescribed to be administered according to a fixed dosing schedule. The oral bioavailability of griseofulvin is highly varia...

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Objective: The purpose of this study was to verify the claimed acid-resistant properties and other performance indicators for AR Caps (Capsule 5 from CapsCanada) and DRcaps (Capsule 6 from Capsugel) and compare them with the immediate release hydroxypropyl methylcellulose "HPMC" capsules (K-CAPS from CapsCanada). Methods: Shell weight variability, reaction to different relative humidity conditions, empty shells response to stress under the absence of moisture, powder leaking, disintegration and dissolution properties were assessed. Results: Shell weight variability was highest among Capsule 4. At 45% RH and 23 o C different types of capsules had similar loss on drying (LOD range: 5.23% -6.68%). In the absence of moisture and following the application of a stress, empty Capsule 4 shells performed the best with the highest percentage of intactness of capsules (80%) followed by Capsule 6 (50%) and then Capsule 5 (20%). Both disintegration and dissolution test results for Capsule 4 deemed satisfactory for conventional release purposes, but Capsule 5 and 6 do not comply with the USP requirement for delayed-release dosage form. None of the tested capsules have the ability to protect hygroscopic encapsulated material from humid conditions as generally claimed. Conclusion: While HPMC capsule made for conventional release properties may be fit for that purpose, the new generation of capsules designed to protect the ingredient from the acid environment of stomach have not performed in such a manner as to comply with the USP requirements for disintegration and dissolution of delayed-release dosage form.

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The purpose of this study was to assess the in vitro performances of "vegetable" capsules in comparison to hard gelatin capsules in terms of shell weight variation, reaction to different humidity conditions, resistance to stress in the absence of moisture, powder leakage, disintegration and dissolution. Two types of capsules made of HPMC produced with (Capsule 2) or without (Capsule 3) a gelling agent and hard gelatin capsules (Capsule 1) were assessed. Shell weight variability was relatively low for all tested capsules shells. Although Capsule 1 had the highest moisture content under different humidity conditions, all capsule types were unable to protect the encapsulated hygroscopic polyvinylpyrrolidone (PVP) powder from surrounding humidity. The initial disintegration for all Capsule 1 occurred within 3 min, but for other types of capsules within 6 min (n = 18). Dissolution of acetaminophen was better when the deionized water (DIW) temperature increased from 32 to 42 °C in case of Capsule 1, but the effect of temperature was not significant for the other types of capsules. Acetaminphen dissolution from Capsule 1 was the fastest (i.e. >90% in 10 min) and independent of the media pH or contents unlike Capsule 2 which was influenced by the pH and dissolution medium contents. It is feasible to use hypromellose capsules shells with or without gelling agent for new lines of pharmaceutical products, however, there is a window for capsule shells manufacturing companies to improve the dissolution of their hypromellose capsules to match the conventional gelatin capsule shells and eventually replace them.